13,14-Dihydroxy groups are critical for the anti-cancer effects of garcinol |
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| Institution: | 1. School of Pharmaceutical Engineering & Life Science, Changzhou University, Jiangsu 213164, PR China;2. Beijing Institute of Dental Research, Beijing Stomatological Hospital, Capital Medical University, Beijing 100050, PR China;1. Department of Psychiatry, Division of Molecular Psychiatry, New Haven, CT 06520, USA;2. Department of Psychology, Yale University, New Haven, CT 06520, USA;3. Interdepartmental Neuroscience Program, Yale University, New Haven, CT 06520, USA;1. Cellular and Molecular Neurobiology Laboratory, Department of Life Science and Bioinformatics, Assam University, Silchar 788011, Assam, India;2. Department of Zoology, Pandit Deendayal Upadhyaya Adarsha Mahavidyalaya (PDUAM), Eraligool 788723, Karimganj, Assam, India;3. Pandit Deendayal Upadhyaya Adarsha Mahavidyalaya (PDUAM), Eraligool-788723, Karimganj, Assam, India;4. Department of Pharmacology and Toxicology, National Institute of Pharmaceutical Education and Research (NIPER)-Ahmedabad, Gandhinagar 382355, Gujarat, India;1. Department of Biochemistry and Molecular Biology, Beijing Normal University, Gene Engineering and Biotechnology, Beijing Key Laboratory, Beijing 100875, PR China;2. Key Laboratory of Protection and Development Utilization of Tropical Crop Germplasm Resources, Ministry of Education, College of Landscape and Horticulture, Hainan University, Haikou 570228, China |
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| Abstract: | In the presence of K2CO3/Cs2CO3 (molar ratio 10:1), garcinol was subjected to methylation by reaction with iodomethane at room temperature to afford 13,14-dimethoxy garcinol. The methylated garcinol derivative was screened against oral cancer cell line SCC15 for cell proliferation and apoptosis. 13,14-Dimethoxy garcinol showed weaker inhibitory activity on SCC15 cell growth than garcinol, and had little effect on cell cycle and apoptosis of SCC15, whereas garcinol effectively induced cell cycle arrest and cell apoptosis. Meanwhile, the ELISA data showed that the inhibitory effect of garcinol on 5-Lox pathway was more potent than 13,14-dimethoxy garcinol (P < 0.05). All these results have confirmed the important role of 13,14-dihydroxy groups for anti-cancer effects of garcinol. |
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| Keywords: | 13 14-Dimethoxy garcinol Anti-cancer Cell apoptosis Cell proliferation |
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