• 1 Antioxidant activity of Erica arborea. 复制标题 收藏 收藏

    【埃里卡(Erica arborea)的抗氧化活性。】 复制标题 收藏 收藏
    DOI:10.1016/j.fitote.2007.03.024 复制DOI
    作者列表:Ay M,Bahadori F,Oztürk M,Kolak U,Topçu G
    BACKGROUND & AIMS: :The antioxidant properties of the methanol extract of leaves and flowers of Erica arborea and the ethyl acetate, butanol and water soluble fractions were investigated. The ethyl acetate extract was found to be the richest for phenolic and flavonoid content which showed the highest antioxidant activity.
    背景与目标: :研究了Erica arborea的叶子和花朵的甲醇提取物以及乙酸乙酯,丁醇和水溶性馏分的抗氧化性能。发现乙酸乙酯提取物中酚和类黄酮含量最丰富,显示出最高的抗氧化活性。
  • 【新型抗氧化剂制剂在囊性纤维化患者中的安全性和有效性的初步研究。】 复制标题 收藏 收藏
    DOI:10.1016/j.jcf.2007.05.001 复制DOI
    作者列表:Papas KA,Sontag MK,Pardee C,Sokol RJ,Sagel SD,Accurso FJ,Wagener JS
    BACKGROUND & AIMS: BACKGROUND:Pancreatic insufficiency and a diminished bile acid pool cause malabsorption of important essential nutrients and other dietary components in cystic fibrosis (CF). Of particular significance is the malabsorption of fat-soluble antioxidants such as carotenoids, tocopherols and coenzyme Q(10) (CoQ(10)). Despite supplementation, CF patients are often deficient in these compounds, resulting in increased oxidative stress, which may contribute to adverse health effects. This pilot study was designed to evaluate the safety of a novel micellar formulation (CF-1) of fat-soluble nutrients and antioxidants and to determine its efficacy in improving plasma levels of these compounds and reducing inflammatory markers in induced sputum. METHODS:Ten CF subjects, ages 8 to 45 years old, were given orally 10 ml of the CF-1 formulation daily for 56 days after a 21-day washout period in which subjects stopped supplemental vitamin use except for a standard multivitamin. Plasma obtained at -3, 0 (baseline), 1, 2, 4, and 8 weeks was assayed for beta-carotene, gamma-tocopherol, retinol, and CoQ(10) as well as for safety parameters (comprehensive metabolic panel and complete blood count). In addition, pulmonary function was measured and induced sputum was assayed for markers of inflammation and quantitative bacterial counts both prior and during dosing. RESULTS:No serious adverse effects, laboratory abnormalities or elevated nutrient levels (above normal) were identified as related to CF-1. Supplementation with CF-1 significantly increased beta-carotene levels at all dosing time points when compared to screening and baseline. In addition, gamma-tocopherol and CoQ(10) significantly increased from baseline in all subjects. Induced sputum myeloperoxidase significantly decreased and there was a trend toward decreases in PMN elastase and total cell counts with CF-1. There was a significant inverse correlation between the antioxidant levels and induced sputum changes in IL-8 and total neutrophils. Lung function and sputum bacterial counts were unchanged. CONCLUSION:The novel CF-1 formulation safely and effectively increased plasma levels of important fat-soluble nutrients and antioxidants. In addition, improvements in antioxidant plasma levels were associated with reductions in airway inflammation in CF patients.
    背景与目标: 背景:胰腺功能不全和胆汁酸池减少导致囊性纤维化(CF)中重要的必需营养素和其他饮食成分吸收不良。特别重要的是脂溶性抗氧化剂,如类胡萝卜素,生育酚和辅酶Q(10)(CoQ(10))的吸收不良。尽管进行了补充,但CF患者通常缺乏这些化合物,导致氧化应激增加,这可能对健康产生不利影响。这项初步研究旨在评估脂溶性营养物质和抗氧化剂的新型胶束制剂(CF-1)的安全性,并确定其在改善这些化合物的血浆水平和减少诱导痰中的炎性标志物方面的功效。
    方法:在21天的清除期后的56天内,每天对10位年龄在8至45岁的CF受试者口服10 ml的CF-1制剂,持续56天,在此期间受试者停止补充维生素的使用,但标准的多种维生素除外。测定在-3、0(基准),1、2、4和8周时获得的血浆中的β-胡萝卜素,γ-生育酚,视黄醇和CoQ(10)以及安全性参数(全面的代谢检查和完整血球计数)。另外,在给药之前和给药期间,测量肺功能并测定诱导痰中的炎症标志物和定量细菌计数。
    结果:未发现与CF-1相关的严重不良反应,实验室异常或营养水平升高(高于正常水平)。与筛选和基线相比,在所有给药时间点补充CF-1都会显着增加β-胡萝卜素的水平。此外,所有受试者的γ-生育酚和辅酶Q(10)均较基线显着增加。诱导的痰髓过氧化物酶显着减少,并且CFN导致PMN弹性蛋白酶和总细胞数减少。 IL-8和总中性粒细胞的抗氧化剂水平与诱导的痰液变化之间存在显着的负相关。肺功能和痰细菌计数不变。
    结论:新型CF-1制剂可安全有效地增加血浆中重要脂溶性营养素和抗氧化剂的含量。另外,抗氧化剂血浆水平的改善与CF患者气道炎症的减轻有关。
  • 【刺五加茎和芽中的酚类化合物和抗氧化活性。】 复制标题 收藏 收藏
    DOI: 复制DOI
    作者列表:Samejo MQ,Memon S,Khan KM,Rajput SM,Gul S,Memon GZ,Panhwar QK
    BACKGROUND & AIMS: :In the present study we demonstrate the identification of phenolic compounds and the phenolic contents of the methanol extracts from stem and buds of Calligonum polygonoides with antioxidant activity. Eleven and nine phenolic compounds were identified and quantified from stem and buds, respectively by high-performance liquid chromatography (HPLC). p-Coumaric acid was predominant in stem and gallic acid in buds. In general, the samples with the highest phenolic contents had the highest antioxidant activities. Stem and buds sparked attention due to their high phenolic contents and antioxidant activities. The Results from present study reveal that the C. polygonoides could be considered as a promising source of antioxidant phytochemicals.
