Novel synthetic organic compounds inspired from antifeedant marine alkaloids as potent bacterial biofilm inhibitors
Novel synthetic organic compounds inspired from antifeedant marine alkaloids as potent bacterial biofilm inhibitors
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DOI：
10.1016/j.bioorg.2015.06.001
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发表时间：
2015-08-01
影响因子：
5.1
通讯作者：
Hampannavar, Girish
中科院分区：
文献类型：
--
作者：
Rane, Rajesh A.;Karpoormath, Rajshekhar;Hampannavar, Girish
本文报道了17种由海洋溴吡咯生物碱衍生的新型合成有机化合物，它们对革兰氏阳性菌产生的生物膜具有潜在的抑制作用。化合物5f对MSSA、MRSA和SE的最低生物膜抑制浓度（MBIC）分别为0.39、0.78和3.125 μ g/mL，是有前景的抗生物膜先导化合物。化合物5b、5c、5d、5e、5f、5h、5i和5j对表皮链球菌的效价与标准药物万古霉素（MBIC = 3.125 μ g/mL）相当。值得注意的是，大多数合成的化合物显示出比万古霉素更好的效价，表明它们具有作为细菌生物膜抑制剂的潜力。对活性最高的杂交株进行细胞活力测定，证实了其抗毒性，有待进一步研究。(C) 2015爱思唯尔公司版权所有。
In this paper, we have reported seventeen novel synthetic organic compounds derived from marine bromopyrrole alkaloids, exhibiting potential inhibition of biofilm produced by Gram-positive bacteria. Compound 5f with minimum biofilm inhibitory concentration (MBIC) of 0.39, 0.78 and 3.125 mu g/mL against MSSA, MRSA and SE respectively, emerged as promising anti-biofilm lead compounds. In addition, compounds 5b, 5c, 5d, 5e, 5f, 5h, 5i and 5j revealed equal potency as that of the standard drug Vancomycin (MBIC = 3.125 mu g/mL) against Streptococcus epidermidis. Notably, most of the synthesized compounds displayed better potency than Vancomycin indicating their potential as inhibitors of bacterial biofilm. The cell viability assay for the most active hybrid confirms its anti-virulence properties which need to be further researched. (C) 2015 Elsevier Inc. All rights reserved.