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Three new dimeric diterpenes from Rhododendron molle

chinese Chemical Letters 2017年第6期28卷 1205-1209页

作者： Shuai-Zhen Zhou Chun-Ping 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 SciencesShanghai 201203 China SIMM-CUHK joint research laboratory for promoting globalization of traditional chinese medicines between shanghai institute of materia medica ChineseAcademy of Sciences and The Chinese University of Hong Kong China School of Biomedical Sciences The Chinese University of Hong Kong Hong Kong China School of Life Science and Technology. shanghaiTech university Shanghai 201203 China

Birhodomolleins A-C（1-3）,three novel diterpenoids dimerized from two grayanane diterpenes through an oxygen bridge,were isolated from the flowers of Rhododendron *** structures were elucidated by interpretation of their 1D and 2D NMR and other spectroscopic *** A（1） contains a rare chloro-substitution on one of the grayanane *** are the first examples of dimeric diterpenes from the Ericaceae family.

关键词： Rhododendron molle Ericaceae Dimeric diterpene Grayanane Birhodomolleins A-C

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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

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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

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

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

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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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