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Biguanides drugs: past success stories and promising future for drug discovery

Biguanides have attracted much attention a century ago and showed resurgent interest in recent years after a long period of dormancy. They constitute an important class of therapeutic agents suitable for the treatment of a wide spectrum of diseases. Therapeutic indications of biguanides include antidiabetic, antimalarial, antiviral, antiplaque, and bactericidal applications.

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 The Mechanism of Action of Biguanides: New Answers to a Complex Question

In the last two decades, the antidiabetic drugs, biguanides, have received considerable interest owing to their presumed antitumor properties. A critical issue that has been at the center of many studies is how they act at the molecular level. Most works propose that biguanides inhibit mitochondrial complex I, which causes ATP depletion and activation of compensatory responses, responsible for the therapeutic properties. However, complex I can only be inhibited with concentrations of biguanides that cannot be tolerated by animals and patients, suggesting that alternative targets and intracellular perturbations are involved.

Articles of Interest

Biguanides. A review of history, pharmacodynamics and therapy

This review on biguanides gives a general survey of biguanide actions on many metabolic models in vivo and in vitro. It focuses especially on the comparison of the 3 antidiabetic biguanides, of which metformin is discussed as the only oral antidiabetic biguanide useful in treatment of type-II diabetes with a minimum risk of side effects when applied in a well controlled regime.

Metformin: historical overview

The awesome voyage of metformin from herbal beginnings to respected therapeutic agent has been turbulent. It was discovered, forgotten, rediscovered, repurposed, rejected, rescued, exonerated and may have further secrets to reveal.

Review of Biguanide (Metformin) Toxicity

In the 1920s, guanidine, the active component of Galega officinalis, was shown to lower glucose levels and used to synthesize several antidiabetic compounds. Metformin (1,1 dimethylbiguanide) is the most well-known and currently the only marketed biguanide in the United States, United Kingdom, Canada, and Australia for the treatment of non-insulin-dependent diabetes mellitus.

“What's in a structure?” The story of biguanides

Considering the extensive literature available on the structural studies on biguanides till date, the representation of incorrect structure is certainly surprising and reveals indifference shown by individuals. The structure of a molecule ‘speaks’ of its properties. While the correct structure helps in preliminary interpretation of the molecular properties, the incorrect structural description may give an erroneous perception about its properties leading to serious consequence

Resources

GoodRx

Biguanides are used to treat diabetes type 2 and PCOS. They work by lowering blood sugar levels along with diet and exercise and by decreasing the amount of glucose that is absorbed. They also help to regulate menstrual cycles.

Diabetes.co.uk

The term biguanide refers to a group of oral type 2 diabetes drugs that work by preventing the production of glucose in the liver, improving the body’s sensitivity towards insulin and reducing the amount of sugar absorbed by the intestines.

ScienceDirect

The biguanides are derivatives of guanidine, a naturally occurring substance found in vegetables such as turnips and cereals... Biguanides are usually supplied as polymers in the salt form, mostly as the hydrochloride.