BuforMin Hydrochloride

Description

Buformin is a biguanide derivative with antihyperglycemic activity. It delays absorption of glucose from the gastrointestinal tract, increases insulin sensitivity and glucose utilization in peripheral cells, and inhibits hepatic gluconeogenesis. It can also deactivate the glycolytic pathway by suppressing glyceraldehyde 3-phosphate dehydrogenase gene expression, which can lead to lactic acidosis. Biguanides, such as buformin, are reported to inhibit the mitochondrial respiratory complex I by inhibiting ubiquinone reduction and by stimulating reactive oxygen species production via the complex I flavin. Some biguanides, including buformin, can also inhibit the mitochondrial ATP synthase. Buformin has also been examined for antitumor activity due to its ability to disrupt the unfolded protein response transcription program during glucose deprivation, which induces cell death in glucose-deprived tumor cells.

Chemical properties

White Solid

Originator

Silubin,Protochemie,Switz.

The Uses of BuforMin Hydrochloride

BuforMin Hydrochloride is a biguanide derivative with antihyperglycemic activity. It delays absorption of glucose from the gastrointestinal tract, increases insulin sensitivity and glucose utilization in peripheral cells, and inhibits hepatic gluconeogenesis. BuforMin Hydrochloride has also been examined for antitumor activity due to its ability to disrupt the unfolded protein response transcription program during glucose deprivation, which induces cell death in glucose-deprived tumor cells.

The Uses of BuforMin Hydrochloride

Buformin, clinically used for diabetes mellitus, is known to improve resistance to insulin in patients. It suppresses the expression of glyceraldehyde 3-phosphate dehydrogenase.

Manufacturing Process

105.6 g of n-butylamine hydrochloride and 79.3 g of dicyandiamide were ground intimately and mixed. The mixture was heated by means of an oil bath, gradually with stirring, and after thirty minutes when the internal temperature had reached 150°C, an exothermic reaction ensued with internal pressure rising to 178°C. The reaction mixture was removed from the oil bath until the internal temperature had fallen to 150°C and then heating was resumed at 150°C for one hour. The cooled fusion mixture was dissolved in 3 liters of acetonitrile and on cooling n-butyl-biguanide hydrochloride precipitated.

Therapeutic Function

Antidiabetic