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槲皮素衍生物的合成及生物活性研究进展 总被引:2,自引:0,他引:2
综述了槲皮素衍生物的合成及生物活性研究进展,介绍了国内外槲皮素氨基酸类、糖苷类、酯类、醚类衍生物及金属配合物的合成方法及其生物活性研究现状.指出槲皮素是一种从天然植物中提取的黄酮醇类化合物,具有抗氧化,抗菌,扩张血管,抗肿瘤及抗突变等多种生物学活性.然而,槲皮素具有水溶性差、生物利用度较低等缺点,临床应用受到限制.为此,国内外学者对其结构进行修饰改造,开发出了一系列具有新颖结构的槲皮素先导化合物,可望为新型槲皮素衍生物的设计合成提供参考. 相似文献
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刺五加叶中黄酮类化合物的结构鉴定 总被引:27,自引:2,他引:25
利用电喷雾质谱发现刺五加叶中存在4种黄酮类化合物,进一步分离得到其中的两种,经核磁质谱鉴定,一种为槲皮甙(槲皮素-3-O-α-L-鼠李糖),另一种为金丝桃甙(槲皮素-3-O-β-D-半乳糖).其余两种难以分离的黄酮甙经电喷雾多级串联质谱分析,初步推断为槲皮素和芦丁(槲皮素-3-O-芦丁糖).以上4种均为黄酮醇类化合物,除金丝桃甙外,其它3种为刺五加叶中尚未见报道的黄酮类成分. 相似文献
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桑叶,又名"铁扇子",芦丁和槲皮素均为桑叶的主要有效成分,具有疏散风热、消肺润燥、清肝明目的功效~([1]).现代药理研究证明,桑叶中功效成分具有降血压、抑制血糖上升等药理作用~([2]).目前,对桑叶中黄酮类化合物的提取方面已有报道~([3~5]),但大多提取时间较长、所需试剂量大.加速溶剂萃取技术是使用常规的溶剂、利用总加温度和提高压力提高萃取效率,大大缩短提取的时间并明显降低萃取溶剂的使用量.本实验探讨了加速溶剂萃取技术提取桑叶中黄酮类化合物的萃取条件,并采用HPLC梯度淋洗法测定了芦丁和槲皮素,方法快捷准确,重现性好,可以满足桑叶中黄酮类物质的测定. 相似文献
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采用溶剂浮选法分离富集鬼箭羽提取液中黄酮类化合物,并利用紫外可见分光光度法和高效液相色谱法对总黄酮及槲皮素的含量作了测定。黄酮类化合物最佳浮选条件为浮选溶剂正丁醇,溶液pH为3.0,氮气流量300 mL·min~(-1),浮选时间50 min。该法运用于鬼箭羽中黄酮化合物的分离富集,总黄酮浮选效率在70.8%~75.0%之间,浮选液旋干后总黄酮的含量是药材提取液旋干后的4.6倍;通过高效液相色谱法研究了以槲皮素为目标物的纯化分离效果,并测定其中槲皮素的含量,结果显示槲皮素浮选效率在88.9%~92.2%之间,浮选液旋干后槲皮素的含量是药材提取液旋干后的5.7倍。 相似文献
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设计合成了10个4-二甲氨基黄酮衍生物,产物结构均经1H NMR,ESI-MS和元素分析确认.采用噻唑蓝(MTT)法测试了化合物对HepG2(人肝癌细胞)的抑制作用,结果表明目标化合物在30μmol/L浓度下对HepG2细胞损伤均有一定的抑制作用,大部分化合物优于对照药物槲皮素,其中化合物5c,5e,5f和5j活性最强,抑制率分别为91.0%,90.1%,95.7%和92.1%,而且化合物5f在10μmol/L浓度下对HepG2的抑制率为93.1%,具有深入研究的价值. 相似文献
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Peroxynitrite (ONOOH/ONOO-) which is formed in vivo under oxidative stress is a strong oxidizing and nitrating agent. It has
been reported that several flavonoids, including quercetin, inhibit the peroxynitrite-induced oxidation and/or nitration of
several molecules tested; however, the mechanism of their protective action against peroxynitrite is not univocally resolved.
