由于细菌生物膜形成引起的抗生素抗性是一个主要的全球健康问题,这使得迫切需要寻找新的治疗方法。在这种情况下,,反式白藜芦醇(RSV),一种多酚天然物质,似乎是预防和根除生物膜相关感染的良好候选者,但其作用机制知之甚少。此外,RSV在生物介质中具有低生物利用度和化学不稳定性,这使得其在递送系统中的包封是必要的。在这项工作中,研究了游离RSV对金黄色葡萄球菌的抗生物膜活性,为了强调可能的作用机制,我们研究了MRSA菌株的抗粘附活性和细胞壁损伤。将游离RSV活性与脂质体中加载的RSV活性进行比较,特别是中性脂质体(L=DOPC/胆固醇)和阳离子脂质体(LG=DOPC/Chol/GLT1),其特征在于促进与细菌相互作用的半乳糖基化两亲物(GLT1)。结果表明,装载在LG中的RSV具有比游离RSV更高的抗粘附和抗生物膜活性。在另一边,游离RSV比包囊RSV具有更高的细菌生长抑制作用,并且可以通过产生孔来破坏细胞壁;然而,这种作用不能阻止细菌再次生长。这种RSV能力可能是其抑菌活性的基础。
Antibiotic resistance due to bacterial biofilm formation is a major global health concern that makes the search for new therapeutic approaches an urgent need. In this context,, trans-resveratrol (RSV), a polyphenolic natural substance, seems to be a good candidate for preventing and eradicating biofilm-associated infections but its mechanism of action is poorly understood. In addition, RSV suffers from low bioavailability and chemical instability in the biological media that make its encapsulation in delivery systems necessary. In this work, the anti-biofilm activity of free RSV was investigated on Staphylococcus aureus and, to highlight the possible mechanism of action, we studied the anti-adherence activity and also the cell wall damage on a MRSA strain. Free RSV activity was compared to that of RSV loaded in liposomes, specifically neutral liposomes (L = DOPC/Cholesterol) and cationic liposomes (LG = DOPC/Chol/GLT1) characterized by a galactosylated amphiphile (GLT1) that promotes the interaction with bacteria. The results indicate that RSV loaded in LG has anti-adherence and anti-biofilm activity higher than free RSV. On the other side, free RSV has a higher bacterial-growth-inhibiting effect than encapsulated RSV and it can damage cell walls by creating pores; however, this effect can not prevent bacteria from growing again. This RSV ability may underlie its bacteriostatic activity.