Галофугинон

Описание

Halofuginone hydrobromide (Halofuginone) is a specific collagen Type I inhibitor that antagonize or inhibit the development of new blood vessels, hence can prevent intimal hyperplasia at a vascular anastomosis. It is used in the treatment or prevention of coccidiosis in both humans and animals.

Химические свойства

Off-White Solid

Использование

Halofuginone is a halogenated derivative of febrigugine. It is Used as an antiprotozoal.

Биологическая активность

Halofuginone is a halogenated derivative of febrifugine, a natural quinazolinone-containing compound found in the Chinese herb D. febrifuga. It has antimalarial and anticoccidial actions. In mammals, halofuginone at 10 ng/ml down-regulates Smad3, blocking TGF-β signaling and preventing both the differentiation of fibroblasts to myofibroblasts and the transitioning of epithelial cells to mesenchymal cells. Through this action, halofuginone blocks fibrosis and tumor progression in a variety of different models. This compound also competitively inhibits prolyl-tRNA synthetase (Ki = 18.3 nM), activating the amino acid starvation response. This prevents the differentiation of TH17 cells, blunting an autoimmune response.