http://jcps.bjmu.edu.cn

Most Read articles

    Published in last 1 year |  In last 2 years |  In last 3 years |  All

    All
    Please wait a minute...
    For Selected: Toggle Thumbnails
    Mechanism of Citri Reticulatae Pericarpium in treating Alzheimer’s disease based on network pharmacology and molecular docking
    Yunli Chen, Renliang Yan, Lisha Li, Yamin Zhang, Xiaomei Xu, Xuehua Lu, Rongqing Xu, Wenjin Lin
    Journal of Chinese Pharmaceutical Sciences    2024, 33 (2): 142-155.   DOI: 10.5246/jcps.2024.02.012
    Abstract228)   HTML25)    PDF(pc) (14711KB)(63)       Save

    The objective of this study was to elucidate the mechanism by which Citri Reticulatae Pericarpium (CRP) treated Alzheimer’s disease (AD) using network pharmacology and molecular docking. Initially, a screening process identified 98 target compounds and 628 related component targets within CRP. Additionally, 2483 AD targets were retrieved from disease databases. Subsequently, an overlapping targets map was constructed, integrating CRP and AD targets, followed by the creation of a protein-protein interaction network map to identify 66 targets closely associated with the treatment of AD using CRP. These targets were identified through topological attribute analysis. To gain further insights, GO function and KEGG pathway enrichment analyses were conducted on the 66 identified targets. The results revealed enrichment in various biological pathways, including the relaxin signaling pathway, calcium signaling pathway, HIF-1 signaling pathway, and IL-17 signaling pathway. Finally, molecular docking verification was performed on the targets and active components of CRP. Active components, such as flavanone, tangeretin, flavonol, carvacrol, and perillaldehyde, were found to form hydrogen bonds with targets, with binding energies below 0 kg/mol. This study utilized network pharmacology and molecular docking methods to systematically elucidate the mechanism by which CRP treats AD. The findings provided a theoretical foundation for future research and clinical investigations.

    Table and Figures | Reference | Related Articles | Metrics | Comments0
    Advances in the treatment of hyperuricemia with traditional Chinese medicine
    Gong Fang, Wenxi Li
    Journal of Chinese Pharmaceutical Sciences    2024, 33 (5): 381-395.   DOI: 10.5246/jcps.2024.05.029
    Abstract187)   HTML15)    PDF(pc) (1533KB)(95)       Save

    Hyperuricemia (HUA), a prevalent metabolic disorder, is closely associated with the development of various diseases. Within Chinese medicine literature, HUA is not explicitly labeled; instead, it falls under categories like “Lijie”, “arthralgia syndrome”, and “gout”. Conversely, modern medical practitioners classify it as “turbid bi” and “Gaozhuo”, among others. Western medicine approaches to treating HUA often involve singular methods with potential toxic and side effects. In contrast, traditional Chinese medicine (TCM), guided by holistic principles and dialectical treatment theories, offers the advantage of multifaceted effects and a broad spectrum of therapeutic targets. This paper aims to review recent research in the application of TCM for the treatment of HUA, providing a foundational basis for clinical diagnosis, treatment, and further investigations in this field.

    Reference | Related Articles | Metrics | Comments0
    A comprehensive comparative analysis of transfection reagents for siRNA delivery
    Shuwen Tong, Xianrong Qi
    Journal of Chinese Pharmaceutical Sciences    2024, 33 (1): 26-34.   DOI: 10.5246/jcps.2024.01.003
    Abstract151)   HTML16)    PDF(pc) (2238KB)(46)       Save

    siRNAs have emerged as essential tools in biological research and hold promise as next-generation therapeutics for gene therapy. However, achieving successful and safe siRNA transfection remains a challenge, especially for cells that are notoriously difficult to transfect. The efficiency of siRNA transfection is influenced by factors such as uptake, cellular availability, and cytotoxicity. Generally, higher transfection efficiency is associated with increased uptake, improved cellular availability, and reduced cytotoxicity. This study aimed to compare the performance of different transfection reagents in delivering siRNAs, focusing on their uptake, knockdown efficacy, and toxicity. All reagents measured in here were good uptaken in HepG2 and HEK293T cells, but low uptake in RAW264.7 cells. Among them, the newly developed CALNP RNAi transfection reagent exhibited distinct uptake profiles when compared to other transfection reagents across various tested cell lines. CALNP RNAi consistently demonstrated superior transfection efficiency and minimal cell toxicity in all the tested cell lines. Furthermore, CALNP RNAi held promise for enabling RNA interference in "hard-to-transfect" cells. This research contributed to our understanding of effective siRNA delivery methods and highlighted the potential of CALNP RNAi transfection reagent as a valuable tool for gene silencing, especially in challenging cellular contexts.

    Table and Figures | Reference | Related Articles | Metrics | Comments0
    Exploring irinotecan adverse reactions in the real world: a study on UGT1A1 heterozygous mutations
    Jing Zuo, Jun Meng, Chao Li, Zhengzheng Xia, Haochun Tang, Anna Li, Xiaofu Ma
    Journal of Chinese Pharmaceutical Sciences    2024, 33 (1): 35-45.   DOI: 10.5246/jcps.2024.01.004
    Abstract136)   HTML13)    PDF(pc) (1599KB)(26)       Save

    This study investigated the prevalence of UGT1A1 genotypes in patients at a specialized tertiary tumor hospital and examined the association between UGT1A1 gene polymorphisms and adverse reactions following irinotecan administration in real-world patients. We conducted a retrospective analysis of data from 42 patients who underwent UGT1A1 genetic testing between May 2017 and December 2021 at the hospital. We specifically focused on 31 of these patients, summarizing the occurrence of both hematological and non-hematological adverse reactions after irinotecan treatment. The findings revealed a heterozygous mutation rate of 21.9% for the UGT1A128 gene, a homozygous mutation rate of 4.9%, and a heterozygous mutation rate of 31.5% for the UGT1A16 gene. Notably, no homozygous mutations were detected. Analysis of patients with UGT1A1*6 and *28 heterozygous mutations showed no significant differences in hematological and non-hematological adverse reactions compared to wild-type patients. Hematological adverse reactions encompassed neutropenia, leukopenia, thrombocytopenia, and anemia, while non-hematological reactions included increased ALT/AST, ALP/GGT, bilirubin, as well as fatigue, nausea, vomiting, and delayed diarrhea. Remarkably, the incidence of delayed diarrhea in patients with UGT1A1*6 and *28 mutations was 100%, suggesting a higher risk in those with double mutations, warranting increased attention. In conclusion, while no significant differences in adverse reactions were observed between UGT1A1 heterozygous mutation patients and wild-type patients following irinotecan application, it is important to note that further confirmation of these findings is necessary through an expanded sample size.

    Table and Figures | Reference | Related Articles | Metrics | Comments0
    Generic development and market exclusivity period in China: an analysis from 2003 to 2020
    Congya Zhou, Tao Huang, Jiahui Gu, Huangqianyu Li, Luwen Shi, Xiaodong Guan
    Journal of Chinese Pharmaceutical Sciences    2024, 33 (1): 57-62.   DOI: 10.5246/jcps.2024.01.006
    Abstract120)   HTML14)    PDF(pc) (1577KB)(20)       Save

    China recently proposed a 6-year regulatory exclusivity period to incentivize research and development in new drugs, orphan drugs, and pediatric drugs. Our study assessed the generic entry status and the duration of market exclusivity for 356 new small-molecule drugs approved in China from 2003 to 2020. Of these, 155 drugs (43.5%) experienced generic entry, with a median market exclusivity period of 5.6 years (interquartile range: 2.4–9.4). Imported drugs, oral common-release agents, and drugs for the nervous system were more prone to generic entry (P < 0.001, P = 0.039, and P < 0.001, respectively). Domestic new drugs had a longer median market exclusivity (8.4 years) compared to imported drugs (5.7 years). Market exclusivity varied from 3.6 years for antineoplastic and immunomodulating agents to 6.8 years for drugs for the alimentary tract and metabolism. If the proposed 6-year regulatory exclusivity is implemented, the market exclusivity duration for new drugs is anticipated to double. It is essential for the government to carefully weigh the impact of such policies on balancing innovation incentives and ensuring drug affordability.

