Composition for preventing or treating aortic valve stenosis comprising 5-hydroxymethylfurfural

Aortic valve calcification prevention material using the small molecule furan compound 5-HMF to inhibit BMP2 and RUNX2

This technology is a pharmaceutical composition and a food composition for prevention and improvement that uses 5-hydroxymethylfurfural (5-HMF), a furan-based small molecule compound, or its salts as an active ingredient to prevent and treat valvular disease and aortic valve stenosis. 5-HMF reduces the expression of osteogenesis-related calcification markers in valvular interstitial cells.

Aortic valve stenosis is one of the three most common cardiovascular diseases in the elderly, but because no target proteins or drugs have been identified to prevent valve calcification, valve replacement surgery has been the only treatment. Replacement surgery places a heavy burden on elderly patients, is costly, and carries risks of stroke, paravalvular leakage, and durability issues. Clinical trials attempting to apply lipid-lowering agents or osteoporosis drugs to valve stenosis have relied on indirect mechanisms and have shown no effect in some cases. 5-HMF was previously known only for its antioxidant and anticancer properties, with its effects on valve calcification remaining unknown.

This technology utilizes the fact that 5-HMF inhibits BMP2, a key signal that transforms valvular interstitial cells into osteoblast-like cells, and the transcription factor RUNX2, thereby breaking the vicious cycle where calcification triggers further calcification. It can be administered in a daily range of 0.001 to 10 g and can be combined with other calcification inhibitors. It can be applied as a treatment to delay progression in early-stage valve calcification patients, as an alternative drug therapy for high-risk elderly patients who cannot undergo surgery, and as a health supplement for the elderly. As a small molecule compound with a simple structure that is also found in food, it lowers the burden of raw material procurement and formulation while directly blocking valve ossification signals.

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Key Features:

• Pharmaceutical composition for preventing or treating valvular disease and aortic valve stenosis comprising 5-hydroxymethylfurfural or a pharmaceutically acceptable salt thereof as an active ingredient
• 5-hydroxymethylfurfural active ingredient that inhibits the expression of calcification markers BMP2 or RUNX2 in valvular interstitial cells
• Pharmaceutical composition for preventing or treating valve calcification configured for a daily administration of 0.001 to 10 g of 5-hydroxymethylfurfural
• Food composition for preventing or improving valve calcification comprising 5-hydroxymethylfurfural or a food-grade salt thereof as an active ingredient

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This invention was developed with support from the Ministry of Science and ICT for the discovery of biomarkers and therapeutic targets to inhibit intractable aortic valve calcification using multi-omics data-based deep learning.

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