Table of Content

24 December 2021, Volume 30 Issue 12

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Original articles

Redox-responsive self-assembly polymeric micelles based on mPEG-β-cyclodextrin and a camptothecin prodrug as drug release carriers

Yiben Lu, Miao Zhang, Yongjun Zheng, Xinyu Hou, Muye He, Kaiyan Lou, Feng Gao

2021, 30(12):  941-955.  DOI: 10.5246/jcps.2021.12.081

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Stimuli-responsive drug delivery systems based on polymeric micelles can achieve controlled drug release to improve the therapeutic outcome and reduce unwanted systematic toxicity and side effects of the cytotoxic drug in chemotherapy but often face challenging synthesis and purification of functionalized biocompatible polymer materials and low drug loading efficiency. In the present study, we reported a novel redox-responsive self-assembly polymeric micelle system, mPEG-β-CD/Ad-SS-CPT, to achieve high loading efficiency and selective delivery of camptothecin (CPT) in a reductive environment inside cancer cells. The host-guest supramolecular micelles utilized a simple β-CD modified PEG, mPEG-β-cyclodextrin (mPEG-β-CD), as the polymeric host with the ease of synthesis and purification. The guest prodrug Ad-SS-CPT contained the disulfide bond as the redox sensitivity group. The selective cleavage of disulfide bond and subsequent drug release in a reductive environment could potentially reduce system toxicity and improve the therapeutic outcome of CPT. In vitro studies showed that the micelles exhibited excellent cytotoxicity against HeLa cells comparable to the free drug. The host-guest polymeric micelles also showed great potentials for multi-drug co-delivery. Collectively, our current findings provided a general and convenient approach to design drug delivery systems based on stimuli-responsive polymeric micelles for disease treatment.



3,4-Dihydroxyacetophenone alleviates lipopolysaccharide-induced acute lung injury as a potential anti-inflammatory and anti-oxidative agent

Yinyan Xu, Min Zhu, Kaiheng Zhou, Taotao Song, Lili Huang

2021, 30(12):  956-968.  DOI: 10.5246/jcps.2021.12.082

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Enhanced inflammatory response and oxidative stress cause acute lung injury (ALI). Controlling inflammation and oxidation can ameliorate ALI. In the present study, we aimed to determine whether 3,4-Dihydroxyacetophenone (compound 1) could ameliorate lipopolysaccharide (LPS)-induced ALI by suppressing inflammation and oxidation. In this study, compound 1 reduced LPS-induced inflammatory cytokines and oxidative stress in RAW 264.7 cells. Moreover, compound 1 suppressed the expression of inflammatory protein p65, inhibited IkBα phosphorylation, decreased the nuclear translocation of p65, and increased the expressions of anti-oxidative protein nuclear factor erythroid 2-related factor 2 (Nrf-2) and heme oxygenase-1 (HO-1), which was reduced by LPS, in leukemia cells in mouse macrophage (RAW 264.7) cells. Furthermore, compound 1 could also ameliorate LPS-induced ALI in vivo, with a reduction of inflammatory cytokines, oxidative stress, and nuclear factor-kappa B (NF-κB) signaling pathway activation. This study emphasized the anti-inflammatory and anti-oxidative activities of compound 1, which could be a valuable therapeutic agent against ALI.



Chemical constituents of the twigs and leaves of Erythrina strica

Fengqiu Li, Dewen Bi, Xuesong Liang, Ruilong Luo, Hongdan Zhuang, Liqin Wang

2021, 30(12):  969-975.  DOI: 10.5246/jcps.2021.12.083

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A total of 15 compounds were extracted from the ethyl acetate extraction of the twigs and leaves of Erythrina strica. Based on NMR spectral data, their structures were identified as loliolide (1), phaseic acid (2), pinnatififidanoid A (3), soyasapogenol E (4), soyasapogenol B (5), 2α,3α,19α,23-tetrahydroxyurs-12-en-28-oic acid (6), 3β,22β,24-trihydroxyolean-12-en-29-oic acid (oxytrogenin) (7), (23Z)-9,19-cycloart-23-ene-3β,25-diol (8), 3,4-dihydroxybenzoic acid (9), syringaresinol (10), (E)-4-hydroxy-dodec-2-enedioic acid (11), lutein (12), ergosterol-5,8-peroxide (13), β-sitosterol (14), and daucosterol (15). Except for compounds 13–15, all the compounds were isolated from this plant for the first time. Moreover, sesquiterpenoids were isolated from Erythrina genus for the first time.



Efficacy evaluation and influencing factors analysis of combined estrogen in the treatment of labial adhesion in children

