| Literature DB >> 25933717 |
Aastha Singh1, Kaneez Fatima1, Arjun Singh1, Akansha Behl2, M J Mintoo2, Mohammad Hasanain3, Raghib Ashraf3, Suaib Luqman1, Karuna Shanker1, D M Mondhe2, Jayanta Sarkar3, Debabrata Chanda1, Arvind S Negi4.
Abstract
3-(3',4',5'-Trimethoxyphenyl)-4,5,6-trimethoxy,2-(3″,4″-methylenedioxybenzylidene)-indan-1-one (1) is an optimized anti-cancer lead molecule obtained on modification of gallic acid, a plant phenolic acid. It exhibited potent cytotoxicities (IC50=0.010-14.76μM) against various human carcinoma cells. In cell cycle analysis, benzylidene indanone 1 induced G2/M phase arrest in both MCF-7 and MDA-MB-231 cells. It also induced apoptosis in DU145 cells which was evident by cleavage of PARP. In Ehrlich ascites carcinoma, benzylidene indanone 1 showed 45.48% inhibition of tumour growth at 20mg/kg dose in Swiss albino mice. Further, in sub-acute toxicity experiment in Swiss-albino mice, it was found to be non-toxic up to 100mg/kg dose for 28days. The lead compound benzylidene indanone 1 can further be optimized for better anti-cancer activity.Entities:
Keywords: 5-Fluorouracil (PubChem CID: 3385); Anticancer; Benzylidene indanone; Caspase; Cell cycle; Colchicine (PubChem CID: 6167); Combretastatin A4 (PubChem CID: 5351344); Ehrlich ascites carcinoma; Gallic acid (PubChem CID: 370); Piperonal (PubChem CID: 8438); Podophyllotoxin (PubChem CID: 10607); Sub-acute toxicity
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Year: 2015 PMID： 25933717 DOI： 10.1016/j.ejps.2015.04.020
Source DB: PubMed Journal: Eur J Pharm Sci ISSN： 0928-0987 Impact factor: 4.384