裂片石莼水提物清除ABTS和DPPH自由基的光谱学研究

研究了大型海藻裂片石莼和富硒裂片石莼水提物清除 2,2'-连氮基-双-(3-乙基苯并二氢噻唑啉-6-磺酸)(ABTS)及 1,1-二苯基-2-三硝基苯肼(DPPH)自由基能力及其光谱学特征。分光光度计法测定,水提物 ABTS 自由基体系测定波长为 734 nm,体系稳定时间为 6 min;DPPH 自由基体系测定波长为 515 nm,体系稳定时间为 30 min。结果表明,裂片石莼水提物具有良好的抗氧化活性,能有效、快速地抑制溶液中 ABTS 和 DPPH 自由基。在优化选择的反应体系中,裂片石莼、富硒裂片石莼和标准抗氧化剂 VC 对 ABTS 自由基的半数抑制浓度(IC₅₀)分别为 76.40 μg/ml、54.11 μg/ml 和 60.69 μg/ml,说明富硒裂片石莼水提取的总抗氧化活性明显优于 VC,富硒培养可以显著提高裂片石莼的抗氧化活性。裂片石莼、高硒裂片石莼和标准抗氧化剂 VC 对 DPPH 自由基的 IC₅₀ 值分别为 123.29 μg/ml、 76.825 μg/ml 和 24.787 μg/ml。综合上述,富硒培养裂片石莼水提物具有优良的抗氧化活性,对水溶性自由基的抑制率明显高于脂溶性自由基,有广阔的开发前景。     

漆树科植物漆酚的多样性及演化关系研究

漆酚是漆树科植物独有的化学成分,具有良好的抗氧化、抗肿瘤、抗病毒等生物活性,极具药物和工业生产开发价值。该研究通过对国内外有关漆树科各类群有关漆酚数据的搜集和整理,开展漆树科漆酚的多样性与分布情况的综合统计;同时在利用核基因ETS和叶绿体基因rps16和trnL-F重建漆树科系统发育树的基础上,探讨漆酚在漆树科及各属间的起源和演化关系。结果表明:(1)漆树科漆酚具有较高的多样性,在其苯环和-R链上都有很大的变异。(2)发现漆酚仅存在于Anacardioideae亚科中,是该亚科的一个重要界定特征。(3)基于漆酚苯环结构和-R链特征的祖先性状重建分析表明,漆树科的漆酚是由邻苯二酚向间苯二酚演化,而漆酚-R链的十五烃(烯)基则是向十七烃(烯)基平行演化。     

紫杉醇的结构修饰及构效关系

本文总结了近年来对紫杉醇进行结构修饰所得到的近80种紫杉醇类似物的合成方法及其构效关系.     

天然产物抗氧化构效关系及作用机理的研究概况

本文简介了近十年来天然抗氧化剂的研究概况,讨论了天然产物抗争氧化活性的构效关系及作用机理。     

生漆化学的一个新研究领域 Ⅰ.饱和漆酚冠醚的合成及应用

本文以中国生漆中所含成份漆酚为原料,合成了一系列具有特殊性能的新型化合物——饱和漆酚冠醚,并开展了这类化合物的应用研究,从而展现了漆化学研究中的一个新的研究领域。     

当归不同提取液中阿魏酸、咖啡酸含量及抗氧化作用的比较研究北大核心CSCD

为考察不同提取条件对当归提取液中阿魏酸和咖啡酸的含量及抗氧化作用的影响,本研究通过HPLC外标一点法检测当归提取液中阿魏酸和咖啡酸的含量,通过DPPH法和ABTS法检测当归提取液的抗氧化作用。研究结果表明,不同提取条件下当归提取液中阿魏酸的含量为0. 574～0. 707 mg/g,咖啡酸为0. 012～0. 082 mg/g;碱水溶液提取时阿魏酸与咖啡酸的含量最高,其抗氧化活性也最强,而95%乙醇提取时的含量最低,抗氧化活性最弱;提取溶剂随醇浓度的增加,咖啡酸的含量逐渐减少,阿魏酸的含量呈现先增加后减少的趋势,30%～50%乙醇提取时各组分有良好的协同抗氧化作用。     

