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生物活性导向分离麻疯树中的脂氧合酶和环氧化酶抑制成分

Bioactivity-guided fractionation of the lipoxygenase and cyclooxygenase inhibiting constituents from Chisocheton polyandrus Merr.

机构信息

Department of Pharmacy, Faculty of Medicine, University of Malaya, 50603 Kuala Lumpur, Malaysia.

出版信息

Fitoterapia. 2012 Jul;83(5):961-7. doi: 10.1016/j.fitote.2012.04.018. Epub 2012 Apr 28.

Abstract

Lipoxygenase (LOX)-inhibiting compounds from the leaves of Chisocheton polyandrus Merr. were isolated in this study using a bioactivity-guided fractionation technique. Two dammarane triterpenoids, dammara-20,24-dien-3-one (1) (IC(50)=0.69±0.07 μM) and 24-hydroxydammara-20,25-dien-3-one (2) (IC(50)=1.11±0.38 μM), were isolated and identified based on the soybean LOX assay. Dammara-20,24-dien-3-one (1) exhibited dual inhibition of both human 5-LOX (IC(50)=24.27±2.92 μM) and cyclooxygenase-2 (COX-2) (IC(50)=3.17±0.90 μM), whereas 24-hydroxydammara-20,25-dien-3-one (2) did not exhibit any significant inhibitory effects. This report is the first to detail the inhibition of LOX and COX by both C. polyandrus and its isolated compounds.

摘要

本研究采用生物活性导向分离技术,从乌桕树叶中分离到具有脂氧合酶(LOX)抑制活性的化合物。根据大豆 LOX 测定法,从分离得到的两种达玛烷三萜类化合物中鉴定出 20,24-二烯-3-酮(1)(IC50=0.69±0.07 μM)和 24-羟基-20,25-二烯-3-酮(2)(IC50=1.11±0.38 μM)。化合物 1 对人 5-脂氧合酶(IC50=24.27±2.92 μM)和环氧化酶-2(COX-2)(IC50=3.17±0.90 μM)均表现出双重抑制作用,而 24-羟基-20,25-二烯-3-酮(2)则没有表现出明显的抑制作用。本报告首次详细报道了乌桕及其分离化合物对 LOX 和 COX 的抑制作用。

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