• 【巴杜拉 (Badula) 和狭叶 (empelia angustifolia) 对苯醌的生物学活性。】 复制标题 收藏 收藏
    DOI:10.1016/S0944-7113(98)80028-7 复制DOI
    作者列表:Lund AK,Adsersen A,Nyman U
    BACKGROUND & AIMS: :In our screening program for antihypertensive plant constituents extracts of the leaves and bark of Badula barthesia showed strong in vitro inhibition of angiotensin converting enzyme (ACE). Rapanone (1), 2,5-dihydroxy-3-tridecyl-1,4-benzoquinone, was isolated as an active constituent of the leaves. The IC(50) values of rapanone and three 3-alkyl-2,5-dihydroxybenzoquinones, (2)-(4), (Z)-2,5-dihydroxy-3-(pentadec-8-enyl)-1,4-benzoquinone, (Z,Z)-2,5-dihydroxy-3-(heptadeca-8,11-dienyl)-1,4-benzoqui-none and (Z)-2,5-dihydroxy-3-(heptadec-8-enyl)-1,4-benzoquinone recently isolated from Embelia angustifolia were determined. The following IC(50) ± S.D. values have been obtained (1) 36 ± 4.6 μM, (2) 19 ± 6.2 μM, (3) 19 ± 8.7 μM and (4) 16 ± 3.0 μ.M. The IC(50) value for the reference compound Captopril was determined to 12 ± 2.6 nM. The antimicrobial activity of the four compounds was determined by thin layer chromatography agar overlay technique as minimum growth inhibitory amount in μg. One yeast, Candida albicans, and four bacteria, Bacillus subtilis, Escherichia coli, Pseudomonas aeruginosa and Staphylococcus aureus were used as test organisms.
    背景与目标: : 在我们的抗高血压植物成分筛选程序中,巴杜拉 (Badula) 的叶片和树皮的提取物显示出对血管紧张素转化酶 (ACE) 的强烈体外抑制作用。分离出雷帕酮 (1),2,5-二羟基-3-三癸基-1,4-苯醌作为叶片的活性成分。雷帕酮和三种3-烷基-2,5-二羟基苯醌,(2)-(4),(Z)-2,5-二羟基-3-(pentadec-8-enyl)-1,4-苯醌,(Z,Z)-2,5-二羟基-3-(heptadeca-8,11-二烯基)-1,测定了最近从angustifolia中分离出的4-苯醌-none和 (Z)-2,5-二羟基-3-(heptadec-8-enyl)-1,4-苯醌。已获得以下IC(50) ± S.D. 值 (1) 36 ± 4.6微米,(2) 19 ± 6.2微米,(3) 19 ± 8.7微米和 (4) 16 ± 3.0微米。参考化合物卡托普利的IC(50) 值确定为12 ± 2.6 nM。通过薄层色谱琼脂覆盖技术确定四种化合物的抗菌活性为最小生长抑制量 (μ g)。以1个酵母菌、白色念珠菌和4个细菌、枯草芽孢杆菌、大肠杆菌、铜绿假单胞菌和金黄色葡萄球菌为试验生物。
  • 【一项基于网络的工作场所健康促进计划的现场测试,以改善饮食习惯,减轻压力并增加体育锻炼: 随机对照试验。】 复制标题 收藏 收藏
    DOI:10.2196/jmir.9.2.e17 复制DOI
    作者列表:Cook RF,Billings DW,Hersch RK,Back AS,Hendrickson A
    BACKGROUND & AIMS: BACKGROUND:Most work sites engage in some form of health promotion programming designed to improve worker health and reduce health care costs. Although these programs have typically been delivered through combinations of seminars and print materials, workplace health promotion programs are increasingly being delivered through the Internet. OBJECTIVE:The purpose of this research was to evaluate the effectiveness of a Web-based multimedia health promotion program for the workplace, designed to improve dietary practices, reduce stress, and increase physical activity. METHODS:Using a randomized controlled trial design with pretest-posttest comparisons within each group, 419 employees of a human resources company were randomly assigned to the Web-based condition or to a condition that provided print materials on the same topics. All subjects were assessed at pretest and posttest through an online questionnaire containing multiple measures of health behavior and attitudes. The test period was 3 months. Questionnaire data were analyzed mainly by analysis of covariance and t tests. RESULTS:Retention rates were good for both groups-85% for the Web-based group and 87% for the print group. Subjects using the Web-based program performed significantly better than the print group on Attitudes Toward a Healthful Diet (F(1,415) = 7.104, P = .008) and Dietary Stage of Change (F(1,408) = 6.487, P = .01), but there were no significant group differences on the five other