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1.
Curr Drug Metab ; 21(7): 525-533, 2020.
Artículo en Inglés | MEDLINE | ID: mdl-32651962

RESUMEN

BACKGROUND: Oxidative stress is among the main causes of metabolic disorders. Hence, there is a need to discover potent antioxidants for therapeutic applications. OBJECTIVE: The objective of this study has been to investigate the phytoconstituents of the methanolic extract of the hard shell of Aegle marmelos fruit and their antioxidant potential. METHODS: Methanolic extract was fractionated using different solvents by liquid-liquid extraction. Characterization of the phytoconstituents was done by using phytochemical tests and GC-MS analysis. The free radical scavenging activity, total reducing power, lipid peroxidation inhibition and cell protection assays against oxidative stress were performed with methanolic extract and its fractions. RESULTS: Therapeutically significant class of compounds, for example, polyphenols, glycosides and sterols were revealed in the hard-shell extract. Differential separation of compounds was achieved by liquid-liquid extraction using different solvents. Six compounds: 4-Hydroxybenzeneacetic acid; 5-Oxo-pyrrolidine-2-carboxylic acid methyl ester; 1-[3-Methyl-3-Butenyl] Pyrrolidine; Trans-sinapyl alcohol; 5-[Hydroxymethyl]-2-furaldehyde and 2,4- Dihydroxy-2,5-dimethyl-3[2H]-furan-3-one, identified in the fruit-shell extract, are being reported for the first time from this plant. Strong antioxidant potential of the extract was evident from efficient scavenging of free radicals. The extract also conferred protection to yeast cells against oxidative damage. CONCLUSION: Results showed that the hard shell of the Aegle marmelos fruit was a potent source for antioxidant compounds, which can be developed for therapeutic applications in the control and management of metabolic diseases.


Asunto(s)
Aegle , Antioxidantes , Antioxidantes/análisis , Antioxidantes/química , Antioxidantes/farmacología , Radicales Libres/química , Frutas/química , Estrés Oxidativo/efectos de los fármacos , Fitoquímicos/análisis , Fitoquímicos/química , Fitoquímicos/farmacología , Extractos Vegetales/análisis , Extractos Vegetales/química , Extractos Vegetales/farmacología , Saccharomycetales/efectos de los fármacos
2.
Curr Top Med Chem ; 19(28): 2567-2578, 2019.
Artículo en Inglés | MEDLINE | ID: mdl-31654510

RESUMEN

BACKGROUND: Biofilm is a critical virulence factor associated with the strains of Candida spp. pathogens as it confers significant resistance to the pathogen against antifungal drugs. METHODS: A systematic review of the literature was undertaken by focusing on natural products, which have been reported to inhibit biofilms produced by Candida spp. The databases explored were from PubMed and Google Scholar. The abstracts and full text of the manuscripts from the literature were analyzed and included if found significant. RESULTS: Medicinal plants from the order Lamiales, Apiales, Asterales, Myrtales, Sapindales, Acorales, Poales and Laurales were reported to inhibit the biofilms formed by Candida spp. From the microbiological sources, lactobacilli, Streptomyces chrestomyceticus and Streptococcus thermophilus B had shown the strong biofilm inhibition potential. Further, the diverse nature of the compounds from classes like terpenoids, phenylpropanoid, alkaloids, flavonoids, polyphenol, naphthoquinone and saponin was found to be significant in inhibiting the biofilm of Candida spp. CONCLUSION: Natural products from both plant and microbial origins have proven themselves as a goldmine for isolating the potential biofilm inhibitors with a specific or multi-locus mechanism of action. Structural and functional characterization of the bioactive molecules from active extracts should be the next line of approach along with the thorough exploration of the mechanism of action for the already identified bioactive molecules.


