RESUMEN
The cytotoxicity-guided study of the dichloromethane and ethanol extracts of Thymus mastichina L. using the HCT colon cancer cell line allowed the identification of nine compounds, sakuranetin (1), sterubin (2), oleanolic acid (3), ursolic acid (4), lutein (5), beta-sitosterol (6), rosmarinic acid (7), 6-hydroxyluteolin-7-O-beta-glucopyranoside (8), and 6-hydroxyapigenin-7-O-beta-glucopyranoside (9). All compounds were tested for their cytotoxicity against the HCT colon cancer cell line. Compound 4 showed cytotoxicity with GI50 value of 6.8 microg/mL. A fraction composed of a mixture (1:1) of triterpenoid acids 3 and 4 displayed improved cytotoxicity with a GI50 of 2.8 microg/mL suggesting a synergistic behavior. This is the first report on the chemical constituents of Thymus mastichina L. based on structural assignments by spectroscopic analysis. The presence of these constituents identified by colon cancer cytotoxicity-guided activity indicates that extracts of T. mastichina L. may have a protective effect against colon cancers.
Asunto(s)
Antineoplásicos Fitogénicos/aislamiento & purificación , Carcinoma/tratamiento farmacológico , Neoplasias Colorrectales/tratamiento farmacológico , Extractos Vegetales/uso terapéutico , Thymus (Planta)/química , Antineoplásicos Fitogénicos/química , Ensayos de Selección de Medicamentos Antitumorales , Flavanonas/aislamiento & purificación , Células HCT116 , Humanos , Fitoterapia , Triterpenos/aislamiento & purificaciónRESUMEN
A variety of 2-hydroxy aldehydes on reaction with 3-butenoic acid afford in a one-pot reaction the corresponding 3-vinylcoumarins. As expected, extension of the delocalized π-electron system accomplished by Heck coupling reactions with aryl halides results in an increased fluorescence of the compounds whose applicability is yet to be established.
Asunto(s)
Cumarinas/síntesis química , Colorantes Fluorescentes/síntesis química , Estirenos/química , Compuestos de Vinilo/síntesis química , Estructura MolecularRESUMEN
Aziridination and unpredicted homologation reaction of N-sulfonylimines were achieved easily with a very simple, rapid and mild procedure through the use of diazomethane without the presence of any catalyst. The method represents an attractive alternative to metal-catalyzed processes.