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Anti-inflammatory activity of sesquiterpene lactones and related compounds.

Abstract
Some sesquiterpene lactones and related compounds were tested for anti-inflammatory activity in rodents. In the edema-induced carrageenan inflammation screen, the alpha-methylene-gamma-lactone moiety of the sesquiterpene lactones was required for inhibitory activity. The 6-hydroxy group of helenalin also was required for potency. In the tenulin series, the 2,3-epoxy derivatives were marginally active. The same structure was required for inhibition of the writhing reflex. In the chronic adjuvant arthritic screen, compounds containing the alpha-methylene-gamma-lactone moiety, the beta-unsubstituted cyclopentenone ring, and the alpha-epoxy cyclopentenone system afforded significant inhibition at 2.5 mg/kg/day. The sesquiterpene lactones were marginally effective against induced pleurisy. The delayed hypersensitivity was suppressed by these agents whereas immunoglobulin synthesis was slightly stimulated. No delerious side effects were observed with these agents from the limited tests performed.
AuthorsI H Hall, K H Lee, C O Starnes, Y Sumida, R Y Wu, T G Waddell, J W Cochran, K G Gerhart
JournalJournal of pharmaceutical sciences (J Pharm Sci) Vol. 68 Issue 5 Pg. 537-42 (May 1979) ISSN: 0022-3549 [Print] United States
PMID311831 (Publication Type: Journal Article, Research Support, U.S. Gov't, P.H.S.)
Chemical References
  • Anti-Inflammatory Agents
  • Anti-Inflammatory Agents, Non-Steroidal
  • Lactones
  • Mitogens
  • Sesquiterpenes
  • Teratogens
Topics
  • Anaphylaxis (physiopathology)
  • Animals
  • Anti-Inflammatory Agents
  • Anti-Inflammatory Agents, Non-Steroidal
  • Antibody Formation (drug effects)
  • Arthritis, Experimental (physiopathology)
  • Edema (physiopathology)
  • Female
  • Fertility (drug effects)
  • Hypersensitivity, Delayed (physiopathology)
  • Lactones (pharmacology)
  • Male
  • Mice
  • Mitogens
  • Passive Cutaneous Anaphylaxis (drug effects)
  • Pleurisy (physiopathology)
  • Pregnancy
  • Rats
  • Sesquiterpenes (pharmacology)
  • Structure-Activity Relationship
  • Teratogens

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