title: Influence of borneol and muscone on geniposide transport through MDCK and MDCK-MDR1 cells as blood-brain barrier in vitro model.
abstract: The objective of this study was (1) to characterize geniposide transport through MDCK and MDCK-MDR1 cell lines to confirm its transport mechanism and (2) to evaluate the effect of borneol and muscone as enhancers of geniposide transport in the BBB models so as to explore the enhancement mechanism. Transport studies of geniposide were performed in both directions, from apical to basolateral and from basolateral to apical sides. Drug concentrations were analyzed by HPLC. Geniposide showed relatively poor absorption in MDCK and MDCK-MDR1 cells, apparent permeability coefficients ranging from 0.323×10(-6) to 0.422×10(-6) cm/s. The in vitro experiments showed that geniposide transport in both directions was not concentration dependent and saturable, indicating purely passive diffusion. The efflux ratio of geniposide was less than 2 in the two cell models, which suggested that geniposide was not P-gp substrates. Geniposide transport in both directions significantly increased when co-administrated with increasing concentrations of borneol and muscone. Actin staining results indicated that borneol and muscone increased geniposide transport in the BBB models may attribute to disassembly effect on tight junction integrity.
authors: School of Chinese Materia Medica, Beijing University of Chinese Medicine, No. 6, Zhonghuan South Road, Wangjing, Chaoyang District, Beijing 100102, China. Electronic address: chenzhenzhen1@126.com.
authors: Zhen-Zhen
authors: ZZ
authors: Chen
authors: Yang
authors: Y
authors: Lu
authors: Shou-Ying
authors: SY
authors: Du
authors: Ke-Xin
authors: KX
authors: Shang
authors: Cheng-Bo
authors: CB
authors: Cai
mesh_terms: D000818:Animals; D001692:Biological Transport / Q000187:drug effects; D001812:Blood-Brain Barrier / Q000378:metabolism*; D001892:Camphanes / Q000494:pharmacology*; D002470:Cell Survival / Q000187:drug effects; D003516:Cycloparaffins / Q000494:pharmacology*; D004285:Dogs; D016503:Drug Delivery Systems; D039823:Iridoids / Q000493:pharmacokinetics*; D061985:Madin Darby Canine Kidney Cells / Q000378:metabolism; D008954:Models, Biological
chemical_list: D001892:Camphanes; D003516:Cycloparaffins; D039823:Iridoids; C007835:geniposide; C022871:isoborneol; C031021:muscone
keywords: Blood–brain barrier; Borneol; Borneol (PubChem CID: 64685); Drug–drug interaction; Geniposide; Geniposide (PubChem CID: 107848); MDCK; Muscone; Muscone (PubChem CID: 10947)