title: P-Glycoprotein- and cytochrome P-450-mediated herbal drug interactions.
abstract: P-Glycoprotein (P-gp), the most extensively studied ATP-binding cassette transporter, functions as a biological barrier by extruding toxic substances and xenobiotics out of cells. Drug efflux pumps such as P-gp play a functional role in determining the pharmacokinetics of drugs administered by oral and parenteral routes. Determining the activity of drug efflux transport proteins has important implications in the identification of substrates and/or inhibitors. The significant role of the small intestine in reducing the oral bioavailability of drugs is due to metabolic enzymes and efflux transporters. The role of cytochrome P-450 3A (CYP3A) and P-gp in intestinal drug disposition has been highlighted. This review examines the structure, localisation and functional role of P-gp, the mechanism of drug efflux and drug-herb interactions.
authors.affiliation: Centre for Biopharmaceutics and Pharmacokinetics, University College of Pharmaceutical Sciences, Kakatiya University, Warangal, AP, India.
authors.forename: Yamsani Shravan
authors.initials: YS
authors.lastname: Kumar
authors.forename: Devandla
authors.initials: D
authors.lastname: Adukondalu
authors.forename: Dharani
authors.initials: D
authors.lastname: Sathish
authors.forename: Yamsani Vamshi
authors.initials: YV
authors.lastname: Vishnu
authors.forename: Gannu
authors.initials: G
authors.lastname: Ramesh
authors.forename: Athukuri Bharagavi
authors.initials: AB
authors.lastname: Latha
authors.forename: Palem Chinna
authors.initials: PC
authors.lastname: Reddy
authors.forename: Manda
authors.initials: M
authors.lastname: Sarangapani
authors.forename: Yamsani Madhusudan
authors.initials: YM
authors.lastname: Rao
mesh_terms: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000037:antagonists & inhibitors / Q000378:metabolism*; D000818:Animals; D065607:Cytochrome P-450 Enzyme Inhibitors; D003577:Cytochrome P-450 Enzyme System / Q000378:metabolism*; D004791:Enzyme Inhibitors / Q000494:pharmacology; D041743:Herb-Drug Interactions / Q000502:physiology*; D006801:Humans; D007408:Intestinal Absorption / Q000187:drug effects / Q000502:physiology; D007413:Intestinal Mucosa / Q000378:metabolism; D004364:Pharmaceutical Preparations / Q000378:metabolism; D028321:Plant Preparations / Q000009:adverse effects* / Q000378:metabolism*
chemical_list: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D065607:Cytochrome P-450 Enzyme Inhibitors; D004791:Enzyme Inhibitors; D004364:Pharmaceutical Preparations; D028321:Plant Preparations; D003577:Cytochrome P-450 Enzyme System