EPA exists wildly in artery vascular endothelium and could be activated by endogenously activated substances and regulate the vascular tone. The endothelium-dependent vascular relaxation mediated by EPA has been used for almost 20 years as an indicator of endothelium dysfunction. In many cardio-vascular diseases, EPA function was down-regulated. The pharmacological profiles of EPA could be characterized by muscarinic properties, as well as non-muscarinic properties in selectivity for agonists and antagonists and in binding characteristics. The endogenous ligand, receptor type and molecular pharmacological characteristics of EPA are waiting to be investigated.

ATP-sensitive potassium channels (KATP channels) play important roles in various tissues under physiological and pathophysiological conditions by coupling cell metabolic status to electrical activity. The KATP channe l is a tetrameric complex of inwardly rectified potassium (Kir) and ATP binding protein (ABP). The Kir subunits form the channel pore, whereas ABP is required for activation and regulation. Both Kir and ABP are divided into different subu nits and the various Kir and ABP subunits “mix and match” to form KATP c hannels with different pharmacological and nucleotide sensitivities. This revie w focuses on the molecular structure, physiological roles, pathophysiological an d pharmacological properties of KATP channels in different tissues.

Aristolochic Acids ; adverse effects ; Drugs, Chinese Herbal ; adverse effects ; Humans ; Kidney Tubular Necrosis, Acute ; chemically induced ; prevention & control

ATP-sensitive potassium channels (KATP channels) play important roles in various tissues tinder physiological and pathophysiological condi- conditions by coupling cell metabolic status to electrical activity. The KATP channel is a tetrameric complex of inwardly rectified potassium (Kir) and ATP binding protein (ABP). The Kir subunits form the channel pore, whereas ABP is required for activation and regulation. Both Kir and ABP are divided into different subunits and the various Kir and ABP subunits "mix and match" to form KATP channels with different pharmacological and nucleotide sensitivities. This review focuses on the molecular structure, physiological roles, pathophysiological and pharmacological proper ties of KATP channels in different tissues.

A simulating method for dripping process of Ginkgo biloba leaf dripping pills based on computational fluid dynamics was constructed. Ginkgo biloba leaf dripping pills was explored as the experimental subject to simulate the dripping process based on FLOW-3D software. The dripping process was simulated through the derivation of the governing equations, the selection of the models, and simulation parameters. Firstly, the droplet morphologies and drop speeds under different liquid viscosity were simulated. It was found that with the increase of the liquid viscosity, the drop speed decreased and the difficulty of droplet preparation gradually increased. The simulation results were consistent with the experiment results. Secondly, the droplet morphologies at different drop speeds were investigated and verified by experiments. It was found that the simulation results had a good correlation with the experiment results. The results shown that the viscosity of the liquid was the critical material attribute, and the drop speed was the critical process parameter, according to the droplet morphology. The establishment of the simulation method can deepen the understanding of the dripping process and provide a reference for the selection of raw materials and process parameters.

Aim To provide practical method for screening human carbonic anhydrase Ⅱ(hCA Ⅱ) inhibitors in drug discovery.Methods hCA Ⅱ protein was obtained from induced BL21(DE3) E.coli containing plasmid pET-28b-hCA Ⅱ.The hCA Ⅱ activity was detected under pH 7.6 and 25℃ by its esterase activity which could decompose PNPA to increase the photoabsorption at 348 nm. After the assay conditions were finally selected, 35 new compounds were tested.Results A practical method for screening hCA Ⅱ inhibitors was successfully constituted by using recombinant hCA Ⅱ protein expressed in E.coli as the source of hCA Ⅱ enzyme.10 new compounds had better inhibitory effect and 9 new compounds had the same inhibitory effect on hCA Ⅱ compared with acetazolamide.Conclusions The hCA II inhibitor screening technique constituted in this work possesses advantages of being reliable, rapid, and practical. 19 new compounds are worth further research for developing high efficiency and low side effect drugs used for high-altitude illness.

Internationality ; Medicine, Chinese Traditional

Objective:This work aims to explore the long-term efficacy and complications of late-course accelerated hyperfrac-tionation (LCAHF) for treating nasopharyngeal carcinoma. Methods:A total of 58 patients who consulted from December 2005 to May 2008 and histologically proven nasopharyngeal carcinoma at initial diagnosis were randomized into an LCAHF group (experimental group) and a conventional fractionation (CF) group (control group). The treatment dose for both groups was 2 Gy per fraction once dai-ly, 5 days a week. After the 40 Gy to 50 Gy dose, the dosage in the LCAHF group was increased to two daily doses at 1.5 Gy per frac-tion 6 h apart, 5 days a week. The total dose in this group was 73 Gy to 76 Gy, the total dose in the CF group was 70 Gy to 76 Gy, with the total course of the treatment shortened by 0.5 weeks to 1.5 weeks in the former group. Results:The 5-year control rates of the naso-pharyngeal cancers was 86% in the LCAHF group and 59% in the CF group (P=0.021), with statistically significant differences be-tween the two groups. The late complications slightly increased in the LCAHF group than in the CF group, but the differences were not statistically significant. Conclusion:LCAHF treatment improves the local control of nasopharyngeal carcinoma without increasing the incidence of long-term complications.