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    The antidepressive effect of the complex consisting of Radix Pseudostellariae, Radix Pueraria and Herba Epimedii: the involvement of NRSF/NRSE-TPH2 signaling
    Xuan Yu, Xinpei Wang, Fan Lei, Yugang Wang, Wei Wang, Yi Ding, Dongming Xing, Zhiyi Yuan, Hong Sun, Lijun Du
    Journal of Chinese Pharmaceutical Sciences    2021, 30 (1): 27-41.   DOI: 10.5246/jcps.2021.01.003
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    Depression is a psychological disease with no particularly effective therapy currently available. In the present study, we aimed to examine the antidepressive activity of a pharmaceutical Chinese medicine called TaiZi (TZ) capsule, consisting of total polysaccharides of Radix Pseudostellariae and total flavonoids of both Radix Pueraria and Herba Epimedii. A tail suspension test and forced swimming test were performed to assess the effect of TZ in vivo. A plasmid of TPH2 (tryptophan hydroxylase-2) was constructed to determine the exact target of TZ in vitro. In addition, mRNA expression was detected using a real-time PCR assay, and the protein expression was investigated using a Western blotting analysis. The results showed that TZ had an anti-depression effect in mouse and rat models with increased serotonin in the brain, and in the upregulation of mRNA and protein expression of TPH2 in the brain simultaneously by inhibition of NRSF (neuron restrictive silencer factor) expression because NRSF could bind to NRSE (neuron restrictive silencer element) to repress TPH2 transcription during the depression conditions. Icariin could bind to NRSE directly and block NRSF protein toward to NRSE for TPH2 inhibition. Therefore, we concluded that TZ had potential antidepressive effects because it could ameliorat the depression-like behavior in the animals, and the underlying mechanism of the effect was involved in NRSF/NRSE-TPH2 signaling. Icariin was identified as the active component of TZ. This study provided a new perspective for the development of antidepression drugs (Chinese medicines) based on NRSF/NRSE -TPH2 signaling.

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    Significance of neutralizing antibodies in COVID-19 therapy: progress and prospect
    Zeqi Zhou, Xiangbin Wang, Xiqing Zhang, Yuan Zhang, Yankai Fu, Zhixian Wang, Yan Su, He Wang, Meng Xiao, Changxiao Liu
    Journal of Chinese Pharmaceutical Sciences    2021, 30 (2): 87-106.   DOI: 10.5246/jcps.2021.02.008
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    SARS-CoV-2 infection is a serious threat to human life and health all over the world, and COVID-19 is a global epidemic caused by SARS-CoV-2 infection. SARS-CoV-2 is highly infectious, strange and variable. Therefore, the treatment of COVID-19 must be urgent and targeted. However, vaccines and currently used drugs generally do not have the above-mentioned characteristics. Although convalescent plasma of COVID-19 has shown a clinical application value in the emergency treatment of critical patients, it shows great limitations. All human recombinant multivalent neutralizing nano-antibodies may meet the deficiency of COVID-19 therapy. Gene engineering technologies have been used to develop specific neutralizing antibody (nAB) drugs for the treatment of COVID-19 worldwide. Some of the candidate nAB drugs have been entered the clinical trials and can be used for the therapy of COVID-19 shortly. In the present review, we studied and analyzed nABs for the treatment of COVID-19 and the progress and prospect from the following five aspects: 1) The biological and clinical characteristics of SARS-CoV-2 infection; 2) The feasibility of plasma therapy for convalescents with COVID-19; 3) The technical routes of developing nAb drugs; 4) The current status of developing global COVID-19 antibodies; 5) The difficulties and clinical use.

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    Plant pharmacophylogeny: past, present and future
    Dacheng Hao, Peigen Xiao
    Journal of Chinese Pharmaceutical Sciences    2020, 29 (12): 831-854.   DOI: 10.5246/jcps.2020.12.075
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    The concept of "pharmacophylogeny" was proposed by Peigen Xiao in the 1980s based on long-term studies of Chinese researchers since ancient times and especially the 1950s. The complicated relationships and connectivity between kinship of medicinal plants, their chemical profiles and therapeutic utilities are consistent goals of pharmacophylogeny studies, which benefit innovative drug R&D. In the present work, we reviewed the origin and a brief history of research in this field, as well as the status quo and recent progress of pharmacophylogeny. The concept "pharmacophylogenomics" is put forward to represent the expanding utility of pharmacophylogeny in botanical drug R&D. Pharmacophylogeny and pharmacophylogenomics are the synthesis of multiple disciplines, such as chemotaxonomy, plant morphology, plant biochemistry/molecular biology and omics, etc. Medicinal plants within the same phylogenetic groups may have the same or similar therapeutic compounds/effects, thus forming the core of pharmacophylogeny, which is the scientific law summed up from practice and applied to practice after refining and sublimation. In the past, pharmacophylogeny plays a big role in looking for alternative resources of imported drugs in China. At present, it continues to play an active role in expanding medicinal plant resources, quality control/identification of herbal medicines, as well as predicting the chemical constituents or active ingredients of herbal medicine and the identification and determination of chemical constituents. In the ongoing future, it will play a bigger role in the search for new drugs, sorting out, summarizing, and improving herbal medicine experiences, thus boosting the sustainable conservation and utilization of traditional/natural?medicinal resources.

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    Preclinical efficacy of a novel cyclin-dependent kinase 9 inhibitor, QHRD107 against acute myeloid leukemia
    Yan Zhou, Hengwen Song, Zhichao Shao, Bomin Yin, Ximei Fu, Dianyou Xie, Lijun Wei
    Journal of Chinese Pharmaceutical Sciences    2021, 30 (2): 146-156.   DOI: 10.5246/jcps.2021.02.012
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    QHRD107 is a specific inhibitor of cyclin-dependent kinase 9 (CDK9). It is a highly potent antiproliferative agent against leukemia cells in vitro. Oral administration of QHRD107 to mice bearing acute myeloid leukemia tumors markedly inhibited tumor growth. In Molm-13 orthotopic model, QHRD107 resulted in remarkable prolongation of animal life span. After single oral administration of QHRD107 to Molm-13 xenograft model, QHRD107 was quickly absorbed and distributed to tumor with high concentration within 1 h. Tumor half-life time (T1/2) was three times longer compared with that of plasma. Under the high exposure of QHRD107 in tumor tissue, fast down-regulation of anti-apoptotic protein Mcl-1 mRNA was noted. Reduction of Ki-67 staining in tumor tissue further demonstrated the apoptosis of tumor cells. Therefore, the results provided evidence that QHRD107 at therapeutic dose had significant antitumor activity against AML cell lines.

