RESUMEN
Chemical investigation of the stem bark of Oroxylum indicum resulted in the isolation and characterization of two new flavonoid glycosides (1, 2), along with seven known compounds (3-9). Their structures were established on the basis of extensive spectroscopic (IR, MS, 2D NMR) data analysis and by the comparison with spectroscopic data reported in the literature. In addition, all the compounds were tested for their ulcer protective effects against various gastric ulceritis inducing models in rats.
Asunto(s)
Antiulcerosos/química , Bignoniaceae/química , Flavanonas/química , Flavonas/química , Flavonoides/química , Animales , Antiulcerosos/aislamiento & purificación , Antiulcerosos/farmacología , Modelos Animales de Enfermedad , Flavanonas/aislamiento & purificación , Flavanonas/farmacología , Flavonas/aislamiento & purificación , Flavonas/farmacología , Flavonoides/aislamiento & purificación , Flavonoides/farmacología , Espectroscopía de Resonancia Magnética , Corteza de la Planta/química , Tallos de la Planta/química , RatasRESUMEN
A series of 8-aminomethylated derivatives (1a-1j) were prepared by Mannich reaction of oroxylin A (1) with appropriate primary or secondary amines and para-formaldehyde. All the compounds were tested for their alpha-glucosidase inhibition activity against both yeast and rat intestinal alpha-glucosidase. Some of the compounds demonstrated significantly better alpha-glucosidase inhibitory activity than the parent compound (oroxylin A).
Asunto(s)
Flavonoides/química , Flavonoides/farmacología , Inhibidores de Glicósido Hidrolasas , Animales , Intestinos/enzimología , Ratas , Saccharomyces cerevisiae/enzimología , Relación Estructura-ActividadRESUMEN
Nimbolide (1), a limonoid isolated from Azadirachta indica, is the chief cytotoxic principle in Neem leaves extract. Using nimbolide as a lead compound for anti-cancer analogue design, a series of nimbolide derivatives have been synthesized and evaluated for in vitro cytotoxic activity against a panel of human cancer cell lines. Out of 10 compounds screened 2g, 2h and 2i showed potent activity.
Asunto(s)
Amidas/química , Antineoplásicos/farmacología , Limoninas/química , Azadirachta/metabolismo , Línea Celular Tumoral , Química Farmacéutica/métodos , Diseño de Fármacos , Humanos , Concentración 50 Inhibidora , Modelos Químicos , Extractos Vegetales/metabolismo , Hojas de la Planta , Plantas Medicinales/metabolismoRESUMEN
The natural product, chrysin (5,7-dihydroxy flavone), obtained from Oroxylum indicum, exhibits numerous biological activities including anticancer, anti-inflammatory, and antiallergic activities. Three series of chrysin analogues were prepared, in which chrysin and heterocyclic moieties are separated by 3-carbon, 4-carbon, and 6-carbon spacers. All the derivatives were screened for antibacterial activity against a panel of susceptible and resistant Gram-positive and Gram-negative organisms. It was observed that most of the derivatives displayed significant activity as compared to their parent compound (chrysin).
Asunto(s)
Antiinfecciosos/farmacología , Química Farmacéutica/métodos , Flavonoides/química , Flavonoides/síntesis química , Extractos Vegetales/metabolismo , Antialérgicos/farmacología , Antibacterianos/química , Antibacterianos/farmacología , Antiinflamatorios/farmacología , Antineoplásicos/farmacología , Carbono/química , Diseño de Fármacos , Evaluación Preclínica de Medicamentos , Flavonoides/metabolismo , Pruebas de Sensibilidad Microbiana , Modelos Químicos , Morfolinas/química , Relación Estructura-ActividadRESUMEN
A series of Oroxylin A derivatives, prepared by alkylation and condensation, were fully characterized by spectroscopic methods. All the derivatives were screened for antibacterial activity against a panel of susceptible and resistant Gram-positive and Gram-negative organisms. It was observed that acylation of 7-OH group in Oroxylin A significantly enhanced the activity as compared to their parent compound (Oroxylin A).