Cholinesterase inhibitory activity of tinosporide and 8-hydroxytinosporide isolated from Tinospora cordifolia: In vitro and in silico studies targeting management of Alzheimer’s disease
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Tinosporide and 8-hydroxytinosporide isolated from Tinospora cordifolia were evaluated for acetylcholinesterase (AChE) and butylcholinesterase (BuChE) inhibitory activities. The structure of the compound was confirmed by spectroscopic analysis, whereas cholinesterase inhibition was investigated by Ellman method using donepezil as standard drug and the data were presented as IC50 (μg/ml ± SEM). Furthermore, donepezil, tinosporide and 8-hydroxytinosporide were executed for docking analysis. The results from the isolated compounds TC-16R confirmed as tinosporide promisingly inhibited AChE with IC50 value of 13.45 ± 0.144, whereas TC-19R confirmed as 8-hydroxytinosporide moderately inhibited AChE with IC50 value of 46.71 ± 0.511. In case of BuChE inhibition, the IC50 values were found to be 408.50 ± 17.197 and 317.26 ± 6.918 for tinosporide and 8-hydroxytinosporide, respectively. The in silico studies revealed that the ligand tinosporide fit with the binding sites and inhibited AChE. Overall, the study findings suggested that tinosporide would be a complementary noble molecule of donepezil which is correlated with its pharmacological activity through in vitro studies, while 8-hydroxytinosporide modestly inhibited BuChE and the results are very close to the standard donepezil.
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Tinosporide shows significant anti-AChE activity.
“The tinosporide shows significant anti-AChE activity.”
From Unlocking the Therapeutic Potential of Medicinal Plants for Alzheimer’s Disease: Preclinical to Clinical Trial Insights (2023) · cites this paper as [132]
Tinosporide is a powerful inhibitor of AChE enzyme and a suitable lead for drug development for cognitive impairment.
“The results of the docking study indicated that donepezil's complementary novel ligand, tinosporide, would be a suitable lead for the development of drugs to be utilized in the treatment of cognitive impairment, as tinosporide is a powerful inhibitor of the AChE enzyme.”
From Unlocking the Therapeutic Potential of Medicinal Plants for Alzheimer’s Disease: Preclinical to Clinical Trial Insights (2023) · cites this paper as [132]
Tinosporide is a complementary molecule of donepezil; 8-hydroxytinosporide modestly inhibits BuChE, close to donepezil.
“The findings suggested that tinosporide would be a complementary noble molecule of donepezil, which is correlated with its pharmacological activity through in vitro studies, whereas 8-hydroxytinosporide inhibited BuChE modestly, and the results are very close to the standard donepezil [132].”
From Unlocking the Therapeutic Potential of Medicinal Plants for Alzheimer’s Disease: Preclinical to Clinical Trial Insights (2023) · cites this paper as [132]
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- Authors
- Adib, M., Islam, R., Ahsan, M., Rahman, A., Hossain, M., Rahman, M. M., Alshehri, S. M., Kazi, M., & Mazid, M. A.
- Affiliations
- University of Dhaka (BD)
- Jagannath University (BD)
- Khulna University (BD)
- King Saud University (SA)
- Corresponding author
- Mazid, Md Abdul
- ORCID
- Venue
- Saudi Journal of Biological Sciences
- Publisher
- Elsevier BV
- Published
- 2021-07
- Volume
- 28
- Issue
- 7
- Pages
- 3893-3900
- ISSN
- 1319-562X (ISSN-L)
- PMC
- PMC8241625
- OpenAlex
- W3149407988
- Cited by
- 19
- References
- 33
- Citations by year
- 2026: 4 · 2025: 3 · 2024: 4 · 2023: 5 · 2022: 2 · 2021: 1
- FWCI
- 1.75
- Type
- journal article
- Language
- en
- Open access
- hybrid
- doi.org
- Licence
- Locations
- Saudi Journal of Biological Sciences (publishedVersion, cc-by-nc-nd)
- PubMed Central (publishedVersion, cc-by-nc-nd)
- PubMed (publishedVersion)
- DOAJ (DOAJ: Directory of Open Access Journals) (submittedVersion, cc-by-sa)
- Funders
- King Saud University (RSP-2020/146)
- University of Dhaka
- Topics
- Health Sciences › Medicine › Pharmacology › Cholinesterase and Neurodegenerative Diseases
- Health Sciences › Medicine › Complementary and alternative medicine › Medicinal Plants and Neuroprotection
- Health Sciences › Medicine › Physiology › Alzheimer's disease research and treatments
- Keywords
- Tinospora cordifolia, acetylcholinesterase inhibition, butyrylcholinesterase inhibition, Alzheimer's disease, donepezil, molecular docking, natural product isolation, cholinesterase inhibitors
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