Effects of Chuanxiongqin hydrochloride on increasing the fluidity of brain cell membrane and scavenging free radicals in model rats with ischemia/reperfusion injury

BACKGROUND: The fluidity of cell membrane can be affected by various factors. Many experiments have confirmed that the ischemia/reperfusion of organic tissue can increase the contents of free radicals, which lead to high rigidity and low fluidity of cell membrane, and the conditions can be changed by Chuanxiongqin. OBJECTIVE: To observe the effect and mechanism of Chuanxiongqin hydrochloride on the fluidity of brain cell membrane in rat models of ischemia/reperfusion. DESIGN: A completely randomized controlled animal trial. SETTINGS: Institute of Brain Sciences; Department of Physiology, Medical College, Datong University. MATERIALS: Twenty male grade Ⅰ Wistar rats of 170-220 g were randomly divided into model group (n =10) and control group (n =10). Chuanxiongqin hydrochloride (molecular mass was 172.2) was purchased from the National Institute for the Control of Pharmaceutical and Biological Products (batch number: 0817-9803); Spin labelers: 5-doxyl-stearlic acid methylester (5DS), 16-doxyl-stearlic acid methylester (16DS), xanthine, xanthine oxidase (XOD) and 5,5-dimeth-1-pyrroline- N-oxide (DMPO) from Sigma Company; Bruker ESP 300 electron paramagnetic resonance (EPR) spectrometer by Bruker Company (Germany). METHODS: The experiments were carried out in the State Key Laboratory of Natural and Biomimetic Drugs, Peking University from June 2001 to July 2002. In the model group, rats were made into models of cerebral ischemia by 30-minute ligation and 2-hour reperfusion of common carotid arteries; The rats in the control group were not made into models. The order parameter (S) and rotational correlation time (τc) were detected with the ESR spectrometer by means of spin labeling. The greater the S and τc, the smaller the fluidity. Meanwhile, the clearance rate of free radicals was detected with ESR spin trapping. The measurement data were compared using the t test. MAIN OUTCOME MEASURES: The S, τc and clearance rates of O2 · and OH· free radicals were compared between the model group and control group. RESULTS: The S and τc in the model group [0.738 4±0.003 5; (8.472±0.027)×10-10 s/circle] were obviously different from those in the control group [0.683 9±0.008 3; (7.945±0.082)×10-10 s/circle, t =5.731, 5.918, P < 0.05], which suggested that ischemia/reperfusion injury decreased the fluidity of brain cell membrane. After adding Chuanxiongqin hydrochloride, there were no obvious differences between the model group [0.688 5±0.030 5; (7.886±0.341)×10-10 s/circle] and control group (P > 0.05), indicating that Chuanxiongqin hydrochloride could recover the fluidity of brain cell membrane after ischemia/reperfusion injury close to the level in the normal control group. Chuanxiongqin hydrochloride could directly scavenge the O2 · and OH· free radicals, and the maximal clearance rates were 83.92% and 44.99% respectively. CONCLUSION: Chuanxiongqin hydrochloride increases the fluidity of membrane of ischemia-injured brain cell by scavenging both O2 ·and OH· free radicals.

Bioinspired-Interpenetrating Network (IPNs) Hydrogel (BIOF-INPs) and TMD <i>in Vitro</i>: Bioadhesion, Drug Release and Build in Free Radical Detection and Defense

In this work, Bioactive-functionalized interpenetrating network (IPNs) hydrogel (BIOF-INPs) were prepared and investigated in vitro for the free radical detection/defense, therapeutic release as well as shear bond strength to dentine, ability to re-mineralize surface of the dentin after application of these bio-inspired materials using a biologically inspired mineralization process in vitro as well as investigating antimicrobial properties of the BIOF-INPs against S. aureous. The aim of this investigation was to evaluate the suitability and flexibility of the designer materials to act as an “in vitro” probe to gain insights into molecular origin of TMD and associated disorders.

