Eeman Marc, Olofsson Gerd, Sparr Emma, Nasir Mehmet Nail, Nylander Tommy, Deleu Magali
Université de Liège, Gembloux Agro-Bio-Tech, Unité de Chimie Biologique Industrielle, Passage des Déportés, 2, B-5030 Gembloux, Belgium.
Physical Chemistry, Center for Chemistry and Chemical Engineering, Lund University, P.O. Box 124, SE-221 00 Lund, Sweden.
Colloids Surf B Biointerfaces. 2014 Sep 1;121:27-35. doi: 10.1016/j.colsurfb.2014.05.019. Epub 2014 May 23.
Based on its outstanding antifungal properties, it is reasonable to believe that fengycin might be efficient to topically treat localized dermatomycoses. Since most of the fungi species involved in the formation of those mycotic skin diseases colonize primarily the stratum corneum (SC), studying the interaction between fengycin and SC-mimicking lipid membranes is a primary step to determine the potential of fengycin to overcome the physical barrier of the skin. In this respect, multilamellar lipid vesicles (MLVs), with a lipid composition mimicking that of the SC, were prepared and characterized by differential scanning calorimetry (DSC). The critical micelle concentration (CMC) of fengycin was also assessed under skin conditions and found to be 1.2±0.1μM. The molecular interactions of fengycin with SC-mimicking MLVs were investigated by both DSC and isothermal titration calorimetry (ITC). Results showed that the interactions were considerably affected by changes in lipid phase behaviour. At 40°C and below, fengycin induced exothermic changes in the lipid structures suggesting that less-ordered lipid domains became more-ordered in presence of fengycin. At 60°C, clearly endothermic interaction enthalpies were observed, which could arise from the "melting" of remaining solid domains enriched in high melting lipids that without fengycin melt at higher temperatures.
基于其出色的抗真菌特性,有理由相信丰原素可能对局部治疗皮肤癣菌病有效。由于参与形成这些真菌性皮肤病的大多数真菌物种主要定植于角质层(SC),因此研究丰原素与模拟SC的脂质膜之间的相互作用是确定丰原素克服皮肤物理屏障潜力的首要步骤。在这方面,制备了具有模拟SC脂质组成的多层脂质囊泡(MLV),并通过差示扫描量热法(DSC)对其进行了表征。还在皮肤条件下评估了丰原素的临界胶束浓度(CMC),发现其为1.2±0.1μM。通过DSC和等温滴定量热法(ITC)研究了丰原素与模拟SC的MLV之间的分子相互作用。结果表明,脂质相行为的变化对相互作用有很大影响。在40°C及以下,丰原素诱导脂质结构发生放热变化,这表明在存在丰原素的情况下,无序程度较低的脂质域变得更加有序。在60°C时,观察到明显的吸热相互作用焓,这可能源于富含高熔点脂质的剩余固态域的“熔化”,这些固态域在没有丰原素的情况下会在更高温度下熔化。