Knowledge mapping of Opuntia Milpa Alta since 1998: A scientometric analysis

建立超高效液相色谱串联四极杆静电场轨道阱质谱方法(UPLC-QE-Orbitrap-MS)对米邦塔仙人掌的叶状茎及果实化学成分进行表征,并对其抗氧化活性进行考察,初步探讨成分与活性的关系。

选择UPLC HSS T3 C₁₈ (2.1 mm×10 mm,1.8 μm)色谱柱,以乙腈-0.1%甲酸水为流动相,梯度洗脱,流速为0.2 mL·min^–1;采用加热电喷雾离子源,正、负离子模式分别进行一级、二级质谱数据采集;采用数据库和文献报道对米邦塔仙人掌叶状茎及果实的化学成分进行表征。采用DPPH、羟自由基(·OH)和超氧阴离子自由基(·${\\mathrm{O}}^{-}_{{2}} $)清除能力测试方法,对米邦塔仙人掌叶状茎及果实的抗氧化活性进行考察。

从米邦塔仙人掌的叶状茎及果实中共表征出39种化合物,其中酚类22个,黄酮类13个,其他成分4个。米邦塔仙人掌叶状茎及果实均具有一定的抗氧化能力,米邦塔仙人掌果实对DPPH的清除能力强于叶状茎,而叶状茎对·OH清除能力稍强于果实,叶状茎皮和果皮清除能力相当,果汁对·${\\mathrm{O}}^{-}_{{2}} $清除能力最强,米邦塔仙人掌的抗氧化活性与其富含的酚酸类成分密切相关。

本研究建立了一种快速、准确、可靠的米邦塔仙人掌茎果化学成分的鉴别方法,为米邦塔仙人掌资源的综合开发利用提供了科学依据。

     

圆果算盘子脂溶性成分及其抗氧化活性研究

目的 分析圆果算盘子的脂溶性成分及其抗氧化活性。方法 利用气相色谱-质谱（GC-MS）联用技术对圆果算盘子药材的脂溶性成分进行分析和鉴定,并通过标准质谱谱库的计算机检索进行化学成分定性;采用清除DPPH自由基及ABTS⁺自由基能力的方法对圆果算盘子的脂溶性成分进行抗氧化活性研究。结果 从圆果算盘子的脂溶性成分中共鉴定出47个成分,同时抗氧化结果显示圆果算盘子的脂溶性成分对DPPH自由基及ABTS⁺自由基的半数清除浓度IC₅₀分别为1.103,0.726 mg·mL^-1。结论 圆果算盘子的脂溶性成分主要为脂肪酸类化合物及醇类,均为首次从该植物中鉴定出;其脂溶性成分具有一定的抗氧化活性。     

裸花水竹草脂溶性成分及其抗氧化活性研究

目的 分析裸花水竹草的脂溶性成分及其抗氧化活性。方法 利用气相色谱-质谱（GC-MS）联用技术对裸花水竹草药材的脂溶性成分进行分析和鉴定,并通过标准质谱谱库的计算机检索进行化学成分定性;采用清除DPPH自由基及ABTS自由基能力的方法对裸花水竹草的脂溶性成分进行抗氧化活性研究。结果 从裸花水竹草的脂溶性成分中共鉴定出23个成分,同时抗氧化结果显示裸花水竹草的脂溶性成分对DPPH自由基及ABTS自由基的半数清除浓度IC₅₀分别为5.255,3.848 mg·mL^-1。结论 裸花水竹草的脂溶性成分主要为不饱和脂肪酸类化合物及植醇,均为首次从该植物中鉴定出;其脂溶性成分具有一定的抗氧化活性。     

