1375592-88-3Relevant academic research and scientific papers
Glycosylated diazeniumdiolate-based oleanolic acid derivatives: Synthesis, in vitro and in vivo biological evaluation as anti-human hepatocellular carcinoma agents
Huang, Zhangjian,Fu, Junjie,Liu, Ling,Sun, Yijun,Lai, Yisheng,Ji, Hui,Knaus, Edward E.,Tian, Jide,Zhang, Yihua
, p. 3882 - 3891 (2012)
A series of O2-glycosylated diazeniumdiolate-based derivatives of oleanolic acid (4-19) were synthesized and their anti-human hepatocellular carcinoma (HCC) activities were evaluated. Compound 6 selectively inhibited HCC, but not non-tumor liver cell proliferation. This inhibition was attributed to high levels of nitric oxide (NO) released in HCC cells. Importantly, 6 exhibited low acute toxicity (LD50 = 173.3 mg kg-1) and potent inhibition of HCC tumor growth in mice (3 mg kg-1 iv). Furthermore, 6 induced HCC cell apoptosis, which was accompanied by lower mitochondrial membrane potentials and Bcl2 expression, but with higher cytochrome C release, Bax, caspase 3 and 9 expression activities in HCC cells. Collectively, 6 may be a promising candidate drug for the intervention of HCC.
