Department of Infections Control and Mycology, Chair of Microbiology, Jagiellonian University Medical College, Cracow, Poland.
Faculty of Chemistry, Jagiellonian University, Cracow, Poland.
Microbiol Spectr. 2023 Jun 15;11(3):e0084423. doi: 10.1128/spectrum.00844-23. Epub 2023 May 11.
The biological activity of polycations is usually associated with their biocidal properties. Their antibacterial features are well known, but in this work, observations on the antifungal properties of macromolecules obtained by methacrylamido propyl trimethyl ammonium chloride (MAPTAC) polymerization are presented. The results, not previously reported, make it possible to correlate antifungal properties directly with the structure of the macromolecule, in particular the molecular mass. The polymers described here have antifungal activity against some filamentous fungi. The strongest effect occurs for polymers with a mass of about 0.5 mDa which have confirmed activity against the multidrug-resistant species Scopulariopsis brevicaulis, Fusarium oxysporum, and Fusarium solani, as well as the dermatophytes Trichophyton mentagrophytes, Trichophyton rubrum, Trichophyton interdigitale, and Trichophyton tonsurans. In addition, this publication describes the effects of these macromolecular systems on serum and blood components and provides a preliminary assessment of toxicity on cell lines of skin-forming cells, i.e., fibroblasts and keratinocytes. Additionally, using a Franz diffusion chamber, a negligibly low transport of the active polymer through the skin was demonstrated, which is a desirable effect for externally applied antifungal drugs. Infectious diseases are a very big medical, social, and economic problem. Even before the COVID-19 pandemic, certain infections were among of the most common causes of death. The difficulties in the treatment of infectious diseases concern in particular fungal diseases, against which we have only a few classes of drugs represented by a few substances. The publication presents the preliminary results of the antifungal activity studies of four MAPTAC polymers on different fungal species and their cytotoxicity to human cells (fibroblasts and keratinocytes). The paper also compares these properties with analogous ones of two commonly used antifungal drugs, ciclopirox and terbinafine.
多聚阳离子的生物活性通常与其杀菌特性相关。它们的抗菌特性众所周知,但在这项工作中,我们观察了通过甲基丙烯酰胺丙基三甲基氯化铵(MAPTAC)聚合得到的大分子的抗真菌特性。这些以前未报道过的结果使我们能够将抗真菌特性与大分子的结构直接相关联,特别是分子量。这里描述的聚合物对一些丝状真菌具有抗真菌活性。最强的效果发生在分子量约为 0.5 mDa 的聚合物上,这些聚合物已经证实对多药耐药物种 Scopulariopsis brevicaulis、Fusarium oxysporum 和 Fusarium solani 以及皮肤真菌 Trichophyton mentagrophytes、Trichophyton rubrum、Trichophyton interdigitale 和 Trichophyton tonsurans 具有活性。此外,本出版物描述了这些高分子系统对血清和血液成分的影响,并对皮肤形成细胞系(即成纤维细胞和角质形成细胞)的毒性进行了初步评估。此外,使用 Franz 扩散室,证明了活性聚合物通过皮肤的低传输,这对于外用抗真菌药物是理想的效果。传染病是一个非常大的医学、社会和经济问题。甚至在 COVID-19 大流行之前,某些感染就是最常见的死亡原因之一。传染病治疗的困难尤其涉及真菌感染,我们只有少数几类药物,其中只有少数几种物质。该出版物介绍了四种 MAPTAC 聚合物对不同真菌物种的抗真菌活性研究及其对人细胞(成纤维细胞和角质形成细胞)的细胞毒性的初步结果。本文还将这些特性与两种常用抗真菌药物环吡酮和特比萘芬的类似特性进行了比较。