Kimura Y, Okuda H, Ogita Z
2nd Department of Medical Biochemistry, School of Medicine, Ehime University, Japan.
J Nat Prod. 1997 Jun;60(6):598-601. doi: 10.1021/np970035l.
Studies on the effects of flavonoids isolated from the roots of Scutellaria baicalensis on the fibrinolytic system induced by trypsin in cultured human umbilical vein endothelial cells (HUVECs) showed that baicalein (1) strongly inhibited the reduction of t-PA production and the elevation of PAI-1 production induced by trypsin. The IC50 for PAI-1 production was 3.7 microM. In addition, wogonin (3), oroxylin A (5), skullcapflavone II (6), and 2',5,5',7-tetrahydroxy-6',8-dimethoxyflavone (7) inhibited the elevation of PAI-1 induced by trypsin, though less strongly; their IC50 were 105, 61, 110, and 88 microM, respectively. These findings suggest that baicalein prevents the thrombotic tendency induced by trypsin.
对从黄芩根部分离出的黄酮类化合物对培养的人脐静脉内皮细胞(HUVECs)中胰蛋白酶诱导的纤维蛋白溶解系统的影响进行的研究表明,黄芩素(1)强烈抑制胰蛋白酶诱导的组织型纤溶酶原激活物(t-PA)产生的减少和纤溶酶原激活物抑制剂-1(PAI-1)产生的升高。PAI-1产生的半数抑制浓度(IC50)为3.7微摩尔。此外,汉黄芩素(3)、木犀草素A(5)、黄芩黄酮II(6)和2',5,5',7-四羟基-6',8-二甲氧基黄酮(7)抑制胰蛋白酶诱导的PAI-1升高,但其作用较弱;它们的IC50分别为105、61、110和88微摩尔。这些发现表明黄芩素可预防胰蛋白酶诱导的血栓形成倾向。