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    Integrated combination delivery of IDO inhibitor and paclitaxel for cancer treatment
    Dakuan Wang, Bo Peng, Mengmeng Qin, Minghui Li, Ge Song, Bing He, Hua Zhang, Wenbing Dai, Qiang Zhang, Xiangbao Meng, Huan Meng, Xueqing Wang
    Journal of Chinese Pharmaceutical Sciences    2021, 30 (1): 1-16.   DOI: 10.5246/jcps.2021.01.001
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    In order to realize the combination of chemotherapy and immunotherapy, a reduction-responsive paclitaxel (PTX) prodrug PEG-SS-PTX was synthesized and used as a carrier to encapsulate IDO inhibitor CY-1-4 for preparing PEG-SS-PTX/CY-1-4 NPs. PEG-SS-PTX/CY-1-4 NPs were evaluated by cytotoxicity, immunogenic cell death (ICD) induction ability and anti-tumor efficacy. Dynamic light scattering (DLS) results showed that the size of PEG-SS-PTX/CY-1-4 NPs was about 149 nm. In vitro experiments indicated that its cytotoxicity was in a concentration-dependent manner, and it induced the ICD of B16-F10 cells. In vivo studies in melanoma mouse model indicated that PEG-SS-PTX/CY-1-4 NPs significantly inhibited the tumor growth and reduced the expression of IDO in tumor tissues. Moreover, it increased the rate of CD8+ T cells in the spleen. In summary, PEG-SS-PTX/CY-1-4 NPs achieved good anti-tumor effects and reduced the dose of chemotherapy drugs, which was a safe and effective combined delivery system.

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    The regulatory effects of mulberry leaf and its extract on intestinal function
    Yawen Wang, Xiaofeng Duan, Xiaoxiao Cheng, Miaoxin Zhang, Li Li, Ding Zhao
    Journal of Chinese Pharmaceutical Sciences    2020, 29 (11): 780-792.   DOI: 10.5246/jcps.2020.11.071
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    Since ancient times, mulberry leaf has a prominent intestinal regulatory effect, and the close relationship between intestinal diseases and other diseases has attracted more and more attention. This article reviewed the relevant articles on the mulberry leaf in recent years and summarized the research progress of mulberry leaf’s biological activities and their effects on human intestinal regulation and the corresponding mechanisms. Multiple components in the mulberry leaf can individually or synergistically affect the human intestine, directly and indirectly promote the digestion, absorption, and transport function of the small intestine, adjust the balance of the flora, enhance the barrier function of the intestinal mucosa, improve the immunity of the part, and facilitate the intestine recovery from illness.
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    A PK/PD model of saxagliptin: to simulate its pharmacokinetics and pharmacodynamics in healthy adults and patients with impaired hepatic function
    Lu Shi, Feng Miao, Guopeng Wang, Wenyan Sun, Yang Liu
    Journal of Chinese Pharmaceutical Sciences    2021, 30 (2): 119-132.   DOI: 10.5246/jcps.2021.02.010
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    In this study, we aimed to develop and evaluate a whole-body physiologically based pharmacokinetic (WB-PBPK)/pharmacodynamic (PD) model for saxagliptin, simulate its pharmacokinetic and pharmacodynamic properties in healthy adults and patients with hepatic function impairment, and provide a new method for the research to the clinical pharmacy of special patients. Based on the drug-specific properties, such as logD, plasma protein binding collected by the published literature, the WB-PBPK model and the PD model were established. After comparing the simulated concentration-time profiles and the pharmacokinetic parameters with data in healthy adults from oral and intravenous clinical investigation, the WB-PBPK model could be optimized. After comparing the simulated DPP-4 inhibition profile with the observed pharmacodynamic in healthy subjects, the PD model could be optimized. The PK/PD model was utilized to predict the mean and variability of the pharmacokinetic and pharmacodynamic profiles in subjects with different hepatic impairment. All of the predicted pharmacokinetic curves were comparable to the observed curves both in healthy subjects and hepatic impairment subjects (Cmax and AUC were less than 1.3-fold). The predicted pharmacodynamic curves were comparable to the observed ones in different oral dosage after optimization, and pharmacodynamics of saxagliptin in hepatic impairment subjects were predicted successfully. The WB-PBPK/PD model can accurately simulate the pharmacokinetics and pharmacodynamics of saxagliptin in normal adults and different hepatic impaired patients.

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    Pharmacodynamic comparison of two different source plants of Murrayae Folium et Cacumen
    Mengqiu Lu, Haizhen Liang, Pengfei Tu, Yong Jiang
    Journal of Chinese Pharmaceutical Sciences    2021, 30 (1): 49-57.   DOI: 10.5246/jcps.2021.01.005
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    A comparison of the pharmacodynamic effects of two source plants of Murrayae Folium et Cacumen (MFC), Murraya exotica L. and Murraya paniculata (L.) Jack, was performed in order to supply reference for its multi-source rationality and interchangeability in clinical practice. According to the traditional efficacy of MFC, the effects of promoting Qi, relieving pain, promoting blood circulation and removing blood stasis were systematically evaluated by the models of writhing response in mice, foot swelling in rats, gastric emptying and small intestine propulsion in mice, and acute blood stasis in rats, respectively. The results showed that both M. exotica and M. paniculata could significantly inhibit the writhing reaction induced by acetic acid in mice and the paw swelling induced by carrageenan in rats, reduce IL-6, TNF-α and PGE2 levels in plasma of paw-swelling rats and increase gastric empty rate and intestinal propulsive rate. The above-mentioned effects were dose-dependent, and there was no significant difference between M. exotica and M. paniculata at the same doses. Therefore, M. exotica and M. paniculata had the similar anti-inflammatory, analgesic and gastrointestinal motility promotion effects, which provided a support for the pharmacodynamic equivalence of the multi-source plants of MFC.

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    Cost-effectiveness analysis of tyrosine kinase inhibitors (erlotinib, gefitinib, afatinib and osimertinib) as first-line therapy for epidermal growth factor receptor-mutated advanced non-small cell lung cancer
    Shaohong Luo, Liangliang Dong, Yiyuan Li, Dan Xu, Min Chen
    Journal of Chinese Pharmaceutical Sciences    2021, 30 (3): 253-263.   DOI: 10.5246/jcps.2021.03.021
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    Gefitinib, erlotinib, afatinib and osimertinib have been recommended as the first-line treatment for epidermal growth factor receptor (EGFR)-mutated advanced non-small cell lung cancer (NSCLC), whereas no studies have compared the cost-effectiveness of these four tyrosine kinase inhibitors (TKIs) simultaneously in China. In the present study, we aimed to estimate the cost-effectiveness of erlotinib, gefitinib, afatinib and osimertinib for untreated EGFR-mutated advanced NSCLC. A Markov model was constructed to compare the 10-year impact of four TKIs for patients with treatment-naive EGFR-mutated advanced NSCLC from the perspective of the Chinese medical system. Clinical data and utility values were derived from published literature, and costs were obtained from Chinese official websites. The primary output indicator was the incremental cost-effectiveness ratio (ICER). Sensitivity analyses were performed to test the robustness of the model. We found that afatinib was estimated to spend the lowest cost with minimum life-years (LYs), while osimertinib was the most expensive regimen with maximum LYs. The ICER of gefitinib versus afatinib was \$732/quality-adjusted life-year (QALY), which was less than the willingness-to-pay (WTP) of \$29 382/QALY. Compared with gefitinib, erlotinib yielded a higher cost and a shorter lifetime, hence it was identified as a dominated strategy. Then, osimertinib was compared to gefitinib, which produced an ICER of \$71 330/QALY, exceeding the WTP. It suggested that gefitinib was the most cost-effective regimen as the first-line treatment for EGFR-mutated advanced NSCLC. Decreasing the osimertinib price or increasing the WTP threshold to \$68 558/QALY might enhance the favorability of the outcome, by which osimertinib might become more cost-effective. One-way sensitivity analysis manifested that the model was robust.