    Table and Figures | Reference | Related Articles | Metrics | Comments0
    Economic burden and healthcare resource utilization of childhood atopic dermatitis in China
    Zhifeng Nie, Ruowei Xiao, Jiafang Song, Sheng Han, Wei Li, He Zhu, Luwen Shi
    Journal of Chinese Pharmaceutical Sciences    2024, 33 (5): 458-469.   DOI: 10.5246/jcps.2024.05.035
    Abstract105)   HTML7)    PDF(pc) (1444KB)(44)       Save

    The primary objective of this study was to estimate the costs and healthcare resource utilization (HCRU) associated with atopic dermatitis (AD) in Chinese pediatric patients and to investigate the factors contributing to the costs of AD. This cross-sectional study employed a convenience sampling approach, with patient-level data obtained from a nationwide survey conducted across 31 provinces in China between February and March of 2022, utilizing an internet-based questionnaire. Caregivers of children under 18 years old with a physician-confirmed diagnosis of atopic dermatitis were recruited, and sociodemographic information, clinical characteristics, HCRU data, time spent on caregiving, and disease-related costs were collected from all eligible participants. A total of 599 eligible families were included in the study. Among them, 82.5% of families reported that their child had at least one outpatient or emergency room visit, while 5.8% of families reported that their child had been hospitalized in the past 12 months. The average annual cost across all cost categories amounted to 28 591.92 yuan per patient per year (PPPY), with 92.8% attributed to direct costs. Out-of-pocket expenses accounted for 90.7% of the cost of outpatient or emergency room visits and 43.4% of the cost of hospitalization. Factors associated with higher annual total costs included moderate (coefficient ± SE: 0.22 ± 0.09, P = 0.012) and severe AD patient groups (coefficient ± SE: 0.58 ± 0.15, P < 0.001), onset of AD on the head, neck, or hands (coefficient ± SE: 0.57 ± 0.14, P < 0.001), use of biological agents (coefficient ± SE: 0.64 ± 0.11, P < 0.001), and use of traditional Chinese medicine (TCM) (coefficient ± SE: 0.26 ± 0.09, P = 0.003), compared with their respective reference groups. This study highlighted a considerable economic burden of AD among pediatric patients in China across different disease severity groups, with significantly higher costs observed in patients with more severe disease. Additionally, factors such as disease severity, clinical characteristics, and treatment modalities might contribute to the higher costs encountered by pediatric patients with AD.

    Table and Figures | Reference | Related Articles | Metrics | Comments0
    Advances of nano-targeted drug delivery systems in traditional Chinese medicine anticancer therapy
    Junchen Ge, Debing Xiang
    Journal of Chinese Pharmaceutical Sciences    2024, 33 (4): 285-304.   DOI: 10.5246/jcps.2024.04.022
    Abstract103)   HTML11)    PDF(pc) (1722KB)(104)       Save

    Cancer has now become the second leading cause of mortality, following cardiovascular and cerebrovascular diseases. Traditional Chinese medicine (TCM) has emerged as a prominent alternative for combating cancer due to its potent therapeutic effects, minimal side effects, numerous targets, and its crucial role in various stages of cancer treatment. However, challenges such as poor solubility, limited permeability, rapid elimination, instability, low bioavailability, and short half-life hinder its clinical application. To overcome these limitations in the anticancer potential of TCM, recent years have seen the integration of nanotechnology in clinical TCM treatments. Nano-targeted drug delivery systems have assumed an increasingly vital role in cancer therapy by synergizing with the active components of TCM for anticancer treatments. Some TCM-based nano-drug carriers have entered clinical trials or been employed in disease diagnosis and treatment, thereby advancing the field of TCM. In light of this, this article provides an overview of the progress made in applying nano-targeted delivery systems to TCM-based anticancer therapy.

    Reference | Related Articles | Metrics | Comments0
    Advancements in glucagon-like peptide-1 receptor agonist therapy for type 2 diabetes
    Yaping Peng, Ying Fu
    Journal of Chinese Pharmaceutical Sciences    2024, 33 (8): 667-685.   DOI: 10.5246/jcps.2024.08.050
    Abstract100)   HTML13)    PDF(pc) (1516KB)(78)       Save

    Glucagon-like peptide-1 receptor agonists (GLP-1RAs) are novel hypoglycemic agents that have garnered widespread acceptance in the treatment of type 2 diabetes, largely attributed to their safety profile, potent hypoglycemic effects, and metabolic advantages. Their primary mechanisms of action encompass promoting insulin release, inhibiting glucagon secretion, bolstering pancreatic islet cell function, curbing appetite, and slowing gastric emptying. This article delves into the clinical evidence underscoring the efficacy of various GLP-1RAs. Notably, these agents have demonstrated marked improvements in glycemic control, significant weight reduction, and substantial cardiovascular and renal protection. Nonetheless, certain adverse effects of GLP-1RAs, such as pancreatitis and intestinal obstruction, have been reported, warranting vigilant monitoring by healthcare professionals. In sum, GLP-1RAs hold significant promise in the management of type 2 diabetes, offering notable cardiovascular and renal advantages.

    Table and Figures | Reference | Related Articles | Metrics | Comments0
    Exploring the impact of anti-diabetic medications on sarcopenia: a comprehensive review
    Litang Tan, Ying Fu
    Journal of Chinese Pharmaceutical Sciences    2024, 33 (6): 481-494.   DOI: 10.5246/jcps.2024.06.036
    Abstract97)   HTML24)    PDF(pc) (1497KB)(39)       Save

    Sarcopenia is a condition characterized by a reduction in muscle mass and/or diminished muscle function, significantly amplifying the risk of falls, fractures, and even mortality among the elderly. Although diabetes can be further complicated by sarcopenia, the precise cause and mechanism remain unclear. Moreover, the impact of anti-diabetic medications, commonly used by individuals with type 2 diabetes, extends beyond glycemic control. These drugs can influence skeletal muscle through diverse mechanisms, affecting the delicate balance between protein synthesis and breakdown, thereby contributing to the development of sarcopenia. This article delves into the potential mechanisms of anti-diabetic drugs on sarcopenia, offering insights from relevant clinical studies and data.

    Table and Figures | Reference | Related Articles | Metrics | Comments0
    Comparative study on ginsenosides of ginsengs from different regions
    Yizheng Sun, Ying Qu, Xiaoyan Liu, Wei Xu, Youbo Zhang
    Journal of Chinese Pharmaceutical Sciences    2023, 32 (12): 961-970.   DOI: 10.5246/jcps.2023.12.077
    Abstract92)   HTML106)    PDF(pc) (6061KB)(46)       Save

    Ginsenosides, unique bioactive components found in ginseng (Panax ginseng Meyer), can be influenced by the geographical area in which the ginseng is grown. In northeastern China, ginseng thrives in diverse living environments that play a significant role in shaping the composition of ginsenosides. This study aimed to explore the variations in ginseng constituents cultivated in different growing regions. UPLC coupled with triple quadrupole tandem time-of-flight mass spectrometry was employed to analyze and characterize the ginsenosides, while multivariate statistical analysis was utilized to identify differences among ginseng samples from various regions. A total of 359 ginsenosides, including 35 potential new compounds, were characterized in the different ginseng samples. Among them, 283 and 312 ginsenosides were identified in ginseng from non-traditional and traditional cultivation regions, respectively. These findings contributed to the expansion of the ginseng compound library and provided valuable insights for future research on ginseng.

    Table and Figures | Reference | Related Articles | Metrics | Comments0
    Design, synthesis, and biological evaluation of covalent inhibitors targeting influenza virus hemagglutinin
    Nian Wang, Chenning Li, Chenxi Cheng, Jianzhong Chen, Pengfei Wang, Xun Lv, Xuebing Li
    Journal of Chinese Pharmaceutical Sciences    2024, 33 (1): 1-14.   DOI: 10.5246/jcps.2024.01.001
    Abstract88)   HTML45)    PDF(pc) (2234KB)(34)       Save

    The ongoing evolution of influenza strains and the limited effectiveness of existing anti-influenza drugs underscore the imperative for novel therapeutics. In addressing this, we developed and synthesized several sialic acid (SA) analogs, designed as potential covalent inhibitors by targeting lysine residues (Lys133 and Lys222) proximal to the substrate binding site of hemagglutinin (HA). The affinities of these compounds for HA were meticulously assessed using surface plasmon resonance (SPR). Intriguingly, all target compounds exhibited superior affinities for HA compared to the parent compound SA. Notably, compound 1d demonstrated a binding potency similar to that of the positive control (2,6-SLN), with KD values of 38.2 μM and 39.6 μM, respectively. Importantly, all compounds demonstrated non-cytotoxicity to MDCK cells, and compound 1d displayed robust inhibitory effects on the influenza virus in vitro. The development of covalent inhibitors targeting HA, as outlined in this study, presented a rational and promising strategy for the creation of potent HA inhibitors.