Jiale Li, Yan Yang, Zhaoqi Huang, Xiaolan Mo

2021, 30(12):  976-985.  DOI: 10.5246/jcps.2021.12.084

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In the present study, we aimed to assess the effect of combined estrogen cream on young girls’ labial adhesions, and to identify the possible factors affecting the treatment outcome. We retrospectively included 123 children with labial adhesions. Variables were collected, including treatment outcomes, conjugated estrogen usage, and dosage, whether it was combined with manual or surgical separation, whether to use erythromycin, and whether to be accompanied with vulvitis. Chi-square test, Fisher’s exact test, and t-test were used to analyze the correlation between influencing factors and treatment outcome in univariate analysis. We used logistic regression analysis to explore the key influencing factors. The use of conjugated estrogen in combination with manual or surgical separation (P = 0.001), and the degree of labial adhesions (P = 0.011) had significant effects on the final treatment outcome. The frequency of conjugated estrogen treatment, whether erythromycin was used in combination during treatment, and whether the children were accompanied by vulvitis had no significant effect on the treatment outcome (P > 0.05). After the logistic regression, we found that whether it was combined with manual or surgical separation (P = 0.000, OR = 0.078, 95% CI = 0.030–0.203), and the degree of labial adhesions in children (P = 0.003, OR = 5.324, 95% CI = 1.767–16.041) were independently related to the effect of conjugated estrogen treatment. The therapeutic effect of conjugated estrogen alone was better for mild adhesion. However, severe adhesions need to consider with manual or surgical separation in combination with conjugated estrogen treatment. It is not recommended to combine erythromycin with routine clinical treatment. Conjugated estrogen once a day can also achieve a good therapeutic effect.



Drug administration and clinical pharmacy column

Comparison of the efficacy and adherence of generic and brand-name entecavirs in chronic hepatitis B patients: a multicenter cohort study

Ying Xie, Hanqiu Zhan, Xiaohong Zhu, Yuan Li, Ruyi Tian, Jing Zhang, Shanshan Chen, Yanling Zhao

2021, 30(12):  986-993.  DOI: 10.5246/jcps.2021.12.085

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In the present study, we aimed to compare the efficacy and adherence of Runzhong^? (generic drug, Chiatai Tianqing, Nanjing) and Baraclude^? (branded drug, Bristol-Myers Squibb) in patients with chronic hepatitis B. We collected patient data from three hospitals within 48 weeks and compared the two groups by using the propensity-score matching method. A total of 4889 patients were enrolled in this study; 503 initiated a brand-name drug, and 4386 received a generic drug. There was no significant difference in the rates of CVR (complete virologic response) and VB (virologic breakthrough) between the Runzhong^? group and Baraclude^? group at 24 and 48 weeks. Similar results for HBeAg loss, medication possession ratio (MPR), and biological response were obtained. Age, gender (HR 0.909 (0.842–0.981)), normal baseline ALT rate (HR 0.789 (0.731–0.851)), HBeAg-positive rate, and baseline undetectable HBV DNA rate (HR 0.306 (0.234–0.399)) were independent factors for achieving CVR.



Antimicrobial stewardship program in China’s tertiary hospitals in 2018: a nationwide cross-sectional online survey

Yue Zhou, Haishaerjiang Wushouer, Xi Zhang, Jiajia Feng, Likai Lin, Bo Zheng, Xiaodong Guan, Luwen Shi

2021, 30(12):  994-1007.  DOI: 10.5246/jcps.2021.12.086

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In the present study, we aimed to assess the development of the antimicrobial stewardship (AMS) program in China’s tertiary hospitals to identify the potential challenges for the AMS program and provide references and benchmarks for strategic policymaking. A nationwide cross-sectional study was conducted online by sending questionnaires to tertiary hospitals under China Antimicrobial Resistance Surveillance System (CARSS). The questionnaire included 5 sections regarding structure, technical support, antimicrobial use management, antimicrobial use surveillance, and education. Descriptive statistics were used for data analysis. Of the 1044 tertiary hospitals under CARSS, 13.4% (140) hospitals participated in the study. Among them, 99.3% (139/140) set up the AMS program. The hospital president (82.1%, 115/140) and medical service department (59.3%, 83/140) were responsible for AMS outcomes in most hospitals. Structured antimicrobial formulary restriction management was adopted by 99.3% (139/140) hospitals. Infectious disease department, infection control department, and microbiological laboratories were established in 87.1% (122/140), 99.3% (139/140) and 100% (140/140) hospitals, respectively. Up to 85.6% (124/140) hospitals applied clinical pathways, and 33.6% (47/140) hospitals implemented hospital-specific guidelines for infectious diseases. Outpatient prescription auditing, inpatient prescription auditing, and prophylactic antimicrobial prescription auditing of aseptic operation were performed in 99.3% (139/140), 98.6% (138/140) and 95.7% (134/140) hospitals, respectively. Up to 97.1% (136/140) hospitals participated in antimicrobial use surveillance network, and 99.3% (139/140) hospitals established the specialized management of carbapenem and tigecycline. Staff education and public education were provided with various ways and frequencies in 100% (140/140) and 90.0% (126/140) hospitals, respectively. AMS programs in China’s tertiary hospitals were primarily headed by hospital presidents and involved collaboration among various disciplines and administrative departments. More efforts should be put to further promote and strengthen the development of hospital-specific guidelines and the establishment of a progress and outcome evaluation system.



News

The group of Professor Suwei Dong have made progress in the study of the mechanism of O-glycosylation modification regulating the aggregation of Amyloid-β

State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University Health Science Center

2021, 30(12):  1008-1009. 

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The group of Professor Suwei Dong have made progress in the study of the mechanism of O-glycosylation modification regulating the aggregation of Amyloid-β.



Others

Contents of Volume 30

Journal of Chinese Pharmaceutical Sciences

2021, 30(12):  1010-1021. 

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Keywords Index of Volume 30

Journal of Chinese Pharmaceutical Sciences

2021, 30(12):  1022-1025. 

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Author Index of Volume 30

Journal of Chinese Pharmaceutical Sciences

2021, 30(12):  1026-1029. 

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Acknowledgements

Journal of Chinese Pharmaceutical Sciences

2021, 30(12):  1030-1030. 

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