抑制的

In clinical. acetylcholinesterase inhibitors reduce the breakdown of synaptic acetylcholine, have been modestly effective in improving the cognitive deficits of Alzheimer's disease.The goal of this work is to determine enzyme kinetics and mechanisms of acetylcholinesterase and butyrlcholinesterase inhibition by five cardiovascular drugs, lovastatin, simvastatin, amlodipine besylate, nifedipine, and hydralazine hydrochloride, and two benzodiazepines, diazepam and chlordiazepoxide hydrochloride. All drugs in this study are reversible mixed-type inhibitors of acetylcholinesterase and butyrylcholinesterase. The pKi values for acetylcholinesterase and butyrylcholinesterase inhibition by the cardiovascular drugs are linearly correlated with the molecular weights of the drugs with the slopes of 0.005 and 0.0021, respectively. Therefore, van der Waals' interactions between acetylcholinesterase and the cardiovascular drugs are stronger than those between butyrylcholinesterase and the drugs. This is probably due to a smaller active site gorge and a more significant peripheral anionic substrate binding site of acetylcholinesterase than those of butyrylcholinesterase.

本研究之目的系决定乙醯胆碱酯酵素和丁醯胆碱酯酵素被五种心脏血管药物lovastatin， simvastatin， amlodipine besylate， nifedipine、hydralazine hydrochloride和两种benzodiazepines：diazepam和Chlordiazepoxide hydrochloride的抑制作用之动力学及机转，这些药物都是乙醯胆碱酯酵素和丁醯胆碱酯酵素的可逆性、混合型之抑制剂，实验结果显示，五种心血管药物对於乙醯胆碱酯酵素及丁醯胆碱酯酵素抑制之pKi值和药物之分子量呈直线之关系，斜率分别为0.005及0.0021因此丁醯胆碱酯酵素，与心血管药物间之凡德瓦作用（van der Waals' ）比乙醯胆碱酯酵素与心血管药物间者弱，这可能原因是丁醯胆碱酯酵素之活性区域比乙醯胆碱酯酵素之活性区域更宽广，但丁醯胆碱酯酵素之周边阴离子区域不及乙醯胆碱酯酵素之周边阴离子区域者明显重要，由於五种心血管药物对於乙醯胆碱酯酵素和丁醯胆碱酯酵素抑制之pKi值存在著线性关系表示此种抑制作用系经过共同之反应机理。

Ovoalbumin-induced rat feet edema was significantly decreased by QLS with the doses of 35 and 70.0 mg·kg-1·d-1 (P.05).Cotton pellet-induced rat granuloma was significantly decreased by QLS with the doses of 35.0 and 70.0 mg·kg-1·d-1 (P.05 or P.01 ) and the granuloma inhibitory rates were 32.40 % and 35.65 %,respectively.

结果：QLS 3个剂量组均不同程度地抑制小鼠耳肿胀度，与空白对照组比较，50及100 mg·kg-1·d-1 QLS组小鼠耳肿胀度均明显减小（P.05或P.01），对小鼠耳肿胀的抑制率分别为53.97%和60.09%；QLS 35.0及70.0 mg·kg-1·d-1组均显著抑制大鼠足肿胀（P.05），且对棉球所致肉芽组织增生有明显的抑制作用（P.05或P.01），大鼠肉芽肿的抑制率分别为32.40 %和35.65 %。

Results: Of 59 superficial bladder cancer samples, sensitivity tests were successfully performed in 45 samples, and the others failed, the successful rate was 76.3%.Diversity of inhibiting rates of antitumor drugs was observed in samples from different individuals. Except MTX in stage of G1 and G3, no correlation has been found between the phenotype of sensitivity assay and the pathological grade and stage. Sensitivity and mean inhibiting rates of antitumor drugs in the primary group were notedly higher than that in the recurrent group.The combination of two therapy agents, which have different mechanisms or different cell-cycle targets, showed significantly more sensitivity and higer mean inhibiting rates than single one in superficial bladder cancer in different individuals.

