Abstract |
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.
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Authors | Debabrata Chanda, Shashi Bhushan, Santosh K Guru, Karuna Shanker, Z A Wani, B A Rah, Suaib Luqman, Dilip M Mondhe, Anirban Pal, Arvind S Negi |
Journal | European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences
(Eur J Pharm Sci)
Vol. 47
Issue 5
Pg. 988-95
(Dec 18 2012)
ISSN: 1879-0720 [Electronic] Netherlands |
PMID | 23017432
(Publication Type: Journal Article)
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Copyright | Copyright © 2012 Elsevier B.V. All rights reserved. |
Chemical References |
- Antineoplastic Agents
- Cyclin-Dependent Kinase Inhibitor p21
- Indans
- NF-kappa B
- Tubulin Modulators
- indacrinone
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Topics |
- Animals
- Antineoplastic Agents
(pharmacokinetics, therapeutic use, toxicity)
- Breast Neoplasms
(drug therapy, metabolism)
- Carcinoma, Ehrlich Tumor
(drug therapy, pathology)
- Cell Cycle
(drug effects)
- Cell Line, Tumor
- Cyclin-Dependent Kinase Inhibitor p21
(metabolism)
- Female
- Humans
- Indans
(pharmacokinetics, therapeutic use, toxicity)
- Leukocytes
(drug effects)
- Male
- Mice
- NF-kappa B
(metabolism)
- Rabbits
- Tubulin Modulators
(pharmacokinetics, therapeutic use, toxicity)
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