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1.
为了寻求杀菌剂的新的先导化合物,用姜黄素、甲醛和仲胺发生Mannich反应得到8个新的姜黄素Mannich碱衍生物,其结构经IR,1H NMR,13C NMR,MS和元素分析所表征.初步抑菌实验结果表明,所有姜黄素Mannich碱衍生物与姜黄素对比,对枯草杆菌、金黄色葡萄球菌、大肠杆菌、青霉、黑霉有更好的抑菌效果.这些结果表明含有哌嗪环的姜黄素Mannich碱抑制霉菌的活性明显(16.88~21.34 mm).  相似文献   

2.
吴文鹏  曹艳 《化学研究》2014,25(6):609-615
用密度泛函理论优化了三苯甲烷(1)和一系列三(4-硝基苯基)甲烷衍生物2,3和4的几何结构,并计算了其红外光谱和拉曼光谱;通过与实验光谱的对比,对实验光谱中的谱峰进行了指认,并从理论上纠正了部分对3和4红外光谱谱峰不合适的实验指认;同时预测了2,3和4的拉曼光谱.结果表明,几种化合物的振动光谱计算结果与相应的实验结果吻合良好;且化合物2,3和4的拉曼光谱具有相似性.  相似文献   

3.
以乙醇为溶剂,用姜黄素、溴乙烷和稀土盐等为原料,合成了二乙基姜黄素镧(Ⅲ)和钐(Ⅲ)配合物,通过IR,1HNMR,MS和元素分析对目标化合物进行了结构表征;并对它们的紫外可见电子光谱、单、双光子荧光光谱进行了研究,同时采用1064nm皮秒脉冲激光通过Z扫描技术拟合得到了双光子吸收系数和吸收截面.结果显示目标物具有较好的光学性质和双光子吸收截面.  相似文献   

4.
姜黄素-N-取代吡唑类衍生物合成及抑菌活性   总被引:1,自引:0,他引:1  
为了寻求杀菌剂的新的先导化合物,用姜黄素与取代酰肼反应得到13个新的姜黄素-N-取代吡唑类衍生物,其结构经IR,1H NMR,13C NMR,MS和元素分析所表征,初步抑菌实验结果表明,在1×10-4mol/L浓度下,所有衍生物与姜黄素对比,对枯草杆菌、金黄色葡萄球菌、大肠杆菌、青霉、黑霉有较好的抑菌效果.其中,3,5-二(4-羟基-3-甲氧基苯基乙烯基)-N-脒基吡唑(3c),3,5-二(4-羟基-3-甲氧基苯基乙烯基)-N-(苯并噻唑-2-硫基乙酰基)吡唑(3k),3,5-二(4-羟基-3-甲氧基苯基乙烯基)-N-(香豆素-3-甲酰基)吡唑(3m)有优异的抑菌效果(抑菌圈16.34~23.81 mm).这些结果表明含有噻唑环、脒基、香豆素环取代基可能有助于提高姜黄素-N-取代吡唑类衍生物的活性.  相似文献   

5.
利用造纸废液中的碱木素(AL)合成了木质素基偶氮聚合物(AL-azo-COOEt),并研究其自组装胶体化过程.木质素偶氮聚合物的成功合成通过核磁共振氢谱(1H NMR)、紫外-可见(UV-Vis)光谱、傅里叶变换红外(FTIR)光谱和元素分析等表征方法得到证实.激光光散射(LLS)监测了AL-azo-COOEt的胶体化过程,自组装形成的胶体球利用透射电镜(TEM)、扫描电镜(SEM)、X射线光电子能谱仪(XPS)和元素分析等进行表征.结果表明,木质素偶氮聚合物通过疏水聚集作用可以形成规整的实心胶体球,且为内部较疏水外部较亲水性质的结构.木质素偶氮聚合物胶体球可以包载疏水性药物阿霉素(DOX),且其缓释性能可以通过缓冲溶液的p H值来调控.  相似文献   

6.
仇秋娟  薛伟  卢平  王贞超  魏学 《合成化学》2011,19(1):36-40,77
采用生物活性因子拼接法将肟酯引入单羰基姜黄素衍生物1,5-二取代芳基-1,4-戊二烯-3-酮中,合成了11个新型不对称1,5-二取代-1,4-戊二烯-3-酮肟酯类姜黄素衍生物,其结构经1H NMR,IR和元素分析表征.初步生物活性测试结果表明,部分化合物具有一定的抗黄瓜花叶病毒(CMV)活性.  相似文献   

