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The endocrine disruptor nonylphenol preferentially blocks cyclooxygenase-1.

机译:内分泌干​​扰物壬基酚优先阻断环氧合酶-1。

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摘要

The anthropogenic chemicals nonylphenol, bisphenol A, phthalic acid benzyl n-butyl ester, phthalic acid di-n-butyl ester and phthalic acid di(2-ethylhexyl) ester have been shown to possess sex hormone-like activity. To explore the possible actions of these chemicals on the autacoid synthesis in the body, we investigated the effects of nonylphenol, bisphenol A, phthalic acid benzyl n-butyl ester, phthalic acid di-n-butyl ester and phthalic acid di(2-ethylhexyl) ester on the activities of cyclooxygenase-1 and -2. Bisphenol A and all three phthalic acid derivatives had no significant effect on the cyclooxygenase-1 and -2 activities up to 100 microM. On the other hand, nonylphenol exhibited a marked inhibition on the cyclooxygenase-1 activity (10-100 microM nonylphenol, 7-95% inhibition), with no detectable change in the activity of cyclooxygenase-2. The inhibition patterns for the substrate, arachidonic acid, and a cofactor, phenol, were competitive and uncompetitive, respectively. These results suggest that nonylphenol can be a selective inhibitor of cyclooxygenase-1 activity.
机译:人为化学物质壬基酚,双酚A,邻苯二甲酸苄基正丁酯,邻苯二甲酸二正丁酯和邻苯二甲酸二(2-乙基己基)酯已显示出具有性激素样活性。为了探讨这些化学物质对人体中autacoid合成的可能作用,我们研究了壬基酚,双酚A,邻苯二甲酸苄基正丁酯,邻苯二甲酸二正丁酯和邻苯二甲酸二(2-乙基己基)的影响。 )酯对环氧合酶-1和-2的活性。双酚A和所有三种邻苯二甲酸衍生物对高达100 microM的环氧合酶-1和-2活性均无明显影响。另一方面,壬基酚对环氧合酶-1的活性有明显的抑制作用(10-100 microM壬基酚,抑制率为7-95%),而环氧合酶-2的活性没有可检测的变化。底物花生四烯酸和辅因子苯酚的抑制模式分别是竞争性的和无竞争性的。这些结果表明壬基酚可以是环氧合酶1活性的选择性抑制剂。

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