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Methylation and acetylation enhanced the antidiabetic activity of some selected flavonoids: In vitro, molecular modelling and structure activity relationship based study

Flavonoids have been reported to exert antihyperglycemic effects and have potential to enhance the current therapy options against type 2 diabetes mellitus. However, the structure activity relationships (SAR) studies of flavonoids against this disease have not been thoroughly comprehended. Hence, in...

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Main Authors: Ahmed, Qamar Uddin, Sarian, Murni Nazira, Mat So'ad, Siti Zaiton, Latip, Jalifah, Arief Ichwan, Solachuddin Jauhari, Hussein, Nurlaili Najmie, Bakhtiar, M. Taher, Alhassan, Alhassan Muhammad, Hamidon, Hanisuhana, Fakurazi, Sharida
Format: Article
Language:English
English
English
Published: MDPI 2018
Subjects:
Q Science (General)
Online Access:http://irep.iium.edu.my/67823/7/67823%20Methylation%20and%20Acetylation%20Enhanced.pdf
http://irep.iium.edu.my/67823/8/67823%20Methylation%20and%20Acetylation%20Enhanced%20SCOPUS.pdf
http://irep.iium.edu.my/67823/19/67823%20Methylation%20and%20Acetylation%20Enhanced%20WOS.pdf
http://irep.iium.edu.my/67823/
https://www.mdpi.com/2218-273X/8/4/149
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spelling my.iium.irep.678232019-01-27T06:52:34Z http://irep.iium.edu.my/67823/ Methylation and acetylation enhanced the antidiabetic activity of some selected flavonoids: In vitro, molecular modelling and structure activity relationship based study Ahmed, Qamar Uddin Sarian, Murni Nazira Mat So'ad, Siti Zaiton Latip, Jalifah Arief Ichwan, Solachuddin Jauhari Hussein, Nurlaili Najmie Bakhtiar, M. Taher Alhassan, Alhassan Muhammad Hamidon, Hanisuhana Fakurazi, Sharida Q Science (General) Flavonoids have been reported to exert antihyperglycemic effects and have potential to enhance the current therapy options against type 2 diabetes mellitus. However, the structure activity relationships (SAR) studies of flavonoids against this disease have not been thoroughly comprehended. Hence, in the present study, 14 structurally related flavonoids viz. wogonin, techtochrysin, norwogonin, isoscutellarein, hypolaetin, kaempferol, quercetin, methyl ether of wogonin, acetate of wogonin, acetate of norwogonin, 8-hydroxy-7-methoxyflavone, chrysin, (+)-catechin and (-)-epicatechin were taken into account for in vitro antidiabetic evaluation. Cell viability of RIN-5F pancreatic cells and 3T3-L1 pre-adipocyte cells was initially tested, then an insulin secretion assay of RIN-5F as well as adipogenesis and glucose uptake measurements of adipocyte were investigated. Subsequently, protein expressions study through adipokines measurement (leptin, adiponectin, TNF-α, RBP-4) via enzyme-linked immunosorbent assay (ELISA) kit, Western blotting analysis against GLUT4 and C/EBP-α as well as molecular docking against GLUT1 were analyzed. The results from cell culture antidiabetic assays (insulin secretion, adipogenesis, and glucose uptake), protein expressions and molecular docking pointed that the methoxy group at position C-8 is responsible for antidiabetic property of selected flavonoids via glucose uptake mechanism indicated by up regulation of GLUT4 and C/EBP-α expressions. The mechanism could be enhanced by the addition of an acetate group at C-5 and C-7 of the flavone skeleton. MDPI 2018-12 Article PeerReviewed application/pdf en http://irep.iium.edu.my/67823/7/67823%20Methylation%20and%20Acetylation%20Enhanced.pdf application/pdf en http://irep.iium.edu.my/67823/8/67823%20Methylation%20and%20Acetylation%20Enhanced%20SCOPUS.pdf application/pdf en http://irep.iium.edu.my/67823/19/67823%20Methylation%20and%20Acetylation%20Enhanced%20WOS.pdf Ahmed, Qamar Uddin and Sarian, Murni Nazira and Mat So'ad, Siti Zaiton and Latip, Jalifah and Arief Ichwan, Solachuddin Jauhari and Hussein, Nurlaili Najmie and Bakhtiar, M. Taher and Alhassan, Alhassan Muhammad and Hamidon, Hanisuhana and Fakurazi, Sharida (2018) Methylation and acetylation enhanced the antidiabetic activity of some selected flavonoids: In vitro, molecular modelling and structure activity relationship based study. Biomolecules, 8 (4). pp. 1-22. ISSN 2218-273X https://www.mdpi.com/2218-273X/8/4/149 10.3390/biom8040149
institution Universiti Islam Antarabangsa Malaysia
