ABSTRACT
Objective To synthesis,nine N-[3-(2-furanyl)-acryloyl]-N'-substituted benzyl piperazine derivatives were synthesized and evaluated for their primary biological activities.Methods First, the furylacrylic acid was synthesized, Then the target compounds could be obtained by direct furylacrylic acid with the different substituted benzyl piperazine derivatives.In the biological active experiments, taking the different concentrations, comparing with the blank test, the inhibitory effect of the target compounds on VSMC proliferation was investigated by MTT.Results The successful synthesis of nine new compounds.The method was mild and get high yields.The structures of these compounds were confirmed by IR 1 H-NMR, MS, and elemental analysis.The results of preliminary activity test showed that the synthesized products exhibited inhibitory activity at different concentrations , and the highest inhibitory rate was 15μg/mL.Pharmacological results showed that the compounds 3e, 3f and 3 g showed the moderate inhibitory activities against vascular smooth muscle cells proliferation were higher than other compounds , and were worth further studying.Conclusion The synthesized compounds have inhibitory activities and could very well lead to the development of novel types of treat atherosclerosis drug .
ABSTRACT
Objective To analyse tratment strategies and to evaluate the relation between different therapies and survival rate of patients of with asynchronous liver metastases after pancreatic cancer surgery (PCLM).Methods From January 2006 to January 2012,48 patients with PCLM were included in this study,and their medical records were retrospectively analyzed.Results Among the 48 patients,27 cases of liver metastases were found within six months after surgery,and the survival rate for 1,3 and 5 years was 22.2％,3.7％ and 0％,respectively,with the median survival of 6 months,and 21 cases of liver metastases were found after six months,and the survival rate for 1,3 and 5 years was 85.7％,30.6％ and 9.2％,with the median survival of 15 months,and the difference between the two groups was statistically significant (P ＜ 0.01).After pancreatic cancer surgery and adjuvant gemcitabine chemotherapy,the probability of liver metastases was 33.3％ (8/24) within six months,the median disease-free survival time was 8 months and the disease-free survival rate for 1,3 and 5 years was 20.8％,4.3％ and 0％.For patients without adjuvant gemcitabine chemotherapy,the probability of liver metastases was 79.2％ (19/24),the median disease-free survival time was 3 months and the disease-free survival rate for 1,3 and 5 years was 4.2％,0％ and 0％,and the difference between the two groups was statistically significant (P ＜ 0.01).The overall survival for patients undergoing resection of liver metastases combined with gemcitabine treatment was better than the other groups (P ＜ 0.01).And the overall survival for patients undergoing transhepatic arterial embolization (TACE) combined with gemcitabine treatment was better than TACE group,gemcitabine group or the observation group (P ＜0.05).There were no difference in overall survival between TACE group,gemcitabine group and observation group.Conclusions Pancreatic cancer patients who develop liver metastasis within six months after surgery have poor prognosis,but postoperative chemotherapy can delay the development of liver metastasis.For patients with resectable lesion,resection of asynchronous liver metastasis is the treatment of choice,and TACE combined with gemcitabine has better efficacy than that of single treatment.
ABSTRACT
Objective To investigate the relationship between the tumor angiogenesis and the clinicopathological variables of hepatocellular carcinoma (HCC) and determine whether tumor angiogenesis can be used as an indicator for predicting invasion, metastasis and prognosis of HCC. Methods Using the immunohistochemical S-P method, CD34 expression was detected in liver tissue from 20 normal individuals, 20 patients with liver cirrhosis and 85 patients with HCC and juxtacancerous tissues and the microvascular density (MVD) determined in those from 85 patients with HCC. Results CD34 was mainly located in the cell cytoplasm of endothelial cells. The CD34 staining was confined to vessels in the portal triad in the above-mentioned various tissues. In HCC tissues, however, sinusoid-like vessels reacted intensively with anti-CD34 and the MVD was 156.5±62.4 (per 0.74 mm2). MVD was correlated to tumor size, number, differentiation, emboli in the portal vein and capsule (P<0.05 or 0.01) but not to HBsAg and AFP (P>0.05). It was also correlated with prognosis of HCC. The mean tumor-free survival of MVD ≥156 was 14 months while that of MVD <156 was 53 months (P<0.01). Conclusion The expression of CD34 in sinusoid-like vessels in HCC tissues represents the neovascularization. Angiogenesis in HCC is associated with the progression of HCC. MVD can be used as an indicator to judge the invasion, metastasis and prognosis of HCC.