scholarly journals The In Vitro Potential of 1-(1H-indol-3-yl) Derivatives against Candida spp. and Aspergillus niger as Tyrosinase Inhibitors

2021 ◽  
Vol 9 (10) ◽  
pp. 2070
Author(s):  
Teresa Gervasi ◽  
Giovanna Ginestra ◽  
Francesca Mancuso ◽  
Davide Barreca ◽  
Laura De Luca ◽  
...  

Given the increased antimicrobial resistance, global effort is currently focused on the identification of novel compounds, both of natural and chemical origin. The present study reports on the antifungal potential of 1-(1H-indol-3-yl) derivatives, previously known as tyrosinase inhibitors. The effect of seven compounds (indicated as 3a–g) was determined against Candida albicans ATCC 10531, three clinical isolates of Candida albicans, two clinical isolates of Candida glabrata, two clinical isolates of Candida parapsilosis and Aspergillus niger ATCC 16404. The effect of these derivatives on tyrosinase enzymatic activity was also evaluated. Results showed a fungicidal activity of compounds 3b, 3c and 3e against all tested strains at concentrations ranging between 0.250 and 1 mg/mL. Furthermore, the association between 3c and fluconazole and between 3b and caspofungin showed a trend of indifference tending toward synergism. Compound 3c was also able to inhibit microbial tyrosinase up to ~28% at the concentration of 0.250 mg/mL. These data could help provide novel therapeutics for topical use to treat fungal infections and increase the potential effectiveness of the association between novel compounds and commercial antifungals in order to combat drug resistance.

Molecules ◽  
2021 ◽  
Vol 26 (19) ◽  
pp. 5760
Author(s):  
Elda M. Melchor-Martínez ◽  
Juan F. Tamez-Fernández ◽  
Gloria María González-González ◽  
David A. Silva-Mares ◽  
Noemí Waksman-Minsky ◽  
...  

Candida albicans is the most commonly implicated agent in invasive human fungal infections. The disease could be presented as minimal symptomatic candidemia or can be fulminant sepsis. Candidemia is associated with a high rate of mortality and high healthcare and hospitalization costs. The surveillance programs have reported the distribution of other Candida species reflecting the trends and antifungal susceptibilities. Previous studies have demonstrated that C. glabrata more frequently presents fluconazole-resistant strains. Extracts from Mexican plants have been reported with activity against pulmonary mycosis, among them Colubrina greggii. In the present study, extracts from the aerial parts (leaves, flowers, and fruits) of this plant were evaluated against clinical isolates of several species of Candida (C. albicans, C. glabrata, C. parapsilosis, C. krusei, and C. tropicalis) by the broth microdilution assay. Through bioassay-guided fractionation, three antifungal glycosylated flavonoids were isolated and characterized. The isolated compounds showed antifungal activity only against C. glabrata resistant to fluconazole, and were non-toxic toward brine shrimp lethality bioassay and in vitro Vero cell line assay. The ethyl acetate and butanol extracts, as well as the fractions containing the mixture of flavonoids, were more active against Candida spp.


2017 ◽  
Vol 89 (3) ◽  
pp. 205-211 ◽  
Author(s):  
Danielle Hall ◽  
Robert Bonifas ◽  
Lauretta Stapert ◽  
Mary Thwaites ◽  
Dean L. Shinabarger ◽  
...  

2002 ◽  
Vol 46 (6) ◽  
pp. 1723-1727 ◽  
Author(s):  
M. A. Pfaller ◽  
S. A. Messer ◽  
R. J. Hollis ◽  
R. N. Jones ◽  
D. J. Diekema

