Formylcolchicine bound to lactosaminated serum albumin is a more active antifibrotic agent than free colchicine

• Published in: Clinica chimica acta Vol. 254; no. 2; pp. 149 - 157
• Main Authors: Palmerini, C.A., Saccardi, C., Floridi, A., Arienti, G.
• Format: Journal Article
• Language: English
• Published: Shannon Elsevier B.V 29.10.1996; Elsevier
• Subjects: Amino Sugars - metabolism; Animals; Biological and medical sciences; Carbon tetrachloride; Carbon Tetrachloride - toxicity; Colchicine; Colchicine - analogs & derivatives; Colchicine - metabolism; Colchicine - therapeutic use; Digestive system; Formylated colchicine; Hydroxyproline; Lactosaminated serum albumin; Liver Cirrhosis, Experimental - chemically induced; Liver Cirrhosis, Experimental - drug therapy; Liver Cirrhosis, Experimental - pathology; Liver fibrosis; Male; Medical sciences; Pharmacology. Drug treatments; Protein Binding; Rats; Rats, Sprague-Dawley; Serum Albumin - metabolism; Colchicine; Liver fibrosis; Lactosaminated serum albumin; Carbon tetrachloride; Hydroxyproline; Formylated colchicine; Rat; Treatment efficiency; Liver; Rodentia; Hepatic disease; Vertebrata; Experimental disease; Mammalia; Structure activity relation; Animal; Fibrosis; Digestive diseases; Poisoning; Formylation; Comparative study
• ISSN: 0009-8981; 1873-3492
• DOI: 10.1016/0009-8981(96)06381-4

Liver fibrosis was induced by chronically (7 weeks) administering CCl 4, to rats. Animals were divided into four groups: (a) controls, (b) treated with CCI, alone, (c) treated with CCl 4 and colchicine and (d) treated with CCl 4 and formyl-colchicine bound to lactosaminated serum albumin (FC-LASA). Liver dysfunction was monitored by biochemical tests (alkaline phosphatase [ALP], γ-glutamyltransferase [γGT], aspartate and alanine transaminases [AST and ALT], albumin and total bilirubin). Fibrosis was evaluated by determining hydroxyproline and by microscopic examination. The exposure to CCl 4 produced major alterations of liver structure and collagen deposition. These effects were partially counteracted by colchicine and to a greater extent by FC-LASA. Morphological findings paralleled biochemical data. The information reported here indicates that colchicine has an antifibrotic activity on the liver of intoxicated rats and that FC-LASA is more active than colchicine itself as an antifibrotic agent.