Norisoboldine

Norisoboldine is an orally active natural aryl hydrocarbon receptor (AhR) agonist. Norisoboldine, as a major isoquinoline alkaloid present in Radix Linderae, can be used for the research of Rheumatoid arthritis and Ulcerative colitis^[1][2]. IC50 & Target: AhR^[2] In Vitro: Norisoboldine (1~30 μM; 0~24 hours; CD4+T cells) activates AhR under hypoxic microenvironment and significantly downregulates mRNA expression of miR-31^[2].
Norisoboldine (30 μM; 0~24 hours; CD4+T cells) inhibits glycolysis in hypoxia^[2].
Norisoboldine (1~30 μM; 0~72 hours; Treg cells) promotes Treg differentiation in hypoxia^[2].
Norisoboldine (10, 30 μM) facilitates the disassociation of HSP90/AhR complexes, the nuclear translocation of AhR, and the formation of AhR/ARNT complexes. Norisoboldine induces generation of Treg cells in hypoxia is independent of miR-31^[2]. In Vivo: Norisoboldine (10~40 mg/kg; p.o.; 20 days) significantly reduces the severity of joint swelling and erythema during the course of the experiment^[1].
Norisoboldine (40 mg/kg; i.g.; 10 days) induces enhancement of CYP1A1 expression and suppresses expressions of Glut1 and HK2 in colons^[2].