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首页> 外文期刊>Journal of toxicology and environmental health, Part A >Comparative mutagenicity of apicidin and apicidin derivatives (SD-0203 and SD-2007), histone deacetylase inhibitors.
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Comparative mutagenicity of apicidin and apicidin derivatives (SD-0203 and SD-2007), histone deacetylase inhibitors.

机译：组蛋白脱乙酰基酶抑制剂Apicidin和Apicidin衍生物（SD-0203和SD-2007）的诱变性比较。

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摘要

The fungal metabolite apicidin [cyclo(N-O-methyl-L-tryptophanyl-L-isoleucinyl-D-pipecolinyl-L-2-amino-8-o xodecanoyl)] is known to inhibit histone deacetylase (HDAC). In this study, the genotoxicity of apicidin and its derivatives were tested using three tests: a bacterial reverse mutation assay (Ames test), an in vitro chromosome aberration (CA) test, and an in vivo micronucleus (MN) test. Apicidin was negative in the Ames test in the presence and absence of the microsomal metabolizing enzyme system. Apicidin induced a significant increase in the total chromosome aberrations in Chinese hamster ovary (CHO) cells. In the MN test, apicidin induced mutagenic activity at the highest dose (1000 microM/kg). The apicidin derivatives SD-0203 and SD-2007 did not induce mutagenic activity in the Ames test and no significant mutagenic potency was observed in the CA test. However, these compounds significantly and dose-dependently increased the number of micronucleated polychromatic erythrocytes (MNPCEs) as well as the PCE/(PCE + NCE) ratio in the MN test. These results suggest that apicidin and its derivatives preferentially induce CA and MN but are not effective in the Ames test.
机译：已知真菌代谢产物阿皮啶[环（N-O-甲基-L-色氨酸-L-异亮氨酸-D-哌啶基-L-2-氨基-8-氧代十二烷酰基）]抑制组蛋白脱乙酰基酶（HDAC）。在这项研究中，使用以下三种测试方法对阿皮定及其衍生物的遗传毒性进行了测试：细菌反向突变分析（Ames测试），体外染色体畸变（CA）测试和体内微核（MN）测试。在存在和不存在微粒体代谢酶系统的情况下，Apicidin在Ames试验中均为阴性。 Apicidin诱导中国仓鼠卵巢（CHO）细胞的总染色体畸变显着增加。在MN测试中，Apicidin以最高剂量（1000 microM / kg）诱导诱变活性。 Apicidin衍生物SD-0203和SD-2007在Ames试验中未诱导诱变活性，在CA试验中未观察到显着的诱变效力。但是，这些化合物显着且剂量依赖性地增加了MN测试中微核多色红细胞（MNPCE）的数量以及PCE /（PCE + NCE）的比率。这些结果表明，阿哌西丁及其衍生物优先诱导CA和MN，但在Ames试验中无效。

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