Asunto(s)
Antifúngicos/farmacología , Biopelículas/efectos de los fármacos , Productos Biológicos/farmacología , Candida/efectos de los fármacos , Candida/patogenicidad , Antifúngicos/química , Antifúngicos/metabolismo , Productos Biológicos/química , Productos Biológicos/metabolismo , Candida/clasificación , Humanos , Pruebas de Sensibilidad Microbiana , Plantas Medicinales , Especificidad de la Especie
3.
Curr Top Med Chem ; 18(27): 2367-2378, 2018.
Artículo en Inglés | MEDLINE | ID: mdl-30582479

RESUMEN

BACKGROUND: Inflammation and oxidative stress are very closely related to pathophysiological processes and linked to multiple chronic diseases. Traditionally, the coconut fruits were used in Guatemala for treatment of dermatitis and inflammation. Isolation of the anti-inflammatory agent from the hard shell of the coconut fruit was targeted in the current study. METHODS: Fractionation of ethanolic extract of the coconut hard shell was done by using column chromatography, solvent treatments and TLC that led to the isolation of a molecule. RESULTS AND DISCUSSION: Spectral characterization of the molecule by LC-MS/MS QTOF, FTIR, 1HNMR, 13C-NMR, HMQC and HMBC indicated that it is a novel keto fatty acid, which is named as nuciferoic acid. Hyaluronidase inhibitory potential of the nuciferoic acid was found to be moderate. It was further docked in all the ten cavities of hyaluronidase and was compared with the substrate hyaluronic acid. Cavity 1 and cavity 4 could be the probable sites of action on hyaluronidase for nuciferoic acid. ADME and toxicological characterization suggested that the key sites of metabolism on nuciferoic acid are C1, C2, C14 and C17. Toxicity prediction against 55 toxicological endpoints revealed that nuciferoic acid does not have any indication of existing toxicological features. CONCLUSION: A novel keto fatty acid, nuciferoic acid, from C. nucifera hard shell has been isolated and characterized. It was found to inhibit hyaluronidase activity, which indicated its potential application as an anti-inflammatory drug or as an adjuvant.


Asunto(s)
Cocos/química , Ácidos Grasos/farmacología , Inhibidores de Glicósido Hidrolasas/farmacología , Hialuronoglucosaminidasa/antagonistas & inhibidores , Cetoácidos/farmacología , Relación Dosis-Respuesta a Droga , Ácidos Grasos/química , Ácidos Grasos/aislamiento & purificación , Inhibidores de Glicósido Hidrolasas/química , Inhibidores de Glicósido Hidrolasas/aislamiento & purificación , Humanos , Hialuronoglucosaminidasa/metabolismo , Cetoácidos/química , Cetoácidos/aislamiento & purificación , Estructura Molecular , Relación Estructura-Actividad
4.
Brain Connect ; 8(1): 49-55, 2018 02.
Artículo en Inglés | MEDLINE | ID: mdl-29065696

RESUMEN

Meditation has a versatile nature to affect cognitive functioning of human brain. Recent researches demonstrated its effects on white matter (WM) properties of human brain. In this research, we aim to investigate WM microstructure of corpus callosum (CC) in long-term meditators (LTMs) of rajayoga meditation using diffusion tensor imaging. For this cross-sectional analysis, 22 LTMs and 17 control participants of age ranging from 30 to 50 years were recruited. Results show high fractional anisotropy values with low mean diffusivity in whole as well as different segments of CC in the LTM group. Also the experience of meditation was correlated with WM properties of CC tracts. Findings may suggest rajayoga meditation to bring potential changes in microstructure of CC segments. Further studies are suggested in clinical population to check its validity and efficacy against disorders involving agenesis of WM.


Asunto(s)
Cuerpo Calloso/diagnóstico por imagen , Meditación , Sustancia Blanca/diagnóstico por imagen , Adulto , Imagen de Difusión Tensora , Femenino , Humanos , Imagen por Resonancia Magnética , Masculino , Persona de Mediana Edad
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