    背景与目标: :在本研究中,我们证明了从具有抗氧化活性的南方五倍体茎和芽中提取的酚类化合物和甲醇提取物中的酚类含量。通过高效液相色谱(HPLC)分别从茎和芽中鉴定和定量了11种和9种酚类化合物。对香豆酸主要在茎中,而没食子酸则在芽中。通常,酚含量最高的样品具有最高的抗氧化活性。茎和芽因其较高的酚含量和抗氧化活性而引起人们的注意。本研究的结果表明,多角梭菌可以被认为是抗氧化剂植物化学物质的有前途的来源。
  • 【蓝莓,燕麦粉和牛奶对多酚,抗氧化活性和潜在生物利用度的基质作用。】 复制标题 收藏 收藏
    DOI:10.3109/09637486.2013.825699 复制DOI
    作者列表:Cebeci F,Şahin-Yeşilçubuk N
    BACKGROUND & AIMS: :In recent years, ready-to eat breakfast cereals prepared with fruit ingredients have gained particular attention due to their polyphenolic contents and health promoting effects. In this study, the matrix effect of blueberry, oat meal, whole milk or skimmed milk on polyphenols, antioxidative potential as well as their potential bioavailability were investigated. The phenolic properties of whole milk, skimmed milk, blueberry and oat meal were investigated and the changes in combinations of the ingredients were determined. Milk addition decreased the total phenolic, flavonoid and anthocyanin content of samples statistically and had negative effect on antioxidant activity showing differences among different methods. According to HPLC results, it was not possible to detect catechin in mixtures due to milk addition. In vitro digestion method was used to determine potential bioavailability of phenolic compounds. According to in vitro digestion procedure results, whole or skimmed milk did not affect the total phenolic content of the proportion passing to the blood from intestine.
    背景与目标: :近年来,以水果成分制成的即食早餐谷物由于其多酚含量和促进健康的作用而受到特别关注。在这项研究中,研究了蓝莓,燕麦粉,全脂牛奶或脱脂牛奶对多酚,抗氧化潜力及其潜在生物利用度的基质作用。研究了全脂牛奶,脱脂牛奶,蓝莓和燕麦粉的酚类性质,并确定了成分组合的变化。牛奶的添加统计地降低了样品中总酚,类黄酮和花青素的含量,并对抗氧化活性产生了负面影响,表明不同方法之间存在差异。根据HPLC结果,由于添加了牛奶,因此无法检测混合物中的儿茶素。体外消化法用于确定酚类化合物的潜在生物利用度。根据体外消化程序的结果,全脂或脱脂牛奶不影响从肠传递到血液的总酚含量。
  • 【橙皮苷和新橙皮苷二氢查耳酮的体外清除剂和抗氧化性能。】 复制标题 收藏 收藏
    DOI:10.1016/S0944-7113(98)80044-5 复制DOI
    作者列表:Suarez J,Herrera MD,Marhuenda E
    BACKGROUND & AIMS: :We have assesed the actions as free radical scavengers and inhibitors on peroxidation of hesperidin and neohesperidin dihydrochalcone, two flavonoids, flavanone and dihydrochalcone respectively, as some of the pharmacological properties of flavonoids group have been related with these activities. Hesperidin just at 10(-4) and 5 · 10(-4)M is able to show a low inhibitory activity in the superoxide anion radicals (O(2)(-)) genesis (8.66 ± 1.40 and 11.69 ± 2.36% respectively), and on the non-enzymatic lipid peroxidation at 10(-3)M dose (9.78 ± 0.35%), without affecting the hydroxyl radical (•OH) formation, generated by the ascorbic acid-Fe(3+)-EDTA system. In the other hand, neohesperidin dihydrochalcone is an authentic antioxidant drug as tested at all doses. It showed a great scavenger activity and/or inhibition of formation on O(2)(-) radicals (31.53 - 84.62%) and a significant scavenging effect on OH radicals (6.00 - 23.49%), as well as an important inhibitory action on non-enzymatic lipid peroxidation (15.43-95.33%).
