抑制剂

RLuciferase/Luciferin system, a new method to detect the MAPK activity in fungus, was founded and proved to be effective and perspective in the study of MAPK pathway in microorganism.

建立了一套切实可行的检测MAPK活性的荧光素酶/荧光素技术体系，并发现MAPK途径抑制剂U0126和CaM抑制剂TFP对MAPK活性都有显著的抑制作用。

The Trypsin inhibitor from Cucurbita pepo var. striaca Seeds was isolated by salting-out and chromatography of Sephadex G-50, the inhibitor activity was detected with BAPNA, the Mw was determined with SDS-PAGE and stablity was studied with different temperature, the side chains of Lys and Cys were modified.

采用分级盐析和Sephadex G-50的方法分离纯化无种皮南瓜籽胰蛋白酶抑制剂，用BAPNA法进行抑制活性的测定，用SDS-PAGE法测定蛋白质的分子量，用不同的温度处理方法对它的热稳定性进行研究，并对抑制剂的Lys和cys进行了化学修饰。

It has been demonstrated that TAK-147 is more potent and brain-specific AChE inhibition than tacrine and physostigmine, and has been approval potentiating choline acetyltransferase activity in cultured rat septal neurons more potent than donepezil, tacrine and revastigmine.

TAK－147 ｛ 3－［l一（phenylmethyl（－4－piperidinyl］－l一门，3，4，5－tetrahydro－IH－l－be.azepln－8－yi（－l－propanone umarate ｝是日本最近研制的一个选择性胆碱酯酶抑制剂。TAK－147与毒扁豆碱和他克林相比是具有更强作用和中枢选择性的胆碱酯酶抑制剂。

To investigated the relationship of the signal transduction pathway and other signal molucules, three signal transduction inhibitors were tested for their effects on L929 cell and the change of caspase activation. The inhitors include Staurosporine Quinacrine (PLA2 inhibitor) andVerapamil (Ca2+ channel blocker).

为了探讨γTNFβ和TNFβ诱导细胞凋亡的信号转导通路与其它信号分子的关系，我们检测了蛋白激酶C抑制剂Staurosporine、磷脂酶A2抑制剂Quinacrine和钙离子通道阻断剂Verapamil对γTNFβ及TNFβ杀伤L929细胞的影响及其伴随的Caspase8和Caspase3活性的变化。

For most viruses,there is aneed for antimicrobials that target unique viral molecular properties.Acycloviris one such drug.It is activated into ahuman herpesvirusDNA polymerase inhibitor exclusively by HHV kinases and,thus,does not suppress other viruses.Here,we show that ACV suppresses HIV-1in HHV-coinfected human tissues,but not in HHV-free tissue or cell cultures.However,addition of HHV-6-infected cells renders these cultures sensitive to anti-HIV ACV activity.We hypothesized that such HIV suppression requires ACV phosphorylation by HHV kinases.Indeed,an ACV monophosphorylated prodrug bypasses the HHV requirement for HIV suppression.Furthermore,phosphorylated ACV directly inhibits HIV-1reverse transcriptase,terminating DNA chain elongation,and can trap RT at the termination site.These data suggest that ACV anti-HIV-1activity may contribute to the response of HIV/HHV-coinfected patients to ACV treatment and could guide strategies for the development of new HIV-1RT inhibitors.

对大多数病毒而言，都需要有针对其分子特性的靶向杀毒剂阿昔洛韦就是这样一种靶向药物在人疱疹病毒酶的特定作用下，阿昔洛韦被激活成为人疱疹病毒DNA聚合酶抑制剂，因此不能再抑制其它的病毒我们的研究发现阿昔洛韦在共感染人疱疹病毒的组织中可以抑制HIV-1，但在无人疱疹病毒感染的组织或细胞中无此作用然而，加入人疱疹病毒-6感染的细胞却使得其对抗HIV的阿昔洛韦变得敏感我们推测这种抑制作用依赖于人疱疹病毒酶导致的阿昔洛韦磷酸化实际上，单磷酸化的阿昔洛韦前体药物无需人疱疹病毒的参与即可抑制HIV此外，磷酸化的阿昔洛韦能直接抑制HIV-1逆转录酶，将其阻止在终止位点，从而终止DNA链的延长这些结果提示阿昔洛韦的抗HIV-1活性决定了艾滋病病毒/人疱疹病毒共感染的患者对阿昔洛韦的治疗反应，也有助于开发新的HIV-1逆转录酶抑制剂

The ventilatory responses of peripheral chemoreflex following 0.1 m l microinjection within the NTS of either PTK inhibitor genistein(10 mol/L), AMPA glutamate receptor inhibitor CNQX (10 mol/L),or inactive PTK inhibitor daidzein (10 mol/L) were recorded.

