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柳叶醉鱼草叶中萜类化合物的α-葡萄糖苷酶抑制和抗疟特性

Alpha-glucosidase inhibitory and antiplasmodial properties of terpenoids from the leaves of Buddleja saligna Willd.

作者信息

Chukwujekwu Jude C, Rengasamy Kannan R R, de Kock Carmen A, Smith Peter J, Slavětínská Lenka Poštová, van Staden Johannes

机构信息

a Research Centre for Plant Growth and Development, School of Life Sciences , University of KwaZulu-Natal , Pietermaritzburg , Scottsville , South Africa .

b Department of Medicine, Division of Pharmacology , University of Cape Town , Cape Town , South Africa , and.

出版信息

J Enzyme Inhib Med Chem. 2016;31(1):63-6. doi: 10.3109/14756366.2014.1003927. Epub 2015 Feb 19.

DOI:10.3109/14756366.2014.1003927
PMID:25694064
Abstract

In our continuing search for biologically active natural product(s) of plant origin, Buddleja saligna, a South African medicinal plant, was screened in line with its traditional use for antidiabetic (yeast alpha glucosidase inhibitory) and antiplasmodial (against a chloroquine sensitive strain of Plasmodium falciparum (NF54)) activities. The hexane fraction showed the most promising activity with regards to its antidiabetic (IC(50) = 260 ± 0.112 µg/ml) and antiplasmodial (IC(50) = 8.5 ± 1.6 µg/ml) activities. Using activity guided fractionation three known terpenoids (betulonic acid, betulone and spinasterol) were isolated from this species for the first time. The compounds displayed varying levels of biological activities (antidiabetic: 27.31 µg/ml ≥ IC(50) ≥ 5.6 µg/ml; antiplasmodial: 14 µg/ml ≥ IC(50) ≥ 2 µg/ml) with very minimal toxicity.

摘要

在我们对具有生物活性的植物源天然产物的持续探索中,南非药用植物柳叶醉鱼草,根据其抗糖尿病(酵母α-葡萄糖苷酶抑制)和抗疟(针对氯喹敏感的恶性疟原虫株(NF54))的传统用途进行了筛选。己烷馏分在抗糖尿病(IC(50) = 260 ± 0.112 µg/ml)和抗疟(IC(50) = 8.5 ± 1.6 µg/ml)活性方面表现出最有前景的活性。通过活性导向分级分离,首次从该物种中分离出三种已知的萜类化合物(桦木酸、桦木酮和菠菜甾醇)。这些化合物表现出不同程度的生物活性(抗糖尿病:27.31 µg/ml ≥ IC(50) ≥ 5.6 µg/ml;抗疟:14 µg/ml ≥ IC(50) ≥ 2 µg/ml),且毒性极小。

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