4-乙炔基联苯中乙炔基在体外的代谢氧化。
The metabolic oxidation of the ethynyl group in 4-ethynylbiphenyl in vitro.
作者信息
Wade A, Symons A M, Martin L, Parke D V
出版信息
Biochem J. 1980 Jun 15;188(3):867-72. doi: 10.1042/bj1880867.
Abstract
- The metabolism of 4-ethynylbiphenyl has been studied in vitro with subcellular fractions of normal and induced rat liver, and rat intestinal microflora (caecal contents). 2. Oxidation was NADPH-dependent, was inhibited by CO and stimulated by pretreatment with phenobarbitone or 3-methylcholanthrene. 3. Oxidation of the ethynyl group occurred in washed microsomal preparations, but not significantly in soluble fractions. Oxidation of the ethynyl group by a microsomal fraction preceded aromatic hydroxylation and no metabolites containing the intact ethynyl group were detected. 4. The major metabolite in liver fractions was biphenyl-4-ylacetic acid. This was the only product produced by a modified Udenfriend system. 5. Metabolism of 4-ethynylbiphenyl by rat caecal contents under anaerobic conditions produced very small amounts of 4-vinylbiphenyl. 6. In a modified Ames test with Salmonella typhimurium TA98, 4-ethynylbiphenyl gave a weak positive result that was doubled after 'activation' with an induced rat S9 fraction.
摘要
- 已利用正常和诱导大鼠肝脏的亚细胞组分以及大鼠肠道微生物群（盲肠内容物）在体外研究了4-乙炔基联苯的代谢情况。2. 氧化反应依赖于NADPH，可被一氧化碳抑制，并受到苯巴比妥或3-甲基胆蒽预处理的刺激。3. 乙炔基的氧化发生在洗涤后的微粒体制剂中，但在可溶部分中不明显。微粒体部分对乙炔基的氧化先于芳香族羟基化，且未检测到含有完整乙炔基的代谢产物。4. 肝脏组分中的主要代谢产物是联苯-4-基乙酸。这是改良的乌登弗里德系统产生的唯一产物。5. 在厌氧条件下，大鼠盲肠内容物对4-乙炔基联苯的代谢产生了极少量的4-乙烯基联苯。6. 在改良的鼠伤寒沙门氏菌TA98艾姆斯试验中，4-乙炔基联苯给出了弱阳性结果，在用诱导的大鼠S9组分“活化”后该结果翻倍。
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