Potential antipsoriatic avarol derivatives as antioxidants and inhibitors of PGE(2) generation and proliferation in the HaCaT cell line.
J Nat Prod
; 67(9): 1459-63, 2004 Sep.
Article
in En
| MEDLINE
| ID: mdl-15387642
ABSTRACT
The synthesis and structure-activity relationships for a series of 14 new avarol derivatives as antioxidants and inhibitors of cell proliferation and PGE(2) generation in human keratinocytes are described. Compound 6 (thiosalicylic derivative) was the most potent inhibitor of superoxide generation in human neutrophils and also potently inhibited PGE(2) generation in the human keratinocyte HaCaT cell line. Compound 7(3'-methylaminoavarone) presented the best antiproliferative profile, by the inhibition of (3)H-thymidine incorporation in HaCaT cells, with potency similar to the reference compound anthralin. None of the avarol derivatives showed any sign of cytotoxicity measured as LDH release in treated keratinocytes. The potency and pharmacological profile of derivatives are also discussed.
Search on Google
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Sesquiterpenes
/
Dinoprostone
/
Salicylates
/
Free Radical Scavengers
/
Antioxidants
Limits:
Humans
Country/Region as subject:
Europa
Language:
En
Journal:
J Nat Prod
Year:
2004
Document type:
Article
Affiliation country:
Spain