Inhibition of reverse transcriptase activity by a flavonoid compound, 5,6,7-trihydroxyflavone.
5,6,7-Trihydroxyflavone (baicalein) is a potent inhibitor of the activities of reverse transcriptases from murine leukemia viruses (MLV) (Rauscher and Moloney strains) and human immunodeficiency virus (HIV). Under the reaction conditions specified for each of the MLV- and HIV-reverse transcriptases, both enzyme activities were inhibited by more than 90% in the presence of 2 micrograms/ml baicalein. The mode of the inhibition by baicalein was competitive with respect to the template.primer, (rA)n.(dT)12-18, and noncompetitive to dTTP substrate. Ki value of baicalein for the MLV-reverse transcriptase was determined to be 0.37 microM.
Ono
K
K
Laboratory of Viral Oncology, Aichi Cancer Center Research Institute, Nagoya, Japan.
Nakane
H
H
Fukushima
M
M
Chermann
J C
JC
Barré-Sinoussi
F
F
D001667:Binding, Competitive; D044950:Flavanones; D005419:Flavonoids / Q000494:pharmacology*; D015497:HIV-1 / Q000201:enzymology*; D008979:Moloney murine leukemia virus / Q000201:enzymology*; D019384:Nucleic Acid Synthesis Inhibitors; D011925:Rauscher Virus / Q000201:enzymology*; D018894:Reverse Transcriptase Inhibitors; D013942:Thymine Nucleotides / Q000378:metabolism
D044950:Flavanones; D005419:Flavonoids; D019384:Nucleic Acid Synthesis Inhibitors; D018894:Reverse Transcriptase Inhibitors; D013942:Thymine Nucleotides; C006680:baicalein; C024157:thymidine 5'-triphosphate