Examinando por Materia "Eugenol"
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- PublicaciónAcceso abiertoEvaluación in vitro de la actividad antifúngica y citotóxica del eugenol y sus derivados semisintéticos frente a Trichophyton spp(Bucaramanga : Universidad de Santander, 2018, 2018-06-26) Rivera Rincón, Yohana; Leal Pinto, Sandra-MilenaDermatophytes are keratinophilic fungi that infect tissues such as skin, hair and nails in humans and animals. The treatment is based on topical, systemic and / or combined therapies with low penetrability, varied effectiveness and adverse effects that make it a challenge to research new natural bioactive molecules. The general objective was to evaluate the antifungal and cytotoxic activity in vitro of the semisynthetic compounds derived from eugenol in fungi of the genus Trichophyton. The antifungal susceptibility of twelve eugenol derivatives was evaluated against: Trichophyton mentagrophytes, Trichophyton rubrum and Trichophyton tonsurans. The MIC was determined by the microdilution method established by CLSI, subcultures from MIC, were incubated for 7 days at 30 ° C to determine MFC. In addition, the inhibition of the radial growth of the mycelium was evaluated by the substrate technique impregnated for 20 days. Likewise, in vitro toxicity in Vero cells was tested by a colorimetric assay, using the MTT tetrazolium salt. Terbinafine used as reference drug. EO, eugenol and derivatives 5,10,11 and 12 showed inhibition of T. mentagrophytes MIC 62.5-500 μg / mL and MFC 125-500 μg/mL Eugenol, derivatives 3,5 and 11 inhibited T. rubrum MIC and MFC 125-250 μg/mL EO, eugenol, compound 11 and 12 inhibited T. tonsurans with MIC and MFC 125-250 μg/mL 100% inhibition of mycelial growth of the three dermatophytes was observed after exposure with 300ug/mL and 100 ug/mL of derivatives 3,5,7-12 and 3, 7-9,12, respectively. Low toxicity in Vero cells was observed (CC50 54.06- <300 ug/mL). New bioactive molecules with antifungal effect and low in vitro toxicity are presented, which represents an advance in the pre-clinical process of development and research of new antifungal agents.
- PublicaciónAcceso abiertoIn vitro susceptibility of Microsporum spp and mammalian cells to Eugenia caryophyllus essential oil, eugenol and semisynthetic derivatives.(Mycoses, 2019-01) Leal Pinto, Sandra-Milena; Herrera Sandoval, Laura-Viviana; Vargas Méndez, Leonor-Yamile; CLINIUDESBackground Microsporum spp. are keratinophilic dermatophytes that mainly invade the stratum corneum of the skin and hair causing clinical symptoms associated with tinea. Its treatment has several limitations, and the search for new active molecules is necessary. Objective To evaluate the antifungal and cytotoxic potential of Eugenia caryophyllus essential oil (EO), eugenol, isoeugenol and methylisoeugenol against Microsporum canis, M. gypseum and Vero cells. Methods The EO was extracted by conventional heating-assisted hydrodistillation, the eugenol obtained commercially and the derivatives through Williamson synthesis. Minimal inhibitory concentration (MICs), minimum fungicidal concentration, inhibition of radial mycelial growth and germination inhibition were used to evaluate the antifungal activity. In addition, a colorimetric test was conducted to evaluate cytotoxic activity. Results MIC and MFC values for all compounds were 62.5-500 μg/mL for both of the species of Microsporum evaluated. Also, concentrations of 300 μg/mL of the compounds inhibited 100% of M. canis mycelium. The inhibition of germination was observed after 6 hours of treatment (11.86 ± 3.46-85.31 ± 0%). No cytotoxicity was observed in Vero cells (CC50 > 105 μg/mL), whereas terbinafine showed CC50 31.00 ± 0.61 μg/mL. Conclusions Our study indicates an interesting bioactivity of isoeugenol and methylisoeugenol against M. canis, M. gypseum and mammalian cells.
