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Chinese Journal of Natural Medicines 2019年第7期17卷 490-497页

作者： CHEN Jia-Yin Jürgen Brockmoller Mladen V.Tzvetkov WANG Li-Jun CHEN Xi-Jing Department of Pharmacy Peking University Shenzhen Hospital Shenzhen 518036 China Institute for Clinical Pharmacology University Medical Center Gottingen Georg-August University Gottingen 37075 Germany Clinical Pharmacokinetics Lab China Pharmaceutical University Nanjing 211198 China

Current study systematically investigated the interaction of two alkaloids, anisodine and monocrotaline, with organic cation transporter OCT1, 2, 3, MATE1 and MATE2-K by using in vitro stably transfected HEK293 cells. Both anisodine and monocrotaline inhibited the OCTs and MATE transporters. The lowest IC50 was 12.9 μmol·L-1 of anisodine on OCT1 and the highest was 1.8 mmol·L-1 of monocrotaline on OCT2. anisodine was a substrate of OCT2(Km = 13.3 ± 2.6 μmol·L-1 and Vmax = 286.8 ± 53.6 pmol/mg protein/min). Monocrotaline was determined to be a substrate of both OCT1(Km = 109.1 ± 17.8 μmol·L^-1, Vmax = 576.5 ± 87.5 pmol/mg protein/min) and OCT2(Km = 64.7 ± 14.8 μmol·L^-1, Vmax = 180.7 ± 22.0 pmol/mg protein/min), other than OCT3 and MATE transporters. The results indicated that OCT2 may be important for renal elimination of anisodine and OCT1 was responsible for monocrotaline uptake into liver. However neither MATE1 nor MATE2-K could facilitate transcellular transport of anisodine and monocrotaline. Accumulation of these drugs in the organs with high OCT1 expression(liver) and OCT2 expression(kidney) may be expected.

关键词： anisodine Monocrotaline Organic cation transporter OCT MATE

Asymmetric Synthesis of anisodine

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Chinese Chemical Letters 2005年第10期16卷 1287-1289页

作者： Yan Fen WU Wen LUE Qiang LU Wen Sheng ZHANG School of Pharmaceutical Sciences Peking University Beijing 100083

anisodine was synthesized from 3α-hydroxy-6β-acetyltropine in 11 steps. Laevorotary isomer of anisodine was prepared from the asymmetric dihydroxylation of compound 10 via the osmium catalyzed process employing p-ch... 详细信息

关键词： anisodine tropine alkaloid total synthesis.

ABSOLUTE CONFIGURATION OF (-)anisodine (A NEW GANGLIO BLOCKING AGENT) AND (-)ANISODINIC ACID

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Science in China,Ser.B 1983年第9期26卷 931-935页

作者：谢晶曦杨靖华赵瑶兴张纯贞 Institute of Materia Medica Chinese Academy of Medical Sciences Beijing Graduate School Chinese University of Seience and Technology

A new tropane alkaloid, (-)anisodlne (Ⅰ), was isolated from the plant of Anisodus tanguticus. It is a novel ganglio blocking agent. The absolute configuration of (-)anisodinic acid (Ⅶ), which-is the side chain of (-)anisodine, was determined by chemical correlation with (R) (-)-2-phenyl-1, 2-propanediol (Ⅳ) and (R) (-)-2-hydroxy-2-phenylpropionic acid (Ⅵ). Thereby (-)anisodine with the absolute configuration shown as (Ⅰ) is 6β, 7β-epoxy-1αH, 5αH-tropan-3α-ol (S) 2’-phenyl-2’, 3’-dihydroxypropionate. Two new tropane alkaloids: 6β, 7β-epoxy-1αH, 5αH-tropan-3α-ol 2’,3’-epox-ypropionate (Ⅲ) and 2’-phenyl-2’-hydroxypropionate (Ⅴ) were prepared and its physical constant is reported in this paper.

关键词： ppm OC ABSOLUTE CONFIGURATION OF AND anisodine A NEW GANGLIO BLOCKING AGENT

STRUCTURE AND ABSOLUTE CONFIGURATION OF anisodine HYDROBROMIDE

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Chinese Science Bulletin 1988年第16期33卷 1397-1399页

作者：鲍光宏徐常富贺存恒穆善田 Institute of Basic Medical Sciences Chinese Academy of Medical Sciences Beijing China-Japan Friendship Hospital Beijing

anisodine is a noval anticholinergic drug extracted from the Datura plant Scoplia tangutic. Its chemical characteristics and pharmacological effects have been investigated. in detail.

关键词： anisodine hydromide absolute configuration X-ray diffraction method

Total Synthesis of anisodine

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Journal of Chinese Pharmaceutical Sciences 2005年第1期14卷 13-17页

作者：吴艳芬卢强吕雯仉文升北京大学药学院药物化学系北京100083

Aim To design a practical synthetic route of anisodine. Methods Starting from3α-hydroxy-6β-acetyltropine, anisodine was synthesized in 11 steps. Result anisodine wasobtainded with an overall yield of 2.6 % . Conclusion Total synthetic route of anisodine wasachieved which may afford a possible route for commercial preparation of anisodine.

关键词： anisodine tropine alkaloid total synthesis

樟柳碱(anisodine)对大鼠大脑皮层单个神经元放电的影响

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科学通报 1984年第20期29卷 1273-1276页

作者：郑永芳鲍光宏中国医学科学院基础医学研究所中国首都医科大学基础医学部

樟柳碱是从茄科植物唐古特山莨菪(Scopolia tangutica)植物中提取出来的一个新的抗胆碱药,其化学结构和药理性质与东莨菪碱相似,中枢作用明显且毒性较小,临床上用于静脉注射中药复合麻醉获得良好效果。关于樟柳碱的中枢作用原理,据报道... 详细信息

樟柳碱是从茄科植物唐古特山莨菪(Scopolia tangutica)植物中提取出来的一个新的抗胆碱药,其化学结构和药理性质与东莨菪碱相似,中枢作用明显且毒性较小,临床上用于静脉注射中药复合麻醉获得良好效果。关于樟柳碱的中枢作用原理,据报道,此药能促进箭毒化猫大脑皮层乙酰胆碱(Ach)释放增加和皮层组织内Ach含量减少。利用离体大鼠大脑皮层

关键词：樟柳碱大鼠 anisodine 神经元放电中枢作用箭毒化药能复合麻醉药理性质皮层组织