    背景与目标: :我们评估了自由基清除剂和抑制剂对橙皮苷和新橙皮苷二氢查尔酮,两种黄酮,黄烷酮和二氢查尔酮的过氧化的作用,因为类黄酮类的某些药理特性与这些活性有关。橙皮苷仅在10(-4)和5·10(-4)M时对超氧阴离子自由基(O(2)(-))的产生具有较低的抑制活性(分别为8.66±1.40和11.69±2.36% ),并且在10(-3)M剂量(9.78±0.35%)的非酶促脂质过氧化作用下,不影响抗坏血酸-Fe(3)-EDTA系统生成的羟基自由基(•OH)的形成。另一方面,新橙皮苷二氢查耳酮是一种经过验证的真正抗氧化剂,在所有剂量下均已测试。它显示出强大的清除剂活性和/或对O(2)(-)自由基的形成的抑制作用(31.53-84.62%)和对OH自由基的显着清除作用(6.00-23.49%),以及对OH自由基的重要抑制作用非酶脂质过氧化(15.43-95.33%)。
  • 【小碱-噻吩杂化物作为多功能试剂的合成及生物学评估:抑制乙酰胆碱酯酶,丁酰胆碱酯酶,Aβ聚集和抗氧化活性。】 复制标题 收藏 收藏
    DOI:10.1016/j.bmc.2013.07.011 复制DOI
    作者列表:Su T,Xie S,Wei H,Yan J,Huang L,Li X
    BACKGROUND & AIMS: :A series of berberine-thiophenyl hybrids were designed, synthesised, and evaluated as inhibitors of acetylcholinesterase (AChE), butyrylcholinesterase (BuChE) and β-amyloid (Aβ) aggregation and as antioxidants. Among these hybrids, compounds 4f and 4i, berberine linked with o-methylthiophenyl and o-chlorothiophenyl by a 2-carbon spacer, were observed to be potent inhibitors of AChE, with IC50 values of 0.077 and 0.042 μM, respectively. Of the tested compounds, 4i was also the most potent inhibitor of BuChE, with an IC50 value of 0.662 μM. Kinetic studies and molecular modelling simulations of the AChE-inhibitor complex indicated that a mixed-competitive binding mode existed for these berberine derivatives. The biological studies also demonstrated that these hybrids displayed interesting activities, including Aβ aggregation inhibition and antioxidant properties.
    背景与目标: :设计,合成并评估了一系列小ber碱-硫代苯基杂化物,作为乙酰胆碱酯酶(AChE),丁酰胆碱酯酶(BuChE)和β-淀粉样蛋白(Aβ)聚集的抑制剂和抗氧化剂。在这些杂种中,观察到化合物4f和4i(通过2碳间隔基与邻甲基硫代苯基和邻氯硫代苯基连接的小ber碱)是有效的AChE抑制剂,IC50值分别为0.077和0.042μM。在测试的化合物中,4i也是BuChE的最强抑制剂,IC50值为0.662μM。 AChE抑制剂复合物的动力学研究和分子建模模拟表明,这些小ber碱衍生物存在混合竞争结合模式。生物学研究还表明,这些杂种表现出有趣的活性,包括抑制Aβ聚集和抗氧化性能。
  • 【希腊Amyntaio电站煤粉褐煤,底灰和飞灰中微量元素的行为研究。】 复制标题 收藏 收藏
    DOI:10.1007/s10661-012-3007-0 复制DOI
    作者列表:Megalovasilis P,Papastergios G,Filippidis A
    BACKGROUND & AIMS: :The Kozani-Ptolemais-Amyntaio basin constitutes the principal coal field of Greece. Approximately 50% of the total power production of Greece is generated by five power stations operating in the area. Lignite samples, together with the corresponding fly ash and bottom ash were collected, over a period of 3 months, from the power plant of Amyntaio and analyzed for their content in 16 trace elements. The results indicate that Y, Nb, U, Rb, Zr, Ni, Pb, Ba, Zn, Sr, Cu, and Th demonstrate an organic affinity during the combustion of lignite, while V has an inorganic affinity. Three elements (Co, Cr, and Sc) show an intermediate affinity.
