Progress in ATP-competitive Kinesin Spindle Protein Inhibitors as Anticancer Agents / 中国药师

Kinesin spindle protein ( KSP) inhibitors is an important direction for the discovery of anticancer agents. Several KSP in-hibitors have been studied in clinic trials. The discovery of ATP-competitive KSP inhibitors may be a new approach for searching novel a-gents to overcome the mutation-mediated resistance to the allosteric inhibitors. The progress in the discovery of ATP-competitive KSP in-hibitors was reviewed in the paper to provide reference for the further development of KSP inhibitors.

Ultrasonic radio frequency analysis technique for noninvasive evaluation of carotid artery intima-media thickness and elasticity in patients with dyslipidemia / 南方医科大学学报

<p><b>OBJECTIVE</b>To assess the value of ultrasonic radio frequency analysis technique for noninvasively evaluation of carotid artery intima-media thickness (IMT) and elasticity in patients with dyslipidemia.</p><p><b>METHODS</b>Radio frequency quality intima-media thickness (RFQIMT) technique and radio frequency quality arterial stiffness ((RF)QAS) technique were used for measurement of IMT and pulse wave velocity (PWV) of the left carotid artery in 86 patients with dyslipidemia and 60 healthy volunteers.</p><p><b>RESULTS</b>Apart from the patients' age, body mass index, systolic blood pressure, diastolic blood pressure, pulse pressure, total cholesterol, triglyceride, low density lipoprotein, high density lipoprotein, fasting blood glucose, IMT and PWV differed significantly between the control and case groups. IMT was positively correlated with PWV (r=0.521, P<0.05). In patients with IMT<1.0 mm (n=81), PWV differed significantly between patients with different number of other atherogenic risk factors (P=0.004), but IMT showed no such variation (P=0.079). In patients with more than 3 and those with 2 other risk factors, PWV increased significantly as compared with those with one risk factor (P=0.002). Multiple linear regression analysis showed that systolic blood pressure, age and fasting blood glucose were independently associated with PWV.</p><p><b>CONCLUSION</b>Ultrasonic radio frequency analysis technique allows accurate measurement of IMT and arterial elasticity, and may thus become a valuable method for evaluating early structural and arterial functional change of the carotid artery.</p>

Preparation and Quality Control of Loxoprofen Sodium Patches / 中国药师

Objective:To study the preparation and quality control of loxoprofen sodium patches and develop an HPLC method for the determination of loxoprofen sodium. Methods:Loxoprofen sodium patches were prepared with CMC-Na and PVP as the adjuvants, and an HPLC method was used to determine the content of loxoprofen sodium. Results:The linear range of loxoprofen sodium was 4-24μg·ml-1(r=0. 999 7), the average recovery was 99. 99%(RSD=0. 99%, n=6). Conclusion:The preparation method is reason-able, simple and stable. The developed HPLC method is specific to determine the content of loxoprofen.

Determination of tetrahydropulmatine content in treatment of winter's diseases in summer path by HPLC / 中国中药杂志

<p><b>OBJECTIVE</b>To establish a high performance liquid chromatography method for the determination of tetrahydropulmatine content in treatment of winter's diseases in summer path.</p><p><b>METHOD</b>The analysis was performed on the Hypersil ODS2 column (4.6 mm x 250 mm, 5 microm) with methanol and 0.1% phosphoric acid solution (adjusted pH to 6.28 with triethylamine) as mobile phase at 63:37. The flow rate was 1.0 mL x min(-1) and the UV detection wavelength was 280 nm.</p><p><b>RESULT</b>The linear range of tetrahydropulmatine was obtained from the range of 2.08 - 49.92 mg x L(-1) (r = 0.999 8). The average recovery was 97.85% with RSD 2.49%.</p><p><b>CONCLUSION</b>This method is simple, reliable and can be used for the determination of tetrahydropulmatine in this preparation.</p>

Effects of Jiawei Buyang Huanwu Decoction on vascular stenosis and oxidative stress after balloon injury of rabbit iliac artery / 中国组织工程研究

BACKGROUND:Modern pharmacological studies have confirmed that Buyang Huanwu Decoction could expand blood vessels,improve microcirculation,decrease oxidative stress,Inflammation and platelet activation,so protect and improve the function of endothelial cells.But its certain mechanism is still unclear,especially for its impact on the restenosis of the coronary artery after percutaneous transluminal coronary angioplasty(PTCA).OBJECTIVE:To investigate the protective effects of Jiawei Buyang Huanwu Decoction on vascular stenosis and oxidative stress after balloon injury of rabbit iliac artery.METHODS:New Zealand rabbits,were randomized and divided into three groups,control group,model group and drug group respectively.Rabbits of control group were fed with common forage,but model group and drug group fed with high fat diet.Two weeks later,the iliac arteries were injured by balloon for model group and drug group.Meanwhile drug group were fed with Jiawei Buyang Huanwu Decoction after the operation,2 mL/kg per day.Control group underwent sham operation control.At the end of4 weeks,serum samples were stored to assay the levels of cholesterol,activity of superoxide dismutase(SOD)and levels of malondialdehyde(MDA).Injured iliac artery was fixed by neural formalin to observe the endothelial hyperplasia by light microscope,and the results were analyzed by picture analysis system.Differences of measurement were compared with one-way analysis of variance as well as repetitive measurements analysis of variance.RESULTS AND CONCLUSION:Iliac artery intima was thin,with Intact structure,without arteriosclerosis In the control group.The vascular lumina were narrower,intima was thicker and there were more enormous arteriosclerosis plaques in model group rabbits.The plaque thickness was reduced and stenosis was mild in drug group.TotaI cholesterol,triglyceridemia,low-density lipoprotein of cholesterol(LDL-C)and MDA levels were significantly lower in the drug group compared with the model group.whereas high-density lipoprotein of cholesterol(HDL-C)and serum SOD levels were significantly greater than the model group(P<0.05).The results showed that Jiawei Buyang Huanwu Decoction has significant preventive effect on intimal hyperplasia and the development of artherosclerosis in rabbits with iliac artery injury,and the mechanism of which may be related to modifying lipid metabolism and cleaning oxygen free radical anti-oxidative stress.