Application of Theories of Free Radicals and Electron Spin Resonance for Research of Traditional Chinese Medicine

The present paper reviews new findings in redoxproperties of the active constituent of Chinese herbalmedicine(CHM),a kind of CHM or a compoundprescription as an antioxidant.Firstly,we have studiedtheir antioxidant and prooxidant actions with electronspin resonance(ESR).The results show that the activecomponents from over 10 kinds of CHM are able toscavenge the oxygen free radicals but propyl gallate

Anxiolytic and free radical scavenging potential of Chinese celery(Apium graveolens) extract in mice

Objective: To elucidate the anxiolytic and free radical scavenging effect of methanolic extract of Apium graveolens(A. graveolens) in adult C57BL/6 mice.Methods: Sixty male mice were divided into 6 groups: control, vehicle, positive control and A. graveolens(125, 250 and 500 mg/kg). Different behavioral models of elevated plus maze, open field, light/dark, hole-board and pentobarbital-induced sleep were used to assess anxiety-like behavior. Biochemical parameters including monoamine oxidase-A(MAO-A) activity, lipid peroxidation, % inhibition of superoxide anion and glutathione peroxidase activity were measured. Histologic studies were also examined.Results: Mice receiving various doses of A. graveolens(125, 250 and 500 mg/kg)showed an alleviation of anxiety-like behavior as evidenced by the battery of behavioral tests. Likewise, A. graveolens treatment was found to significantly decrease MAO-A activity, lipid peroxidation as well as cause a significant increase of % inhibition of superoxide anion and glutathione peroxidase activity in both cortex and striatum. The total number of survival neurons found in the frontal cortex and striatum was significantly higher than that of the vehicle-treated group.Conclusions: Taken together, we showed that A. graveolens improve the behavioral changes which might be related to the inhibition of free radicals and modulation of MAOA activity resulting in an increased number of survival neurons. Our findings suggest the therapeutic potential of A. graveolens in the treatment of anxiety.

Why Static O-H Bond Parameters Cannot Characterize the Free Radical Scavenging Activity of Phenolic Antioxidants: ab initio Study

The static O-H bond parameters including O-H bond length, O-H charge difference, O-H Mulliken population and O-H bond stretching force constant (k) for 17 phenols were calculated by ab initio method HF/6-31G**. In combination with the O-H bond dissociation enthalpies (BDE) of the phenols determined by experiment, it was found that there were poor correlationships between the static O-H bond parameters and O-H BDE. Considering the good correlationship bt tween O-H BDE and logarithm of free radical scavenging rate constant for phenolic antioxidant, it is reasonable to believe that the ineffectiveness of static O-H bond parameters in characterizing antioxidant activity arises from the fact that they cannot measure the O-H BDE.

SYNTHESIS AND FREE RADICAL RING-OPENING POLYMERIZATION OF 2-METHYL-AND 2-METHYL-9-n-BUTYL-(-7-METHYLENE-1,4,6-TRIOXA-SPIRO (4, 4)NONANE)

This paper describes the synthesis and free radical ring-opening polymerization of 2-methyl-and 2-methyl-9-n-butyl (-7-methylene-1, 4, 6-trioxaspiro (4, 4) nonane). The structures of the two polymers were verified by IR, 'H and ^(13)C NMR spectra. The substituent on 9-position of 7-methylene-trioxaspiro (4, 4) nonane affects the structure of polymer and polymerization activity. The polymerization mechanism is discussed.

Biological effects of implantation and penetration of nitrogenion beams on wheat seeds

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量子化学计算白藜芦醇与芝麻酚在油脂中的抗氧化协同作用

目的:研究白藜芦醇与芝麻酚间的抗氧化协同机理。方法:通过DPPH和氢过氧化物分别检测葵花子油中自由基和过氧自由基的含量变化,并结合诱导期的测定,优化组合白藜芦醇与芝麻酚二者比例,并采用量子化学计算模拟反应过程。结果:在180℃加热2 h,添加白藜芦醇与芝麻酚的葵花籽油中,总自由基含量分别为(0.08±0.03),(0.20±0.03)mol/L,相比于空白[(0.44±0.01)mol/L],白藜芦醇具有最佳抑制效率,且芝麻酚清除过氧自由基的能力最强。二者在纯化的葵花籽油中发生协同作用的最佳添加量为1400,200 mg/kg,且在180℃降解速率下,白藜芦醇具有保护芝麻酚的作用。结论:利用量子化学的手段发现二者存在动态平衡的过程,由于白藜芦醇的添加量是芝麻酚的7倍,所以反应更倾向于白藜芦醇向芝麻酚自由基供H。

