Silva Bruna L R, Simão Gisele, Campos Carmem D L, Monteiro Cinara R A V, Bueno Laryssa R, Ortis Gabriel B, Mendes Saulo J F, Moreira Israel Viegas, Maria-Ferreira Daniele, Sousa Eduardo M, Vidal Flávia C B, Monteiro Cristina de Andrade, Monteiro-Neto Valério, Fernandes Elizabeth S
Programa de Pós-Graduação em Biodiversidade e Biotecnologia da Rede BIONORTE, Universidade Federal do Maranhão, São Luís 65085-040, MA, Brazil.
Programa de Pós-Graduação em Biotecnologia Aplicada à Saúde da Criança e do Adolescente, Faculdades Pequeno Príncipe, Av. Iguaçu No 333, Curitiba 80230-020, PR, Brazil.
Antibiotics (Basel). 2022 Dec 19;11(12):1842. doi: 10.3390/antibiotics11121842.
Oropharyngeal candidiasis/candidosis is a common and recurrent opportunistic fungal infection. Fluconazole (FLZ), one of the most used and effective antifungal agents, has been associated with a rise of resistant species in immunocompromised patients undergoing prophylactic therapy. Sulforaphane (SFN), a compound from cruciferous vegetables, is an antimicrobial with yet controversial activities and mechanisms on fungi. Herein, the in silico and antifungal activities of SFN against were investigated. In silico analyzes for the prediction of the biological activities and oral bioavailability of SFN, its possible toxicity and pharmacokinetic parameters, as well as the estimates of its gastrointestinal absorption, permeability to the blood-brain barrier and skin, and similarities to drugs, were performed by using different software. SFN in vitro anti- activities alone and in combination with fluconazole (FLZ) were determined by the broth microdilution method and the checkerboard, biofilm and hyphae formation tests. Amongst the identified probable biological activities of SFN, nine indicated an antimicrobial potential. SFN was predicted to be highly absorbable by the gastrointestinal tract, to present good oral availability, and not to be irritant and/or hepatotoxic. SFN presented antifungal activity against and prevented both biofilm and hyphae formation by this microorganism. SFN was additive/synergistic to FLZ. Overall, the data highlights the anti- activity of SFN and its potential to be used as an adjuvant therapy to FLZ in clinical settings.
口腔念珠菌病是一种常见的复发性机会性真菌感染。氟康唑(FLZ)是最常用且有效的抗真菌药物之一,在接受预防性治疗的免疫功能低下患者中,它与耐药菌株的增加有关。萝卜硫素(SFN)是一种来自十字花科蔬菜的化合物,是一种对真菌具有争议性活性和作用机制的抗菌剂。在此,研究了SFN对[具体对象未提及]的计算机模拟和抗真菌活性。通过使用不同软件对SFN的生物活性、口服生物利用度、可能的毒性和药代动力学参数进行了计算机模拟分析,以及对其胃肠道吸收、血脑屏障和皮肤通透性以及与药物的相似性进行了估计。通过肉汤微量稀释法、棋盘法、生物膜和菌丝形成试验测定了SFN单独以及与氟康唑(FLZ)联合的体外抗[具体对象未提及]活性。在已确定的SFN可能的生物活性中,有九种表明具有抗菌潜力。预测SFN可被胃肠道高度吸收,具有良好的口服生物利用度,且无刺激性和/或肝毒性。SFN对[具体对象未提及]具有抗真菌活性,并可防止该微生物形成生物膜和菌丝。SFN与FLZ具有相加/协同作用。总体而言数据突出了SFN的抗[具体对象未提及]活性及其在临床环境中作为FLZ辅助治疗的潜力。