Composition for inhibiting PAR2 activity comprising punicalagin

Anti-inflammatory composition using pomegranate-derived punicalagin for PAR2 inhibition

This technology utilizes punicalagin, an ellagitannin-based natural compound found in pomegranates, to specifically inhibit PAR2 receptor activity. It provides pharmaceutical, health functional food, and cosmetic compositions for the prevention and treatment of inflammatory diseases such as colitis, pancreatitis, conjunctivitis, and nephritis.

The PAR2 receptor is activated by various proteases and is involved in numerous inflammatory diseases, yet few natural inhibitors are known. In particular, steroids and immunosuppressants used to treat lupus nephritis often cause significant side effects with long-term use and are associated with frequent relapses upon discontinuation.

This technology leverages the mechanism by which punicalagin inhibits calcium increase and chloride secretion triggered by PAR2 activity, while reducing the secretion of inflammatory cytokines such as IL-6, IL-8, and TNF-α. As a plant-derived natural compound, it carries a lower risk of toxicity and side effects. It can be applied to treatments for inflammatory bowel disease and nephritis, anti-inflammatory health supplements, and soothing cosmetics, offering a safe alternative for managing chronic inflammation that requires long-term care.

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Key Features:

• Pharmaceutical composition for preventing or treating inflammatory diseases in patients with PAR2 activation, comprising punicalagin or a pharmaceutically acceptable salt thereof
• PAR2 inhibition-based composition where the target inflammatory disease is limited to one or more of colitis, pancreatitis, conjunctivitis, or nephritis
• Action of inhibiting calcium increase or chloride secretion caused by PAR2 activity, or inhibiting the secretion of cytokines such as IL-6, IL-8, GMCSF, TNF-α, and IL-1β
• Health functional food and cosmetic compositions for preventing or improving inflammatory diseases, comprising a food-grade or cosmetically acceptable salt of punicalagin

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This invention was developed with support from the Ministry of Science and ICT for the development of small-molecule PAR2 receptor inhibitors for the treatment of inflammatory diseases.

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