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马达加斯加干燥森林中 Athroisma proteiforme 的抗疟原虫和抗增殖伪愈创木烷型倍半萜。

Antiplasmodial and antiproliferative pseudoguaianolides of Athroisma proteiforme from the Madagascar Dry Forest.

机构信息

Department of Chemistry, M/C 0212, Virginia Tech, Blacksburg, Virginia 24061, United States.

出版信息

J Nat Prod. 2011 Oct 28;74(10):2174-80. doi: 10.1021/np200499d. Epub 2011 Oct 13.

Abstract

Investigation of extracts from the plant Athroisma proteiforme (Humbert) Mattf. (Asteraceae) for antimalarial activity led to the isolation of the five new sesquiterpene lactones 1-5 together with centaureidin (6). The structures of the new compounds were deduced from analyses of physical and spectroscopic data, and the absolute configuration of compound 1 was confirmed by an X-ray crystallographic study. Athrolides C (3) and D (4) both showed antiplasmodial activities with IC50 values of 6.6 (3) and 7.2 μM (4) against the HB3 strain and 5.5 (3) and 4.2 μM (4) against the Dd2 strain of the malarial parasite Plasmodium falciparum. The isolates 1-6 also showed antiproliferative activity against A2780 human ovarian cancer cells, with IC50 values ranging from 0.4 to 2.5 μM.

摘要

对植物 Athroisma proteiforme (Humbert) Mattf.(菊科)提取物进行抗疟活性研究,分离得到了五个新的倍半萜内酯化合物 1-5 以及 centaureidin(6)。新化合物的结构是通过分析物理和光谱数据推断出来的,化合物 1 的绝对构型通过 X 射线晶体学研究得到了确认。Athrolides C(3)和 D(4)均表现出抗疟原虫活性,对 HB3 株疟原虫 Plasmodium falciparum 的 IC50 值分别为 6.6(3)和 7.2 μM(4),对 Dd2 株的 IC50 值分别为 5.5(3)和 4.2 μM(4)。化合物 1-6 对人卵巢癌细胞 A2780 也具有抗增殖活性,IC50 值范围为 0.4-2.5 μM。

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