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从越南千金藤中分离得到的生物碱的乙酰胆碱酯酶抑制活性

Acetylcholinesterase Inhibitory Activity of Alkaloids Isolated from Stephania venosa.

作者信息

Kongkiatpaiboon Sumet, Duangdee Nongnaphat, Prateeptongkum Saisuree, Chaijaroenkul Wanna

出版信息

Nat Prod Commun. 2016 Dec;11(12):1805-1806.

Abstract

Stephania venosa (Blume) Spreng or "Sa-Bu-Leud" is a Thai medicinal plant used for treatment of cancer and diabetes, and as a blood-tonic and aphrodisiac. This plant .ontains alkaloids as its major components and has been of interest for its acetylcholinesterase (AChE) inhibitory activity. Phytochemical screening - of S. venosa was made using HPLC analysis and showed the chemical variation between the same species from different provenances. Fractionation of .S..venosa extract yielded three alkaloids, namely, dicentrine, crebanine, and tetrahydropalmatine. AChE inhibitory potential of the isolated alkaloids was evaluated using Ellman's AChE inhibition assay. Dicentrine, crebanine, and tetrahydropalmatine inhibited-AChE activity with IC(50) values of 93.5, 86.6, and 168.6 μg/mL, respectively. The AChE inhibitory activity of the tertiary protoberberine alkaloid, tetrahydropalriiatine, was lower than that of the aporphine alkaloids, dicentrine and crebanine, whereas the quaternary protoberberine alkaloid, berberine, showed a higher AChE inhibitory effect than the others.

摘要

地不容(Stephania venosa (Blume) Spreng),又称“萨布勒德”,是一种泰国药用植物,用于治疗癌症和糖尿病,还可作为补血剂和壮阳药。这种植物主要成分是生物碱,其乙酰胆碱酯酶(AChE)抑制活性备受关注。采用高效液相色谱(HPLC)分析法对不同产地的地不容进行植物化学筛选,结果显示同一物种之间存在化学差异。地不容提取物经分离得到三种生物碱,即双苄基异喹啉碱、克班宁和延胡索乙素。采用埃尔曼AChE抑制试验评估分离出的生物碱的AChE抑制潜力。双苄基异喹啉碱、克班宁和延胡索乙素对AChE活性的抑制IC(50)值分别为93.5、86.6和168.6 μg/mL。叔胺原小檗碱类生物碱延胡索乙素的AChE抑制活性低于阿朴啡类生物碱双苄基异喹啉碱和克班宁,而季铵原小檗碱类生物碱小檗碱的AChE抑制作用则高于其他生物碱。

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