7.
改性聚苯乙烯微球的制备及其胶体晶体的组装   总被引:10,自引:0,他引:10  
采用甲基丙烯酸改性的无皂乳液聚合方法制备了尺寸为210 nm、含羧基的聚苯乙烯(PS)微球,用红外光谱、透射电子显微镜和粒度分析仪对其形状和结构进行分析,结果表明,经甲基丙烯酸改性后得到了表面为高密度电荷的单分散性PS微球.用垂直沉积法快速制备出在较大范围(大于1 cm2)呈现很好有序性的密排结构聚苯乙烯胶体晶体薄膜,其在590 nm波长处存在光子带隙.在电子显微镜下,观察到这种胶体晶体是面心立方(fcc)密排结构.  相似文献   

8.
采用海藻酸酰胺衍生物通过Ugi多组分反应制备了新颖的聚合物-二氧化硅(Oct-Alg-Si O_2)纳米粒子.通过氢核磁共振波谱(~1H NMR)和X射线光电子能谱(XPS)对Oct-Alg-Si O_2的结构和表面元素组分进行了表征.采用透射电子显微镜(TEM)、Zeta电位和激光粒度分析仪对Oct-Alg-Si O_2的形貌、粒径和胶体性能进行了探索.结果表明,海藻酸酰胺衍生物共价接枝到氨基二氧化硅(Si O_2-NH_2)纳米粒子的表面,提高了其平均直径,调控了其Zeta电位,在水介质中能够表现出良好的分散稳定性.以10%的液体石蜡为油相,采用Oct-Alg-Si O_2制备了Pickering乳液.在油水界面能够形成液滴粒径为5.7μm的稳定Pickering乳液.随着水相p H值的增大,乳液体积分数增大,稳定性增强.细胞相容性实验结果表明,Oct-Alg-Si O_2纳米粒子具有极好的生物相容性.  相似文献   

9.
姜黄素衍生物与类似物的构效关系研究进展   总被引:1,自引:0,他引:1  
根据目前对姜黄素衍生物与类似物的结构与药理作用的关系的研究现状,论述了姜黄素衍生物与类似物的结构与其抗氧化、抗炎和抗肿瘤的药理作用的关系,包括对姜黄素及其衍生物与类似物的结构修饰与其活性之间的关系的论述。大量的实验结果显示姜黄素衍生物与类似物的药理作用与其结构中所具有的官能团有着密切的关系,这为新药开发提供了一个很好的方向。  相似文献   

10.
姜黄素类似物的合成及其生物活性的测定   总被引:2,自引:1,他引:1  
实验合成了姜黄素的Knoevenagel缩合物4-(2-呋喃次甲基)姜黄素C1,氨基硫脲Schiff 碱配体E1,及其Schiff 碱配体的Zn(Ⅱ)配合物D1.采用DPPH法测定了产品清除自由基的能力,结果表明产品C1对DPPH自由基清除率为82.0%.在pH7.2的Tris-Hcl缓冲溶液中,采用紫外光谱和荧光光谱研究了C1与鲱鱼精DNA的相互作用,结果表明,C1与DNA是通过嵌插模式发生相互作用的,其键合常数为Kq =9.31×103.  相似文献   

11.
Curcumin is the source of the spice turmeric having potential application in tumor treatment but has limited therapeutic utility because of its poor aqueous solubility. Curcumin suppresses the onset of tumors as well as their growth and metastasis. Cyclodextrin-based nanosponges (NS) have been used to increase the solubility of curcumin and to control its release. The aim of the study was to formulate the complex of curcumin with β-cyclodextrin nanosponge obtained with dimethyl carbonate as a cross linker. The particle size of loaded nanosponge was found to be 487.3 nm with minimum polydispersibility index (0.476). The loaded NS have shown more solubilization efficiency (20.89 μg/ml) in comparison with plain curcumin (0.4 μg/ml) and β-CD complex (5.88 μg/ml). The zeta potential was sufficiently high (?27 mV) which indicates formation of a stable colloidal nanosuspension. The curcumin nanosponge complex (CrNS) was characterized for FTIR, XRD and DSC studies and it confirmed the interactions of curcumin with NS. The in vitro drug release of curcumin was controlled over a prolonged period of time. The in vitro hemolysis study showed that the complex was non-hemolytic. CrNS sample showed only a slight reduction in cytotoxicity against MCF-7 cells, which concludes that there is no change in molecular structure of curcumin in CrNS formulation.  相似文献   

