Rutaecarpine

Rutaecarpine, an alkaloid of Evodia rutaecarpa, is an inhibitor of COX-2 with an IC₅₀ value of 0.28 μM. Rutaecarpine can target and activate the NRF2/HO-1 pathway to reduce craniofacial injury. Rutaecarpine sttenuates oxidative stress-induced traumatic brain injury (TBI) and reduces secondary injury via the PGK1/KEAP1/NRF2 signaling pathway. Rutaecarpine can cross the blood-brain barrier (BBB). IC50 & Target:IC50: 0.28 μM(COX-2)^[1] In Vitro:Rutaecarpine has shown a variety of intriguing biological properties such as anti-thrombotic, anticancer, anti-inflammatory and analgesic, anti-obesity and thermoregulatory, vasorelaxing activity, as well as effects on the cardiovascular and endocrine systems^[2]. Rutaecarpine inhibits COX-2 and COX-1 dependent phases of PGD2 generation in BMMC in a concentration-dependent manner with an IC₅₀ of 0.28 μM and 8.7 μM, respectively. It inhibits COX-2-dependent conversion of exogenous arachidonic acid to PGE₂ in a dose-dependent manner by the COX-2-transfected HEK293 cells^[1]. In Vivo:Rutaecarpine showed in vivo anti-inflammatory activity on rat l-carrageenan induced paw edema by intraperitoneal administration^[1]. Rutaecarpine significantly decreases the number of antibody-forming cells and causes weight decrease in spleen in a dose-dependent manner. In addition, rutaecarpine administered mice exhibit reduced splenic cellularity, decreased numbers of total T cells, CD4+ cells, CD8+ cells, and B cells in spleen. IL-2, interferon and IL-10 mRNA expressions are suppressed significantly by rutaecarpine treatment. The number of CD4+IL-2+ cells is reduced significantly following administration of mice with rutaecarpine^[3].