Thirteen novel oleanolic acid (OA) derivatives were designed and synthesized with modification at positions of C-3, C-12 and C-28 of OA. Their structures were confirmed by MS, 1H NMR and elemental analysis. Their in vitro cytotoxicities against various cancer cell lines (SGC7901, MCF-7 and A549) were evaluated by MTT assay. The results indicated that the tested derivatives were found to have stronger cell growth inhibitory activity than OA. Among them, compounds II2 and II3 showed more potent cytotoxicity on MCF-7 and A549 tumor cells than gefitinib (positive control). They are worthy to be studied further.

Objective To observe the effects of Dengzhanhua Capsule on kidney tissue inflammatory cytokines in chronic renal failure rats;To explore its possible mechanism for the efficacy in chronic renal failure. Methods Sixty SD rats were randomly divided into normal control group, model group, benazepril group and Dengzhanhua group, 15 rats in each group. Chronic renal failure rat model was established by Platt 5/6 nephrectomized. Benazepril (0.29 mg/100 g) was given to rats in the benazepril group by gastrogavage. Dengzhanhua Capsule (0.3 g/100 g) was given to rats in the Dengzhanhua group by gastrogavage. Normal saline was given to rats in the normal group and the model group by gastrogavage. The whole treatment period was twelve weeks. Expressions of TGF-β1 and PAI-1 were determined by semi-quantitative RT-PCR after treatment. Concentrations of kidney tissue inflammatory cytokines IL-6 and TNF-α were determined by ELISA. Results Expressions of TGF-β, PAI-1 and IL-6, TNF-αin benazepril group and Dengzhanhua group were significantly lower than those in model group (P<0.05). Compared with benazepril group, it was significantly lower in Dengzhanhua group (P<0.05). Conclusion Dengzhanhua Capsule can reduce kidney tissue inflammatory in chronic renal failure rats, and inhibit renal fibrosis.