Document Detail

Heterocyclic derivatives of all-trans retinoic acid: in vitro effects on fibroblast/keratinocyte growth and differentiation, and in vivo effects on guinea-pig skin.
MedLine Citation:
PMID:  10488685     Owner:  NLM     Status:  MEDLINE    
We investigated the biological effects of five all-trans retinoic acid derivatives, bearing heterocyclic ring systems in the side chain. Growth assays performed on submerged human fibroblast and keratinocyte cultures revealed that (E)4-[2-(5-terbuthyl-thiophen-2-yl)propenyl]benzoic acid (compound 5) is the best compound among the studied derivatives for it exhibits a weaker antiproliferative activity and induces, like all-trans retinoic acid does, a significant increase in fibroblast and keratinocyte growth. The morphological and morphometrical analyses of submerged human fibroblast cultures and human epidermis reconstructed in vitro showed that the compound 5 behaves similarly to all-trans retinoic acid: it induces a decrease in all the cell parameters of submerged fibroblast cultures, and modulates the differentiation of keratinocytes in in vitro reconstructed epidermis. Compound 5 induces thickening of epidermis in vivo, one of the most remarkable pharmacological effects of retinoids on skin, but compared to all-trans retinoic acid, it induces a weaker irritation on guinea-pig skin in terms of both erythema and scaling. Compound 5 could then represent a promising candidate for the treatment of certain dermatological diseases.
P P Parnigotto; M T Conconi; C Bortoletto; S Manfredini; F Montesi; M Schiavon; F M Cancellotti
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Pharmacology & toxicology     Volume:  85     ISSN:  0901-9928     ISO Abbreviation:  Pharmacol. Toxicol.     Publication Date:  1999 Aug 
Date Detail:
Created Date:  1999-10-27     Completed Date:  1999-10-27     Revised Date:  2005-11-17    
Medline Journal Info:
Nlm Unique ID:  8702180     Medline TA:  Pharmacol Toxicol     Country:  DENMARK    
Other Details:
Languages:  eng     Pagination:  49-55     Citation Subset:  IM    
Interdepartmental Centre for the Study of Keratinocytes: Pharmaceutical and Clinical Applications, University of Padua, Italy.
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MeSH Terms
Cell Differentiation / drug effects
Child, Preschool
Coloring Agents
Fibroblasts / drug effects,  ultrastructure
Fluorescent Antibody Technique
Guinea Pigs
Heterocyclic Compounds / pharmacology*
Keratinocytes / drug effects*,  ultrastructure
Keratolytic Agents / pharmacology*
Skin / cytology*,  drug effects,  growth & development*,  ultrastructure
Tetrazolium Salts
Tretinoin / analogs & derivatives*,  pharmacology*
Reg. No./Substance:
0/Coloring Agents; 0/Heterocyclic Compounds; 0/Keratolytic Agents; 0/Tetrazolium Salts; 0/Thiazoles; 298-93-1/thiazolyl blue; 302-79-4/Tretinoin

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