化合物毒性及三维结构参数的定量构效关系研究

目的：建立小分子化合物毒性的三维定量构效关系模型,探索化合物毒性数据和三维结构参数之间关系的方法。方法：利用比较分子力场分析方法（CoMFA）,建立了一组对发光菌有急性毒性的小分子的三维定量构效模型。结果：模型的交叉验证相关系数q^2=0．731,非交叉验证相关系数r^2=0．973,标准偏差SE=0．122,F=70．910。结论：该模型具有较好的预测能力,表明在甲基的邻对位减小取代基体积或电负性可以降低化合物毒性。     

银杏酸单体的合成及构效关系研究进展

银杏酸的研究已经成为继银杏黄酮和内酯后的热点.本文综述了银杏酸同系物的结构及部分单体的合成研究进展,分析了合成路线,讨论了各合成方法的特点及适用性,并总结了银杏酸的结构和部分药理活性的关系.     

黄酮类化合物结构与清除活性氧自由基效能关系的研究

以X－XOD体系产生O2,Luminol作为发光增强,用化学发光法测定了12种黄酮单体清除O2,反应的速率常数（k3),其K3值在10^-5-10^-6(mol/L)^-1sec^-1之间,以k3值的大小作为比较指标,对黄酮体的结构与清O2活力之间的关系进行了探讨,同时又用化学发光法测定了这些黄酮试样在1mol/L浓度时对V -H2O2-C^2 - 酵母多糖体系产生的．OH的抑制,显示出黄酮类化合物在清除O2和．OH时的活性部位和作用机制并不完全相同,认为4－OH和双键是清O2的主要活性部位,而环邻二羟基（3,4,．－di-OH)则是清除．OH的关键功能团。     

硬枝树花粗提物的抗氧化作用

采用DPPH和ABTS法对硬枝树花石油醚(30~60)、二氯甲烷、乙酸乙酯、甲醇等4个溶剂依次提取得到的浸膏物,进行抗氧化活性测定试验。结果表明:甲醇提取物,乙酸乙酯和二氯甲烷提取物在0.4~1.0 mg/mL检测浓度范围内对.DPPH的清除效果和质量浓度呈现一定的量效关系。甲醇提取物在1 mg/mL时,清除率高达93.99%,二氯甲烷提取物在1 mg/mL时清除率为92.32%,均高于同质量浓度的BHT。乙酸乙酯和二氯甲烷提取物在0.4~1.0mg/mL检测浓度范围内对ABTS.+自由基清除率与质量浓度呈现一定的量效关系,在1 mg/mL时,二氯甲烷提取物对ABTS.+自由基清除率为65.6%,乙酸乙酯提取物对ABTS.+自由基清除率为48%。     

河南产景天三七抗氧化活性研究

用清除二苯代苦味酰基(DPPH)自由基、2,2′-连氨-(3-乙基苯并噻唑啉-6-磺酸)二氨盐(ABTS)自由基和铁离子还原/抗氧化能力(FRAP)测定法对洛阳和信阳产景天三七(Sedum aizoon)体外总抗氧化活性进行评价,并与阳性对照丁基羟基茴香醚(BHA)、没食子酸丙酯(PG)和二丁基羟基甲苯(BHT)比较。发现洛阳和信阳景天三七有较好的体外抗氧化活性。洛阳和信阳产乙酸乙酯部位活性最强,正丁醇部位活性次之。在6个提取部位中,信阳产景天三七乙酸乙酯部位活性最强,其清除DPPH、ABTS自由基能力强于阳性对照BHA和BHT,还原Fe3+的能力大于阳性对照BHT,洛阳产景天三七乙酸乙酯部位和正丁醇部位活性次之。     

Phytochemicals,Essential Oils Composition and Antioxidant Activity of Astragalus spp., Phlomis olivieri and Daphne mucronata in Habitats of Central Iran

