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用于抗菌和抗肝癌应用的新型咪唑鎓-硫代乙内酰脲杂化物及其锰(III)配合物

Novel imidazolium-thiohydantoin hybrids and their Mn(iii) complexes for antimicrobial and anti-liver cancer applications.

作者信息

Ismail Lamia A, Zakaria R, Hassan Eman M, Alfaifi Mohammad Y, Shati Ali A, Elbehairi Serag Eldin I, El-Bindary A A, Elshaarawy Reda F M

机构信息

Department of Chemistry, Faculty of Science, Port Said University Port Said 42526 Egypt.

Biology Department, Faculty of Science, King Khalid University Abha 9004 Saudi Arabia.

出版信息

RSC Adv. 2022 Oct 5;12(44):28364-28375. doi: 10.1039/d2ra05233d. eCollection 2022 Oct 4.

Abstract

We present the effective synthesis and structural characterization of three novel imidazolium-thiohydantoin ligands (IMTHs, 5a-c) and their Mn(iii) complexes (Mn(iii)IMTHs, 6a-c) in this study. The findings of elemental analyses, spectral analyses and magnetic measurements will be used to infer the stoichiometry, coordination styles, and geometrical aspects of Mn(iii)IMTHs. The new compounds were evaluated for their chemotherapeutic potential against ESKAPE pathogens and liver cancer (HepG2). According to the MIC and MBC values, the bactericidal and bacteriostatic activities of IMTHs have been significantly improved following coordination with the Mn(iii) ion. The MTT assay results showed that all Mn(iii)IMTHs had the potential to reduce the viability of liver carcinoma (HepG2) cells in a dose-dependent manner, with the BF-supported complex (6b) outperforming its counterparts (6a and 6c) as well as a clinical anticancer drug (VBL). Additionally, Mn-IMTH (6b) showed the highest level of selectivity (SI = 32.05) for targeting malignant cells (HepG2) over healthy cells (HL7702).

摘要

在本研究中,我们展示了三种新型咪唑鎓-硫代乙内酰脲配体(IMTHs,5a - c)及其锰(iii)配合物(Mn(iii)IMTHs,6a - c)的有效合成和结构表征。元素分析、光谱分析和磁性测量的结果将用于推断Mn(iii)IMTHs的化学计量、配位方式和几何结构。对这些新化合物针对ESKAPE病原体和肝癌(HepG2)的化疗潜力进行了评估。根据MIC和MBC值,IMTHs与锰(iii)离子配位后,其杀菌和抑菌活性得到了显著提高。MTT分析结果表明,所有Mn(iii)IMTHs都有潜力以剂量依赖的方式降低肝癌(HepG2)细胞的活力,其中硼氟支持的配合物(6b)优于其同类物(6a和6c)以及一种临床抗癌药物(长春碱)。此外,锰-IMTH(6b)对恶性细胞(HepG2)相对于健康细胞(HL7702)表现出最高水平的选择性(SI = 32.05)。

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