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从韩国三叶爬山虎中分离出的新型芪衍生物的抗疟活性。

Antiplasmodial activity of novel stilbene derivatives isolated from Parthenocissus tricuspidata from South Korea.

作者信息

Son Il Hong, Chung Ill-Min, Lee Sun-Joo, Moon Hyung-In

机构信息

Inam Neuro Science Research Center, Department of Neurology, Wonkwang University Sanbon Medical Center, Sanbon-dong, Gunpo-city, Kyunggi-Do 435-040, South Korea.

出版信息

Parasitol Res. 2007 Jun;101(1):237-41. doi: 10.1007/s00436-006-0454-y. Epub 2007 Jan 9.

DOI:10.1007/s00436-006-0454-y
PMID:17211658
Abstract

New stilbene glycoside, piceid-(1-->6)-beta-D -glucopyranoside (compound 2, Fig. 1), was isolated from the MeOH extract of the leaves of Parthenocissus tricuspidata (Vitaceae) together with four known compounds, piceid (compound 1, Fig. 1), resveratrol (compound 3, Fig. 1), longistylin A (compound 4, Fig. 1), and longistylin C (compound 5, Fig. 1). Their structures were determined spectroscopically, particularly by 2D nuclear magnetic resonance (NMR) spectroscopic and chemical analysis. The antiplasmodial activity of isolated compounds were determined in vitro against a chloroquine-sensitive strain of Plasmodium falciparum (D10). Among the compounds isolated, piceid-(1-->6)-beta-D-glucopyranoside (2) had the most potential inhibition, with inhibitory concentration (IC(50)) values of 5.3 microM. To our knowledge, antiplasmodial activity of functional group position of stilbene is now being reported for the first time in this study. The result shows that the 3, 4'-position in stilbenes might play an essential role in antiplasmodial activity.

摘要

新的芪糖苷,白藜芦醇-(1→6)-β-D-吡喃葡萄糖苷(化合物2,图1),与四种已知化合物,白藜芦醇苷(化合物1,图1)、白藜芦醇(化合物3,图1)、长柱香蒲素A(化合物4,图1)和长柱香蒲素C(化合物5,图1)一起,从爬山虎(葡萄科)叶片的甲醇提取物中分离得到。它们的结构通过光谱学方法确定,特别是二维核磁共振(NMR)光谱和化学分析。对分离得到的化合物进行体外抗疟活性测定,针对氯喹敏感的恶性疟原虫(D10)株。在分离得到的化合物中,白藜芦醇-(1→6)-β-D-吡喃葡萄糖苷(2)具有最强的潜在抑制作用,抑制浓度(IC50)值为5.3微摩尔。据我们所知,本研究首次报道了芪官能团位置的抗疟活性。结果表明,芪类化合物中的3,4'-位在抗疟活性中可能起重要作用。

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