Abstract
A new compound, 1,3,4,5-tetragalloylapiitol ( 1), was isolated from the aqueous extract of the plant Hylodendron gabunensis and was found to be a potent inhibitor of RNase H enzymatic activity. The structure of 1 was elucidated by NMR analyses to be an apiitol ( 2) sugar moiety substituted with four gallic acid residues. Optical rotation measurements of the free sugar following basic hydrolysis indicated that the 3 S absolute configuration was the same as that of d-apiitol. Compound 1 inhibited HIV-1, HIV-2, and human RNase H with IC 50 values of 0.24, 0.13, and 1.5 microM, respectively, but it did not show inhibition of E. coli RNase H at 10 microM.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, N.I.H., Intramural
MeSH terms
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Anti-HIV Agents / chemistry
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Anti-HIV Agents / isolation & purification*
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Anti-HIV Agents / pharmacology*
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Cameroon
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Erythritol / analogs & derivatives*
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Erythritol / chemistry
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Erythritol / isolation & purification
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Erythritol / pharmacology
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Fabaceae / chemistry*
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HIV-1 / drug effects
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HIV-2 / drug effects
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Humans
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Inhibitory Concentration 50
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Molecular Structure
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Plant Leaves / chemistry
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Plants, Medicinal / chemistry*
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Ribonuclease H / antagonists & inhibitors*
Substances
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1,3,4,5-tetragalloylapiitol
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Anti-HIV Agents
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3-(hydroxymethyl)erythritol
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Ribonuclease H
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Erythritol