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    Comparative authentication of crude drugs from subgenus Asarum species in China based on microscopic features
    Yaoli Li, Zhong Liu, Jie Yu, Mingying Shang, Baibo Xie, Feng Xu, Shao-Qing Cai
    Journal of Chinese Pharmaceutical Sciences    2020, 29 (12): 855-867.   DOI: 10.5246/jcps.2020.12.076
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    According to the Chinese Pharmacopoeia, the Chinese medicinal material (Asari Radix et Rhizoma) Xixin is derived from the species Asarum heterotropoides var. mandshuricum, A. sieboldii, and A. sieboldii var. seoulense. However, many species of the genus Asarum are labeled as "Xixin", "Tu-Xixin" or "Nan-Xixin" for sale in producing areas. To distinguish Chinese Asarum species and to ensure their safety and efficacy, we examined the microscopic characteristics of subg. Asarum plants in China (including subg. Asarum plants in the classification system of Flora Reipublicae Popularis Sinicae and the later published Asarum yunnanense) using a hand microtome and a microscopic digital imaging system based on our previous research. Microscopic features of the blades, petioles, and roots of A. yunnanense were investigated for the first time. Moreover, we compared nine species and one variety of the subg. Asarum (i.e. , A. yunnanense, A. caudigerellum, A. himalaicum, A. pulchellum, A. debile, A. caulescens, A. renicordatum, A. caudigerum, A. caudigerum var. cardiophyllum and A. geophilum) in China based on microscopic characteristics of the blades. Several parameters, such as morphological characteristics and distribution of hairs on both upper and lower leaf epidermises; morphological characteristics of hair cells; anticlinal walls of lower epidermal cells; size relationship between outer periclinal walls and cavity outlines of oil cells on lower leaf epidermis; presence or absence of the irregular cells containing red to brown substances among mesophyll cells; and the diameter of the largest vessels in midribs of the blades, were used for discrimination among species. To the best of our knowledge, we provided the first identification key for the 10 taxa based on blade microscopic characteristics that could be used to distinguish these taxa. Based on the key, 23 commercial samples collected from seven provinces of China were authenticated as whole dried herbs of A. himalaicum, A. caudigerellum, A. caudigerum, A. pulchellum and A. caulescens. These findings indicated that microscopic approach and related techniques were convenient and feasible and could be used for the authentication of crude drugs from Chinese subg. Asarum species.

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    A biography of Academician Zhicen Lou
    Journal of Chinese Pharmaceutical Sciences
    Journal of Chinese Pharmaceutical Sciences    2020, 29 (12): 829-831.  
    Abstract187)      PDF (1247KB)(31)       Save
    A biography of Academician Zhicen Lou.
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    Pharmacokinetics, pharmacodynamics and safety of a single-dose long-acting Risperidone injection in Chinese patients with schizophrenia
    Xiaojiao Li, Shuxin Luan, Hong Zhang, Hongquan Wan, Hong Chen, Chengjiao Liu, Chang Liu, Yanhua Ding
    Journal of Chinese Pharmaceutical Sciences    2021, 30 (3): 206-217.   DOI: 10.5246/jcps.2021.03.016
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    In the present study, we aimed to determine the pharmacokinetics (PK), pharmacodynamics (PD), adverse events (AEs), and their relationships in Chinese patients with schizophrenia after a single dose of long-acting risperidone. Schizophrenic patients (six females and seven males) were enrolled in this study. Serial blood samples were collected after drug administration during 63 d, and the drug concentrations were analyzed by LC-MS/MS. Safety and tolerance were evaluated by monitoring the AEs, changes in clinical laboratory results, 12-lead ECG, vital signs, physical examination, and injection-site reactions. The extrapyramidal symptoms were evaluated using the ESRS. Efficacy was evaluated by the PANSS and BPRS. Twelve out of the 13 participants completed the trial. There were few clinically meaningful changes in mean clinical laboratory values, vital signs, or ECG parameters, except for the prolactin level and body weight. There were no serious AEs, and those observed were reversible. Significant clinical improvements in PANSS and PANSS-derived BPRS total scores were observed. The mean (standard deviation, coefficient of variation) values for these PK parameters were as follows: Cmax, 8.954 (8.059, 90.0%) ng/mL; area under the curve AUC0–t, 2453 (1156, 47.1%) ng?h/mL; AUC0–∞, 2472 (1160, 46.9%) ng?h/mL; tmax, 830.0 (min: 744.0, max: 984.0, 11.8%) h; and t1/2, 68.56 (10.77, 15.7%) h. The PK characteristics of long-acting risperidone showed a high level of inter-individual variation, while there were no clear correlations between PK, efficacy and AEs among the patients in the present study.

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    Phytochemistry, biological properties and quality control of Chuanxiong Rhizoma: a review
    Jinhui Shi, Ruiyue Li, Siyu Yang, Hongmei Zhang
    Journal of Chinese Pharmaceutical Sciences    2020, 29 (11): 755-779.   DOI: 10.5246/jcps.2020.11.070
    Abstract186)   HTML60)    PDF (1995KB)(95)       Save
    Chuanxiong Rhizoma is a widely used Chinese herbal medicine in the past 2000 years. Chuanxiong Rhizoma is composed of volatile oils, phthalide lactones, phenolic acids, polysaccharides and other compounds. To date, more than 149 compounds in Chuanxiong Rhizoma have been isolated and identified, and some of them have been reported to possess promising biological properties on cardiovascular and central nervous system disorders besides their anti-cancer and antioxidant effects. Modulation of inflammatory mediators and apoptotic factors are believed to contribute to its bioactivities. Analytical methods, such as HPLC, GC and UPLC, are employed for qualitative evaluation of Chuanxiong Rhizoma. In this work, harvest period, growing habitat, processing method and storage, which can affect the quality of Chuanxiong Rhizoma, were also discussed. Comprehensive quality control methods should be developed to ensure the safety, quality and efficacy use of Chuanxiong Rhizoma. Herein, we collected and analyzed the literature of Chuanxiong Rhizoma published on CNKI, ScienceDirect, Springer link, Wiley and PubMed in past two decades, and up-t o-date information of Chuanxiong Rhizoma was provided in this paper. We suggested ligustilide, bu tylidenephthalide and total senkyunolides as the chemical markers to evaluate the quality of Chuanxiong Rhizoma. Additionally, the influences of soil conditions and processing methods on Chuanxiong Rhizoma as future research perspectives should also be further assessed.
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    Protective effect of hydroxysafflor yellow A on Parkinson cell model and its network pharmacology analysis
    Shuang Li, Chunyan Guo, Shuangshuang Li, Sihan You, Xiujuan Yu
    Journal of Chinese Pharmaceutical Sciences    2020, 29 (12): 880-895.   DOI: 10.5246/jcps.2020.12.078
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    As an effective component of safflower, hydroxysafflor yellow A (HSYA) has the effect of promoting blood circulation, removing blood stasis, and relieving pain, and it has a certain effect on blood stasis and wind-induced Parkinson’s disease (PD). However, the current research mostly involves a single intervention mechanism, which is not conducive to the clinical transformation of this type of drugs. In the present study, rotenone was used to construct a PD cell model, and the protective effect of HSYA on the PD cell model was evaluated by cell viability and mitochondrial membrane potential. TTD database was used to query PD-related therapeutic targets, Swiss Target Prediction database to query HSYA-related targets, STRING database was used to search the gene interaction relationship of common targets, and ClueGO pathway was adopted to enrich and analyze common targets and their interaction targets, as well as to explore the comprehensive intervention mechanism. The results showed that rotenone could successfully establish the PD cell model, and HSYA had significant protective effect on PD cell model. Through the network pharmacological analysis, 36 PD-related therapeutic targets and 88 HSYA-related targets were queried. The common targets of PD and HSYA were FKBP1A, HTR1A, SLC6A4 and SLC6A3. To enrich four common targets and their interaction targets through REACTOME pathway, eight cell signal pathways were obtained, and six cell biological processes were obtained through biological process pathway enrichment.