    背景与目标: :Kozani-Ptolemais-Amyntaio盆地是希腊的主要煤田。希腊约有50%的电力生产是由该地区的五个发电厂产生的。在3个月内,从Amyntaio电厂收集了褐煤样品以及相应的粉煤灰和底灰,并分析了16种微量元素的含量。结果表明,Y,Nb,U,Rb,Zr,Ni,Pb,Ba,Zn,Sr,Cu和Th在褐煤燃烧过程中表现出有机亲和力,而V具有无机亲和力。三个元素(Co,Cr和Sc)显示出中等亲和力。
  • 【减少辐射暴露的个人经验:切尔诺贝利事故发生后的前两周,在基辅保护家庭。】 复制标题 收藏 收藏
    DOI:10.1097/01.HP.0000226143.54179.dd 复制DOI
    作者列表:Eremenko VA,Droppo JG Jr
    BACKGROUND & AIMS: :The Chernobyl nuclear reactor accident occurred in 1986. The plume from the explosions and fires was highly radioactive and resulted in very high exposure levels in the surrounding regions. This paper describes how the people in Kiev, Ukraine, a city 120 km (90 miles) south of Chernobyl, and in particular one individual in that city, Professor Vitaly Eremenko, became aware of the threat before the official announcement and the steps he took to mitigate potential impacts to his immediate family. The combination of being informed and using available resources led to greatly reduced consequences for his family and, in particular, his newborn granddaughter. He notes how quickly word of the some aspects of the hazard spread in the city and how other aspects appear to not have been understood. Although these events are being recalled as the 20 anniversary of the terrible event approaches, the lessons are still pertinent today. Threats of possible terrorist use of radiation dispersal devices makes knowledge of effective individual actions for self-protection from radiation exposures a topic of current interest.
    背景与目标: 切尔诺贝利核反应堆事故发生在1986年。爆炸和大火中的烟流具有很高的放射性,并导致周围地区的暴露水平很高。本文介绍了乌克兰基辅市(切尔诺贝利以南120公里(90英里))的人们,尤其是该市的一个人维塔利·埃雷缅科(Vitaly Eremenko)教授在正式宣布宣布采取行动之前如何意识到这一威胁以及他采取的措施减轻对他的直系亲属的潜在影响。知情和使用可用资源的结合,大大减少了对他的家人,特别是对他的新生孙女的影响。他指出,危害的某些方面在城市中传播的速度有多快,而其他方面似乎还没有被理解。尽管这些事件是在可怕事件发生20周年之际被召回的,但今天的课程仍然有意义。恐怖分子可能会使用辐射扩散装置来构成威胁,这使人们了解有效的个人防护措施,以自我保护免受辐射照射成为当前关注的话题。
  • 【氯化亚铁可下调小鼠对金黄色红球菌感染的炎症反应。】 复制标题 收藏 收藏
    DOI:10.1248/bpb.b12-00672 复制DOI
    作者列表:Yimin,Tao H,Kohanawa M,Zhao S,Kuge Y,Tamaki N
    BACKGROUND & AIMS: :The healthy drink Pairogen is mainly composed of ferrous ferric chloride water that reportedly changes the status of intracellular water from oxidative to antioxidative. Here, we investigated whether Pairogen affects host immune function in a murine model of granulomatous inflammation in response to Rhodococcus aurantiacus (R. aurantiacus) infection. Longitudinal ingestion of Pairogen markedly improved the survival of infected mice in a concentration-dependent manner. Compared to mice received water, mice that ingested 10-fold-diluted Pairogen displayed rapid bacterial elimination, decreased production of tumor necrosis factor (TNF)-α and interleukin (IL)-6, and high levels of IL-10 in organs during the initial phase of infection. Moreover, histological studies showed significant reduction in the number and size of granulomas as well as amelioration of oxidative stress in the livers of mice ingested 10-fold-diluted Pairogen at 14 d post-infection. These characteristics were further pronounced in first-generation (F1) mice that also ingested 10-fold-diluted Pairogen. Following stimulation with heat-killed R. aurantiacus, the production of TNF-α, IL-6, and IL-10 by macrophages from F1 mice was similar to that detected in vivo, while their gene expression levels in these cells were significantly lower than the levels in macrophages from mice received water. Heat-killed R. aurantiacus also induced the expression of heme oxygenase-1 mRNA in the cells from F1 mice. Taken together, these results indicate that Pairogen contributes to the negative regulation of the immuno-inflammatory response to R. aurantiacus infection in mice by modulating the cellular redox state. Longitudinal ingestion of Pairogen further enhances the defense function in mouse progeny.