    Table and Figures | Reference | Related Articles | Metrics | Comments0
    Unraveling the pharmacological mechanisms of Shenqi Fuzheng injection in chronic obstructive pulmonary disease: a network pharmacology and molecular docking approach
    Fanglin Liu, Chunjuan Zhang, Qiuyue Shen, Xicheng Zhou, Yue Zhao, Fengfeng Fu, Fang Liu
    Journal of Chinese Pharmaceutical Sciences    2024, 33 (4): 339-351.   DOI: 10.5246/jcps.2024.04.026
    Abstract88)   HTML6)    PDF(pc) (7123KB)(44)       Save

    The Shenqi Fuzheng injection (SFI) represents a traditional Chinese medicine (TCM) formulation integrating Astragalus membranaceus (Huangqi, HQ) and Codonopsis pilosula (Danshen, DS). This investigation delved into elucidating the potential mechanisms and molecular targets of SFI in the context of chronic obstructive pulmonary disease (COPD) through comprehensive network pharmacology and molecular docking analyses. Initially, we probed the databases for potential bioactive compounds of SFI and identified relevant COPD-related target genes. Subsequent analyses, conducted using Cytoscape 3.9.1 and STRING, facilitated the construction of a protein-protein interaction (PPI) network to discern key target genes. Following this, Gene Ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) enrichment analyses were employed to delineate putative SFI-related signaling pathways, and the results were validated through molecular docking analyses. The network pharmacology analyses revealed a total of 65 active components (35 associated with DS and 30 with HQ) and 233 key targets. Notably, the top five bioactive components (quercetin, apigenin, daidzein, kaempferol, and luteolin) and the top five targets (TP53, AKT1, EP300, MAPK1, and JUN) exhibited substantial affinity and stable binding, with a binding energy ≤ –5.0 kcal/mol in molecular docking analyses. These findings suggested that SFI potentially exerted therapeutic effects on COPD through the concerted action of multiple compounds and pathways. Additionally, the outcomes of this study laid a solid foundation for understanding the pharmacological aspects of SFI, offering valuable insights for its prospective clinical application as an adjuvant therapeutic agent for COPD.

    Table and Figures | Reference | Related Articles | Metrics | Comments0
    Chinese herbal enema therapy for the treatment of chronic kidney disease
    Yonghao Sang, Jie Yun, Lijuan Dai, Liqun Song
    Journal of Chinese Pharmaceutical Sciences    2024, 33 (4): 305-315.   DOI: 10.5246/jcps.2024.04.023
    Abstract86)   HTML10)    PDF(pc) (1609KB)(66)       Save

    Chronic kidney disease (CKD) has emerged as a pressing public health issue characterized by increasing incidence and mortality rates. The imperative for effective treatments to halt its progression cannot be overstated. Central to the concept of the "gut-kidney axis" is the belief that as CKD advances, uremic toxins (UTs) gradually build up, undermining the integrity of the intestinal barrier and resulting in an imbalanced gut microbiota. This dysbiosis in the gut microbiota, coupled with the compromised intestinal barriers, intensifies renal damage by furthering UT accumulation and inducing systemic inflammation. Grounded in this understanding, the use of Chinese herbal enemas has shown promising outcomes in CKD management. This review consolidates both domestic and international studies related to the "gut-kidney axis" and delves into the combination of Chinese herbal enemas with standard therapy, colon dialysis, and traditional oral Chinese medicine practices. Our aim is to shed light on novel perspectives and pinpoint emerging avenues for the evolving therapeutic landscape of CKD.

    Reference | Related Articles | Metrics | Comments0
    A network pharmacology for exploring the pharmacological mechanism of the herbal formula Xiaoyao pills on insomnia
    Dan Wang
    Journal of Chinese Pharmaceutical Sciences    2024, 33 (2): 169-177.   DOI: 10.5246/jcps.2024.02.014
    Abstract84)   HTML6)    PDF(pc) (7419KB)(22)       Save

    The study aimed to investigate the potential mechanism of the Xiaoyao pills (XYP) for treating insomnia using network pharmacology. The researchers employed several analytical methods and databases to predict and screen the active components and targets of XYP, as well as potential targets related to insomnia. Comparative analysis was then conducted to identify overlapping genes between the active component targets and insomnia-related targets. The researchers constructed networks of the active component-target and target pathways using Cytoscape software and the STRING database. Additionally, Gene Ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) enrichment analyses were performed using the DAVID database. The findings revealed 161 active components present in XYP and identified 76 potential targets associated with these active components. Furthermore, 36 overlapping genes were identified as both active component targets and targets related to insomnia treatment. The network pharmacology analysis highlighted the potential significance of radix bupleuri, Chinese angelica, and liquorice in the treatment of insomnia. The proposed mechanism of XYP in treating insomnia involved 10 core targets: TNF, IL1B, CASP3, TP53, HSP90AA1, PPARG, SLC6A4, ESR1, GSK3B, and AChE. The treatment of insomnia using XYP was found to primarily affect seven enriched GO terms and six related pathways. Notably, XYP targeted TNF, IL1B, CASP3, TP53, HSP90AA1, PPARG, SLC6A4, ESR1, GSK3B, and AChE, while participating in pathways such as neuroactive ligand-receptor interaction, pathways in cancer, and calcium signaling pathway. These findings provided valuable insights into the potential molecular targets and pathways through which XYP might exert its therapeutic effects in treating insomnia.

    Table and Figures | Reference | Related Articles | Metrics | Comments0
    PI3K/AKT/mTOR pathway inhibition and miR-210-mediated suppression of Atg7 promote autophagy in TOPC-induced apoptosis of H1975 cells
    Wuyinxiao Zheng, Haiping Li, Laichun Luo, Chunling Hu, Pengtao You
    Journal of Chinese Pharmaceutical Sciences    2023, 32 (11): 881-892.   DOI: 10.5246/jcps.2023.11.071
    Abstract81)   HTML7)    PDF(pc) (2959KB)(11)       Save

    TOPC (2-(2,5,5,8a-tetramethyl-3,4,4a,5,6,7,8,8a-octahydronaphthalen-1-yl) ethyl piperazine-1-carbodithioate) is a coleolic acid-dithiocarbamate derivative synthesized by our team. Notably, this compound exhibits superior inhibitory effects on the proliferation of human non-small-cell lung cancer (NSCLC) cell lines A549 and H1975 compared to coleolic acid. The primary objective of this study was to investigate the potential molecular mechanisms of TOPC against H1975 cells. Cell proliferation was assessed using the MTT assay, while apoptosis induced by TOPC was evaluated using Hoechst 33342 staining and Western blotting analysis. The expressions of autophagy proteins and the associated PI3K/AKT/mTOR signaling pathway were determined through Western blotting analysis. The transfection efficiency of the miR-210 mimic, inhibitor, and inhibitor NC, as well as the expressions of miR-210 and Atg7, were assessed using qRT-PCR. TOPC demonstrated significant inhibition of A549 and H1975 cell proliferation. Hoechst 33342 staining and Western blotting analysis revealed that TOPC induced apoptosis in H1975 cells. Moreover, TOPC induced autophagy in H1975 cells, as evidenced by increased expressions of autophagy-related proteins, such as Beclin-1, Atg5, Atg7, Atg12, and LC3-II. Additionally, qRT-PCR demonstrated that TOPC significantly downregulated the expression of miR-210 in H1975 cells. Further investigation suggested that TOPC-induced autophagy was mediated by inhibiting the PI3K/AKT/mTOR signaling pathway and suppressing the function of miR-210 on Atg7. The findings clearly demonstrated that TOPC substantially suppressed the growth of A549 and H1975 cells, making it a promising therapeutic agent for NSCLC. Its potential merits further development.

    Table and Figures | Reference | Related Articles | Metrics | Comments0
    Exploring the mechanism of Astragalus and Salvia miltiorrhiza in the treatment of chronic glomerulonephritis: A network pharmacology approach
    Nianjing Qi, Mingxun Yang, Shan Mao
    Journal of Chinese Pharmaceutical Sciences    2024, 33 (7): 620-630.   DOI: 10.5246/jcps.2024.07.046
    Abstract81)   HTML5)    PDF(pc) (7079KB)(24)       Save

    To elucidate the mechanism underlying the therapeutic impact of Astragalus-Danshen in chronic glomerulonephritis (CGN), a comprehensive exploration was conducted utilizing network pharmacology. The TCMSP database was employed to aggregate the chemical constituents and targets associated with Astragalus and Danshen. Simultaneously, disease targets specific to CGN were sourced from the Genecards database. The convergence of these datasets yielded a set of intersection genes, representing potential targets for CGN treatment through Astragalus-Danshen formulations. Subsequently, protein interaction networks and "chemical composition-target" networks were meticulously constructed. Core targets were subjected to GO and KEGG enrichment analyses. The investigation revealed a total of 240 targets corresponding to 20 and 65 chemical components of Astragalus and Danshen, respectively. From this pool, 86 potential targets associated with CGN treatment were discerned, ultimately identifying 29 core targets. Noteworthy among these were TNF, JUN, TP53, IL1B, RELA, MMP9, CASP3, IL10, MAPK14, MYC, and TGFB1. KEGG enrichment analysis illuminated pathways pertinent to CGN, encompassing the IL-17 signaling pathway, TNF signaling pathway, and the AGE-RAGE signaling pathway in diabetic complications. In summary, Astragalus-Danshen exhibited a potential anti-inflammatory and renoprotective effect on CGN, particularly through modulating the IL-17 signaling pathway, TNF signaling pathway, and AGE-RAGE signaling pathway in diabetic complications, involving key regulators such as TNF, JUN, TP53, IL1B, MAPK14, and others.

