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从大马士革蔷薇中分离出的纯化合物的抗HIV活性及作用机制。

The anti-HIV activity and mechanisms of action of pure compounds isolated from Rosa damascena.

作者信息

Mahmood N, Piacente S, Pizza C, Burke A, Khan A I, Hay A J

机构信息

MRC Collaborative Centre, London, United Kingdom.

出版信息

Biochem Biophys Res Commun. 1996 Dec 4;229(1):73-9. doi: 10.1006/bbrc.1996.1759.

Abstract

Water and methanol extracts of Rosa damascena exhibited moderate anti-HIV activity. The anti-viral activities of 9 compounds isolated from the methanol extract were compared. The tetrahydroxyflavanone (kaempferol, 1), was effective in reducing the maturation of infectious progeny virus apparently due to selective inhibition of the viral protease. On the other hand the pentahydroxyflavone (quercetin, 2) and two 3-substituted derivatives of kaempferol appeared to inhibit HIV-infection by preventing binding of gp120 to CD4. 2-Phenylethanol-O-(6-O-galloyl)-beta-D-glucopyranoside 8 interacted irreversibly with gp120 and neutralized virus infectivity. The differences in the modes of action of 1 and 8 can account for the apparent synergy of their anti-viral activities.

摘要

大马士革蔷薇的水提取物和甲醇提取物表现出中等程度的抗HIV活性。对从甲醇提取物中分离出的9种化合物的抗病毒活性进行了比较。四羟基黄酮(山奈酚,1)能有效降低感染性子代病毒的成熟,这显然是由于对病毒蛋白酶的选择性抑制。另一方面,五羟基黄酮(槲皮素,2)和山奈酚的两种3-取代衍生物似乎通过阻止gp120与CD4结合来抑制HIV感染。2-苯基乙醇-O-(6-O-没食子酰基)-β-D-吡喃葡萄糖苷8与gp120发生不可逆相互作用并中和病毒感染性。1和8作用方式的差异可以解释它们抗病毒活性明显的协同作用。

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