6-[3-(4-Fluorophenyl)-1H-pyrazol-4-yl]-3- [(2-naphthyloxy)methyl][1,2,4]triazolo[3,4-b][1,3,4]- thiadiazole as a potent antioxidant and an anticancer agent induces growth inhibition followed by apoptosis in HepG2 cells

Sunil, Dhanya and Isloor, Arun M and Shetty, Prakash and Satyamoorthy, K and Prasad, Bharath AS (2010) 6-[3-(4-Fluorophenyl)-1H-pyrazol-4-yl]-3- [(2-naphthyloxy)methyl][1,2,4]triazolo[3,4-b][1,3,4]- thiadiazole as a potent antioxidant and an anticancer agent induces growth inhibition followed by apoptosis in HepG2 cells. Arabian Journal of Chemistry, 3. pp. 211-217. ISSN 1878-5352

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Abstract

In this paper we have investigated the in vitro antioxidant property of two triazolothiadiazoles, 6-[3-(4-fluorophenyl)-1H-pyrazol-4-yl]-3-[(2-naphthyloxy)methyl][1,2,4]triazolo[3,4-b]- [1,3,4]thiadiazole (FPNT) and 6-[3-(4-chlororophenyl)-1H-pyrazol-4-yl]-3-[(phenyloxy)methyl]- [1,2,4]triazolo[3,4-b][1,3,4]thiadiazole (CPPT) by spectrophotometric DPPH and ABTS radical scavenging methods as well as by lipid peroxide assay. The anticancer activity along with possible mechanism of action of triazolo-thiadiazoles in Hep G2 cells was explored using MTT assay, [3H] thymidine assay, flow cytometry and chromatin condensation studies. Both FPNT and CPPT exhibited a dose dependent cytotoxic effect on hepatocellular carcinoma cell line, HepG2. The IC50 value was very low for both the compounds when compared to standard drug, doxorubicin. Incorporation of [3H] thymidine in conjunction with cell cycle analysis suggested that FPNT inhibited the growth of HepG2 cells. Flow cytometric studies revealed more percentage of cells in sub-G1 phase, indicating apoptosis, which was further confirmed through chromatin condensation studies by Hoechst staining. FPNT was found to be a potent antioxidant when compared to the standard in DPPH, ABTS radical scavenging assays and lipid peroxidation studies.

Item Type: Article
Uncontrolled Keywords: CPPT; HepG2 cell lines; Cytotoxicity; Apoptosis; Antioxidant
Subjects: Life Sciences > MLSC Manipal
Depositing User: Admin MIT
Date Deposited: 16 Feb 2012 09:46
Last Modified: 25 Oct 2013 07:03
URI: http://eprints.manipal.edu/id/eprint/2975

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