Antioxidant and Hypoglycemic Ability of Ardisia gigantifolia Stapf Parts

[Objectives]To study the antioxidant and hypoglycemic effects of different parts of Ardisia gigantifolia Stapf.[Methods]The hydroxyl radical scavenging activity,DPPH radical scavenging activity and total antioxidant capacity of ABTS of 75%ethanol extract of A.gigantifolia Stapf and the petroleum ether,ethyl acetate,n-butanol,chloroform and aqueous extract were measured with Vc as positive control.At the same time,acarbose was used as reference substance to determine the inhibitory effect of each polar site onα-glucosidase.[Results]All parts of A.gigantifolia Stapf had antioxidant activity,among which ethyl acetate had the strongest antioxidant activity,and the scavenging rate of hydroxyl radical and DPPH radical was higher than that of positive control.The results showed that petroleum ether,ethyl acetate and chloroform had a good inhibitory effect onα-glucosidase(better than acarbose).[Conclusions]The ethyl acetate part of A.gigantifolia Stapf had the best antioxidant activity and inhibitory effect onα-glucosidase.It provides a basis for further research and development of A.gigantifolia Stapf.

基于RTCA技术研究抗体偶联药物的旁观者效应的检测方法

目的 利用实时无标记细胞分析(RTCA)系统评估抗体偶联药物(ADC)的旁观者效应。方法 采用RTCA系统监测抗原阳性细胞(Ag^(+))和抗原阴性细胞(Ag^(-))的共培养状态,观察Ag^(-)的细胞存活情况;采用重复实验验证结果的可靠性和一致性,并采用单因素方差分析比较不同细胞比例培养组在单个时间点的Ag^(-)存活率。结果 加入抗体偶联药物后,随着共培养时间的延长,Ag^(-)存活率下降;此外,在单个时间点(96 h)上,与0%Ag^(+)细胞的Ag^(-)细胞存活率相比,10%Ag^(+)细胞的Ag^(-)细胞存活率为89.07%(P=0.156),25%Ag^(+)细胞的Ag^(-)存活率为68.93%(P=0.0026),50%Ag^(+)、75%Ag^(+)和90%Ag^(+)细胞的Ag^(-)存活率分别为35.28%、13.99%和12.02%(P<0.0001)。在 Ag^(+)细胞比例为25%~90%时,旁杀伤效果显著;重复性结果显示不同Ag^(+)细胞的旁杀伤率的相对标准偏差(RSD)均小于30%。结论 结合RTCA技术和共培养方式的方法,可以更准确地模拟旁观者效应的生物学过程,为后续的抗体偶联药物开发提供有价值的参考。

阿美替尼、吉非替尼治疗EGFR突变局部晚期非小细胞肺癌的效果及预后

目的探讨阿美替尼、吉非替尼治疗表皮生长因子受体(EGFR)突变局部晚期非小细胞肺癌(NSCLC)的效果及预后。方法选取2019年3月至2022年9月确诊的100例EGFR突变局部晚期NSCLC,根据治疗方式不同分为A组(n=57)和B组(n=43),A组采用阿美替尼治疗,B组采用吉非替尼治疗,均持续治疗2个周期。比较2组的客观缓解率(ORR)和疾病控制率(DCR)、治疗前后血清EGFR水平和免疫球蛋白指标[免疫球蛋白M(IgM)、免疫球蛋白A(IgA)、免疫球蛋白G(IgG)]、毒副反应发生率,所有患者随访12~42个月,绘制生存曲线,比较2组中位总生存期(OS)和中位无进展生存期(PFS)。结果A组ORR和DCR分别为28.07%和77.19%,B组分别为11.63%和44.19%,差异均有统计学意义(P<0.05)。治疗后,A组血清EGFR水平较B组低,IgM、IgA和IgG水平较B组高,差异有统计学意义(P<0.05)。A组<3级毒副反应发生率为71.93%,≥3级毒副反应发生率为21.05%,B组<3级毒副反应发生率为48.84%,≥3级毒副反应发生率为41.86%,差异有统计学意义(P<0.05)。A组中位OS和中位PFS分别为16.9个月和5.8个月,B组中位OS和中位PFS分别为10.5个月和4.0个月,差异有统计学意义(P<0.05)。结论与吉非替尼比较,阿美替尼治疗EGFR突变局部晚期NSCLC患者效果更好,可以更好控制病情发展,改善EGFR水平和免疫指标,提高患者生存率,且具有一定的安全性。

