抗抑制剂

Many antibodies against pro-inflammatory cytokines and inhibitors of inducible NO synthase have been produced, but most of them are agents targeting one factor and cant efficiently block the development of systemic inflammation.

尽管已经研制出许多抗促炎细胞因子抗体及诱生型NO合酶(inducible NO synthase，iNOS)抑制剂等，但多为单因素抗炎制剂，不能有效地阻断全身性炎症的发展。

There are two main classes of antidepressant used for treating cataplexy - the Tricyclic antidepressants and the Selective Serotonin Reuptake Inhibitors.

主要有两种类别的抗抑郁药用于治疗猝倒-三环抗抑郁药和选择性血清素再吸收抑制剂。

After careful studying their relative importance to immune response and the possibility of the match, seventeen sequences of interest were selected for further experiment, including ESTss analogous to 11.5KD antibacterial peptide, lysozyme, serine protease and its inhibitor, lectin, antifreeze protein, et al. Primers designed according to the sequences were used to amplify the corresponding ESTss from both blood and cephalothorax cDNA library.

在仔细分析了它们在免疫系统中的重要性和在对虾中出现的可能性之后，从中选出了17条可能编码抗菌肽，溶菌酶，凝集素、丝氨酸蛋白酶及其抑制剂，抗冻蛋白等蛋白质的序列，以此为依据设计引物，在中国对虾的血液和头胸部cDNA文库中扩增相应的序列。

The calmodulin antagonists (calmidazolium, W7agarose) and anticalmodulin serum had inhibitory effect on the extracellular reduction of ferricyanide with their concentration that yielded 50% inhibition were 1.5 μmol/L, 10 μmol/L and 10 mg/L respectively.

结果表明，大分子的CaM抑制剂W7agarose、小分子抑制剂calmidazolium及CaM的抗血清对跨质膜铁氰化钾的还原均有不同程度的抑制作用，半抑制浓度分别为10μmol／L、1.5μmol／L和10mg／L。

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

Studies also indicated that genistein exsists not only in soybeans but also in many kinds of plants such as vegetables and fruits.As a potential anticancer agent, the actional mechanisms of genistein mainly includes as follows:First, genistein can depress the activity of protein tyrosine kinase and transduction pathways for the phosphorylation of receptors and mitosis signal. So genistein can lead to cells' proliferation depressed. Second, genistein has minimal effects of phytoestrogens. It can be combined with estrogen receptor and improve the synthesis of cellular sex hormone binding glulobin, and improve the activity of UDP-glucuronyl transferase. Through these pathways, it can inhibit the cell activity of breast cancer and prostate cancer.

作为一个很有潜力的抗肿瘤物质，三羟异黄酮的作用机制主要包括：①抑制蛋白酪氨酸激酶活性，可阻抑PTK引起的受体磷酸化和有丝分裂的信号传递，导致癌细胞增殖受抑；②弱雌激素作用：可通过与体内雌激素受体结合，并可增加细胞内性激素结合球蛋白的合成，增加UDP-葡糖醛酸转移酶的活性等途径抑制乳腺癌和前列腺癌细胞活性；③拓扑酶Ⅰ和Ⅱ抑制剂，抑制细胞活性；④上调细胞周期性负性调节因子P21WAF1/CIP1的表达，使之负性调节因子作用增强；⑤可阻止胰岛素样生长因子-Ⅰ、肝细胞生长因子和神经生长因子的作用而抑制肿瘤生长；⑥其他：抗氧化作用、抑制热休克蛋白、诱导细胞凋亡、抑制新生血管生成和抑制多种耐药相关蛋白等。

Alpha-1 antitrypsin is the most abundant circulating protease inhibitor in the body, Dr. Lomas said. Its most common deficiency mutation is the Z allele, where the amino acid lysine is exchanged for glutamic acid at position 342 in the polypeptide chain (Glu342Lys). About 1 in 1700 whites of northern European descent are homozygotes for this mutation and thus have plasma antitrypsin levels that are 10% to 15% below normal, he said.

