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Birhodomolleins D and E, two new dimeric grayanane diterpenes with a 3-O-2＇ linkage from the fruits of Rhododendron pumilum

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chinese Chemical Letters 2018年第1期29卷 123-126页

作者： RuiZhang Chunping Tang Chang-Qiang Ke Sheng Yao Ge Lin Yang Ye State Key laboratory of Drug research and Natural Products Chemistry Department Shanghai Institute of Materia Medica Chinese Academy of Sciences Shanghai 201203 China University of chinese Academy of Sciences Beijing 100049 China SIMM-CUHK joint research laboratory for promoting globalization of traditional chinese medicines between shanghai institute of materia medica Chinese Academy of Sciences and The Chinese University of Hang Kong Hang Kong SAR China School of Biomedical Sciences The Chinese University of Hang Kong Hang Kong SAR China School of Life Science and Technology ShanghaiTech University Shanghai 201210 China

Two new dimeric diterpenes, birhodomolleins D （1） and E （2）, were characterized from the fruits of Rhododendron pumilum. Their structures featured two grayanane diterpenes dimerized through an oxygen bridge locating at C-3 and C-2＇. They are the first examples of dimeric grayanane diterpenes with a 3-O-2＇ linkage from the Ericaceae family. Their structures were elucidated on the basis of comprehensive analysis of spectroscopic data.

关键词： Rhododendron pumilumEricaceaeDimeric diterpeneGrayananeBirhodomollein DBirhodomollein E

Polyoxypregnanes as safe, potent, and specific ABCB1-inhibitory pro-drugs to overcome multidrug resistance in cancer chemotherapy in vitro and in vivo

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Acta Pharmaceutica Sinica B 2021年第7期11卷 1885-1902页

作者： Xu Wu Chun Yin Jiang Ma Stella Chai Chunyuan Zhang Sheng Yao Onat Kadioglu Thomas Efferth Yang Ye Kenneth Kin-Wah To Ge Lin School of Biomedical Sciences Faculty of Medicinethe Chinese University of Hong KongHong Kong 999077China joint research laboratory of promoting globalization of traditional chinese medicines between the chinese University of Hong Kong and shanghai institute of materia medica Chinese Academy of SciencesHong Kong 999077China State Key laboratory of Drug research and Natural Products Chemistry Department Shanghai Institute of Materia MedicaChinese Academy of SciencesShanghai 201203China Department of Pharmaceutical Biology Johannes Gutenberg UniversityMainz 55099Germany School of Pharmacy Faculty of Medicinethe Chinese University of Hong KongHong Kong 999077China laboratory of Molecular Pharmacology Department of PharmacologySchool of PharmacySouthwest Medical UniversityLuzhou 646000China

Multidrug resistance(MDR)mediated by ATP binding cassette subfamily B member 1(ABCB1)is significantly hindering effective cancer ***,currently,no ABCB1-inhibitory drugs have been approved to treat MDR cancer clinically,mainly due to the inhibitor specificity,toxicity,and drug ***,we reported that three polyoxypregnanes(POPs)as the most abundant constituents of Marsdenia tenacissima(***)were novel ABCB1-modulatory pro-drugs,which underwent intestinal microbiota-mediated biotransformation in vivo to generate active *** metabolites at non-toxic concentrations restored chemosensitivity in ABCB1-overexpressing cancer cells via inhibiting ABCB1 efflux activity without changing ABCB1 protein expression,which were further identified as specific non-competitive inhibitors of ABCB1 showing multiple binding sites within ABCB1 drug *** POPs did not exhibit ABCB1/drug metabolizing enzymes interplay,and their repeated administration generated predictable pharmacokinetic interaction with paclitaxel without obvious toxicity in *** further showed that these POPs enhanced the accumulation of paclitaxel in tumors and overcame ABCB1-mediated *** results suggested that these POPs had the potential to be developed as safe,potent,and specific pro-drugs to reverse ABCB1-mediated *** work also provided scientific evidence for the use of *** in combinational chemotherapy.

关键词： Multidrug resistance ABCB1 Polyoxypregnane Combination chemotherapy Marsdenia tenacissima

Honokiol: A naturally occurring lignan with pleiotropic bioactivities

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chinese Journal of Natural medicines 2021年第7期19卷 481-490页

作者： CHEN Cheng ZHANG Qing-Wen YE Yang LIN Li-Gen State Key laboratory of Quality research in chinese Medicine Institute of Chinese Medical SciencesUniversity of MacaoMacaoChina State Key laboratory of Drug research Shanghai Institute of Materia MedicaChinese Academy of SciencesShanghai 201203China

Honokiol is the dominant biphenolic compound isolated from the Magnolia tree,and has long been considered as the active constituent of the traditional chinese herb,‘Houpo’,which is widely used to treat symptoms due to‘stagnation of qi’.Pharmacological studies have shown that honokiol possesses a wide range of bioactivities without obvious *** protects the liver,kidneys,nervous system,and cardiovascular system through reducing oxidative stress and relieving ***,honokiol shows anti-diabetic property through enhancing insulin sensitivity,and anti-obese property through promoting browning of *** vivo and in vitro studies indicated that honokiol functions as an anti-cancer agent through multiple mechanisms:inhibiting angiogenesis,promoting cell apoptosis,and regulating cell cycle.A variety of therapeutic effects of honokiol may be associated with its physiochemical properties,which make honokiol readily cross the blood brain barrier and the blood-cerebrospinal fluid barrier,with high *** the future,more clinical researches on honokiol are needed to fully authenticate its therapeutic values.

