This technology utilizes dimethyl itaconate (DITA), an endogenous substance produced within the body, as an active ingredient in pharmaceutical compositions and health functional foods to prevent and treat insulin resistance syndromes such as hyperinsulinemia, type 2 diabetes, obesity, hypertension, dyslipidemia, and atherosclerosis. DITA restores impaired insulin responsiveness in muscle cells, normalizing glucose metabolism.
Metformin, used to improve insulin resistance, carries a risk of lactic acidosis, while glitazone-class drugs (PPARγ agonists) have the side effect of stimulating adipocyte differentiation genes, leading to fat accumulation. As most existing drugs are chemically synthesized exogenous substances, there has been a lack of safe and effective treatments for insulin resistance, with concerns even extending to hepatotoxicity at high doses.
This technology confirms the mechanism by which DITA increases AMPK phosphorylation and upregulates FGF21 and PPARδ expression to restore insulin signaling in muscle cells where insulin resistance was induced by palmitic acid. The health functional food can be formulated as powders, granules, tablets, capsules, or beverages. Applicable as a new drug candidate for type 2 diabetes, a health functional food for metabolic syndrome, and an adjuvant therapy for patients with obesity or dyslipidemia, it utilizes a naturally occurring metabolic substance to provide a means of improving insulin sensitivity while reducing the risks of lactic acidosis, fat accumulation, and hepatotoxicity associated with existing synthetic drugs.
This invention was developed with support from the Ministry of Science and ICT for research on the therapeutic effects of the endogenous metabolite kynurenic acid on non-alcoholic fatty liver disease through the amelioration of endoplasmic reticulum stress.
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