Letters in Applied Microbiology
Volume 45 Issue 2 Page 148-153, August 2007
To cite this article: S. Johann, C. Soldi, J.P. Lyon, M.G.
Pizzolatti, M.A. Resende (2007)
Antifungal activity of the amyrin
derivatives and in vitro inhibition of Candida albicans adhesion
to human epithelial cells
Letters in Applied Microbiology 45 (2), 148–153.
doi:10.1111/j.1472-765X.2007.02162.x
Antifungal activity of the amyrin derivatives and in vitro inhibition of Candida albicans adhesion to human epithelial cells
- S. Johann11 Departamento de Microbiologia, Instituto de Ciências Biológicas, Universidade Federal de Minas Gerais, Belo Horizonte, MG, Brazil,
- C. Soldi22 Departamento de Química, Universidade de Santa Catarina, Florianópolis, SC, Brazil,
- J.P. Lyon11 Departamento de Microbiologia, Instituto de Ciências Biológicas, Universidade Federal de Minas Gerais, Belo Horizonte, MG, Brazil,
- M.G. Pizzolatti22 Departamento de Química, Universidade de Santa Catarina, Florianópolis, SC, Brazil and
- M.A. Resende11 Departamento de Microbiologia, Instituto de Ciências Biológicas, Universidade Federal de Minas Gerais, Belo Horizonte, MG, Brazil
E-mail: maresend@icb.ufmg.br
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 α- and β-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, α- and β-amyrin formiate (2) and α-
and β-amyrin acetate (3) were the most active, inhibiting all the
Candida species tested in concentrations that ranged from 30 to
250 μg ml
1. α- and β-amyrin
formiate inhibited the adhesion ability of C. albicans to buccal
epithelial cells (BEC) in 65·3%.
Conclusions: α- and β-amyrin formiate and α- and β-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, α- and β-amyrin formiate was as effective as fluconazole in inhibiting the adhesion of C. albicans to buccal epithelial cells.