title: Comparison of isorhamnetin absorption properties in total flavones of Hippophae rhamnoides L. with its pure form in a Caco-2 cell model mediated by multidrug resistance-associated protein.
abstract: Total flavones of Hippophae rhamnoides L. (TFH) are extracted from the widely distributed thorny bush Sea buckthorn (Hippophae rhamnoides L.). Isorhamnetin (IS) is one of the representative ingredients in TFH. In this study, the absorption properties of IS in TFH and its pure form were compared through transepithelial transport and cellular uptake experiments in a Caco-2 cell model. Our results show that the absorption properties of IS in TFH and its pure form were remarkably different: (1) Both PappAB and PappBA of IS in TFH were dramatically increased compared with those of IS pure form; consequently, its Pratio was 2.3-fold higher than that of IS; (2) Both the accumulation and efflux of IS in TFH were significantly enhanced compared with the single compound. One likely reason for these differences is that the multiple components in TFH significantly down regulated the mRNA expression level of MRP2, which lead to a decrease in the protein level of MRP2, based on western blotting and RT-PCR assays. This study highlights the significant differences in the absorption properties of flavonoid components in different forms and the potential multi-component interactions in TFH.
authors: Research Center for Health and Nutrition, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China; Institute of Digestive Diseases, Longhua Hospital, Shanghai University of Traditional Chinese Medicine, Shanghai 200032, China. Electronic address: rosexie_1996@hotmail.com.
authors: Yan
authors: Y
authors: Xie
authors: Research Center for Health and Nutrition, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China; Institute of Chinese Materia Medica, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
authors: Jingze
authors: J
authors: Duan
authors: Research Center for Health and Nutrition, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China; Institute of Chinese Materia Medica, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
authors: Qingxue
authors: Q
authors: Fu
authors: Research Center for Health and Nutrition, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
authors: Mengxin
authors: M
authors: Xia
authors: Research Center for Health and Nutrition, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
authors: Lei
authors: L
authors: Zhang
authors: Pharmacy Department, Shanghai TCM-integrated Hospital, Shanghai University of Traditional Chinese Medicine, Shanghai 200082, China.
authors: Guowen
authors: G
authors: Li
authors: Institute of Chinese Materia Medica, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
authors: Tao
authors: T
authors: Wu
authors: Institute of Digestive Diseases, Longhua Hospital, Shanghai University of Traditional Chinese Medicine, Shanghai 200032, China. Electronic address: jiliver@vip.sina.com.
authors: Guang
authors: G
authors: Ji
mesh_terms: D018435:ATP Binding Cassette Transporter, Subfamily B / Q000378:metabolism; D000818:Animals; D015153:Blotting, Western; D018938:Caco-2 Cells; D002470:Cell Survival; D004848:Epithelium / Q000378:metabolism; D047309:Flavones / Q000493:pharmacokinetics*; D031281:Hippophae / Q000737:chemistry*; D006801:Humans; D007408:Intestinal Absorption; D000089762:Multidrug Resistance-Associated Protein 2; D027425:ATP-Binding Cassette, Sub-Family C Proteins / Q000096:biosynthesis / Q000235:genetics / Q000378:metabolism*; D010936:Plant Extracts / Q000494:pharmacology*; D011794:Quercetin / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D017207:Rats, Sprague-Dawley
chemical_list: D018435:ATP Binding Cassette Transporter, Subfamily B; D047309:Flavones; D000089762:Multidrug Resistance-Associated Protein 2; D027425:ATP-Binding Cassette, Sub-Family C Proteins; D010936:Plant Extracts; D011794:Quercetin; C000715087:ABCC2 protein, human; C047368:3-methylquercetin
keywords: Absorption; Baicalein (PubChem CID: 5281605); Caco-2 cells; Catechin (PubChem CID: 73160); Hypaconitine (PubChem CID: 23337); Isorhamnetin; Isorhamnetin (PubChem CID: 5281654); Kaempferol (PubChem CID: 5280863); MRP2; Mesaconitine (PubChem CID: 416228); Osthole (PubChem CID: 10228); Paclitaxel (PubChem CID: 441276); Paeoniflorin (PubChem CID: 442534); Quercetin (PubChem CID: 5280343); TFH