Recently microwave-induced chemical synthesis of curcumin-metformin adduct to enhance the efficacy of metformin in preventing the formation of Advanced Glycation End Products （AGEs） has been reported from authors＇ ...Recently microwave-induced chemical synthesis of curcumin-metformin adduct to enhance the efficacy of metformin in preventing the formation of Advanced Glycation End Products （AGEs） has been reported from authors＇ laboratory. The present studies describe microwave-induced chemical synthesis and mass spectral characterization of curcumin-phenformin adducts using LC-MS/MS. The mechanism of formation and its analytical data via Thin-Layer Chromatography （TLC） combined with MS/MS fragmentation revealed a major six membered ring adduct and a minor eight membered ring isomer. A facile chemical synthesis and identification of major and minor isomers presented in this study may offer novel therapeutic strategies for inhibiting AGEs as well as anti-cancer treatments.展开更多
Background:In previous studies,we have shown that the combination of metformin and gefitinib inhibits the growth of bladder cancer cells.Here we examined whether the metformin analogue phenformin,either used alone or ...Background:In previous studies,we have shown that the combination of metformin and gefitinib inhibits the growth of bladder cancer cells.Here we examined whether the metformin analogue phenformin,either used alone or in combination with gefitinib,could inhibit growth of bladder cancer cells.Methods:The growth-inhibitory effects of phenformin and gefitinib were tested in one murine and two human bladder cancer cell lines using MTT and clonogenic assays.Effects on cell migration were assessed in a wound healing assay.Synergistic action between the two drugs was assessed using CompuSyn software.The potential involvement of AMPK and EGFR pathways in the effects of phenformin and gefitinib was explored using Western blotting.Results:In MTT and clonogenic assays,phenformin was>10-fold more potent than metformin in inhibiting bladder cancer cell growth.Phenformin also potently inhibited cell migration in wound healing assays,and promoted apop-tosis.AMPK signaling was activated;EGFR signaling was inhibited.Phenformin was synergistic with gefitinib,with the combination of drugs showing much stronger anticancer activity and apoptotic activation than phenformin alone.Conclusions:Phenformin shows potential as an effective drug against bladder cancer,either alone or in combination with gefitinib.展开更多
文摘Recently microwave-induced chemical synthesis of curcumin-metformin adduct to enhance the efficacy of metformin in preventing the formation of Advanced Glycation End Products （AGEs） has been reported from authors＇ laboratory. The present studies describe microwave-induced chemical synthesis and mass spectral characterization of curcumin-phenformin adducts using LC-MS/MS. The mechanism of formation and its analytical data via Thin-Layer Chromatography （TLC） combined with MS/MS fragmentation revealed a major six membered ring adduct and a minor eight membered ring isomer. A facile chemical synthesis and identification of major and minor isomers presented in this study may offer novel therapeutic strategies for inhibiting AGEs as well as anti-cancer treatments.
基金supported by grants to X.Y.from the Hunan Natural Science Foundation(2016JJ2187)the Key Project of Hunan Province 2016(2016JC2036)+1 种基金Start-up Funds of the Key Laboratory of Study and Discovery of Targeted Small Molecules of Hunan Province(2017TP1020)by a grant to M.P.from the Chinese National Science Foundation(81703008).
文摘Background:In previous studies,we have shown that the combination of metformin and gefitinib inhibits the growth of bladder cancer cells.Here we examined whether the metformin analogue phenformin,either used alone or in combination with gefitinib,could inhibit growth of bladder cancer cells.Methods:The growth-inhibitory effects of phenformin and gefitinib were tested in one murine and two human bladder cancer cell lines using MTT and clonogenic assays.Effects on cell migration were assessed in a wound healing assay.Synergistic action between the two drugs was assessed using CompuSyn software.The potential involvement of AMPK and EGFR pathways in the effects of phenformin and gefitinib was explored using Western blotting.Results:In MTT and clonogenic assays,phenformin was>10-fold more potent than metformin in inhibiting bladder cancer cell growth.Phenformin also potently inhibited cell migration in wound healing assays,and promoted apop-tosis.AMPK signaling was activated;EGFR signaling was inhibited.Phenformin was synergistic with gefitinib,with the combination of drugs showing much stronger anticancer activity and apoptotic activation than phenformin alone.Conclusions:Phenformin shows potential as an effective drug against bladder cancer,either alone or in combination with gefitinib.
