Synthesis of azaisoflavones and their inhibitory activities of NO production in activated microglia.
A series of azaisoflavones were synthesized and their biological activities were evaluated for nitric oxide (NO) production and inducible NO synthase (iNOS) expression in BV-2 microglia cell lines. Among these compounds, compound 8d was the most potent with IC(50) 7.83 microM for inhibition of NO production. Also, compound 8d inhibited expression of iNOS in LPS-induced BV2 cells. This result suggests that compound 8d inhibited the production of NO by suppressing the expression of iNOS.
Jin
Guo Hua
GH
College of Pharmacy, Sookmyung Women's University, 52 Hyochangwon-Gil, Yongsan-Gu, Seoul 140-742, Republic of Korea.
Ha
Sang Keun
SK
Park
Hye Min
HM
Kang
Bomi
B
Kim
Sun Yeou
SY
Kim
Hee-Do
HD
Ryu
Jae-Ha
JH
Jeon
Raok
R
D000818:Animals; D002460:Cell Line; D002626:Chemistry, Pharmaceutical / Q000379:methods; D015195:Drug Design; D020128:Inhibitory Concentration 50; D007529:Isoflavones / Q000737:chemistry*; D051379:Mice; D017628:Microglia / Q000187:drug effects / Q000378:metabolism*; D008956:Models, Chemical; D009569:Nitric Oxide / Q000737:chemistry*; D052247:Nitric Oxide Synthase Type II / Q000378:metabolism*; D015363:Quinolones / Q000737:chemistry; D013696:Temperature; D013778:Tetrazolium Salts / Q000494:pharmacology; D013844:Thiazoles / Q000494:pharmacology
D007529:Isoflavones; D015363:Quinolones; D013778:Tetrazolium Salts; D013844:Thiazoles; D009569:Nitric Oxide; D052247:Nitric Oxide Synthase Type II; C022616:thiazolyl blue