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《理化检验(化学分册)》2010,(11)
采用荧光光谱法研究丹参酮Ⅰ(TSNⅠ)与人血清白蛋白(HSA)结合反应的特征。试验发现:丹参酮Ⅰ对人血清白蛋白有较强的荧光猝灭作用。根据由Stern-Vol mer方程和Lineweaver-Burk双倒数方程得到的荧光猝灭常数,判断由于与丹参酮Ⅰ反应而导致人血清白蛋白的荧光猝灭属静态猝灭。并从所计算得到的热力学参数ΔH和ΔS,推断人血清白蛋白与丹参酮Ⅰ反应的结合力为静电力。根据同步荧光光谱研究的结果表明:人血清白蛋白的构象不因与丹参酮Ⅰ反应而改变。 相似文献
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运用荧光光谱、紫外光谱和计算机模拟分子对接等技术,研究了在模拟生理条件下还原型辅酶烟酰胺腺嘌呤二核苷酸(NADH)与人血清白蛋白(HSA)的作用方式及热力学特征。结果表明,NADH与人血清白蛋白的荧光猝灭机理属于静态猝灭;NADH与HSA在温度283K和310K时的结合常数和结合位点数分别为1.972×104 L.mol-1、0.9657和1.468×104 L.mol-1、0.9105,通过热力学计算得到反应的热力学参数;同步荧光光谱表明NADH使色氨酸残基的微环境亲水性增强;分子模型研究表明,二者通过疏水力、静电力和氢键共同作用结合。 相似文献
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用荧光光谱、紫外吸收光谱和圆二色谱等光谱学方法研究在近似生理条件下咖啡因与人血清白蛋白(HSA)的结合作用.实验结果表明咖啡因与人血清白蛋白的结合主要是动态猝灭过程,并获得了不同温度下,咖啡因与人血清白蛋白的结合位点数,结合常数以及△H、△G和△S等热力学参数.根据所得结果可推断咖啡因与人血清白蛋白的作用力主要是氢键和范德华力,由FRET能量转移理论计算出咖啡因与人血清白蛋白间的结合距离.同时用同步荧光光谱、圆二色谱和三唯荧光光谱,考察了咖啡因对人血清白蛋白二级结构的影响. 相似文献
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光谱法测定伊曲康唑与牛血清和人血清白蛋白相互作用 总被引:3,自引:0,他引:3
用荧光光谱和紫外吸收光谱法, 在pH=7.4±0.1的0.1 mol·L-1磷酸缓冲溶液中, 研究了伊曲康唑与牛血清白蛋白(BSA)和人血清白蛋白(HSA)的相互作用. 实验结果表明, 伊曲康唑与牛血清白蛋白和人血清白蛋白作用的猝灭常数均随着温度的升高而降低, 伊曲康唑可以有规律地使血清白蛋白内源荧光猝灭, 其猝灭机理可认为是伊曲康唑与白蛋白形成复合物的静态猝灭. 获得了在不同温度下, 伊曲康唑与血清白蛋白作用的结合常数以及△G、△H和△S等热力学参数. 根据所得结果可推断伊曲康唑与白蛋白的作用力主要为疏水作用力, 同时, 利用荧光共振能量转移理论(FRET)计算得出了伊曲康唑与白蛋白结合位置的距离d. 而且, 利用同步荧光光谱和紫外光谱揭示了该反应中蛋白的结构和其微环境的变化. 相似文献
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采用荧光光谱研究了模拟生理务件下抗精神病药布南色林与人血清白蛋白的相互作用,结果表明,布南色林对人血清白蛋白的内源性荧光具有猝灭作用且猝灭方式为静态猝灭.布南色林与人血清白蛋白形成了1∶1的复合物,结合常数K=1.80×104L/mol,且金属离子对结合反应具有较显著的影响.根据不同温度下的热力学函数确定了布南色林与人血清白蛋白的相互作用力类型以氢键和范德华力为主.同步荧光光谱和傅立叶变换红外光谱表明布南色林对人血清白蛋白二级结构的含量产生影响,α-螺旋和β-折叠的含量降低,β-转角和无卷曲规则的含量明显升高. 相似文献
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Uroš Grošelj Mojca Žorž Amalija Golobič Branko Stanovnik Jurij Svete 《Tetrahedron》2013,69(52):11092-11108
A new and simple synthesis of novel N-protected methyl 5-substituted-4-hydroxypyrrole-3-carboxylates, which exist in equilibrium with their 4-oxo tautomers, has been developed in two steps starting from N-protected α-amino acids. The key intermediates are enaminones, which can also be isolated, characterized, and used for the construction of other functionalized heterocycles, before they spontaneously decompose to pyrrole products. 4-Hydroxypyrroles are prone to partial aerial oxidation but can be efficiently alkylated or reduced to stable polysubstituted pyrrolidine derivatives. 相似文献
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The chemoselectivity in the intramolecular CH insertion of various diazosulfonamides has been experimentally studied. The results reveal that the aliphatic 1,4-, 1,5-, or 1,6-C(sp3)?H insertions of diazosulfonamides are not accessible, while the aromatic 1,5-C(sp2)?H insertion can be realized specifically by adjusting the diazo-adjacent group. In addition, the general chemoselectivities in the intramolecular CH insertions of diazosulfonyl compounds are summarized. Generally, diazosulfones undergo both aromatic 1,5-C(sp2)?H and aliphatic 1,5- and 1,6-C(sp3)?H insertions, while diazosulfonates undergo aliphatic 1,5- and 1,6-C(sp3)?H insertions. However, diazosulfonamides only undergo aromatic 1,5-C(sp2)?H insertion. 相似文献
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N-Heterocyclic carbene-palladacyclic complexes 3 were successfully achieved in a one-pot procedure under mild conditions. The structure of 3a was unambiguously confirmed by X-ray single crystal diffraction and it was an active catalyst in the Buchwald-Hartwig amination and α-arylation of ketones even at very low catalyst loadings (0.01?mol%). 相似文献
