产品
编 号:F367011
分子式:C16H14O4
分子量:270.28
产品类型
结构图
CAS No: 480-37-5
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生物活性:
Pinostrobin is a flavonoid with anti-cancer, antioxidant, antiviral and neuroprotective activities. Pinostrobin has oral activity. Pinostrobin is a potent PCSK9 inhibitor that inhibits the catalytic activity of PCSK9. Pinostrobin can be used in the research of viral infections, cancer, leukemia, cardiovascular and cerebrovascular diseases, cirrhosis, inflammation and neurological diseases.
体内研究:
Pinostrobin (20 mg/kg , 50 mg/kg, i.g., daily for 7 days) 呈剂量依赖性地延缓 HSV-1 感染小鼠模型的病变发展。Pinostrobin (Single oral 10 and 20 mg/kg) 可通过抑制 LPS 诱导的炎症大鼠模型体内的 TNF-α 和 IL-1β 水平起到消炎作用。Pinostrobin (daily oral 30 and 60 mg/kg for 2 months) 对硫代乙酰胺 Thioacetamide (TAA) (HY-Y0698) 所致肝硬化大鼠具有肝保护作用。Pinostrobin在大鼠体内的相关药动学参数RouteDose (mg/kg)AUC0-t (ng·min/mL)MRT (h)Cmax (ng/mL)Tmax (h)t1/2 (min)
i.g.0.53817.806.26615.3544.34
Animal Model:Female Sprague Dawley (SD) rats (200–250 g), LPS (5 mg/kg) was administered after 2 h of the final dose.
Dosage:Single oral 10 and 20 mg/kg
Administration:p.o.
Result:Did not cause any signs of abnormal behavior and toxicity in the rats.Dose-dependent resulted in significant reductions in the levels of two cytokines, TNF-α and IL-1β.
Animal Model:healthy female male Sprague Dawley rats (6–7 weeks old, weighed between 180 and 210 g), Thioacetamide (HY-Y0698)-induced liver cirrhosis in rats
Dosage:daily oral 30 and 60 mg/kg for 2 months, single oral 500mg/kg
Administration:p.o.
Result:Significantly reduced liver index and hepatocyte proliferation in rats, and significantly reduce cell damage.Significantly down-regulated the expression levels of PCNA and α-SMA.The activities of antioxidant enzymes (SOD) and CAT in liver homogenate were increased, and the level of malondialdehyde (MDA) was decreased. The levels of serum bilirubin, total protein, albumin and liver enzymes (ALP, ALT and AST) recovered to normal.Decreased the levels of TNF-a and IL-6 and increased the levels of IL-10 in rats.Acute toxicity with a higher dose of 500 mg/kg Pinostrobin did not manifest any toxicological signs in rats.
体外研究:
Pinostrobin (0-100 μg/mL, 72 h) 抑制 HSV-1 病毒的 EC50 为 22.71 μg/mL。Pinostrobin (25-200 μM, 3 days) 通过刺激 cAMP/PKA 和 p38 MAPK 信号通路中相关黑色素生成调节因子的表达,促进 B16F10 细胞生成黑色素,且对细胞无毒性。Pinostrobin (130 and 150 μM, 48 h) 通过调控 miR-410-5p 和 SFRP5 诱导急性白血病细胞 NB4 和 MOLT-4 凋亡。Pinostrobin (0-200 μM, 24-96 h) 通过 ROS 介导的宫颈癌细胞 (HeLa, Ca Ski, SiHa) 线粒体损伤,有效地诱导细胞凋亡,同时对非癌细胞 HEK293 不具有毒性。