    背景与目标: 健康饮品Pairogen主要由氯化亚铁水组成,据报道,其改变了细胞内水的状态,从氧化性变为抗氧化性。在这里,我们调查了Pairogen是否会影响肉芽肿性炎症小鼠模型中的宿主免疫功能,以应对金黄色葡萄球菌(R. aurantiacus)感染。纵向摄入Pairogen可以显着提高被感染小鼠的存活率,且浓度依赖性。与接受水的小鼠相比,摄入10倍稀释的Pairogen的小鼠在该过程中表现出快速的细菌清除,降低的肿瘤坏死因子(TNF)-α和白介素(IL)-6的产生以及高水平的IL-10。感染的初始阶段。此外,组织学研究表明,感染后14 d摄入10倍稀释的Pairogen的小鼠肝脏中肉芽肿的数量和大小显着减少,并且氧化应激得到改善。这些特征在也摄取了10倍稀释的Pairogen的第一代(F1)小鼠中更加明显。用热杀死的金黄色葡萄球菌刺激后,F1小鼠巨噬细胞产生的TNF-α,IL-6和IL-10与体内检测到的相似,而它们在这些细胞中的基因表达水平明显低于老鼠的巨噬细胞中的水平接受了水。热杀死的金黄色葡萄球菌还诱导了F1小鼠细胞中血红素加氧酶-1 mRNA的表达。综上所述,这些结果表明Pairogen通过调节细胞的氧化还原状态,对小鼠对金黄色葡萄球菌感染的免疫炎症反应作出了负调控。纵向摄取Pairogen可以进一步增强小鼠后代的防御功能。
  • 【(S,S)-和(R,R)-癸二异水芹树脂二糖苷(SDGs)的合成和抗氧化剂评估。】 复制标题 收藏 收藏
    DOI:10.1016/j.bmcl.2013.07.062 复制DOI
    作者列表:Mishra OP,Simmons N,Tyagi S,Pietrofesa R,Shuvaev VV,Valiulin RA,Heretsch P,Nicolaou KC,Christofidou-Solomidou M
    BACKGROUND & AIMS: :Secoisolariciresinol diglucosides (SDGs) (S,S)-SDG-1 (major isomer in flaxseed) and (R,R)-SDG-2 (minor isomer in flaxseed) were synthesized from vanillin via secoisolariciresinol (6) and glucosyl donor 7 through a concise route that involved chromatographic separation of diastereomeric diglucoside derivatives (S,S)-8 and (R,R)-9. Synthetic (S,S)-SDG-1 and (R,R)-SDG-2 exhibited potent antioxidant properties (EC50=292.17±27.71 μM and 331.94±21.21 μM, respectively), which compared well with that of natural (S,S)-SDG-1 (EC50=275.24±13.15 μM). These values are significantly lower than those of ascorbic acid (EC50=1129.32±88.79 μM) and α-tocopherol (EC50=944.62±148.00 μM). Compounds (S,S)-SDG-1 and (R,R)-SDG-2 also demonstrated powerful scavenging activities against hydroxyl [natural (S,S)-SDG-1: 3.68±0.27; synthetic (S,S)-SDG-1: 2.09±0.16; synthetic (R,R)-SDG-2: 1.96±0.27], peroxyl [natural (S,S)-SDG-1: 2.55±0.11; synthetic (S,S)-SDG-1: 2.20±0.10; synthetic (R,R)-SDG-2: 3.03±0.04] and DPPH [natural (S,S)-SDG-1: EC50=83.94±2.80 μM; synthetic (S,S)-SDG-1: EC50=157.54±21.30 μM; synthetic (R,R)-SDG-2: EC50=123.63±8.67 μM] radicals. These results confirm previous studies with naturally occurring (S,S)-SDG-1 and establish both (S,S)-SDG-1 and (R,R)-SDG-2 as potent antioxidants and free radical scavengers for potential in vivo use.
    背景与目标: :香豆素中的异麦草烯醇二葡萄糖苷(SDGs)(S,S)-SDG-1(亚麻籽中的主要异构体)和(R,R)-SDG-2(亚麻子中的次要异构体)是通过香豆素通过芥子异豆香树脂醇(6)和葡萄糖基供体7合成的通过简洁的方法,包括非对映体二糖苷衍生物(S,S)-8和(R,R)-9的色谱分离。合成的(S,S)-SDG-1和(R,R)-SDG-2表现出强大的抗氧化性能(分别为EC50 = 292.17±27.71μM和331.94±21.21μM),与天然(S,S)-SDG-1 S)-SDG-1(EC50 = 275.24±13.15μM)。这些值显着低于抗坏血酸(EC50 = 1129.32±88.79μM)和α-生育酚(EC50 = 944.62±148.00μM)的值。化合物(S,S)-SDG-1和(R,R)-SDG-2也显示出对羟基[天然(S,S)-SDG-1的强大的清除活性:3.68±0.27; m / z]。合成的(S,S)-SDG-1:2.09±0.16;合成的(R,R)-SDG-2:1.96±0.27],过氧[自然的(S,S)-SDG-1:2.55±0.11;合成(S,S)-SDG-1:2.20±0.10;合成的(R,R)-SDG-2:3.03±0.04]和DPPH [天然的(S,S)-SDG-1:EC50 = 83.94±2.80μM;合成(S,S)-SDG-1:EC50 = 157.54±21.30μM;合成的(R,R)-SDG-2:EC50 = 123.63±8.67μM]自由基。这些结果证实了以前对天然存在的(S,S)-SDG-1的研究,并确定了(S,S)-SDG-1和(R,R)-SDG-2都是潜在的体内潜在抗氧化剂和自由基清除剂用。
  • 【α-树突毒素和树突毒素K对麻醉大鼠海马中细胞外兴奋性氨基酸和脑电图谱功率的影响。】 复制标题 收藏 收藏
    DOI:10.1016/s0304-3940(00)01530-5 复制DOI
    作者列表:Richards DA,Morrone LA,Bagetta G,Bowery NG
    BACKGROUND & AIMS: :Dendrotoxins, important pharmacological tools for studying K(+) channels, are potently convulsant in the central nervous system and evidence suggests that different members of the dendrotoxin family may act at pre- or post-synaptic sites. Using a combination of intrahippocampal infusion, microdialysis and electroencephalograph (EEG) recording, we have compared the effects of alpha-dendrotoxin and dendrotoxin K on extracellular levels of excitatory amino acids in anaesthetised rats. Our findings show that although infusion of 35 pmol of both peptides was associated with elevated extracellular aspartate and glutamate, these increased levels were more sustained with dendrotoxin K. Furthermore, there was EEG evidence of an associated transient functional change consistent with an action on pre-synaptic K(+) channels. In contrast, infusion of alpha-dendrotoxin produced only a brief effect on amino acid levels and no evidence of a functional consequence.
