Background/ Aim: There is evidence that inhibitory effects of biguanides on oxidative phosphorylation require uptake of biguanides into the mitochondria. In this study the action of two biguanides that enter the mitochondria (buformin and phenformin) were compared with the action of two biguanides with poor uptake (phenyl biguanide and proguanil). Materials and Methods: Effects on growth, glucose uptake and medium acidification were studied with two human colon cancer cells and seven bladder cancer cell lines. Results: Growth inhibition was greatest with proguanil followed by phenformin, buformin and phenylbiguanide. In contrast, increased glucose uptake and acidification of the medium was observed with buformin and phenformin, with no change or less acidification of the medium with phenyl biguanide and proguanil. Conclusion: The effect of biguanides on glucose metabolism requires mitochondrial uptake while the mechanism for growth inhibition by biguanides remains to be defined.
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