ABSTRACT
<p><b>OBJECTIVE</b>To discuss the effect of protein kinase C (PKC) on regulation of ecto-5'-nucleotidase activity by lysophosphatidylcholine(LPC) in human umbilical endothelial cells (HUVEC).</p><p><b>METHODS</b>Experiments were conducted in HUVEC grown on dishes which were divided into 4 groups (n=15): (1) Control group in which only eAMP (5 micromol/L) was added; (2) LPC group in which HUVEC were incubated with LPC (10 micromol/L) before eAMP was added; (3) Chelerythrine group in which cells were pre-incubated with the PKC inhibitor chelerythrine (100 micromol/L) before LPC and eAMP were added; (4) alpha, beta-Methyladenosine-5'-Diphosphate (AOPCP) group in which cells were incubated with AOPCP (10 micromol/L) before eAMP was added. Etheno-adenosine production was detected at 15th, 30th, 45th min with high performance liquid chromatography(HPLC) respectively.</p><p><b>RESULTS</b>Comparing to the control group LPC significantly increased etheno-adenosine production at three time points respectively (P < 0.05). Furthermore, PKC inhibitor chelerythrine abolished this effect of LPC and the ethenoadenosine production at three time points were at the same level of control group (P > 0.05). CD73 inhibitor AOPCP significantly decreased the etheno-adenosine production compared to the other three groups (P < 0.01).</p><p><b>CONCLUSION</b>Ecto-5'-nucleotidase can be modulated within minutes following exposure of HUVEC to LPC and this response may be mediated by PKC in HUVEC.</p>
Subject(s)
Humans , 5'-Nucleotidase , Metabolism , Cells, Cultured , GPI-Linked Proteins , Metabolism , Human Umbilical Vein Endothelial Cells , Cell Biology , Metabolism , Lysophosphatidylcholines , Pharmacology , Protein Kinase C , Physiology , Up-RegulationABSTRACT
To search for potential antitumor drugs with potent efficiency and low toxicity, a novel 1,4,7-triazacyclodecane and its platinum (II) complex were synthesized. These compounds were characterized by elemental analysis, IR, 1H NMR, 13C NMR, MS spectra, thermoanalysis and conductivity measurement. Antitumor activity study indicated these compounds had strong antitumor activity in vitro to some extent. Inhibition of human liver tumor of CA was examined by antitumor rate and growth rate, complex C showed inhibition activity on transplanting-tumor growth of CA, 12 mg x kg(-1) was as potent as cisplatin, its ID50 was 853.6 mg x kg(-1).