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Shashikant U. Dighe Surya K. Samanta Shivalinga Kolle Sanjay Batra 《Tetrahedron》2017,73(17):2455-2467
An efficient iodine-mediated oxidative Pictet-Spengler reaction in dimethyl sulphoxide (DMSO) using terminal alkynes as the 2-oxoaldehyde surrogate for the synthesis of aryl (9H-pyrido[3,4-b]indol-1-yl)methanones is described. The scope of the protocol includes the total synthesis of Fascaplysin, Eudistomins Y1 and Y2. The methodology is extended for preparing pyrrolo[1,2-a]-quinoxaline and indolo[1,5-a]quinoxaline derivatives. The utility of 1-aroyl-β-carbolines was demonstrated by performing palladium-catalyzed β-carboline directed ortho-C(sp2)-H functionalization of the phenyl ring with thiomethyl (SMe) group using DMSO as source and for accessing 4-aryl-canthin-6-ones. 相似文献
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In this Letter, we described a facile method for constructing fused bicyclic 1-arylpyrazol-5-one ring system. We employed various methylene-containing carboxylic acids as the substrates and proved that the pyrazolone ring closure requires activated methylene group in intermediate II. Accordingly, a series of structurally diversified, fused bicyclic 1-arylpyrazol-5-ones was prepared in moderate to high yields using the requisite substrates. 相似文献
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Synthesis of substituted pyrrolo[1,2-a]pyrazines and pyrazino[1,2-a]indoles from the Morita-Baylis-Hillman derivatives of acrylates via saponification followed by Curtius reaction is described. 相似文献
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用正丁胺作为碳源,采用射频辉光放电制备碳膜,选用激光染料R6G和聚乙二醇混合液作为蒸气源,采用单源热蒸发,在蒸发室与染料同时沉积得到混合膜,用拉曼光谱和红外光谱分析了碳膜的结构和键合方式,分析表明:碳膜中存在胺基团和氢原子.混合膜的荧光谱测量结果表明,认为正丁胺对染料荧光谱的影响是因为胺基和氢原子的存在. 相似文献
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Jona Mirnik Eva Pušavec Kirar Sebastijan Ričko Uroš Grošelj Amalija Golobič Franc Požgan Bogdan Štefane Jurij Svete 《Tetrahedron》2017,73(24):3329-3337
A series of 20 CuAIAC reactions between eight 4-acylamino substituted pyrazolidine-3-one-1-azomethine imines and four terminal ynones were performed using Cu0 as catalyst. The corresponding fluorescent cycloadducts were obtained in very high yields upon simple workup. Thus, Cu-metal turned out to be a better catalyst than CuI in terms of yield and ease of isolation. Availability of azomethine imines, mild reaction conditions, and simple workup enable a “click” access to libraries of densely substituted 2,3-dihydro-1H,5H-pyrazolo[1,2-a]pyrazol-1-ones. Reactivity of differently substituted dipoles was evaluated experimentally and by quantum chemical methods (DFT). 相似文献
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George E. Magoulas Thomas Garnelis Constantinos M. Athanassopoulos Dionissios Papaioannou George Mattheolabakis Konstantinos Avgoustakis Dimitra Hadjipavlou-Litina 《Tetrahedron》2012,68(35):7041-7049
(E)-4-(Fullerenopyrrolidin-1-yl)-3-methylbut-2-enoic acid and its corresponding succinimidyl ester, readily obtained through Prato-type modification of C60, were used for the selective N-acylation of polyamines. The thus obtained conjugates were evaluated for their antioxidative and anti-inflammatory activity and their cytotoxicity was determined. Members of this family of compounds showed interesting anti-lipid peroxidation, anti-lipoxygenase and anti-inflammatory activity and comparable cytocompatibility to spermidine. 相似文献