百合酸豆奶配方优化及抗氧化性研究

以大豆、百合、蔗糖为主要对象,探究蔗糖添加量、百合汁添加量、菌种添加量和发酵时间4个单因素不同的水平对百合酸豆奶的总酸含量和感官评分的影响程度。基于Design Expert软件设计试验方案,运用Box-behnken建立数据模型和二阶多项非线性回归方程,用感官得分为指标优化百合酸豆奶原料组分比例,获得百合酸豆奶的蔗糖添加量、百合汁添加量和菌种添加量的最佳配比。结果表明,百合酸豆奶的最佳配方为蔗糖添加量8.3%,百合汁添加量11.8%,菌种添加量0.3%,优化后验证试验的样品感官评分为89.85分(n=3),与预测值90.15分接近,偏差为0.33%。测得百合酸豆奶持水性为81.01%,黏度为1287.90 mPa·s,百合多糖的含量为187.01 mg/100 g。百合酸豆奶对DPPH、O2-·和ABTS自由基清除率分别为57.81%,65.82%,78.91%,百合酸豆奶的自由基清除率大小顺序为ABTS·>O2-·>DPPH·,自由基的清除率为未添加百合酸豆奶的1.58倍,1.52倍和1.26倍,表明百合酸奶的抗氧化性能力明显高于普通豆酸奶。

智能型药物控释可视化系统的构建与表征——高分子实验的新设计与教学实践

介绍一个涵盖高分子化学、物理化学与仪器分析等领域的实验新设计与教学实践。通过水相自由基沉淀聚合法合成一种温敏性微凝胶,并使用紫外-可见分光光度计和动态光散射仪对其温度响应特性进行表征,进而将其用作载体材料以设计构建智能型药物控释系统,利用微凝胶低温溶胀、高温收缩的特性,实现药物的装载、释放。提出结合色彩理论与化学知识来理解药物释放过程,以在可见光区存在明显吸收的药物作为模型药物,将“没有明显实验现象”的药物释放过程“可视化”,以更加直观的方式观测药物释放过程,并在此“可视化”感性认识的基础上,理性分析药物释放过程的分子扩散机理。本实验取材于广受关注且已有较多验证的研究前沿成果,绿色环保,并且可拓展至其他响应性高分子及药物,具有普适性。本实验主要目标是在锻炼学生基本操作能力的同时,培养他们发现问题、解决问题的研究技能,提升学生创新能力。

