title: 13,14-Dihydroxy groups are critical for the anti-cancer effects of garcinol.
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.
authors.affiliation: School of Pharmaceutical Engineering & Life Science, Changzhou University, Jiangsu 213164, PR China.
authors.forename: Chao-Ming
authors.initials: CM
authors.lastname: Han
authors.affiliation: Beijing Institute of Dental Research, Beijing Stomatological Hospital, Capital Medical University, Beijing 100050, PR China.
authors.forename: Xin-Ying
authors.initials: XY
authors.lastname: Zhou
authors.affiliation: School of Pharmaceutical Engineering & Life Science, Changzhou University, Jiangsu 213164, PR China.
authors.forename: Jing
authors.initials: J
authors.lastname: Cao
authors.affiliation: Beijing Institute of Dental Research, Beijing Stomatological Hospital, Capital Medical University, Beijing 100050, PR China. Electronic address: xinyanzhangzh@126.com.
authors.forename: Xin-Yan
authors.initials: XY
authors.lastname: Zhang
authors.affiliation: School of Pharmaceutical Engineering & Life Science, Changzhou University, Jiangsu 213164, PR China. Electronic address: xinchen@cczu.edu.cn.
authors.forename: Xin
authors.initials: X
authors.lastname: Chen
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects*; D002453:Cell Cycle / Q000187:drug effects; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D006801:Humans; D008745:Methylation; D009055:Mouth / Q000166:cytology / Q000187:drug effects / Q000473:pathology; D009062:Mouth Neoplasms / Q000188:drug therapy* / Q000473:pathology; D013729:Terpenes / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D013729:Terpenes; C054597:garcinol
keywords: 13,14-Dimethoxy garcinol; Anti-cancer; Cell apoptosis; Cell proliferation