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.
Publication types
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Comparative Study
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Research Support, Non-U.S. Gov't
MeSH terms
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Anti-HIV Agents / chemistry*
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Anti-HIV Agents / pharmacology*
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CD4 Antigens / metabolism
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Cells, Cultured
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Gallic Acid / analogs & derivatives
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Gallic Acid / chemistry
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Gallic Acid / pharmacology
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Glucosides / chemistry
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Glucosides / pharmacology
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HIV Envelope Protein gp120 / metabolism
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HIV Protease Inhibitors / chemistry
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HIV Protease Inhibitors / pharmacology
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HIV-1 / drug effects*
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HIV-1 / growth & development
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Plant Extracts / chemistry
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Plant Extracts / pharmacology
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Plants, Medicinal / chemistry*
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Protein Binding
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Protein Processing, Post-Translational / drug effects
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Virus Replication / drug effects
Substances
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2-phenylethanol-O-(6-O-galloyl)glucopyranoside
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Anti-HIV Agents
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CD4 Antigens
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Glucosides
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HIV Envelope Protein gp120
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HIV Protease Inhibitors
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Plant Extracts
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Gallic Acid