Natural product inspired allicin analogs as novel anti-cancer agents |
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| Institution: | 1. Department of Gastroenterology, Second Affiliated Hospital of Xi''an Jiaotong University, The Key Laboratory of Gastrointestinal Motility Disorders of Shaanxi Province, Xi''an, Shaanxi Province 710004, China;2. Department of Biological Science and Engineering, The Key Laboratory of Biomedical Information Engineering of Ministry of Education, School of Life Science and Technology, Xi''an Jiaotong University, Xi''an, Shaanxi Province 710049, China |
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| Abstract: | A series of novel analogs of Allicin (S-allyl prop-2-ene-1-sulfinothioate) present in garlic has been synthesized in high yield. Synthesized 23 compounds were evaluated against different breast cancer cells (MDA-MB-468 and MCF-7) and non-cancer cells (WI38). Four compounds (3f, 3h, 3m and 3u) showed significant cytotoxicity against cancer cells whereas nontoxic to the normal cells. Based on the LD50 values and selectivity index (SI), compound 3h (S-p-methoxybenzyl (p-methoxyphenyl)methanesulfinothioate) was considered as most promising anticancer agent amongst the above three compounds. Further bio-chemical studies confirmed that compound 3h promotes ROS generation, changes in mitochondrial permeability transition and induced caspase mediated DNA damage and apoptosis. |
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| Keywords: | Sulfenyl sulfoxide Allicin garlic Anti-cancer ROS Caspase 3 Apoptosis |
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