Buformin (hydrochloride)

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.¹ It can also deactivate the glycolytic pathway by suppressing glyceraldehyde 3-phosphate dehydrogenase gene expression, which can lead to lactic acidosis.² 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.³ Some biguanides, including buformin, can also inhibit the mitochondrial ATP synthase.³ 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.⁴

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1. Miller, R.A., Chu, Q., Xie, J., et al. Biguanides suppress hepatic glucagon signalling by decreasing production of cyclic AMP. Nature 494(7436), 256-260 (2013).

2. Yano, A., Kubota, M., Iguchi, K., et al. Buformin suppresses the expression of glyceraldehyde 3-phosphate dehydrogenase. Biol. Pharm. Bull. 29(5), 1006-1009 (2006).

3. Bridges, H.R., Jones, A.J.Y., Pollak, M.N., et al. Effects of metformin and other biguanides on oxidative phosphorylation in mitochondria. Biochem. J. 462(3), 475-487 (2014).

4. Saito, S., Furuno, A., Sakurai, J., et al. Chemical genomics identifies the unfolded protein response as a target for selective cancer cell killing during glucose deprivation. Cancer Res. 69(10), 4225-4234 (2015).