共查询到19条相似文献,搜索用时 78 毫秒
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《日用化学工业》2021,51(8)
以姜黄素为原料,通过高压均质工艺获得姜黄素乳液。以乳液粒径为评价指标,优化工艺参数,并测定姜黄素乳液在光照、温度条件下的稳定性,进一步测试姜黄素乳液对体外脂多糖LPS诱导细胞模型及体内TPA诱导动物模型的抗炎活性及其对炎症因子表达的调控作用。结果表明,姜黄素乳液高压均质工艺条件为60 MPa、35℃、均质处理1 h,循环6次,所制备的姜黄素乳液粒径为(200±50)nm,姜黄素含量为5%,姜黄素乳液及其化妆品配方在光照、60℃条件下稳定性良好;姜黄素乳液浓度为1~50μg/m L对LPS诱导的产生的NO有显著的抑制作用,涂抹剂量为0.4mg/ear的姜黄素乳液对TPA诱导的小鼠耳肿胀抑制率达57%以上,其可能是通过抑制炎症反应过程中的关键性细胞因子IL-6、TNF-α的分泌和释放从而发挥抗炎作用。 相似文献
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姜黄素类化合物及姜黄素衍生物对酪氨酸酶抑制作用的研究 总被引:2,自引:0,他引:2
从中药姜黄的提取物中分离了姜黄素、单去甲氧基姜黄素及双去甲氧基姜黄素,并对姜黄素进行了引入羧酸基团、乙酰化、氢化等结构修饰,合成了4个姜黄素衍生物,并测试了这些化合物对酪氨酸酶的抑制活性。结果表明,天然姜黄素类化合物中单去甲氧基姜黄素的活性最强,IC50为0.076 mmol/L;姜黄素的结构修饰化合物中,带羧基的姜黄素衍生物表现出很强的抑制活性,IC50为0.056 mmol/L。抑制动力学研究表明,单去甲氧基姜黄素及带羧基的姜黄素衍生物对酪氨酸酶的抑制均属于非竞争性抑制类型。 相似文献
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阿尔兹海默病,老年痴呆最主要的类型,威胁老年人健康的四大杀手之一。全球每3秒新增一名阿尔兹海默病患者,到2050年,阿尔茨海默氏病(AD)将影响全世界约1.15亿人。AD与大脑中发现的老年斑和神经原纤维缠结中错误折叠和聚集的蛋白质(β-淀粉样蛋白和tau蛋白)积累有关。目前可用的AD药物只能暂时缓解症状,尚无有效的治疗方法。姜黄素作为拥有多途径、多靶点的复杂分子。其可以针对AD的多种病理机制、致病原因发生作用,姜黄素治疗AD的机制包括抑制Aβ形成,Aβ聚集和促进Aβ清除,抑制炎症,氧化应激和凋亡等,因而成为一种很有前景的治疗AD的多靶点新的生物活性药物。但由于其溶解度低,生物利用率差,不稳定等特点使其在临床应用中受到一定的限制。本研究旨在收集姜黄素及其修饰制剂在AD实验模型中的作用。 相似文献
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姜黄素衍生物具有杀虫、抑菌、抗病毒、消炎抗氧化、抗癌等多种生物活性。概述了对姜黄素芳环及芳环上酚羟基、β-二酮、活泼亚甲基进行修饰,或者对去掉活泼亚甲基和一个羰基后的1,4-戊二烯-3-酮类化合物进一步修饰后,得到的化合物具有较高的生物活性,并展望了其未来的发展前景。 相似文献
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Androgen receptor antagonists have been proved to be effective anti-prostate cancer agents. 3D-QSAR and Molecular docking methods were performed on curcumin derivatives as androgen receptor antagonists. The bioactive conformation was explored by docking the potent compound 29 into the binding site of AR. The constructed Comparative Molecular Field Analysis (CoMFA) and Comparative Similarity Indices Analysis (CoMSIA) models produced statistically significant results with the cross-validated correlation coefficients q(2) of 0.658 and 0.567, non-cross-validated correlation coefficients r(2) of 0.988 and 0.978, and predicted correction coefficients r(2) (pred) of 0.715 and 0.793, respectively. These results ensure the CoMFA and CoMSIA models as a tool to guide the design of novel potent AR antagonists. A set of 30 new analogs were proposed by utilizing the results revealed in the present study, and were predicted with potential activities in the developed models. 相似文献
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在导电聚合物中,聚苯胺(PANI)由于具有很高的导电性、热稳定性、容易制备等性质而受到了格外的关注。但由于PANI分子链骨架的刚性较强,分子间相互作用力大,导致其溶解、加工性能较差,对其实际应用造成了极大限制。为了改善提高聚苯胺的溶解性和加工性能,大量的研究人员对PANI展开了深入的研究。本文介绍了采用乳液聚合法和反相乳液聚合法合成聚苯胺,;介绍了聚苯胺苯环上和氨基氮上取代或改性两大类衍生物,分析了聚苯胺及其衍生物的结构,对其研究和应用作了简要综述。。 相似文献
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Damian Pawelski Alicja Walewska Sylwia Ksiezak Dariusz Sredzinski Piotr Radziwon Marcin Moniuszko Ramesh Gandusekar Andrzej Eljaszewicz Ryszard Lazny Krzysztof Brzezinski Marta E. Plonska-Brzezinska 《International journal of molecular sciences》2021,22(21)
