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Effects of curcumin analogue, 2, 6-bis (2, 5-dimethoxybenzylidene) cyclohexanone (BDMC33) on the activities of drug-metabolizing enzymes in cultured Caco-2 cell model

Poor systemic delivery of curcumin outside the gut due to its rapid metabolism has severely limited its application to many chronic diseases. Previously, our research group synthesized curcumin analogues 2, 6-bis (2, 5-dimethoxybenzylidene) cyclohexanone (BDMC33) that has potent anti-inflammatory ac...

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Main Authors: Yakubu, Ndatsu, Ahmad, Syahida, Abas, Faridah, Mohammed, Umaru Alhassan
Format: Article
Language:English
Published: International Journal of Pharmaceutical Sciences and Drug Research 2016
Online Access:http://psasir.upm.edu.my/id/eprint/54083/1/Effects%20of%20curcumin%20analogue.pdf
http://psasir.upm.edu.my/id/eprint/54083/
http://ijpsdr.com/IJPSDR.2016.8.1.9
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spelling my.upm.eprints.540832018-02-27T09:16:28Z http://psasir.upm.edu.my/id/eprint/54083/ Effects of curcumin analogue, 2, 6-bis (2, 5-dimethoxybenzylidene) cyclohexanone (BDMC33) on the activities of drug-metabolizing enzymes in cultured Caco-2 cell model Yakubu, Ndatsu Ahmad, Syahida Abas, Faridah Mohammed, Umaru Alhassan Poor systemic delivery of curcumin outside the gut due to its rapid metabolism has severely limited its application to many chronic diseases. Previously, our research group synthesized curcumin analogues 2, 6-bis (2, 5-dimethoxybenzylidene) cyclohexanone (BDMC33) that has potent anti-inflammatory activities. Therefore, the aim of this study is to evaluate the effects of curcumin analog (BDMC33) on the activities of drug metabolizing enzymes in Caco-2 cells, which was compared with that of curcumin and 3-(2-Fluoro-benzylidene)-5-(2-fluorocyclohexylmethylene)-piperidin-4-one (EF-24). BDMC-33 was synthesized through the appropriate reaction of the aromatic aldehyde with cyclohexanone, under base catalyzed aldol condensation, at the ratio of ketone: aldehyde (1:2). Activity of drug metabolizing enzymes such as NADPH-cytochrome p450 reductase (CPR), UDP-glucuronosyltransferase (UGT), glutathione-S-transferase (GST) and Sulfotransferase (SULT) in Caco-2 cells were evaluated upon exposure to 50µM of BDMC33, curcumin, and EF-24, separately, for 4 hours. The BDMC33, EF-24, and curcumin treatments did not affect the activities of UGT, GST, SULT, and CPR in respect to their controls (29.45, 27.18, 23.64 and 2.08µmol/mg), respectively, at all periods of incubation. Hence, BDMC33 was able to maintain the activities of both phases I and II drug metabolizing enzymes, and therefore it could be a potential lead, anti-inflammatory agents. International Journal of Pharmaceutical Sciences and Drug Research 2016 Article PeerReviewed text en http://psasir.upm.edu.my/id/eprint/54083/1/Effects%20of%20curcumin%20analogue.pdf Yakubu, Ndatsu and Ahmad, Syahida and Abas, Faridah and Mohammed, Umaru Alhassan (2016) Effects of curcumin analogue, 2, 6-bis (2, 5-dimethoxybenzylidene) cyclohexanone (BDMC33) on the activities of drug-metabolizing enzymes in cultured Caco-2 cell model. International Journal of Pharmaceutical Sciences and Drug Research, 8 (1). pp. 57-64. ISSN 0975-248X http://ijpsdr.com/IJPSDR.2016.8.1.9
institution Universiti Putra Malaysia
building UPM Library
collection Institutional Repository
continent Asia
country Malaysia
