Ethyl 5-methyl-imidazo[1,2-a]pyridine-2-carboxyl-ate.

The title compound, C(11)H(12)N(2)O(2), was synthesized from the reaction of 6-methyl-pyridin-2-amine and ethyl 3-bromo-2-oxopropionate. In the mol-ecular structure, the six- and five-membered rings are individually almost planar with r.m.s. deviations of 0.003 and 0.002 Å, respectively. The two rings are almost coplanar, the dihedral angle between their planes being 1.4 (3)°. Inter-molecular C-H⋯O and C-H⋯N hydrogen bonds are present in the crystal structure.

[Intensive insulin therapy in critically ill patients].

OBJECTIVE: To observe the effect of intensive insulin therapy on improving the condition of critically ill patients. METHODS: A prospective, randomized, controlled study involving adults receiving mechanical ventilation was performed. On admission, critically ill patients were randomly assigned to receive intensive insulin therapy (infusion of insulin only if the blood glucose level exceeded 6.1 mmol/L and maintenance of blood glucose at a level 4.4-6.1 mmol/L, IT group) and conventional treatment (infusion of insulin only if the blood glucose level exceeded 11.9 mmol/L and maintenance of blood glucose at a level 10.0-11.1 mmol/L, CT group). The blood glucose was detected every 4 hours. The days of stay in the intensive care unit (ICU), time of the ventilatory support needed, the time for retention of tracheal intubation, the morning blood glucose level (6 am), the intake of nonprotein calories per day, the dosage of required insulin per day,therapeutic intervention scoring system-28 (TISS-28) score,human leukocyte antigen (locus) DR (HLA-DR), CD4+/CD8+, the mortality rate,acute renal failure (serum creatine >221 micromol/L), bilirubinemia (total bilirubin >34.2 micromol/L),the number of patients who received red-cell transfusions,fever (temperature in mouth >38.5 centigrade) and the rate of hypoglycemia were determined and registered. RESULTS: In a total of 116 patients enrolled, intensive insulin therapy reduced mortality rate (44.83 % with conventional treatment, compared with 12.07 % with intensive insulin therapy,P< 0.01). Intensive insulin therapy reduced the days of stay in ICU, TISS-28 score per day, time of the ventilatory support needed, time for retention of tracheal intubation, mean morning blood glucose levels (6 am) compared with those in CT group (P<0.05 or P<0.01), and patients receiving intensive insulin therapy were less likely to require intensive care. Intensive insulin therapy also raised consumption of insulin per day, HLA-DR and CD4+/CD8+ obviously (P<0.05 or P<0.01). Compare with the morbidity between two groups, the incidence of fever due to infection, acute renal failure and red-cell transfusions were higher in CT group (all P<0.01). CONCLUSION: Intensive insulin therapy maintaining blood glucose at a level 4.4-6.1 mmol/L reduces mortality rate among critically ill patients.

[Effects of nucleotides on apoptosis of thymocytes].

OBJECTIVE: To study the effects of nucleotides on apoptosis of thymocytes in mice. METHODS: Apoptosis model in vivo was first established and 25 KM mice, 4 weeks old, were randomly divided into 5 groups. One group was control, and the others were test groups. Mice in test groups were injected with DEX (25 mg/kg) and the controls were treated with normal saline. 4, 8, 16, and 24 hours later the thymus and spleen were weighed and lymphocytes in thymus were separated. The apoptosis of lymphocytes was analyzed by using DNA electrophoresis and flow cytometry. 16 hours later lymphocytes apoptosis reached a peak and lasted 24 hours. Methods used to establish apoptosis model in vivo were: mice (4 weeks old) were injected with DEX (25 mg/kg), and thymus lymphocytes were separated 16 hours later and analyzed. The effects of nucleotides on apoptosis of mice thymocytes were investigated in experiment 2. Sixty KM mice, 20 g +/- 2g, 4 weeks old, were divided into four treatments: negative control group (NC), positive control group (PC), nucleotides-additive group 1 (NTS1) and nucleotides-additive group 2 (NTS2). RESULTS: Body weight gained in NST1 and NST2 were 3.71 g, 4.01 g respectively, significantly higher than NC (2.74 g) (P < 0.01) and in NST2 was significantly higher than in PC (2.96 g) (P < 0.01). Thymus index and spleen index were decreased significantly (P < 0.01), and no difference was found with the supplementation of nucleotides (P > 0.05). [Ca2+]i increased to 167.37 nmol/L, 191.16 nmol/L, 180.78 nmol/L in PC, NST1 and NST2 with DEX, being significantly higher than in NC (103.76 nmol/L) (P < 0.01). The percent of apoptosised thymocytes in groups were 0.31%, 11.93%, 9.82%, 11.15%, respectively. Thymus index and spleen index, cell apoptosis and [Ca2+]i were not differed significantly among PC, NTS1 and NTS2 groups. CONCLUSION: Nucleotides should have no significant effects on apoptosis of thymocytes in mice in vivo.

[Effect and mechanism of arsenic trioxide on chemosensitivity of human lung adenocarcinoma cells].

OBJECTIVE: To study the apoptosis and chemosensitive effect of As(2)O(3) on human lung adenocarcinoma cell line A549. METHODS: MTT colorimetric assay, immunohistochemical method, flow cytometry and RT-PCR were applied to observe the different effects induced by As(2)O(3) with different concentrations on A549 cells. RESULTS: 1, 2 micro mol/L As(2)O(3) increased Fas expression and inhibited the expression of bcl-2, MRP and LRP; G(1) arrest was observed and the cells were more sensitive to cisplatin. A549 cells in the presence of 5 micro mol/L As(2)O(3) showed growth inhibition and up-regulation of bcl-2, MRP and LRP expressions; but their chemosensitivity to cisplatin did not change. CONCLUSION: As(2)O(3) in low concentrations can increase the chemosensitivity of A549 cells by regulating the expression of apoptosis genes, anti-apoptosis genes and drug-resistant genes and affecting the cell cycle progress.