دورية أكاديمية
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Design, synthesis, biological activity and structure-activity relationship studies of chalcone derivatives as potential anti-Candida agents.

التفاصيل البيبلوغرافية
العنوان: Design, synthesis, biological activity and structure-activity relationship studies of chalcone derivatives as potential anti-Candida agents.
المؤلفون: Andrade JT; Laboratório de Microbiologia Médica, Universidade Federal de São João del-Rei (UFSJ)-Campus Centro Oeste Dona Lindu, Divinópolis, Minas Gerais, Brazil., Santos FRS; Laboratório de Microbiologia Médica, Universidade Federal de São João del-Rei (UFSJ)-Campus Centro Oeste Dona Lindu, Divinópolis, Minas Gerais, Brazil.; Laboratório de Síntese Orgânica e Nanoestruturas, Universidade Federal de São João del-Rei (UFSJ)-Campus Centro Oeste Dona Lindu, Divinópolis, Minas Gerais, Brazil., Lima WG; Laboratório de Microbiologia Médica, Universidade Federal de São João del-Rei (UFSJ)-Campus Centro Oeste Dona Lindu, Divinópolis, Minas Gerais, Brazil., Sousa CDF; Laboratório de Microbiologia Médica, Universidade Federal de São João del-Rei (UFSJ)-Campus Centro Oeste Dona Lindu, Divinópolis, Minas Gerais, Brazil., Oliveira LSFM; Laboratório de Patologia Experimental, Universidade Federal de São João del-Rei (UFSJ)-Campus Centro Oeste Dona Lindu, Divinópolis, Minas Gerais, Brazil., Ribeiro RIMA; Laboratório de Patologia Experimental, Universidade Federal de São João del-Rei (UFSJ)-Campus Centro Oeste Dona Lindu, Divinópolis, Minas Gerais, Brazil., Gomes AJPS; Laboratório de Desenvolvimento Farmacotécnico, Universidade Federal de São João del-Rei (UFSJ)-Campus Centro Oeste Dona Lindu, Divinópolis, Minas Gerais, Brazil., Araújo MGF; Laboratório de Farmacologia, Universidade Federal de São João del-Rei (UFSJ)-Campus Centro Oeste Dona Lindu, Divinópolis, Minas Gerais, Brazil., Villar JAFP; Laboratório de Síntese Orgânica e Nanoestruturas, Universidade Federal de São João del-Rei (UFSJ)-Campus Centro Oeste Dona Lindu, Divinópolis, Minas Gerais, Brazil., Ferreira JMS; Laboratório de Microbiologia Médica, Universidade Federal de São João del-Rei (UFSJ)-Campus Centro Oeste Dona Lindu, Divinópolis, Minas Gerais, Brazil. jackmaria4@gmail.com.
المصدر: The Journal of antibiotics [J Antibiot (Tokyo)] 2018 Aug; Vol. 71 (8), pp. 702-712. Date of Electronic Publication: 2018 Apr 19.
نوع المنشور: Journal Article
اللغة: English
بيانات الدورية: Publisher: Nature Publishing Group Country of Publication: England NLM ID: 0151115 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1881-1469 (Electronic) Linking ISSN: 00218820 NLM ISO Abbreviation: J Antibiot (Tokyo) Subsets: MEDLINE
أسماء مطبوعة: Publication: 2009- : London : Nature Publishing Group
Original Publication: Tokyo, Japan Antibiotics Research Assn.
مواضيع طبية MeSH: Drug Design*, Antifungal Agents/*pharmacology , Candida albicans/*drug effects , Candidiasis, Vulvovaginal/*drug therapy , Chalcones/*chemical synthesis , Chalcones/*pharmacology, Animals ; Antifungal Agents/chemical synthesis ; Candida albicans/isolation & purification ; Cell Line ; Chlorocebus aethiops ; Cricetinae ; Female ; Humans ; Microbial Sensitivity Tests ; Rats ; Rats, Wistar ; Structure-Activity Relationship ; Vero Cells
مستخلص: Vulvovaginal candidiasis (VVC) affects millions of women around the world every year. Candida albicans is the most frequently isolated pathogen in women and its rapid ability to develop resistance to first and second line therapies has boosted the search for new and effective antifungal agents. In this study, we show the in vitro anti-Candida activity of fifteen synthetic chalcone analogs and their antifungal potential in an in vivo model of VVC. Chalcone 12 showed potent antifungal effects, being able to inhibit the growth of Candida spp. at a concentration of 15.6 µg mL -1 . In addition, mechanism of action studies have indicated the ergosterol fungal membrane as the target of this compound. Despite a considerable antifungal activity, the chalcone 12 showed high cytotoxicity in kidney cells lineages. Moreover, this compound was able to reduce Candida-associated virulence, impairing yeast-hyphal transition in C. albicans. An in vivo model of VVC showed that chalcone 12 significantly reduces the fungal load. Taken together, these findings showed that the chalcone 12 is a potent anti-Candida agent in vitro beyond of contribute to improve the fungal infection in a model of CVV. However, it showed low selectivity and high toxicity, suggesting molecular modifications to minimize these proprieties.
المشرفين على المادة: 0 (Antifungal Agents)
0 (Chalcones)
تواريخ الأحداث: Date Created: 20180421 Date Completed: 20190503 Latest Revision: 20191210
رمز التحديث: 20240628
DOI: 10.1038/s41429-018-0048-9
PMID: 29674635
قاعدة البيانات: MEDLINE
الوصف
تدمد:1881-1469
DOI:10.1038/s41429-018-0048-9