Epibatidine: A Promising Natural Alkaloid in Health
Open accessAbstract
Epibatidine is a natural alkaloid that acts at nicotinic acetylcholine receptors (nAChRs). The present review aims to carefully discuss the affinity of epibatidine and its synthetic derivatives, analogues to nAChRs for α4β2 subtype, pharmacokinetic parameters, and its role in health. Published literature shows a low affinity and lack of binding of epibatidine and its synthetic analogues to plasma proteins, indicating their availability for metabolism. Because of its high toxicity, the therapeutic use of epibatidine is hampered. However, new synthetic analogs endowed from this molecule have been developed, with a better therapeutic window and improved selectivity. All these aspects are also discussed here. On the other hand, many reports are devoted to structure–activity relationships to obtain optically active epibatidine and its analogues, and to access its pharmacological effects. Although pharmacological results are obtained from experimental studies and only a few clinical trials, new perspectives are open for the discovery of new drug therapies.
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Bioactive molecules such as phenolic compounds, flavonoids and non-flavonoids, carotenoids, and others can exert neuroprotective effects by suppressing activation of microglia that modulates inflammatory processes in the CNS.
“Reports show that bioactive molecules such as phenolic compounds, flavonoids and non-flavonoids, carotenoids, and others can exert neuroprotective effects by suppressing the activation of the microglia that modulates inflammatory processes in the CNS [119,157].”
From Multi-Target Mechanisms of Phytochemicals in Alzheimer’s Disease: Effects on Oxidative Stress, Neuroinflammation and Protein Aggregation (2022) · cites this paper as [157]
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- Authors
- Salehi, B., Sestito, S., Rapposelli, S., Peron, G., Calina, D., Sharifi-Rad, M., Sharopov, F., Martins, N., & Sharifi-Rad, J.
- Affiliations
- Bam University of Medical Sciences (IR)
- University of Pisa (IT)
- University of Padua (IT)
- Department of Clinical Pharmacy, University of Medicine and Pharmacy Craiova, Craiova 200349, Romania
- Department of Medical Parasitology, Zabol University of Medical Sciences, Zabol 61663-335, Iran
- Tajik State Medical University (TJ)
- Universidade do Porto (PT)
- Zabol Medicinal Plants Research Center, Zabol University of Medical Sciences, Zabol 61615-585, Iran
- Corresponding author
- Martins, Natália
- ORCID
- Venue
- Biomolecules
- Publisher
- MDPI AG
- Published
- 2018-12-23
- Volume
- 9
- Issue
- 1
- Pages
- 6
- ISSN
- 2218-273X (ISSN-L)
- PMC
- PMC6359223
- OpenAlex
- W2906609434
- Cited by
- 91
- References
- 44
- Citations by year
- 2026: 3 · 2025: 7 · 2024: 10 · 2023: 18 · 2022: 22 · 2021: 23 · 2020: 8
- FWCI
- 1.50
- Type
- journal article
- Language
- en
- Open access
- gold
- dx.doi.org
- Licence
- Locations
- Biomolecules (publishedVersion, cc-by)
- Europe PMC (PubMed Central) (publishedVersion, cc-by)
- PubMed Central (publishedVersion, cc-by)
- PubMed (publishedVersion)
- Portuguese National Funding Agency for Science, Research and Technology (RCAAP Project by FCT) (submittedVersion, cc-by)
- CINECA IRIS Institutial research information system (University of Pisa) (submittedVersion, cc-by)
- DOAJ (DOAJ: Directory of Open Access Journals) (submittedVersion, cc-by-sa)
- Institutional Research Information System (Università degli Studi di Brescia) (submittedVersion)
- UnissResearch (Università degli Studi di Sassari) (submittedVersion, cc-by)
- Funders
- Fundação para a Ciência e a Tecnologia (01-0145, NORTE-01-0145-FEDER-000012, UID/BIM/04293/2013, UID/BIM/04293, NORTE2020, NORTE-01-0145)
- Topics
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmacology › Alkaloids: synthesis and pharmacology
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Nicotinic Acetylcholine Receptors Study
- Physical Sciences › Chemistry › Organic Chemistry › Advanced Synthetic Organic Chemistry
- Keywords
- epibatidine, natural alkaloids, nicotinic acetylcholine receptors, synthetic analogues, pharmacokinetics, plasma protein binding, toxicity, structure-activity relationship, drug discovery
- MeSH terms
- Alkaloids, Analgesics, Attention Deficit Disorder with Hyperactivity, Cytochrome P-450 Enzyme System, Humans, Isoxazoles, Pyridines, Pyrrolidines, Quantum Theory, Receptors, Nicotinic, Bridged Bicyclo Compounds, Heterocyclic, Neurodegenerative Diseases
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