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    Tolvaptan, an FDA-approved drug, inhibits Zika virus infection both in vitro and in vivo
    Xiuxiu Chen, Ronghua Luo, Zhaiwen Yao, Changbo Zheng, Qiuju Tang, Wei Pang, Fang Wang, Liumeng Yang, Sidong Xiong, Yongtang Zheng
    Journal of Chinese Pharmaceutical Sciences    2021, 30 (3): 218-229.   DOI: 10.5246/jcps.2021.03.017
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    As a previously neglected member of flavivirus, Zika virus (ZIKV) has recently emerged and caused a global health concern because of its link to microcephaly and other congenital defects. Currently, no anti-ZIKV vaccine or therapy is commercially available. In this drug-screening study, tolvaptan, an FDA-approved drug, was identified to possess the activity against ZIKV strains of Asian lineage with low cytotoxicity using plaque and MTT assays. The anti-ZIKV activity of tolvaptan was also demonstrated using virus yield reduction assay and Western blotting analysis. Time-of-drug-addition assay showed that tolvaptan exerted its anti-ZIKV activity between 6 and 14 h post-ZIKV inoculation, concurrent with the post-entry events of ZIKV life cycle. Tolvaptan also exhibited inhibitory effects on ZIKV strains of African lineage, indicating that its anti-ZIKV activity was not strain dependent. Notably, tolvaptan could also reduce ZIKV-induced mortality in infected mice. Overall, these results suggested that tolvaptan was a potential therapeutic candidate against ZIKV that is worth further evaluation.

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    The group of Professor Tao Liu used a supramolecular recognition strategy to achieve reversible regulation of protein
    State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University Health Science Center
    Journal of Chinese Pharmaceutical Sciences    2021, 30 (2): 183-184.  
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    The group of Professor Tao Liu used a supramolecular recognition  strategy to achieve reversible regulation of protein.
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    Fabrication of deoxycholic acid-modified polymeric micelles and their transmembrane transport
    Qi Liu, Leqi Wang, Xinping Hu, Chuhang Zhou, Yingwei Tang, Yining Ma, Xiaoxiao Wang, Yan Liu
    Journal of Chinese Pharmaceutical Sciences    2021, 30 (1): 17-26.   DOI: 10.5246/jcps.2021.01.002
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    Oral administration is the best way for the most patients due to the good compliance, and intestinal epithelium is the main barrier of oral drug absorption. In order to overcome the small intestine epithelial barrier to orally deliver water-insoluble drugs, deoxycholic acid (DA), a substrate of the intestinal bile acid transporters, conjugated poly(2-ethyl-2-oxazoline)-poly(D,L-lactide) (DA-PEOz-PLA) was designed and synthesized, and deoxycholic acid-modified polymeric micelles composed of DA-PEOz-PLA and mPEG-PLA were fabricated to encapsulate model drug coumarin 6 (C6) based on intestinal bile acid pathway. The structure of DA-PEOz-PLA was confirmed using 1H NMR and TLC, and the molecular weight measured by GPC was 10 034 g/mol with a PDI of 1.51. The C6-loaded polymeric micelles with drug loading content of 0.085% were characterized to have 40.11 nm in diameter and uniform spherical morphology observed by TEM. Furthermore, the deoxycholic acid-modified polymeric micelles were demonstrated to further enhance the transmembrane transport efficiency. The mechanic study evidenced that anchorage of deoxycholic acid onto the micelles surface enriched their transcellular transport pathway. Therefore, the designed deoxycholic acid-modified polymeric micelles might have a promising potential for oral delivery of water-insoluble drugs.

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    Intestinal anti-inflammatory effects of main components of the fruits of Euodia rutaecarpa in a co-culture model of the human colorectal adenocarcinoma cells and RAW264.7 macrophages
    Shi Wang, Lu Liu, Youbo Zhang, Wei Xu, Xiuwei Yang
    Journal of Chinese Pharmaceutical Sciences    2020, 29 (12): 868-879.   DOI: 10.5246/jcps.2020.12.077
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    Alkaloids are the main active constituents of the nearly ripe fruits of Euodia rutaecarpa (Juss.) Benth., which possesses antitumor, anti-inflammatory, analgesic and antimicrobial activities. In this study, we aimed to assess the potential anti-inflammatory effects of six main components, evodiamine, rutaecarpine, dehydroevodiamine, evocarpine, dihydroevocarpine and 1-methyl-2-undecyl-4-(1H)-quinolone, in the nearly ripe fruits of E. rutaecarpa. In the co-culture system consisting of the human colorectal adenocarcinoma (Caco-2) cells and RAW264.7 macrophages, inflammation was induced in RAW264.7 cells with 2 μg/mL lipopolysaccharide. The results indicated that evodiamine, rutaecarpine, and dehydroevodiamine significantly down-regulated the mRNA expressions of pro-inflammatory cytokines (Il-6, Il-1β and Tnf-α) and inflammatory mediators, such as cyclooxygenase-2 (Cox-2) and inducible nitric oxide synthase (iNos). Besides, the drug administration group showed a higher transepithelial electrical resistance and a lower tight junction permeability compared with the model group. Taken together, the tested compounds possessed anti-inflammatory effects. Our findings laid the foundation for further research on the anti-inflammatory mechanism of the nearly ripe fruits of E. rutaecarpa.

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    Secondary metabolites from a deep-sea-derived Aspergillus versicolor F77
    Ying Kang, Chanjuan Zhang, He Zhang, Dong Liu
    Journal of Chinese Pharmaceutical Sciences    2021, 30 (1): 42-48.   DOI: 10.5246/jcps.2021.01.004
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    Chemical examination of fermentation products of a deep-sea-derived fungus Aspergillus versicolor F77 led to the isolation of two new compounds acetyl-sydonol (1) and 2-hydroxydiorcinol D (2), a new natural product 1-(2,4-dimethoxyphenyl)-1,2-dihydro-3H-pyrazol-3-one (3), together with four known compounds sydonol (4), (S)-sydonic acid (5), aspergillusene A (6) and diorcinol D (7). Their structures were determined through the extensive spectroscopic analysis and comparison with the reported data in literature. Compound 6 showed moderate NF-κB inhibitory activity.

