Mechanism of action of phenytylbiguanide (phenformin) in normal subjects. II. Intestinal absorption versus nonintestinal effects

Halpern, Alfredo; Wajchenberg, B. L.; Fazia, A.I.M.

doi:10.1016/0026-0495(74)90053-5

Metabolism

1974

DOI: 10.1016/0026-0495(74)90053-5

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Mechanism of action of phenytylbiguanide (phenformin) in normal subjects. II. Intestinal absorption versus nonintestinal effects

Alfredo Halpern

B. L. Wajchenberg

A.I.M. Fazia

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1976

1981

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Cited by 5 publications

(1 citation statement)

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“…1 -2 There is evidence, however, that suggests that phenformin acts by increasing the physiologic responsiveness of human peripheral tissues to circulating insulin. 3 " 6 An effect of biguanides on the binding of insulin to the target cell, the initial step in insulin action, 7 was the possibility investigated in this study.…”

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confidence: 99%

Phenformin Increases Insulin Binding to Human Cultured Breast Cancer Cells

et al. 1980

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The effect of the hypoglycemic biguanide, phenformin, on the binding of insulin to MCF-7 cells, an in vitro line derived from a human breast cancer, has been investigated. Cells incubated for 24 h in the presence of 1.0 micrograms/ml of phenformin bound 62.2 +/- 8.1% (mean +/- SE) more 125I-insulin than did controls. The phenformin effect was dose-dependent over the concentration range of 0.1 micrograms/ml to 10.0 micrograms/ml. The increased binding was due to an increase in receptor number without a change in binding affinity. This demonstration of increased receptor number in response to phenformin exposure provides support for the hypothesis that one action of phenformin is to enhance tissue sensitivity to insulin.

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mentioning

confidence: 99%

Phenformin Increases Insulin Binding to Human Cultured Breast Cancer Cells

et al. 1980

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Phenformin stimulation of insulin binding to human cultured lymphocytes

Iwamoto

Goldfine

1981

J Endocrinol Invest

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The effects of the oral hypoglycemic agent, phenformin, were studied on the binding of 125I-insulin to its receptors in IM-9 human cultured lymphocytes. Three h after the addition of 5 microgram/ml of phenformin to these cells there was detectable stimulation of 125I-insulin binding; maximal effects were seen after 18 h. A detectable effect of phenformin was seen at 1 microgram/ml and maximal effects were seen at 5 microgram/ml. These studies demonstrate therefore than phenformin increases the binding of 125I-insulin to human cultured lymphocytes, and raise the possibility that phenformin could act in vivo to regulate insulin receptors.

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Mechanism of action of phenethylbiguanide (phenformin) in man. III. Interrelationship between ethanol and phenethylbiguanide (PBG) in normal and diabetic subjects

et al. 1976

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Mechanism of action of phenytylbiguanide (phenformin) in normal subjects. II. Intestinal absorption versus nonintestinal effects

Cited by 5 publications

References 13 publications

Phenformin Increases Insulin Binding to Human Cultured Breast Cancer Cells

Phenformin Increases Insulin Binding to Human Cultured Breast Cancer Cells

Phenformin stimulation of insulin binding to human cultured lymphocytes

Mechanism of action of phenethylbiguanide (phenformin) in man. III. Interrelationship between ethanol and phenethylbiguanide (PBG) in normal and diabetic subjects

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