Isosinensetin

Isosinensetin is a flavonoid compound and an inhibitor of HIV-1 protease and PTP1B (IC₅₀: 2.61 µM; K_i: 0.92 µM). Isosinensetin inhibits P-glycoprotein (P-gp) in MDR1-MDCKII cells. Isosinensetin has multiple activities such as anti-tumor, anti-viral, anti-inflammatory, and antioxidant effects. Isosinensetin can be used in the research of various diseases including cancer, inflammation, osteoporosis, diabetes, etc^{[1][2][3][4][5]}. In Vitro:Isosinensetin (0.1-100 μM; 4-24 h) can significantly inhibit P-gp (IC₅₀: 4.2 μM), and increase the cytotoxicity induced by paraquat in MDR1-MDCKII cells^[1].
Isosinensetin (250 μg/mL) can inhibit erythrocyte hemolysis with an inhibition rate of 92.08%^[2].
Isosinensetin (40-80 μM; 1 h) can increase the intracellular calcium ion concentration, promote the expression of hTAS2R50 and proglucagon, and stimulate the secretion of GLP-1 in NCI-H716 cells ^[3].
Isosinensetin (0-10 μM; 0-7 days) can inhibit the formation of osteoclasts and their bone resorption function in BMMs. The mechanism involves the inhibition of the ROS-mediated NF-κB/MAPK signaling pathway^[4]. In Vivo:Isosinensetin (5-10 mg/kg; intraperitoneal injection; once every two days; 6 weeks) alleviates estrogen deficiency-induced osteoporosis in mice^[4].