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红霉素-金属配合物:一步合成、分子对接分析及对病原菌的抗菌效能

Erythromycin-metal complexes: One-step synthesis, molecular docking analysis and antibacterial proficiency against pathogenic strains.

作者信息

Egu Samuel Attah, Abah Lian Ojotule, Hussaini Jumai Zainab, Onoja Alexander David, Ali Irfan, Habib Atiya, Qureshi Urooj, Idih Sunday Okpanachi, Edegbo Emmanuel, Achimugu Lawrence, Omale Aminu, Michael Ojochide Charity, Adaji Mohammed Umar, Omale Jamila Audu

机构信息

Department of Pure and Industrial Chemistry, Kogi State University, Anyigba, Kogi State, Nigeria.

Genomics and Molecular Biology Training and Research Laboratory, Kogi State University, Anyigba, Kogi State, Nigeria.

出版信息

Heliyon. 2024 Aug 3;10(16):e35536. doi: 10.1016/j.heliyon.2024.e35536. eCollection 2024 Aug 30.

Abstract

The study focused on the extraction of free erythromycin from commercially manufactured tablets and the use of metal salts to synthesize erythromycin-metal complexes, specifically involving silver (Ag), nickel (Ni), cobalt (Co), and copper (Cu). The synthesis was confirmed through various methods, including elemental analysis, thermogravimetric analysis, Fourier-transform infrared (FTIR), and UV-visible spectroscopy. The microbiological investigation involved and as test organisms. The NCCLS broth microdilution reference method was used to determine the minimum fungicidal concentration and minimum inhibitory concentration of the complexes. The synthesized complexes were highly effective against a variety of fungi and bacteria, with compound Ery-Cu having MIC as low as 1.56 mg/mL, Ery-Cu and Ery-Ni with MBCs of 6.25 mg/mL and Ery-Cu having MFC of 6.25 mg/mL. Dose-dependent inhibitory effects were found upon examination of the antimicrobial susceptibility of specific complexes (Cu, Ni, Co and Ag) at varying concentrations of 100, 50, 25 and 12.5 mm/mL. Antibiotic susceptibility testing revealed efficacy against the tested pathogens. The study suggests that the synthesis of erythromycin-metal complexes, coupled with their antibacterial effectiveness against a diverse spectrum of bacteria and fungi, as they showed promising inhibitory properties when tested against a range of test species (, and ), could lead to the development of innovative antibacterial agents. Molecular docking simulations were used to examine the interactions between metal complexes with proteins filamentous temperature-sensitive protein Z and lanosterol 14-demethylase. The study highlights the need for further exploration in pharmaceutical research.

摘要

该研究聚焦于从市售片剂中提取游离红霉素,以及使用金属盐合成红霉素 - 金属配合物,具体涉及银(Ag)、镍(Ni)、钴(Co)和铜(Cu)。通过多种方法确认了合成过程,包括元素分析、热重分析、傅里叶变换红外光谱(FTIR)和紫外可见光谱。微生物学研究使用了[此处原文缺失两种受试生物名称]作为受试生物。采用美国国家临床实验室标准化委员会(NCCLS)肉汤微量稀释参考方法来测定配合物的最低杀菌浓度和最低抑菌浓度。合成的配合物对多种真菌和细菌具有高效性,化合物Ery - Cu的最低抑菌浓度低至1.56毫克/毫升,Ery - Cu和Ery - Ni的最低杀菌浓度为6.25毫克/毫升,Ery - Cu的最低杀真菌浓度为6.25毫克/毫升。在检测特定配合物(Cu、Ni、Co和Ag)在100、50、25和12.5毫米/毫升不同浓度下的抗菌敏感性时,发现了剂量依赖性抑制作用。抗生素敏感性测试显示对受试病原体有效。该研究表明,红霉素 - 金属配合物的合成及其对多种细菌和真菌的抗菌有效性,因为它们在针对一系列受试物种([此处原文缺失受试物种名称])进行测试时显示出有前景的抑制特性,可能会促成创新抗菌剂的开发。使用分子对接模拟来研究金属配合物与丝状温度敏感蛋白Z和羊毛甾醇14 - 脱甲基酶之间的相互作用。该研究强调了在药物研究中进一步探索的必要性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e31b/11363837/4ca6701c0e1d/gr1.jpg

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