Natural sesquiterpen lactones as acetylcholinesterase inhibitors
Open accessAbstract
Background and the purpose of the study: The amount of elder people who suffer from Alzheimer disease is continuously increasing every year. Cholinesterase inhibitors have shown to be effective in alleviating the symptoms of the disease, thus opening a field of research for these treatments. Herbal products, owning a reputation as effective agents in many biological studies are now drawing attention for inhibiting acetylcholinesterase, in other words, Alzheimer disease. In the present study, the ability of three sesquiterpene lactones from Inula oculus-christi and I. aucheriana to inhibit AChE has been evaluated through Ellman assay. Materials and Methods: Gaillardin and pulchellin C were obtained from I. oculus-christi and britannin from I. aucheriana by chromatographic methods. They were dissolved in methanol in concentration of 3 mg/mL and the AChEI activity of the compounds was determined by Ellman method using Acethylthiocholine iodide as the substrate and 5, 5'-dithiobis-2-nitrobenzoic acid as the reagent, in 96-well plates at 405 nm. Results: AChEI activity of the examined compounds was obtained as 67.0, 25.2 and 10.9% in concentration of 300 µg/L for gaillardin, britannin and pulchellin C, respectively. Conclusion: Among the three sesquiterpene lactones, gaillardin with 67% inhibition of AChE could be considered a good candidate for future Alzheimer studies.
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Gaillardin from Inula oculus-christi and I. aucheriana had AChE IC50 = 729 μM.
“It was observed that out of the three evaluated compounds, the Gaillardin (36) was the most versatile secondary metabolites (IC50 for AChE 729 μM) present in the plants and can be investigated for further AD studies.”
From Acetylcholinesterase Inhibitory Potential of Various Sesquiterpene Analogues for Alzheimer’s Disease Therapy (2021) · cites this paper as [123]
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- Authors
- HAJIMEHDIPOOR, H., MOSADDEGH, M., NAGHIBI, F., HAERI, A., & HAMZELOO-MOGHADAM, M.
- Affiliations
- Shahid Beheshti University (IR)
- Shahid Beheshti University of Medical Sciences, Iran
- Venue
- Anais da Academia Brasileira de Ciências
- Publisher
- FapUNIFESP (SciELO)
- Published
- 2014-06
- Volume
- 86
- Issue
- 2
- Pages
- 801-806
- ISSN
- 0001-3765 (ISSN-L)
- OpenAlex
- W2000930848
- Cited by
- 22
- References
- 24
- Citations by year
- 2026: 1 · 2025: 2 · 2024: 1 · 2023: 3 · 2022: 1 · 2021: 4 · 2020: 5 · 2017: 3 · 2015: 2
- FWCI
- 1.22
- Type
- journal article
- Language
- en
- Open access
- diamond
- doi.org
- Licence
- cc-by-nc
- Locations
- Anais da Academia Brasileira de Ciências (publishedVersion, cc-by-nc)
- PubMed (publishedVersion)
- LA Referencia (Red Federada de Repositorios Institucionales de Publicaciones Científicas) (publishedVersion, other-oa)
- Americanae (AECID Library) (submittedVersion, other-oa)
- DOAJ (DOAJ: Directory of Open Access Journals) (submittedVersion)
- Redalyc (Universidad Autónoma del Estado de México) (submittedVersion)
- Funders
- Shahid Beheshti University of Medical Sciences
- Topics
- Health Sciences › Medicine › Pharmacology › Cholinesterase and Neurodegenerative Diseases
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Cancer Research › Sesquiterpenes and Asteraceae Studies
- Life Sciences › Agricultural and Biological Sciences › Plant Science › Phytochemistry and Biological Activities
- Keywords
- sesquiterpene lactones, acetylcholinesterase inhibitors, Alzheimer's disease, Inula oculus-christi, herbal products, Ellman assay
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