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Bioorg Med Chem Lett ; 22(6): 2350-3, 2012 Mar 15.
Artículo en Inglés | MEDLINE | ID: mdl-22365754

RESUMEN

Four new compounds, oliganthins A-D (1-4), and one known caged xanthone gaudichaudione H (5) were isolated from the stems of Garcinia oligantha. The structures of the new compounds were elucidated by spectroscopic evidences. All of the five compounds were evaluated for their apoptosis-inducing effects using HeLa-C3 cells which have been genetically engineered to produce a fluorescent biosensor capable of detecting caspase-3 activation. All of them induced cell apoptosis at 10 µM or lower concentrations. The apoptotic activity of oliganthins A, B and gaudichaudione H were further confirmed by detecting the cleavage of PARP, which is the substrate of activated caspase-3, in these compounds-treated cells using the method of Western blot. Moreover, the values of IC(50) were measured for all five compounds on HeLa cells using the MTT assay. Among them, gaudichaudione H had the lowest IC(50) value of 0.90 µM, while the other four new compounds had IC(50) values of 1.58, 1.52, 4.15, and 7.82 µM, respectively. These results show that gaudichaudione H has the strongest apoptosis-inducing effect and cell growth inhibition effect among these xanthones and it may have the potential to be developed into a new anticancer agent.


Asunto(s)
Antineoplásicos Fitogénicos/química , Apoptosis/efectos de los fármacos , Garcinia/química , Xantenos/química , Xantonas/química , Antineoplásicos Fitogénicos/aislamiento & purificación , Antineoplásicos Fitogénicos/farmacología , Western Blotting , Caspasa 3/genética , Caspasa 3/metabolismo , Femenino , Expresión Génica , Genes Reporteros , Células HeLa , Humanos , Espectroscopía de Resonancia Magnética , Extractos Vegetales/química , Tallos de la Planta/química , Poli(ADP-Ribosa) Polimerasas/genética , Poli(ADP-Ribosa) Polimerasas/metabolismo , Neoplasias del Cuello Uterino/tratamiento farmacológico , Neoplasias del Cuello Uterino/patología , Xantenos/aislamiento & purificación , Xantenos/farmacología , Xantonas/aislamiento & purificación , Xantonas/farmacología
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