V79中国仓鼠细胞将反式-N-乙酰氧基-4-乙酰氨基芪和反式-N-羟基-4-乙酰氨基芪脱乙酰化为具有致突变性和细胞毒性的代谢产物。
V79 Chinese hamster cells deacetylate trans-N-acetoxy-4-acetylaminostilbene and trans-N-hydroxy-4-acetylaminostilbene to mutagenic and cytotoxic metabolites.
作者信息
Glatt H, Oesch F, Neumann H G
机构信息
Institute of Toxicology of the University, Mainz, Federal Republic of Germany.
出版信息
Cell Biol Toxicol. 1986 Jun;2(2):213-21. doi: 10.1007/BF00122690.
The N-acetoxy and N-hydroxy derivatives of trans-4-acetylaminostilbene (AAS) were demonstrated to induce gene mutations at the hgprt locus and to be cytotoxic in V79 cells. These cells deacetylated AAS. Paraoxon inhibited the deacetylation of AAS by more than 99% and reduced the mutagenicity and cytotoxicity of N-hydroxy-AAS and N-acetoxy-AAS to about one-tenth. Hence, deacetylated metabolites, formed by the target cells, were important for the observed biological effects.
反式-4-乙酰氨基芪（AAS）的N-乙酰氧基和N-羟基衍生物被证明可在次黄嘌呤鸟嘌呤磷酸核糖转移酶（hgprt）位点诱导基因突变，并对V79细胞具有细胞毒性。这些细胞可使AAS脱乙酰化。对氧磷抑制AAS的脱乙酰化作用超过99%，并将N-羟基-AAS和N-乙酰氧基-AAS的致突变性和细胞毒性降低至约十分之一。因此，由靶细胞形成的脱乙酰化代谢产物对观察到的生物学效应很重要。
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