title: Evaluation of the in vivo anti-inflammatory and analgesic and in vitro anti-cancer activities of curcumin and its derivatives.
abstract: Curcumin, obtained from turmeric, has several biological properties to make it a desirable template for drug development. A lipophilic derivative of curcumin, diacetyl curcumin (DAC) and a hydrophilic derivative, diglutaryl curcumin (DGC) were synthesized and their in vivo analgesic and anti-inflammatory activities were compared with those of curcumin and aspirin. The in vitro anti-cancer activities of curcumin and the two derivatives against three cell cancer lines were compared with those against a non-cancerous cell line. The inhibitory effects were comparable to each other and nearing that of curcumin while they showed low inhibitory effect towards the non-cancerous cell line. The mouse tail flick assay showed that curcumin, DAC and DGC increased latency time. DGC was most effective as an analgesic, even more so than aspirin. The maximum percentage effect (MPE) was highest with DGC at 3 hours. The carrageenan induced paw edema model indicated anti-inflammatory activity of all three curcumin formulations. The percentage inhibition of paw edema was maximum for DAC, followed by aspirin and curcumin.
authors.affiliation: Department of Medicinal Chemistry, Organomed Corporation, 11 Grandview St., Unit 8, Coventry, RI 02816, USA. Jacob@organomed.com
authors.forename: James N
authors.initials: JN
authors.lastname: Jacob
authors.forename: Dinesh K
authors.initials: DK
authors.lastname: Badyal
authors.forename: Suman
authors.initials: S
authors.lastname: Bala
authors.forename: Masoud
authors.initials: M
authors.lastname: Toloue
mesh_terms: D000700:Analgesics / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use*; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use*; D001241:Aspirin / Q000494:pharmacology / Q000627:therapeutic use; D002460:Cell Line; D045744:Cell Line, Tumor; D003474:Curcumin / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use*; D004487:Edema / Q000188:drug therapy; D006801:Humans; D051379:Mice; D051381:Rats
chemical_list: D000700:Analgesics; D000893:Anti-Inflammatory Agents; D003474:Curcumin; D001241:Aspirin