کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1357644 981264 2016 7 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Triterpene sapogenin–polyarginine conjugates exhibit promising antibacterial activity against Gram-positive strains
ترجمه فارسی عنوان
تریترپن سابوژنینا پلی گارینین کنگواتیک فعالیت ضد میکروبی امیدوار کننده را در برابر سوء قندهای گرم مثبت نشان می دهد
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
چکیده انگلیسی

Triterpene sapogenins are a group of biologically active compounds with antibacterial activity. However, the limited solubility and poor bioavailability of triterpene sapogenins restrict their therapeutic application. Polyarginine peptides are small cationic peptides with high affinities for multiple negatively charged cell membranes and possess moderate antibacterial activities. In this study, we designed and synthesized a series of sapogenin–polyarginine conjugates in which the triterpene sapogenin moiety was covalently appended to the positively charged polyarginine via click chemistry. A clear synergistic effect was found, and the conjugates exhibited potent and selective antibacterial activity against Gram-positive strains. Among them, BAc-R3 was the most promising compound, which was also proven to be nontoxic toward mammalian cells as well as stable in plasma. The mechanism of BAc-R3 primarily involves an interaction with the bacterial membrane, similar to that of antimicrobial peptides (AMPs). This scaffold design opens an avenue for the further development of novel antibiotics comprised of the combination of a peptide and a natural product.

Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 24, Issue 13, 1 July 2016, Pages 2999–3005
نویسندگان
, , , , , ,