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    Camrelizumab (SHR-1210), a humanized anti-PD-1 IgG4 mAb, exhibits superior anti-tumor activity and a favorable safety profile in preclinical studies
    Xing Sun, Changyong Yang, Kan Lin, Caihong Zhou, Chen Liao, Limin Zhang, Xinsheng Jin, Langyong Mao, Hua Ying, Weikang Tao, Lianshan Zhang
    Journal of Chinese Pharmaceutical Sciences    2021, 30 (5): 393-408.   DOI: 10.5246/jcps.2021.05.031
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    Camrelizumab is a humanized monoclonal antibody (mAb) against human PD-1. It demonstrated a single digit nanomolar binding affinity to human and cynomolgus monkey PD-1, but no cross-reactivity to murine PD-1. It exhibited potent PD-1/PD-L1 blocking activity as well as the T cell activation in vitro. The distinct binding sites of cameralizumab were perfectly overlapped with the PD-L1 binding sites, which supported its excellent ability in blocking PD-1/PD-L1 interaction. It also significantly inhibited the growth of murine MC-38 and B16F10 cell in humanized PD-1 transgenic mice with a superior inhibitory effect compared with the other marketed anti-PD-1 antibodies. Furthermore, camrelizumab also displayed a favorable pharmacokinetic (PK) and safety profile in cynomolgus monkeys. Besides, we showed that camrelizumab only bound to VEGFR2 with a very low affinity and did not activate VEGF pathways even at very high doses. Collectively, we provided evidence that cameralizumab was an ideal therapeutic candidate for cancer treatment, encouraging further evaluation of its efficacy/safety in the clinical setting.

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    Riboflavin-modified lipo-polyplexes co-delivering CXCR4 siRNA and doxorubicin for treatment of highly metastatic cancer
    Kaisen Li, Rudong Wang, Yiwei Peng, Dawen Dong, Xianrong Qi
    Journal of Chinese Pharmaceutical Sciences    2021, 30 (3): 189-205.   DOI: 10.5246/jcps.2021.03.015
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    SDF-1/CXCR4 has been recognized as one of the most relevant chemokine signaling pathways to cancer metastasis, and siRNA targeting CXCR4 may provide potential improvements to treat those highly metastatic cancers, especially when combined with chemotherapy. In the present study, we constructed riboflavin-modified lipo-polyplexes to co-deliver CXCR4 siRNA and doxorubicin for cancer therapy. Doxorubicin was covalently conjugated to polyethyleneimine (PEI) with acid-cleavable hydrazine bond, and the obtained acid-sensitive conjugate was efficiently condensed with siRNA to form polyplexes, which were further coated with riboflavin-tailed lipid-membrane to prepare the lipo-polyplexes conveniently. Utilizing the fact that tumor cells overexpress riboflavin receptors, the riboflavin modification effectively enhanced uptake of lipo-polyplexes by tumor cells in a receptor-mediated manner. The riboflavin-modified lipo-polyplexes co-delivering CXCR4 siRNA and doxorubicin effectively decreased viability and invasiveness of tumor cells in vitro, and inhibited primary tumor growth and tumor metastasis in vivo.

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    Quality evaluation of Polyporus umbellatus based on HPLC specific chromatogram and fingerprint analysis
    Weijuan Jia, Shizhong Chen, Jianhua Sun, Zongli Bai, Yazhuo Huang, Yuankuan Zhang, Hong Wang
    Journal of Chinese Pharmaceutical Sciences    2020, 29 (12): 896-907.   DOI: 10.5246/jcps.2020.12.079
    Abstract148)   HTML7)    PDF (3377KB)(74)       Save

    To evaluate the quality of Polyporus umbellatus, we established a simple, repeatable and reliable method based on high performance liquid chromatography (HPLC) for specific chromatogram and fingerprint analysis, which was applied to analyze samples of medicinal materials and decoction pieces collected from different regions. Finally, ten characteristic peaks were designated in the specific chromatograms and applied to the authenticate identification of P. umbellatus samples. Nine common peaks were designated in the fingerprints, and then the similarities between 32 batches of samples were calculated. Among them, eight compounds were identified by HPLC-APCI-IT-TOF-MSn, four of which were identified in specific chromatograms and four in fingerprints. In the present study, we, for the first time, combined HPLC specific chromatograms and fingerprints for the species identification and quality evaluation of P. umbellatus. Collectively, our findings provided a new method for establishing a comprehensive quality standard of P. umbellatus.

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    Identification of major compounds of total flavonoids from Smilax china and evaluation of anti-inflammatory effect on phenol mucilage-induced pelvic inflammation in rats
    Jiaqian Chen, Chen Jin, Bolun Xu, Huang Zhan, Rongrong Fu, Fengqin Li, Huilian Huang
    Journal of Chinese Pharmaceutical Sciences    2021, 30 (2): 157-168.   DOI: 10.5246/jcps.2021.02.013
    Abstract147)   HTML582)    PDF (1747KB)(19)       Save

    As a Chinese medicinal plant, Smilax china is traditionally used in the treatment of pelvic inflammatory disease (PID). Flavonoids have been identified as the anti-inflammatory bioactive fraction. However, the high content of total flavonoids has not been extracted from S. china. The therapeutic effects and mechanisms of total flavonoids are still unknown. In the present study, we aimed to obtain the effective parts of flavonoids in S. china, and elucidate the mechanism of action on PID. The anti-inflammatory effect was evaluated on phenol mucilage-induced pelvic inflammation in rats. This was the first time that total flavonoids in high concentration (up to 55.6%) were obtained in S. china. A total of 15 compounds were separated and identified by NMR, and the total flavonoids were detected with HPLC. TFSC caused a reduction in serum levels of IL-6 and IL-1β. These results suggested that TFSC had a significant anti-PID effect, probably due to inhibition of the inflammatory reaction.

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    Integrating ancient and modern approaches to traditional Chinese medicinal authentication
    Zhongzhen Zhao, Hubiao Chen, Ping Guo, Zhitao Liang, Eric Brand, Lailai Wong, Jing Liu
    Journal of Chinese Pharmaceutical Sciences    2020, 29 (12): 908-914.   DOI: 10.5246/jcps.2020.12.080
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    Authentication is a key component of quality control, and the quality of Chinese medicinal materials directly impacts clinical efficacy. Chinese medicinal quality control is an important concern of the wider community, and it is intricately connected to the future and development of Chinese medicine. Macroscopic identification has been used for thousands of years in Chinese medicine, and it continues to be effective for resolving important issues related to quality control in the modern-day. However, new challenges have emerged for macroscopic identification. For example, new botanical varieties have emerged, with differences in macroscopic features related to cultivated vs. wild materials. Changes in processing methods and cultivation techniques also affect these features. Consequently, continual progress and innovation in Chinese medicinal authentication methods are needed. Macroscopic identification is based on organoleptic assessment, microscopy, and research of ancient texts, such as the Bencao. In addition to collecting information from traditional experience-based differentiation, innovation can take advantage of new technologies that can provide even more detailed, precise information about morphology. In the present review, we summarized inheritance and innovation in the scientific exposition of Chinese medicinal authentication, featuring a review of specialized publications, description of the establishment of a Chinese medicine specimen center and Chinese Medicine digital project, the expansion of authentication technologies, and the formation of a cultural project dedicated to the Compendium of Materia Medica.

