Membrane interactions of phytochemicals as their molecular mechanism applicable to the discovery of drug leads from plants
Open accessAbstract
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.
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The antibacterial activity of oxygenated monoterpenes is mediated by their penetration into the fatty acid acyl chains of membrane lipid bilayers, disrupting cell membrane permeability and fluidity.
“The antibacterial activity of oxygenated monoterpenes was previously reported to be mediated by their penetration into the fatty acid acyl chains of membrane lipid bilayers, which disrupted cell membrane permeability and fluidity (Tsuchiya 2015).”
From In vitro antimicrobial potency of Elettaria cardamomum ethanolic extract against multidrug resistant of food poisoning bacterial strains (2022) · cites this paper as Tsuchiya 2015
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- Authors
- Tsuchiya, H.
- Affiliations
- Asahi University (JP)
- Corresponding author
- Tsuchiya, Hironori
- ORCID
- Tsuchiya, Hironori
- Venue
- Molecules
- Publisher
- MDPI AG
- Published
- 2015-10-16
- Volume
- 20
- Issue
- 10
- Pages
- 18923-18966
- ISSN
- 1420-3049 (ISSN-L)
- PMC
- PMC6332185
- OpenAlex
- W1931359360
- Cited by
- 237
- References
- 167
- Citations by year
- 2026: 30 · 2025: 25 · 2024: 25 · 2023: 18 · 2022: 25 · 2021: 26 · 2020: 32 · 2019: 17 · 2018: 13 · 2017: 14 · 2016: 12
- FWCI
- 1.26
- Type
- journal article
- Language
- en
- Open access
- gold
- dx.doi.org
- Licence
- Locations
- Molecules (publishedVersion, cc-by)
- Europe PMC (PubMed Central) (publishedVersion, other-oa)
- PubMed Central (publishedVersion, cc-by)
- PubMed (publishedVersion)
- Institutional Repositories DataBase (IRDB) (submittedVersion, cc-by-nc-nd)
- DOAJ (DOAJ: Directory of Open Access Journals) (submittedVersion)
- Funders
- Japan Society for the Promotion of Science (26463078, 23593005)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Lipid Membrane Structure and Behavior
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Protein Interaction Studies and Fluorescence Analysis
- Physical Sciences › Computer Science › Computational Theory and Mathematics › Computational Drug Discovery Methods
- Keywords
- phytochemicals, membrane interactions, membrane fluidity, membrane microviscosity, membrane permeability, drug discovery from plants, flavonoids, terpenoids, stilbenoids, capsaicinoids, phloroglucinol, naphthodianthrones, organosulfur compounds, alkaloids, ginsenosides, pentacyclic triterpenes, curcuminoids, lead compound identification
- MeSH terms
- Animals, Capsaicin, Cell Membrane, Flavonoids, Humans, Plant Extracts, Stilbenes, Terpenes, Drug Discovery
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