Heterocyclic Derivatives ofall-transRetinoic Acid:in vitroEffects on Fibroblast/Keratinocyte Growth and Differentiation, andin vivoEffects on Guinea-Pig Skin
| Autor: | Chiara Bortoletto, Francesco Maria Cancellotti, Maria Teresa Conconi, Stefano Manfredini, Mariano Schiavon, Pier Paolo Parnigotto, Francesco Montesi |
|---|---|
| Rok vydání: | 1999 |
| Předmět: |
Keratinocytes
Health Toxicology and Mutagenesis Guinea Pigs Cell Retinoic acid Fluorescent Antibody Technique Tetrazolium Salts Tretinoin X-RECEPTOR VITAMIN-A EPIDERMAL-KERATINOCYTES INDUCTION CELLS TRANSGLUTAMINASE DERMATOLOGY TRETINOIN APOPTOSIS INVITRO Biology Toxicology chemistry.chemical_compound Keratolytic Agents Isomerism Heterocyclic Compounds In vivo medicine Animals Humans Coloring Agents Fibroblast Skin Benzoic acid Pharmacology VITAMIN-A INVITRO Epidermis (botany) INDUCTION Infant EPIDERMAL-KERATINOCYTES Cell Differentiation Fibroblasts X-RECEPTOR Molecular biology In vitro APOPTOSIS Thiazoles medicine.anatomical_structure Biochemistry chemistry Child Preschool CELLS TRANSGLUTAMINASE DERMATOLOGY Keratinocyte |
| Zdroj: | Pharmacology & Toxicology. 85:49-55 |
| ISSN: | 1600-0773 0901-9928 |
| DOI: | 10.1111/j.1600-0773.1999.tb00066.x |
| Popis: | 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 exibits 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. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Plný text