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    A comparative study on different multiple cropping patterns of Bupleurum chinense
    Jiquan Liu, Yu Wang, Jianing Liu, Xin Liu, Runli He
    Journal of Chinese Pharmaceutical Sciences    2021, 30 (2): 169-178.   DOI: 10.5246/jcps.2021.02.014
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    Bupleurum chinense is a genuine medicinal material in Shanxi Province, and planting B. chinense is one of the main sources for local farmers to increase their income. In B. chinense cultivation, wheat-B. chinense, maize-B. chinense and soybean-B. chinense are commonly used as multiple cropping patterns. In the present study, we studied the effects of three different multiple cropping patterns on N, P and K levels of soil, photosynthetic parameters, agronomic characteristics, saikosaponin A, C and D contents, yield and economic benefits of B. chinense. The results showed that the soybean-B. chinense multiple cropping pattern was beneficial to the enrichment of N in the soil, thus promoting photosynthetic parameters, growth, saikosaponin accumulation, yield and economic benefits of B. chinense. It is suggested that soybean-B. chinense multiple cropping was an appropriate multiple cropping pattern for local cultivation of B. chinense.

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    Detection of minor constituents in TongMai Granules using NP×RP off-line two-dimensional liquid chromatography coupled with orbitrap mass spectrometry
    Lulu Xu, Zhanpeng Shang, Yue Chai, Yang Zhang, Rong Yu, Min Ye, Xue Qiao
    Journal of Chinese Pharmaceutical Sciences    2020, 29 (11): 793-803.   DOI: 10.5246/jcps.2020.11.072
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    TongMai Granules is a Chinese medicine patent drug to treat cardiovascular diseases. It is prepared from the water extract of Dan-shen, Chuan-xiong and Ge-gen. The main compounds of TongMai Granules are isoflavone glycosides, isoflavones, and phenolic acids. However, it is difficult to detect low-polar compounds such as tanshinones and phthalides though they may also contribute to the therapeutic effect. In this work, an off-line two-dimensional chromatography method was developed to enrich the minor constituents in TongMai Granules. The extract was subjected to an SEP-PAK silica SPE column and eluted with petroleum ether, ethyl acetate–methanol ( 6:1 , v/v), and methanol, successively. The three fractions were then analyzed using ultra-high performance liquid chromatography coupled with orbitrap mass spectrometry (UHPLC/orbitrap-MS). The isoflavones from Ge-gen, phenolic acids from Dan-shen and phthalides from Chuan-xiong were distributed in different fractions. A total of 131 compounds, including 59 from Ge-gen, 26 from Dan-shen, 43 from Chuan-xiong, and 3 common ones from Dan-shen and Chuan-xiong were tentatively identified. Among them, 26 compounds were identified by comparing with reference standards. This study set a good example for comprehensive analysis of the constituents in traditional Chinese medicine formula.
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    Development and challenges of professional Master of pharmacy education in China
    Jie Gu, Yanli Liu, Fengguo Xu, Yongze Zhang, Rong Shao, Tao Lu
    Journal of Chinese Pharmaceutical Sciences    2021, 30 (1): 69-76.   DOI: 10.5246/jcps.2021.01.007
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    In the present work, we aimed to describe the current situation and developing trend of professional Master of pharmacy education in China. Systematic searches of websites for literatures related to the specialty of professional Master of pharmacy were conducted. E-mail or telephone inquires were made directly to 108 pharmacy institutions (schools and universities) in China offering the MPharm program. The MPharm program was established in China in 2010, which primarily focuses on cultivating professionals in fields, such as drug technology transformation, inspection and regulation of drugs, registration and distribution of drugs, and pharmaceutical services. After 9 years of development, it has almost completed the overall design of its higher education paradigm with Chinese characteristics. With the rapid development of the pharmaceutical industry in China, the professional degree of pharmacy education program at the master’s level is insufficient to meet social and market demand for qualified professionals. Therefore, doctoral-level programs are now being promoted.

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    Determination and pharmacokinetic study of p-hydroxyphenethyl anisate following intravenous and oral administration in rats by RP-HPLC method
    Xiuwei Yang, Youbo Zhang, Wei Xu
    Journal of Chinese Pharmaceutical Sciences    2020, 29 (11): 804-812.   DOI: 10.5246/jcps.2020.11.073
    Abstract130)   HTML5)    PDF (3387KB)(51)       Save
    In the present study, we developed a rapid and specific reversed-phase high-performance liquid chromatographic (RP-HPLC) method for the quantification of p -hydroxyphenethyl anisate (HPA), one of the main bioactive constituents of the roots and rhizomes of Notopterygium incisum and N. franchetii , in rat plasma after an intravenous (20 mg/kg , i.v. ) and an intragastrical (200 mg/kg , i.g. ) administration to rats, respectively. The method involved a plasma clear-up step using liquid-liquid extraction by EtOAc , followed by RP-HPLC separation and detection. Separation of HPA was performed on an analytical Diamonsil TM ODS C 18 column with the mobile phase of MeOH–H 2 O at ratios of 75:25 (v/v) for i.v. and 70:30 (v/v) for i.g. administration. The flow-rate was 1.0 mL/min, and UV detection was performed at 256 nm. The calibration curves were linear over the ranges of 0.05–5.0 μ g/mL ( r 2 = 0.9984) for i.v. and 0.5–10.0 μ g/mL ( r 2 = 0.9995) for i.g. administration in rat plasma. The extraction recoveries were in the range of 82.01%–87.97%. The intra- and inter-day precisions were between 1.71% and 3.99%, with accuracies ranging from 91.22% to 110.5%. The absolute bioavailability of an orally administered HPA in rats was about 48.17%. The developed method was suitable for the determination and pharmacokinetic study of HPA in rat plasma.
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    Proteomic analysis on cellular response induced by nanoparticles reveals the nano-trafficking pathway through epithelium
    Jian Zhang, Mengmeng Qin, Dan Yang, Wenbing Dai, Hua Zhang, Xueqing Wang, Bing He, Qiang Zhang
    Journal of Chinese Pharmaceutical Sciences    2021, 30 (2): 107-118.   DOI: 10.5246/jcps.2021.02.009
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    The application of nanomedicines in oral drug delivery effectively promotes the drug absorption and transportation through enterocytes. Nevertheless, the absence of mechanism studies on efficacy and safety limits their final translation in humans. Although the vesicular trafficking has been verified as the general character for transport of nanomedicines, the deeper mechanism in molecular mechanism is still unclear. Moreover, the cellular transport of nanomedicines is a dynamic process involved by different organelles and components. However, most of existing studies just pay attention to the static location of nanomedicines, but neglect the dynamic biological effects on cells caused by them. Here, we prepared gold nanoparticles (AuNPs) as the model and cultured epithelial cell monolayer to explore the nano-bio interactions at the molecular level. The traditional pharmacological inhibition strategy and subcellular imaging technology elucidated the macropinocytosis/endosome/MVB/lysosome pathway during the transportation of AuNPs. Proteomics strategy based on mass spectrometry (MS) was utilized to identify and quantify proteins involved in the cellular transport of nanomedicines. Multiple proteins related to subcellular structure, signal transduction, energy transformation and metabolism regulation were demonstrated to be regulated by nanoparticle transport. These alterations of protein expression clarified the effects of intracellular proteins and verified the conventional findings. More importantly, it revealed a feedback mechanism of cells to the nano-trafficking. We believed that these new regulatory mechanisms provided new insights into the efficient transport of nanomedicines through epithelial barriers.

