合成因子

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。

It starts transmitting information by integrating with lagen and stromatin by irritating osteocytes and chondrocytes to form rapidly extracellular matrix so as to promote repair of bone and cartilage injury.

转化生长因子β通过刺激骨、软骨细胞合成胶原和基质蛋白，快速形成细胞外基质，达到其促进骨、软骨损伤修复的作用。

Annual average temperature and average temperature in January mainly affected accumulation of oleic and linoleic.

年平均气温和1月平均气温是影响油酸和亚油酸合成的主要因子。

Average annual relative humidity and annual average temperature mainly affected accumulation of linolenic.

年平均相对湿度和年平均气温是影响核桃亚麻酸合成的主要生态因子。

Thyroid hormone responsive spot 14, expressed in lipogenic tissues, is suggested as a transcription factor to regulate gene expression of rate-limiting enzymes in lipogenesis. Two THRSP isoforms, THRSPα and THRSP β, were detected at cDNA levels in chickens and ducks.

甲状腺激素应答Spot 14 (Thyroid hormone responsive spot14， THRSP)是一个参与多种脂肪合成限速酶基因表达的转录调控因子，在动物肝脏、乳腺和脂肪组织中高度表达。

There are four kind of isoforms of endothelin in human and other mammals named ET-1, ET-2, ET-3 and ET-β, which are slightly different in construction and pharmacological effect. In human beings, ET-1 is the dominative subtypes. ET-1 remains in blood at a low level about 5ng per liter on physical state. It is synthesized, stored, released and metabolized locally. The half-life of ET-1 is about 1 hour. ET-1 is the most potent vasoconstrictive factor till now, and it is more functional in vein than in artery. In vascular bed, there are two kind of ET receptors. Type A mainly located in smooth muscle cells, whereas type B in endothelial cells. The latter can stimulate intimal hyperplasia via a parasecretion way and activate some oncogenes such as c-fos and c-myc and then enhance their expression. These alterations result in constriction of blood vessels, thus the SMC steps into proliferate state from silent state.

人及哺乳动物体内有四种结构及药理学性质略有差异的异物体，分别为ET-1、ET-2、ET-3、ET-β，而在人主要是ET-1，在生理条件下，ET-1在血浆中含量较低，约为5ng〓，故ET-1不是一个循环激素，而是局部合成释放，局部起作用的活性物质，半衰期约1小时，ET-1是目前已知的最强的血管收缩剂，对静脉的作用比动脉强，在血管床，ET受体有A、B两型，A型主要分布在平滑肌细胞，B型主要分布在内皮细胞，它可以通过旁分泌途径刺激内膜增生，具有有丝分裂原效应，可以激活某些癌基因如C-fos、C-myc使其表达增强引起血管收缩，使静止期SMC进入增殖期，还可以通过信号传导途径，与bFGF、GTF-β、PDGF等生长因子协同作用，起共有丝分裂原作用。

The first, selecting Mannitol of polyhydric and Dextran ofpolysaccharide as subsidiary material, In accordance with differentusing quantities, making up eight recipes, freeze-drying test is madewith eight recipes differently. By adjusting recipe, to select themethod of two factors three levels. The best recipe determined is thatof Mannitol(160mg/bottle) and Dextran(40mg/bottle), Solving theproblem of description、moisture(≤1.5%)、solution(≤6s)、stability(95.0～110.0%) etc., The quality of preparation has beenimproved.

首先，选择赋形剂多元醇类的甘露醇和多糖类的右旋糖酐作为辅料，按照不同的用量，组合成8种处方进行冷冻干燥试生产，采用二因素三水平的满因子分析法，通过处方调整，确定甘露醇160mg／瓶、右旋糖酐40mg／瓶为最佳处方，解决了冻干制剂在性状、水分(≤1.5％)、溶解性(≤6s)和含量稳定性(95.0～110.0％)等方面的不足，提高了产品质量。

To observe the effect of diterpenoid compound 5F from Pteris semipinnata L.(5F) on the cell proliferation, collagen synthesis and the expression of connective tissues growth factor in human pterygium fibroblasts cultured in vitro.

观察半边旗二萜类化合物5F(5F)对体外培养的人翼状胬肉成纤维细胞增殖和胶原合成及结缔组织生长因子表达的影响。

A gelator (G2) synthesized from 1,2,4,5-benzene tetracarboxylic acid and 4-hydroxy pyridine at molar ratio of 1:4 was characterized by 1H-NMR and FT-IR.

采用1H-NMR和FT-IR表征了在摩尔比1：4条件下，由均苯四甲酸和对羟基吡啶合成的一种凝胶因子(G2)。

The mechanism may be it can interference the thermotaxic center, descend the level of plasma cellular factor TNF - one of the endogenous pyrogens, inhibit the synthesis and release of central febril media PGE〓 and cAMP.

其机理可能与直接干扰体温调节中枢作用，降低血浆中作为内生致热原之一的细胞因子TNF水平，抑制中枢发热介质PGE〓、cAMP的合成释放等有关。

As she looked at Warrington's manly face, and dark, melancholy eyes, she had settled in her mind that he must have been the victim of an unhappy attachment.

每逢看到沃林顿那刚毅的脸，那乌黑、忧郁的眼睛，她便会相信，他一定作过不幸的爱情的受害者。

Maybe they'll disappear into a pothole.

也许他们将在壶穴里消失