被抑制的

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。

The effects on mouse's ileum can totally been inhibited by atropine, eserine, fugutoxin, and morphine.

对小鼠回肠的作用可完全被阿托品抑制，或被毒扁豆碱、河豚毒素或吗啡抑制。

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。

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 effect of genistein (0.8 mg/kg) was partially inhibited by L-NAME, or by sodium orthovanadate (50 μg/kg), a potent inhibitor of protein tyrosine phosphatase;(2) genistein also decreased the PP of renal vascular bed in a dose-dependent manner and the effect of genistein was completely inhibited by pretreatment with sodium orthovanadate, but unaffected by L-NAME; and (3) genistein decreased the PP of mesenteric vascular bed in a dose-dependent manner, an effect which was partially inhibited by sodium orthovanadate, but unaffected by L-NAME.

GST的这一效应可被L-硝基精氨酸甲酯部分阻断，预先注射蛋白酪氨酸磷酸酶抑制剂正钒酸钠(50 μg/kg)，可部分抑制GST (0.8 mg/kg)引起的效应；(2)向肾血管灌注环路中直接注射 GST 也可剂量依赖性地降低肾动脉的灌流压，预先注射正钒酸钠可完全抑制GST引起的效应，而L-NAME对此效应没有影响；(3)肠系膜血管灌流环路中注射GST可剂量依赖性地降低其灌流压，这一效应可被正钒酸钠部分抑制，而L-NAME对此无影响。

The effect of genistein (0.8 mg/kg) was partially inhibited by L-NAME, or by sodium orthovanadate (50 μg/kg), a potent inhibitor of protein tyrosine phosphatase;(2) Genistein also decreased the PP of renal vascular bed in a dose-dependent manner. The effect of genistein was completely inhibited by pretreatment with sodium orthovanadate, but unaffected by L-NAME;(3) Genistein decreased the PP of mesenteric vascular bed in a dose-dependent manner, an effect which was partially inhibited by sodium orthovanadate, but unaffected by L-NAME.

GST的这一效应可被L-硝基精氨酸甲酯部分阻断，预先注射蛋白酪氨酸磷酸酶抑制剂正钒酸钠(50 μg/kg)，可部分抑制GST (0.8 mg/kg)引起的效应；(2)向肾血管灌注环路中直接注射 GST 也可剂量依赖性地降低肾动脉的灌流压，预先注射正钒酸钠可完全抑制GST引起的效应，而L-NAME对此效应没有影响；(3)肠系膜血管灌流环路中注射GST可剂量依赖性地降低其灌流压，这一效应可被正钒酸钠部分抑制，而L-NAME对此无影响。

The HE activity was almost completely inhibited by SBTI, p-APMSF, bestatin and NEM, greatly inhibited by ovomucoid, TLCK, IAM, chymostatin and PMSF, and slightly inhibited by pepstatin A, TPCK, LBTI and leupeptin. And these results imply that HE is most probably a trypsin-type serine protease.

抑制剂对其酶活性的影响结果显示，该孵化酶的活性几乎可被SBTI、p-APMSF、Bestatin和NEM所完全抑制，被ovomucoid、TLCK、IAM、chymostatin和PMSF所强烈抑制，而对pepstatin A、TPCK、LBTI和leupeptin不敏感，表明该酶极可能是一种属于胰蛋白酶类型的丝氨酸蛋白酶。

According to the results, the germicidal efficacy was influenced by the concentration of ethanol, concentration of Tryptone Soy Brothculture medium and contact time of bacatericide. The optimal treatment for inhibition of the growth of pathogenic bacteria bioflims by ethanol was: ethanol concentration of 70%, contact time of 40 min and in 0%TSB.

实验结果表明，乙醇浓度、胰酶大豆肉汤培养基浓度、作用时间均能影响抑制病原菌生物被膜，乙醇抑制生物被膜细菌生长的最佳条件为：乙醇浓度70%，处理时间40 min，TSB浓度为0。

The agglutination for rabbit was the highest among erythrocytes of human, rabbit, common carp and crucian carp. The hemagglutinating activity for rabbit could not be inhibited by D-fructose, D-mannose, D-galactose, glucose, sucrose, manrmn, gamma-globulin and egg albumin, but inhibited by bovine-thyroglobulin, and the minimum inhibitory concentration was 3.10 mg/ml.

该凝集素可以凝集人的A、B、AB、O型红细胞，且凝集活性相同，在对人、兔、鲤、鲫的红细胞的凝集作用中，对兔红细胞的凝集作用最强，且不被己测试的D-半乳糖、D-果糖、D-甘露糖、葡萄糖、蔗糖、甘露聚糖、γ-球蛋白、卵清蛋白所抑制，仅被牛甲状腺球蛋白抑制，最小抑制质量浪度为3.10mg/ml。

The majority of BA tested didn′t contract to NE, only a small number of BA contracted to NE but with obvious lower afficacy, lower affinity and tachyphylaxis to NE than RA.

按研究BA和RA平滑肌V〓受体时我们发现，尽管BA和RA在V〓受体的分布上没有差别，但在无钙介质中，AVP引起的收缩在BA则被明显抑制，而在RA则仅被轻度抑制。

The split between the two groups can hardly be papered over.

这两个团体间的分歧难以掩饰。

This approach not only encourages a greater number of responses, but minimizes the likelihood of stale groupthink.

这种做法不仅鼓励了更多的反应，而且减少跟风的可能性。