Abstract
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.
Highlights
Contrary to the general belief that the majority of drugs are synthetic in origin, a number of important medicines are natural products or originate from plants
If phytochemicals show the membrane interactions associated with disease-preventive and therapeutic potentials, they would be the candidates for drug leads, which may lead to the development of novel drugs and enhance the medicinal values of plants containing them
Different techniques such as differential scanning calorimetry (DSC), electron spin resonance (ESR), nuclear magnetic resonance (NMR), electron paramagnetic resonance (EPR), X-ray diffraction, and fluorometry are used for studying the membrane interactions of phytochemicals
Summary
Contrary to the general belief that the majority of drugs are synthetic in origin, a number of important medicines are natural products or originate from plants. A variety of phytochemicals are known to possess antitumor (antiproliferative, cancer-preventive, and apoptosis-inducing), antimicrobial (microbial growth-inhibiting, antibacterial, and antifungal), anti-inflammatory, analgesic, anesthetic, antioxidant (lipid peroxidation-inhibiting and radical scavenging), neuroprotective, and antiplatelet (platelet aggregation-inhibiting and antithrombotic) activity. These diverse bioactivities would provide plants with disease-preventive and therapeutic potentials. The interaction with biomembrane-constituting lipids is referred to as one of the important mechanisms underlying the diverse effects of phytochemicals. A novel mechanistic point of view of phytochemicals would lead to a better understanding of their pharmacological effects, an insight into their medicinal potentials, and a strategic implication for discovering drug leads from plant resources. Kopeć et al [3] recently published an excellent review in which they reviewed the molecular dynamics simulations of the interactions between lipid bilayer membranes and various molecules including drugs and plant extracts
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