The kinetics of the reaction of quercetin with peroxynitrite was studied by stopped-flow as well as by conventional spectrophotometry
under acidic, neutral and alkaline pH. The obtained results show that the protective mechanism of quercetin against peroxynitrite
toxicity cannot be explained by direct scavenging of peroxynitrite. We propose that quercetin acts via scavenging intermediate
radical products of peroxynitrite decomposition (it is an excellent scavenger of ·NO2) and/or via reduction of target radicals
formed in the reaction with peroxynitrite. 相似文献
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We report here the first chemical synthesis of three depsides related to quercetinase‐catalyzed degradation of kaempferol, quercetin, and myricetin. The three depsides were constructed through the coupling of suitably protected phloroglucinol carboxylic acid and hydroxy‐perbenzylated, derivatives of gallic, protocatechuic, and 4‐hydroxy benzoic acids. The three synthesized target compounds proved to be identical to their natural counterparts, arising from quercetinase action on corresponding flavonols. 相似文献
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Abstract In this present study, different forms of quercetin encapsulated beads were synthesized, namely ionic cross-linked gel beads and cryogel beads. Fourier Transform Infrared (FT-IR) spectra of the beads were used to characterize and prove quercetin encapsulation in alginate beads. Swelling and drying profiles were studied. Besides, release kinetics of quercetin molecules from gel beads and cryogels were carefully investigated in two different solvent/media; dimethyl sulfoxide (DMSO) and Roswell Park Memorial Institute Medium (RPMI-1640). Based upon the release kinetic studies, it is found that quercetin release from alginate cryogel beads fits the first-order release model in DMSO and it depends on the concentration of quercetin in the beads. The release of quercetin from alginate gel beads was described by the Higuchi release model, which highlights the release of quercetin molecules through the pores of the matrix. In RPMI-1640, the release of quercetin from both forms of alginate beads fits zero-order release model and it indicates a constant release of quercetin per unit time. Finally, the radical scavenging activity of the quercetin quantities was tested by the 2,2-diphenyl-1-picrylhydrazyl (DPPH) test, and successful results were obtained compared to reference material. 相似文献
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Determination of quercetin in human plasma after ingestion of commercial canned green tea by semi-micro HPLC with electrochemical detection 总被引:1,自引:0,他引:1
Determination of quercetin in human plasma was carried out by semi-micro high-performance liquid chromatography with electrochemical detection. Peak heights for quercetin were found to be linearly related to the amount of each quercetin injected from 1.5 to 750 pg. The detection limit (signal-noise ratio, S/N = 3) of the present method for quercetin was 0.3 pg. Glucuronic and sulfate forms of quercetin in plasma were hydrolyzed enzymatically using beta-glucuronidase and sulfatase, respectively. Quercetin in plasma and the hydrolyzed solution were extracted with ethyl acetate and determined by the present method. The time courses of concentrations of quercetin in human plasma showed maxima at 1-1.5 h after ingestion of 340 mL of commercial canned green tea. 相似文献
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5,7-dihydroxy-3-[beta-D-glucopyranosyl-(1-->2)-beta-D-glucopyranosyl-(1-->2)-beta-D-glucopyranosyl]-2-(3,4-dihydroxyphenyl)-4H-1-benzopyran-4-one (quercetin 3-sophorotrioside), a flavonol triglycoside, isolated from Pisum sativum shoots and showing protective effects on liver injury induced by chemicals, was synthesized for the first time. The target compound was successfully synthesized in eight linear steps and in 39% overall yield through a combination of phase-transfer-catalyzed (PTC) quercetin C-3 glycosylation and silver triflate (AgOTf) promoted carbohydrate chain elongation using both sugar bromide and trichloroacetimidate donors. 相似文献
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以芦丁(RT)-槲皮素(QT)为混合模板分子制备了芦丁-槲皮素复合模板分子印迹聚合物。 优化了制备条件,研究了模板用量比、功能单体及交联剂用量对印迹聚合物吸附性能的影响。 用傅里叶红外光谱和扫描电镜对分子印迹聚合物进行结构表征。 探讨了分子印迹聚合物的吸附动力学、等温吸附及键合位点特征,考察了其选择识别性能,并以分子印迹聚合物为吸附介质,萃取分离芦丁粗提液中的目标化合物。 结果表明,当槲皮素与芦丁的摩尔比为3:2,且模板总量与功能单体及交联剂用量摩尔比为1:8:10时,所得分子印迹聚合物的吸附性能最好,对槲皮素和芦丁的吸附量分别达47.86和60.97 mg/g。 吸附可在3.5 h内达到平衡,显示了较快的吸附动力学。 Scatchard分析表明,分子印迹聚合物基体中存在四类不同性能的键合位点,分别为芦丁和槲皮素的高亲和键合位点及非选择键合位点。 相对分布系数(k=Kd(RT)/Kd(QT),Kd=qe/ρe,Kd为分布系数,qe为平衡吸附量,ρe为平衡质量浓度)大于1,表明了分子印迹聚合物对芦丁具有更高的选择键合作用,当模拟混合物中芦丁和槲皮素浓度分别为0.07和0.03 mmol/L时,相对分布系数和分离因子(α=qe(RT)/qe(QT))分别达6.669和25.02。 另外,以乙腈、甲醇及甲醇-醋酸混合物依次为洗脱剂,通过分子印迹固相萃取可从槐米提取物中分离芦丁和槲皮素两种黄酮类化合物,总回收率分别为96.70%和94.67%。 相似文献
