S Johann1, C Soldi, J P Lyon, M G Pizzolatti, M A Resende. 1. Departamento de Microbiologia, Instituto de Ciências Biológicas, Universidade Federal de Minas Gerais, Belo Horizonte, MG, Brazil.
Abstract
AIMS: The antifungal activity of amyrin pentacyclic triterpene and 15 synthetic derivatives was evaluated against Candida species. Additionally, inhibition of adhesion of Candida albicans to human epithelial cells in vitro was determined. METHODS AND RESULTS: Esterification of alpha- and beta-amyrin with a variety of acyl chlorides produced a series of analogue derivatives. These substances were synthesized to evaluate the antifungal properties against Candida species. Among the 15 derivatives, alpha- and beta-amyrin formiate (2) and alpha- and beta-amyrin acetate (3) were the most active, inhibiting all the Candida species tested in concentrations that ranged from 30 to 250 microg ml(-1). alpha- and beta-amyrin formiate inhibited the adhesion ability of C. albicans to buccal epithelial cells (BEC) in 65.3%. CONCLUSIONS: alpha- and beta-amyrin formiate and alpha- and beta-amyrin acetate derivatives exhibited potential antifungal activity against Candida spp. and amyrin formiate showed inhibition of the adhesion ability of C. albicans to buccal epithelial cells. SIGNIFICANCE AND IMPACT OF THE STUDY: This study demonstrated that two derivatives of amyrin pentacyclic triterpene exhibited significant antifungal activity against Candida species. Additionally, alpha- and beta-amyrin formiate was as effective as fluconazole in inhibiting the adhesion of C. albicans to buccal epithelial cells.
AIMS: The antifungal activity of amyrin pentacyclictriterpene and 15 synthetic derivatives was evaluated against Candida species. Additionally, inhibition of adhesion of Candida albicans to human epithelial cells in vitro was determined. METHODS AND RESULTS: Esterification of alpha- and beta-amyrin with a variety of acyl chlorides produced a series of analogue derivatives. These substances were synthesized to evaluate the antifungal properties against Candida species. Among the 15 derivatives, alpha- and beta-amyrin formiate (2) and alpha- and beta-amyrin acetate (3) were the most active, inhibiting all the Candida species tested in concentrations that ranged from 30 to 250 microg ml(-1). alpha- and beta-amyrin formiate inhibited the adhesion ability of C. albicans to buccal epithelial cells (BEC) in 65.3%. CONCLUSIONS:alpha- and beta-amyrin formiate and alpha- and beta-amyrin acetate derivatives exhibited potential antifungal activity against Candida spp. and amyrin formiate showed inhibition of the adhesion ability of C. albicans to buccal epithelial cells. SIGNIFICANCE AND IMPACT OF THE STUDY: This study demonstrated that two derivatives of amyrin pentacyclictriterpene exhibited significant antifungal activity against Candida species. Additionally, alpha- and beta-amyrin formiate was as effective as fluconazole in inhibiting the adhesion of C. albicans to buccal epithelial cells.