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 |
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Authors: | Dhanya Sunil Arun M Isloor Prakash Shetty K Satyamoorthy AS Bharath Prasad |
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Institution: | 1. Department of Chemistry, Manipal Institute of Technology, Manipal University, Manipal 576 104, India;2. Department of Chemistry, National Institute of Technology-Karnataka, Surathkal, Mangalore 575 025, India;3. Department of Printing and Media Engineering, Manipal Institute of Technology, Manipal University, Manipal 576 104, India;4. Department of Biotechnology, Manipal Life Sciences Centre, Manipal University, Manipal 576 104, India |
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Abstract: | In this paper we have investigated the in vitro antioxidant property of two triazolo-thiadiazoles, 6-3-(4-fluorophenyl)-1H-pyrazol-4-yl]-3-(2-naphthyloxy)methyl]1,2,4]triazolo3,4-b]1,3,4]thiadiazole (FPNT) and 6-3-(4-chlororophenyl)-1H-pyrazol-4-yl]-3-(phenyloxy)methyl]1,2,4]triazolo3,4-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. |
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Keywords: | FPNT CPPT HepG2 cell lines Cytotoxicity Apoptosis Antioxidant |
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