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Cholinesterase inhibitory activity of tinosporide and 8-hydroxytinosporide isolated from Tinospora cordifolia: In vitro and in silico studies targeting management of Alzheimer’s disease

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 E...

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Autores principales: Adib, Mohiminul, Islam, Rashedul, Ahsan, Monira, Rahman, Arifur, Hossain, Mahmud, Rahman, Md Mustafizur, Alshehri, Sultan M., Kazi, Mohsin, Mazid, Md Abdul
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8241625/
https://www.ncbi.nlm.nih.gov/pubmed/34220245
http://dx.doi.org/10.1016/j.sjbs.2021.03.063
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author Adib, Mohiminul
Islam, Rashedul
Ahsan, Monira
Rahman, Arifur
Hossain, Mahmud
Rahman, Md Mustafizur
Alshehri, Sultan M.
Kazi, Mohsin
Mazid, Md Abdul
author_facet Adib, Mohiminul
Islam, Rashedul
Ahsan, Monira
Rahman, Arifur
Hossain, Mahmud
Rahman, Md Mustafizur
Alshehri, Sultan M.
Kazi, Mohsin
Mazid, Md Abdul
author_sort Adib, Mohiminul
collection PubMed
description 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 IC(50) (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 IC(50) value of 13.45 ± 0.144, whereas TC-19R confirmed as 8-hydroxytinosporide moderately inhibited AChE with IC(50) value of 46.71 ± 0.511. In case of BuChE inhibition, the IC(50) 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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spelling pubmed-82416252021-07-02 Cholinesterase inhibitory activity of tinosporide and 8-hydroxytinosporide isolated from Tinospora cordifolia: In vitro and in silico studies targeting management of Alzheimer’s disease Adib, Mohiminul Islam, Rashedul Ahsan, Monira Rahman, Arifur Hossain, Mahmud Rahman, Md Mustafizur Alshehri, Sultan M. Kazi, Mohsin Mazid, Md Abdul Saudi J Biol Sci Original Article 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 IC(50) (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 IC(50) value of 13.45 ± 0.144, whereas TC-19R confirmed as 8-hydroxytinosporide moderately inhibited AChE with IC(50) value of 46.71 ± 0.511. In case of BuChE inhibition, the IC(50) 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. Elsevier 2021-07 2021-03-30 /pmc/articles/PMC8241625/ /pubmed/34220245 http://dx.doi.org/10.1016/j.sjbs.2021.03.063 Text en © 2021 Published by Elsevier B.V. on behalf of King Saud University. https://creativecommons.org/licenses/by-nc-nd/4.0/This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).
spellingShingle Original Article
Adib, Mohiminul
Islam, Rashedul
Ahsan, Monira
Rahman, Arifur
Hossain, Mahmud
Rahman, Md Mustafizur
Alshehri, Sultan M.
Kazi, Mohsin
Mazid, Md Abdul
Cholinesterase inhibitory activity of tinosporide and 8-hydroxytinosporide isolated from Tinospora cordifolia: In vitro and in silico studies targeting management of Alzheimer’s disease
title Cholinesterase inhibitory activity of tinosporide and 8-hydroxytinosporide isolated from Tinospora cordifolia: In vitro and in silico studies targeting management of Alzheimer’s disease
title_full Cholinesterase inhibitory activity of tinosporide and 8-hydroxytinosporide isolated from Tinospora cordifolia: In vitro and in silico studies targeting management of Alzheimer’s disease
title_fullStr Cholinesterase inhibitory activity of tinosporide and 8-hydroxytinosporide isolated from Tinospora cordifolia: In vitro and in silico studies targeting management of Alzheimer’s disease
title_full_unstemmed Cholinesterase inhibitory activity of tinosporide and 8-hydroxytinosporide isolated from Tinospora cordifolia: In vitro and in silico studies targeting management of Alzheimer’s disease
title_short Cholinesterase inhibitory activity of tinosporide and 8-hydroxytinosporide isolated from Tinospora cordifolia: In vitro and in silico studies targeting management of Alzheimer’s disease
title_sort cholinesterase inhibitory activity of tinosporide and 8-hydroxytinosporide isolated from tinospora cordifolia: in vitro and in silico studies targeting management of alzheimer’s disease
topic Original Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8241625/
https://www.ncbi.nlm.nih.gov/pubmed/34220245
http://dx.doi.org/10.1016/j.sjbs.2021.03.063
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