Synthesis and biological evaluation of curcumin-like diarylpentanoid analogues for anti-inflammatory, antioxidant and anti-tyrosinase activities

A series of 46 curcumin related diarylpentanoidanalogues were synthesized and evaluated for their anti-inflammatory, antioxidant and anti-tyrosinaseactivities. Among these compounds 2, 13 and 33 exhibited potent NO inhibitory effect on IFN-γ/LPS-activated RAW 264.7 cells as compared to l-NAME and cu...

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Main Authors: Ka-Heng, Lee, Ab. Aziz, Farida Haryani, Ahmad, Syahida, Abas, Faridah, Shaari, Khozirah, Israf Ali, Daud Ahmad, Lajis, Nordin
Format: Article
Language:English
English
Published: Elsevier 2009
Subjects:
Online Access:http://psasir.upm.edu.my/id/eprint/16920/
http://psasir.upm.edu.my/id/eprint/16920/1/Synthesis%20and%20biological%20evaluation%20of%20curcumin.pdf
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author Ka-Heng, Lee
Ab. Aziz, Farida Haryani
Ahmad, Syahida
Abas, Faridah
Shaari, Khozirah
Israf Ali, Daud Ahmad
Lajis, Nordin
author_facet Ka-Heng, Lee
Ab. Aziz, Farida Haryani
Ahmad, Syahida
Abas, Faridah
Shaari, Khozirah
Israf Ali, Daud Ahmad
Lajis, Nordin
author_sort Ka-Heng, Lee
building UPM Institutional Repository
collection Online Access
description A series of 46 curcumin related diarylpentanoidanalogues were synthesized and evaluated for their anti-inflammatory, antioxidant and anti-tyrosinaseactivities. Among these compounds 2, 13 and 33 exhibited potent NO inhibitory effect on IFN-γ/LPS-activated RAW 264.7 cells as compared to l-NAME and curcumin. However, these series of diarylpentanoidanalogues were not significantly inhibiting NO scavenging, total radical scavenging and tyrosinase enzyme activities. The results revealed that the biologicalactivity of these diarylpentanoidanalogues is most likely due to their action mainly upon inflammatory mediator, inducible nitric oxide synthase (iNOS). The present results showed that compounds 2, 13 and 33 might serve as a useful starting point for the design of improved anti-inflammatory agents.
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spelling upm-169202015-09-28T00:56:48Z http://psasir.upm.edu.my/id/eprint/16920/ Synthesis and biological evaluation of curcumin-like diarylpentanoid analogues for anti-inflammatory, antioxidant and anti-tyrosinase activities Ka-Heng, Lee Ab. Aziz, Farida Haryani Ahmad, Syahida Abas, Faridah Shaari, Khozirah Israf Ali, Daud Ahmad Lajis, Nordin A series of 46 curcumin related diarylpentanoidanalogues were synthesized and evaluated for their anti-inflammatory, antioxidant and anti-tyrosinaseactivities. Among these compounds 2, 13 and 33 exhibited potent NO inhibitory effect on IFN-γ/LPS-activated RAW 264.7 cells as compared to l-NAME and curcumin. However, these series of diarylpentanoidanalogues were not significantly inhibiting NO scavenging, total radical scavenging and tyrosinase enzyme activities. The results revealed that the biologicalactivity of these diarylpentanoidanalogues is most likely due to their action mainly upon inflammatory mediator, inducible nitric oxide synthase (iNOS). The present results showed that compounds 2, 13 and 33 might serve as a useful starting point for the design of improved anti-inflammatory agents. Elsevier 2009-08 Article PeerReviewed application/pdf en http://psasir.upm.edu.my/id/eprint/16920/1/Synthesis%20and%20biological%20evaluation%20of%20curcumin.pdf Ka-Heng, Lee and Ab. Aziz, Farida Haryani and Ahmad, Syahida and Abas, Faridah and Shaari, Khozirah and Israf Ali, Daud Ahmad and Lajis, Nordin (2009) Synthesis and biological evaluation of curcumin-like diarylpentanoid analogues for anti-inflammatory, antioxidant and anti-tyrosinase activities. European Journal of Medicinal Chemistry, 44 (8). pp. 3195-3200. ISSN 0223-5234 Anti-inflammatory agents Antioxidants 10.1016/j.ejmech.2009.03.020 English
spellingShingle Anti-inflammatory agents
Antioxidants
Ka-Heng, Lee
Ab. Aziz, Farida Haryani
Ahmad, Syahida
Abas, Faridah
Shaari, Khozirah
Israf Ali, Daud Ahmad
Lajis, Nordin
Synthesis and biological evaluation of curcumin-like diarylpentanoid analogues for anti-inflammatory, antioxidant and anti-tyrosinase activities
title Synthesis and biological evaluation of curcumin-like diarylpentanoid analogues for anti-inflammatory, antioxidant and anti-tyrosinase activities
title_full Synthesis and biological evaluation of curcumin-like diarylpentanoid analogues for anti-inflammatory, antioxidant and anti-tyrosinase activities
title_fullStr Synthesis and biological evaluation of curcumin-like diarylpentanoid analogues for anti-inflammatory, antioxidant and anti-tyrosinase activities
title_full_unstemmed Synthesis and biological evaluation of curcumin-like diarylpentanoid analogues for anti-inflammatory, antioxidant and anti-tyrosinase activities
title_short Synthesis and biological evaluation of curcumin-like diarylpentanoid analogues for anti-inflammatory, antioxidant and anti-tyrosinase activities
title_sort synthesis and biological evaluation of curcumin-like diarylpentanoid analogues for anti-inflammatory, antioxidant and anti-tyrosinase activities
topic Anti-inflammatory agents
Antioxidants
url http://psasir.upm.edu.my/id/eprint/16920/
http://psasir.upm.edu.my/id/eprint/16920/
http://psasir.upm.edu.my/id/eprint/16920/1/Synthesis%20and%20biological%20evaluation%20of%20curcumin.pdf