结果：14例失败，45例获得成功，总体可评价率为76.3％，不同抗癌药物对不同个体膀胱癌的抑制率存在明显差异；除MTX对膀胱癌G1和G3级平均抑制率差异有统计学意义外，其它抗癌药物对不同个体膀胱癌细胞的平均抑制率与膀胱癌的病理分级、分期均无关；抗癌药物对初发膀胱癌的敏感率和平均抑制率均高于复发膀胱癌；两种不同作用机制的抗癌药物联合应用对不同个体膀胱癌细胞的敏感率和平均抑制率均高于单一药物，二者敏感率和平均抑制率差异有统计学意义。

The extent of inhibition of depolarization by superfusion of ethanol for 5 minutes was 41.8±3.3 ％(n=17). The addition of 5 nM and 20 nM KT5720 (a selective protein kinase A inhibitor) and 250 μM H9 dihydrochloride (a non-selective protein kinase inhibitor), into the intracellular solution significantly attenuated the inhibitory effects of ethanol.

当分别将5 nM或20 nM KT5720（选择性蛋白质激酶A抑制剂）或250 μM H9 dihydrochoride（非选择性蛋白质激酶抑制剂）置入细胞内液时，乙醇的抑制作用明显被减弱；但乙醇的抑制作用不受到5 nM或20 nM calyculin A（磷酸酶1/2A抑制剂）的影响。

It is the fluorosilicic ion that exsits in the slurry and plays an important role in flotation, fluorosilicic ion not only reacted with Fe〓 on the surface of aegirine to form ionic compound, but also formed stable Si-F bond in Si-O etching reaction. Only ionic compound was obtained when it was attached to hematite surface according to the theories of coordination chemistry, Compared with SiF〓, Fatty acid ion preferentially acts with Fe〓 on the minerals surface, therefore, SiF〓 Can't obstruct the adsorption of collector on the surface of hematite completly, but can reduce the flotation recovery of aegirine selectively.

运用FTIR、XPS等测试方法仔细研究了氟硅酸盐抑制剂对含铁硅酸盐钠辉石的选择性抑制作用机理，氟硅酸盐在弱酸性条件下对赤铁矿浮选的抑制作用很微弱，而对含铁硅酸盐钠辉石强烈抑制，从而扩大了两者之间的浮选差异；SiF〓是矿浆中起抑制作用的主要成分，SiF〓不仅与钠辉石表面的Fe〓形成离子型配合物，而且还与Si-O键形成稳定的Si-F共价键，而与赤铁矿表面只能形成离子型配合物，根据晶体配位场理论，与SiF〓相比较羧酸根离子将优先与矿物表面Fe〓发生配位作用，因此SiF〓的存在并不能完全阻碍捕收剂在赤铁矿表面的吸附作用，却能够选择性地抑制钠辉石的上浮。

Wenxin capsule can promote endolethial cells releasing CO and synthesing 〓, enhance activity of HO, induce angiectasis through activating guanylic cyclase and adenglate cyclate of intracellar of vessel smooth muscle cell to enhance content of intracellar cGMP and AMP. 3. Wenxin capsule can inhibit releasing of platelet activiting factor 〓 which inhibit platelet aggregation and have antithrombosis function. 4. Wenxin capsule can promote activity of t-PA, reduce activity of PAI-1, strengthen fibrinolytic function, therefore inhibit fibrin disposition. 5. Wenxin capsule can inhibit synthesis of smooth muscle cellular DNA. Its function don't kill it directly but prevent transformation from period Go to peried S. 6. Wenxin capsule is an effective prescription of anti-coronary atherosclerosis atherosis. The results of image pattern analysis tastifies that area of lipid plaque in treating group reduce 54% and 58% in contrast with that in control group. The results of light, electro- microscopy show that structure of endolethial cell and smooth muscle cell in treating group is more integral than that in control group.

其作用机制之一是由于该药具有良好的调脂降脂作用，其不仅能明显降低血清LDL-c及升高HDL-c含量，且能有效阻止TC沉积于血管壁，从而保护内皮细胞结构完整；此外，温心胶囊尚具有明显的抗氧化作用，该药不仅能明显降低血浆LPO含量，且能提高SOD活性，同时其对血红素在细胞内代谢的调节作用也参与了抗氧化过程。2 温心胶囊能明显促进内皮细胞释放CO及合成〓，提高HO活性，通过激活血管平滑肌细胞内鸟苷酸环化酶及腺苷酸环化酶引起细胞内cGMP、AMP浓度增加而引起血管舒张。3 温心胶囊能明显抑制血小板激活因子〓的释放，从而抑制血小板聚集，抗血栓形成。4 温心胶囊能明显提高t-PA活性，降低PAI-1活性，增强纤溶功能，从而抑制纤维蛋白沉积。5 温心胶囊能明显抑制平滑肌细胞DNA合成，其抑制作用不是直接杀伤抑制，而是阻止细胞由Go期向S期转化。6 温心胶囊是抗冠状动脉粥样硬化的有效制剂，图象分析结果证实，该药治疗组脂斑面积比对照组缩小了54％和58％，光电镜结果显示内皮细胞及平滑肌细胞结构较为完整。