    Table and Figures | Reference | Related Articles | Metrics | Comments0
    Exploring the main active components and potential mechanisms of Taohong Siwu Decoction for the treatment of Alzheimer’s disease based on network pharmacology
    Shuang Li, Luyao Sun, Sihan You, Jiayi Zhang, Hongyan Yin, Jinmeng Cao, Xinxing Liu, Chunyan Guo, Xifu Liu
    Journal of Chinese Pharmaceutical Sciences    2024, 33 (6): 525-542.   DOI: 10.5246/jcps.2024.06.039
    Abstract80)   HTML11)    PDF(pc) (5803KB)(24)       Save

    Taohong Siwu Decoction (THSWD), a traditional Chinese prescription renowned for its efficacy in promoting blood circulation and alleviating blood stasis, was investigated in this study to delineate its potential active components and discern the core targets (CTs) and signaling pathways implicated in the treatment of Alzheimer’s disease (AD). Initially, 25 active compounds (ACs) and 478 corresponding active ingredient targets (AITs) of THSWD were meticulously identified by scrutinizing the active ingredients and their targets through the Traditional Chinese Medicine Systems Pharmacology (TCMSP) and Similarity Ensemble Approach (SEA) databases. Subsequently, a comprehensive compilation of 724 AD-related targets was assembled from the Therapeutic Target Database (TTD), DisGeNET, DrugBank, Genetic Association Database (GAD), and GeneCards databases. Through a meticulous alignment of AITs with disease-related targets, 64 overlapping targets (OTs) emerged as critical intersections. To distill the key compounds, an intricate analysis of the interrelationships among the 25 ACs and 64 OTs resulted in the identification of 21 first-level key compounds (FKCs). Further scrutiny through protein-protein interaction (PPI) analysis of the 64 OTs revealed 33 CTs. KEGG cluster analysis of these CTs yielded the top 73 pathways, forming the basis for constructing a network diagram encompassing "21 FKCs-33 CTs-73 pathways" using Cytoscape 3.7.2 software. Refining the network through the selection of topological parameters led to the identification of 19 second key components (SKCs). This information was then employed to construct a refined network, "19 SKCs-33 CTs-73 pathways", providing deeper insights into the intricate connections within the system. Further analyses culminated in the creation of a comprehensive network map, encapsulating "6 single drugs-8 potential active ingredients-13 core targets-54 signaling pathways", elucidating the multifaceted intervention of THSWD in AD. These results offered a novel perspective for understanding the pharmacodynamic material basis of THSWD and paved the way for in-depth investigations into its mechanisms of action and clinical applications in the context of AD.

    Table and Figures | Reference | Related Articles | Metrics | Comments0
    Polymer-lipid nanoparticles enhance liver-targeted delivery of therapeutic base editor plasmid for the treatment of hereditary tyrosinemia type 1 (HT-1)
    Datong Gao, Meng Lin, Yiwei Peng, Jiajia Li, Yiliang Yang, Yulu Teng, Siyu Chen, Wen Sun, Zinan Wu, Quan Yuan, Zhenzhen Yang, Yanxia Zhou, Xinru Li, Xianrong Qi
    Journal of Chinese Pharmaceutical Sciences    2024, 33 (3): 189-200.   DOI: 10.5246/jcps.2024.03.015
    Abstract80)   HTML20)    PDF(pc) (15465KB)(30)       Save

    Hereditary tyrosinemia type 1 (HT-1) is a rare autosomal recessive genetic disease with no effective cure at present. In recent years, gene-editing techniques such as base editor (BE) have been explored for treating HT-1. However, the delivery of nucleic acids faces challenges due to existing physiological barriers. In the present study, we constructed an asialoglycoprotein receptor (ASGPR)-targeted polymer-lipid nanoparticle to enhance the delivery efficiency of therapeutic nucleic acids for HT-1. To deliver BE plasmids, a biodegradable cationic polymer, acrylate-amino alcohol copolymer was synthesized and demonstrated superior transfection efficiency compared to the commercially available transfection reagent, Hieff TransTM. Subsequently, DOPE-PEG-GalNAc was combined with copolymer nanoparticles to enhance the hepatocyte delivery of the nanoparticles. Upon loading the recombinant BE plasmid, Fah-pCMV-ABE6.3-EGFP, the polymer-lipid nanoparticles exhibited remarkable hepatocyte selectivity, with a transfection efficiency over 70-fold higher than that of the free plasmid. The study suggested that polymer-lipid nanoparticles, in combination with liver-targeted ligands, could effectively enhance the liver-targeted delivery of therapeutic BE plasmids, providing a promising vector for gene therapy of HT-1.

    Table and Figures | Reference | Related Articles | Metrics | Comments0
    Assessment of acute toxicity and antitumor efficacy of Shizao decoction
    Liwei Ma, Zhe Chen, Guoshan Shi, Yujing Wang, Song Chen, Shiyu Ni, Jing Li, Pengling Ge, Jicheng Liu
    Journal of Chinese Pharmaceutical Sciences    2024, 33 (4): 329-338.   DOI: 10.5246/jcps.2024.04.025
    Abstract79)   HTML5)    PDF(pc) (2351KB)(41)       Save

    This study aimed to assess the acute toxicity of Shizao decoction (SZD) in KM mice and its antitumor activity, offering insights into drug safety and antitumor efficacy. In experiments, specific pathogen-free (SPF) KM mice were administered either saline (as a blank control) or SZD, and the half-lethal dose (LD50) was determined. Additionally, SPF-grade SD rats were treated with SZD to produce SZD-medicated serum (SZD-MS). Assays, including the MTT method, lactic dehydrogenase (LDH) release, colony formation, and flow cytometry, were utilized to measure the inhibitory effects on cancer cell proliferation and induction of apoptosis. The toxicity tests revealed that none of the mice died after oral administration of SZD, rendering it impossible to establish an LD50 value. Notably, serum biochemistry results significantly diverged from those of the blank control group (P < 0.05). Histopathology, using hematoxylin and eosin (H&E) staining, unveiled that SZD exerted detectable damage on the liver and kidneys of the mice. In terms of antitumor activity, SZD-MS demonstrated a significant inhibition of proliferation in five tumor cell lines when compared to the vehicle control (P < 0.05, P < 0.01). This finding was further supported by the increased LDH release from H22 cells (P < 0.05), a reduction in colony formation (P < 0.05, P < 0.01), and an elevated apoptosis rate (P < 0.01). In conclusion, the study revealed that the maximum oral dosage of SZD, set at 0.8 mL/d for each mouse (roughly 120 times the standard adult daily dose), presented minimal toxicity. Moreover, it possessed promising anti-ascite tumor activity, suggesting its safety and therapeutic potential.

    Table and Figures | Reference | Related Articles | Metrics | Comments0
    Unraveling the mechanisms of compound Sophora flavescens injection in melanoma treatment: A network pharmacology
    Xuyang Cui, Zhongjie Ji, Panyang Shi, Xiaocen Wei, Yuning Ma, Mengzhen Xing
    Journal of Chinese Pharmaceutical Sciences    2024, 33 (5): 448-457.   DOI: 10.5246/jcps.2024.05.034
    Abstract78)   HTML4)    PDF(pc) (3251KB)(36)       Save

    In this paper, the mechanism of effect of compound Sophora flavescens injection on the prevention and treatment of melanoma was studied through network pharmacology. TCMSP database was used to explore the active ingredients of Sophora flavescens and Poria cocos in compound Sophora flavescens injection, the drug targets of Sophora flavescens and Poria cocos were detected by Pubchem and Swiss Target Prediction databases, the disease targets related to melanoma were retrieved through GeneCards, OMIM, TTD and CTD databases, and Cytoscape 3.9.1 was used to establish a TCM-component-disease-target network. The interaction network of intersecting target proteins was established by String and Cytoscape, and the topological analysis was performed according to the MCC algorithm by the Cyto-Hubba plug-in to screen the key targets. Finally, GO and KEGG analyses of the relevant targets were performed using the Metascape database. Finally, a total of 60 active ingredients were screened in the compound Sophora flavescens injection, including quercetin, norcetin and white junen. There are 916 targets related to melanoma tumors, including AKT1, EGFR, ESR1, etc. In addition, the anti-melanoma functions of Sophora flavescens injection include the regulation of phosphorylation effects and the effects of oxidative stress responses, and exert anti-tumor effects by regulating cancer pathways, endocrine pathways, Th17 cell differentiation channels and other information pathways. This study reported for the first time the potential mechanism of compound Sophora flavescens injection in the treatment of melanoma disease, and provided ideas and basis for follow-up experimental research.

