title: Synthesis and evaluation of chalcone derivatives as inhibitors of neutrophils' chemotaxis, phagocytosis and production of reactive oxygen species.
abstract: Inhibitory effects on neutrophils' chemotaxis, phagocytosis and production of reactive oxygen species (ROS) are among the important targets in developing anti-inflammatory agents and immunosuppressants. Eight series of chalcone derivatives including five newly synthesized series were assessed for their inhibitory effects on chemotaxis, phagocytosis and ROS production in human polymorphonuclear neutrophils (PMNs). Inhibition of PMNs' chemotaxis and phagocytosis abilities were investigated using the Boyden chamber technique and the Phagotest kit, respectively, while ROS production was evaluated using luminol- and lucigenin-based chemiluminescence assay. The new derivatives (4d and 8d), which contain 4-methylaminoethanol functional group were active in all the assays performed. It was also observed that some of the compounds were active in inhibiting chemotaxis while others suppressed phagocytosis and ROS production. The information obtained gave new insight into chalcone derivatives with the potential to be developed as immunomodulators.
authors.affiliation: Drugs and Herbal Research Centre, Faculty of Pharmacy, Universiti Kebangsaan Malaysia, Jalan Raja Muda Abd. Aziz, 50300, Kuala Lumpur, Malaysia.
authors.forename: Syed N A
authors.initials: SN
authors.lastname: Bukhari
authors.forename: Yasmin
authors.initials: Y
authors.lastname: Tajuddin
authors.forename: Vannessa J
authors.initials: VJ
authors.lastname: Benedict
authors.forename: Kok W
authors.initials: KW
authors.lastname: Lam
authors.forename: Ibrahim
authors.initials: I
authors.lastname: Jantan
authors.forename: Juriyati
authors.initials: J
authors.lastname: Jalil
authors.forename: Malina
authors.initials: M
authors.lastname: Jasamai
mesh_terms: D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis / Q000494:pharmacology; D002470:Cell Survival / Q000187:drug effects; D002599:Chalcone / Q000138:chemical synthesis / Q000494:pharmacology; D002634:Chemotaxis, Leukocyte / Q000187:drug effects*; D004983:Ethanolamines / Q000737:chemistry; D006801:Humans; D007166:Immunosuppressive Agents / Q000138:chemical synthesis / Q000494:pharmacology; D009504:Neutrophils / Q000187:drug effects / Q000276:immunology / Q000378:metabolism; D010587:Phagocytosis / Q000187:drug effects*; D017382:Reactive Oxygen Species / Q000378:metabolism*; D013329:Structure-Activity Relationship
chemical_list: D000893:Anti-Inflammatory Agents; D004983:Ethanolamines; D007166:Immunosuppressive Agents; D017382:Reactive Oxygen Species; D002599:Chalcone
keywords: chalcones; chemotaxis; inhibitors; phagocytosis; reactive oxygen species; structure-activity relationship