ABSTRACT The in vitro activities of ravuconazole and voriconazole were compared with those of amphotericin B, flucytosine (5FC), itraconazole, and fluconazole against 6,970 isolates of Candida spp. obtained from over 200 medical centers worldwide. Both ravuconazole and voriconazole were very active against all Candida spp. (MIC at which 90% of the isolates tested are inhibited [MIC90], 0.25 μg/ml; 98% of MICs were ≤1 μg/ml); however, a decrease in the activities of both of these agents was noted among isolates that were susceptible-dose dependent (fluconazole MIC, 16 to 32 μg/ml) and resistant (MIC, ≥ 64 μg/ml) to fluconazole. Candida albicans was the most susceptible species (MIC90 of both ravuconazole and voriconazole, 0.03 μg/ml), and C. glabrata was the least susceptible species (MIC90, 1 to 2 μg/ml). Ravuconazole and voriconazole were each more active in vitro than amphotericin B, 5FC, itraconazole, and fluconazole against all Candida spp. and were the only agents with good in vitro activity against C. krusei. These results provide further evidence for the spectrum and potency of ravuconazole and voriconazole against a large and geographically diverse collection of Candida spp.


2021 ◽  
Vol 10 (15) ◽  
pp. e440101523110
Author(s):  
Luanna de Oliveira e Lima ◽  
Larissa Alves Silva ◽  
Mariana Cavalcante Fonseca ◽  
Hermez Diniz-Neto ◽  
Edeltrudes de Oliveira Lima ◽  
...  

Introdução: A candidíase está relacionada a uma grande variedade de manifestações clínicas que se expressam desde infecções na pele e mucosas à infecção sistêmica. Sendo esta última associada a uma alta taxa de mortalidade global, variando de 36% a 63% em diferentes grupos de pacientes. A terapêutica de infecções fúngicas invasivas é limitada pois há apenas três classes de fármacos convencionais utilizados. Diante deste cenário, estratégias de uso racional dos antifúngicos e busca de novas alternativas terapêuticas se fazem necessárias. Objetivo: Avaliar a atividade antifúngica in vitro do monoterpeno di-hidrojasmona frente cepas de Candida albicans e Candida parapsilosis fluconazol resistentes. Metodologia: As concentrações inibitórias mínimas (CIM) e fungicida mínima (CFM) foram determinadas pelo método de microdiluição. Posteriormente foi observado se a ação antifúngica de di-hidrojasmona ocorre via parede celular (ensaio com sorbitol) ou via membrana (ensaio com ergosterol exógeno). Resultados: A di-hidrojasmona apresentou uma CIM entre 128 - 256 µg/mL e a CFM teve os mesmos valores de CIM, respectivamente. No ensaio com ergosterol exógeno, a CIM da di-hidrojasmona aumentou na presença do ergosterol exógeno sugerindo que o mecanismo de ação do monoterpeno ocorre a partir de sua ligação ao ergosterol presente na membrana. Não houve alteração frente ao uso do sorbitol. Conclusão: Baseado nestes resultados, o presente estudo demonstra que di-hidrojasmona possui forte atividade antifúngica e sugere que esta atividade esteja relacionada a sua ligação ao ergosterol da membrana fúngica. Logo, di-hidrojasmona demostra ser um promissor bioproduto na busca de alternativas para o tratamento das candidíases.


2021 ◽  
Vol 7 (12) ◽  
pp. 1070
Author(s):  
Pratibha Sharma ◽  
Mehak Chaudhary ◽  
Garima Khanna ◽  
Praveen Rishi ◽  
Indu Pal Kaur

Fungi are reported to cause a range of superficial to invasive human infections. These often result in high morbidity and at times mortality. Conventional antifungal agents though effective invariably exhibit drug interactions, treatment-related toxicity, and fail to elicit significant effect, thus indicating a need to look for suitable alternatives. Fungi thrive in humid, nutrient-enriched areas. Such an environment is well-supported by the oral cavity. Despite this, there is a relatively low incidence of severe oral and periodontal fungal infections, attributed to the presence of antimicrobial peptides hosted by saliva, viz. histatin 5 (Hstn 5). It displays fungicidal activity against a variety of fungi including Candida albicans, Candida glabrata, Candida krusei, Cryptococcus neoformans, and unicellular yeast-like Saccharomyces cerevisiae. Candida albicans alone accounts for about 70% of all global fungal infections including periodontal disease. This review intends to discuss the scope of Hstn 5 as a novel recourse for the control of fungal infections.


