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Oridonin is a diterpenoid that has been found in R. rubescens and has diverse biological activities.1,2,3 It binds to β-arrestin-1 and -2 (Kds = 362 and 563 nM, respectively) and acts as a modulator by inhibiting β-arrestin recruitment and receptor desensitization and internalization of various G protein-coupled receptors (GPCRs).1 It is selective for β-arrestin over Gαs, Gαq, Gα12, and Gi.1 Oridonin also inhibits Akt1 and Akt2 (IC50s = 8.4 and 8.9 µM, respectively).2 Oridonin decreases the proliferation of, and induces cell cycle arrest and apoptosis in, KYSE-70, KYSE-410, and KYSE-450 esophageal cancer cells at 20 µM. Oridonin (40 and 160 mg/kg) reduces tumor growth in a patient-derived xenograft (PDX) mouse model of esophageal squamous cell carcinoma. It is also a covalent inhibitor of NLRP3 inflammasome assembly and activation.3 It reduces plasma, white adipose tissue, and liver levels of IL-1β in wild-type but not Nlrp3-/- mice in a model of high-fat diet-induced type 2 diabetes at 3 mg/kg.
WARNING This product is not for human or veterinary use.
1. Small-
2. Targeting AKT with oridonin inhibits growth of esophageal squamous cell carcinoma in vitro and patient-
3. Oridonin is a covalent NLRP3 inhibitor with strong anti-