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In search of safe pain relief: The analgesic and anti-inflammatory activity of phytosteryl ibuprofenates.
- Source :
-
Steroids [Steroids] 2019 Sep; Vol. 149, pp. 108420. Date of Electronic Publication: 2019 May 31. - Publication Year :
- 2019
-
Abstract
- β-Sitosteryl (S)-ibuprofenate (2), stigmasteryl (S)-ibuprofenate (3), ergosteryl (S)-ibuprofenate (4), and cholesteryl (S)-ibuprofenate (5) were prepared in 70-75% yields by Steglich esterification and were characterized by 1D and 2D NMR, as well as by MS. The new esters were evaluated in in vivo pain models of antinociception and anti-inflammation using the writhing, formalin, and carrageenan tests, in mice and rats, and the results were compared with those of (S)-ibuprofen (1). Damage to the gastric mucosa of animals was also assessed. The results indicated that 2-5 have comparable or eventually better activity than 1 at the same mg/kg doses. Since the molecular weight ratio of esters 2-5 to ibuprofen is about 3-1, the amount of truly incorporated ibuprofen was roughly one third to achieve similar effects. This resulted in minimal gastrointestinal damage in the stomach of the animals, in contrast to the large gastric injury caused by (S)-ibuprofen.<br /> (Copyright © 2019 Elsevier Inc. All rights reserved.)
- Subjects :
- Analgesics adverse effects
Analgesics therapeutic use
Animals
Anti-Inflammatory Agents, Non-Steroidal adverse effects
Anti-Inflammatory Agents, Non-Steroidal therapeutic use
Ibuprofen adverse effects
Ibuprofen therapeutic use
Mice
Analgesics chemistry
Analgesics pharmacology
Anti-Inflammatory Agents, Non-Steroidal chemistry
Anti-Inflammatory Agents, Non-Steroidal pharmacology
Ibuprofen chemistry
Ibuprofen pharmacology
Pain drug therapy
Subjects
Details
- Language :
- English
- ISSN :
- 1878-5867
- Volume :
- 149
- Database :
- MEDLINE
- Journal :
- Steroids
- Publication Type :
- Academic Journal
- Accession number :
- 31153933
- Full Text :
- https://doi.org/10.1016/j.steroids.2019.05.012