The effect of methylation on the wogonin’s in vitro and in silico antidiabetic activity

Wogonin is one of the flavonoids that has been reported to exert antihyperglycemic effect against type 2 diabetes mellitus. However, the structure activity relationships (SAR) studies of wogonin against this disease have not been carried out. Hence, the objective of this study was to determine the e...

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Main Authors:	Sarian, Murni Nazira, Ahmed, Qamar Uddin, Alhassan, Alhassan Muhammad, Latip, Jalifah
Format:	Conference or Workshop Item
Language:	English English English
Published:	2018
Subjects:	Q Science (General)
Online Access:	http://irep.iium.edu.my/69003/ http://irep.iium.edu.my/69003/1/PRCO03_Murni_Qamar_2nd%20Abstract.pdf http://irep.iium.edu.my/69003/7/4IPRC.pdf http://irep.iium.edu.my/69003/12/69003_PRC%202018_CU%20Conference.pdf

id	iium-69003
recordtype	eprints
spelling	iium-690032018-12-28T04:28:50Z http://irep.iium.edu.my/69003/ The effect of methylation on the wogonin’s in vitro and in silico antidiabetic activity Sarian, Murni Nazira Ahmed, Qamar Uddin Alhassan, Alhassan Muhammad Latip, Jalifah Q Science (General) Wogonin is one of the flavonoids that has been reported to exert antihyperglycemic effect against type 2 diabetes mellitus. However, the structure activity relationships (SAR) studies of wogonin against this disease have not been carried out. Hence, the objective of this study was to determine the effect of methylation on wogonin and some structurally related flavonoids to recognize important positions responsible and their correlation. 13 chemical analogues of wogonin were selected and subjected to cytotoxicity test (MTT) on two different cell lines namely RIN-5F pancreatic and 3T3-L1 pre-adipocytes. Subsequently, the compounds were subjected to in vitro antidiabetic investigation using RIN-5F to determine the insulin secretagogue activity via ELISA as well as on 3T3-L1 adipocytes to determine the insulin sensitizing activity via adipogenesis and fluorescence glucose uptake tests. Next, the adipokines viz. leptin, tumor necrosis factor-α (TNF-α), adiponectin, and retinol binding protein-4 (RBP-4) were measured to investigate the biochemical reactions. Afterward, western blotting was performed to check GLUT4 and C-EBPα protein expressions. To further understand the mechanism, molecular docking study against GLUT1 receptor was executed. Results of in vitro antidiabetic (insulin secretion, adipogenesis, glucose uptake), and protein expression showed that the methyl ether group at position C-8 is responsible for wogonin’s antidiabetic capacity via glucose uptake and upregulation of GLUT4 and C/EBP-α. The results might prove worthy of developing semi-synthetic analogs that may retain substantial antidiabetic capacity. 2018-08-24 Conference or Workshop Item NonPeerReviewed application/pdf en http://irep.iium.edu.my/69003/1/PRCO03_Murni_Qamar_2nd%20Abstract.pdf application/pdf en http://irep.iium.edu.my/69003/7/4IPRC.pdf application/pdf en http://irep.iium.edu.my/69003/12/69003_PRC%202018_CU%20Conference.pdf Sarian, Murni Nazira and Ahmed, Qamar Uddin and Alhassan, Alhassan Muhammad and Latip, Jalifah (2018) The effect of methylation on the wogonin’s in vitro and in silico antidiabetic activity. In: 4th International Pharmaceutical Research Conference 2018, 25th-26th August 2018, Cyberjaya, Malaysia. (Unpublished)
repository_type	Digital Repository
institution_category	Local University
institution	International Islamic University Malaysia
building	IIUM Repository
collection	Online Access
language	English English English
topic	Q Science (General)
spellingShingle	Q Science (General) Sarian, Murni Nazira Ahmed, Qamar Uddin Alhassan, Alhassan Muhammad Latip, Jalifah The effect of methylation on the wogonin’s in vitro and in silico antidiabetic activity
description	Wogonin is one of the flavonoids that has been reported to exert antihyperglycemic effect against type 2 diabetes mellitus. However, the structure activity relationships (SAR) studies of wogonin against this disease have not been carried out. Hence, the objective of this study was to determine the effect of methylation on wogonin and some structurally related flavonoids to recognize important positions responsible and their correlation. 13 chemical analogues of wogonin were selected and subjected to cytotoxicity test (MTT) on two different cell lines namely RIN-5F pancreatic and 3T3-L1 pre-adipocytes. Subsequently, the compounds were subjected to in vitro antidiabetic investigation using RIN-5F to determine the insulin secretagogue activity via ELISA as well as on 3T3-L1 adipocytes to determine the insulin sensitizing activity via adipogenesis and fluorescence glucose uptake tests. Next, the adipokines viz. leptin, tumor necrosis factor-α (TNF-α), adiponectin, and retinol binding protein-4 (RBP-4) were measured to investigate the biochemical reactions. Afterward, western blotting was performed to check GLUT4 and C-EBPα protein expressions. To further understand the mechanism, molecular docking study against GLUT1 receptor was executed. Results of in vitro antidiabetic (insulin secretion, adipogenesis, glucose uptake), and protein expression showed that the methyl ether group at position C-8 is responsible for wogonin’s antidiabetic capacity via glucose uptake and upregulation of GLUT4 and C/EBP-α. The results might prove worthy of developing semi-synthetic analogs that may retain substantial antidiabetic capacity.
format	Conference or Workshop Item
author	Sarian, Murni Nazira Ahmed, Qamar Uddin Alhassan, Alhassan Muhammad Latip, Jalifah
author_facet	Sarian, Murni Nazira Ahmed, Qamar Uddin Alhassan, Alhassan Muhammad Latip, Jalifah
author_sort	Sarian, Murni Nazira
title	The effect of methylation on the wogonin’s in vitro and in silico antidiabetic activity
title_short	The effect of methylation on the wogonin’s in vitro and in silico antidiabetic activity
title_full	The effect of methylation on the wogonin’s in vitro and in silico antidiabetic activity
title_fullStr	The effect of methylation on the wogonin’s in vitro and in silico antidiabetic activity
title_full_unstemmed	The effect of methylation on the wogonin’s in vitro and in silico antidiabetic activity
title_sort	effect of methylation on the wogonin’s in vitro and in silico antidiabetic activity
publishDate	2018
url	http://irep.iium.edu.my/69003/ http://irep.iium.edu.my/69003/1/PRCO03_Murni_Qamar_2nd%20Abstract.pdf http://irep.iium.edu.my/69003/7/4IPRC.pdf http://irep.iium.edu.my/69003/12/69003_PRC%202018_CU%20Conference.pdf
first_indexed	2023-09-18T21:37:55Z
last_indexed	2023-09-18T21:37:55Z
_version_	1777412945480777728

The effect of methylation on the wogonin’s in vitro and in silico antidiabetic activity

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