氯酸盐屏蔽废水COD测定的消除策略及反应机制

向废水中投加氯酸盐,即所谓的“COD(化学需氧量)去除剂”,可降低COD检测值,呈现出水符合COD排放标准的假象.从本质上而言,氯酸盐的添加并未实际去除COD,而仅仅是作为氧化剂减少了在高温消解过程中重铬酸钾的消耗量,导致测定的COD数值偏小,因此氯酸盐只是起到了掩蔽作用.为消除氯酸盐对COD的掩蔽作用,提出了一种以亚硫酸盐为还原剂的预处理工艺:根据氯酸盐含量投加相应的亚硫酸氢钠进行去除,进而测定出真实的COD.结果表明,当[SO_(3)^(2-)][ClO_(3)^(-)]摩尔比为5-6、温度为60℃时,经过1h的反应可以有效的消除氯酸盐对COD测定的影响,此时SO_(3)^(-)和ClO_(3)^(-)同步耗尽.基于ESR(电子自旋共振)分析,可知氯酸盐与亚硫酸盐首先通过单电子转移反应生成SO_(3)^(-),生成的SO_(3)与溶解氧进一步发生反应生成SO_(4)^(-),而CO_(3)^(-)的还原中间体(ClO_(2)、ClO_(2),和CIO^(-))可与亚硫酸根继续通过氧转移反应而被还原,最终产物为Cl^(-);通过反应前后的三维荧光光谱图发现生成的自由基虽然可以氧化部分有机物,但是并未发生矿化反应,因此经处理后所测定的COD值即为真实值。总而言之,本研究所提出的亚硫酸盐消除氯酸盐对COD测定干扰的方法切实可行,为完善COD测定方法及理论提供参考.

不同采收期虫草参多酚对羟基自由基介导的DNA氧化损伤保护作用的研究

采用Folin-酚法测定两个采收地(S1和S2)三个采收期(T1、T2和T3)虫草参游离酚和结合酚提取物的多酚含量。采用HPLC法检测多酚提取物中没食子酸、绿原酸、咖啡酸和迷迭香酸的含量。同时,评价了虫草参多酚提取物对羟基自由基(·OH)介导的DNA氧化损伤的保护作用。结果显示,虫草参游离酚和结合酚提取物的多酚含量范围分别为86.53~181.40和89.70~193.58μg GAE/mg;咖啡酸在结合酚中含量较高,且S2采收地高于S1;而迷迭香酸在游离酚中含量较高,且在T1和T3采收期,S2采收地的高于S1,相反在T2采收期,S2采收地的低于S1;虫草参游离酚(25~300μg/mL)和结合酚(3.125~50μg/mL)提取物对DNA氧化损伤保护作用的双螺旋百分比范围分别为1.81%~55.04%和1.67%~70.83%。相较于游离酚,结合酚提取物表现出更好的保护效果。

气相色谱-质谱联用分析莳萝子中挥发油和油脂的化学成分及其抗氧化活性研究

目的 提取莳萝子的挥发油和油脂,并对其组成进行分析,筛选出活性成分,为莳萝子挥发油、油脂的临床应用研究提供依据。方法 2021年6月至2022年2月采用水蒸气蒸馏法提取挥发油,经石油醚索氏提取油脂,用气相色谱-质谱联用(GCMS)联用仪分析鉴定其组分,并通过检测清除自由基能力评价抗氧化活性。结果 莳萝子挥发油提取率为(5.850±0.141)%,共鉴定出19种化合物,主要含有黄酮类化合物(61.418%)及萜类化合物(29.471%);莳萝子油脂提取率为(13.168±0.117)%,共鉴定出16种化合物,主要包括亚油酸甲酯(5.58%)、顺式亚油酸(5.58%)、十八碳六烯酸甲酯(56.73%)等。1,1-二苯基-2-三硝基苯肼(DPPH)自由基清除率结果是挥发油的IC50值(半抑制浓度)为42.963 mg/L,油脂的IC50值为28.430 mg/L;2’-联氨-双(3-乙基苯并噻唑啉-6-磺酸)二胺盐(ABTS)自由基清除率结果是莳挥发油的IC50值为21.129 mg/L,油脂的IC50值为9.722 mg/L。结论 莳萝子挥发油、油脂均具有较强的抗氧化能力。

