Palanco Ana Cerrejón, Lacorte Singulani Junya de, Costa-Orlandi Caroline Barcelos, Gullo Fernanda Patrícia, Strohmayer Lourencetti Natália Manuela, Gomes Paulo César, Ayusso Gabriela Miranda, Dutra Luiz Antônio, Silva Bolzani Vanderlan da, Regasini Luis Octávio, Soares Mendes-Giannini Maria José, Fusco-Almeida Ana Marisa
School of Pharmaceutical Sciences, UNESP - São Paulo State University, Araraquara, São Paulo, Brazil.
Institute of Biosciences, Letters & Exact Sciences, UNESP - São José do Rio Preto, São Paulo, Brazil.
Future Microbiol. 2017 Oct;12:1123-1134. doi: 10.2217/fmb-2017-0062. Epub 2017 Sep 6.
This work aimed to evaluate the activity of 3'-hydroxychalcone against Cryptococcus gattii in planktonic and biofilm forms and their toxicity using alternative animal models.
MATERIALS & METHODS: Minimum inhibitory concentration and minimum fungicide concentration were determined. Biofilm formation and the susceptibility tests were performed by the 2,3-bis-(2-methoxy-4-nitro-5-sulfophenyl)-5-[carbonyl(phenylamino)]-2H-tetrazolium hydroxide assay. Toxicity and efficacy were checked in Danio rerio and Galleria mellonella models.
The compound 3'-hydroxychalcone showed fungicidal activity against C. gattii in both planktonic and biofilm forms. The toxicity in zebrafish embryos revealed a low lethal concentration. In G. mellonella, the compound did not show antifungal activity and larvae toxicity.
Because of the activity of 3'-hydroxychalcone against C. gattii in vitro, molecular modifications should be made to improve efficacy and to reduce toxicity in vivo. [Formula: see text].
本研究旨在使用替代动物模型评估3'-羟基查耳酮对浮游和生物膜形式的加氏隐球菌的活性及其毒性。
测定最低抑菌浓度和最低杀菌浓度。通过2,3-双-(2-甲氧基-4-硝基-5-磺基苯基)-5-[羰基(苯基氨基)]-2H-氢氧化四唑法进行生物膜形成和药敏试验。在斑马鱼和大蜡螟模型中检查毒性和疗效。
化合物3'-羟基查耳酮对浮游和生物膜形式的加氏隐球菌均显示出杀菌活性。斑马鱼胚胎的毒性显示出低致死浓度。在大蜡螟中，该化合物未显示出抗真菌活性和幼虫毒性。
由于3'-羟基查耳酮在体外对加氏隐球菌具有活性，应进行分子修饰以提高疗效并降低体内毒性。[公式：见正文]
