Abstract
The bioassay-directed isolation of Terminalia chebula fruits afforded four human immunodeficiency virus type 1 (HIV-1) integrase inhibitors, gallic acid ( 1) and three galloyl glucoses ( 2 - 4). In addition, four flavonol glycoside gallates ( 5 - 8) from Euphorbia pekinensis containing the galloyl moiety also showed the inhibitory activity at a level comparable to those of 2 - 4. By comparison with the activities of the compounds not bearing this moiety, it is proposed that the galloyl moiety plays a major role for inhibition against the 3'-processing of HIV-1 integrase of these compounds.
Publication types
-
Letter
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Benzopyrans / pharmacology
-
Carbohydrate Sequence
-
Euphorbia*
-
Flavonoids / chemistry
-
Flavonoids / isolation & purification
-
Flavonoids / pharmacology
-
Fruit / chemistry
-
Gallic Acid / analogs & derivatives
-
Gallic Acid / pharmacology*
-
Glucosides / pharmacology
-
Glycosides / pharmacology
-
HIV Integrase / drug effects*
-
HIV Integrase Inhibitors / pharmacology*
-
Hydrolyzable Tannins*
-
Molecular Sequence Data
-
Molecular Structure
-
Plant Extracts / chemistry
-
Plant Extracts / pharmacology
-
RNA-Directed DNA Polymerase / drug effects
-
Rutin / pharmacology
-
Tannins / pharmacology*
-
Terminalia*
Substances
-
1,3,6-tri-O-galloylglucopyranose
-
Benzopyrans
-
Flavonoids
-
Glucosides
-
Glycosides
-
HIV Integrase Inhibitors
-
Hydrolyzable Tannins
-
Plant Extracts
-
Tannins
-
chebulagic acid
-
pentagalloylglucose
-
glucogallin
-
Rutin
-
Gallic Acid
-
HIV Integrase
-
RNA-Directed DNA Polymerase