棉花皮苷的抗氧化活性及对肝癌细胞生长的抑制作用研究

目的探讨棉花皮苷的抗氧化性及对肝癌细胞生长的抑制作用。方法本研究首次应用化学发光法和分光光度法系统评价了棉花皮苷对超氧阴离子自由基(O2.)、羟基自由基(.OH)、H2O2等活性氧和二苯代苦味酰基自由基(DPPH.)自由基的清除作用。采用MTT实验评价了棉花皮苷对人肝癌HepG2细胞生长的影响。结果棉花皮苷对O2.、.OH、H2O2和DPPH.等自由基均有较强的清除能力。与常用的抗氧化剂Vit C相比,其抗氧化效果明显强于VitC。棉花皮苷可以以剂量及时间依赖方式抑制肝癌细胞生长、增殖。结论棉花皮苷具有较强的抗氧化和抗肝癌生物活性。     

方格星虫多肽的结构分析及体外抗氧化活性

目的 以方格星虫为原料,酶解制备水溶性多肽并考察其抗氧化活性,探究其结构-活性关系。方法 利用5种蛋白酶酶解新鲜方格星虫,并结合超滤方法得到高分子量(>50kDa)、中分子量(5～50 kDa)和低分子量(＜5kDa)的酶解肽段;利用氨基酸自动分析仪测定方格星虫酶解肽的氨基酸组成。综合考察多肽对1,1-二苯基-2-苦基肼(DPPH.)自由基、羟基自由(.OH)、超氧阴离子自由基( O-2.)的清除能力以及还原力效果,评价方格星虫多肽抗氧化活性;利用高效液相色谱-串联质谱方法鉴定小分子肽的氨基酸组成和序列结构。结果 胰蛋白酶水解方格星虫4h得到的酶解液蛋白含量最高,并在酶解液中检测确定了17种氨基酸,其中精氨酸含量最高13.65%。高中低三组肽段中,低分子量肽段的抗氧化活性优于其他：对DPPH 自由基和羟自由基清除能力大小顺序为低分子量>高分子量>中分子量、对超氧阴离子清除能力大小顺序为低分子量>高分子量≈ 中分子量、还原能力强弱顺序为高分子量>低分子量 > 中分子量。经高效液相色谱-串联质谱联鉴定了GFAGDDAPR、GLGGLSPEK 、LDLAGR和VTKEIPR 4个肽段。结论 低分子量的方格星虫酶解多肽具有较好的抗氧化活性,有潜力用作生物医药或化妆品工业的原料。     

蕲艾挥发油的化学成分及其体外抗氧化活性研究

目的：分析蕲艾挥发油的化学成分,对蕲艾挥发油体外抗氧化活性进行研究。方法：采用水蒸气蒸馏法提取蕲艾挥发油,运用气相色谱-质谱连用技术（GC-MS）分析蕲艾挥发油化学成分。通过清除1,1-二苯基-2-三硝基苯肼（DPPH）有机自由基法研究蕲艾挥发油的清除自由基作用,运用紫外-可见分光光度法测定蕲艾挥发油、抗氧化剂2,6-二叔丁基-4-甲基苯酚（BHT）和维生素E的清除率,并进行比较。结果：蕲艾挥发油检测到40种化学成分,初步鉴定了27种化合物,占总挥发性成分89.12%,其化学成分主要为侧柏酮（25.17%）、桉油精（23.42%）、樟脑（8.58%）、α-柏酮（7.76%）、4-萜品醇（4.7%）和冰片（3.34%）等。蕲艾挥发油的体外抗氧化试验表明,清除DPPH能力从强至弱的顺序为BHT > 蕲艾挥发油 > 维生素E。结论：蕲艾挥发油主要由酮类和萜类组成,并具有较好的体外抗氧化活性。     

猪仔笠多糖成分的提取及抗氧化活性研究

目的建立猪仔笠中多糖的提取方法 ,并对其抗氧化活性进行研究,为猪仔笠的资源开发及应用提供实验依据。方法利用经典水提醇沉法,从猪仔笠中提取多糖成分,并利用苯酚-硫酸法测定多糖的含量,分别采用水杨酸法和邻苯三酚自氧法测定多糖对羟基自由基(.OH)的清除作用以及对超氧阴离子自由基(O2-)的清除作用。结果实验结果表明利用石油醚连续回流提取,能够提取出猪仔笠中的多糖成分,含量为7.03%;在多糖浓度为1600μg.mL-1时,对羟自由基清的除率可达到70.92%,对超氧阴离子自由基(.O2-)的清除率达到53.19%。结论猪仔笠中的多糖具有显著的抗氧化活性。     

