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Antifungal efficacy of atorvastatin-containing emulgel in the treatment of oral and vulvovaginal candidiasis
Medical Mycology ( IF 2.7 ) Pub Date : 2020-08-21 , DOI: 10.1093/mmy/myaa071
Ari Soares de Oliveira Neto 1 , Israel Lucas Antunes Souza 1 , Maria Eliza Samuel Amorim 2 , Thalita de Freitas Souza 3 , Vinicius Novaes Rocha 4 , Rene Oliveira do Couto 2 , Rodrigo Luiz Fabri 3 , Marcelo Gonzaga de Freitas Araújo 1
Affiliation  

Drug repositioning has been an important ally in the search for new antifungal drugs. Statins are drugs that act to prevent sterol synthesis in both humans and fungi and for this reason they are promissory candidates to be repositioned to treat mycoses. In this study we evaluated the antifungal activity of atorvastatin by in vitro tests to determine the minimum inhibitory concentration against azole resistant Candida albicans and its mechanisms of action. Moreover, the efficacy of both atorvastatin-loaded oral and vaginal emulgels (0.75%, 1.5% and 3% w/w) was evaluated by means of in vivo experimental models of oral and vulvovaginal candidiasis, respectively. The results showed that atorvastatin minimal inhibitory concentration against C. albicans was 31.25 μg/ml. In oral candidiasis experiments, the group treated with oral emulgel containing 3.0% atorvastatin showcased total reduction in fungal load after nine days of treatment. Intravaginal delivery atorvastatin emulgel showed considerable effectiveness at the concentration of 3% (65% of fungal burden reduction) after nine days of treatment. From these findings, it is possible to assert that atorvastatin may be promising for drug repositioning towards the treatment of these opportunistic mycoses.

中文翻译:

含阿托伐他汀乳剂治疗口腔和外阴阴道念珠菌病的抗真菌作用

药物重新定位一直是寻找新抗真菌药物的重要盟友。他汀类药物是用于阻止人类和真菌中甾醇合成的药物,因此它们是重新定位以治疗真菌病的候选药物。在这项研究中,我们通过体外试验评估了阿托伐他汀的抗真菌活性,以确定对唑类抗性白色念珠菌的最小抑制浓度及其作用机制。此外,分别通过口腔和外阴阴道念珠菌病的体内实验模型评估了载有阿托伐他汀的口服和阴道乳剂(0.75%、1.5% 和 3% w/w)的功效。结果表明,阿托伐他汀对白色念珠菌的最小抑制浓度为 31.25 μg/ml。在口腔念珠菌病实验中,用含有 3.0% 阿托伐他汀的口服乳剂治疗的组在治疗 9 天后表现出真菌负荷完全减少。治疗 9 天后,阴道内给药阿托伐他汀乳剂在浓度为 3%(真菌负担减少的 65%)时显示出相当大的有效性。根据这些发现,可以断言阿托伐他汀可能有望重新定位药物以治疗这些机会性真菌病。
更新日期:2020-08-21
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