This invention provides the application of cyperene in the preparation of
olfactory receptor Olfr43 specific
agonist drugs, relating to the field of
small molecule pharmaceutical technology of
traditional Chinese medicine. This invention constructs Hana3A... Olfr43‑FLuc‑RLuc A
heterologous OR dual-
luciferase screening platform revealed that cyperene can activate the downstream pathway of the
olfactory receptor Olfr43, significantly increasing
intracellular cAMP levels. Cellular experiments further verified that cyperene stimulation significantly increased the mNRA and
protein expression levels of Olfr43 in cells, raising downstream cAMP levels. This, in turn, inhibited the expression of lipid synthesis-related genes by phosphorylating
CREB, promoting HES-1, and inhibiting DGAT2
protein expression, ultimately reducing TC and TG in the HepG2
hyperlipidemia model. This invention is the first to propose that cyperene can act as a specific
agonist targeting the
olfactory receptor Olfr43 to regulate downstream cAMP changes. This invention provides a new option for the development of highly effective agonists specifically targeting Olfr43 / OR1A1.