Antifungal activity of the amyrin derivatives and in vitro inhibition of Candida albicans adhesion to human epithelial cells.
OBJECTIVE
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.


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.


CONCLUSIONS
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.
Johann
S
S
Departamento de Microbiologia, Instituto de Ciências Biológicas, Universidade Federal de Minas Gerais, Belo Horizonte, MG, Brazil.
Soldi
C
C
Lyon
J P
JP
Pizzolatti
M G
MG
Resende
M A
MA
D000328:Adult; D000935:Antifungal Agents / Q000737:chemistry / Q000494:pharmacology*; D002176:Candida albicans / Q000187:drug effects* / Q000502:physiology*; D002448:Cell Adhesion / Q000187:drug effects; D002478:Cells, Cultured; D004847:Epithelial Cells / Q000382:microbiology*; D006801:Humans; D008826:Microbial Sensitivity Tests; D009061:Mouth Mucosa / Q000166:cytology / Q000382:microbiology*; D009828:Oleanolic Acid / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology
D000935:Antifungal Agents; D009828:Oleanolic Acid; C036380:beta-amyrin