content_provider Universiti Putra Malaysia
content_source UPM Institutional Repository
url_provider http://psasir.upm.edu.my/
language English
description Poor systemic delivery of curcumin outside the gut due to its rapid metabolism has severely limited its application to many chronic diseases. Previously, our research group synthesized curcumin analogues 2, 6-bis (2, 5-dimethoxybenzylidene) cyclohexanone (BDMC33) that has potent anti-inflammatory activities. Therefore, the aim of this study is to evaluate the effects of curcumin analog (BDMC33) on the activities of drug metabolizing enzymes in Caco-2 cells, which was compared with that of curcumin and 3-(2-Fluoro-benzylidene)-5-(2-fluorocyclohexylmethylene)-piperidin-4-one (EF-24). BDMC-33 was synthesized through the appropriate reaction of the aromatic aldehyde with cyclohexanone, under base catalyzed aldol condensation, at the ratio of ketone: aldehyde (1:2). Activity of drug metabolizing enzymes such as NADPH-cytochrome p450 reductase (CPR), UDP-glucuronosyltransferase (UGT), glutathione-S-transferase (GST) and Sulfotransferase (SULT) in Caco-2 cells were evaluated upon exposure to 50µM of BDMC33, curcumin, and EF-24, separately, for 4 hours. The BDMC33, EF-24, and curcumin treatments did not affect the activities of UGT, GST, SULT, and CPR in respect to their controls (29.45, 27.18, 23.64 and 2.08µmol/mg), respectively, at all periods of incubation. Hence, BDMC33 was able to maintain the activities of both phases I and II drug metabolizing enzymes, and therefore it could be a potential lead, anti-inflammatory agents.
format Article
author Yakubu, Ndatsu
Ahmad, Syahida
Abas, Faridah
Mohammed, Umaru Alhassan
spellingShingle Yakubu, Ndatsu
Ahmad, Syahida
Abas, Faridah
Mohammed, Umaru Alhassan
Effects of curcumin analogue, 2, 6-bis (2, 5-dimethoxybenzylidene) cyclohexanone (BDMC33) on the activities of drug-metabolizing enzymes in cultured Caco-2 cell model
author_facet Yakubu, Ndatsu
Ahmad, Syahida
Abas, Faridah
Mohammed, Umaru Alhassan
author_sort Yakubu, Ndatsu
title Effects of curcumin analogue, 2, 6-bis (2, 5-dimethoxybenzylidene) cyclohexanone (BDMC33) on the activities of drug-metabolizing enzymes in cultured Caco-2 cell model
title_short Effects of curcumin analogue, 2, 6-bis (2, 5-dimethoxybenzylidene) cyclohexanone (BDMC33) on the activities of drug-metabolizing enzymes in cultured Caco-2 cell model
title_full Effects of curcumin analogue, 2, 6-bis (2, 5-dimethoxybenzylidene) cyclohexanone (BDMC33) on the activities of drug-metabolizing enzymes in cultured Caco-2 cell model
title_fullStr Effects of curcumin analogue, 2, 6-bis (2, 5-dimethoxybenzylidene) cyclohexanone (BDMC33) on the activities of drug-metabolizing enzymes in cultured Caco-2 cell model
title_full_unstemmed Effects of curcumin analogue, 2, 6-bis (2, 5-dimethoxybenzylidene) cyclohexanone (BDMC33) on the activities of drug-metabolizing enzymes in cultured Caco-2 cell model
title_sort effects of curcumin analogue, 2, 6-bis (2, 5-dimethoxybenzylidene) cyclohexanone (bdmc33) on the activities of drug-metabolizing enzymes in cultured caco-2 cell model
publisher International Journal of Pharmaceutical Sciences and Drug Research
publishDate 2016
url http://psasir.upm.edu.my/id/eprint/54083/1/Effects%20of%20curcumin%20analogue.pdf
http://psasir.upm.edu.my/id/eprint/54083/
http://ijpsdr.com/IJPSDR.2016.8.1.9
_version_ 1643835560217804800
score 13.211869

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