    Table and Figures | Reference | Related Articles | Metrics | Comments0
    HH-A, a honokiol derivative, alleviates hypoxic brain injury in the animal ischemic model by interacting with hemoglobin
    Yuying Zhang, Pingping Zhang, Hanxin Ding, Xin Zhang, Ye Liu
    Journal of Chinese Pharmaceutical Sciences    2024, 33 (2): 98-109.   DOI: 10.5246/jcps.2024.02.009
    Abstract77)   HTML11)    PDF(pc) (2983KB)(29)       Save

    Exposure to hypoxic conditions can result in significant brain damage, such as that experienced during an ischemic stroke. Thus, finding ways to mitigate ischemia/hypoxia-induced brain tissue damage is a critical issue that needs addressing. HH-A, a derivative of honokiol, has demonstrated potent pharmacological activities and medicinal properties in treating brain ischemia/reperfusion injury. However, its effect on anti-hypoxic responses during stroke remains largely unexplored. In the present study, we subjected male Sprague-Dawley rats to 24 h of hypoxia (oxygen content at 11%) or to 7 d of permanent middle cerebral artery occlusion. We discovered that both 1 mg/kg (i.v.) and 40 mg/kg (i.g.) of HH-A elevated arterial oxygen saturation after 24 h of hypoxia and significantly reduced the infarct volume after 7 d of ischemia. Furthermore, fluorescence staining with hypoxyprobe-1 indicated that HH-A significantly mitigated the severity of hypoxia in brain tissue. Hematoxylin and eosin staining, along with neuronal nuclei immunofluorescent staining, further revealed that HH-A curbed the death of brain cells. To identify potential protein partners of HH-A, we used a molecular fishing approach based on surface plasmon resonance technology. A high binding affinity was detected between HH-A and the hemoglobin subunit beta, with an estimated binding free energy of –8.7 kcal/mol. These findings suggested that HH-A was capable of enhancing hypoxia tolerance and alleviating brain injury caused by ischemia.

    Table and Figures | Reference | Related Articles | Metrics | Comments0
    Study on the potential mechanism of Pu Gong Ying in treating breast hyperplasia based on network pharmacology and molecular docking
    Zhiyong Sun, Shuli Gao, Yang Zhang, Gangqiang Xue, Zilin Yuan, Shaonan Wang
    Journal of Chinese Pharmaceutical Sciences    0, (): 893-910.   DOI: 10.5246/jcps.2023.11.072
    Abstract77)   HTML4)    PDF(pc) (14503KB)(28)       Save

    In the present study, network pharmacology was employed to elucidate the targets and pathways involved in the treatment of breast hyperplasia (BH) by Pu Gong Ying (PGY). Molecular docking was utilized to analyze the interaction between PGY and key targets based on the findings of network pharmacology. The intersection of 261 targets associated with 15 PGY compounds and 2455 targets related to BH yielded 90 common targets (89 of which were included in the protein-protein interaction (PPI) network, while one target did not exhibit interactions with any other targets in the PPI network). The top 10 hub targets ranked in the PPI network and the top 10 targets according to the Molecular Complex Detection (MOCDE) score were intersected, resulting in the identification of CASP3, EGFR, ESR1, ERBB2, MMP9, and PTGS2 as key targets, as determined by different algorithms. Gene Ontology (GO) functional enrichment analysis revealed 284 biological components. Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway analysis identified 125 pathways, primarily associated with the regulation of pathways in cancer, the PI3K-Akt signaling pathway, the MAPK signaling pathway, microRNAs in cancer, chemical carcinogenesis-receptor activation, and others. Molecular docking results demonstrated the favorable binding efficacy of PGY9, PGY10, and PGY11 with the core targets. The findings suggested that PGY exerted its therapeutic effects on BH through multiple targets and biological pathways. This study contributed to the understanding of the molecular mechanisms underlying BH development and provided implications for BH-targeted therapy and even breast cancer prevention.

    Table and Figures | Reference | Related Articles | Metrics | Comments0
    The morphology and in vitro antioxidative effect of ionized polysaccharide from Angelica Sinensis
    Jie Wang, Zizhen Huang, Weijiao Xue, Yan Zhang, Chunxia Tan
    Journal of Chinese Pharmaceutical Sciences    2024, 33 (4): 316-328.   DOI: 10.5246/jcps.2024.04.024
    Abstract75)   HTML13)    PDF(pc) (2233KB)(29)       Save

    abstract

    Table and Figures | Reference | Related Articles | Metrics | Comments0
    Advancements in sequential and combination treatments for osteoporosis
    Jia Zheng, Ying Fu
    Journal of Chinese Pharmaceutical Sciences    2024, 33 (7): 587-596.   DOI: 10.5246/jcps.2024.07.043
    Abstract75)   HTML16)    PDF(pc) (1389KB)(44)       Save

    Osteoporosis, a prevalent systemic degenerative disease, poses significant challenges to China’s national health, particularly due to complications such as fractures. Therapeutic interventions for osteoporosis primarily involve bone resorption inhibitors (antiresorptive) and bone formation promoters (anabolic). Numerous studies underscore the importance of sequential and combination treatments using diverse drug types. Such approaches have shown considerable efficacy in increasing bone mineral density, reducing fracture risk, and preventing the progression of osteoporosis. This article aimed to consolidate various sequential treatment schemes, offering valuable insights for clinicians in their practice.

    Table and Figures | Reference | Related Articles | Metrics | Comments0
    Advancements in anti-tuberculosis drug potentiators: targeting mechanisms of tuberculosis resistance
    Jianhui Yang, Xiao Wang, Jinbo Zhang, Yishuang Liu
    Journal of Chinese Pharmaceutical Sciences    2024, 33 (2): 89-97.   DOI: 10.5246/jcps.2024.02.008
    Abstract74)   HTML43)    PDF(pc) (1593KB)(17)       Save

    Tuberculosis (TB) constitutes a formidable global health challenge, exacerbated by the rise of multidrug-resistant TB (MDR-TB) strains. The effectiveness of anti-TB drugs has been hindered by this emergence of resistance. To address this, the development of synergistic compounds, informed by drug resistance mechanisms, holds promise for mitigating resistance emergence and shortening treatment durations. This review focuses on the amalgamation of anti-TB drugs with potentiators targeting the cell wall, efflux pump, and β-lactamase. Our aim is to offer insights that guide the future development of novel potentiators with enhanced efficacy and reduced toxicity.

    Table and Figures | Reference | Related Articles | Metrics | Comments0
    Quercetin, the key constituent of Astragali Radix, modulates ferroptosis in PASMCs and attenuates hypoxia pulmonary hypertension via the MAPK signaling pathway
    Xia Li, Beibei Cheng, Junlan Tan, Jiajing Wan, Yuhong Wang, Aiguo Dai
    Journal of Chinese Pharmaceutical Sciences    2024, 33 (8): 714-729.   DOI: 10.5246/jcps.2024.08.053
    Abstract73)   HTML17)    PDF(pc) (3036KB)(28)       Save

    This study delved into the mechanism by which the principal component of Astragali Radix regulated ferroptosis in the context of hypoxia-induced pulmonary hypertension, employing a combination of network pharmacology and experimental validation techniques. Active constituents of Astragali Radix and their corresponding targets were identified using the TCMSP database, while therapeutic targets associated with hypoxia-induced pulmonary hypertension were sourced from the GeneCards database. The Venn online tool facilitated the identification of overlapping targets between the active constituents of Astragali Radix and hypoxia-induced pulmonary hypertension. Interaction network diagrams depicting the relationship between Astragali Radix’s active constituents and their targets were constructed using Cytoscape software, with core targets and sub-networks identified using the CytoHubba plug-in. Gene ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway enrichment analyses were conducted using the DAVID database. Additionally, the FerrDb database was consulted to analyze genes implicated in regulating ferroptosis. The investigation revealed 18 active constituents selected from Astragali Radix, with quercetin emerging as the key component. A total of 35 potential targets associated with Astragali Radix in regulating ferroptosis and addressing hypoxia-induced pulmonary hypertension were predicted. Experimental validation demonstrated that quercetin could inhibit the MAPK signaling pathway, resulting in reduced Fe2+ and lipid peroxide levels, increased GPX4 expression, and the reversal of ferroptosis. In summary, this study elucidated the fundamental constituents and pivotal signaling pathways through which Astragali Radix modulated ferroptosis and mitigated hypoxia-induced pulmonary hypertension. Specifically, quercetin, a core constituent of Astragali Radix, was observed to inhibit ferroptosis in pulmonary arterial smooth muscle cells via the MAPK pathway and alleviate hypoxia-induced pulmonary hypertension.

