Baicalin, an inhibitor of HIV-1 production in vitro.
The flavonoid baicalin markedly inhibits replication of human immunodeficiency virus type 1 (HIV-1) in a concentration-dependent manner in normal peripheral blood mononuclear cells (PBMC) stimulated with phytohemagglutinin (PHA) in vitro. The effect was more pronounced when the cells were pretreated with baicalin. Furthermore, baicalin inhibits HIV-1 replication in PHA-stimulated PBMC from asymptomatic HIV-1-seropositive carriers. The 50% inhibitory concentration for HIV-1 replication was approximately 0.5 microg/ml. At the concentration of 2 microg/ml of baicalin, copy numbers of HIV-1 proviral DNA were approximately 50 times less than in untreated controls. In a cell-free infection system, baicalin inhibited the activity of HIV-1 reverse transcriptase (RT), but not the activity of human DNA polymerases alpha and gamma (DNA polymerase beta was slightly inhibited), suggesting that the anti-HIV-1 effect of baicalin may at least partly be due to inhibition of HIV-1 RT.
Kitamura
K
K
AIDS Research Center, National Institute of Infectious Diseases, Tokyo, Japan.
Honda
M
M
Yoshizaki
H
H
Yamamoto
S
S
Nakane
H
H
Fukushima
M
M
Ono
K
K
Tokunaga
T
T
D019380:Anti-HIV Agents / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use / Q000633:toxicity; D015704:CD4 Antigens / Q000187:drug effects / Q000378:metabolism; D002478:Cells, Cultured; D005419:Flavonoids / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use / Q000633:toxicity; D015699:HIV Envelope Protein gp120 / Q000187:drug effects / Q000378:metabolism; D015658:HIV Infections / Q000188:drug therapy*; D054303:HIV Reverse Transcriptase / Q000378:metabolism; D015497:HIV-1 / Q000187:drug effects* / Q000235:genetics; D006801:Humans; D007963:Leukocytes, Mononuclear / Q000187:drug effects / Q000821:virology; D015394:Molecular Structure
D019380:Anti-HIV Agents; D015704:CD4 Antigens; D005419:Flavonoids; D015699:HIV Envelope Protein gp120; C038044:baicalin; D054303:HIV Reverse Transcriptase