This technology is a composition for preventing, improving, and treating Graves' ophthalmopathy, using E-type or Z-type isomer compounds (Chemical Formulas 1 and 2) with a 17-ethylidene steroid backbone as active ingredients. The same active ingredient is formulated for use in pharmaceutical, food, and cosmetic applications.
Graves' ophthalmopathy causes exophthalmos, diplopia, and vision loss due to orbital adipocyte differentiation and inflammatory responses, yet its pathological mechanism remains unclear. While high-dose glucocorticoids have been the primary treatment for decades, there is still a lack of drugs capable of halting disease progression or achieving a cure.
This technology inhibits NFkB, ERK, JNK, AKT, and p38 signaling, thereby reducing the expression of differentiation transcription factors such as C/EBPα, C/EBPβ, PPARγ, and SREBP1, as well as inflammatory cytokines. Consequently, it effectively blocks the adipocyte differentiation of orbital fibroblasts. It can be applied to the development of thyroid eye disease treatments and functional foods or cosmetics for eye area improvement, offering a new targeted therapeutic option to complement existing steroid treatments.
This invention was developed with support from the Ministry of Science and ICT for research on the role of chemokines in the pathogenesis of thyroid eye disease.
WO2020-235967A1