Synthesis and anti-tumor activity of oleanolic acid derivatives / 药学学报

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.

The relationship between TGFbeta1 and TIMP-1 and its effects on the diagnosis of hepatic fibrosis / 中华肝脏病杂志

<p><b>OBJECTIVE</b>To detect the expressions of serum transforming growth factor beta (TGFbeta1) and tissue inhibitor of metalloproteinase 1 (TIMP-1) in patients with chronic hepatitis B (CHB) in different phases of their liver fibrosis and to investigate the effects of TGFbeta1 and TIMP-1 on the diagnosis of hepatic fibrosis and the relationship between them.</p><p><b>METHODS</b>Serum TGFbeta1 and TIMP-1 were detected by enzyme-linked immunosorbent assay and serum HA, LN, PIIINP were detected by radioimmunoassay in 40 CHB patients and 12 healthy persons. Liver biopsies were performed on the 40 patients. The relationships between the TGFbeta1 and TIMP-1 and hepatic fibrosis stages, hepatitis grades and the relevance of the five serum makers of the patients were analyzed.</p><p><b>RESULTS</b>Serum TGFbeta1, TIMP-1 rose in the early stage of liver fibrosis and their sensitivities were higher than that of HA, LN and PIIINP. Serum levels of TGFbeta1 and TIMP-1 increased significantly with the development of fibrosis and had positive correlations with other fibrotic makers such as HA, LN and PIIINP.</p><p><b>CONCLUSION</b>TGFbeta1 and TIMP-1 are involved in the course of developing hepatic fibrosis and TIMP-1 may be regulated by TGFbeta1. Both of them can be used as diagnostic markers of early hepatic fibrosis.</p>