Effect of Insulin-Dependent Cytoplasmic Regulator on Murine Melanoma KML Cell Proliferation

Insulin-dependent cytoplasmic regulator (IDR), the activity of which correlates with the insulin level in blood, was isolated from rat liver and fractionated on a Sephadex G-25 column. Radioautography established that IDR stimulates by 30% proliferation of murine melanoma KML cells in culture. This is indicated by ³ H-thymidine incorporation into the cell nucleus. It is proposed that insulin stimulates proliferation of the melanoma KML cell cultures through an intracellular intermediate, IDR     

1,3-取代吲哚-2-酮衍生物的合成与肿瘤细胞毒活性研究

以苯胺为原料,通过肟化、环合生成二氢吲哚-2,3-二酮,再对其进行N-烷基化、亲核加成和磺酰化反应得到目标化合物5a～5g和7a～7e。通过¹H NMR、¹³C NMR确认其结构。采用噻唑蓝（MTT）法测试了目标化合物对乳腺癌细胞MDA-MB-231、鼠黑色素瘤细胞B16、鼠结肠癌细胞CT26三种肿瘤细胞的体外抑制活性。结果表明,化合物7d、7e具有明显的肿瘤细胞毒活性,其中化合物7d对MDA-MB-231的细胞毒活性比阳性药五氟尿嘧啶更强,IC₅₀为4.63±0.14μmol/L。本文结果可为进一步研究具有肿瘤细胞毒活性的吲哚酮类衍生物提供参考。     

Effects of Vanadyl Complexes with Acetylacetonate Derivatives on Non-Tumor and Tumor Cell Lines

Vanadium has a good therapeutic potential, as several biological effects, but few side effects, have been demonstrated. Evidence suggests that vanadium compounds could represent a new class of non-platinum, metal antitumor agents. In the present study, we aimed to characterize the antiproliferative activities of fluorescent vanadyl complexes with acetylacetonate derivates bearing asymmetric substitutions on the β-dicarbonyl moiety on different cell lines. The effects of fluorescent vanadyl complexes on proliferation and cell cycle modulation in different cell lines were detected by ATP content using the CellTiter-Glo Luminescent Assay and flow cytometry, respectively. Western blotting was performed to assess the modulation of mitogen-activated protein kinases (MAPKs) and relevant proteins. Confocal microscopy revealed that complexes were mainly localized in the cytoplasm, with a diffuse distribution, as in podocyte or a more aggregate conformation, as in the other cell lines. The effects of complexes on cell cycle were studied by cytofluorimetry and Western blot analysis, suggesting that the inhibition of proliferation could be correlated with a block in the G2/M phase of cell cycle and an increase in cdc2 phosphorylation. Complexes modulated mitogen-activated protein kinases (MAPKs) activation in a cell-dependent manner, but MAPK modulation can only partly explain the antiproliferative activity of these complexes. All together our results demonstrate that antiproliferative effects mediated by these compounds are cell type-dependent and involve the cdc2 and MAPKs pathway.     

Effect of Deacetylation on Statmhokinetic Activity of Colchicine Derivatives

Screening of colchicine derivatives that was carried out with the tumor culture CaPa in a cytotoxicity test showed that deacetylation decreases the cytotoxicity and increases the mitotic index. Lower toxicity of the deacetylated colchicine derivatives was also noted.     

哥纳三醇类似物抗A2780肿瘤细胞活性及三维定量构效关系研究

以合成的54个哥纳三醇类似物为研究对象, 测试了其体外抑制肿瘤A2780细胞株的活性, 对其中的37个化合物用比较分子力场(CoMFA)研究了哥纳三醇类似物结构与抑制A2780肿瘤细胞活性的三维定量构效关系, 提出了对哥纳香醇甲结构改造的方法, 对寻找更好活性的化合物有重要的指导意义     

香豆素及其衍生物在二甲基亚砜中的电还原性质

采用循环伏安法对香豆素及其衍生物的电还原进行研究；香豆素的电还原发生在羰基上；如果香豆素衍生物分子上含有吸电子基团，则还原电位正移；如果含有给电子基因，则还原电位负移；如果同时含有吸电子和给电子基因，则表现综合结果。     