异紫草酸纯化提取工艺及抗氧化活性研究

探究丹参多酚酸中异紫草酸的最佳分离纯化方法及其体外抗氧化活性。通过MCI Gel色谱柱、LH-20凝胶色谱柱、动态轴向加压制备液相联用分离得到高纯度异紫草酸,并与传统硅胶柱层析法分离效果进行对比。通过·OH清除实验、DPPH自由基清除实验和铁氰化钾还原实验测定异紫草酸的体外抗氧化活性。所建立方法分离得到的异紫草酸纯品归一化法百分含量达到98.7%,传统硅胶柱层析法无法分离得到异紫草酸纯品。异紫草酸对·OH和DPPH的半数清除率浓度(IC50)分别为0.277 mg·mL^-1、17.43μg·mL^-1,其抗氧化能力与浓度剂量呈现依赖关系。MCI-Gel/LH-20凝胶/C18键合填料柱层析法可用于高纯度异紫草酸的分离。异紫草酸具有清除自由基及抗氧化活性,可用于治疗心脑血管疾病药物的开发。     

风轮菜活性部位体外抗氧化作用的实验研究

目的研究风轮菜活性部位(CCE)的体外抗氧化活性,为将其开发为新的抗氧化药物提供实验依据。方法通过体外实验测定CCE对超氧阴离子(O-2)、羟基自由基(.OH)及有机自由基DPPH.的清除作用以及对亚铁离子-维生素C(Fe2+-VitC)诱导的小鼠肝脂质过氧化的影响。建立高浓度葡萄糖损伤人脐静脉内皮细胞(HUVECs)的体外模型,测定CCE对细胞超氧化物歧化酶(SOD)和乳酸脱氢酶(LDH)活性的影响。结果CCE能有效清除O-2、.OH和DPPH自由基,其中.OH的清除力最强,对Fe2+-VitC诱导的肝匀浆脂质过氧化反应有明显的抑制作用,且呈浓度依赖性。此外,CCE能明显提高高糖刺激下内皮细胞中的SOD水平,降低LDH活性。结论CCE具有显著的体外抗氧化活性。     

北极放线菌T-2-3胞外多糖体外抗氧化作用研究

为找外源性的自由基清除剂和抗氧化剂,课题对北极放线菌T-2-3胞外多糖(Arctic Streptomyces sp.extracellular polysaccharide,ASEP)的抗氧化能力进行了研究。通过测定总还原能力(T-AOC)、亚铁离子鳌合能力、超氧阴离子自由基(O2-.)清除能力、羟基自由基(.OH)清除能力和H2O2清除能力,对ASEP和进一步分离组分ASEP-3进行了抗氧化活性初步评价。此外,体外检测了ASEP和ASEP-3对.OH诱导的小鼠肝线粒体MDA生成影响,对H2O2引起的小鼠红细胞溶血的抑制作用及对.OH诱导的肝线粒体肿胀程度的影响。结果显示,ASEP具有一定的抗氧化活性,当ASEP和ASEP-3浓度为200μg/mL时,其对.OH的清除作用分别达到58.0%和99.5%,对O2-.的清除作用达到38.9%和74.2%,对H2O2的清除作用达到12.1%和20.4%,对H2O2引起的氧化溶血的抑制作用达到10.2%和22.8%,对小鼠肝线粒体脂质过氧化的保护作用达到7.9%和14.5%,均呈一定的量效关系,表明ASEP具有一定的抗氧化作用。     

Affective and Anxiety Disorders and Alcohol and Drug Dependence:

Depression and anxiety frequently coexist in patients with substance use disorders. This clinically-oriented article examiens the relationship between these conditions and emphasizes data showing that substances of abuse can cause signs and symptoms of both depression and anxiety. These substance-related syndromes appear to have a different course and prognosis than uncomplicated, independent anxiety and major depressive disorders, and clinicians should consider the role of alcohol and other drugs in all patients presenting with these complaints. The authors will also outline an approach for diagnosing and managing patients with the combination of a substance use and depressive or anxiety disorder.     