    Table and Figures | Reference | Related Articles | Metrics | Comments0
    Integrated serum pharmacochemistry and network pharmacology analyses reveal the bioactive metabolites and potential functional mechanism of Piper longum L. in the treatment of gastric ulcer in rats
    Hong Zhang, Shasha Zhang, Huanyun Wang, Yue Liang, Shikui Wu, Lijun Sun, Huimin Xia, Yunxia Bai, Huiwen Zhang
    Journal of Chinese Pharmaceutical Sciences    2024, 33 (2): 156-168.   DOI: 10.5246/jcps.2024.02.013
    Abstract72)   HTML7)    PDF(pc) (5718KB)(9)       Save

    The fruit of Piper longum L. (PL) is widely utilized in China for medicinal and dietary purposes, and it is also used in Ayurvedic medicine in India to treat gastric disorders and other ailments. In the present study, a strategy combining serum pharmacochemistry with network pharmacology was proposed to screen the bioactive metabolites derived from PL and explore their potential functional mechanisms. The strategy primarily involved investigating the anti-gastric ulcer activities, network pharmacology analysis, and metabolite identification. The results demonstrated the efficacy of PL in protecting against ethanol-induced gastric ulcers. Through network pharmacology approaches, potential drug-disease common targets were identified. GO enrichment analysis predicted that PL might influence multiple biological processes, such as lipid metabolism and inflammatory response. KEGG enrichment analysis suggested the involvement of the TNF and AGE-RAGE signaling pathways. Molecular docking further indicated that the synergistic effect of sesamin, piperine, and other ingredients could be the main contributors to PL’s anti-inflammatory and antibacterial activities. Additionally, the serum pharmacochemistry of PL was established, enabling the screening of absorbed components and metabolites for their anti-gastric ulcer activity. A total of 23 prototypes and 17 metabolites were found to significantly contribute to the anti-gastric ulcer activity, suggesting that these bioactive compounds could serve as potential active components of PL. Overall, this investigation provided an experimental foundation to support the clinical application of PL in gastric ulcer therapy.

    Table and Figures | Reference | Related Articles | Metrics | Comments0
    Hugan Buzure granule ameliorates immune liver injury through the EGFR/Ras/PI3K/AKT signaling pathway: A network pharmacology study and experimental validation
    Zhengru Han, Wanci Song, Yang Luo, Min Xiao, Mengheng Wang, Wuyinxiao Zheng, Hanxiong Dan, Qiang Yin, Hailong Yin, Pengtao You
    Journal of Chinese Pharmaceutical Sciences    2024, 33 (2): 123-141.   DOI: 10.5246/jcps.2024.02.011
    Abstract71)   HTML10)    PDF(pc) (10378KB)(14)       Save

    Hugan Buzure granule (HBG) is a traditional prescription in Uygur medicine that is known for its hepatoprotective properties. In a previous study, the authors have investigated the mechanism through which HBG protects against immune liver injury (ILI) by regulating immune balance and inhibiting apoptosis mediated by the IRF1/JNK signaling pathway. However, not all mechanisms are thoroughly explored. To address this issue, the present study further investigated the mechanism by which HBG reduced concanavalin A (ConA)-induced ILI in mice using network pharmacology and in vivo experiments. Initially, the livers of the mice were examined through pathological sections, which prompted further screening. The TCMSP, PharmMapper, and GeneCards databases were employed to identify the active compounds and key targets of HBG in the treatment of ILI. Subsequently, the key targets and related signaling pathways were screened using network pharmacology and molecular docking. The efficacy and mechanism of HBG against ILI were explored in a ConA-induced mouse model. Key proteins were analyzed, and their expression levels were detected using Western blotting analysis. The network pharmacology analysis revealed 16 compounds and 53 targets associated with HBG. The component-target-pathway (C-T-P) network and molecular docking indicated that EGFR, HRAS, AKT1, and PIK3R1 were the key targets of HBG in the context of ILI. TUNEL staining results demonstrated that HBG significantly reduced apoptosis in mice with ILI. Moreover, HBG markedly upregulated the expression of p-EGFR, Ras, p-AKT, p-PI3K, p-BAD, and Bcl-2, while down-regulating the levels of Bax, cleaved-caspase 9, and cleaved-caspase 3 proteins, as compared to the ConA group. These findings suggested that HBG alleviated ILI by inhibiting apoptosis through the EGFR/Ras/PI3K/AKT signaling pathway.

    Table and Figures | Reference | Related Articles | Metrics | Comments0
    Real-world safety study of posaconazole oral suspension in children under 13 years of age
    Yingqiu Tu, Minfang Lai, Nan Zhong, Hongxiao Cao, Zhenggang Huang
    Journal of Chinese Pharmaceutical Sciences    2024, 33 (4): 352-357.   DOI: 10.5246/jcps.2024.04.027
    Abstract71)   HTML3)    PDF(pc) (1527KB)(37)       Save

    In the present study, we aimed to investigate the safety of posaconazole oral suspension in children under 13 years of age. A retrospective analysis was conducted on six cases of pediatric patients with acute lymphocytic leukemia who received prophylactic or sequential treatment with posaconazole oral suspension. Among the six patients (four boys and two girls) with an average age of (8.67 ± 1.86) years, one child developed bilateral lower limb edema after 7 d of posaconazole oral suspension, and two children experienced elevated levels of liver enzymes during the course of treatment. In conclusion, common adverse reactions of posaconazole included liver damage and gastrointestinal symptoms. However, reports of lower limb edema in patients are rare. Further studies with larger sample sizes are needed to evaluate the safety of posaconazole oral suspension in children under 13 years of age.

    Table and Figures | Reference | Related Articles | Metrics | Comments0
    Design, synthesis, and biological assessment of prodrugs for nitroreductase-based HSP90 inhibitor BIIB021: exploring their potential as anticancer agents
    Zhengrong Wu, Qinjian Xie, Peng Jing, Tianfeng Zhang, Jiaxi Han, Dian He
    Journal of Chinese Pharmaceutical Sciences    2024, 33 (1): 15-25.   DOI: 10.5246/jcps.2024.01.002
    Abstract68)   HTML48)    PDF(pc) (2224KB)(22)       Save

    A series of prodrugs based on BIIB021, designed for nitroreductase (NTR), were synthesized and tested in vitro for their cytotoxic effects as potential anticancer agents. The results revealed that compounds 1c and 2c exhibited promising antitumor activity, with IC50 values of 0.72 and 1.12 μM, respectively. Notably, both compounds demonstrated lower toxicity to normal WI-38 cells compared to the positive control BIIB021 (IC50 = 495.51 and 570.27 μM vs. 261 μM). Cell cycle analysis indicated that both compounds induced cell cycle arrest in the G2/M phase, accompanied by a concomitant decrease in the population of the G0/G1 phase in HeLa cells, ultimately leading to apoptosis. These preliminary findings suggested that compounds 1c and 2c held the potential to serve as promising lead compounds for further structural optimization and in vivo validation studies.

    Table and Figures | Reference | Related Articles | Metrics | Comments0
    A network pharmacological study to investigate the combination of LHQW-XYS in the treatment of COVID-19 olfactory impairment-associated
    Xiaoyu Wei, Luhang Yu, Mengru Li, Qiang Xu
    Journal of Chinese Pharmaceutical Sciences    2024, 33 (7): 631-646.   DOI: 10.5246/jcps.2024.07.047
    Abstract68)   HTML8)    PDF(pc) (4685KB)(37)       Save

    To explore the target of action of LHQW-XYS on the main components of COVID-19 olfactory impairment by using network pharmacological methods and try to reveal its mechanism of action in the treatment related to COVID-19 induced olfactory impairment, we used the TCMSP platform to obtain potential active ingredients through oral utilization and drug-like properties screening; the Swiss TargetPrediction platform to predict the targets of the active ingredients and construct a drug-ingredient-target network, and then obtained the gene targets of COVID-19 olfactory injury through GeneCards, OMIM, and TTD platforms to intersect the drug targets and disease genes to obtain common targets. The drug targets and disease genes were intersected to obtain common targets. STRING and Cytoscape 3.8.2 software were used to construct the target-disease gene PPI network, screen the key targets and core gene clusters, and analyze the key targets by GO and KEGG enrichment analyses with the help of the Metascape platform, and then map the screened core active ingredients and their targets into the pathway to construct the core active ingredients-targets-pathway network. The core active ingredient-target-pathway network was constructed, and finally, molecular docking was carried out. The results showed that there were 4669 potential targets, 5609 disease targets, and 17 drug-disease cross-targets for the active ingredients of LHQW-XYS. The GO and KEGG enrichment analyses indicated that the mechanism of LHQW-XYS in the treatment of olfactory impairment in COVID-19 may be due to the regulation of related signaling pathways, such as Serotonergic synapse and Regulation of lipolysis in adipocytes. Molecular docking showed that six active components (quercetin, luteolin, kaempferol, 7-methoxy-2-methylisoflavone, wogonin, medicarpin) and two key genes (PTGS2, PPARG) had good binding properties. In the end, we conclude that LHQW-XYS may act on Serotonergic synapse and Regulation of lipolysis in adipocyte pathways to achieve anti-COVID-19 olfactory impairment-associated effects.

