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奥米甘安及其逆行类似物单独及与氟康唑联合的抗真菌活性。

Anticandidal Activity of Omiganan and Its Retro Analog Alone and in Combination with Fluconazole.

机构信息

Department of Microbiology, Faculty of Medicine, Wroclaw Medical University, Wroclaw, Poland.

Department of Inorganic Chemistry, Faculty of Pharmacy, Medical University of Gdańsk, Gdansk, Poland.

出版信息

Probiotics Antimicrob Proteins. 2021 Aug;13(4):1173-1182. doi: 10.1007/s12602-021-09757-9. Epub 2021 Mar 2.

DOI:10.1007/s12602-021-09757-9
PMID:33655458
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8342346/
Abstract

Vulvovaginal candidiasis (VVC) is a vaginal infection that manifests itself as several symptoms which can lead to various life-threatening complications. The majority of VVC is caused by Candida albicans strains, and it is estimated that approximately 75% of women worldwide would suffer from this condition at least once during their lifetime. Surprisingly, the detailed pathomechanism of yeast-like fungi invasions in vagina is not yet fully understood. However, the ability to form biofilm on vaginal mucosa is considered as one of the critical factors associated with failure of the therapy and recurrences of the disease. Antimicrobial peptides (AMPs) are a promising class of compounds that are receiving a growing interest owing to their antibacterial, antifungal, and antibiofilm properties. Omiganan is a synthetic analog of Indolicidin that is characterized by wide spectrum of antimicrobial and antibiofilm activities. Recent reports suggest improved activity of analogs with a reversed sequence (retro-analog concept). Therefore, Omiganan and its retro analog were tested against planktonic forms and biofilm of 18 Candida strains isolated from VVC. Moreover, the synergy between the AMPs and fluconazole was studied as well. The AMPs appeared to be effective against C. albicans biofilm, and the reversion of the sequence generally led to an improved antimicrobial activity. Furthermore, confocal and scanning electron microscopic visualizations revealed the effectiveness of AMPs-fluconazole combinations also against fluconazole-resistant strains.

摘要

外阴阴道念珠菌病(VVC)是一种阴道感染,表现为多种症状,可导致各种危及生命的并发症。大多数 VVC 是由白色念珠菌菌株引起的,据估计,全世界约有 75%的女性在其一生中至少会患一次这种疾病。令人惊讶的是,酵母样真菌侵袭阴道的详细发病机制尚未完全了解。然而,在阴道黏膜上形成生物膜的能力被认为是与治疗失败和疾病复发相关的关键因素之一。抗菌肽(AMPs)是一类很有前途的化合物,由于其具有抗菌、抗真菌和抗生物膜特性,越来越受到关注。奥米加南是一种吲哚西丁的合成类似物,具有广谱的抗菌和抗生物膜活性。最近的报告表明,具有反转序列的类似物(反转类似物概念)的活性得到了改善。因此,奥米加南及其反转类似物被测试了对来自 VVC 的 18 株念珠菌分离株的浮游形式和生物膜的作用。此外,还研究了 AMPs 与氟康唑之间的协同作用。AMPs 似乎对白色念珠菌生物膜有效,而且序列的反转通常会提高抗菌活性。此外,共聚焦和扫描电子显微镜观察显示,AMP-氟康唑联合用药对氟康唑耐药菌株也有效。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/269e/8342346/1dddd2cb6b30/12602_2021_9757_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/269e/8342346/efd3998e618d/12602_2021_9757_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/269e/8342346/c2a1763be2b7/12602_2021_9757_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/269e/8342346/b4c007c8ea2f/12602_2021_9757_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/269e/8342346/1dddd2cb6b30/12602_2021_9757_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/269e/8342346/efd3998e618d/12602_2021_9757_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/269e/8342346/c2a1763be2b7/12602_2021_9757_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/269e/8342346/b4c007c8ea2f/12602_2021_9757_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/269e/8342346/1dddd2cb6b30/12602_2021_9757_Fig4_HTML.jpg

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