Metformin (hydrochloride)

Metformin is a biguanide with diverse biological activities.^1,2,3,4 Metformin (250 mg/kg, i.p.) increases hepatic AMPK activity and reduces blood glucose by more than 50% in a liver kinase B1-dependent manner in mice fed normal and high-fat diets, respectively, and reduces blood glucose by 40% in ob/ob mice.² It reduces weight gain, hepatic lipid droplet content, and total cholesterol, LDL cholesterol, and triglyceride levels in the plasma of diet-induced obese mice when administered at doses of 10 or 50 mg/kg per day.⁴ It also reverses increased hepatic triglyceride and apolipoprotein A5 levels, as well as hepatic steatosis, in a dose-dependent manner in an ob/ob mouse model of non-alcoholic fatty liver disease (NAFLD).⁵ Metformin (250 mg/kg) reduces tumor growth in an HCT116 p53^-\- human colon cancer mouse xenograft model, but has no effect on HCT116 p53^-\- tumors overexpressing recombinant S. cerevisiae Ndi1 NADH dehydrogenase, a single-subunit ortholog of the multi-subunit mammalian mitochondrial complex I.³ Formulations containing metformin have been used in the treatment of type 2 diabetes.

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1. Viollet, B., Guigas, B., Garcia, N.S., et al. Cellular and molecular mechanisms of metformin: An overview. Clin. Sci. (Lond.) 122(6), 253-270 (2012).

2. Shaw, R.J., Lamia, K.A., Vasquez, D., et al. The kinase LKB1 mediates glucose homeostasis in liver and therapeutic effects of metformin. Science 310, 1642-1646 (2005).

3. Wheaton, W.W., Weinberg, S.E., Hamanaka, R.B., et al. Metformin inhibits mitochondrial complex I of cancer cells to reduce tumorigenesis. Elife 3:e02242, (2014).

4. Kim, E.K., Lee, S.H., Jhun, J.Y., et al. Metformin prevents fatty liver and improves balance of white/brown adipose in an obesity mouse model by inducing FGF21. Mediators Inflamm. 5813030, (2016).

5. Lin, M.-J., Dai, W., Scott, M.J., et al. Metformin improves nonalcoholic fatty liver disease in obese mice via down-regulation of apolipoprotein A₅ as part of the AMPK/LXRα signaling pathway. Oncotarget 8\(65), 108802-108809 (2017).

Bonglack, E.N., Messinger, J.E., Cable, J.M., et al. Monocarboxylate transporter antagonism reveals metabolic vulnerabilities of viral-driven lymphomas. Proc. Natl. Acad. Sci. USA 118(25), e2022495118 (2021).

Cheng, F., da Silva, S.R., Huang, I.-C., et al. Suppression of Zika virus infection and replication in endothelial cells and astrocytes by PKA inhibitor PKI 14-22. J. Virol. 92(4), e02019-02017 (2018).