Inhibition of HIV-1 integrase by galloyl glucoses from Terminalia chebula and flavonol glycoside gallates from Euphorbia pekinensis.
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.
Ahn
Mi-Jeong
MJ
Kim
Chul Young
CY
Lee
Ji Suk
JS
Kim
Tae Gyun
TG
Kim
Seung Hee
SH
Lee
Chong-Kyo
CK
Lee
Bo-Bin
BB
Shin
Cha-Gyun
CG
Huh
Hoon
H
Kim
Jinwoong
J
D001578:Benzopyrans / Q000494:pharmacology; D002240:Carbohydrate Sequence; D028481:Euphorbia; D005419:Flavonoids / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D005638:Fruit / Q000737:chemistry; D005707:Gallic Acid / Q000031:analogs & derivatives / Q000494:pharmacology*; D005960:Glucosides / Q000494:pharmacology; D006027:Glycosides / Q000494:pharmacology; D019427:HIV Integrase / Q000187:drug effects*; D019428:HIV Integrase Inhibitors / Q000494:pharmacology*; D047348:Hydrolyzable Tannins; D008969:Molecular Sequence Data; D015394:Molecular Structure; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology; D012194:RNA-Directed DNA Polymerase / Q000187:drug effects; D012431:Rutin / Q000494:pharmacology; D013634:Tannins / Q000494:pharmacology*; D029766:Terminalia
C106217:1,3,6-tri-O-galloylglucopyranose; D001578:Benzopyrans; D005419:Flavonoids; D005960:Glucosides; D006027:Glycosides; D019428:HIV Integrase Inhibitors; D047348:Hydrolyzable Tannins; D010936:Plant Extracts; D013634:Tannins; C076178:chebulagic acid; C435084:pentagalloylglucose; C060474:glucogallin; D012431:Rutin; D005707:Gallic Acid; D019427:HIV Integrase; D012194:RNA-Directed DNA Polymerase