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

被引:134
作者
Lee, Ka-Heng [1 ]
Aziz, Farida Haryani Ab. [1 ]
Syahida, Ahmad [1 ,2 ]
Abas, Faridah [2 ,3 ]
Shaari, Khozirah [2 ,4 ]
Israf, Daud Ahmad [2 ,5 ]
Lajis, Nordin Haji [2 ,4 ]
机构
[1] Univ Putra Malaysia, Fac Biotechnol & Biomol Sci, Upm Serdang 43400, Selangor, Malaysia
[2] Univ Putra Malaysia, Inst Biosci, Upm Serdang 43400, Selangor, Malaysia
[3] Univ Putra Malaysia, Fac Food Sci & Technol, Upm Serdang 43400, Selangor, Malaysia
[4] Univ Putra Malaysia, Fac Sci, Upm Serdang 43400, Selangor, Malaysia
[5] Univ Putra Malaysia, Fac Med & Hlth Sci, Upm Serdang 43400, Selangor, Malaysia
关键词
Anti-inflammatory; Antioxidant; Anti-tyrosinase; Diarylpentanoids; iNOS; CHALCONE DERIVATIVES; OXIDE; INHIBITORS; DESIGN; AGENTS;
D O I
10.1016/j.ejmech.2009.03.020
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of 46 curcumin related diarylpentanoid analogues were synthesized and evaluated for their antiinflammatory, antioxidant and anti-tyrosinase activities. Among these compounds 2,13 and 33 exhibited potent NO inhibitory effect on IFN-gamma/LPS-activated RAW 264.7 cells as compared to L-NAME and curcumin. However, these series of diarylpentanoid analogues were not significantly inhibiting NO scavenging, total radical scavenging and tyrosinase enzyme activities. The results revealed that the biological activity of these diarylpentanoid analogues 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. (C) 2009 Elsevier Masson SAS. All rights reserved.
引用
收藏
页码:3195 / 3200
页数:6
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