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从莲花掌属植物中分离得到的杀利什曼原虫和逆转多重耐药成分。

Leishmanicidal and reversal multidrug resistance constituents from Aeonium lindleyi.

机构信息

Instituto Universitario de Bio-Orgánica Antonio González, Universidad de La Laguna, La Laguna, Tenerife, Spain.

出版信息

Planta Med. 2011 Jan;77(1):77-80. doi: 10.1055/s-0030-1250144. Epub 2010 Jul 21.

Abstract

A new bicyclic diterpene with a labdane skeleton, 7-oxo-labd-8-en-15-ol ( 1), along with two known diterpenes and ten flavonoids were isolated from the leaves of Aeonium lindleyi (Crassulaceae). Their structures were elucidated on the basis of spectroscopic data, including 1D and 2D NMR experiments, and comparison with spectroscopic data reported in the literature. Labdan-8 α,15-diol (2) and labd-8(17)-en-3 β,15-diol (3) showed leishmanicidal activity against Leishmania tropica (IC (50) = 77.0 µM) and Leishmania braziliensis (IC (50) = 68.0 µM) similar to ketoconazole used as positive control. 5,3'-Dihydroxy-3,7,4',5'-tetramethoxyflavone (8) and combretol (9) showed moderate activity (growth inhibition 87.3 and 73.0 %, respectively, at 50 µM) against a multidrug-resistant L. tropica line.

摘要

从长生草属(景天科)植物 Aeonium lindleyi 的叶子中分离得到一种具有贝壳杉烷骨架的新二环二萜 7-氧代贝壳杉-8-烯-15-醇(1),以及两种已知的二萜和十种类黄酮。根据光谱数据,包括 1D 和 2D NMR 实验,并与文献中报道的光谱数据进行比较,确定了它们的结构。贝壳杉烷-8α,15-二醇(2)和贝壳杉烷-8(17)-烯-3β,15-二醇(3)表现出对利什曼原虫热带株(IC50=77.0 μM)和利什曼原虫巴西株(IC50=68.0 μM)的杀利什曼原虫活性,与用作阳性对照的酮康唑相当。5,3'-二羟基-3,7,4',5'-四甲氧基黄酮(8)和考布醇(9)对一株多药耐药的利什曼原虫热带株表现出中等活性(在 50 μM 时的生长抑制率分别为 87.3%和 73.0%)。

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