This study evaluated several secondary metabolites, essential oils (EOs) compositions, and antioxidant activity in four medicinal plants that originated in Isfahan rangelands. The species were Astragalus verus, Astragalus adscendens, Daphne mucronata, and Phlomis olivieri. Thirty-two genotypes of these species were evaluated for different biochemical traits. Based on the evaluation of EOs compounds, GC/MS analysis revealed the total number of identified compounds. These compounds were 25, 22, 12, and 22 for A. adscendens, A. verus, D. mucronata, and P. olivieri, respectively. The dominant compounds were phthalate (59.88 %) in A. adscendens, phytol (38.02 %) in A. verus, hexanoic acid (32.05 %) in D. mucronata and β-cubebene (30.94 %) in P. olivieri. Phytochemical analysis showed that D. mucronata, A. adscendens, and P. olivieri had the highest total phenolics content (TPC) (18.24 mg gallic acid equivalent/g dry weight), total flavonoids content (5.57 mg QE/g DW), and total anthocyanins content (0.23 mg/g DW), respectively. The highest total chlorophyll (0.27 mg/g DW), total carotenoids (0.03 mg/g DW), and antioxidant activity (71.36 %) were observed in A. adscendens, A. adscendens and A. verus, respectively. Among all genotypes, the highest TPC (20.1 mg GAE/g DW) was observed in genotype 5 of D. mucronata. This study provided new information on the chemical compounds within the distribution range of these ecologically dominant rangeland species in Isfahan province, Iran. The data revealed that superior genotypes from these species are rich in natural antioxidants and bioactive compounds. Thus, they can be used in ethno pharmacological fields, food, and industrial applications.     

益智的抗氧化作用

本文探讨了益智(Alpinia oxyphylla Miquel)超临界CO2提取物及其渣的水提物、正丙醇提取物和乙酸乙酯提取物的抗氧化作用,测定了总酚含量、黄酮含量、抗氧化力、还原能力、DPPH清除率.结果表明,益智超临界CO2提取物和正丙醇提取物的总酚含量最高,均为5.53%,乙酸乙酯提取物的总酚含量为4.04%,水提物总酚含量最低,为O.89%.抗氧化力与酚含量相关(R2=0.703).四种提取物中黄酮含量顺序为:乙酸乙酯提取物(6.29%)＞丙醇提取物(5.81%)＞水提取物(4.85%)＞超临界CO2提取物(4.70%).在还原能力、清除DPPH自由基和羟自由基方面,乙酸乙酯提取物表现出了很强的抗氧化能力,呈现剂量依赖关系.     

卷丝苣苔和勐醒芒毛苣苔抗氧化活性研究

利用3种方法DPPH、ABTS和FRAP分析两种苦苣苔科植物卷丝苣苔和勐醒芒毛苣苔提取物总抗氧化作用.在4种提取物中,卷丝苣苔甲醇提取物对DPPH自由基的清除能力(IC50=4.92μg/mL)比阳性对照BHT作用强(IC50=18.79 μg/mL);卷丝苣苔甲醇提取物对ABTS自由基的清除能力(IC50=11.10 μg/mL)比BHT(IC50=6.04 μg/mL)略低;卷丝苣苔甲醇提取物还原Fe3+的能力(FRAP=2403.77±38.05 μmol TE/g)比BHT(FRAP=1748.49±3.46 μmol TE/g)高.在4种提取物中,卷丝苣苔甲醇提取物抗氧化能力最高.     

苦碟子注射液抗氧化成分的分离与活性评价研究

苦碟子注射液经盐酸酸化,HPD大孔树脂柱分离,得到总酚酸部分,以抗坏血酸(Vc)做为阳性对照,利用清除二苯代苦味酰基(DPPH)自由基法和铁离子还原/抗氧化能力(FRAP)法对其进行抗氧化活性评价,研究结果表明,总酚酸部分具有较好的抗氧化能力。为此,我们利用大孔树脂柱色谱、MDS-5反相制备色谱对总酚酸进一步分离,共获得6个酚酸类成分。采用上述活性评价的方法对所获得的6个成分进行了抗氧化活性评价,发现除芹菜素-7-O-β-D葡萄糖醛酸苷外,其它5个酚酸类成分均具有很强的抗氧化活性,其清除DPPH自由基能力及总抗氧化能力好于或与阳性对照Vc相当。     

Antifungal Activity,Structure-Activity Relationship and Molecular Docking Studies of 1,2,4-Triazole Schiff Base Derivatives

