来自巴基斯坦药用植物凝固茄（Withania coagulans）的具有杀利什曼原虫活性的睡茄内酯
Leishmanicidal active withanolides from a pakistani medicinal plant, Withania coagulans.
作者信息
Kuroyanagi Masanori, Murata Miki, Nakane Takahisa, Shirota Osamu, Sekita Setsuko, Fuchino Hiroyuki, Shinwari Zabta K
机构信息
Faculty of Pharmaceutical Sciemces at Kagawa Campus, Tokushima Bunri Universiyty, Shido, Sanuki, Kagawa, Japan.
出版信息
Chem Pharm Bull (Tokyo). 2012;60(7):892-7. doi: 10.1248/cpb.c12-00264.
In the course of screening for leishmanicidal constituents from Asian and South American medicinal plants, a Pakistani medicinal plant, Withania coagulans, showed activity. We therefore studied the active components of the methanol extract of aerial parts of W. coagulans. From the ethyl acetate soluble fraction of the extract, four new withanolides (1-4) were isolated along with seven known withanolides (5-11). The new compounds were elucidated to be (14R,15R,17S,20S,22R)-14,15,17,20-tetrahydroxy-1-oxowitha-2,5,24-trienolide (1), (14R,15R,17S,20S,22R)-14,15,17,20-tetrahydroxy-1-oxowitha-3,5,24-trienolide (2), (14S,17R,20S,22R)-14,17,20-trihydroxy-1-oxowitha-2,5,24-trienolide (3), and (14S,17R,20S,22R)-14,17,20-trihydroxy-1-oxowitha-3,5,24-trienolide (4), from 1H-NMR, 13C-NMR, 2D-NMR and high resolution (HR)-MS data. Some of these compounds having the partial structure 1-oxo-2,5-diene showed strong leishmanicidal activity against Leishmania major.
在从亚洲和南美洲药用植物中筛选抗利什曼原虫成分的过程中，一种巴基斯坦药用植物——凝固茄表现出了活性。因此，我们研究了凝固茄地上部分甲醇提取物的活性成分。从该提取物的乙酸乙酯可溶部分中，分离出了4个新的睡茄内酯（1 - 4）以及7个已知的睡茄内酯（5 - 11）。通过¹H - NMR、¹³C - NMR、二维NMR和高分辨（HR）- MS数据，确定新化合物为（14R，15R，17S，20S，22R）- 14,15,17,20 - 四羟基 - 1 - 氧代 - 威 - 2,5,24 - 三烯醇内酯（1）、（14R，15R，17S，20S，22R）- 14,15,17,20 - 四羟基 - 1 - 氧代 - 威 - 3,5,24 - 三烯醇内酯（2）、（14S，17R，20S，22R）- 14,17,20 - 三羟基 - 1 - 氧代 - 威 - 2,5,24 - 三烯醇内酯（3）和（14S，17R，20S，22R）- 14,17,20 - 三羟基 - 1 - 氧代 - 威 - 3,5,24 - 三烯醇内酯（4）。这些具有部分结构1 - 氧代 - 2,5 - 二烯的化合物中，有些对硕大利什曼原虫表现出很强的抗利什曼原虫活性。
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