title: Recommended Daily Dose of Sesame Lignans Has No Influence on Oral Absorption of P-Glycoprotein Substrates in Rats.
abstract: Sesamin (SM) and episesamin (ESM) are constituents of sesame seeds, which are used in health foods and considered to have various beneficial effects in the prevention of lifestyle-related diseases. P-Glycoprotein (P-gp) is an ATP-binding cassette transporter involved in drug absorption in the human gastrointestinal tract. A recent report indicated that SM influences P-gp-mediated drug transport. In the present study, we investigated whether SM and ESM inhibit P-gp in vitro, using Caco-2 cells and the typical P-gp substrates rhodamine123 (Rho123) and fexofenadine. SM and ESM showed no effect on accumulation of these compounds, indicating that SM and ESM do not influence P-gp function. In addition, an in vivo study using Rho123 indicated that SM and ESM do not affect absorption of P-gp substrates. Overall, these results suggest that health foods containing SM and ESM are unlikely to interact with P-gp substrates.
authors.affiliation: Laboratory of Clinical Pharmacokinetics, Graduate School of Pharmaceutical Sciences, Takasaki University of Health and Welfare.
authors.forename: Takumi
authors.initials: T
authors.lastname: Tomono
authors.forename: Kyoma
authors.initials: K
authors.lastname: Otsuka
authors.forename: Kentaro
authors.initials: K
authors.lastname: Yano
authors.forename: Masahiko
authors.initials: M
authors.lastname: Kanagawa
authors.forename: Hiroshi
authors.initials: H
authors.lastname: Arakawa
authors.forename: Takuo
authors.initials: T
authors.lastname: Ogihara
mesh_terms: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000378:metabolism*; D000818:Animals; D001692:Biological Transport; D018938:Caco-2 Cells; D004149:Dioxoles / Q000494:pharmacology*; D004347:Drug Interactions; D018565:Food-Drug Interactions; D006801:Humans; D007408:Intestinal Absorption / Q000187:drug effects; D017705:Lignans / Q000494:pharmacology*; D008297:Male; D010936:Plant Extracts / Q000494:pharmacology; D017208:Rats, Wistar; D020112:Rhodamine 123 / Q000493:pharmacokinetics*; D012639:Seeds / Q000737:chemistry*; D031685:Sesamum / Q000737:chemistry*; D016593:Terfenadine / Q000031:analogs & derivatives* / Q000493:pharmacokinetics
chemical_list: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D004149:Dioxoles; D017705:Lignans; D010936:Plant Extracts; D020112:Rhodamine 123; D016593:Terfenadine; C093230:fexofenadine; C054125:sesamin