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

The anti-HIV activity and mechanisms of action of pure compounds isolated from Rosa damascena
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DOI:
10.1006/bbrc.1996.1759
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发表时间:
1996-12-04
影响因子:
3.1
通讯作者:
Hay, AJ
Hay, AJ
中科院分区:
生物学4区
文献类型:
--
作者:
Mahmood, N;Piacente, S;Hay, AJ

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野蔷薇的水提取物和甲醇提取物具有一定的抗HIV活性。比较了9个化合物的抗病毒活性。四羟基黄烷酮(山奈酚,1),是有效地减少感染性子代病毒的成熟,显然是由于选择性抑制病毒蛋白酶,另一方面,五羟基黄酮(槲皮素,2)和山奈酚的两个3-取代衍生物似乎抑制HIV感染,通过阻止结合的gp 120的CD 4。2-苯乙醇-O-(6-O-没食子酰基)-β-D-吡喃葡萄糖苷8与gp 120不可逆地相互作用并中和病毒感染性。1和8的作用模式的差异可以解释它们的抗病毒活性的明显协同作用。(C)出版社:Academic Press,Inc.
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. (C) 1996 Academic Press, Inc.