Bardoxolone Methyl作用于小鼠巨噬细胞,对interferon-Ƴ诱导的一氧化氮的产生具有强效的抑制活性,其IC50 为0.1 nM 。 Bardoxolone Methyl降低白血病HL-60,KG-1和NB4细胞的生存能力,其IC50分别为 0.4,0.4,和0.27μM。 CDDO-ME诱导促凋亡Bax蛋白表达,抑制ERK1 / 2的活化,并且它抑制Bcl-2的磷酸化,这有助于诱导细胞凋亡。 Bardoxolone Methyl可有效地抑制(IL)-1beta, phorbol ester, okadaic acid, hydrogen peroxide, lipopolysaccharide, 和cigarette smoke激活的组成型和可诱导的NF-κB的肿瘤坏死因子。
Bardoxolone Methyl(60 mg/kg)体内用药,可减少肺肿瘤的数量,大小和降低严重程度。 Bardoxolone Methyl还可显著降低LPS刺激下的体内炎症因子的反应,诱导脾脏HO-1蛋白表达,对抗致死剂量的LPS保护小鼠。
CDDO Methyl Ester is a synthetic triterpenoid that inhibits I κBα kinase and enhances apoptosis induced by TNF and chemotherapeutic agents through down-regulation of expression of nuclear factor κB-reg ulated gene products in human leukemic cells. CDDO Methyl Ester is a novel therapeutic agent in the treatment of acute myeloid leukemia and in the treatment of pancreatic cancer as well as other forms of cancer.