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

机译：植物化学物质的膜相互作用作为其分子机理适用于从植物中发现药物引线

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摘要

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.
机译：除了与功能性蛋白质（例如受体，离子通道和酶）相互作用外，多种药物还可以机械作用于膜脂，从而改变生物膜的理化性质，如麻醉药，肾上腺素能，胆碱能药，非甾体类抗炎药，止痛药所报道的那样。 ，抗肿瘤，抗血小板，抗微生物和抗氧化药物。除这些膜作用药物外，还假定具有两亲或疏水结构的生物活性植物成分，植物化学物质与由磷脂和胆固醇制备的生物膜和仿生膜相互作用，从而导致膜流动性，微粘度，有序性，弹性的改变以及渗透性，且药效与其药理作用一致。一种新颖的植物化学机理观点将有助于人们更好地了解其生物活性，深入了解其药用价值，并从植物中发现药物线索具有战略意义。本文通过突出不同种类植物化学物质的膜特性引起的变化，来回顾它们之间的膜相互作用。待审查的植物化学物质包括膜相互作用的类黄酮，萜类化合物，二苯乙烯类化合物，辣椒素类化合物，间苯三酚，萘二酮，有机硫化合物，生物碱，蒽醌类，人参皂甙，五环三萜酸和姜黄素。在参考以前的筛选和分离研究的同时，还讨论了膜相互作用对植物化学药物前导物发现的适用性。

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