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    A simple and sensitive electrochemical impedimetric immunosensor for the detection of apolipoprotein E4 based on CeZnO nanoparticle
    Ying Zhang, Cong Li, Yi Liu, Lin Chu, Juncheng Zou, Youqi Yan, Xin Hu, Xiaomei Ling
    Journal of Chinese Pharmaceutical Sciences    2021, 30 (3): 239-245.   DOI: 10.5246/jcps.2021.03.019
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    Human apolipoprotein E4 (APOE4) is an important risk factor for late-onset Alzheimer’s disease (AD). However, little progress has been made for the detection of APOE4, and most of existing detection methods suffer from time-consuming process and expensive instruments. This study firstly proposed a simple and sensitive electrochemical method for detection of APOE4 based on carboxyl-rich CeZnO nanoparticles. Under the optimal conditions, the fabricated immunosensor exhibited a good linear relationship ranging from 10 to 100 ng/mL with the detection limit of 1.8 ng/mL (S/N = 3). The proposed electrochemical immunosensor had excellent selectivity, reproducibility and stability. Good performance was observed for sensitive determination of APOE4 in human serum sample, which provided a strong support for the detection of APOE4 and early clinical prevention of AD.

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    The impact of the provincial reimbursement scheme on the use of targeted anticancer medications in Zhejiang, China: a controlled interrupted time-series analysis
    Cong Huang, Carolina Oi Lam Ung, Haishaerjiang Wushouer, Ziyue Xu, Yichen Zhang, Xiaodong Guan, Luwen Shi
    Journal of Chinese Pharmaceutical Sciences    2021, 30 (7): 590-597.   DOI: 10.5246/jcps.2021.07.047
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    To alleviate problems with access and affordability, six targeted anticancer medications (TAMs) were listed in the Provincial Reimbursement Drug List (PRDL) for the first time in Zhejiang, China in February 2015. In the present study, we aimed to evaluate the implementation of the PRDL policy on TAMs use. Using the pharmaceutical procurement data of these six listed TAMs (study group) and four unlisted TAMs (control group) from 22 tertiary hospitals in Zhejiang, China dated between January 2014 and February 2017, interrupted time-series analysis was adopted to examine differences in the average hospital purchasing volume (HPV) and the average hospital purchasing spending (HPS) between the two groups. The average daily cost of listed TAMs in the study group was decreased after April 2015. After enlistment, the average HPV per month was significantly increased by 34.6 defined daily doses (DDDs) (P < 0.001), and the average HPS per month was significantly increased by USD 6614.9 (P < 0.001) for the listed TAMs in the study group (n = 6). Neither the average HPV nor the average HPS changed significantly for the unlisted TAMs in the control group (n = 4). The PRDL policy showed positive effects on improving patients’ affordability and promoting access to TAMs in Zhejiang. The government should conduct further price negotiations and include more TAMs with clinical benefits into reimbursement schemes to relieve patients’ financial burden and promote access.

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    The group of Professor Pengfei Tu/Kewu Zeng has made progress in the study of anti-cerebral ischemia target of Cistanche deserticola
    State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University Health Science Center
    Journal of Chinese Pharmaceutical Sciences    2021, 30 (2): 185-186.  
    Abstract124)      PDF (1665KB)(6)       Save
    The group of Professor Pengfei Tu/Kewu Zeng has made progress  in the study of anti-cerebral ischemia target of Cistanche deserticola.
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    Quality evaluation of Farfarae Flos by ITS/ITS2 and HPLC fingerprint analysis
    Zijuan Lu, Yan Jia, Jie Xing, Shuxian Xiao, Yulong Wang, Wenjie Qin, Xuemei Qin, Zhenyu Li
    Journal of Chinese Pharmaceutical Sciences    2021, 30 (1): 58-68.   DOI: 10.5246/jcps.2021.01.006
    Abstract123)   HTML22)    PDF (3716KB)(20)       Save

    The flower bud of Tussilago farfara L., also known as Farfarae Flos (FF), is commonly used in the traditional Chinese medicine (TCM) for the treatment of cough, bronchitis and asthmatic disorders. In this study, 26 samples from five provinces across northern China were collected, and internal transcribed spacer-polymerase chain reaction (ITS-PCR) coupled with high performance liquid chromatography (HPLC) fingerprint profiling was used for the quality evaluation of FF. The results of the ITS sequence analysis showed the high similarity values among these samples. ITS2 sequence exhibited less molecular diversity compared with ITS1, and no obvious correlation was found between the variation of ITS with the production areas or cultivation methods. The results of HPLC fingerprints in combination with the similarity analysis suggested that relative contents of phenylpropanoids and flavonoids varied among the 26 FF samples, and there was also no obvious difference among the different habitats. The phenylpropanoids and the flavonoids showed similar fluctuating patterns, and positive correlation among them was also observed. The results presented in this study suggested that FF from different habits showed high similarities, and ITS-PCR coupled with HPLC fingerprint profiling could be used as a valuable approach for the quality evaluation of FF.

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    A strategy for structure-activity relationship study on antioxidants in Echinops latifolius Tausch extracts by online HPLC-radical scavenging detection coupled with ESI-IT-TOF-MSn
    Xin Dong, Hong Wang, Feixiang Ma, Jianping Gao, Shizhong Chen, Peifeng Xue
    Journal of Chinese Pharmaceutical Sciences    2021, 30 (4): 267-279.   DOI: 10.5246/jcps.2021.04.022
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    Echinops latifolius Tausch (ELT) is the traditional Mongolian medicine for the treatment of osteoporosis, and the ambiguous composition of active ingredients is an important factor in restricting the modernization and globalization of this herb. Considering the traditional activity screening strategy is time-consuming and labor intensive, online HPLC active ingredient detection coupled with ESI-IT-TOF-MSn strategy was employed in this study to isolate, identify and screen active compounds from the herbal medicines at the same time. The structure-activity relationship of these compounds was elucidated as well. Owing to the association of osteoporosis progression and oxidative stress, the antioxidants screening from ELT could be a good interpretive of the active substance in this herb. Meanwhile, DPPH equivalent method was an indicative of the most powerful antioxidant in ELT. Consequently, the screening and identification of the antioxidants in ELT was performed by using on-line HPLC-radical scavenging detection coupled with ESI-IT-TOF-MSn strategy, and the structure-activity relationship was investigated based on DPPH equivalent method. Finally, 20 constituents (including apigenin glucosides, caffeic acid, biscaffeoylquinic acids, biscaffeoylquinic acid methyl esters, ect.) were characterized in ELT extracts, and 18 components showed appreciable radical scavenging capacity. In addition, the structure-activity relationship study was carried out based on 14 compounds isolated from our laboratory, and the structural requirements of the compounds on antioxidant activity were obtained: (1) compounds with phenolic hydroxyl groups could have antioxidant activity; (2) the antioxidant activity could not be facilitated by the number of hydroxyl groups, but affected by the number of caffeoyl groups; (3) the substitution position of caffeoyl on quinic acid had a greater influence on DPPH activity; (4) methoxy groups could reduce the antioxidant activity. Collectively, this work provided the biochemical perspective to link active compounds and anti-osteoporosis action of ELT, and further explained how ELT worked in osteoporosis patients with bone loss.

