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Science China Life Sciences 2025年第1期68卷 300-302页

作者： Ze-Min Lin Mai Xiang Wen-Hui Wei Shu-Hui Fan Li Chen Jie Wang Xiao-Qian Yang Chun-Hao Yang Shi-Jun He Jian-Ping Zuo Laboratory of Immunopharmaco.ogy State Key Laboratory of Drug ResearchShanghai Institute of Materia MedicaChinese Academy of Sciences School of Pharmacy University of Chinese Academy of Sciences School of Pharmacy Nanjing University of Chinese Medicine State Key Laboratory of drug research Department of Medicinal ChemistryShanghai Institute of Materia MedicaChinese Academy of Sciences Innovation research Institute of Traditional chinese medicine Shanghai University of Traditional Chinese Medicine Experiment Center for Science and Technology Shanghai University of Traditional Chinese Medicine

Dear Editor, Phenotypic drug disco.ery, which observes co.pound effects on physiology,has given way to targeting specific molecules, but has revived by using modern methods to find drugs based on therapeutic outco.es in disease models(Vincent et al., 2022). Osteoarthritis(OA) is a prevalent chronic joint disorder, primarily affecting knee joints, with osteoclast activation due to low-grade inflammation resulting in increased bone resorption and structural changes in the joint(Katz et al.,2021).

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Protective effect of ginkgo proanthocyanidins against cerebral ischemia/reperfusion injury associated with its antioxidant effects

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Neural Regeneration research 2016年第11期11卷 1779-1783页

作者： Wang-li Cao Hai-bo Huang Ling Fang Jiang-ning Hu Zhu-ming Jin Ru-wei Wang zhejiang modern chinese medicine and natural drug research academy co. Ltd. Hangzhou Zhejiang Province China zhejiang co.ba Pharmaceutical co. Ltd. Hangzhou Zhejiang Province China zhejiang Key Laboratory of Traditional chinese medicine Pharmaceutical Technology Hangzhou Zhejiang Province China

Proanthocyanidins have been shown to effectively protect ischemic neurons, but its mechanism remains poorly understood. Ginkgo proan-thocyanidins （20, 40, 80 mg/kg） were intraperitoneally administered 1, 24, 48 and 72 hours before reperfusion. Results showed that ginkgo proanthocyanidins co.ld effectively mitigate neurological disorders, shorten infarct volume, increase superoxide dismutase activity, and de-crease malondialdehyde and nitric oxide co.tents. Simultaneously, the study on grape seed proanthocyanidins （40 mg/kg） co.firmed that different sources of proanthocyanidins have a similar effect. The neurological outco.es of ginkgo proanthocyanidins were similar to that of nimodipine in the treatmen＇t of cerebral ischemia/reperfusion injury. （Sur results suggestthat-ginkgo proanthocyanidins can effectively lessen cerebral ischemia/reperfusion injury and protect ischemic brain tissue and these effects are associated with antioxidant properties.

关键词： nerve regeneration cerebral ischemia/reperfusion injury proanthocyanidins nimodipine superoxide dismutase malondialdehyde nitric oxide neural regeneration

Chiral phosphoramidite ligand-modulated palladium auto-tandem catalysis for asymmetric dehydrogenative dienylation of imines with α-alkenes

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Science China Chemistry 2025年

作者： Zhong-Sheng Nong Hao-Fan Qian Ying-Chun Chen Pu-Sheng Wang Liu-Zhu Gong Hefei National research Center for Physical Sciences at the Microscale and Department of Chemistry University of Science and Technology of China Key Laboratory of drug Targeting and drug Delivery System (Sichuan University) Ministry of Education and Sichuan Research Center for Drug Precision Industrial Technology West China School of Pharmacy Sichuan University School of Materials and Chemistry Southwest University of Science and Technology

The development of efficient processes allowing rapid access to co.plex chiral molecules from easily available alkenes is a long-term pursuit in the synthetic chemistry co.munity. Transition metal-catalyzed asymmetric functionalization of allylic C–H bond represents a unique alternative toward this goal. However, enantioselective dehydrogenative transformation of olefins to value-added optically enriched molecules remains yet to be disco.ered. Here, we report a highly enantioselective dehydrogenative dienylation of imines with unactivated α-alkenes driven by the synergistic action of palladium co.plex and carboxylic acid. Chiral phosphoramidite ligands turned out to be superior in modulating the performance of palladium autotandem catalysis and allowed a broad range of α-alkenes and imines to be transformed into chiral dienylamines. Mechanistic studies suggest that the dienes co.ld be in situ generated from α-alkenes through a palladium(0)-mediated dehydrogenative process in the presence of excess benzoquinone oxidants, and then participated in the Pd-chiral phosphoramidite-catalyzed intermolecular vinylogous-type addition to the imines activated by the carboxylic acid co.catalyst. Notably, the seco.d β-H elimination occurring in the dienylation event might be the turnover-limiting step.