Results: Tyroserleutide can significantly increase the life span of H22 tumor-bearing mice by 50-70% in dosages of 20ug/kg/d-80ug/kg/d,specially the high dosage of 80ug/ml can significantly increase the life span by 69.24%; Tyroserleutide can inhibit the growth of transplanted hepatocellular tumor BEL-7402 in nude mice,the rate of tumor inhibition was25-50% in dosages of 40-320ug/ml ,the inhibition rate of 160ng/ml was 44.03%; Tyroserleutide could inhibit the growth of H22 and BEL-7402 tumor in a dose-dependent manner. Simultaneously, tumoricidal activity of tyroserleutide against BEL-7402 cell line in vitro was observed hinger when compared with the control group(P.05).The inhibition effect of 72hrs was higher than 24hrs,48hrs,96hrs.And specially the high dosage of 160ug/ml can significantly inhibit growth of tumor cell by 19.36%. Tyroserleutide can activated PEM and marked enhance cytotoxicity andphagocytosis functions in vitro and in vivo. The OD values of cytotoxicity were observed hinger when compared with the control group(P.05).The cytotoxicity of macrophages activated by tyroserleutide against BEL-7402 and B16-F10 was 35.58%,61.2% in vitro and21.39%,47.63% in vivo. The cytotoxicity rate of nude mice PEM was 32.86%,73.07% in vivo. Furthermore, tyroserleutide alone could stimulated the production of IL-1B TNF- a and NO by M . Tyroserleutide and LPS could synergistically activated M producing more cytotoxicity effectors. Conclusion: Tyroserleutide had inhibition functions against hepatoma carcinoma .Its possible mechanisms were related to the affect that Tyroserleutide could inhibit tumor cell directively and induce tumor cells apoptosis or death effectively.

结果：酪丝亮肽能显著延长腹水型肝癌H_(22)小鼠的生存时间，给药剂量为80μg／kg／d时疗效最显著，达到69.24％，在20μg／kg／d-80μg／kg／d剂量范围内生命延长率为50-70％，给药剂量与荷瘤鼠生存时间呈现一定量效关系；酪丝亮肽能显著抑制人肝癌BEL-7402移植瘤裸鼠的肿瘤生长，给药剂量为160μg／kg／d时疗效最显著，抑制率为44.03％，并且在40-320μg／kg／d剂量范围内抑制率为25-50％，给药剂量与肿瘤抑制率呈现一定量效关系；酪丝亮肽体外对人肝癌BEL-7402细胞生长有一定的抑制作用，在作用72hrs时各浓度酪丝亮肽对肿瘤细胞的抑制作用较24hrs、48hrs、96hrs明显，其中浓度为100μg／ml时抑制率达19.36％；酪丝亮肽体内外均能增强小鼠腹腔巨噬细胞对肿瘤细胞的杀伤：体外作用中巨噬细胞对BEL-7402、B16-F10的杀伤功能明显增强，与效应细胞对照组相比有显著性差异(P＜0.05)杀伤率分别达到35.58％、61.2％；体内作用中巨噬细胞对BEL-7402、B16-F10的杀伤功能明显增强，与生理盐水对照组相比有显著性差异(P 。05)，杀伤率分别达到21.39%、47.63%；裸鼠腹腔巨噬细胞经酪丝亮肤作用后对BEL一7402、B 16一F10杀伤功能明显增强，与生理盐水对照组相比有显著性差异(P.05)，最高杀伤率分别达到32.86%、73.07%；酪丝亮肤能增强单核巨噬细胞系统的吞噬功能，吞噬指数与生理盐水组比较有显著性差异(P.05)；酪丝亮肤体外作用能促进小鼠腹腔巨噬细胞分泌合成细胞毒效应分子IL一lp、TNF一Q和NO，与效应细胞对照组相比有显著性差异(P.05)；酪丝亮肤体内作用能促进小鼠腹腔巨噬细胞分泌合成细胞毒效应分子IL一lp、TNF一Q和NO，与生理盐水对照组相比有显著性差异(P.05)；酪丝亮肤能促进鼠巨噬细胞株R戌W264.7分泌合成IL一1p和NO，IL一1日、NO水平分别在酪丝亮肤作用24hrs、12hrs时达到高峰，酪丝亮肤单独应用能提高巨噬细胞的分泌合成功能，而且酪丝亮肤能与LPS协同作用刺激巨噬细胞的细胞毒效应分子分泌合成。