12.
The anti‐cancer mechanisms of curcumin have been reported to include suppressions of angiogenesis and tumor proliferation. The main goal of this research is to increase the solubility of curcumin by cold atmospheric plasma (CAP) and assess the effects of modified curcumin by charging with tri‐polyphosphate chitosan nanoparticles for MCF‐7, MDA‐MB‐231 breast cancer cells, and human fibroblast cells. Curcumin modification was done by CAP and its solubility was evaluated by spectrophotometry. After loading modified curcumin into nano‐chitosan‐TPP, nanocurcumin was characterized by scanning electron microscopy. Cellular viability and apoptosis of treated cells were assessed by MTT and Annexin V. The changes of messenger RNA expression of TP5353 and VEGF genes were analyzed by real‐time PCR. CAP was able to transform the curcumin to possess hydrophilic characteristics after 90 seconds. The mean diameter of Curcumin loaded chitosannanoparticles (NPs) were determined as 48 nm. MTT results showed that the IC50 of nano Cur‐chitosan‐TPP was effectively decreased compared to free curcumin in MCF‐7 (15 μg/mL at 72 hours vs 20 μg/mL at 48 hours). Additionally, nano Cur‐chitosan‐TPP had no significant effect on normal cells (Human dermal fibroblas: HDF), whereas it also decreased the viability of triple negative breast cancer cell line (MDA‐MB‐231). Real‐time PCR results showed that expression level of TP53 gene was upregulated (P = .000), whereas VEGF gene downregulated (P = .000) in treated MCF‐7 cells. Curcumin loaded chitosan nanoparticles have led to an induction of apoptosis (79.93%) and cell cycle arrest (at S and G2M). Modified‐curcumin‐tri‐polyphosphate chitosan nanoparticles using CAP can be considered as a proper candidate for breast cancer treatment.  相似文献   

13.
Synthesis and cytotoxic activity of novel curcumin analogues   总被引:3,自引:0,他引:3  
Five novel curcumin analogues bearing different substituents at 4-position of phenyl group were synthesized. Their structures were confirmed by NMR and HRMS spectrum. Their cytotoxic activities against six tumor cell lines were tested by the standard MTT assay in vitro. The results indicated that four analogues (1A-1C, 1E) with solubilizing moieties showed selective potent cytotoxicity against HepG2, HeLa and CT26 cell lines, and analogue 1A and 1C exhibited more potent cytotoxicity than curcumin against CT26 cell line. It was suggested that introduction of appropriate substituents to 4-position of phenyl group might be a potential option for structural modification of curcumin.  相似文献   

14.
The bactericidal properties of myristic acid and curcumin were revealed in a number of studies. However, whether curcumin-loaded myristic acid microemulsions can be used to inhibit Staphylococcus epidermidis, which causes nosocomial infections, has not been reported. Our aim was to develop curcumin-loaded myristic acid microemulsions to inhibit S. epidermidis on the skin. The interfacial tension, size distribution, and viscosity data of the microemulsions were characterized to elucidate the physicochemical properties of the curcumin microemulsions. Curcumin distribution in neonate pig skin was visualized using confocal laser scanning microscopy. Dermal curcumin accumulation (326?μg/g skin) and transdermal curcumin penetration (87?μg/cm(2)/d) were obtained with the microemulsions developed herein. Curcumin at the concentration of 0.86?μg/mL in the myristic acid microemulsion could inhibit 50% of the bacterial growth, which was 12 times more effective than curcumin dissolved in dimethyl sulfoxide (DMSO). The cocktail combination of myristic acid and curcumin in the microemulsion carrier synergistically inhibited the growth of S. epidermidis. The results we obtained highlight the potential of using curcumin-loaded microemulsions as an alternative treatment for S. epidermidis-associated diseases and acne vulgaris.  相似文献   

15.
Curcumin widely exists in food, and rapid selective and accurate detection of curcumin have great significance in chemical industry. In this experiment, a new magnetic biocompatibility molecularly imprinted polymer was prepared with nontoxic and biocompatible Zein to adsorb curcumin selectively. The polymer has high biocompatibility, good adsorption capacity, and specific adsorption for curcumin. Combined with portable electrochemical workstations, the polymer can be used to detect curcumin rapidly and cost‐effectively. Using curcumin as a template and Zein as the crosslinking agent, the polymers were synthesized on the surface of Fe3O4 particles for solid phase extraction. The experimental results showed that the polymer reached large adsorption capacity (32.12 mg/g) with fast kinetics (20 min). The adsorption characteristic of the polymer followed the Langmuir isotherm and pseudo‐second‐order kinetic models. Hexacyanoferrate was used as electrochemical probe to generate signals, and the linear range was 5–200 µg/mL for measuring curcumin. The experimental analysis showed that the polymer was an ideal material for selective accumulation of curcumin from complex samples. This approach has been successfully applied to the determination of curcumin in food samples with electrochemical detection, indicating that this is a feasible and practical technique.  相似文献   

