Zinc coupling potentiates anti-HIV-1 activity of baicalin.
Baicalin (BA) has been shown with anti-HIV-1 activity. Zinc is a nutrient element. The anti-HIV-1 activity of zinc complex of baicalin (BA-Zn) in vitro was studied and compared with the anti-HIV-1 activities between BA and BA-Zn in the present study. Our results suggested that BA-Zn has lower cytotoxicity and higher anti-HIV-1 activity compared with those of BA in vitro. The CC50s of BA-Zn and BA were 221.52 and 101.73 microM, respectively. The cytotoxicity of BA-Zn was about 1.2-fold lower than that of BA. The BA and BA-Zn inhibited HIV-1 induced syncytium formation, HIV-1 p24 antigen and HIV-1 RT production. The EC50s of BA-Zn on inhibiting HIV-1 induced syncytium formation (29.08 microM) and RT production (31.17 microM) were lower than those of BA (43.27 and 47.34 microM, respectively). BA-Zn was more effective than BA in inhibiting the activities of recombinant RT and HIV-1 entry into host cells. Zinc coupling enhanced the anti-HIV-1 activity of baicalin.
Laboratory of Molecular Immunopharmacology, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming 650223, PR China.
Qian
Q
Wang
Yu-Tian
YT
Wang
Shao-Ping
SP
Pu
Yong-Tang
YT
Zheng
D019380:Anti-HIV Agents / Q000494:pharmacology*; D002460:Cell Line; D004396:Coloring Agents / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D004357:Drug Synergism; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D004797:Enzyme-Linked Immunosorbent Assay; D005419:Flavonoids / Q000494:pharmacology*; D016655:HIV Core Protein p24 / Q000737:chemistry; D054303:HIV Reverse Transcriptase / Q000737:chemistry; D015497:HIV-1 / Q000378:metabolism*; D006801:Humans; D008956:Models, Chemical; D011994:Recombinant Proteins / Q000737:chemistry; D013601:T-Lymphocytes / Q000378:metabolism / Q000821:virology; D013778:Tetrazolium Salts / Q000494:pharmacology; D013844:Thiazoles / Q000494:pharmacology; D013997:Time Factors; D015032:Zinc / Q000737:chemistry*
D019380:Anti-HIV Agents; D004396:Coloring Agents; D004791:Enzyme Inhibitors; D005419:Flavonoids; D016655:HIV Core Protein p24; D011994:Recombinant Proteins; D013778:Tetrazolium Salts; D013844:Thiazoles; C038044:baicalin; D054303:HIV Reverse Transcriptase; C022616:thiazolyl blue; D015032:Zinc