Inhibition of reverse transcriptases by flavonoids.
Selected naturally occurring flavonoids were shown to inhibit three reverse transcriptases (RT): avian myeloblastosis (AMV) RT, Rous-associated virus-2 (RAV-2) RT and Maloney murine leukemia virus (MMLV) RT when poly (rA)oligo(dT)12-18 or rabbit globin mRNA were used as template. Amentoflavone, scutellarein and quercetin were the most active compounds and their effect was concentration-dependent. The enzymes exhibited differential sensitivity to the inhibitory effects of the flavonoids. The compounds also inhibited rabbit globin mRNA-directed, MMLV RT-catalyzed DNA synthesis. Amentoflavone and scutellarein inhibited ongoing new DNA synthesis catalyzed by RAV-2 RT. Kinetic studies were performed in an attempt to elucidate the mechanism of action of amentoflavone and scutellarein. A model is proposed for the mechanism of action of the flavonoids on RT activity.
Spedding
G
G
Department of Medicine, State University of New York, Buffalo General Hospital 14203.
Ratty
A
A
Middleton
E
E
D000818:Animals; D001354:Avian Leukosis Virus / Q000201:enzymology; D009189:Avian Myeloblastosis Virus / Q000201:enzymology; D044946:Biflavonoids; D044950:Flavanones; D005419:Flavonoids / Q000494:pharmacology*; D007700:Kinetics; D015394:Molecular Structure; D008979:Moloney murine leukemia virus / Q000201:enzymology; D011794:Quercetin / Q000494:pharmacology*; D012190:Retroviridae / Q000201:enzymology*; D018894:Reverse Transcriptase Inhibitors; D047310:Apigenin
D044946:Biflavonoids; D044950:Flavanones; D005419:Flavonoids; D011794:Quercetin; D018894:Reverse Transcriptase Inhibitors; C011164:amentoflavone; C458179:scutellarein; D047310:Apigenin