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紫花前胡酮类衍生物的抗疟原虫和细胞毒性活性研究

Antiplasmodial and cytotoxic activity of khellactone derivatives from Angelica purpuraefolia Chung.

机构信息

Department of Applied Life Science, Kon Kuk University, Seoul, 143-701, South Korea.

出版信息

Phytother Res. 2010 Mar;24(3):469-71. doi: 10.1002/ptr.3056.

DOI:10.1002/ptr.3056
PMID:19960419
Abstract

The methanolic extract of the rhizomes parts of Agelica purpuraefolia was investigated for its activity against chloroquine-sensitive strains of Plasmodium falciparum using the parasite lactate dehydrogenase assay method. Two natural khellactone, (+)-4'-Decanoyl-cis-khellactone (1) and (+)-3'-Decanoyl-cis-khellactone (2) were isolated from the rhizomes parts of A. purpuraefolia. Two compounds were evaluated for in vitro antiplasmodial activities as well as their cytotoxic potential on SK-OV-3 cancer cell line cells. Compounds 1, 2 showed notable growth inhibitory activity against chloroquine-sensitive strains of Plasmodium falciparum with IC(50) values from 1.5 and 2.4 microM. This compound showed no significant cytotoxicity (IC(50) > 100 microM) evaluated using SK-OV-3 cancer cell line cells. This is the first report on the antiplasmodial activity of the compounds from A. purpuraefolia.

摘要

紫茎泽兰根部分的甲醇提取物,通过寄生虫乳酸脱氢酶试验方法,研究其对氯喹敏感株恶性疟原虫的活性。从紫茎泽兰的根部分离得到两种天然的对映贝壳杉烯酮,(+)-4′-癸酰基-顺式贝壳杉烯酮(1)和(+)-3′-癸酰基-顺式贝壳杉烯酮(2)。两种化合物被评估了体外抗疟原虫活性以及对 SK-OV-3 癌细胞的细胞毒性。化合物 1、2 对氯喹敏感株恶性疟原虫表现出显著的生长抑制活性,IC(50)值为 1.5 和 2.4μM。使用 SK-OV-3 癌细胞系细胞,该化合物没有显示出明显的细胞毒性(IC(50)>100μM)。这是首次报道来自紫茎泽兰的化合物的抗疟原虫活性。

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