building IIUM Library
collection Institutional Repository
continent Asia
country Malaysia
content_provider International Islamic University Malaysia
content_source IIUM Repository (IREP)
url_provider http://irep.iium.edu.my/
language English
English
English
topic Q Science (General)
spellingShingle Q Science (General)
Ahmed, Qamar Uddin
Sarian, Murni Nazira
Mat So'ad, Siti Zaiton
Latip, Jalifah
Arief Ichwan, Solachuddin Jauhari
Hussein, Nurlaili Najmie
Bakhtiar, M. Taher
Alhassan, Alhassan Muhammad
Hamidon, Hanisuhana
Fakurazi, Sharida
Methylation and acetylation enhanced the antidiabetic activity of some selected flavonoids: In vitro, molecular modelling and structure activity relationship based study
description Flavonoids have been reported to exert antihyperglycemic effects and have potential to enhance the current therapy options against type 2 diabetes mellitus. However, the structure activity relationships (SAR) studies of flavonoids against this disease have not been thoroughly comprehended. Hence, in the present study, 14 structurally related flavonoids viz. wogonin, techtochrysin, norwogonin, isoscutellarein, hypolaetin, kaempferol, quercetin, methyl ether of wogonin, acetate of wogonin, acetate of norwogonin, 8-hydroxy-7-methoxyflavone, chrysin, (+)-catechin and (-)-epicatechin were taken into account for in vitro antidiabetic evaluation. Cell viability of RIN-5F pancreatic cells and 3T3-L1 pre-adipocyte cells was initially tested, then an insulin secretion assay of RIN-5F as well as adipogenesis and glucose uptake measurements of adipocyte were investigated. Subsequently, protein expressions study through adipokines measurement (leptin, adiponectin, TNF-α, RBP-4) via enzyme-linked immunosorbent assay (ELISA) kit, Western blotting analysis against GLUT4 and C/EBP-α as well as molecular docking against GLUT1 were analyzed. The results from cell culture antidiabetic assays (insulin secretion, adipogenesis, and glucose uptake), protein expressions and molecular docking pointed that the methoxy group at position C-8 is responsible for antidiabetic property of selected flavonoids via glucose uptake mechanism indicated by up regulation of GLUT4 and C/EBP-α expressions. The mechanism could be enhanced by the addition of an acetate group at C-5 and C-7 of the flavone skeleton.
format Article
author Ahmed, Qamar Uddin
Sarian, Murni Nazira
Mat So'ad, Siti Zaiton
Latip, Jalifah
Arief Ichwan, Solachuddin Jauhari
Hussein, Nurlaili Najmie
Bakhtiar, M. Taher
Alhassan, Alhassan Muhammad
Hamidon, Hanisuhana
Fakurazi, Sharida
author_facet Ahmed, Qamar Uddin
Sarian, Murni Nazira
Mat So'ad, Siti Zaiton
Latip, Jalifah
Arief Ichwan, Solachuddin Jauhari
Hussein, Nurlaili Najmie
Bakhtiar, M. Taher
Alhassan, Alhassan Muhammad
Hamidon, Hanisuhana
Fakurazi, Sharida
author_sort Ahmed, Qamar Uddin
title Methylation and acetylation enhanced the antidiabetic activity of some selected flavonoids: In vitro, molecular modelling and structure activity relationship based study
title_short Methylation and acetylation enhanced the antidiabetic activity of some selected flavonoids: In vitro, molecular modelling and structure activity relationship based study
title_full Methylation and acetylation enhanced the antidiabetic activity of some selected flavonoids: In vitro, molecular modelling and structure activity relationship based study
title_fullStr Methylation and acetylation enhanced the antidiabetic activity of some selected flavonoids: In vitro, molecular modelling and structure activity relationship based study
title_full_unstemmed Methylation and acetylation enhanced the antidiabetic activity of some selected flavonoids: In vitro, molecular modelling and structure activity relationship based study
title_sort methylation and acetylation enhanced the antidiabetic activity of some selected flavonoids: in vitro, molecular modelling and structure activity relationship based study
publisher MDPI
publishDate 2018
url http://irep.iium.edu.my/67823/7/67823%20Methylation%20and%20Acetylation%20Enhanced.pdf
http://irep.iium.edu.my/67823/8/67823%20Methylation%20and%20Acetylation%20Enhanced%20SCOPUS.pdf
http://irep.iium.edu.my/67823/19/67823%20Methylation%20and%20Acetylation%20Enhanced%20WOS.pdf
http://irep.iium.edu.my/67823/
https://www.mdpi.com/2218-273X/8/4/149
_version_ 1643619034250346496
score 13.211869

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