Journal of Chinese Pharmaceutical Sciences

Phytochemistry and pharmacological activities of Ficus carica latex: a systematic review

Haneen Mohammad, Muhammed Alzweiri

2022, 31(2): 81-96. DOI: 10.5246/jcps.2022.02.007

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Ficus carica tree produces a white sap that is traditionally used for the treatment of skin conditions, such as warts. Ficus carica latex is considered a rich source of proteins and metabolites that have various pharmacological activities. Most of the latex pharmacological activities are attributed to its phenolic content, such as anticancer, antiviral, antioxidant, anti-angiogenic, hepatoprotective, and wound-healing activities. Moreover, Ficus carica latex contains proteases that are involved in the treatments of skin conditions, such as warts, and display antiparasitic activity. Additionally, chitinase enzymes and coumarins are isolated from Ficus carica latex and involved in the antimicrobial activities of latex.

Improvement of Kdo's efficient large-scale chemical synthesis method

Ao Sun, Zipeng Li, Ting Liu, Xiangbao Meng, Shuchun Li, Zhongjun Li

2022, 31(2): 97-107. DOI: 10.5246/jcps.2022.02.008

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Kdo residues are widely distributed in bacteria. They are components of bacterial lipopolysaccharide (LPS) and capsular polysaccharides, which can be recognized by the human adaptive immune system, and have great potential for developing new sugar chips and antibacterial vaccines. By improving the existing methods, we optimized the Kdo chemical synthesis method, which was able to efficiently synthesize Kdo monosaccharides with high purity, laying a foundation for the construction of subsequent compound libraries. Kdo acylation can easily form 1,5-lactones and reduce the efficiency of synthesis. By changing the synthesis sequence, we avoided the formation of Kdo 1,5-lactones, improved the synthesis efficiency of Kdo glycals, and provided a new strategy for derivatization.

The protective effect of W026B on global cerebral ischemia/reperfusion injury model in rats

Ziyi Wang, Xiaoyan Liu, Yuanjun Zhu, Ye Liu, Pingping Zhang, Yinye Wang

2022, 31(2): 108-116. DOI: 10.5246/jcps.2022.02.009

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Cerebral ischemia seriously affects the quality of life and health of human worldwide. W026B is a newly synthesized lignan derivative that has a protective effect on the focal cerebral ischemia/reperfusion model, while it is unclear whether W026B has a cerebral protective effect on the model of global cerebral ischemia/reperfusion (GCI/R). In this study, we investigated the protective effect of W026B on the four-vessel occlusion GCI/R model. The results showed that W026B obviously increased the survival rate of rats during 7 d after GCI/R and significantly improved neurological deficits within 7 d after GCI/R. It evidently enhanced the number of survival neurons in the hippocampus of GCI/R rats. Furthermore, W026B notably lowered the level of ROS, and increased the activity of SOD in the hippocampus of GCI/R rats. Moreover, it also decreased the expression of NF-κB p65 and the level of IL-6 apparently. In addition, W026B evidently lowered the activity of caspase-3. In conclusion, this study firstly proves that W026B has the protective effect on GCI/R rats. Its cerebral protective effect maybe related to the inhibition of oxidative stress, inflammatory response, and cell apoptosis during GCI/R. These results provide new evidence with the protective effect of W026B on cerebral ischemia/reperfusion injury.

Investigation on the mechanism of YQHX against cerebral ischemic injury based on network pharmacology and molecular docking

Yan Shang, Xiaoyuan Lin, Tiantian Zhang, Lihua Xie, Guoheng Hu

2022, 31(2): 117-133. DOI: 10.5246/jcps.2022.02.010

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Cerebral ischemia (CI) is the world’s second-largest lethal disease, with a high recurrence and teratogenic rate. Traditional Chinese medicine (TCM) YQHX (a pharmaceutical preparation from herbs) has a certain effect in the clinical treatment of CI, while its underlying mechanism remains largely undetermined. To explore the potential mechanism, we used network pharmacology and molecular docking in the present study. TCMSP and CNKI databases were used to explore the active ingredients of YQHX; the Pharmmapper database was used to get the ingredient targets; the OMIM, GeneCards, and DisGeNET databases were used to obtain the disease targets; the Venn diagram was used to obtain the intersection targets, the Cytoscape was used to visualize results and plug-in MCODE to obtain core targets; the Metascape database was used to perform GO and KEGG pathway enrichment analyses on core targets. The top 20 KEGG pathway enrichment pathways were used to construct the "ingredient-target-pathway" network by Cytoscape; the top 10 ingredients and the top five protein targets were used for molecular docking with AutoDock Vina software, and PyMoL and Ligplus software were used to visualize the results. A total of 83 active ingredients were screened from YQHX. Moreover, 432 corresponding targets, 2005 disease-related targets, and 140 drug-disease intersection targets were obtained. GO biological function and KEGG pathway enrichment analyses yielded 507 biological function entries and 141 signaling pathways. KEGG pathway enrichment was mainly involved in cell proliferation, adhesion, migration, and other processes. Molecular docking results showed that the key ingredients and core targets screened had a strong binding activity, including EGFR, MAP2K1, and KDR. The combination of miltionone I and miltiodiol was relatively stable. The main biological mechanism of YQHX in the treatment of CI might play a role through the signaling pathway related to the tyrosine kinase receptor, which was also the improvement of the theory of "benefiting qi and activating blood circulation for promoting the production of blood and blood vessels".