Synthesis and anti-nociceptive and anti-inflammatory effects of gaultherin and its analogs

The synthesis of gaultherin (1) and its analogs was carried out to provide 11 glycosides under phase-transfer catalytic conditions. The activities of all synthesized compounds were evaluated by nitric oxide production inhibitory assay in vitro. Methyl 2-O-(4-O-β-d-galactopyranosyl)-β-d-glucopyranosylbenzoate (5f) showed significantly anti-nociceptive and anti-inflammatory effects by the evaluation in vivo. Structure–activity relationships within these compounds were discussed.     

Modelling and simulation of variability and uncertainty in toxicokinetics and pharmacokinetics

Two important methodological issues within the framework of the variability and uncertainty analysis of toxicokinetic and pharmacokinetic systems are discussed: (i) modelling and simulation of the existing physiologic variability in a population; and (ii) modelling and simulation of variability and uncertainty when there is insufficient or not well defined (e.g. small sample, semiquantitative, qualitative and vague) information available. Physiologically based pharmacokinetic models are especially suited for separating and characterising the physiologic variability from the overall variability and uncertainty in the system. Monte Carlo sampling should draw from multivariate distributions, which reflect all levels of existing dependencies in the intact organism. The population characteristics should be taken into account. A fuzzy simulation approach is proposed to model variability and uncertainty when there is semiquantitative, qualitative and vague information about the model parameters and their statistical distributions cannot be defined reliably.     

成骨细胞的功能与损伤和骨质疏松的防治

骨质疏松是一种全身性骨骼疾病,导致骨折风险增加。成人的骨量通过破骨细胞的骨吸收和成骨细胞的骨形成作用来维持动态平衡,治疗骨质疏松症的理想策略是抑制破骨细胞的骨吸收和/或增强成骨细胞的骨形成功能。目前针对保护成骨细胞及增强其功能的骨质疏松疗法相对较少。因此,本文针对成骨细胞相关功能蛋白、各种细胞损伤机制（内质网应激、氧化应激、机械过载、微小RNA和长链非编码RNA的影响等）及骨质疏松的治疗与预防作一综述,以期为针对增强成骨细胞功能的骨质疏松治疗策略提供新思路。     

Self-stimulation and amphetamine: Tolerance to d and l isomers and cross tolerance to cocaine and methylphenidate

The effects of the d and l isomers of amphetamine on self-stimulation responding were tested following acute and chronic administration. Tolerance and post-drug depression of responding occurred in tests with both isomers, indicating no role for p-hydroxynorephedrine (PHN) which is one of the metabolites of d-amphetamine. In the second experiment, d-amphetamine, methylphenidate and cocaine all produced quantitatively and qualitatively similar effects on self-stimulation responding following acute administration. Following chronic administration of d-amphetamine, animals showed tolerance to all three drugs, indicating cross-tolerance among them. These data are consistent with an hypothesis that tolerance and post-drug depression following chronic amphetamine treatment are the result of decreases in postsynaptic receptor sensitivity, which would lead to a decreased effectiveness of all three drugs, regardless of their pre-synaptic mechanisms.     

益生菌与肿瘤防治

益生菌广泛存在于自然界中,通过维持宿主体内菌群平衡、影响肠屏障功能和调节免疫应答等作用,提高宿主健康水平,被公认为"肠道健康卫士".一些益生菌可以增强机体的免疫功能,抑制致癌物质,影响肿瘤细胞的基因表达,对肿瘤具有拮抗作用.大量研究表明,益生菌在未来的肿瘤防治中有很好的应用和发展前景.     

