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.
Faculty of Biotechnology and Biomolecular Sciences, Universiti Putra Malaysia, UPM Serdang, Selangor, Malaysia.
Ka-Heng
KH
Lee
Farida Haryani
FH
Ab Aziz
Ahmad
A
Syahida
Faridah
F
Abas
Khozirah
K
Shaari
Daud Ahmad
DA
Israf
Nordin Haji
NH
Lajis
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