    背景与目标: :Dendrotoxins是研究K()通道的重要药理工具,在中枢神经系统中很强惊厥,证据表明树突毒素家族的不同成员可能在突触前或突触后部位起作用。使用海马内输注,微透析和脑电图(EEG)记录的组合,我们比较了α-树突毒素和树突毒素K对麻醉大鼠兴奋性氨基酸细胞外水平的影响。我们的发现表明,尽管输注35 pmol的两种肽都与升高的细胞外天冬氨酸和谷氨酸有关,但树突毒素K可使这些升高的水平更持久。突触K()通道。相反,输注α-树突毒素仅对氨基酸水平产生短暂影响,而没有功能后果的证据。
  • 【博来霉素,放线菌素-D和顺铂治疗卵巢生殖细胞恶性肿瘤有助于减少药物不良反应。】 复制标题 收藏 收藏
    DOI:10.3892/or.7.6.1235 复制DOI
    作者列表:Sumi T,Ishiko O,Yoshida H,Ogita S
    BACKGROUND & AIMS: :Sixteen ovarian germ-cell malignancy (OGCM) patients between 1983 and 1999 were randomly divided into the BEP group (n=6; bleomycin, etoposide and cisplatin) and the BAP group (n=10; bleomycin, actinomycin-D and cisplatin). The patients were evaluated for adverse drug reactions (ADRs) based on severity-grading of the National Cancer Institute Common Toxicity Criteria. The ADRs in the BAP group were milder than in the BEP group, as seen in regard to alopecia (p=0.0126), low hemoglobin (p=0.0147), and decreased neutrophil count (p=0.0197). The five-year survival rate was 87.5% in the BAP group and 83.3% in the BEP group, and the difference was not significant (p=0.5954). BAP therapy is likely to be more beneficial for OGCM patients than BEP therapy, because ADRs are reduced with no difference in outcome.
    背景与目标: :1983年至1999年间,将16例卵巢生殖细胞恶性肿瘤(OGCM)随机分为BEP组(n = 6;博来霉素,依托泊苷和顺铂)和BAP组(n = 10;博来霉素,放线菌素D和顺铂) 。根据美国国家癌症研究所共同毒性标准的严重程度对患者进行药物不良反应(ADR)评估。就脱发(p = 0.0126),低血红蛋白(p = 0.0147)和中性粒细胞减少(p = 0.0197)而言,BAP组的ADR比BEP组轻。 BAP组的五年生存率为87.5%,BEP组的为83.3%,差异不显着(p = 0.5954)。与AEP疗法相比,BAP疗法对OGCM患者可能更有益,因为ADR减少且结果无差异。
  • 【评价蜜糖腰果苹果花蜜的抗氧化和诱变活性。】 复制标题 收藏 收藏
    DOI:10.1016/j.fct.2013.08.026 复制DOI
    作者列表:da Silva RA,Dihl RR,Nascimento e Santos D,de Abreu BR,de Lima A,de Andrade HH,Lehmann M
    BACKGROUND & AIMS: :In vitro chemical properties and antioxidant potential and in vivo mutagenic activity of honey-sweetened cashew apple nectar (HSCAN), a beverage produced from the cashew pseudo-fruit (Anacardium occidentale L.) and of its constituents were assessed. Analytical procedures were carried out to investigate the honey used in the HSCAN preparation, and the results observed are in accordance with Brazilian legal regulations, except for diastase number. HSCAN and pulp were investigated for ascorbic acid, carotenoid, anthocyanin and total phenolic contents, and both showed high acid ascorbic concentrations. Antioxidant capacity using 2,2-diphenyl-1-picrylhydrazyl radical (DPPH) and/or β-carotene/linoleic acid systems were applied and demonstrated a weak antioxidant capacity of honey and HSCAN, but cashew apple pulp demonstrated high antioxidant capacity. A weakly positive mutagenic effect of cashew pulp 20% was observed using the somatic mutation and recombination test (SMART) in Drosophila melanogaster only in the high-bioactivation (HB) cross. On the contrary, HSCAN was not mutagenic in both standard and high bioactivation crosses. HSCAN exhibited slight antioxidant activity, which could be associated with the high amount of ascorbic acid found in the samples evaluated. The beverage prepared did not induce DNA damage in somatic cells of D. melanogaster, which means that it is neither mutagenic nor recombinagenic in this test system.