The effect of spironolactone on the levels of GATA4 protein and hypoxia inducible factor-1α in patients receiving coronary stent implantation

Yumei Lou, Xiaoying Ge, Zhelan Zheng, Linyuan Xie, Jiangfang Lian, Wenjun Shen, Kenan Lou, Wanying Hu, Dexing Hu

2022, 31(2): 134-141. DOI: 10.5246/jcps.2022.02.011

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In the present study, we aimed to explore the protective effect of spironolactone on cardiac function in patients undergoing coronary stent implantation by determining the serum levels of GATA4 and hypoxia-inducible factor-1α (HIF-1α) proteins before and after the coronary stent implantation. A total of 134 patients undergoing coronary stent implantation in our hospital from March 2019 to March 2020 were retrospectively selected using the propensity score matching (PSM) method. Of the 134 patients, 67 patients taking spironolactone were used as a test group, and the other 67 patients without taking spironolactone were used as a control group. In all patients, the levels of serum GATA4, HIF-1α, and troponin I proteins were determined before as well as 24 h and 6 months after the coronary stent implantation. Left ventricular ejection fraction (LVEF) and left ventricular systolic global longitudinal strain (GLS) were determined before and 6 months after the coronary stent implantation. There were no significant differences in the HIF-1α level between the two groups before and 6 months after the operation, while the HIF-1α level was significantly lower in the test group compared with the control group at 24 h after the operation (P < 0.01). There were no significant differences in the GATA4 protein level between the two groups before and 24 h after the operation, while the GATA4 protein level was significantly lower in the test group compared with the control group at 6 months after the operation (P < 0.01). There was no significant difference in LVEF between the two groups before and 6 months after the operation. GLS was significantly improved at 6 months after the operation compared with that before the operation in both groups, while GLS was significantly better in the test group compared with the control group at 6 months after the operation (P < 0.01). Collectively, spironolactone could protect cardiac function probably by improving myocardial hypoxia and inhibiting myocardial remodeling.

The analysis and improvements of pharmacist-led parenteral nutrition prescription review strategies

Yingqiu Tu, Tiantian Xu, Hongwei Peng, Zhangren Chen, Xin Lai, Qing Wan, Decheng Pan, Jie Zhang

2022, 31(2): 142-152. DOI: 10.5246/jcps.2022.02.012

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To improve the efficiency and correctness of the review, we aimed to continuously improve the review strategy of parenteral nutrition (PN) prescriptions. A calculation formula (CF) and an electronic prescription reviewing system (EPRS) were designed to improve efficiency. The improvements were divided into three periods: pre-improvement, improvement period-1 (CF was used), and improvement period-2 (EPRS-CF was used). A retrospective analysis for inpatients receiving PN support from January to May 2019, June to October 2019, and June to October 2020, was conducted to evaluate the defect and efficiency of the PN prescription review. Compared with the pre-improvement period, the efficiency of the PN prescription review in the CF period was improved. In addition, in the EPRS-CF period, the efficiency and correctness of the PN prescription review were remarkably increased (P < 0.01). Moreover, through the verification of PN prescriptions in the EPRS-CF period, pharmacists improved the efficiency and correctness of the PN prescription review. Besides, the PDCA (plan-do-check-act) circulation method could help improve the PN reviewing process in the future.

Severe and lethal adverse reactions of linezolid—a summary analysis of case reports

Yanyu Pei, Jihui Hao, Wenqi Duan, Yujing Zheng, Ming Zhao, Liping Yang

2022, 31(2): 153-161. DOI: 10.5246/jcps.2022.02.013

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A systematic summary was used to evaluate case reports of adverse drug reactions (ADRs) caused by linezolid, and to explore the effects and severity on human organs or systems in the real world. The databases, such as PubMed, Embase, Cochrane Library, and CINAHL, were searched using "linezolid" + "case reports" as search terms from the establishment of each database to 31st December 2019, and the case reports on ADRs related to linezolid were collected. A total of 159 case reports were finally included in the analysis, including 189 patients. The ratio of male to female was 0.89:1, and the average age was (52.42 ± 23.43) years old. The results showed that linezolid-related severe ADRs mainly occurred in the nervous system (n = 86) and blood system (n = 44), followed by the metabolic system (n = 31) and gastrointestinal system (n = 18). Other systems reported less frequently were the skin tissue (n = 6), renal and urinary system (n = 3), cardiovascular systems (n = 2), and hepatobiliary system (n = 2). The most common linezolid-related ADRs were serotonin syndrome (n = 40), followed by optic neuropathy (n = 25) and thrombocytopenia (n = 22). The most severe ADR was lactic acidosis (n = 29), and its death rate was as high as 31.0%. In the blood system ADRs, 11 cases had underlying diseases of renal impairment, and four of them died. Moreover, 22 cases with thrombocytopenia were mainly elderly over 65 years old (n = 17), and there were also one infant and one child with thrombocytopenia. We first reported that lactic acidosis and blood system ADRs mostly occurred within 28 d, and the nervous system ADRs mostly occurred after 28 d. Besides, irreversible auditory neuropathy (n = 1), hypophosphatemia (n = 1), bradycardia (n = 1), and tooth discoloration mostly occurring in minors (n = 5) were the linezolid-related ADRs, which were not described in the instructions, related guidelines, and clinical trials of linezolid. The most severe linezolid-related ADRs was lactic acidosis that occurred within 28 d. Renal damage and special populations might be the main risk factors in the blood system ADRs. Minor linezolid-related ADRs were rare, while there were still some cases of auditory neuropathy, hypophosphatemia, bradycardia, and tooth discoloration.

The research result of Professor Liu Tao's team was selected as one of the Top 10 Domestic Medical Science and Technology News in 2021

School of Pharmaceutical Sciences, Peking University Health Science Center

2022, 31(2): 162-162.

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