title: The role of turmerones on curcumin transportation and P-glycoprotein activities in intestinal Caco-2 cells.
abstract: The rhizome of Curcuma longa (turmeric) is often used in Asia as a spice and as a medicine. Its most well-studied component, curcumin, has been shown to exhibit poor bioavailability in animal studies and clinical trials. We hypothesized that the presence of lipophilic components (e.g., turmerones) in turmeric extract would affect the absorption of curcumin. The effects of turmerones on curcumin transport were evaluated in human intestinal epithelial Caco-2 cells. The roles of turmerones on P-glycoprotein (P-gp) activities and mRNA expression were also evaluated. Results showed that in the presence of α- and aromatic turmerones, the amount of curcumin transported into the Caco-2 cells in 2 hours was significantly increased. α-Turmerone and verapamil (a P-gp inhibitor) significantly inhibited the efflux of rhodamine-123 and digoxin (i.e., inhibited the activity of P-gp). It is interesting that aromatic turmerone significantly increased the rhodamine-123 efflux and P-gp (MDR1 gene) mRNA expression levels. The effects of α- and aromatic turmerones on curcumin transport as well as P-gp activities were shown here for the first time. The presence of turmerones did affect the absorption of curcumin in vitro. These findings suggest the potential use of turmeric extract (including curcumin and turmerones), rather than curcumin alone, for treating diseases.
authors.affiliation: Institute of Chinese Medicine, The Chinese University of Hong Kong, Shatin, Hong Kong, China.
authors.forename: Grace G L
authors.initials: GG
authors.lastname: Yue
authors.forename: Sau-Wan
authors.initials: SW
authors.lastname: Cheng
authors.forename: Hua
authors.initials: H
authors.lastname: Yu
authors.forename: Zi-Sheng
authors.initials: ZS
authors.lastname: Xu
authors.forename: Julia K M
authors.initials: JK
authors.lastname: Lee
authors.forename: Po-Ming
authors.initials: PM
authors.lastname: Hon
authors.forename: Mavis Y H
authors.initials: MY
authors.lastname: Lee
authors.forename: Edward J
authors.initials: EJ
authors.lastname: Kennelly
authors.forename: Gary
authors.initials: G
authors.lastname: Deng
authors.forename: Simon K
authors.initials: SK
authors.lastname: Yeung
authors.forename: Barrie R
authors.initials: BR
authors.lastname: Cassileth
authors.forename: Kwok-Pui
authors.initials: KP
authors.lastname: Fung
authors.forename: Ping-Chung
authors.initials: PC
authors.lastname: Leung
authors.forename: Clara B S
authors.initials: CB
authors.lastname: Lau
mesh_terms: D018435:ATP Binding Cassette Transporter, Subfamily B; D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000819:agonists / Q000037:antagonists & inhibitors / Q000235:genetics / Q000378:metabolism*; D000070997:ATP Binding Cassette Transporter, Subfamily G, Member 2; D018528:ATP-Binding Cassette Transporters / Q000819:agonists / Q000235:genetics / Q000378:metabolism; D000230:Adenocarcinoma / Q000188:drug therapy / Q000378:metabolism; D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry / Q000302:isolation & purification / Q000378:metabolism / Q000494:pharmacology*; D018938:Caco-2 Cells; D002470:Cell Survival / Q000187:drug effects; D003110:Colonic Neoplasms / Q000188:drug therapy / Q000378:metabolism; D030024:Curcuma / Q000737:chemistry; D003474:Curcumin / Q000032:analysis / Q000737:chemistry / Q000378:metabolism*; D020895:Enterocytes / Q000187:drug effects* / Q000378:metabolism; D005765:Gastrointestinal Agents / Q000302:isolation & purification / Q000494:pharmacology*; D005786:Gene Expression Regulation / Q000187:drug effects; D006801:Humans; D007408:Intestinal Absorption / Q000187:drug effects*; D007659:Ketones / Q000302:isolation & purification / Q000494:pharmacology; D000089762:Multidrug Resistance-Associated Protein 2; D027425:ATP-Binding Cassette, Sub-Family C Proteins / Q000819:agonists / Q000235:genetics / Q000378:metabolism; D009363:Neoplasm Proteins / Q000819:agonists / Q000037:antagonists & inhibitors / Q000235:genetics / Q000378:metabolism; D008517:Phytotherapy; D010936:Plant Extracts / Q000737:chemistry; D012333:RNA, Messenger / Q000378:metabolism; D012717:Sesquiterpenes / Q000302:isolation & purification / Q000494:pharmacology*; D012995:Solubility
chemical_list: D018435:ATP Binding Cassette Transporter, Subfamily B; D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D000070997:ATP Binding Cassette Transporter, Subfamily G, Member 2; D018528:ATP-Binding Cassette Transporters; D000972:Antineoplastic Agents, Phytogenic; D003474:Curcumin; D005765:Gastrointestinal Agents; D007659:Ketones; D000089762:Multidrug Resistance-Associated Protein 2; D027425:ATP-Binding Cassette, Sub-Family C Proteins; D009363:Neoplasm Proteins; D010936:Plant Extracts; D012333:RNA, Messenger; D012717:Sesquiterpenes; C513055:ABCB1 protein, human; C116614:ABCG2 protein, human; C573008:alpha-turmerone; C078098:ar-turmerone; C012596:turmeric extract