16.
The cell surface glycoprotein CD44 was implicated in the progression, metastasis and apoptosis of certain human tumors. In this study, we used atomic force microscope (AFM) to monitor the effect of curcumin on human hepatocellular carcinoma (HepG2) cell surface nanoscale structure. High-resolution imaging revealed that cell morphology and ultrastructure changed a lot after being treated with curcumin. The membrane average roughness increased (10.88 ± 4.62 nm to 129.70 ± 43.72 nm) and the expression of CD44 decreased (99.79 ± 0.16% to 75.14 ± 8.37%). Laser scanning confocal microscope (LSCM) imaging showed that CD44 molecules were located on the cell membrane. The florescence intensity in control group was weaker than that in curcumin treated cells. Most of the binding forces between CD44 antibodies and untreated HepG2 cell membrane were around 120-220 pN. After being incubated with curcumin, the major forces focused on 70-150 pN (10 μM curcumin-treated) and 50-120 pN (20 μM curcumin-treated). These results suggested that, as result of nanoscale molecular redistribution, changes of the cell surface were in response to external treatment of curcumin. The combination of AFM and LSCM could be a powerful method to detect the distribution of cell surface molecules and interactions between molecules and their ligands.  相似文献   

17.
Curcumin, the primary active ingredient in the spice turmeric, was converted to reactive monofunctional derivatives (carboxylic acid/azide/alkyne). The derivatives were employed to produce a 3 + 2 azide-alkyne "clicked" curcumin dimer and a poly(amidoamine) (PAMAM) dendrimer-curcumin conjugate. The monofunctional curcumin derivatives retain biological activity and are efficient for labeling and dissolving amyloid fibrils. The curcumin dimer selectively destroys human neurotumor cells. The synthetic methodology developed affords a general strategy for attaching curcumin to various macromolecular scaffolds.  相似文献   

18.
Mitochondrial dysfunction has been associated with diverse pathological conditions globally. Specifically, in adipose tissues, mitochondrial dysfunction is the primary cause of obesity and obesity-related illnesses. An existing drugs such as atorvastatin and other lipid-lowering drugs demonstrated adverse effects and initiated other diseases. Thus, we need to explore new methods to prevent and treat obesity. In this study, we used the cell screening method to identify several natural compounds that increase adipocyte UCP1 gene expression. The identified drug Curcumin was evaluated in cell models and the In-silico model. We found curcumin is an active compound of turmeric belonging to Zingiberaceae (ginger family), which activates the Nrf2 mechanism. Curcumin potentially endorses the expression of UCP1 in the brown adipocyte in vitro cellular model. Curcumin plays an important role that modulating mitochondrial function and improving mitochondrial DNA quantification, ATP production, and cell viability. We have established an efficient in vitro cell experiment system to study the metabolic regulation of UCP1. The in-silico model revealed curcumin-UCP1 interaction. Curcumin, via enhancing mitochondrial activity, could be a helpful therapeutic molecule against metabolic disorders or obesity-related diseases. Curcumin will be the subject of more research in both human and murine models, which will provide novel therapeutic pathways for the treatment of metabolic illnesses by modulating the control of mitochondrial function.  相似文献   

19.
该文结合倒置显微镜、原子力显微镜(AFM)、CCK-8和流式细胞术定性定量研究了姜黄素对人肝癌细胞株HepG2细胞的毒性.AFM探测结果表明,姜黄素能够引起细胞发生不同程度的形变.细胞体积和高度均随细胞形变程度的加深而下降.细胞表面平均粗糙度(Ra)、均方根粗糙度(Rq)和粒径分布均随细胞形变程度的加深而增大.而AFM...  相似文献   

20.
 采用高效毛细管电泳法测定人尿中姜黄素的含量,建立了一种测定体液中姜黄素的简便的分析方法。所用缓冲溶液为15 mmol/L的硼砂溶液(pH 9.24),运行电压为20 kV,检测波长262 nm。姜黄素的峰面积与其质量浓度的线性关系良好,其线性范围为10~300 mg/L,健康人尿中姜黄素的4个浓度水平的添加回收率均大于96.3%,相对标准偏差(RSD)小于2.3%。该法灵敏、快速、准确,可用于体液中姜黄素的批量检测。  相似文献   

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