Lomas博士表示，甲一型抗胰蛋白酵素是身体内最充分的循环蛋白酶抑制剂，最常见的缺损突变在Z对偶基因，该处的胺基酸 lysine与麸氨酸在多胜肽链的第342位置交换(Glu342Lys)；北欧血统白人每1，700人有1人是此一突变的同合子，因此血浆抗胰蛋白酵素值比正常低10%到15%。

Canavalia ensiformis protein has relatively high nutritional value,but the unprocessed Canavalia ensiformis protein contains a number of anti nutritional factors such as hemagglutinin ,trypsin inhibitors that limit its used as human food and animal feed.

洋刀豆蛋白是一种具有较高营养价值的植物蛋白质，但是其中含有的一些抗营养因子，如血球凝集素(ConcanavalinA ，简称ConA)、胰蛋白酶抑制剂等，限制了它在人类食用植物蛋白和动物饲料中的应用，其中ConA是最主要的抗营养因子。

Several anti-tumor cell lines and carbonic anhydrase Ⅱ model were established. More than 10000 compounds and extracts from plants were screened using these models and about 10 compounds showed strong inhibitory activities. Two species of plants Inula helianthus-aquatica and Saussurea deltoidea were chosen to investigate chemical and bioactivity constituents based on the results of screening of extracts and fractions. 58 compounds were isolated and identified from these two plants, 6 compounds were found to be new and 14 compounds showed anti-tumor activities. We also studied the anti-tumor mechanism of the compound bigelovin isolated from Inula helianthus-aquatica. Bigelovin was found with apoptotic activity against cell line U266 by lowering the amount of important transcription factor E2F-1 which inhibits the cell cycle at G0/G1 stage. Docking study on 7 natural new phenolic inhibitors of CA Ⅱ and 3D-QSAR study on 61 sulfonamide inhibitors of CA Ⅱwere also investigated. The calculated results were in good correlation with experimental results.

基于以上两种重要疾病和研究组方向，本论文工作开展了多个肿瘤细胞株和碳酸酐酶Ⅱ靶标模型的建立和筛选工作，累计筛选1万多个/次样品，发现10余个活性较强化合物；从粗提取物筛选结果中选取两种抗肿瘤活性强的菊科植物水朝阳旋覆花(Inula helianthus-aquatica)和三角叶凤毛菊进行了系统化学和活性成分研究，分离鉴定了58个化合物，发现6个新化合物和14个抗肿瘤活性化合物；通过合作对水朝阳旋覆花中活性较强的bigelovin进行了抗肿瘤作用机制研究，发现它可能是通过降低G2期重要的转录因子E2F-1，致使细胞周期阻滞在G0/G1期，引起多发性骨髓瘤U266细胞凋亡；开展了7个新的天然酚类CAⅡ抑制剂的对接研究和61个合成的系列磺酰胺类CAⅡ抑制剂的3D-QSAR分析，结果表明计算与实验一致。

Rabeprazole belongs to a class of antisecretory compounds ( benzimidazole proton-pump inhibitors) that do not exhibit anticholinergic or histamine H2 -receptor antagonist properties, but suppress gastric acid secretion by inhibiting the gastric H +/K +-ATPase at the secretory surface of the gastric parietal cell.

雷贝拉唑属于抗分泌药物，苯并咪唑的替代品，质子泵抑制剂。不具有抗胆碱活性和组胺h2受体拮抗活性，但是能够胃壁细胞分泌表面的H +/K +-ATPase而抑制胃酸分泌。

Breath, muscle contraction of the buttocks; arch body, as far as possible to hold his head, right leg straight towards the ceiling (peg-leg knee in order to avoid muscle tension).

呼气，收缩臀部肌肉；拱起身体，尽量抬起头来，右腿伸直朝向天花板（膝微屈，以避免肌肉紧张）。

The cost of moving grain food products was unchanged from May, but year over year are up 8%.

粮食产品的运输费用与5月份相比没有变化，但却比去年同期高8％。