- PublicaciónAcceso abiertoIn vitro susceptibility of Microsporum spp. and mammalian cells to Eugenia caryophyllus essential oil, eugenol and semisynthetic derivatives(2019) Leal Pinto, Sandra Milena; Herrera Sandoval, Laura Viviana; Vargas Méndez, Leonor-YamileBackground: Microsporum spp. are keratinophilic dermatophytes that mainly invade the stratum corneum of the skin and hair causing clinical symptoms associated with tinea. Its treatment has several limitations, and the search for new active molecules is necessary.Objective: To evaluate the antifungal and cytotoxic potential of Eugenia caryophyllusessential oil (EO), eugenol, isoeugenol and methylisoeugenol against Microsporum canis, M. gypseum and Vero cells.Methods: The EO was extracted by conventional heating-assisted hydrodistillation, the eugenol obtained commercially and the derivatives through Williamson synthe-sis. Minimal inhibitory concentration (MICs), minimum fungicidal concentration, inhi-bition of radial mycelial growth and germination inhibition were used to evaluate the antifungal activity. In addition, a colorimetric test was conducted to evaluate cyto-toxic activity.Results: MIC and MFC values for all compounds were 62.5-500 μg/mL for both of the species of Microsporum evaluated. Also, concentrations of 300 μg/mL of the compounds inhibited 100% of M. canis mycelium. The inhibition of germination was observed after 6 hours of treatment (11.86 ± 3.46-85.31 ± 0%). No cytotoxicity was observed in Vero cells (CC50 > 105 μg/mL), whereas terbinafine showed CC5031.00 ± 0.61 μg/mL.Conclusions: Our study indicates an interesting bioactivity of isoeugenol and meth-ylisoeugenol against M. canis, M. gypseum and mammalian cells.
- PublicaciónAcceso abiertoSemisynthetic eugenol derivatives as antifungal agents against dermatophytes of the genus Trichophyton(Microbiology Society, 2019-07-01) Leal Pinto, Sandra-Milena; Rivera Rincón, Yohana; Herrera Sandoval, Laura-Viviana; Lizarazo, Juan-Camilo; Rincón, John-Jairo; Vargas Méndez, Leonor-Yamile; CLINIUDESPurpose. Eugenol, the main component of clove bud essential oil (Eugenia caryophyllus), has been linked to antimicrobial, anti-inflammatory, insecticidal and immunomodulatory properties. The purpose of this study was to evaluate the antifungal and cytotoxic activity of eugenol, the essential oil of Eugenia caryophyllus, and some semisynthetic derivatives of eugenol against dermatophytes of the genus Trichophyton. Methodology. We evaluated the antifungal effect of the compounds, determining the minimum inhibitory concentrations (MICs) by the microdilution method and the minimum fungicidal concentrations by cultures from the inhibitions. Additionally, the inhibition of the radial growth of the mycelium of the dermatophyte fungi was tested by poisoned substrate. Cytotoxicity was measured by the colorimetric method on Vero cells. Results. All of the eugenol compounds tested exhibited antifungal properties, showing MICs of 62.5–500 µg ml−1 , determined within three dermatophyte species: Trichophyton rubrum, Trichophyton mentagrophytes and Trichophyton tonsurans. Among these derivatives, methyl isoeugenol, at concentrations of 300 and 100 µg ml−1, was found to completely inhibit (100 %) radial growth of the mycelium of all three species after 20 days of treatment. Additionally, phenotypic variations related to the decrease in pigment production of T. rubrum were observed after treatment with O-ethyl and O-butyl isoeugenol derivatives. Meanwhile, all of the tested (iso)eugenol molecules exhibited moderate toxicity in Vero cells [50 % cytotoxic concentration (the concentration required for a 50 % reduction in cell viability; CC50): 54.06–265.18 µg ml−1 ). Conclusion. The results suggest that the semisynthetic eugenol derivatives (SEDs) show promising antifungal activity and selectivity against dermatophyte fungi.