Inhibition of HIV infection by baicalin--a flavonoid compound purified from Chinese herbal medicine.
Baicalin (BA), (formulated as 7-D-glucuronic acid-5,6-dihydroxy-flavone), was purified from the plant Scutellaria Baicalensis Georgi. It has been used as a traditional Chinese herbal medicine. The inhibitory effect of BA against human immunodeficiency virus (HIV-1) infection and replication has been studied in vitro. The compound inhibits HIV-1 infection and replication as measured by: (1) a quantitative focal syncytium formation on CEM-ss monolayer cells; and (2) HIV-1 specific core antigen p24 expression and retroviral reverse transcriptase (RT) activity in the HIV-1-infected H9 cells. We have further demonstrated that the enzymatic activity of purified recombinant HIV-1/RT was inhibited by BA. In addition to lymphoid cell lines, the anti-HIV-1 activity of BA was also observed in cultures of primary human peripheral blood mononuclear cells infected with HIV-1 in vitro. Neither cytotoxic nor cytostatic effects on the indicator cells were found under the assay condition. This data suggests that BA may serve as a useful drug for the treatment and prevention of HIV infections.
Li
B Q
BQ
Biological Carcinogenesis and Development Program, Program Resources Inc./DynCorp, National Cancer Institute-Frederick Cancer Research and Development Center, MD 21202-1201.
Fu
T
T
Yan
Y D
YD
Baylor
N W
NW
Ruscetti
F W
FW
Kung
H F
HF
D000998:Antiviral Agents / Q000494:pharmacology*; D015496:CD4-Positive T-Lymphocytes / Q000382:microbiology; D002478:Cells, Cultured; D003588:Cytopathogenic Effect, Viral / Q000187:drug effects; D004365:Drugs, Chinese Herbal / Q000494:pharmacology*; D005419:Flavonoids / Q000494:pharmacology*; D016655:HIV Core Protein p24 / Q000096:biosynthesis; D054303:HIV Reverse Transcriptase; D015497:HIV-1 / Q000187:drug effects* / Q000502:physiology; D006801:Humans; D007963:Leukocytes, Mononuclear / Q000382:microbiology; D018894:Reverse Transcriptase Inhibitors; D014779:Virus Replication / Q000187:drug effects
D000998:Antiviral Agents; D004365:Drugs, Chinese Herbal; D005419:Flavonoids; D016655:HIV Core Protein p24; D018894:Reverse Transcriptase Inhibitors; C038044:baicalin; D054303:HIV Reverse Transcriptase