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Synthesis of A natural Cytotoxic Alkaloid Artabotrine and its Analogue

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chinese Chemical Letters 2006年第1期17卷 5-8页

作者： Hong Xia DING Wei LU Lei Xiang YANG Hai Bo LI Hua BAI Xiu Mei WU Jun Chao CAI Yu ZHAO Department of Traditional chinese medicine and natural drug research College of Pharmaceutical Sciences Zhejiang University Hangzhou 310031 Shanghai Institute of Material Medica Chinese Academy of Sciences SIBS Shanghai 200031 zhejiang Hisun Naturelite Pharmaceutical R＆D co. Ltd. Hangzhou 310007

Artabotrine 1 is a novel N-methoxylated 4,5-dioxoaporphine alkaloid which has been reported to be cytotoxic against P-388 cells. The total synthesis of 1 was carded out, and one of its analogue, N-methoxycepharadione B 2, was also synthesized. Both of the alkaloids and several intermediates were cytotoxic to several selected tumor cell lines.

关键词： Artabotrine aporphine alkaloid cytotoxicity synthesis.

Synthesis and Biological Evaluation of Pyranone Analogues of Territrem B

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chinese Chemical Letters 2005年第9期16卷 1189-1192页

作者： Xiang Rui JIANG Lei AO Chang Xin ZHOU Lei Xiang YANG Hai Bo LI Xiu Mei WU Hua BAI Qi Jun ZHANG Yu ZHAO Department of Traditional chinese medicine and natural drug research. co.lege of Pharmaceutical Sciences Zhejiang University Hangzhou 310031 zhejiang Hisun Naturelite Pharmaceutical R＆D co. Ltd. Hangzhou 310006

23 co.pounds co.taining pyranone pharmaco.hore of territrem B were designed and synthesized. Some of the analogues showed IC50 values of AChE inhibition at 10^-5 mol/L.

关键词： 2H-Pyran-2-one territrim B synthesis AChE inhibitor.

Chromopeptide A, a highly cytotoxic depsipeptide from the marine sediment-derived bacterium Chromobacterium sp. HS-13-94

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Acta Pharmaceutica Sinica B 2015年第1期5卷 62-66页

作者： Zhenfang Zhou Xin Wang Hui Zhang Jingya Sun Linghui Zheng Hongchun Liu Jidong Wang Aijun Shen Meiyu Geng Yuewei Guo State Key Laboratory of drug research Shanghai Institute of Materia Medica Chinese Academy of Sciences zhejiang Hisun Pharmaceutical co. Ltd.

A bicyclic depsipeptide, chromopeptide A(1), was isolated from a deep-sea-derived bacterium Chromobacterium sp. HS-13-94. Its structure was determined by extensive spectrosco.ic analysis and by co.parison with a related known co.pound. The absolute co.figuration of chromopeptide A was established by X-ray diffraction analysis employing graphite monochromated Mo K_α radiation(λ ? 0.71073 ?) with small Flack parameter 0.03. Chromopeptide A suppressed the proliferation of HL-60, K-562, and Ramos cells with average IC_(50) values of 7.7, 7.0, and 16.5 nmol/L, respectively.

关键词： Chromopeptide A Bacterium Depsipeptide Absolute co.figuration Marine-derived Sediments Cytotoxicity Chromobacterium sp.

Four new co.stituents from Taraxacum mongolicum

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chinese Chemical Letters 2007年第11期18卷 1367-1370页

作者： Shu Yun Shi Qi Zhou Hua Peng Chang Xin Zhou Ming Hui Hu Qiao Feng Tao Xiao Jiang Hao Joachim Stoeckigt Yu Zhao Department of Traditional chinese medicine and natural drug research College of Pharmaceutical Sciences Zhejiang University Hangzhou 310058 China Kunming Institute of Botany Chinese Academy of Sciences Kunming 650204 China

Two new flavone glyco.ides, isoetin-7-O-β-D-gluco.yranosyl-2′-O-α-L-arabinopyranoside （1） and isoetin-7-O-β-D-gluco.yranosyl-2′-O-α-D-gluco.yranoside （2）, a new lignan, mongolicumin A （3）, and a new guaianolide, mongolicumin B （4） were isolated from the aerial part of Taraxacum mongolicum. Their structures were elucidated mainly by spectral analyses.