    Table and Figures | Reference | Related Articles | Metrics | Comments0
    Elucidating the mechanisms underlying Taohong Siwu Decoction in preventing arteriovenous fistula failure: A comprehensive study combining network pharmacology, molecular docking, and dynamic simulation
    Shisheng Han, Yi Wang
    Journal of Chinese Pharmaceutical Sciences    2024, 33 (6): 511-524.   DOI: 10.5246/jcps.2024.06.038
    Abstract67)   HTML9)    PDF(pc) (3176KB)(25)       Save

    Arteriovenous fistula (AVF) failure poses a significant prognostic challenge for patients undergoing hemodialysis. This study aimed to elucidate the mechanisms underlying the potential therapeutic effects of Taohong Siwu Decoction (TSD) in addressing AVF failure. A comprehensive approach integrating network pharmacology, molecular docking, and dynamic simulation was employed to validate it. The active constituents and putative targets of TSD were acquired from the Traditional Chinese Medicine Systems Pharmacology (TCMSP), Traditional Chinese Medicine Integrative Platform (TCMIP), and SwissTargetPrediction databases. Targets relevant to AVF failure were retrieved from the Online Mendelian Inheritance in Man (OMIM), DisGeNET, and GeneCards databases. The construction of the herb-ingredient-target network and protein-protein interaction (PPI) network was carried out using Cytoscape. Furthermore, we performed GO and KEGG enrichment analyses using the Metascape database. Molecular docking was executed with AutoDock, and results were visualized via PyMOL software. Additionally, molecular dynamics simulations were conducted using GROMACS. In this comprehensive analysis, we identified a total of 66 active ingredients and 769 potential targets, which subsequently led us to identify 87 targets closely associated with AVF failure. Notably, 10 key ingredients and 15 core targets were singled out. Among the pivotal constituents were gibberellin A120, gibberellin A30, kaempferol, and paeoniflorin, while core targets included TNF-α, IL-6, VEGFA and MMP9. Enrichment analyses, encompassing GO and KEGG, illuminated that TSD’s potential therapeutic effects in addressing AVF failure might hinge on the modulation of inflammation, shear stress, and extracellular matrix remodeling. Furthermore, molecular docking investigations and dynamic simulations corroborated strong binding interactions between the key active constituents and the core targets. Consequently, it is plausible that TSD may enhance AVF patency primarily by regulating processes related to inflammation, shear stress, and extracellular matrix remodeling. These findings constitute a solid molecular rationale for the application of TSD in the context of AVF failure.

    Table and Figures | Reference | Related Articles | Metrics | Comments0
    Preparation of core-shell targeted tracer recombinant human interleukin II microspheres via coaxial electrostatic spraying
    Yuan Zhu, Jiaqi Xu, Xiaoyan Chen, Yingshu Feng, Caleb Kesse Firempong, Haibing He, Hongfei Liu
    Journal of Chinese Pharmaceutical Sciences    2024, 33 (6): 495-510.   DOI: 10.5246/jcps.2024.06.037
    Abstract65)   HTML14)    PDF(pc) (20757KB)(15)       Save

    The potential application of recombinant human interleukin-2 (rhIL-2) in promoting immune cell proliferation and differentiation for the treatment of lung cancer is acknowledged. However, the inherent challenges associated with the short half-life and instability of rhIL-2 necessitate its encapsulation into microspheres for sustained release administration. In this study, the coaxial electrostatic spray technique was employed to fabricate rhIL-2-loaded core-shell microspheres. Quantum dots served as tracer materials, and the core-shell composite microspheres were fashioned with chitosan coating the rhIL-2 and quantum dots conjugates in the core layer and hyaluronic acid in the shell layer. A systematic exploration of factors such as carrier concentration, positive voltage, pinhole diameter, and spray flow rate was conducted using a single-factor method. The coaxial electrostatic spray process parameters for core-shell microsphere preparation were also meticulously optimized. The results indicated that the developed core-shell microspheres exhibited a favorable particle size ranging from 1.2 to 2.0 μm, accompanied by encapsulation efficiency and drug loading values of 78.39% ± 1.96% and 19.58 ± 2.76 μg/mg, respectively. In vitro release studies demonstrated a sustained release effect without any discernible burst release phenomenon. Biological activity assessments revealed that rhIL-2 within the core-shell microspheres mirrored the efficacy of the free protein drug. Additionally, in vivo imaging analysis attested to the active targeting properties of the microspheres. These findings robustly supported the successful development of sustained-release targeted rhIL-2-loaded microspheres, providing a theoretical foundation for protein-microsphere formulations.

    Table and Figures | Reference | Related Articles | Metrics | Comments0
    GAS5, as the ceRNA of miR-223-3p, mediates pyroptosis and inhibits the proliferation of brain glial cells U87, and quercetin can enhance its effect
    Yanqiang Sun, Hongliang Li, Kangxue Chen, Jie Li, Zhonglei Sun
    Journal of Chinese Pharmaceutical Sciences    2024, 33 (3): 230-240.   DOI: 10.5246/jcps.2024.03.018
    Abstract65)   HTML4)    PDF(pc) (2718KB)(22)       Save

    This study explored the inhibitory effect of miR-223-3p on the proliferation of brain glioma cells and its potential mechanism in relation to growth arrest-specific transcripts (GAS5). We utilized the StarBase tool to predict the binding of GAS5 to miR-223-3p, further confirming the binding relationship between GAS5 and miR-223-3p through a dual luciferase reporter assay and RNA immunoprecipitation. In vitro cultured U87 brain glial cells were categorized into four groups: the control group, quercetin group, GAS5 inhibition group, and quercetin + si-GAS5 group. We analyzed and compared the impacts of quercetin on GAS5/miR-223-3p and pyroptotic proteins (NLRP3, ASC, caspase-1, GSDMD, and GSDME), as well as the proliferative capacity of U87 cells. StarBase’s predictions indicated that GAS5 bound to miR-223-3p. This was corroborated by the dual luciferase reporter assay and RNA immunoprecipitation assay, which demonstrated a direct binding between GAS5 and miR-223-3p. Quercetin was observed to enhance GAS5 expression, inhibit the expression of miR-223-3p and pyroptotic proteins (NLRP3, ASC, caspase-1, GSDMD, and GSDME), and suppress the proliferation and invasion of U87 cells (P < 0.05). Downregulation of GAS5 expression correlated with an increase in the expression of miR-223-3p and pyroptotic proteins (NLRP3, ASC, caspase-1, GSDMD, and GSDME), promoting the proliferation and invasion of RC-4B/C cells (P < 0.05). Quercetin was able to reverse the increase in miR-223-3p expression and pyroptotic proteins (NLRP3, ASC, caspase-1, GSDMD, and GSDME) induced by the downregulation of GAS5, thereby inhibiting the proliferation and invasion of U87 cells (P < 0.05). In conclusion, quercetin might inhibit the proliferation of U87 brain glioma cells by promoting the expression of GAS5, which in turn competitively inhibited miR-223-3p and suppressed the pyroptotic signaling pathway.

    Table and Figures | Reference | Related Articles | Metrics | Comments0
    Analyzing the mechanism and experimental validation of Astilbe chinensis in the treatment of rheumatoid arthritis through network pharmacology
    Ying Chen, Haixia Ying, Tingting Cai, Yunling Xu
    Journal of Chinese Pharmaceutical Sciences    2024, 33 (3): 248-257.   DOI: 10.5246/jcps.2024.03.020
    Abstract64)   HTML5)    PDF(pc) (4608KB)(28)       Save

    To unravel the active components and potential mechanisms of Astilbe chinensis in treating rheumatoid arthritis (RA), we employed a comprehensive strategy that combined network pharmacology and biological activity verification. Firstly, we identified the relevant compounds in A. chinensis from the literature, and RA-related targets were gathered through DisGeNET, GeneCards, and OMIM databases. Subsequently, compound-target and protein-protein interaction networks were constructed to predict the key compounds and promising protein targets of A. chinensis. Finally, these predictions were validated through in vitro anti-inflammatory activity experiments. A total of 29 potential active compounds and 117 intersecting pharmacological targets were identified. Among them, key active compounds included 3β,6β-dihydroxy olean-12-en-27-oic acid (astilbic acid), 3β-acetoxyolean-12-en-27-oic acid (3-acetyl oleanolic acid), 3β-hydroxyurs-12-en-27-oic acid, 4-O-galloylbergenin, and (+)/(-)-catechin. Key targets were identified as AKT1, MMP9, EGFR, CASP3, and HSP90AA1. GO enrichment analysis indicated that signal transduction, proteolysis, and negative regulation of the apoptotic process were closely associated with A. chinensis treatment in RA. KEGG pathway analysis indicated that pathways in cancer, osteoclast differentiation, and endocrine resistance might be crucial for A. chinensis intervention in RA. This finding suggested that multiple components in A. chinensis could regulate various signaling pathways and targets, playing preventive and therapeutic roles in RA. In vitro experiments demonstrated that A. chinensis extracts inhibited the secretion of inflammatory factors (NO, TNF-α, and IL-6) and significantly suppressed the expression of inducible nitric oxide synthase (iNOS), IL-6, and TNF-α mRNA in LPS-induced RAW 264.7 cells. Collectively, our findings not only established the theoretical basis for the efficacy of A. chinensis in treating RA but also provided a direction for subsequent research.

