Evaluation of (-)-Fenchone antimicrobial activity against oral Candida albicans and toxicological parameters: an in silico, in vitro and ex vivo study.

IF 1.1 4区 综合性期刊 Q3 MULTIDISCIPLINARY SCIENCES Anais da Academia Brasileira de Ciencias Pub Date : 2024-11-01 eCollection Date: 2024-01-01 DOI:10.1590/0001-3765202420240273
André A Dos Santos, Abrahão A DE Oliveira-Filho, Bráulio A Teixeira, José Lucas F M Galvão, Maria Alice A DE Medeiros, Millena S Alves, David Henrique X Barbosa, Rodrigo P Mafra, Ulrich Vasconcelos, Edeltrudes O Lima
{"title":"Evaluation of (-)-Fenchone antimicrobial activity against oral Candida albicans and toxicological parameters: an in silico, in vitro and ex vivo study.","authors":"André A Dos Santos, Abrahão A DE Oliveira-Filho, Bráulio A Teixeira, José Lucas F M Galvão, Maria Alice A DE Medeiros, Millena S Alves, David Henrique X Barbosa, Rodrigo P Mafra, Ulrich Vasconcelos, Edeltrudes O Lima","doi":"10.1590/0001-3765202420240273","DOIUrl":null,"url":null,"abstract":"<p><p>Candida albicans is the primary species causing oral candidiasis. Its increasing drug resistance drives the search for more effective antifungal agents. Therefore, we assessed toxicological parameters and the antimicrobial activity and mechanisms of action of the monoterpene (-)-fenchone against oral C. albicans. We conducted an in silico study using PASS online and AdmetSAR, followed by evaluation of antifungal activity through Minimum Inhibitory Concentration (MIC), Minimum Fungicidal Concentration (MFC), association study with miconazole, and assays with sorbitol and ergosterol. Inhibition of biofilm formation and disruption of preformed biofilm were considered. Toxicity was also assessed through hemolysis assay. The in silico study revealed a higher likelihood of the compound being active for antifungal activity, as well as promising pharmacokinetic and toxicity characteristics. Subsequently, (-)-fenchone exhibited predominantly fungicidal activity (MIC90 = 8 μg/mL; MFC = 16 μg/mL), including against miconazole-resistant C. albicans isolates. The substance does not appear to act by damaging the fungal cell wall or plasma membrane, and exhibited synergy with miconazole. There was activity in inhibiting biofilm formation but not in disrupting preformed biofilm. Finally, the product exerted low hemolytic activity at more than MIC×10. Based on these results, (-)-fenchone may represent a promising therapeutic alternative for oral candidiasis.</p>","PeriodicalId":7776,"journal":{"name":"Anais da Academia Brasileira de Ciencias","volume":null,"pages":null},"PeriodicalIF":1.1000,"publicationDate":"2024-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Anais da Academia Brasileira de Ciencias","FirstCategoryId":"103","ListUrlMain":"https://doi.org/10.1590/0001-3765202420240273","RegionNum":4,"RegionCategory":"综合性期刊","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"2024/1/1 0:00:00","PubModel":"eCollection","JCR":"Q3","JCRName":"MULTIDISCIPLINARY SCIENCES","Score":null,"Total":0}
引用次数: 0

Abstract

Candida albicans is the primary species causing oral candidiasis. Its increasing drug resistance drives the search for more effective antifungal agents. Therefore, we assessed toxicological parameters and the antimicrobial activity and mechanisms of action of the monoterpene (-)-fenchone against oral C. albicans. We conducted an in silico study using PASS online and AdmetSAR, followed by evaluation of antifungal activity through Minimum Inhibitory Concentration (MIC), Minimum Fungicidal Concentration (MFC), association study with miconazole, and assays with sorbitol and ergosterol. Inhibition of biofilm formation and disruption of preformed biofilm were considered. Toxicity was also assessed through hemolysis assay. The in silico study revealed a higher likelihood of the compound being active for antifungal activity, as well as promising pharmacokinetic and toxicity characteristics. Subsequently, (-)-fenchone exhibited predominantly fungicidal activity (MIC90 = 8 μg/mL; MFC = 16 μg/mL), including against miconazole-resistant C. albicans isolates. The substance does not appear to act by damaging the fungal cell wall or plasma membrane, and exhibited synergy with miconazole. There was activity in inhibiting biofilm formation but not in disrupting preformed biofilm. Finally, the product exerted low hemolytic activity at more than MIC×10. Based on these results, (-)-fenchone may represent a promising therapeutic alternative for oral candidiasis.