关键词： Honokiol Natural sources Ethnopharmacological uses Physicochemical properties Bioactivities Clinical trials

Current Status and Future Perspective in the globalization of traditional chinese medicines

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World Journal of traditional chinese Medicine 2015年第1期1卷 1-4页

作者： Wan-Ying Wu Wen-Zhi Yang Jin-Jun Hou De-An Guo shanghai research Center for Modernization of traditional chinese Medicine and National Engineering laboratory for TCM Standardization Technology Shanghai Institute of Materia Medica Chinese Academy of Sciences

globalization of traditional chinese medicines started around 1996, which was initiated by the chinese government. However, substantial progress was only achieved in recent years including the adoption of TCM quality monographs in the western pharmacopoeias(United States Pharmacopoeia and European Pharmacopoeia) and registration in main stream drug regulatory agencies such as US Food and Drug Administration(FDA) and European medicines Agency(EMA). So far, several TCM herbal quality monographs were adopted by the United States Pharmacopoeia including chinese Salvia, Ganoderma lucidum and Panax notoginseng, etc. Over 45 TCM quality monographs were recorded in the European Pharmacopoeia with 20 more in progress. After the successful registration of the first TCM product named Diao Xin Xue Kang as traditional medicine via the medicines Evaluation Board of the Netherlands, several other TCM herbal products are in the registration process in several European member states. So far, there has been still not any TCM product authorized as a drug by the FDA regardless of a few TCM products in phase III or phase II clinical trials. This review summarizes the progress made in the globalization of traditional chinese medicines in recent years and future issues in this regard.

关键词： globalization traditional chinese Medicine(TCM) Quality Monograph Registration regulation

Reversal of P-gp-mediated Multidrug Resistance of Anticancer Agents by Herbal Components

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Reversal of P-gp-mediated Multidrug Resistance of Anticancer...

Isatis indigotica:from(ethno)botany,biochemistry to synthetic biology

第十四届全国中药和天然药物学术研讨会

作者： Chun Yin Kenneth K.W.To Stella Chai Yang Ye Ge Lin School of Biomedical Sciences The Chinese University of Hong Kong joint research laboratory of promoting globalization of traditional chinese medicines between shanghai institute of materia medica Chinese Academy of Sciences and The Chinese University of Hong Kong School of Pharmacy The Chinese University of Hong Kong State Key laboratory of Drug research and Natural Products Chemistry Department Shanghai Institute of Materia MedicaChinese Academy of Sciences

＜正＞One of the major obstacles to successful anticancer chemotherapy is multidrug resistance（MDR）.The overexpression of ATP-binding cassette（ABC）transporters to pump anticancer drugs out of resistant cancer cells can cause MDR.P-glycoprotein（P-gp）is the most extensively studied ABC transporter conferring *** present study aimed to demonstrate

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Molecular Horticulture 2021年第1期1卷 1-14页

作者： Jingxian Feng Doudou Huang Yingbo Yang Junfeng Chen Shi Qiu Zongyou Lv Xueqi Ma Yuanyu Li Rongrong Li Ying Xiao Wansheng Chen research and Development Center of chinese Medicine Resources and Biotechnology The Ministry of Education(MOE)Key Laboratory for Standardization of Chinese MedicinesInstitute of Chinese Materia MedicaShanghai University of Traditional Chinese MedicineShanghai 201203China Jiangsu Kanion Pharmaceutical Co. LtdJiangsu 222001LianyungangChina medical Guarantee Center Changzheng HospitalNaval Medical UniversityShanghai 200003China

Isatis indigotica Fort.(chinese woad)is a species with an ancient and well-documented history as an indigo dye and medicinal *** is often confused with Isatis tinctoria L.(European woad),a medicinal plant in ***,the differences between *** and *** are systematically *** usage development history,clinical applications and pharmacological activities,and chemical components of *** are also ***,indole alkaloids,and their corresponding derivatives have been identified as the major active ingredients of *** and are associated with anti-viral,anti-inflammatory,anti-cancer,and other health-promoting *** progress has been made in understanding the biosynthetic pathway and regulation mechanism of lignans and indole alkaloids in ***,the results from which should facilitate the process of targeted metabolic engineering or synthetic ***,multiple biotechnology methods such as polyploid breeding and genetic engineering have been used with *** to result in,for example,greater yields,higher levels of bioactive component accumulation,and enhanced stress tolerance to salt,drought,and *** issues require additional analyses,and suggestions for future research on *** are also discussed.

关键词： Isatis indigotica Lignans Indole alkaloids Metabolic engineering Synthetic biology