Metabolic-induced cytotoxicity of diosbulbin B in CYP3A4-expressing cells

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• 作者：Ji-zong Jiang^a ; Bao-hua Yang^a ; Li-li Ji^a ; ^b ; Li Yang^a ; ^b ; Yu-Chang Mao^c ; Zhuo-han Hu^c ; Zheng-tao Wang^a ; ^b ; Chang-hong Wang^a ; ^b ; ^{wchcxm@hotmail.com}
• 关键词：AP ; Acetaminophen ; CCK ; 2H&ndash ; Tetrazolium ; 5-(2 ; 4-disulfophenyl)-3-(2-methoxy&ndash ; 4-nitrophenyl)&ndash ; 2-(4-nitrophenyl)- ; innersalt ; sodium salt ; CYP450 ; Cytochrome P450 ; DB ; Diosbulbin B ; DMEM ; Dulbecco's Modified Eagle Medium ; DMF ; N ; N-Dimethylformamide ; DMSO ; Dimethyl Sulphoxide ; FBS ; Fetal bovine serum ; GSH ; Glutathione ; IS ; Internal standard ; KT ; ketoconazole ; MLM ; Mouse liver microsomes ; MRM ; Multiple reaction mode ; MS/MS ; Mass spectrometry tandem and mass spectrometry ; MTT ; 3-(4 ; 5-Dime
• 刊名：Toxicology in Vitro
• 出版年：2017
• 出版时间：February 2017
• 年：2017
• 卷：38
• 期：Complete
• 页码：59-66
• 全文大小：653 K
• 卷排序：38

文摘

DB is susceptive toxic to CYP3A4 high expression cell lines. Cytotoxicity of DB is closely related to metabolism activation by CYP3A4. The reactive metabolites of DB induce cytotoxicity or anti-tumor effect. Ketoconazole as CYP3A4 inhibitor can reduce the cytotoxicity of DB.