Curcumin (CUR) is a natural compound that exhibits anti-inflammatory, anti-bacterial, and other biological properties. However, its application as an effective drug is problematic due to its poor oral bioavailability, solubility in water, and poor absorption from the gastrointestinal tract. The aim of this work is to synthesize monocarbonyl analogs of CUR based on the 9-methyl-9-azabicyclo[3.2.1]nonan-3-one (pseudopelletierine, granatanone) scaffold to improve its bioavailability. Granatane is a homologue of tropane, whose structure is present in numerous naturally occurring alkaloids, e.g., l-cocaine and l-scopolamine. In this study, ten new pseudopelletierine-derived monocarbonyl analogs of CUR were successfully synthesized and characterized by spectral methods and X-ray crystallography. Additionally, in vitro test of the cytotoxicity and anti-inflammatory properties of the synthesized compounds were performed. 相似文献
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John Amalraj Claudia E. Vergara Matías Monroy-Crdenas Ramiro Araya-Maturana Maximiliano Martínez-Cifuentes 《International journal of molecular sciences》2022,23(23)
The electrochemical behavior of N-methyl- and N-benzyl-4-piperidone curcumin analogs were studied experimentally and theoretically. The studied compounds present different substituents at the para position in the phenyl rings (-H, -Br, -Cl, -CF3, and -OCH3). We assessed their electrochemical behavior by differential pulse and cyclic voltammetry, while we employed density functional theory (DFT) M06 and M06-2x functionals along with 6-311+G(d,p) basis set calculations to study them theoretically. The results showed that compounds suffer a two-electron irreversible oxidation in the range of 0.72 to 0.86 V, with surface concentrations ranging from 1.72 × 10−7 to 5.01 × 10−7 mol/cm2. The results also suggested that the process is diffusion-controlled for all compounds. M06 DFT calculations showed a better performance than M06-2x to obtain oxidation potentials. We found a good correlation between the experimental and theoretical oxidation potential for N-benzyl-4-piperidones (R2 = 0.9846), while the correlation was poor for N-methyl-4-piperidones (R2 = 0.3786), suggesting that the latter suffer a more complex oxidation process. Calculations of the BDEs for labile C-H bonds in the compounds suggested that neither of the two series of compounds has a different tendency for a proton-coupled electron transfer (PCET) oxidation process. It is proposed that irreversible behavior is due to possible dimerization of the compounds by Shono-type oxidation. 相似文献
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HPLC法测定保健食品中姜黄素含量的研究 总被引:3,自引:0,他引:3
建立了高效液相色谱法(HPLC)测定保健食品中姜黄素含量的方法.用甲醇对样品进行超声提取,以ZORBAX XDB-C18(5 μm,4.6×250 mm)为分析柱,乙腈:磷酸盐缓冲液=50:50为流动相,流量1.0 mL·min-1,检测波长为425 nm,姜黄素在8~500 ng范围内呈良好线性,相关系数为0.99999,检出限为0.1 ng;回收率在97.8%~102.1%之间.本方法操作简便、快速,结果准确、可靠,可作为保健食品中姜黄素的质量控制监测. 相似文献