Departamento de Microbiologia, ICB, UFMG, Av. Pres. Antonio Carlos, Pampulha, Belo Horizonte, MG 31270-901, Brazil.
J Appl Microbiol. 2009 Oct;107(4):1279-86. doi: 10.1111/j.1365-2672.2009.04307.x. Epub 2009 Apr 9.
The antifungal activity of (R)-goniothalamin (1) and (S)-goniothalamin (ent-1) was evaluated against six Candida species. The in vitro effect of these compounds on yeast adhesion to human buccal epithelial cells (BEC) and Candida albicans and C. dubliniensis biofilms progression were also investigated.
Yeast susceptibility was evaluated by broth microdilution assay and showed that ent-1 exhibited higher potency against all fungal clinical isolated when compared to compound 1. Compounds 1 and ent-1 were as potent as fluconazole in inhibiting the adhesion of C. albicans and C. dubliniensis to BEC. XTT-reducing assay and scanning electron microscopy revealed that 1 and ent-1 were twice as potent as fluconazole in the inhibition of yeast biofilms progression.
Our findings indicate that compounds 1 and ent-1 are potent anticandidal agents.
This study highlights goniothalamin enantiomers as promising lead compounds for the design of new antifungal with inhibitory activity on yeast adhesion and biofilm progression.
评估(R)-钩藤素(1)和(S)-钩藤素(ent-1)对六种念珠菌的抗真菌活性。还研究了这些化合物对酵母与人颊上皮细胞(BEC)和白色念珠菌和杜氏念珠菌生物膜进展的粘附的体外影响。
通过肉汤微量稀释法评估酵母易感性,结果表明与化合物 1 相比,ent-1 对所有真菌临床分离株均表现出更高的活性。化合物 1 和 ent-1 在抑制白色念珠菌和杜氏念珠菌与 BEC 粘附方面与氟康唑一样有效。XTT 还原测定和扫描电子显微镜显示,1 和 ent-1 在抑制酵母生物膜进展方面的效力是氟康唑的两倍。
我们的研究结果表明,化合物 1 和 ent-1 是有效的抗真菌剂。
本研究强调了钩藤素对映异构体作为设计具有抑制酵母粘附和生物膜进展活性的新型抗真菌药物的有前途的先导化合物。