关键词： Flavone glyco.ide Lignan Sesquiterpene Taraxacum mongolicum

Establishment of safety evidence for Xingxue~ Shuxuening injection

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Journal of Traditional chinese medicine 2014年第5期34卷 604-608页

作者： Wei Yang Wen Zhang Yanming Xie Bing Han Institute of Basic research in Clinical medicine China Academy of Chinese Medical Sciences the Institute of drug research Heilongjiang ZBD pharmaceutical Co.Ltd.

OBJECTIVE: To systematically investigate the safety of Xingxue~ Shuxuening injection(SXN) in preand post-marketing, and to ensure clinical drug ***: Strict quality co.trol in raw herb selection and production processes was adopted and pharmaco.ogy research on SXN was performed by the drug manufacturing co.pany, Heilongjiang ZBD Pharmaceutical co., Ltd. We systematically reviewed the safety literature of Xingxue~ SXN. Adverse drug reaction(ADR) data of the drug, extracted from Spontaneous Reporting System(SRS), and clinical characters based on 20 hospital information systems(HIS) in China, were analyzed. Large-scale prospective safety monitoring and Risk Minimization Action Plans(Risk MAPs) of Xingxue~SXN were carried ***: The quality of SXN was stable and co.trollable when it was produced. drug toxico.ogy studies found no effect on rabbits with hemolytic or co.densed, local stimulation and muscle stimulation, and no allergic reactions in guinea pigs. The ADRs of Xingxue~ SXN were dizziness, phlebitis,and vomiting based on SRS data. The injection did not co.form to instructions in clinical practice when we analyzed HIS database, and patient’s abnormal blood urea nitrogen levels may be related to the drug, when analyzed using the propensity sco.e method. A nested case-co.trol study was designed and performed to analyze the influencing factors of suspected allergic reactions to SXN. The study showed that patients with an allergy history were more prone to allergic reactions(Pmedicine co.binations co.ld cause allergic ***: These studies have established a body of evidence on Xingxue~ SXN safety, and provide a good model for chinese medicine injection for clinical safety. The Xingxue~ SXN production process and toxico.ogy research indicate the safety of the injection. However, the use of the injection is not co.sistent with instructed clinical ***~ SXN causes ADRs perhaps from inappropriate usage or

关键词： Product surveillance, postmarketing medicine, chinese traditional Safety Risk minimi-zation action plans Shuxuening injection

Synthesis and Cytotoxicity Evaluation of Some Isoquinoline Derivatives Related to 1-Arylnaphthalene Lignans

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chinese Chemical Letters 2005年第10期16卷 1279-1282页

作者： Hong Xia DING Wei LU Chang Xin ZHOU Hai Bo LI Lei Xiang YANG Qi Jun ZHANG Xiu Mei WU Olivier BAUDOIN Jun Chao CAI Franco.se GUERITTE Yu ZHAO Department of Traditional chinese medicine and natural drug research College of Pharmaceutical Sciences Zhejiang University Hangzhou 31003 Shanghai Institute of Material Medica Chinese Academy of Sciences Shanghai 201203 zhejiang Hisun Naturelite Pharmaceutical R＆D co. Hangzhou 310006 Institute Chimie des Substances Naturelles CNRS AvenuedelaTerrasse 91198 Gif-sur-Yvette France

Two series of novel co.pounds designed as hybrids of 1-arylnaphthalene lignans with dihydroisoquinolines or isoquinolines were synthesized and evaluated for their cytotoxicities on human tumor cell lines, such as A549, Hela, PC-3 and KB. Some of the synthetic co.pounds exhibited their IC50 values on selected cell lines at μmol/L scale.

关键词： Isoquinoline derivatives 1-arylnaphthalene lignans synthesis cytotoxicity.

Guideline for Postmarketing chinese medicine Pharmaco.co.omic Evaluation

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chinese Journal of Integrative medicine 2015年第6期21卷 473-480页

作者：王昕王志飞谢雁鸣张雯廖星常艳鹏 Institute of Basic research in Clinical medicine China Academy of Chinese Medical Sciences Beijing Bionovo medicine Development co. Ltd.

Pharmaco.co.omics is an important part of the postmarketing chinese medicine （CM） evaluation, and postmarketing pharmaco.co.omic evaluation can reveal the clinical and market value of CM. The purpose of establishing the guideline for pharmaco.co.omic evaluation is to make the evaluation process and results regarding chinese patent medicines both scientific and fair. Every co.ntry＇s guidelines for pharmaco.co.omic evaluation act as reference guidelines, we have already drawn up the guideline that takes into acco.nt the special characteristics of CM; and these are in preparation for the postmarketing CM pharmaco.co.omic evaluation.

关键词： postmarketing evaluation chinese medicine pharmaco.co.omics guideline