在孤束核处分别微量注射蛋白酪氨酸激酶的抑制剂genistein和其非活动性抑制剂daidzein 以及 AMPA受体阻断剂CNQX，观察这些药物对外周化学感受性反射的影响。

This study aims at the expression of Wnt signaling pathway inhibitor FrpHE and DKK-1 induced by ectogenous factor.

本课题的目的在于研究外源性因素对Wnt通路抑制剂FrpHE和DKK-1的诱导表达，我们选择抗癌药物p53及化疗药阿霉素、羟喜树碱、顺铂作为外源性诱导剂，以期弄清Wnt通路及其抑制剂FrpHE和DKK-1是否能够被p53和化疗药这两类药物所调节。

PART 2:The molecular mechanisms of Nontypeable Haemophilus influenzae induced inflammatory response in respiratory epithelial cells Objective:Nontypeable Haemophilus influenzaewas traditionally considered as an extracellular pathogen in respiratory infections.In this study,we established a model of infected cells to confirm NTHI was also a facultatively intracellular pathogen.Mitogen activated protein kinasesare the important signal transduction pathway in mediating inflammatory response induced by NTHI in respiratory epithelium.In this study,we elucidate the impact of NTHI,and its SCF and EP on the expression of MAPK and subsequent proinflammatory mediators.

第二部分：NTHI致呼吸道上皮细胞炎症反应的分子机制研究目的：通过建立呼吸道上皮细胞株的体外NTHI感染模型，确认NTHI在细胞内的存活，观察NTHI及其组分(可溶性胞质成分SCF、外膜蛋白EP)对呼吸道上皮细胞MAPK信号传导通路和后续的前炎症因子表达的影响，并应用特异性ERK-MAPK抑制剂U0126、p38 MAPK抑制剂SB203580特异性阻断下游MAPK信号传导通路，观察它们对呼吸道上皮细胞分泌前炎症因子表达的影响。

Fie years after initiation of treatment, 79% patients were still on renin-angiotensin inhibitors, 65% on -blockers, 56% on spironolactone, and 83% on statins. Notably, multiple drug treatment and increased seerity of heart failure was associated with persistence of treatment. Nonpersistence with renin-angiotensin inhibitors,-blockers, and statins was associated with increased mortality with hazard ratios for death of 1.37 (95% CI, 1.31 to 1.42), 1.25 (95% CI, 1.19 to 1.32), 1.88 (95% CI, 1.67 to 2.12), respectiely.

开始治疗5年后，有79％病人继续使用肾素血管紧张素抑制剂，65％用阻滞剂，56％用安体舒通，83％使用他汀类，值得注意的是，联合用药和心衰的加重同坚持治疗相关，无法坚持使用肾素血管紧张素抑制剂，阻滞剂，安体舒通，他汀类药物的病人同增加的死亡率相关，其死亡危险比分别为1.37 (95%可信区间， 1.31 － 1.42)， 1.25 (95%可信区间， 1.19 － 1.32)， 1.88 (95%可信区间， 1.67 － 2.12)，。

The synergism ratios of piperonyl butoxide to alpha-cypermethrin in these three strains were similar(about 20-fold), which suggested metabolic detoxification probably confers about 20-fold inherent resistance in the B-type whitefly, as PBO is a mixed function oxygenase and esterase inhibitor and glutathione S-transferase is not affinity to resistance in B. tabaci. The synergism ratio of triphenyl phosphate to alpha-cypermethrin in the NJ strain was 12-fold, which implied the synergism of PBO in the B-type whitefly is mainly due to inhibiting esterase activity.

增效试验表明PBO对这三个品系的增效作用均为20倍左右，因为在烟粉虱中PBO即是多功能氧化酶抑制剂，也是酯酶抑制剂，而谷胱甘肽S-转移酶与抗性无关，因此推断代谢酶在B型烟粉虱对高效氯氰菊酯的抗性发展中起到的相对作用可能为20倍左右，而且这种抗性是B型烟粉虱天生的；TPP对NJ品系的增效作用为12倍，说明PBO增效作用主要是由于抑制酯酶而引起的，即代谢抗性大部分由酯酶所贡献。

Do not gum up the work by telling mother what we are going to do .

别告诉母亲我们要干的事，那会把事情搞糟的。

In recent years, application of the partial prestressed concrete beam s is developed.

近年来，随着部分预应力砼梁应用的推广，发现我国规范所采用的名义拉应力法的计算结果不稳定。