ABSTRACT
<p><b>OBJECTIVE</b>To observe the effects of Danhong Injection (丹红注射液) and its main components, including daiclzein and hydroxysafflor yellow A (HSYA), on the anticoagulation, fibrinolysis, anti-apoptosis in hypoxia model of vein endothelial cells (VECs).</p><p><b>METHODS</b>VECs were prepared and were put in a hypoxia environment, which consisted of mixed gas of 95% N and 5% CO mixed gas, when reached confluent culture. Five groups used different treatments, including normal control group, hypoxia group, daiclzein group, HSYA group and Danhong Injection group. The VECs were identified by fluorescence double labeling methods. The morphology was observed by a phase contrast microscopy. The effects of Danhong Injection, daiclzein and HSYA on 6 keto prostaglandin F1α (6-keto-PGF1α) level was measured by the method of radioimmunoassay (RIA). Superoxide dismutase (SOD) activity was tested by water soluble tetrazolium salt. The content of malondialdehyde (MDA) was measured by thiobarbituric acid. The activities of tissue-type plasminogen activator (t-PA) and plasminogen activator inhibitor (PAI) were measured by the method of chromogenic substrate. The contents of endothelin (ET) and nitric oxide (NO) were detected by non-equilibrium RIA and enzymelinked immunosorbent assay. Cells apoptosis rate was determined by flow cytometry.</p><p><b>RESULTS</b>Compared with the normal control group, the floating cells number, PAI activity, ET and MDA contents, and cells apoptosis rate in the culture solution of hypoxia group were all significantly increased, whereas the 6-keto-PGF1α and NO contents, and t-PA and SOD activities were decreased significantly (P<0.01). Compared with the hypoxia group, Danhong Injection markedly increased the 6-keto-PGF1α content and SOD activity, regulated PAI and t-PA activities, ET and NO contents, and decreased MDA content and cells apoptosis rate (P<0.05 or P<0.01).</p><p><b>CONCLUSIONS</b>Danhong Injection and its main components played an important role in protecting primary VECs from hypoxic damage by regulating the secretion and vasomotor function of VECs. The function of Danhong Injection was most remarkable.</p>
Subject(s)
Animals , Humans , Infant, Newborn , Rabbits , 6-Ketoprostaglandin F1 alpha , Metabolism , Apoptosis , Blood Coagulation , Cell Count , Cells, Cultured , Drugs, Chinese Herbal , Pharmacology , Endothelial Cells , Metabolism , Endothelins , Metabolism , Factor VIII , Metabolism , Fibrinolysis , Fluorescent Antibody Technique , Injections , Malondialdehyde , Metabolism , Nitric Oxide , Metabolism , Plasminogen Inactivators , Metabolism , Superoxide Dismutase , Metabolism , Tissue Plasminogen Activator , Metabolism , Umbilical Veins , Cell BiologyABSTRACT
<p><b>AIM</b>To find new anticancer drug based on the structure of 10-hydroxy camptothecin.</p><p><b>METHODS</b>Six camptothecin glycosides (7-12) were synthesized by phase transfer catalysis. The structures of all compounds synthesized were determined by 1H NMR, IR and MS. Their antitumor activity was evaluated on cancer cells in vitro, and inhibitory activity against Topo I was evaluated by molecular biologic method.</p><p><b>RESULTS AND CONCLUSION</b>The result indicated that the yield of camptothecin glycosides by phase transfer catalysis is much higher than by the method from literature, camptothecin glycosides have much lower cytotoxicities on cancer cell in vitro, but have better inhibitory activity of topo I.</p>