title: Evaluation of the in vivo anti-inflammatory and analgesic activity of a highly water-soluble aspirin conjugate.
abstract: Glucose-aspirin (GA) was synthesized by conjugating aspirin (ASA) to the 3-carbon of glucose to produce a stable water-soluble aspirin derivative. The in vivo activities were compared with those of aspirin. The mouse tail flick assay showed that at 120 min., both aspirin and GA showed the maximum possible effect, and the higher dose (200 mg/kg) generally had less of an effect than the lower dose (100 mg/kg). Per cent inhibition of paw oedema was 63% and 69% for ASA and GA at 100 mg/kg, respectively. In the tail immersion test, the increase in reaction time was significantly greater with GA as compared to aspirin (100 mg/kg) at 60 min. In conclusion, there was significant anti-inflammatory and analgesic activity for GA at the doses studied under the experimental conditions.
authors.affiliation: Organomed Corporation, Coventry, RI 02816, USA. info@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
mesh_terms: D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D001241:Aspirin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D002351:Carrageenan / Q000494:pharmacology; D004195:Disease Models, Animal; D004305:Dose-Response Relationship, Drug; D004487:Edema / Q000188:drug therapy; D005960:Glucosides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D006868:Hydrolysis; D051379:Mice; D015394:Molecular Structure; D017288:Pain Threshold / Q000187:drug effects; D051381:Rats; D012995:Solubility; D014867:Water / Q000737:chemistry*
chemical_list: C582668:3-O-(2'-acetoxy)benzoyl-2-glucopyranose; D000894:Anti-Inflammatory Agents, Non-Steroidal; D005960:Glucosides; D014867:Water; D002351:Carrageenan; D001241:Aspirin