Saraswat Juhi, Wani Farooq Ahmed, Dar Khalid Imtiyaz, Rizvi M Moshahid Alam, Patel Rajan
Biophysical Chemistry Laboratory, Centre for Interdisciplinary Research in Basic Sciences, Jamia Millia Islamia, New Delhi 110025, India.
Department of Bioscience, Jamia Millia Islamia, New Delhi 110025, India.
ACS Omega. 2020 Mar 17;5(12):6376-6388. doi: 10.1021/acsomega.9b03777. eCollection 2020 Mar 31.
Growing antibiotic resistance has become a major health problem and has encouraged many researchers to find an alternative class of antibiotics. Combination therapy (covalent/noncovalent) is supposed to increase antibacterial activity leading to a decrease in administration dosage, thus lowering the risk of adverse side effects. The covalent coupling sometimes leads to instability and loss in the structure of AMPs. Therefore, herein, we have reported innovative research involving the noncovalent coupling of melittin (MEL), an antimicrobial peptide with a series of synthesized less toxic pyrrolidinium-based ionic liquids (ILs) for which MTT assay was performed. The antibacterial results of conjugates showed remarkable improvement in the MIC value as compared to MEL and ILs alone against and In addition, hemocompatibility results suggested good selectivity of the noncovalent conjugate as a potential antibiotic agent. Further, the docking study was employed to acquire the most favorable conformation of MEL in the presence of ILs. The best possible complex was further studied using various spectroscopic techniques, which showed appreciable binding and stability of the complex.
日益增长的抗生素耐药性已成为一个主要的健康问题，并促使许多研究人员寻找另一类抗生素。联合疗法（共价/非共价）有望提高抗菌活性，从而降低给药剂量，进而降低产生副作用的风险。共价偶联有时会导致抗菌肽结构的不稳定性和损失。因此，在此我们报告了一项创新性研究，该研究涉及蜂毒肽（MEL，一种抗菌肽）与一系列合成的低毒吡咯烷鎓基离子液体（ILs）的非共价偶联，并进行了MTT测定。与单独的MEL和ILs相比，共轭物的抗菌结果显示其MIC值有显著提高。此外，血液相容性结果表明非共价共轭物作为潜在抗生素具有良好的选择性。此外，采用对接研究来获得ILs存在下MEL的最有利构象。使用各种光谱技术对最佳可能的复合物进行了进一步研究，结果表明该复合物具有明显的结合和稳定性。
