喹啉衍生物对枯草芽孢杆菌抗菌活性的分子相互作用研究:计算生物学和体外研究解释。

IF 2.4 4区 生物学 Q3 BIOCHEMISTRY & MOLECULAR BIOLOGY
Molecular Biotechnology Pub Date : 2024-11-01 Epub Date: 2023-11-06 DOI:10.1007/s12033-023-00933-6
Anagha S Setlur, Chandrashekar Karunakaran, V Anusha, Aditya A Shendre, Akshay Uttarkar, Vidya Niranjan, H G Ashok Kumar, Raviraj Kusanur
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引用次数: 0

摘要

细菌感染正在演变,主要问题之一是抗菌耐药性的出现和流行。此外,某些枯草芽孢杆菌菌株已经对几种抗生素产生耐药性。为了对抗这种威胁,本工作旨在了解合成的两种喹啉衍生物对枯草芽孢杆菌的抗菌活性。通过Protox II、SwissADME和T.E.S.T(毒性评估软件工具)进行的毒性预测显示,这些衍生物无毒,几乎没有副作用。在Schrodinger中用两种喹啉衍生物(参考Q1和Q2)与枯草芽孢杆菌的选定靶蛋白(PDB ID:2VAM和FSE)对接进行的分子对接研究证明了理想的结合能(2VAM-Q1: - 4.63 kcal/mol和2VAM-Q2: - 4.46 kcal/mol和1FSE-Q1: - 3.51 kcal/mol,1FSE-Q2: - 6.34kcal/mol)。这些配合物在100ns下模拟,结果显示它们的稳定性和轻微的构象变化。通过圆盘扩散法进行的抗微生物测定显示了抑制区,表明枯草芽孢杆菌受到Q1和Q2的抑制,Q2的表现略好于Q1,表明其对该生物体的有效性,需要在前瞻性研究中对其他细菌进行进一步研究。因此,本研究表明,我们的新型喹啉衍生物对枯草芽孢杆菌具有抗菌性能,可以作为有效的抗菌剂。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Investigating the Molecular Interactions of Quinoline Derivatives for Antibacterial Activity Against Bacillus subtilis: Computational Biology and In Vitro Study Interpretations.

Bacterial infections are evolving and one of the chief problems is emergence and prevalence of antibacterial resistance. Moreover, certain strains of Bacillus subtilis have become resistant to several antibiotics. To counteract this menace, the present work aimed to comprehend the antibacterial activity of synthesized two quinoline derivatives against Bacillus subtilis. Toxicity predictions via Protox II, SwissADME and T.E.S.T (Toxicity Estimation Software Tool) revealed that these derivatives were non-toxic and had little to no adverse effects. Molecular docking studies carried out in Schrodinger with two quinoline derivatives (referred Q1 and Q2) docked against selected target proteins (PDB IDs: 2VAM and1FSE) of B. subtilis demonstrated ideal binding energies (2VAM-Q1: - 4.63 kcal/mol and 2VAM-Q2: - 4.46 kcal/mol, and 1FSE-Q1: - 3.51 kcal/mol, 1FSE-Q2: - 6.34 kcal/mol). These complexes were simulated at 100 ns and the outcomes revealed their stability with slight conformational changes. Anti-microbial assay via disc diffusion method revealed zones of inhibition showing that B. subtilis was inhibited by both Q1 and Q2, with Q2 performing slightly better than Q1, pointing towards its effectiveness against this organism and necessitating further study on other bacteria in prospective studies. Thus, this study demonstrates that our novel quinoline derivatives exhibit antibacterial properties against Bacillus subtilis and can act as potent anti-bacterials.

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来源期刊
Molecular Biotechnology
Molecular Biotechnology 医学-生化与分子生物学
CiteScore
4.10
自引率
3.80%
发文量
165
审稿时长
6 months
期刊介绍: Molecular Biotechnology publishes original research papers on the application of molecular biology to both basic and applied research in the field of biotechnology. Particular areas of interest include the following: stability and expression of cloned gene products, cell transformation, gene cloning systems and the production of recombinant proteins, protein purification and analysis, transgenic species, developmental biology, mutation analysis, the applications of DNA fingerprinting, RNA interference, and PCR technology, microarray technology, proteomics, mass spectrometry, bioinformatics, plant molecular biology, microbial genetics, gene probes and the diagnosis of disease, pharmaceutical and health care products, therapeutic agents, vaccines, gene targeting, gene therapy, stem cell technology and tissue engineering, antisense technology, protein engineering and enzyme technology, monoclonal antibodies, glycobiology and glycomics, and agricultural biotechnology.
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