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首页> 外文期刊>Antimicrobial agents and chemotherapy. >Two diarylurea electron transport inhibitors reduce Staphylococcus aureus hemolytic activity and protect cultured endothelial cells from lysis.
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Two diarylurea electron transport inhibitors reduce Staphylococcus aureus hemolytic activity and protect cultured endothelial cells from lysis.

机译：两种二芳基脲电子传输抑制剂可降低金黄色葡萄球菌的溶血活性并保护培养的内皮细胞免于裂解。

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Reduction in electron transport is associated with decreased production in alpha-toxin despite the fact that Staphylococcus aureus is able to grow from 1 CFU to >10(7) CFU. Similarly, under anaerobic conditions, S. aureus does not produce alpha-toxin. Although the pathways that connect oxidative metabolism and toxin production are unknown, agents are available that exhibit greater inhibition of plant versus mammalian electron transport. Herbicides block electron transport in plants by inhibiting the formation of phosphoquinol (QH(2)) in plants. Commercial use in farming is possible because these compounds are much less active against the quinones found mammalian mitochondria. Because bacterial electron transport systems are closer to plant than mammalian systems, we hypothesized that inhibitors of respiration might be able to reduce S. aureus electron transport and block the production of alpha-toxin. We studied two compounds and found that the effective dose for the inhibition of bacterial respiration was 50 to >3,500 times lower than the concentration required to cause similar inhibition of rat mitochondrial respiration. Compounds I and II also reduced toxin production in S. aureus without causing overt toxicity to cultured endothelial cells. Finally, the compounds reduced the damage caused by S. aureus when cocultured with the endothelial cells. This raises the possibility that compounds that inhibit bacterial respiration might be prove valuable for the prevention of toxin production in S. aureus.
机译：尽管金黄色葡萄球菌能够从1 CFU生长到> 10（7）CFU，但电子运输的减少与α-毒素的产生减少有关。同样，在厌氧条件下，金黄色葡萄球菌不会产生α-毒素。尽管连接氧化代谢和毒素产生的途径尚不清楚，但与哺乳动物电子运输相比，仍可获得对植物具有更大抑制作用的药物。除草剂通过抑制植物中的磷酸喹啉（QH（2））的形成来阻止植物中的电子运输。由于这些化合物对发现于哺乳动物线粒体中的醌的活性低得多，因此可能在商业上用于农业。因为细菌电子传输系统比哺乳动物系统更接近植物，所以我们假设呼吸抑制剂可能能够减少金黄色葡萄球菌的电子传输并阻止α-毒素的产生。我们研究了两种化合物，发现抑制细菌呼吸的有效剂量比引起对大鼠线粒体呼吸的类似抑制作用所需的浓度低50至3500倍。化合物I和II还减少了金黄色葡萄球菌中的毒素产生，而对培养的内皮细胞没有明显的毒性。最后，当与内皮细胞共培养时，这些化合物减少了由金黄色葡萄球菌引起的损害。这增加了抑制细菌呼吸的化合物可能被证明对预防金黄色葡萄球菌毒素产生有价值的可能性。

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