The fungicidal activity of methanol extract was higher than that of ethylacetate extract. The bioassay showed that the methanol extracts of strain As fermentation products had certain degree fungicidical activity against Botrytis cinerea, Alternaria longipes, Glomerella cingulata, Curvulavia lunata, Gibberella zeae, Valsa malt under the concentration of 4000μg/mL, the inhibiting ratio against pathogen growth was ranging from 62.9%~85.1%; The results of the inhibition of spore germination indicated that the fermentation products exhibited obvious inhibition rate against Alternaria longipes, the EC50 values was 62.5328μg/mL; The bioassay showed that the methanol extracts of strain As fermentation products had certain degree fungicidical activity against Bacillus cereus , Bacillus subtilis.

其中甲醇提取物的抑菌活性较乙酸乙酯好，在4000μg/mL浓度下对番茄灰霉病菌、烟草赤星病菌、苹果炭疽病菌、玉米弯孢叫斑病菌、小麦赤霉病菌、苹果腐烂病菌6种植物病原真菌均有抑制作用，抑制率在62.9%~85.1%；抑制孢子萌发试验表明：菌丝体甲醇提取物对烟草赤星病菌的毒力较好，其EC50仅为62.5328μg/mL；抑制细菌活性表明菌丝体甲醇提取物对蜡状芽孢杆菌和枯草芽孢杆菌有一定的抑制作用，而对大肠杆菌无明显的抑制作用。

However, membrane suppressors also have certain disadvantages compared to packed bed suppressors such as cost, leakage of regenerant causing higher detector background, the requirement for an external supply of regenerant solution and the fact that membrane suppressors are complex and not user serviceable.

&然而，与填充床抑制器相比，膜抑制器也有不足之处，如成本，再生剂泄漏导致更高的检测器背景，需要外部提供再生溶液，以及膜抑制器的复杂性和用户难以操作的事实等等，因此，开发低价、高性能填充床抑制器会更有益。&这正是万通致力所为！万通MSM抑制器提供十年的保用期，是现有的最成熟、尖端的填充床抑制器。

The depressing ability of the macromolecule organic depressants can be improved by the increase of their D.S.. The high D.S. CPVA and CPEG show strong depressing ability to calcite, while CPEG indicates strong depressing ability to diaspore, and HPAM to pyrite.The depressing mechanism of organic depressants was confirmed by the measurements of zeta potential, contact angles, adsorption capacity and IR spectrum.

利用动电位、接触角、吸附量和红外光谱等测试方法和手段，探讨了抑制剂的作用机理：苯氧乙酸类小分子抑制剂与方解石之间可发生较强的化学作用，可以选择性地吸附在方解石表面，使捕收剂发生解吸或阻止捕收剂在矿物表面的吸附而使矿物受到抑制；大分子抑制剂则主要是依靠亲固基吸附在矿物表面，再利用其长链的强亲水性而使矿物受到抑制。

According to the clear water experiment, aeration performance of the new equipment is good with high total oxygen transfer coefficient and oxygen utilization ratio.

曝气设备的动力效率在叶轮转速为120rpm～150rpm时取得最大值，此时氧利用率和充氧能力也具有较高值。

The environmental stability of that world - including its crushing pressures and icy darkness - means that some of its most famous inhabitants have survived for eons as evolutionary throwbacks, their bodies undergoing little change.

稳定的海底环境─包括能把人压扁的压力和冰冷的黑暗─意谓海底某些最知名的栖居生物已以演化返祖的样态活了万世，形体几无变化。