Isosinensetin exhibits HIV-1 protease inhibiting and antioxidant activities. It is a natural product isolated and purified from the fruit of Citrus aurantium L..
Isosinensetin, a polymethoxylated flavone extracted from pericarpium citri reticulatae viride, exhibits inhibition on P-glycoprotein (P-gp) in MDR1-MDCKII cells[3]. Isosinensetin, exhibited significant inhibition (>50 %) on OATP1B1 (Organic anion transporting polypeptide 1B1) in OATP1B1-HEK293 cells, which reduced the OATP1B1-mediated influx of methotrexate, accordingly decreased its cytotoxicity in OATP1B1-HEK293 cells and increased its AUC0-t in different extents in rats, from 28.27%-82.71 %. In bosentan-induced rat liver injury models, isosinensetin reduced the levels of serum total bile acid (TBA) and the liver concentration of bosentan in different degrees[4].
搜索
