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在沙特阿拉伯生长的 Kleinia odora 三萜类成分的体外抗原生动物活性。

In vitro antiprotozoal activity of triterpenoid constituents of Kleinia odora growing in Saudi Arabia.

机构信息

Department of Pharmacognosy, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia.

出版信息

Molecules. 2013 Jul 31;18(8):9207-18. doi: 10.3390/molecules18089207.

Abstract

Two lupane and four ursane triterpenes, namely epilupeol (1), lupeol acetate (2), ursolic acid (3), brein (4), 3β 11α-dihydroxy urs-12-ene (5) and ursolic acid lactone (6) were isolated from aerial parts of Kleinia odora and identified. Compounds 1 and 3-6 were isolated for the first time from K. odora. The triterpene constituents were investigated for antiprotozoal potential against erythrocytic schizonts of Plasmodium falciparum, intracellular amastigotes of Leishmania infantum and Trypanosoma cruzi and free trypomastigotes of T. brucei. Cytotoxicity was determined against MRC-5 fibroblasts to assess selectivity. The ursane triterpenes were found to be active against more than one type of the tested parasites, with the exception of compound 6. This is also the first report on the occurrence of ursane type triterpenes in the genus Kleinia and their antiprotozoal potential against P. falciparum, L. infantum, T. cruzi, and T. brucei.

摘要

从 Kleinia odora 的地上部分分离得到了两种羽扇豆烷和四种熊果酸三萜类化合物,分别为表羽扇醇(1)、羽扇醇乙酸酯(2)、熊果酸(3)、brein(4)、3β11α-二羟基熊-12-烯(5)和熊果酸内酯(6)。化合物 1 和 3-6 均首次从 K. odora 中分离得到。对三萜类化合物进行了抗疟原虫(抗疟原虫裂殖体)、抗利什曼原虫(抗利什曼原虫内阿米巴)和锥虫(抗锥虫自由体)的活性测试,并用 MRC-5 成纤维细胞测定细胞毒性以评估选择性。除化合物 6 外,熊果酸三萜类化合物对多种类型的寄生虫均具有活性。这也是羽扇豆烷型三萜类化合物首次在 Kleinia 属中被发现,且具有抗疟原虫(抗疟原虫裂殖体)、抗利什曼原虫(抗利什曼原虫内阿米巴)、锥虫(抗锥虫自由体)的潜在作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8848/6269755/fcd2fc22ad4b/molecules-18-09207-g001.jpg

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