描述 |
甲磺酸Crinatol(BWA770U)是一种口服活性和抗癌剂,是DNA插入剂中芳基甲基氨基丙二醇类的成员。甲磺酸克司他醇对人乳腺癌症细胞具有体外细胞毒性,但对正常人皮肤成纤维细胞没有细胞毒性[1][2][3]。
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相关类别 |
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体外研究 |
甲磺酸Crinatol(1.3μg/mL;24-72小时)抑制 HepG2细胞细胞的复制,使细胞活力降低 35%[2]。 细胞活力测定[2]细胞系:HepG2细胞浓度:1.3μg/mL培养时间:24小时、48小时、72小时和126小时结果:48小时时细胞活力受到抑制。
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体内研究 |
甲磺酸Crinatol(25 mg/kg;口服;单剂量)显示出口服活性,并通过放射自显影显示大鼠粪便提取物的稳定代谢物谱[2]。
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参考文献 |
[1]. Adams DJ. In vitro pharmacodynamic assay for cancer drug development: application to crisnatol, a new DNA intercalator. Cancer Res. 1989 Dec 1;49(23):6615-20. [2]. Patel DK, et al. Metabolism of a novel antitumor agent, crisnatol, by a human hepatoma cell line, Hep G2, and hepatic microsomes. Characterization of metabolites. Biochem Pharmacol. 1991 Jul 5;42(2):337-46. [3]. Patel DK, et al. Disposition, metabolism, and excretion of the anticancer agent crisnatol in the rat. Drug Metab Dispos. 1991 Mar-Apr;19(2):491-7.
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