苝酰亚胺衍生物在肿瘤治疗中的应用进展

目前恶性肿瘤已成为人类因疾病死亡的主要因素。化疗是当前肿瘤治疗的主要方式之一,然而常用的化疗药物存在诸多缺陷,如副作用大、易产生耐药性、难以监测等。开发高效低毒治疗药物是当前肿瘤治疗的研究热点之一。通过特定的纳米药物载体可提升药物在病变区域的有效浓度,提高杀伤肿瘤细胞效率,降低抗肿瘤药物毒副作用。苝酰亚胺衍生物(perylenediimides derivatives,PDI)是一种稳定性高、荧光效率优异的纳米分子材料,且易修饰,可连接特定基团,增强其生物兼容性并行使多种功能,可作为药物载体、抗肿瘤药物、荧光示踪剂等用于肿瘤诊断和治疗。本文综述PDI在药物载体、肿瘤细胞抑制剂和荧光示踪剂三方面的研究进展。为PDI应用于临床总结理论研究成果,并进一步指导其实际应用工作的开展。     

四唑及其衍生物的理论研究Ⅷ: 硝氨四唑衍生物的从头算

运用从头计算法,在HF/6-31G^*水平下,全优化计算了7种硝氨四唑衍生物的分子几何和电子结构。结果表明,标题物的四唑环近似为平面构型;2H式中性分子的芳香性大于相应的1H式异构体。5-硝氨-1H四唑分子内氢键使硝氨基与环共面;其余标题物中硝氨基与环垂直。不同水平下的总能量计算表明,标题物中电子相关效应显著;1H式中性分子较2H式的能量高,5-硝氨四唑负离子在三个负离子中最稳定。根据电荷分布阐明了四唑环质子化位置和标题物与金属的配位方式。此外还计算了各标题物的红外光谱及热力学性质。     

N-方酰麻黄碱配体的合成及催化前手性芳酮的不对称还原反应

方酸与醇反应成方酸二酯,后者与天然麻黄碱反应得到N-方酰麻黄碱或N-方酰双麻黄碱。单N-方酰麻黄碱与脂肪胺及硫氢化钠等反应合成了C-3位含氮和含硫的系列配体。首次将这些方酰麻黄碱配体经原位制备手性恶唑硼烷催化前手性芳酮及二酮的不对称还原反应,得到化学产率和e.e.值分别为85%-98%和52.5%-87.4%的手性仲醇。新化合物的结构已IR,^1H NMR,MS和元素分析所证实,化合物4b的晶体结构用X射线射确认。     

胆红素及其两亲衍生物的Langmuir-Blodgett膜研究

研究了亚相酸度和金属离子对胆红素(1)及其两个两亲衍生物胆红素二(十八烷基)酯(2)和胆红素二(十八烷基)酰胺(3)的单分子膜和LB膜性能的影响.通过π-A等温线、X射线光电子能谱、紫外-可见光谱等方法,研究了它们在有序分子膜中的分子伸展及与金属离子的配位方式.胆红素及其两亲衍生物与金属离子在有序分子膜中的配位(生成1:1型配合物)明显不同于其在本体溶液中的配位(1:1,1:2或2:1型配合物).小角X射线衍射表明1,2和3形成双层膜间距分别为2.15,5.55和5.65nm的Y型LB膜.     

Paradigms and Paradoxes: Thoughts on the Enthalpy of Formation of Guanidine and Its Monosubstituted Derivatives

Despite their seeming simplicity, substituted guanidines have not particularly caught the attention of the thermochemical community. The current paper compares the enthalpy of formation of solid substituted guanidines with correspondingly substituted benzenes, also as solids.     

石墨烯及其衍生物在食品安全监测中的应用

综述了近年来石墨烯及其衍生物构建的传感器在食品基本组成成分、食品添加剂以及食品中残留的农药、重金属、抗生素等物质分析与监测方面的应用,并展望了石墨烯的发展与应用前景。     

GLC Determination of Pseudoephedrine and Related Ephedrines in Serum as The Heptafluorobutyryl Derivatives

Abstract

A method capable of determining therapeutic blood levels of pseudoephedrine in man is described. The procedure involves partial purification by extraction, formation of the heptafluorobutyryl derivative, and electron capture detection of the prepared derivatives. Serum levels of pseudoephedrine in man are presented. Chemical reactivity, stability and gas chromatographic properties of the ephedrine derivatives are discussed.     