2001 ◽  
Vol 45 (6) ◽  
pp. 1905-1907 ◽  
Author(s):  
Manuel Cuenca-Estrella ◽  
Emilia Mellado ◽  
Teresa M. Dı́az-Guerra ◽  
Araceli Monzón ◽  
Juan L. Rodrı́guez-Tudela

ABSTRACT The in vitro activity of the azasordarin GW 471558 was compared with those of amphotericin B, flucytosine, itraconazole, and ketoconazole against 177 clinical isolates of Candidaspp. GW 471558 showed potent activity against Candida albicans, Candida glabrata, and Candida tropicalis, even against isolates with decreased susceptibility to azoles. Candida krusei, Candida parapsilosis, Candida lusitaniae, and Candida guilliermondii are resistant to GW 471558 in vitro (MICs, >128 μg/ml).


2015 ◽  
Vol 21 (5-6) ◽  
pp. 255-266
Author(s):  
Carmen A. Vides-Peña ◽  
Nalleth D. Bolaño-Ardila ◽  
Máryuris V. Vides-Peña ◽  
Susana B. Córdoba

Introducción: la candidemia es una enfermedad grave, con elevada morbi-mortalidad y cuyo tratamiento no siempre conduce a la cura. La distribución de especies de Candida y la sensibilidad antifúngica varía según el área geográfica, incluso entre centros de salud de una misma región. Objetivo: establecer la distribución de especies de Candida y su sensibilidad in vitro frente a diferentes antifúngicos. Materiales y métodos: se realizó un estudio descriptivo, prospectivo y transversal entre noviembre de 2013 y mayo de 2014 de casos de candidemias en una institución de salud de Valledupar, Colombia. Las Concentraciones Inhibitorias Mínimas (CIM) se determinaron según el protocolo estándar M27-A3-S4. Resultados: Se estudiaron 40 aislados clínicos de Candida spp. obtenidos de sangre (97,5%) y médula ósea (2,5%). Del total, 15 (37,5%) fueron caracterizados como Candida tropicalis, 13 (32,5%) del Complejo Candida albicans, cinco (12,5%) del Complejo Candida glabrata, tres (7,5%) como Candida guilliermondii, tres (7,5%) del Complejo Candida parapsilosis y uno (2,5%) como Candida krusei. No se observó resistencia a la anfotericina B ni al voriconazol en ninguno de los aislados, pero sí al fluconazol en uno (6,6%) de Candida tropicalis y uno (33,3%) del Complejo Candida parapsilosis y a la caspofungina en el aislado de Candida krusei y en uno (20%) del Complejo Candida glabrata. Conclusiones: la epidemiología local de las levaduras causantes de candidemia mostró mayor prevalencia de especies no-albicans, entre las que se encontró resistencia a los antifúngicos evaluados, lo que es relevante para la elección e instauración de un tratamiento eficaz.


2017 ◽  
Vol 9 (2) ◽  
pp. 71
Author(s):  
Nurhasanah Nurhasanah ◽  
Fauzia Andrini ◽  
Yulis Hamidy

Shallot (Allium ascalonicum L.) has been known as traditional medicine. Shallot which has same genus with garlic(Allium sativum L.) contains allicin that is also found in garlic and has been suspected has fungicidal activity toCandida albicans. It is supported by several researches. Therefore, shallot is suspected has antifungal activity too.The aim of this research was to know antifungal activity of shallot’s water extortion againsts Candida albicans invitro. This was a laboratory experimental research which used completely randomized design, with diffusion method.Shallot’s water extortion was devided into three concentrations, there were 50%, 100% and 200%. Ketoconazole 2%was positive control and aquadest was negative control. The result of this research based on analysis of varians(Anova), there was significant difference between several treatments and was confirmed with Duncan New MultipleRange Test (DNMRT) p<0,05, there was significant difference between 100% shallot’s water extortion with othertreatments, but there was no significant difference between 50% shallot’s water extortion with 200% shallot’s. Theconclusion was shallot’s water extortion had antifungal activity againsts Candida albicans with the best concentration100%, but it was lower than ketoconazole 2%.


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