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Molecules 2015, 20(10), 18923-18966; doi:10.3390/molecules201018923

Membrane Interactions of Phytochemicals as Their Molecular Mechanism Applicable to the Discovery of Drug Leads from Plants

Department of Dental Basic Education, Asahi University School of Dentistry, 1851 Hozumi, Mizuho, Gifu 501-0296, Japan
Academic Editors: Maurizio Battino, Etsuo Niki and José L. Quiles
Received: 11 September 2015 / Revised: 11 October 2015 / Accepted: 14 October 2015 / Published: 16 October 2015
(This article belongs to the Special Issue 20th Anniversary of Molecules—Recent Advances in Natural Products)
View Full-Text   |   Download PDF [1162 KB, uploaded 16 October 2015]   |  


In addition to interacting with functional proteins such as receptors, ion channels, and enzymes, a variety of drugs mechanistically act on membrane lipids to change the physicochemical properties of biomembranes as reported for anesthetic, adrenergic, cholinergic, non-steroidal anti-inflammatory, analgesic, antitumor, antiplatelet, antimicrobial, and antioxidant drugs. As well as these membrane-acting drugs, bioactive plant components, phytochemicals, with amphiphilic or hydrophobic structures, are presumed to interact with biological membranes and biomimetic membranes prepared with phospholipids and cholesterol, resulting in the modification of membrane fluidity, microviscosity, order, elasticity, and permeability with the potencies being consistent with their pharmacological effects. A novel mechanistic point of view of phytochemicals would lead to a better understanding of their bioactivities, an insight into their medicinal benefits, and a strategic implication for discovering drug leads from plants. This article reviews the membrane interactions of different classes of phytochemicals by highlighting their induced changes in membrane property. The phytochemicals to be reviewed include membrane-interactive flavonoids, terpenoids, stilbenoids, capsaicinoids, phloroglucinols, naphthodianthrones, organosulfur compounds, alkaloids, anthraquinonoids, ginsenosides, pentacyclic triterpene acids, and curcuminoids. The membrane interaction’s applicability to the discovery of phytochemical drug leads is also discussed while referring to previous screening and isolating studies. View Full-Text
Keywords: phytochemical; molecular mechanism; membrane interaction; membrane fluidity; drug lead phytochemical; molecular mechanism; membrane interaction; membrane fluidity; drug lead

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Tsuchiya, H. Membrane Interactions of Phytochemicals as Their Molecular Mechanism Applicable to the Discovery of Drug Leads from Plants. Molecules 2015, 20, 18923-18966.

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