Background: Curcuminoids are promising cancer chemopreventive agents. Curcumin, demethoxycurcumin(DMC) and bisdemethoxycurcumin(BDMC) are the major bioactive curcuminoids in turmeric. However, comprehensive metabolic ...Background: Curcuminoids are promising cancer chemopreventive agents. Curcumin, demethoxycurcumin(DMC) and bisdemethoxycurcumin(BDMC) are the major bioactive curcuminoids in turmeric. However, comprehensive metabolic studies of these three curcuminoids are still limited.Objective: To identify the metabolites of curcumin, DMC and BDMC in rats after oral administration of solid lipid nanoparticles(SLNs).Methods: Male Sprague-Dawley rats(250 ± 20 g, body weight) were randomly divided into 4 groups(n=3), and were orally administered with curcumin-SLN, DMC-SLN, BDMC-SLN, or blank-SLN, respectively. Plasma samples(500 μL) via the angular vein were collected at 1, 2 and 4 h post dosing, and the urine and feces samples were collected at 0–12 h and 12–24 h post-intake. An HPLC-DAD-ESI-MSnmethod was developed to identify the metabolites. The structures of phase II metabolites were further confirmed by enzyme hydrolysis.Results: A total of 34 metabolites were identified in rats plasma, urine, and feces. Most of them were phase II metabolites, including glucuronide conjugates and sulfate conjugates. Among them, the glucuronide conjugates were the major metabolites in rats plasma. In the meanwhile, the three parent curcuminoids were detected in high amounts in the urine and feces samples.Conclusion: The possible metabolic pathways of curcuminoids in rats were proposed.展开更多
基金supported by the National Natural Science Foundation of China(Grant No.81222054 and 81302742)State Administration of Traditional Chinese Medicine(No.201307002)the Key Research Project of Department of Education of Sichuan(11ZA005)
文摘Background: Curcuminoids are promising cancer chemopreventive agents. Curcumin, demethoxycurcumin(DMC) and bisdemethoxycurcumin(BDMC) are the major bioactive curcuminoids in turmeric. However, comprehensive metabolic studies of these three curcuminoids are still limited.Objective: To identify the metabolites of curcumin, DMC and BDMC in rats after oral administration of solid lipid nanoparticles(SLNs).Methods: Male Sprague-Dawley rats(250 ± 20 g, body weight) were randomly divided into 4 groups(n=3), and were orally administered with curcumin-SLN, DMC-SLN, BDMC-SLN, or blank-SLN, respectively. Plasma samples(500 μL) via the angular vein were collected at 1, 2 and 4 h post dosing, and the urine and feces samples were collected at 0–12 h and 12–24 h post-intake. An HPLC-DAD-ESI-MSnmethod was developed to identify the metabolites. The structures of phase II metabolites were further confirmed by enzyme hydrolysis.Results: A total of 34 metabolites were identified in rats plasma, urine, and feces. Most of them were phase II metabolites, including glucuronide conjugates and sulfate conjugates. Among them, the glucuronide conjugates were the major metabolites in rats plasma. In the meanwhile, the three parent curcuminoids were detected in high amounts in the urine and feces samples.Conclusion: The possible metabolic pathways of curcuminoids in rats were proposed.
