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药理试验证明紫杉醇能有效抑制多种人癌细胞,包括KB细胞、HCT-8、A2780及MCF-7细胞的生长,IC50分别为0.0019,0.0036及0.01μg/ml。实验治疗指出,紫杉醇对黑色素瘤B-16,Walker癌肉瘤及对裸鼠的人卵巢癌异种移植瘤的生长有明显抑制作用。药理研究显示紫杉醇可促进微管蛋白聚合并抑制其解聚;明显影响L-1210细胞的周期移行,使细胞阻断在G2+M期。此外,还出现多倍体细胞群体。药代动力学参数:t1/2α为0.12h,t1/2β为5.02h,AUC为11.82(μg·h)/ml,Vc为0.50L/kg,CLs为0.42L/(h·kg)
Pharmacological tests show that paclitaxel can effectively inhibit the growth of a variety of human cancer cells, including KB cells, HCT-8, A2780 and MCF-7 cells with IC50 of 0.0019, 0.0036 and 0.01 μg / ml, respectively. Experimental treatment pointed out that paclitaxel significantly inhibited the growth of melanoma B-16, Walker Carcinosarcoma and human ovarian cancer xenografts in nude mice. Pharmacological studies have shown that paclitaxel can promote tubulin polymerization and depolymerization; significantly affect the cycle of L-1210 cells, blocking cells in the G2 + M phase. In addition, polyploid cell populations also appear. Pharmacokinetic parameters: t1 / 2α 0.12h, t1 / 2β 5.02h, AUC 11.82 (μg · h) / ml, Vc 0.50 L / kg, CLs 0.42 L / ( h · kg)