查看原文
分享 分享
微信好友 朋友圈 QQ好友 复制链接
本刊更多论文
评估(-)-葑酮对口腔白色念珠菌的抗菌活性和毒理学参数:一项体内、体外和体外研究。
白色念珠菌是引起口腔念珠菌病的主要菌种。它的耐药性不断增加,促使人们寻找更有效的抗真菌剂。因此,我们评估了单萜 (-)-fenchone 对口腔白色念珠菌的毒理学参数、抗菌活性和作用机制。我们使用 PASS 在线和 AdmetSAR 进行了一项硅学研究,然后通过最低抑菌浓度 (MIC)、最低杀菌浓度 (MFC)、与咪康唑的关联研究以及与山梨醇和麦角甾醇的检测评估了抗真菌活性。还考虑了抑制生物膜形成和破坏已形成的生物膜。还通过溶血试验对毒性进行了评估。硅学研究显示,该化合物具有抗真菌活性的可能性较高,而且药代动力学和毒性特征也很好。随后,(-)-fenchone 主要表现出杀菌活性(MIC90 = 8 μg/mL;MFC = 16 μg/mL),包括对耐咪康唑的白僵菌分离株。该物质似乎不是通过破坏真菌细胞壁或质膜发挥作用,而是与咪康唑协同作用。在抑制生物膜形成方面有活性,但在破坏已形成的生物膜方面没有活性。最后,该产品在 MIC×10 以上时的溶血活性较低。基于这些结果,(-)-葑酮可能是治疗口腔念珠菌病的一种有前途的替代疗法。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
求助全文
约1分钟内获得全文 去求助
来源期刊
Anais da Academia Brasileira de Ciencias
Anais da Academia Brasileira de Ciencias 综合性期刊-综合性期刊
CiteScore
2.20
自引率
0.00%
发文量
347
审稿时长
1 months
期刊介绍: The Brazilian Academy of Sciences (BAS) publishes its journal, Annals of the Brazilian Academy of Sciences (AABC, in its Brazilianportuguese acronym ), every 3 months, being the oldest journal in Brazil with conkinuous distribukion, daking back to 1929. This scienkihic journal aims to publish the advances in scienkihic research from both Brazilian and foreigner scienkists, who work in the main research centers in the whole world, always looking for excellence. Essenkially a mulkidisciplinary journal, the AABC cover, with both reviews and original researches, the diverse areas represented in the Academy, such as Biology, Physics, Biomedical Sciences, Chemistry, Agrarian Sciences, Engineering, Mathemakics, Social, Health and Earth Sciences.
期刊最新文献
Academic impact and scientific quality should not be conflated. Clinical evaluation of combined autologous Platelet-Rich Plasma and Volume-Controlled Ozone Therapy in Facial Rejuvenation: A randomized controlled Pilot Study. Comprehensive assessment of the health condition of managed honey bees potentially exposed to contamination with agrochemical residues. In vitro induced cold memory fails to enhance embryogenic cultures development in Araucaria angustifolia. Evaluation of (-)-Fenchone antimicrobial activity against oral Candida albicans and toxicological parameters: an in silico, in vitro and ex vivo study.
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
现在去查看 取消
×
提示
确定
0
微信
客服QQ
Book学术公众号 扫码关注我们
反馈
×
意见反馈
请填写您的意见或建议
请填写您的手机或邮箱
已复制链接
已复制链接
快去分享给好友吧!
我知道了
×
扫码分享
扫码分享
Book学术官方微信
Book学术文献互助
Book学术文献互助群
群 号:481959085
Book学术
文献互助 智能选刊 最新文献 互助须知 联系我们:info@booksci.cn
Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。
Copyright © 2023 Book学术 All rights reserved.
ghs 京公网安备 11010802042870号 京ICP备2023020795号-1