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Liu YC Yang ZY Du J Yao XJ Lei RX Zheng XD Liu JN Hu HS Li H 《Chemical & pharmaceutical bulletin》2008,56(4):443-451
The interactions of kaempferol and quercetin with intravenous immunoglobulin (IVIG) were studied in vitro by spectroscopic methods including fluorescence spectra, Fourier transformation infrared (FT-IR) spectra and circular dichroism (CD) spectra. The binding parameters for the reactions calculated according to the Sips equation suggested that the bindings of IVIG to kaempferol and quercetin were characterized by two binding sites with the average affinity constants K(o) at 1.032 x 10(4) M(-1) and 1.849 x 10(4) M(-1), respectively. The binding of IVIG with quercetin is stronger than that of IVIG with kaempferol. They were of non-specific and weak drug-protein interactions. Docking was used to calculate the interaction modes between kaempferol and quercetin with IVIG. The secondary structural compositions of free IVIG and its kaempferol, quercetin complexes were calculated by the FT-IR difference spectra, self-deconvolution, second derivative resolution enhancement and the curve-fitting procedures of amide I band respectively, which are in good agreement with the analyses of CD spectra. The effect of 3'-OH substituent in quercetin is distinct between the interactions of IVIG with kaempferol and quercetin for the secondary structure of the protein. The observed spectral changes indicate a partial unfolding of the protein structure, but the typical beta structural conformation of IVIG is still retentive in the presence of both drugs in aqueous solution. The average binding distances between the chromophores of IVIG with kaempferol (4.30 nm) and quercetin (4.35 nm) were obtained on the basis of the theory of F?rster energy transfer. IVIG can serve as transport protein (carrier) for kaempferol and quercetin. 相似文献
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Amaral JS Valentão P Andrade PB Martins RC Seabra RM 《Molecules (Basel, Switzerland)》2008,13(6):1321-1332
Walnut leaves from nine different cultivars (Arco, Franquette, Hartley, Lara, Marbot, Mayette, Meylannaise, Parisienne and Rego) were studied for their phenolic compounds. Samples were harvested along three consecutive years, at two different geographical locations, in order to evaluate if significant differences in the phenolics composition can be related with genetic, climatic or geographical factors. Nine compounds (3-caffeoylquinic, 3-p-coumaroylquinic and 4-p-coumaroylquinic acids, quercetin 3- galactoside, quercetin 3-arabinoside, quercetin 3-xyloside, quercetin 3-rhamnoside, a quercetin 3-pentoside derivative and a kaempferol 3-pentoside derivative) were quantified using an HPLC-DAD methodology. The qualitative profiles were identical for all samples, but differences were observed in terms of individual compounds' contents. Multivariate statistical analysis was carried out, showing that significant differences exist among production years, which can be related to climatic reasons. 相似文献
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Ying Zhang Hai-Yang Zhong Stanislas Nsanzamahoro Xiao-Jun Yao Wei-Feng Wang Jun-Li Yang 《Electrophoresis》2021,42(11):1221-1228
Screening enzymatic active compounds is one of the important fields in drug research. α-Glucosidase can hydrolyze carbohydrates to monosaccharides after meals and lead to the rise of blood glucose levels in human body. Thus, the inhibition of α-glucosidase activity is an effective approach for the diabetes treatment. In this work, we developed a new method to simultaneously screen multiple bioactive compounds within a single CE running. The affect factors on the method performance, including injection, mixing, incubation, separation and detection, were carefully analyzed and discussed. Under the optimum, the mixture consisting of two internal standards (DMSO and 4-nitrophenol) and five compounds (lyoniresinol, hydroxytyrosol, rutin, kaempferol, and quercetin) was simultaneously screened, and kaempferol and quercetin showed stronger activity and this conclusion was also supported by offline assay. Furthermore, molecular docking was employed for investigating its interaction mechanism. Eventually, the established method has been applied to screen potential α-glucosidase inhibitors from an extract of Lycium barbarum and the peak area of rutin, taxifolin, quercetin, and chlorogenic acid in L. barbarum samples changed before and after the enzymatic reaction, confirming that these four compounds had potential inhibitory activities, which was consistent with the literature data. The present work provides a promising method for the target and rapid discovery of bioactive compounds from a plant extract or mixture. 相似文献