Fourteen novel Schiff base compounds ( AS-1 ∼ AS-14 ) containing 5-amino-1H-1,2,4-triazole-3-carboxylic acid and substituted benzaldehyde were successfully synthesized, and their structures were verified by melting point, elemental analysis (EA) and spectroscopic techniques (Fourier Transform Infra-Red (FT-IR) and Nuclear Magnetic Resonance (NMR)). In vitro hyphal measurements were used to investigate the antifungal activities of the synthesised compounds against Wheat gibberellic, Maize rough dwarf and Glomerella cingulate. The preliminary studies indicated that all compounds had good inhibitory effect on Wheat gibberellic and Maize rough dwarf, among which the compounds of AS-1 (7.44 mg/L, 7.27 mg/L), AS-4 (6.80 mg/L, 9.57 mg/L) and AS-14 (5.33 mg/L, 6.53 mg/L) showed better antifungal activity than that of the standard drug fluconazole (7.66 mg/L, 6.72 mg/L); while inhibitory effect against Glomerella cingulate was poor, only AS-14 (5.67 mg/L) was superior to that of fluconazole (6.27 mg/L). The research of structure-activity relationship exhibited that the introduction of halogen elements on the benzene ring and electron withdrawing groups at the 2,4,5 positions on the benzene ring was beneficial to the improvement of the activity against Wheat gibberellic, while the large steric hindrance was not conducive to the improvement of the activity. Additionally, except for AS-1 , AS-3 and AS-10 , the other compounds had one or several ratio systems to achieve synergistic effect after recombination with pyrimethamine, among which AS-7 had significant synergistic effect and was expected to be a combinated agent with application prospects. Finally, the molecular docking results of isocitrate lyase with Wheat gibberellic displayed that the presence of hydrogen bonds enabled stable binding of compounds to receptor proteins, and the residues of ARG A: 252, ASN A: 432, CYS A: 215, SER A: 436 and SER A: 434 were the key residues for their binding. Comparing the docking binding energy and biological activity results, it was revealed that the lower the docking binding energy was, the stronger the inhibitory ability of the Wheat gibberellic, when the same position on the benzene ring was substituted.     

欧李果实酚类物质及抗氧化活性特征研究

以内蒙古地区36种欧李优系资源果实为试验材料,分析欧李果实品质性状的9项指标含量差异及变异系数探究其多样性,通过相关性、主成分、聚类分析对其品质性状进行综合评价,筛选酚类品质优异的欧李优系资源,为内蒙古欧李种质资源创新利用提供理论依据。结果表明,(1)9项品质性状指标变异系数为5.91%~31.03%,总黄酮最高,可滴定酸最低。(2)欧李果实3种酚类物质与总还原力、·OH清除率、DPPH·清除率及果肉色泽多表现极显著正相关(P<0.01)。(3)通过主成分分析提取的3个主成分累计贡献率为73.54%,分别为酚类因子、酸度因子和总抗氧化因子;建立欧李种质综合评价数学模型:F=[10×(46.213×F_(1)+15.132×F_(2)+12.197×F_(3))/73.542]+60,综合得分最高为MY37(84.53),综合表现最差为MY9(29.61)。(4)系统聚类评价,将36份优系资源聚为4大类,其中第Ⅰ类群综合表现最优,分别为MY5、MY36、MY37、MY38、MY41、MY47、MY50,为酚类物质积累型,多为红色果肉,酸含量适中,同时这7份优系资源综合得分均在前10位,此类群可作为高酚类品质欧李种质资源。     

紫草提取物的体外抗氧化活性研究

为研究紫草色素(LEP)的体外抗氧化活性,采用常规回流方法提取LEP,测定了LEP对超氧自由基(O2)和1,1-二苯基-2-苦苯肼自由基(DPPH.)的清除能力,及其对β-胡萝卜素/亚油酸自氧化体系的抑制作用。结果表明,LEP对DPPH.和O2均有较强的清除能力,并且对β-胡萝卜素/亚油酸自氧化体系有明显的抑制作用,说明紫草的药理作用可能与LEP较强的抗氧化能力有关。     

Phytochemical Profiles and Antioxidant Activity of Rehmannia glutinosa from Different Production Locations

The chemical components and antioxidant activity of 16 Rehmannia glutinosa samples were investigated to reveal the high‐quality raw resource for pharmaceutical products. 22 main chemical components were detected with significant content differences (P<0.05). The contents of 14 substances reached the maximum in S1 sample such as catalpol (6.74 mg g^?1), rehmaionoside A (1.93 mg g^?1) and rehmannioside D (5.13 mg g^?1). However, the content distribution of the other eight substances had no obvious change regulation. Three antioxidant evaluation methods commonly showed that S1 sample had strong antioxidant activity with a low IC₅₀ value of 0.022 mg mL^?1, a high ABTS value of 524.196 μmol equiv. Trolox g^?1, and a high FRAP value of 200.517 μmol equiv. Trolox g^?1. Considered the medicinal value, S1 had high quality based on the present phytochemical profiles and antioxidant activity. These results also indicated that the root extracts of R. glutinosa could become useful supplement for pharmaceutical products as new antioxidant agents.