Synthesis and anti-inflammatory activities of mono-carbonyl analogues of curcumin.
Curcumin has been extensively studied for its anti-inflammatory activities. However, its potential beneficial effects on various disease preventions and treatments are limited by its unstable structure. The beta-diketone moiety renders curcumin to be rapidly metabolized by aldo-keto reductase in liver. In the present study, a series of curcumin analogues with more stable chemical structures were synthesized and several compounds showed an enhanced ability to inhibit lipopolysaccharide (LPS)-induced TNF-alpha and IL-6 synthesis in macrophages.
Liang
Guang
G
College of Pharmacy, Wenzhou Medical College, Wenzhou, Zhejiang 325035, PR China.
Li
Xiaokun
X
Chen
Li
L
Yang
Shulin
S
Wu
Xudong
X
Studer
Elaine
E
Gurley
Emily
E
Hylemon
Phillip B
PB
Ye
Faqing
F
Li
Yueru
Y
Zhou
Huiping
H
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis* / Q000494:pharmacology*; D003474:Curcumin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology*; D003512:Cyclohexanones / Q000138:chemical synthesis / Q000494:pharmacology; D003517:Cyclopentanes / Q000138:chemical synthesis / Q000494:pharmacology; D015850:Interleukin-6 / Q000096:biosynthesis; D008070:Lipopolysaccharides / Q000037:antagonists & inhibitors / Q000494:pharmacology; D008264:Macrophages / Q000187:drug effects / Q000276:immunology; D051379:Mice; D014409:Tumor Necrosis Factor-alpha / Q000096:biosynthesis
D000894:Anti-Inflammatory Agents, Non-Steroidal; D003512:Cyclohexanones; D003517:Cyclopentanes; D015850:Interleukin-6; D008070:Lipopolysaccharides; D014409:Tumor Necrosis Factor-alpha; C007201:cyclopentanone; D003474:Curcumin