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金 (I) 和银 (I) 复合物含有混合硫胺/硫尿素联结体作为潜在的莱什曼尼cidal 剂

Alice P Borges¹, Malu M S Obata², Silvia H Libardi³

¹Bioactive Compounds Development Research Group, Federal University of Triângulo Mineiro, Av. Dr. Randolfo Borges 1400, Uberaba 38025-440, MG, Brazil.

|April 27, 2024

概括

含有尿素连接体的新型金属复合物对Leishmania寄生虫表现出强大的leishmanicidal活性,为目前不充分的Leishmaniasis治疗提供了一个有希望的替代方案.

科学领域:

药用化学医学化学
寄生虫学的寄生虫学
无机化学无机化学

背景情况:

莱什曼病影响全球超过10亿人,治疗选择有限且过时.
开发新型治疗剂对于对抗这种被忽视的热带疾病至关重要.

研究的目的:

为了合成和表征新的金属复合物银 (I) 和金 (I) 与thiourea配体.
评估这些复合物的leishmanicidal活性和细胞毒性.
调查复合物的相互作用与来自Leishmania braziliensis的旧黄色酶 (OYE).

主要方法:

尿素配体的合成及其随后的复合与Ag (I) 和Au (I) 离子.
使用光谱技术 (FTIR,NMR,UV-vis,发射),元素分析,ESI-MS和单晶XRD进行表征.
在体外对Vero细胞的细胞毒性和针对Leishmania infantum和Leishmania braziliensis的leishmanicidal活性进行了评估.
使用DFT和生化试验进行酶相互作用研究的计算分析.

主要成果:

几种合成的Ag(I) 和Au(I) 氨酸复合物表现出显著的细胞外雷什曼尼cidal活性.
一些复合物与标准药物Glucantime相比表现出更高的活性,对Leishmania物种的选择性各不相同.
相互作用研究表明,老黄色酶 (LbOYE) 是这些新型化合物的潜在生物标.

结论:

开发的金属-尿素复合物代表了用于莱什曼病治疗的有前途的新类化合物.
这些复合物提供了一种潜在的治疗策略,提高了疗效,并可能具有新的作用机制.
准LbOYE可能是观察到的莱什曼尼cidal效应的一个关键因素.

关键词:

酶学研究是指酶学研究.混合化合物混合化合物混合化合物莱什曼尼cidal活动活动.分子对接的分子对接.硫胺酸硫胺的使用方法这种酸氨酸酸.

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