厄洛替尼治疗晚期非小细胞肺癌的临床疗效及安全性观察

目的 探讨厄洛替尼治疗晚期非小细胞肺癌(NSCLC)的临床疗效和安全性。方法 回顾性纳入中国科学技术大学附属第一医院(安徽省立医院)收治的69例晚期非小细胞肺癌患者病历资料,根据NSCLC患者确诊后应用药物治疗种类的不同,将69例纳入患者分为对照组和观察组。观察组(34例)给予厄洛替尼治疗,对照组(35例)给予常规化疗,比较2组的临床疗效及不良反应的差异。结果 2组的客观缓解率及疾病控制率比较,差异均无统计学意义(P>0.05);对照组和观察组的中位无进展生存期分别为4.2个月和12.6个月,差异有统计学意义(P<0.05)。观察组患者的性别、年龄、治疗时机和表皮生长因子受体突变类型对中位无进展生存期均无显著影响(P>0.05)。观察组不良事件以皮疹和转氨酶升高为主,其中皮疹的发生率高于对照组(P<0.05)。结论 相对常规化疗,厄洛替尼有利于疾病的控制、显著延长生存时间,但其皮疹的毒性反应更大。

Effects of Micelle on Pyrazoles as Antioxidants in Radical-induced Oxidation of DNA

Effects of 4-（1,3-diphenyl-1H-pyrazol-5-yl）phenol（APP）,4-（1,5-diphenyl-lH-pyrazol-3-yl）phenol（BPP） and 4-（3,5-diphenyl-1H-pyrazol-1-yl）phenol（CPP） on 2,2＇-azobis-（2-amidinopropane hydrochloride）（AAPH）-induced oxidation of DNA were measured in the presence of various concentrations of Triton X-100,cetyltrimethylammonium bromide（CTAB）,or sodium dodecyl sulfate（SDS） in order to clarify the influence of neutral,cationic and anionic microenvironments on antioxidant capacities of APP,BPP and CPP.Although these surfactants can protect DNA against AAPH-induced oxidation,the pyrazoles in the presence of these surfactants functioned as prooxidants when the concentrations of Triton X-100 and CTAB increased.However,CPP exhibited antioxidant property with the increase of the concentration of CTAB.On the contrary,APP,BPP and CPP were antioxidants in the presence of various concentrations of SDS.The added surfactants resulted in the complication of the microenvironments around DNA,pyrazoles and peroxyl radical（ROO＊） derived from AAPH.The anionic charge of SDS was beneficial to enhancing the antioxidant effectiveness of these pyrazoles.It can be concluded that the charge property of surfactants markedly influenced the behavior of an antioxidant in AAPH-induced oxidation of DNA.

香青兰多糖的提取、测定及其对活性氧自由基的清除作用

建立了热水提取、乙醇沉淀、Sevag法去蛋白、有机溶剂分离纯化提取香青兰多糖的方法,并用苯酚 硫酸比色法测定其含量;同时采用生物化学法测定了香青兰多糖对活性氧自由基O2 -·、·OH和H2 O2 的清除能力和还原能力,以枸杞多糖作为对照品。实验结果表明:香青兰中多糖含量为6 38% ,回收率为93 6 %～10 5 6 % ,RSD =2 3% (n =4 )。香青兰多糖对O2 -·、·OH和H2 O2 具有良好的清除能力,同时还有较强的还原能力,它们的活性大小与多糖的用量呈正相相关性,且均比枸杞多糖的活性强。

菜籽多酚和Vc在化学模拟体系中清除超氧阴离子和羟自由基的能力

研究菜籽多酚、Vc、菜籽多酚与Vc混合物在化学模拟体系中清除超氧阴离子自由基OH.O2.与羟自由基.OH自由基的能力。用邻苯三酚自氧化法测定抗氧化剂清除OH.O2.的能力,用铁氧化邻二氮菲-Fe2+法测定抗氧化剂清除.OH的能力。结果表明:菜籽多酚、Vc、菜籽多酚与Vc的混合物清除OH.O2.、.OH都不呈剂量-效应关系。菜籽多酚在0.25mg/ml浓度时对OH.O2.与.OH的清除率均最高,分别达51.40%和84.82%。Vc在0.80mg/ml时对OH.O2.的清除率最高,达80.39%;在0.40mg/ml时对.OH的清除率最高,达91.35%。当总浓度为0.25mg/ml时,菜籽多酚与Vc的混合物没有协同增加清除OH.O2.的作用;菜籽多酚与Vc按7∶3、8∶2两种比例混合,在清除.OH时有协同增效作用,协同增效的最佳比例为7∶3,最大清除率达78.78%。