扁桃酸及其衍生物对映体的手性识别研究

以两种手性氨基醇作为主体,运用1H NMR分别考察其对客体7个扁桃酸衍生物对映异构体的手性识别能力。结果表明,主客体物质的量之比为1∶1时,主体诱导客体对叔丁基扁桃酸消旋体最高产生37.6 Hz的化学位移差值。     

香兰素及其主要衍生物化学性质的CNDO/2研究

用CNDO/2法研究了香兰素,并对香兰素及其三个主要衍生物的化学性质作了理论分析。结果为合成香兰素系列香料提供了理论依据。     

聚苯乙烯细胞培养板表面的糖化温敏修饰及其对细胞行为的影响

采用紫外光固定化法, 对组织培养用聚苯乙烯板进行半乳糖糖化温敏修饰. 通过红外光谱(ATR-FTIR)和X射线光电子能谱(XPS)对改性表面的化学组成及结构进行了表征, 并采用原子力显微镜(AFM)观察了改性表面形貌, 发现改性表面比未经修饰表面粗糙度增加. 静态接触角测试结果表明, 改性表面具有良好的温度响应性. 对人肝肿瘤(HepG-2)细胞在改性表面的吸/脱附行为的研究结果表明, HepG-2细胞在半乳糖糖化温敏表面表现出比在未经修饰聚苯乙烯细胞培养板表面更好的生长趋势, 当环境温度降低时, 细胞发生自动脱附, 避免了酶解法对细胞功能造成的损伤.     

Effect of Kaempferol and Its Glycoside Derivatives on Antioxidant Status of HL-60 Cells Treated with Etoposide

Kaempferol is a well-known antioxidant found in many plants and plant-based foods. In plants, kaempferol is present mainly in the form of glycoside derivatives. In this work, we focused on determining the effect of kaempferol and its glycoside derivatives on the expression level of genes related to the reduction of oxidative stress—NFE2L2, NQO1, SOD1, SOD2, and HO-1; the enzymatic activity of superoxide dismutases; and the level of glutathione. We used HL-60 acute promyelocytic leukemia cells, which were incubated with the anticancer drug etoposide and kaempferol or one of its three glycoside derivatives isolated from the aerial parts of Lens culinaris Medik.—kaempferol 3-O-[(6-O-E-caffeoyl)-β-d-glucopyranosyl-(1→2)]-β-d-galactopyranoside-7-O-β-d-glucuropyranoside (P2), kaempferol 3-O-[(6-O-E-p-coumaroyl)-β-d-glucopyranosyl-(1→2)]-β-d-galactopyranoside-7-O-β-d-glucuropyranoside (P5), and kaempferol 3-O-[(6-O-E-feruloyl)-β-d-glucopyranosyl-(1→2)]-β-d-galactopyranoside-7-O-β-d-glucuropyranoside (P7). We showed that none of the tested compounds affected NFE2L2 gene expression. Co-incubation with etoposide (1 µM) and kaempferol (10 and 50 µg/mL) leads to an increase in the expression of the HO-1 (9.49 and 9.33-fold at 10 µg/mL and 50 µg/mL, respectively), SOD1 (1.68-fold at 10 µg/mL), SOD2 (1.72-fold at 10–50 µg/mL), and NQO1 (1.84-fold at 50 µg/mL) genes in comparison to cells treated only with etoposide. The effect of kaempferol derivatives on gene expression differs depending on the derivative. All tested polyphenols increased the SOD activity in cells co-incubated with etoposide. We observed that the co-incubation of HL-60 cells with etoposide and kaempferol or derivative P7 increases the level of total glutathione in these cells. Taken together, our observations suggest that the antioxidant activity of kaempferol is related to the activation of antioxidant genes and proteins. Moreover, we observed that glycoside derivatives can have a different effect on the antioxidant cellular systems than kaempferol.     

重氮树脂与牛血清白蛋白共价结合自组装膜及其表面细胞培养

细胞支架作为组织工程的组成部分为细胞生长提供了最佳微环境 ,并对细胞生长与功能进行控制 .由于细胞对支架表面的生物识别是细胞附着、生长和增殖的基本前提 ,所以对材料表面的功能化是一个重要的课题 [1,2 ] . Shoichet等 [3 ] 通过化学反应或等离子体处理的方法 ,将蛋白质引入到材料表面而使其功能化 .基片在两种带有相反电荷的聚电解质溶液中交替吸附 ,其表面形成致密有序的超薄自组装膜 ,这种层 -层自组装技术不仅制备方法简单 ,无需特殊的设备 ,而且对膜组成和厚度能随意调控 ,以水为介质 ,对环境友好 [4～ 6] ,无疑是一项重要的表…