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首页> 外文期刊>RSC Advances >A ZnII complex of ornidazole with decreased nitro radical anions that is still highly active on Entamoeba histolytica
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A ZnII complex of ornidazole with decreased nitro radical anions that is still highly active on Entamoeba histolytica

机译：Ornidazole的ZnII复合物，其纯净的根部阴离子降低，仍然在entamoeba histolytica上高度活跃

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A monomeric complex of Zn ~(II) with ornidazole [Zn(Onz) _(2) Cl _(2) ] decreases formation of the nitro-radical anion (R–NO _(2) ˙ ~(?) ), and this is realized by recording it in an enzyme assay using xanthine oxidase, which is a model nitro-reductase. Although the formation of R–NO _(2) ˙ ~(?) is essential for drug action, as it is also associated with neurotoxic side effects, it is imperative to control its generation in order to avoid excess presence. With a decrease in R–NO _(2) ˙ ~(?) , while the neurotoxic side effects should decrease, it can be expected that a compromise with regard to therapeutic efficacy will be seen since the complex will be less active in the free radical pathway. Since R–NO _(2) ˙ ~(?) is crucial for the functioning of 5-nitroimidazoles, we attempted to find out if its biological activity is affected in any way in our effort to control its formation. For this purpose, Entamoeba histolytica (HM1:IMS Strain) was chosen as a biological target to realize the performance of the complex with respect to ornidazole (R–NO _(2) ). The experiments revealed that the complex not only compares well with ornidazole, but in fact, under longer exposure times, it also performs better than it. This efficacy of the complex was seen despite a decrease in R–NO _(2) ˙ ~(?) , as identified by an enzyme assay, and this was probably due to certain attributes of the complex formation that are not known for ornidazole. These attributes outweigh any loss in efficacy in the free radical pathway following complex formation. This is certainly an advantage of complex formation and helps to improve the therapeutic index. This study has attempted to look at some of the possible reasons why the complex performs better than ornidazole. One reason is its ability to bind to DNA better than ornidazole does, and this can be understood by following the interaction of ornidazole and its Zn( II ) complex with calf-thymus DNA using cyclic voltammetry. Therefore, this study showed that despite a decrease in R–NO _(2) ˙ ~(?) , the complex does not compromise its efficacy, and this was examined using a biological target. In addition, the complex is likely to have less toxic side effects on the host of the disease-causing microbes.
机译：Zn〜（II）的单体络合物用甲酰胺α[Zn（ONZ）_（2）Cl _（2）]降低了硝基 - 自由基阴离子的形成（R-No _（2）˙〜（？）），和通过使用黄嘌呤氧化酶在酶测定中将其记录为硝基还原酶来实现这一点。虽然形成R-No _（2）˙〜（？）对于药物作用至关重要，但它也与神经毒性副作用有关，因此必须控制其生成以避免过量存在。 r-no _（2）˙〜（？）减少，而神经毒性副作用应降低，可以预期，由于复杂的复杂在自由中的剧烈活跃时，将看到对治疗效果的折衷自由基途径。由于R-No _（2）˙〜（？）对于5-硝基咪唑的功能至关重要，我们试图了解其生物学活动是否以任何方式控制其努力控制其形成。为此目的，选择EntamoEBA组织olyTICA（HM1：IMS菌株）作为生物靶标，以实现与ORNIDAZOLE的复合物的性能（R-NO _（2））。实验表明，复杂的复杂性不仅与ornidazole相比很好，但实际上，在更长的曝光时间下，它也比它更好。尽管R-No _（2）℃〜（α）降低，但是通过酶测定鉴定的效果，这可能是由于Ornidazole不知道的复杂形成的某些属性是由于蛋白质的含量。这些属性在复杂的形成后自由基途径中的任何损失差异。这肯定是复杂地层的优势，并有助于改善治疗指数。这项研究试图看一些可能的原因，为什么复合物表现优于Ornidazole。一种原因是它比ornidazole更好地与DNA结合DNA的能力，这可以通过使用循环伏安法与小牛胸腺DNA与CALF-Thymus DNA相互作用来理解。因此，该研究表明，尽管R-No _（2）℃〜（？）减少，但复合物不会损害其功效，并且使用生物靶标检验该方法。此外，复合物可能对引起疾病的微生物的宿主具有较小的毒性副作用。

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