    背景与目标: :对蜂蜜加糖的腰果苹果花蜜(HSCAN)的体外化学性质,抗氧化剂潜力和体内诱变活性进行了评估,该饮料是由腰果假果(Anacardium occidentale L.)生产的饮料及其成分。进行了分析程序以调查HSCAN制剂中使用的蜂蜜,观察到的结果符合巴西法律法规,但发乳酶数量除外。对HSCAN和纸浆进行了抗坏血酸,类胡萝卜素,花色苷和总酚含量的调查,结果均显示出较高的酸性抗坏血酸浓度。应用了使用2,2-二苯基-1-吡啶并肼基(DPPH)和/或β-胡萝卜素/亚油酸体系的抗氧化能力,证明了蜂蜜和HSCAN的抗氧化能力较弱,但腰果苹果浆显示出较高的抗氧化能力。仅在高生物激活(HB)杂交中,使用果蝇果蝇的体细胞突变和重组试验(SMART)观察到了腰果果肉20%的弱阳性诱变作用。相反,HSCAN在标准和高生物激活杂交中均不致突变。 HSCAN表现出轻微的抗氧化活性,这可能与所评估样品中发现的大量抗坏血酸有关。所制备的饮料不会在黑腹果蝇的体细胞中引起DNA损伤,这意味着该饮料在该测试系统中既不诱变也不重组。
  • 【ERα表达缺失的内分泌抗性乳腺癌细胞通过减少caspase7介导的HDAC3裂解而保留了增殖能力。】 复制标题 收藏 收藏
    DOI:10.1007/s13402-019-00439-x 复制DOI
    作者列表:Yu S,Gong X,Ma Z,Zhang M,Huang L,Zhang J,Zhao S,Zhu T,Yu Z,Chen L
    BACKGROUND & AIMS: PURPOSE:Endocrine therapy is the most commonly used approach for the treatment of estrogen receptor (ERα)-positive breast cancer. The cure rate of patients with ERα-positive breast cancer is, however, limited due to the occurrence of endocrine resistance. Loss of ERα is one major mechanism for the occurrence of endocrine resistance. Recent studies have shown that pan-HDAC inhibitors may be effective in reversing endocrine resistance. However, the molecular mechanism underlying this reversal has remained largely unknown. Here we aimed to unravel this mechanism. METHODS:Endocrine resistant breast cancer cell lines were established through exposure to tamoxifen. mRNA expression was assessed by qRT-PCR and protein expression by Western blotting. The effect of HDAC3 inhibition on the viability of endocrine resistant breast cancer cells was evaluated using CCK-8 and colony forming assays. Immunohistochemistry was used to detect protein expression in primary breast cancer tissues. RESULTS:We found that in endocrine resistant breast cancer cells loss of ERα led to HDAC3 stabilization via decreased ERα-mediated caspase7 expression, resulting in reduced caspase7-mediated HDAC3 cleavage. We also found that the ERα-caspase7-HDAC3 axis determined the global H3K9 and H4K16 acetylation status, which was positively correlated with ERα expression. Finally, we found that inhibition of HDAC3 significantly decreased the viability of endocrine resistant breast cancer cells exhibiting ERα deficiency. The ERα-caspase7-HDAC3 axis was subsequently verified in primary endocrine resistant breast cancer samples. CONCLUSIONS:From our data we conclude that the ERα-caspase7-HDAC3 axis may play a role in promoting the proliferation of endocrine resistant breast cancer cells. HDAC3 may serve as a therapeutic target for (a subset of) endocrine resistant breast cancers exhibiting ERα loss.
