Singh Gurpreet, Wani Naiem Ahmad, Rahim Junaid Ur, Shankar Sudha, Rai Rajkishor, Katoch Meenu
Microbial Biotechnology Division, CSIR-Indian Institute of Integrative Medicine, Canal Road, Jammu-Tawi, 180001, India.
Academy of Scientific and Innovative Research (AcSIR), Ghaziabad, 201002, India.
J Antibiot (Tokyo). 2022 Apr;75(4):236-242. doi: 10.1038/s41429-022-00508-8. Epub 2022 Feb 10.
In the present work, piperic acid and 4-ethylpiperic acid (EPA) amides with amino acids (C1-C8) were bio-evaluated for their antimicrobial activity and biofilm inhibition against Gram-positive and Gram-negative bacterial strains. Among all, EPA-β-Pip(Bzl)-OMe, C2 displayed the potent antimicrobial activity with MIC of 6.25 μg ml against Gram-negative bacteria Escherichia coli. In combination studies, the FIC indices suggested that C1 and C2 have a synergistic effect with ciprofloxacin against E. coli and Bacillus subtilis, whereas C5 exhibited a synergistic effect with ciprofloxacin against all the tested bacteria. The inhibitory effect of amides C1, C2, and C5 on the biofilm formation of test strains was significantly potentiated by co-administration with ciprofloxacin. Furthermore, the effective concentrations of C2 in combination reduced drastically compared to alone for biofilm inhibition. At these concentrations, C2 showed negligible hemolytic and cytotoxic activities.
在本研究中,对胡椒酸和4-乙基胡椒酸(EPA)与氨基酸(C1 - C8)形成的酰胺进行了生物评价,考察其对革兰氏阳性和革兰氏阴性细菌菌株的抗菌活性及生物膜抑制作用。其中,EPA-β-Pip(Bzl)-OMe,C2对革兰氏阴性菌大肠杆菌表现出强效抗菌活性,最低抑菌浓度(MIC)为6.25μg/ml。在联合研究中,分数抑菌浓度(FIC)指数表明,C1和C2与环丙沙星联合对大肠杆菌和枯草芽孢杆菌具有协同作用,而C5与环丙沙星联合对所有测试细菌均表现出协同作用。与环丙沙星共同给药时,酰胺C1、C2和C5对测试菌株生物膜形成的抑制作用显著增强。此外,与单独使用相比,C2联合使用时生物膜抑制的有效浓度大幅降低。在这些浓度下,C2的溶血和细胞毒性活性可忽略不计。