Synthesis and biological evaluation of curcumin-like diarylpentanoid analogues for anti-inflammatory, antioxidant and anti-tyrosinase activities.
A series of 46 curcumin related diarylpentanoid analogues were synthesized and evaluated for their anti-inflammatory, 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.
Lee
Ka-Heng
KH
Faculty of Biotechnology and Biomolecular Sciences, Universiti Putra Malaysia, UPM Serdang, Selangor, Malaysia.
Ab Aziz
Farida Haryani
FH
Syahida
Ahmad
A
Abas
Faridah
F
Shaari
Khozirah
K
Israf
Daud Ahmad
DA
Lajis
Nordin Haji
NH
D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001713:Biphenyl Compounds / Q000378:metabolism; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D003474:Curcumin / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015195:Drug Design; D005029:Ethylenediamines; D016166:Free Radical Scavengers / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D020128:Inhibitory Concentration 50; D014442:Monophenol Monooxygenase / Q000037:antagonists & inhibitors*; D009569:Nitric Oxide / Q000096:biosynthesis / Q000378:metabolism; D010851:Picrates / Q000378:metabolism; D013424:Sulfanilamides
D000893:Anti-Inflammatory Agents; D001713:Biphenyl Compounds; D005029:Ethylenediamines; D016166:Free Radical Scavengers; C095000:Griess reagent; D010851:Picrates; D013424:Sulfanilamides; D009569:Nitric Oxide; C004931:1,1-diphenyl-2-picrylhydrazyl; D014442:Monophenol Monooxygenase; D003474:Curcumin