ROCHA, M. A. N.; http://lattes.cnpq.br/8784128618433735; ROCHA, Marcelo Antônio Nóbrega da.
Abstract:
Dermatophytosis is a fungal disease that affects the skin, hair and nails
mainly by Trichophyton rubrum, Microsporum canis and Nannizzia gypsea.
Treatment occurs by administering ketoconazole, itraconazole and terbinafine.
However, the ability of dermatophytes to develop biofilms makes therapy difficult,
as it impairs the permeation of drugs in infected tissues. So, research to find new
anti-dermatophyte biofilm drugs is crucial. Therefore, the aim of this study was to
evaluate the antifungal activity of Riparin 2 and its synthetic counterparts NOR-2
and DINOR-2 against the fungal growth of biofilms of T. rubrum, M. canis and N.
gypsea. For this, the microdilution technique was used with ciclopirox as a
positive control. The quantification of in vitro biofilm biomass was evaluated after
staining with 0.5% crystal violet, and the viability of the biofilm by quantification
of the CFU number. The ex vivo model was performed on fragments of human
nails, which were evaluated by visualization in light microscopy and quantification
of the CFU number (viability). The compounds RIP2 and NOR-2 showed
antifungal activity against strains of T. rubrum, M. canis and N. gypsea, but
DINOR2 did not show significant antifungal activity against dermatophytes.
Furthermore, RIP2 and NOR-2 significantly reduced the viability of biofilms in vitro
and ex vivo (p < 0.05). RIP2 was more potent than NOR-2, possibly due to the
distance between the chemical chain portions in these compounds. Therefore,
this study can serve to direct the research of compounds with anti-dermatophyte
activity, since the RIP2 and NOR-2 molecules showed promise in terms of
antifungal and antibiofilm activity.