Dihydroagarofuranoid Sesquiterpenes as Acetylcholinesterase Inhibitors from Celastraceae Plants: Maytenus disticha and Euonymus japonicus
Abstract
Natural cholinesterase inhibitors have been found in many biological sources. Nine compounds with agarofuran (epoxyeudesmane) skeletons were isolated from seeds and aerial parts of Maytenus disticha and Euonymus japonicus. The identification and structural elucidation of compounds were based on spectroscopic data analyses. All compounds had inhibitory acetylcholinesterase (AChE) activity. These natural compounds, which possessed mixed or uncompetitive mechanisms of inhibitory activity against AChE, may be considered as models for the design and development of new naturally occurring drugs for management strategies for neurodegenerative diseases. This is the first report of these chemical structures for seeds of M. disticha.
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Agarofuran compounds may act as lead compounds in designing new, less toxic, highly selective anticholinesterase agents along with other positive therapeutic effects.
“Studies conducted on the agarofuran compounds with a motive of developing some new AChE inhibitors have achieved great success in the past years and suggested that agarofuran compounds may act as lead compounds in the designing of new, less toxic, and highly selective anticholinesterase agents along with some other positive therapeutic effects [130,131].”
From Acetylcholinesterase Inhibitory Potential of Various Sesquiterpene Analogues for Alzheimer’s Disease Therapy (2021) · cites this paper as [131]
Compounds 44-51 are selective inhibitors for AChE activity.
“On the other hand, these compounds are found to be selective inhibitors for AChE activity.”
From Acetylcholinesterase Inhibitory Potential of Various Sesquiterpene Analogues for Alzheimer’s Disease Therapy (2021) · cites this paper as [131]
Compounds 44-51 isolated from seeds of Maytenus disticha and Euonymus japonicas exhibited AChE inhibitory activity with IC50 values of 0.1-0.4 mg/mL.
“The compounds isolated from seeds of M. disticha and E. japonicas showed the AChE inhibitory activity with the IC50 (mg/mL) of 0.1 ± 0.01 (44), 0.3 ± 0.02 (45), 0.1 ± 0.004 (46), 0.1 ± 0.006 (47), 0.1 ± 0.002 (48), 0.3 ± 0.015 (49), 0.4 ± 0.006 (50) and 0.4 ± 0.009 for the compound (51).”
From Acetylcholinesterase Inhibitory Potential of Various Sesquiterpene Analogues for Alzheimer’s Disease Therapy (2021) · cites this paper as [131]
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Arya, A., Chahal, R., Rao, R., Rahman, M. H., Kaushik, D., Akhtar, M. F., Saleem, A., Khalifa, S. M. A., El-Seedi, H. R., Kamel, M., et al. (2021) · Biomolecules · doi:10.3390/biom11030350 · Cited by 111 · see citing works
- Authors
- Alarcón, J., Cespedes, C. L., Muñoz, E., Balbontin, C., Valdes, F., Gutierrez, M., Astudillo, L., & Seigler, D. S.
- Affiliations
- University of Bío-Bío (CL)
- Laboratorio de Sı́ntesis y Biotransformación de Productos Naturales, Facultad de Ciencias, Universidad del Bı́o-Bı́o, Avenida Andrés Bello s/n, Casilla 447, CP 3780000, Chillán, Chile
- Instituto de Quı́mica, Universidad de Talca, Talca, Chile
- Universidad de Talca (CL)
- University of Illinois Urbana-Champaign (US)
- Corresponding author
- Alarcón, Julio
- Venue
- Journal of Agricultural and Food Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2015-11-19
- Volume
- 63
- Issue
- 47
- Pages
- 10250-10256
- ISSN
- 0021-8561 (ISSN-L)
- 1520-5118
- OpenAlex
- W2412757402
- Cited by
- 33
- References
- 30
- Citations by year
- 2026: 2 · 2025: 3 · 2024: 4 · 2023: 2 · 2022: 3 · 2021: 3 · 2020: 5 · 2019: 5 · 2018: 2 · 2017: 4
- FWCI
- 2.42
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Journal of Agricultural and Food Chemistry (publishedVersion)
- PubMed (publishedVersion)
- Funders
- Fondo Nacional de Desarrollo Científico y Tecnológico (1130463)
- Topics
- Life Sciences › Agricultural and Biological Sciences › Plant Science › Phytochemistry and Biological Activities
- Health Sciences › Medicine › Pharmacology › Cholinesterase and Neurodegenerative Diseases
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Bioactive natural compounds
- Keywords
- sesquiterpenes, acetylcholinesterase inhibitors, Euonymus japonicus, Celastraceae, seed chemical composition
- MeSH terms
- Acetylcholinesterase, Cholinesterase Inhibitors, Humans, Kinetics, Plant Extracts, Sesquiterpenes, Structure-Activity Relationship, Molecular Structure, Maytenus, Euonymus
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