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Eur J Pharm Sci ; 47(5): 988-95, 2012 Dec 18.
Artículo en Inglés | MEDLINE | ID: mdl-23017432

RESUMEN

The present study describes anticancer effect of gallic acid based indanone derivative (1). Indanone 1 exhibited in vivo anticancer activity against Erhlich ascites carcinoma in Swiss albino mice by inhibiting tumor growth by 54.3% at 50 mg/kg b.wt. It showed antitubulin effect by inhibiting tubulin polymerase enzyme. In cell cycle analysis, it inhibited G2/M phase and induced apoptosis. It significantly suppressed VEGF-R1, VEGF-R2 and HIF-α in human breast cancer MCF-7 cells, thus exhibiting antiangiogenic activity. In acute oral toxicity, indanone 1 was well tolerated and was found to be non-toxic up to 1000 mg/kg b.wt. in Swiss albino mice. Pharmacokinetic studies in rabbits revealed rate of absorption, half life, volume of distribution with high plasma and blood clearance after i.v. administration. Indanone 1, is a safe and moderately active anticancer agent.


Asunto(s)
Antineoplásicos/uso terapéutico , Neoplasias de la Mama/tratamiento farmacológico , Carcinoma de Ehrlich/tratamiento farmacológico , Indanos/uso terapéutico , Moduladores de Tubulina/uso terapéutico , Animales , Antineoplásicos/farmacocinética , Antineoplásicos/toxicidad , Neoplasias de la Mama/metabolismo , Carcinoma de Ehrlich/patología , Ciclo Celular/efectos de los fármacos , Línea Celular Tumoral , Inhibidor p21 de las Quinasas Dependientes de la Ciclina/metabolismo , Femenino , Humanos , Indanos/farmacocinética , Indanos/toxicidad , Leucocitos/efectos de los fármacos , Masculino , Ratones , FN-kappa B/metabolismo , Conejos , Moduladores de Tubulina/farmacocinética , Moduladores de Tubulina/toxicidad
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