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      https://www.ias.ac.in/article/fulltext/jcsc/131/10/0107

    • Keywords

       

      Antioxidant; anticancer; sulfur-containing BHT; HT29; MCF7

    • Abstract

       

      In the present study, a series of multipotent antioxidants (MPAOs), namely sulfur-containing BHT (S-BHT), derivatives were rationally designed and synthesized, and their inhibitory activities against free radicals and human cancer cell lines, HT29 (colon cancer) and MCF7 (breast cancer) were further evaluated. The experimental results showed that the Six out-of-eight S-BHT compounds had excellent antioxidant activity against DPPH radical with major enhancement compared to BHT. Among them, compounds 2b, 2a and 3b attained over 45% lower IC50 values than BHT. In vitro cytotoxicity, MTT assay was carried out using two human cancer cell lines, HT29 (colon cancer) and MCF7 (breast cancer) in addition to their non-tumorigenic counterparts to explore selectivity. In line with antioxidant activity, compounds 2a and 2b displayed the highest cytotoxicity effect on both cancer types. Interestingly, 2b not only exhibited superior cancer inhibition but also scored high selectivity index (SI = 5.2, 12.5) in colon and breast tissues, respectively, exceeding that of the standard chemotherapeutic drugs used 5-Fluorouracil (5-FU) and Tamoxifen (Tmx), with lower IC50 values. The results indicated that the symmetric S-BHT derivatives were significantlyenhanced by the antioxidant potency and their ability as useful and promising selective anticancer agents.

    • Author Affiliations

       

      MOHD H AHMAD1 NOORSAADAH ABD RAHMAN2 FARKAAD A KADIR3 LINA A AL-ANI1 NAJIHAH M HASHIM4 WAGEEH A YEHYE1

      1. Nanotechnology and Catalysis Research Centre (NANOCAT), Block 3A, Institute of Graduate Studies Building, University of Malaya, 50603 Kuala Lumpur, Malaysia
      2. Department of Chemistry, Faculty of Science, University of Malaya, 50603 Kuala Lumpur, Malaysia
      3. Department of Anatomy and Medical Imaging, Faculty of Medical and Health Sciences, School of Medical Sciences, University of Auckland, 1142 Auckland, New Zealand
      4. Department of Pharmacy, Faculty of Medicine, University of Malaya, 50603 Kuala Lumpur, Malaysia
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