Cocoa and Related Flavonoids for Treatment of Diarrhea

Case Number CH-068

Inventors: Horst Fischer, PhD and Beatte Illek, PhD

This invention provides novel methods and compositions for the use of the CFTR chloride ion channel as a novel drug target for the treatment of diseases that are characterized by defective or hyperactive chloride ion transport functions of epithelial tissues, such as intestines, lungs, skin, eyes, pancreas, liver and reproductive organs, including the treatment of diarrhea.

In the developing world, about 2.5 million children under 5 years of age die of diarrhea every year. In the developed countries, secretory diarrhea causes significant morbidity. In the US, 2.4 million physician visits account for more than 200,000 hospitalizations of children under 5 years and many deaths in the elderly.

The underlying cellular mechanism during secretory diarrhea is the sustained activation of the CFTR chloride ion channel. This constant activation results in the hypersection of salt and water into the lumen of the intestine. Currently, there is no drug on the market that targets the CFTR chloride ion channel for the treatment of diarrhea.

A novel treatment option is the inhibition of CFTR activity, which will reduce the amount of water flux. Dose-dependent effects of flavonoid compounds present in cocoa, or molecularly closely related compounds, were tested and found to have inhibitory effects of cAMP-stimulated chloride ion secretion in the intestine.

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