Cytotoxicity of flutamide and 2-hydroxyflutamide and their effects on CYP1A2 mRNA in primary rat hepatocytes
文献类型：期刊论文
| 作者 | Wang, HX; Ma, XC; Deng, QL; Li, D |
| 刊名 | ACTA PHARMACOLOGICA SINICA
 |
| 出版日期 | 2002-06 |
| 卷号 | 23期号:6页码:562-566 |
| 关键词 | flutamide 2-hydroxyflutamide cytotoxicity cytochrome P-450CYP1A2 |
| ISSN号 | 1671-4083 |
| 文献子类 | Article |
| 英文摘要 | AM: To compare the cytotoxicity of flutamide and its active metabolite 2-hydroxyflutamide and their effects on cytochrome P-450 1A2 mRNA in primary rat hepatocytes. METHODS: After the isolation of hepatocytes and the primary incubation for 4 h, flutamide and 2-hydroxyflutamide were added respectively to the medium at the concentration of 10, 20, and 50 mg/L and incubated for 8 h. Cytotoxicity of hepatocytes was assessed by Trypan blue exclusion, lactate dehydrogenase (LDH) leakage, percentage of alanine aminotransferase (ALT) or aspartate aminotransferase (AST) release, and reduced glutathione (GSH). The effect of flutamide and 2-flutamide on the CYP1A2 mRNA level was further analyzed by Northern blot. RESULTS: After incubation for 8 h, cell viability was observed by Trypan blue exclusion. The increase of ALT and AST activity and the decrease of glutathione content were also noted at 10, 20, and 50 mg/L of flutamide and 50 mg/L of 2-hydroxyfluramide as compared with normal rat hepatocytes. Induction of CYP1A2 mRNA were 2-, 5-, and 7.5-fold at 10, 20, and 50 mg/L of flutamide and 3.5-fold at 50 mg/L of 2-hydroxyflutamide. CONCLUSION: Cytotoxicity of flutamide and its effect on CYP1A2 mRNA were stronger than those of its active metabolite 2-hydroxyflutamide in primary rat hepatocytes. |
| WOS关键词 | LIVER |
| WOS研究方向 | Chemistry ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000176101400014 |
| 出版者 | SHANGHAI INST MATERIA MEDICA |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/274352]  |
| 专题 | 新药研究国家重点实验室 中科院受体结构与功能重点实验室 |
| 通讯作者 | Li, D |
| 作者单位 | 1.Fudan Univ, Sch Pharm, Dept Pharmacol, Shanghai 200032, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Biol Sci, Inst Materia Med, State Key Lab Drug Res, Shanghai 200031, Peoples R China |
| 推荐引用方式 GB/T 7714 | Wang, HX,Ma, XC,Deng, QL,et al. Cytotoxicity of flutamide and 2-hydroxyflutamide and their effects on CYP1A2 mRNA in primary rat hepatocytes[J]. ACTA PHARMACOLOGICA SINICA,2002,23(6):562-566. |
| APA | Wang, HX,Ma, XC,Deng, QL,&Li, D.(2002).Cytotoxicity of flutamide and 2-hydroxyflutamide and their effects on CYP1A2 mRNA in primary rat hepatocytes.ACTA PHARMACOLOGICA SINICA,23(6),562-566. |
| MLA | Wang, HX,et al."Cytotoxicity of flutamide and 2-hydroxyflutamide and their effects on CYP1A2 mRNA in primary rat hepatocytes".ACTA PHARMACOLOGICA SINICA 23.6(2002):562-566. |
入库方式： OAI收割
来源：上海药物研究所
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