    背景与目标: 目的:内分泌治疗是治疗雌激素受体(ERα)阳性乳腺癌的最常用方法。然而,由于发生内分泌耐药性,ERα阳性乳腺癌患者的治愈率受到限制。 ERα的丢失是内分泌耐药性发生的主要机制之一。最近的研究表明,泛HDAC抑制剂可能有效逆转内分泌抵抗力。但是,这种逆转的分子机制仍是未知之数。在这里,我们旨在揭示这种机制。
    方法:通过接触他莫昔芬建立内分泌抗性乳腺癌细胞系。通过qRT-PCR评估mRNA表达,并通过蛋白质印迹法评估蛋白质表达。使用CCK-8和集落形成试验评估了HDAC3抑制对内分泌抗性乳腺癌细胞活力的影响。免疫组织化学用于检测原发性乳腺癌组织中的蛋白表达。
    结果:我们发现在内分泌抗性乳腺癌细胞中,ERα的丢失通过减少ERα介导的caspase7表达而导致HDAC3稳定,从而导致caspase7介导的HDAC3裂解减少。我们还发现,ERα-caspase7-HDAC3轴决定了整体H3K9和H4K16的乙酰化状态,这与ERα的表达呈正相关。最后,我们发现抑制HDAC3会显着降低表现出ERα缺乏的内分泌抗性乳腺癌细胞的活力。随后在原发性内分泌抵抗性乳腺癌样本中验证了ERα-caspase7-HDAC3轴。
    结论:根据我们的数据,我们得出结论,ERα-caspase7-HDAC3轴可能在促进内分泌抗性乳腺癌细胞的增殖中发挥作用。 HDAC3可以用作表现出ERα缺失的内分泌耐药性乳腺癌(的一部分)的治疗靶标。
  • 【运动训练和慢性摄入乙醇对大鼠肝脏和血浆抗氧化系统的相互作用。】 复制标题 收藏 收藏
    DOI:10.1002/(sici)1099-1263(199705)17:3<189::aid-jat43 复制DOI
    作者列表:Husain K,Somani SM
    BACKGROUND & AIMS: This study was undertaken in order to investigate the interactive effects of exercise training and chronic ethanol consumption on the antioxidant system in rat liver and plasma. Fisher-344 rats were treated in separate groups as followssedentary control (SC); exercise training (ET) for 6.5 weeks; ethanol 20% (2.0 g kg-1, p.o.) for 6.5 weeks; and ET and ethanol administration. In liver, ET significantly decreased the malondialdehyde (MDA) level (73% of SC). Chronic ethanol significantly increased catalase (CAT) activity and MDA levels (126% and 135% of SC), respectively, and also depleted the reduced glutathione (GSH) level and the reduced to oxidized glutathione (GSH/GSSG) ratio (81% and 38% of SC), respectively. Exercise training plus ethanol significantly increased CAT and glutathione reductase (GR) activity (126% and 118% of SC), respectively, and decreased the MDA level (67% of SC). In plasma, ethanol significantly enhanced CAT activity and MDA levels (173% and 221% of SC), respectively. Ethanol ingestion also increased the CAT/superoxide dismutase (SOD) ratio (216% of SC) in plasma. Training plus ethanol ingestion significantly increased CAT activity and MDA levels (208% and 148% of SC), respectively, and increased CAT/SOD and glutathione peroxidase (GSH-Px)/SOD ratios (279% and 142% of SC), respectively. The data indicate that the combination of exercise and ethanol ingestion resulted in an enhanced hepatic CAT and GR activity to eliminate H2O2 and to maintain endogenous GSH levels. Thus, training ameliorated the ethanol-induced oxidative injury in the liver. The ratio of CAT/SOD in plasma increased twofold due to chronic ethanol intake and threefold due to the combination, which may be used as an index of oxidative stress.

    背景与目标: 进行这项研究是为了研究运动训练和长期饮酒对大鼠肝脏和血浆中抗氧化系统的相互作用。将Fisher-344大鼠按以下对照进行单独治疗;运动训练(ET)6.5周;乙醇20%(2.0 g kg-1,p.o.)6.5周;以及ET和乙醇的管理。在肝脏中,ET显着降低了丙二醛(MDA)水平(SC的73%)。慢性乙醇分别显着增加过氧化氢酶(CAT)活性和MDA水平(SC的126%和135%),并且还减少了降低的谷胱甘肽(GSH)水平和降低的氧化型谷胱甘肽(GSH / GSSG)比例(分别为81%和分别为SC的38%)。运动训练加乙醇可显着提高CAT和谷胱甘肽还原酶(GR)的活性(分别为SC的126%和118%),并降低MDA水平(SC的67%)。在血浆中,乙醇显着提高了CAT活性和MDA水平(分别为SC的173%和221%)。摄入乙醇还会增加血浆中CAT /超氧化物歧化酶(SOD)的比例(SC的216%)。训练加乙醇摄入分别显着增加了CAT活性和MDA水平(分别为SC的208%和148%),并提高了CAT / SOD和谷胱甘肽过氧化物酶(GSH-Px)/ SOD的比率(分别为SC的279%和142%) 。数据表明,运动和乙醇摄入的结合导致增强的肝脏CAT和GR活性,从而消除了H2O2并维持了内源性GSH的水平。因此,训练减轻了乙醇引起的肝脏氧化损伤。血浆中CAT / SOD的比率由于长期摄入乙醇而增加了两倍,而由于二者的结合而增加了三倍,可用作氧化应激指标。

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