Delattin Nicolas, De Brucker Katrijn, Craik David J, Cheneval Olivier, De Coninck Barbara, Cammue Bruno P A, Thevissen Karin
Centre of Microbial and Plant Genetics, KU Leuven, Leuven, Belgium.
Institute for Molecular Bioscience, University of Queensland, Brisbane, Australia.
Antimicrob Agents Chemother. 2014 Aug;58(8):4974-7. doi: 10.1128/AAC.03336-14. Epub 2014 Jun 9.
We performed a structure-activity relationship study of the antibiofilm plant-derived decapeptide OSIP108. Introduction of positively charged amino acids R, H, and K resulted in an up-to-5-fold-increased antibiofilm activity against Candida albicans compared to native OSIP108, whereas replacement of R9 resulted in complete abolishment of its antibiofilm activity. By combining the most promising amino acid substitutions, we found that the double-substituted OSIP108 analogue Q6R/G7K had an 8-fold-increased antibiofilm activity.
我们对源自植物的抗生物膜十肽OSIP108进行了构效关系研究。引入带正电荷的氨基酸R、H和K，与天然OSIP108相比，对白色念珠菌的抗生物膜活性提高了5倍，而替换R9则导致其抗生物膜活性完全丧失。通过组合最有前景的氨基酸取代，我们发现双取代的OSIP108类似物Q6R/G7K的抗生物膜活性提高了8倍。
