Derivatives of colchicine preferentially taken up by the liver: an approach to the treatment of liver fibrosis.
The distribution in the mouse of colchicine and of two colchicine derivatives, namely formylcolchicine/formylated serum albumin (FC/FTSA) and formylcolchicine/lactosaminated serum albumin (FC/LASA), was studied. The presence of radioactivity after the intravenous injection of labelled colchicine or of its derivatives was determined in liver, small intestine, kidney and blood. The radioactivity of the derivatives was better retained than that of colchicine. The derivatives accumulated in the liver to a much greater extent than colchicine, but were scarcely present in the gut. Tropism towards the liver might be important for the use of FC/LASA and FC/FTSA to control liver fibrosis.
Palmerini
C A
CA
Dipartimento di Biologia Cellular e Molecolare, Università di Perugia, Italy.
Floridi
A
A
Arienti
G
G
D000818:Animals; D003078:Colchicine / Q000031:analogs & derivatives* / Q000493:pharmacokinetics* / Q000494:pharmacology; D005260:Female; D006801:Humans; D007421:Intestine, Small / Q000378:metabolism; D008099:Liver / Q000378:metabolism*; D051379:Mice; D008807:Mice, Inbred BALB C; D012709:Serum Albumin / Q000493:pharmacokinetics*; D014018:Tissue Distribution
D012709:Serum Albumin; C046912:lactosaminated serum albumin; C096138:4-formylcolchicine; D003078:Colchicine