title: Evaluation of Antifungal Activity and Mode of Action of New Coumarin Derivative, 7-Hydroxy-6-nitro-2H-1-benzopyran-2-one, against Aspergillus spp.
abstract: Aspergillus spp. produce a wide variety of diseases. For the treatment of such infections, the azoles and Amphotericin B are used in various formulations. The treatment of fungal diseases is often ineffective, because of increases in azole resistance and their several associated adverse effects. To overcome these problems, natural products and their derivatives are interesting alternatives. The aim of this study was to examine the effects of coumarin derivative, 7-hydroxy-6-nitro-2H-1-benzopyran-2-one (Cou-NO2), both alone and with antifungal drugs. Its mode of action against Aspergillus spp. Cou-NO2 was tested to evaluate its effects on mycelia growth and germination of fungal conidia of Aspergillus spp. We also investigated possible Cou-NO2 action on cell walls (0.8 M sorbitol) and on Cou-NO2 to ergosterol binding in the cell membrane. The study shows that Cou-NO2 is capable of inhibiting both the mycelia growth and germination of conidia for the species tested, and that its action affects the structure of the fungal cell wall. At subinhibitory concentration, Cou-NO2 enhanced the in vitro effects of azoles. Moreover, in combination with azoles (voriconazole and itraconazole) Cou-NO2 displays an additive effect. Thus, our study supports the use of coumarin derivative 7-hydroxy-6-nitro-2H-1-benzopyran-2-one as an antifungal agent against Aspergillus species.
authors.affiliation: Pharmaceutical Science Department, Federal University of Paraíba, 58051-970 João Pessoa, PB, Brazil.
authors.forename: Felipe Queiroga Sarmento
authors.initials: FQ
authors.lastname: Guerra
authors.affiliation: Laboratory of Synthesis and Drug Delivery, Biological Science Department, State University of Paraíba, 58020-540 João Pessoa, PB, Brazil.
authors.forename: Rodrigo Santos Aquino
authors.initials: RS
authors.lastname: de Araújo
authors.affiliation: Pharmaceutical Science Department, Federal University of Paraíba, 58051-970 João Pessoa, PB, Brazil.
authors.forename: Janiere Pereira
authors.initials: JP
authors.lastname: de Sousa
authors.affiliation: Center of Education and Heath, Federal University of Campina Grande, 58175-000 Cuité, PB, Brazil.
authors.forename: Fillipe de Oliveira
authors.initials: Fde O
authors.lastname: Pereira
authors.affiliation: Laboratory of Synthesis and Drug Delivery, Biological Science Department, State University of Paraíba, 58020-540 João Pessoa, PB, Brazil.
authors.forename: Francisco J B
authors.initials: FJ
authors.lastname: Mendonça-Junior
authors.affiliation: Laboratory of Synthesis and Drug Delivery, Biological Science Department, State University of Paraíba, 58020-540 João Pessoa, PB, Brazil.
authors.forename: José M
authors.initials: JM
authors.lastname: Barbosa-Filho
authors.affiliation: Pharmaceutical Science Department, Federal University of Paraíba, 58051-970 João Pessoa, PB, Brazil.
authors.forename: Edeltrudes
authors.initials: E
authors.lastname: de Oliveira Lima