Soufian Safieh, Hassani Leila
Department of Biology, Payame Noor University, Arak 38195-466, Iran.
Pak J Biol Sci. 2011 Jul 15;14(14):729-35. doi: 10.3923/pjbs.2011.729.735.
Two new analogs of Aurein 1.2 antimicrobial peptide were synthesized and the antimicrobial activities were investigated. The results showed that the activity of G1R/F3W analog was higher than the native peptide and the F3W analog. Circular dichroism studies also showed that the secondary structure of the F3W was concentration-dependent, whereas, there was no such relationship seen in the case of G1R/F3W analog. It has been proposed that G1R/F3W activity was based on a single mechanism (snorkeling), while Aurein 1.2 and F3W utilized the snorkeling mechanism at low concentrations (0-0.01 mM) and the carpet mechanism at higher concentrations (0.01-0.1 mM). This study suggests that one pay attention to the concentration of biomolecules in peptide-based drug design.
合成了两种新的奥瑞因1.2抗菌肽类似物，并对其抗菌活性进行了研究。结果表明，G1R/F3W类似物的活性高于天然肽和F3W类似物。圆二色性研究还表明，F3W的二级结构与浓度有关，而G1R/F3W类似物则不存在这种关系。有人提出，G1R/F3W的活性基于单一机制（潜泳），而奥瑞因1.2和F3W在低浓度（0-0.01 mM）时利用潜泳机制，在较高浓度（0.01-0.1 mM）时利用毯式机制。这项研究表明，在基于肽的药物设计中要注意生物分子的浓度。