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    Analysis of the effect of HCV resistance-associated substitutions on the short-term efficacy of DAA after single administration in three phase Ib clinical trials
    Jing Zhou, Hong Zhang, Xiaojiao Li, Xiangshi Song, Mengmeng Zhang, Yanhua Ding
    Journal of Chinese Pharmaceutical Sciences    2021, 30 (2): 133-145.   DOI: 10.5246/jcps.2021.02.011
    Abstract121)   HTML753)    PDF (1463KB)(58)       Save

    As crucial factors in hepatitis C virus (HCV) management, resistance-associated substitutions (RASs) are associated with the treatment outcome of some direct-acting antiviral (DAA)-based regimens. In this study, we mainly analyzed the impact of baseline Y93H or Y93Y/H on the short-term efficacy after single administration of NS5A inhibitors in three phase Ib clinical trials (yimitasvir phosphate, KW-136 and fopitasvir), and analyzed the prevalence of baseline RASs and treatment-emergent RASs. A total of 94 treatment-na?ve HCV genotype (GT)-1b (n = 63) and GT-2a (n = 31) Chinese patients were enrolled in three phase 1b clinical trials. We investigated RASs in 77 patients with next generation or Sanger sequencing. In the 7-day trial of yimitasvir phosphate, the mean maximum HCV RNA decrease of patients with baseline Y93H or Y93Y/H was lower than that of patients without the mutation in the 30 mg and 200 mg cohorts (0.83 vs. 2.45 log10 IU/mL and 1.92 vs. 2.63 log10 IU/mL). In the 3-day trial of KW-136, the mean maximum HCV RNA decrease in patients with baseline Y93H or Y93Y/H was lower than that of patients without the mutation in the 30, 60 and 120 mg cohorts (1.58 vs. 2.89 log10 IU/mL, 3.16 vs. 4.09 log10 IU/mL and 3.00 vs. 5.04 log10 IU/mL, respectively). In the 3-day trial of fopitasvir, only 30 mg group had baseline Y93H or Y93Y/H, and the average maximum HCV RNA decrease of patients with baseline Y93H or Y93Y/H was lower than that of patients without the mutation (1.45 vs. 3.59 log10 IU/mL). In the three trials, baseline RASs were observed in 54 patients (70.1%; 54/77). The most prevalent baseline RASs were Y93H and Y93Y/H (18.2%; 14/77), followed by L31M (16.9%; 13/77). The most common RASs after single administration of DAA were Y93H and Y93Y/H. Our data could provide reference for future clinical treatment and clinical trial.

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    Academician Zhicen Lou and the Discipline of Pharmacognosy in Peking University
    Shaoqing Cai
    Journal of Chinese Pharmaceutical Sciences    2020, 29 (11): 819-822.  
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    Academician Zhicen Lou and the Discipline of Pharmacognosy in Peking University.
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    Comparison of quality control standards of PET radiopharmaceuticals for tumor in Pharmacopoeia of Europe, the United States and People’s Republic of China
    Yizi Zhu, Huajun Li, Yubo Zhang, Chaoran Zhao, Shuai Lu, Mingxuan Fan, Mei Han
    Journal of Chinese Pharmaceutical Sciences    2021, 30 (3): 246-252.   DOI: 10.5246/jcps.2021.03.020
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    To improve the relevant methods of the quality control standards of tumor Positron Emission Computed Tomography (PET) radiopharmaceuticals and to reduce the clinical application risks of such drugs, this article compares and analyzes the similarities and differences of the quality control standards of tumor PET radiopharmaceuticals in the Pharmacopoeia of People’s Republic of China (ChP2020), European Pharmacopoeia (EP8.0) and United States Pharmacopoeia (USP39), focusing on comparing and analyzing the identification (identification method), inspection (pH, residual solvent, bacterial endotoxin, sterility, and impurities), and content determination (radionuclear purity, radiochemical purity, and radioactive concentration) of tumor PET radiopharmaceuticals. The quality control standards of ChP2020 for tumor PET radiopharmaceuticals are relatively equivalent to the quality control standards of USP39 but are not as stringent as those of EP8.0. In general, EP8.0 has the most comprehensive and strict quality control standards for tumor PET radiopharmaceuticals. The quality control standards of tumor PET radiopharmaceuticals in the Chinese Pharmacopoeia can be improved by referring to international standards, especially the European Pharmacopoeia.

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    Flavonoid C-glycosides from the seeds of Hovenia dulcis Thunb.
    Fangfang Xu, Biao Sun, Xiaoqi Zhang, Bo Liu
    Journal of Chinese Pharmaceutical Sciences    2020, 29 (11): 813-818.   DOI: 10.5246/jcps.2020.11.074
    Abstract112)   HTML3)    PDF (1465KB)(47)       Save
    Ten known flavonoid C -glycosides identified as 2 ′′ - O - β - D -glucopyranosyl isovitexin ( 1 ), spinosin ( 2 ), 6 ′′′ -acetyl spinosin ( 3 ), 6 ′′′ - p -hydroxycinnamoyl-2 ′′ O - β - D -glucopyranosyl isovitexin ( 4 ), 6 ′′′ - p -hydroxy-cinnamoyl spinosin ( 5 ), 6 ′′′ -( E )-feruloyl O - β - D -glucopyranos yl isovitexin ( 6 ), isospinosin ( 7 ), isovitexin ( 8 ), swertisin ( 9 ), swertiajaponin ( 10 ) were purified from the seeds of Hovenia dulcis Thunb. Their structures were confirmed by spectroscopic data analysis and comparison with previous literature. All compounds were obtained from H. dulcis for the first time.  
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    Author Index of Volume 29
    Journal of Chinese Pharmaceutical Sciences
    Journal of Chinese Pharmaceutical Sciences    2020, 29 (12): 932-935.  
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    Extractum trametes robiniophila murr protects murine podocyte via actin cytoskeleton stabilization
    Xuan Luo, Qing Du, Haiyan Zhao, Wenhai Fan, Xin Gao, Xia Gao
    Journal of Chinese Pharmaceutical Sciences    2021, 30 (3): 230-238.   DOI: 10.5246/jcps.2021.03.018
    Abstract108)   HTML6)    PDF (1353KB)(65)       Save

    The Chinese medicine Extractum trametes robiniophila murr (ETRM) is the extract of a type of fungus. Recent studies have suggested that ETRM efficiently improves the effacement of podocyte foot processes in adriamycin (ADR)-induced nephrotic rats. In the present study, we aimed to assess whether ETRM modulated the actin rearrangements of podocytes and involved signaling molecules, including α-actinin-4 and nephrin. Podocytes were treated with ADR (0.5 μmol/L), ADR (0.5 μmol/L) + dexamethasone (Dex) (1 μmol/L), ADR (0.5 μmol/L) + ETRM (10 mg/mL). The F-actin in the podocytes was stained by fluorescent phallotoxins and observed by confocal microscopy. The expression levels of α-actinin-4 and nephrin were tested by real-time PCR and Western blotting analysis. The administration of ETRM could significantly prevent ADR-treated podocytes from actin rearrangement. Both ETRM and Dex could stabilize podocyte actin cytoskeletons. Moreover, α-actinin-4 might act as a potential target for ETRM functionality in podocyte actin rearrangements. However, pretreatment with ETRM could not inhibit the up-regulation of nephrin as a result of ADR treatment. ETRM could improve the cytoskeleton stability in ADR-induced actin rearrangement of podocytes via regulating α-actinin-4 expression.

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