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OBJECTIVE To study the effects of disodium cantharidinate on the pharmacokinetic behavior of capecitabine in rats. METHODS Rats were randomly divided into two control groups and two experimental groups with 6 rats in each group. Two control groups were intraperitoneally injected with normal saline， and two experimental groups were intraperitoneally injected with Disodium cantharidinate injection of 0.5 mL/kg， for 7 consecutive days. Eight days after medication， control group 1 and experimental group 1 were given capecitabine 5 mg/kg intragastrically， while control group 2 and experimental group 2 were given capecitabine 5 mg/kg intravenously. Blood samples were collected at different time points after administration. After extraction with ethyl acetate， the concentration of capecitabine in rat plasma was determined by UPLC-MS/MS method using tolbutamide as the internal standard. The pharmacokinetic parameters were calculated by DAS 2.0 software. RESULTS Compared with control group 1， MRT0－∞， cmax， AUC0－30 h， AUC0－∞ and F of experimental group 1 were increased significantly， while CLz/F was decreased significantly （P＜0.01）. Compared with control group 2， t1/2， MRT0－30 h， MRT0-∞， AUC0－30 h and AUC0－∞ of experimental group 2 were increased significantly （P＜0.01）. CONCLUSIONS Disodium cantharidinate can increase the plasma exposure of capecitabine in rats， improve its oral bioavailability， prolong the average residence time， and reduce its clearance rate.
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Objective To evaluate the efficacy and safety of disodium cantharidinate injection combined with transcatheter arterial chemoembolization(TACE) compared with TCAE alone in the treatment of hepatocellular carcinoma(HCC) by meta-analysis.Methods Databases of Pubmed, CNKI,Wangfang and VIP were searched electronically, and the randomized controlled trials about disodium cantharidinate injection combined with TACE in the treatment of HCC were included.Meta-analyses were conducted after the quality of the included studies was assessed.Results Seven eligible studies that included a total of 562 HCC patients were identified in the present meta-analysis.The combined results showed that disodium cantharidinate injection combined with TACE in the treatment of HCC, compared with TACE alone, could increase effective rate ( RR =1.31, 95%CI 1.10-1.56) and clinical benefit rate (RR =1.20, 95%CI 1.04 -1.39), improve the life quality (RR =1.60, 95%CI 1.26 -2.03) and improved the 1, 2 year survival (RR =1.57 with 95%CI 1.28 -1.93 and RR =2.08 with 95%CI 1.46 -2.97, respectively).Conclusion Meta-analysis indicates that the efficacy of disodium cantharidinate injection combined with TACE is superior to TACE alone for the patients with HCC.
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Objective To investigate the effect of disodium cantharidinateon in vitro lymphocyte immune response in lung cancer patients.Methods Twenty non-small cell lung cancer patients diagnosed by pathological diagnosis were selected.The effects of different concentrations of disodium cantharidinate and vitamin B6 on lymphocyte proliferation and CD4 + CD25 + T cells,CD25 + FOXP3 + T cells,CD4 + and CD8 + T cells were detected by methyl thiazolyl tetrazolium assay and flow cytometry.Results When the concentrations of disodium cantharidinate and vitamin B6 was less than 10 μg/ml,with the growth of concentration,it stimulated the proliferation of peripheral blood lymphocytes.When the concentration was more than 10 μg/ml,with the growth of concentration,the absorbance value decreased,and the stimulating effect weakened.When the concentration of disodium cantharidinate and vitamin B6 injection was less than 10 μg/ml,with the growth of concentration,CD4 +/CD8 + ratio increased significantly,and CD4 + CD25 +/CD4 + and CD25 + FOXP3 + T cells were significantly lower,which showed statistically significant differences (t =2.171,P =0.032 ; t =2.103,P =0.041 ; t =3.662,P =0.002 ; t =3.201,P =0.003 ; t =3.233,P =0.003).But when the concentration was more than 10 μg/ml,The differences of CD4 +/CD8 + ratio,CD4 + CD25 +/CD4 + and CD25 + FOXP3 + T cells in 10,15,20 μg/ml groups were not statistically significant,which showed that disodium cantharidinate and vitamin B6 injection had a positive effect on enhancing the immune function of lymphocytes in lung cancer in a concentration dependent manner,but high concentration was unhelpful.Conclusion Disodium cantharidinate and vitamin B6 injection can promote lung cancer in vitro lymphocyte proliferation as well as increase its immunity in a certain range.
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Objective To study the growth inhibision effect of disodium cantharidinate and Vitamin B6 injection on hepatocellular carcinoma cell line HepG2.Methods Different concentrations of disodium cantharidinate and Vitamin B6 injection were applied on the hepatocellular carcinoma cell line HepG2.The inhibition rate of HepG2 growth was measured by MTT assay.The apoptotic rate was detected with flow cytometry,and the morphology of apoptosis was observed by fluorescence microscope.Results The growth of HepG2 cells was significantly inhibited as well as the apoptosis of HepG2 cells was significantly encouraged by disodium cantharidinate and Vitamin B6 injection(P
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Objective:To observe the inhibitory effect of disodium cantharidinate on human hepatoma cell line HepG2 and investi-gate its possible mechanisms. Methods:HepG2 cells were treated with different concentration of disodium cantharidinate,The in- hibiton of cell proliferation,cell cycle distribution,expression of Survivin and activity of Caspase-3 were respectively evaluated by MTT assay,flow cytometry,immunocytochemistry,and chromatometry. Results:Disodium cantharidinate could inhibit the proliferation of HepG2 cells. The IC50 at 24,48,72 h after intervention were 2.41?0.48,0.72?0.08,and 0.39?0.04 ug/ml,The cells of G2/M phase and activity of Caspase-3 were increased.the expression respectively of Survivin were inhibited after the intervention of disodium cantharidinate. Conclusion:The inhibitory effect of disodium cantharidinate on HepG2 cells may be mediated by the block of cellcycle,enhancement of Caspase-3,and inhibition of Survivin.