Acamprosate and naltrexone treatment effects on ethanol and sucrose seeking and intake in ethanol-dependent and nondependent rats

Rationale  Two pharmacotherapies are approved for treating alcohol craving (acamprosate and naltrexone), but both have shown mixed findings in animals and humans. Objectives  The present experiments utilized a “reinforcer blocking” approach (i.e., rats were able to consume ethanol during treatment) to better understand the efficacy of these treatments for ethanol seeking and drinking using ethanol-dependent and nondependent rats. Materials and methods  In “nondependent” experiments, drugs (acamprosate 50, 100, and 200 mg/kg; naltrexone 0.1, 0.3, and 1.0 mg/kg) were administered over 3-week periods prior to operant sessions with a low response requirement to gain access to reinforcers for 20 min. For “dependent” experiments, rats were made dependent in vapor/inhalation chambers. Results  Acamprosate and naltrexone had similar effects on intake in nondependent and dependent rats; neither drug was selective for ethanol over sucrose drinking. In nondependent animals, naltrexone was more efficacious at more doses than acamprosate, and acamprosate’s effects were limited to a dose that also had adverse effects on body weight. Both pharmacotherapies showed more selectivity when examining reinforcer seeking. In nondependent rats, acamprosate and naltrexone had response-attenuating effects in ethanol, but not sucrose, groups. In dependent animals, acamprosate had selective effects limited to a decrease in sucrose seeking. Naltrexone, however, selectively decreased ethanol-seeking in nondependent rats. Conclusions  The naltrexone-induced decreases in seeking suggested a change in incentive motivation which was selective for ethanol in nondependent rats. The “nondependent” paradigm may model early stages of “problem drinking” in humans, and the findings suggest that naltrexone could be a good intervention for this level of alcohol abuse and relapse prevention.     

Antiinfective and encrustation-inhibiting materials--myth and facts

Catheters, urethral and ureteral stents and other urological implants are frequently affected by encrustration and infection due to their permanent contact with urine. Indwelling urinary catheters provide a haven for microorganisms and thus require extensive monitoring. Several surface modification techniques have been proposed to improve the performance of devices including the immobilization of biomolecules, the incorporation of hydrophilic grafts to reduce protein adsorption, the creation of hydrophobic surfaces, the creation of microdomains to regulate cellular and protein adhesion, new polymers and antimicrobial coatings. Physico-chemical explanation to elucidate the mechanism of such encrustation or infection inhibiting materials is still not available. Our series of experiments showed a marked decrease of silver-activity in biological fluids which corresponds with the controversial clinical results obtained with silver coated urinary catheters. Rifampicin/minocycline coated catheters had very low activity against Gram-negative rods, enterococci and Candida spp., the main causing organisms of urinary catheter infection. Surface engineered materials and antimicrobial drug delivery systems will be the next generation of sophisticated urinary catheters and stents, if both efficacy as well as efficiency has been proved clinically.     

Alprazolam and lorazepam single and multiple-dose effects on psychomotor skills and sleep

Summary The effects of alprazolam 0.5 mg and lorazepam 2 mg on cognitive and psychomotor skills were assessed in twelve normal volunteer subjects in a randomised, double-blind, crossover design. Single and multiple dose effects were monitored using a battery of tests comprising critical flicker fusion threshold (CFFT), choice reaction time (CRT), simulated car tracking, and subjective ratings of perceived sedation (LARS) and of sleep behaviour (LSEQ). Compared with placebo baseline scores, treatment with lorazepam 2 mg (both single and multiple doses) resulted in a widespread impairment of CRT, tracking accuracy, and CFFT. Single doses of alprazolam 0.5 mg reduced CFFT with respect to the placebo baseline. Single and multiple dose treatment with both drugs resulted in subjective reports of sedation, a reduction of sleep onset latency, and improved sleep quality. Only lorazepam 2 mg significantly disrupted the integrity of behaviour on waking from sleep. These results suggest important pharmacodynamic differences between the two drugs in the doses used.