    Table and Figures | Reference | Related Articles | Metrics | Comments0
    Advancements in cellular senescence-based therapeutic approaches for colorectal cancer: a comparative study of Chinese and western medications
    Tao Zhang, Haochen Han, Liang Zhao, Yijing Zhang, Yu Deng, Yongheng He
    Journal of Chinese Pharmaceutical Sciences    2024, 33 (5): 396-411.   DOI: 10.5246/jcps.2024.05.030
    Abstract64)   HTML12)    PDF(pc) (1609KB)(24)       Save

    Colorectal cancer (CRC) is a prevalent malignant neoplasm with complex and poorly understood etiology. Cellular senescence, characterized by irreversible cell division arrest, plays a crucial role in the development of CRC by acting as a defense mechanism against tumor formation. Current clinical treatment modalities for CRC, such as surgery, radiotherapy, and chemotherapy, often come with significant side effects and high costs, placing a substantial physical and psychological burden on patients. Consequently, exploring Chinese medicinal treatments with milder side effects and consistent efficacy is essential. Recent research has highlighted the potential of traditional Chinese medicine (TCM) components and formulations to modulate the senescence process of cancer cells and exhibit anticancer properties. These findings offer a promising avenue for the prevention and treatment of CRC within clinical settings. However, a comprehensive evaluation of how TCM can control cellular senescence to prevent and manage CRC is currently lacking. This article aims to provide a comprehensive overview of pharmaceutical compounds from western medicine, individual components of TCM, and their combinations in recent research that target cellular senescence as part of CRC treatment. The objective is to present new perspectives on CRC treatment and drug development.

    Table and Figures | Reference | Related Articles | Metrics | Comments0
    Failure mode and effect analysis of the risk management of non-integral-dosage drug dispensing in PIVAS
    Kuikui Geng, Juan He, Sheng Rong, Zhaohu Jia, Xiangxiang Zhang, Tianlu Shi
    Journal of Chinese Pharmaceutical Sciences    2024, 33 (7): 597-608.   DOI: 10.5246/jcps.2024.07.044
    Abstract64)   HTML5)    PDF(pc) (1526KB)(18)       Save

    To mitigate risks associated with the prescription examination, marking, dispensing, checking, and review of non-integral-dosage drugs in Pharmacy Intravenous Admixture Service (PIVAS), we formed a project team. Employing the failure mode and effect analysis (FMEA) management method, we identified potential risks in four critical steps of the non-integral-dosage drug dispensing process within PIVAS drug management: prescription verification, mixed allocation, and verification. For each step, we assigned scores for severity, incidence, and detectability, subsequently calculating the Risk Priority Number (RPN) to prioritize identified risks. Targeted measures for improvement were developed for steps with the highest RPN values. A total of 31 risk factors were documented in the management of non-integral-dosage drugs, with the dispensing process being particularly vulnerable. Specific measures were devised for eight high RPN risks. Following a 3-month optimization and improvement period, RPN values and incidences of internal differences were significantly reduced. The implemented measures demonstrated effective risk control. Notably, we established a comprehensive conversion system for partial-dose drug dispensing, directly translating into a volume of suction fluid for dispensing personnel based on doctor orders. This eliminated the need for manual secondary calculations, thereby standardizing and automating the dispensing of non-integral-dosage drugs in PIVAS. Simultaneously, our project team conducted a dissolution test on 23 types of drugs with non-integral dosage, revealing that the solvent volume increased for 11 types after dissolution. The dosage conversion for partial dosage was recalibrated based on the volume of the final solution to ensure dosage accuracy. Through the application of failure mode and effect analysis, we systematically managed the risks associated with non-integral-dosage drugs in PIVAS. This approach addressed safety concerns in the dispensing process, reduced errors, and ensured the safe and precise administration of medication to patients.

    Table and Figures | Reference | Related Articles | Metrics | Comments0
    Effect of Huanglian Jiedu Decoction on cardiac endoplasmic reticulum stress in spontaneously hypertensive rats
    Xiaoming Zhang, Shihui Zhu, Yiwen Gao, Jianxiang Li, Nan Zhang, Guihua Yue
    Journal of Chinese Pharmaceutical Sciences    2024, 33 (7): 609-619.   DOI: 10.5246/jcps.2024.07.045
    Abstract63)   HTML8)    PDF(pc) (2238KB)(19)       Save

    Huanglian Jiedu Decoction (HLJDD) is a quintessential prescription renowned for its heat-clearing and detoxifying properties. It is primarily prescribed to counteract the syndrome characterized by the excessive heat of the Sanjiao fire. Notably, the hyperactivity of liver fire is frequently linked with hypertension, where wind fire and wind toxicity emerge as pivotal pathogenic factors. This study aimed to investigate the impact of HLJDD on the endoplasmic reticulum in spontaneously hypertensive rats (SHR), further delving into the interplay between endoplasmic reticulum stress (ERS) and myocardial remodeling and damage. Fifty SHR rats were stratified randomly into five cohorts: model, low-dose HLJDD, medium-dose HLJDD, high-dose HLJDD, and captopril groups. For comparison, a set of Wistar-Kyoto (WKY ) rats served as the baseline control group, with each group comprising 10 rats. While the model and control groups received equivalent volumes of normal saline via gavage, the other groups were administered the respective drug dosages through the same route daily for a span of 6 weeks. Upon the experiment’s conclusion, metrics such as the heart mass index (HWI) and left ventricular mass index (LVWI) were assessed. Cardiac tissue anomalies were identified using H&E staining, while ERS-related protein and mRNA expression levels were ascertained via Western blotting analysis and qPCR. Moreover, TUNEL staining was employed to detect cardiomyocyte apoptosis. The findings indicated that increasing HLJDD concentrations corresponded with escalated HWI and LVWI in rat hearts (P < 0.05). There was a marked enhancement in myocardial structural integrity, accompanied by a notable reduction in collagen fibers. The mRNA and protein expressions of myocardial inositol-dependent enzyme 1α (IRE1α), X-box binding protein 1 (XBP1), glycoregulatory protein 78 (GRP78), and CCAAT enhancer binding protein homologous protein (CHOP) in the medium and high-dose groups saw significant declines (P < 0.05). These effects mirrored those observed in the captopril group. The study underscored HLJDD’s efficacy in mitigating myocardial tissue damage in SHR. This therapeutic effect was potentially attributed to the downregulation of IRE1α, XBP1, GRP78, and CHOP, curbing excessive ERS, diminishing cardiomyocyte apoptosis, and thereby conferring cardioprotection.

    Table and Figures | Reference | Related Articles | Metrics | Comments0
    Advancements in pharmacological effects and administration routes of hydrogen gas: A comprehensive research overview
    Hui Zhang, Hongmei Zhang, Jun Peng, Yun Ling
    Journal of Chinese Pharmaceutical Sciences    2024, 33 (6): 571-578.   DOI: 10.5246/jcps.2024.06.042
    Abstract62)   HTML5)    PDF(pc) (1397KB)(33)       Save

    Hydrogen, the simplest element in the universe. Hydrogen gas is colorless, odorless, and tasteless. As a reducing agent composed of two atoms. It exhibits strong reducing power and possesses numerous pharmacological effects, including anti-oxidation, antifatigue, anti-radiation, anti-inflammation, hypoglycemic, and hypolipidemic effects. Various methods exist for supplying hydrogen, but inhaling the gas is dangerous, drinking hydrogen-rich water is ineffective, and injecting hydrogen-rich saline is inconvenient. The most viable approach for clinical use is oral medicine, which produces hydrogen in vivo. Hydrogen gas holds promising potential as a clinical medicine in the future.

    Reference | Related Articles | Metrics | Comments0
    The research group of Prof. Yanxing Jia has made new progress in the field of total synthesis of natural products
    State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University Health Science Center
    Journal of Chinese Pharmaceutical Sciences    2024, 33 (4): 374-375.  
    Abstract62)      PDF(pc) (1822KB)(26)       Save
    The research group of Prof. Yanxing Jia has made new progress in the field of total synthesis of natural products.
    Related Articles | Metrics | Comments0