dietary measures. Both groups also showed improvement from pretest to posttest on most dietary measures, as indicated by significant t tests. Within the Web-based group, dosage analyses showed significant effects of the number of times the subject accessed the program on measures of Dietary Self-Efficacy (F(2,203) = 5.270, P = .003), Attitudes Toward a Healthful Diet (F(2,204) = 2.585, P = .045), and Dietary Stage of Change (F(2,200) = 4.627, P = .005). No significant differences were found between the two groups on measures of stress or physical activity, although t tests of pretest-posttest changes indicated that both groups improved on several of these measures. The Web-based group gave significantly higher ratings to the program materials than the print group on all health topics and in their overall evaluation (F(1,410) = 9.808, P = .002). CONCLUSIONS:The Web-based program was more effective than print materials in producing improvements in the areas of diet and nutrition but was not more effective in reducing stress or increasing physical activity. The higher ratings given to the Web-based program suggest that workers preferred it to the print materials. Both groups showed numerous pretest-posttest improvements in all health topics, although such improvements might be attributable in part to a Hawthorne effect. Results suggest that a multimedia Web-based program can be a promising means of delivering health promotion material to the workforce, particularly in the area of diet and nutrition.
    背景与目标:
  • 【乳腺癌患者首次复发后的多方面心理社会干预计划: 可行性研究。】 复制标题 收藏 收藏
    DOI:10.1002/pon.1101 复制DOI
    作者列表:Akechi T,Taniguchi K,Suzuki S,Okamura M,Minami H,Okuyama T,Furukawa TA,Uchitomi Y
    BACKGROUND & AIMS: :We developed a novel multifaceted psychosocial intervention program which involves screening for psychological distress and comprehensive support including individually tailored psychotherapy and pharmacotherapy provided by mental health professionals. The purpose of the present study was to investigate the feasibility of the intervention program and its preliminary usefulness for reducing clinical psychological distress experienced by patients with recurrent breast cancer. The subjects who participated in the 3 months intervention program completed psychiatric diagnostic interview and several self-reported measures regarding psychological distress, traumatic stress, and quality of life. The assessments were conducted before the intervention (T1), after the intervention (T2), and 3 months after the intervention (T3). A total of 50 patients participated in the study. The rates of participation in and adherence to the intervention program were 85 and 86%, respectively. While the proportion of psychiatric disorders at T2 (11.6%) was not significantly different from that at T1 (22.0%) (p = 0.15), the proportion of that at T3 (7.7%) had significantly decreased compared with that at T1 (p = 0.005). The novel intervention program is feasible, is a promising strategy for reducing clinically manifested psychological distress and further controlled studies are warranted.
    背景与目标: : 我们开发了一种新颖的多方面的社会心理干预计划,其中包括筛查心理困扰和全面支持,包括由精神卫生专业人员提供的个性化心理治疗和药物疗法。本研究的目的是研究干预计划的可行性及其对减少复发性乳腺癌患者遭受的临床心理困扰的初步作用。参加3个月干预计划的受试者完成了精神病学诊断访谈,并完成了一些有关心理困扰,创伤压力和生活质量的自我报告措施。评估在干预前 (T1),干预后 (T2) 和干预后3个月 (T3) 进行。共有50名患者参加了这项研究。参与和遵守干预计划的比率分别为85和86%。尽管T2 (11.6%) 的精神疾病比例与T1 (22.0%) 无显着差异 (p = 0.15),但与T1 (p = 0.005) 相比,T3 (7.7%) 的精神疾病比例显着降低)。新的干预计划是可行的,是减少临床表现的心理困扰的有前途的策略,需要进一步的对照研究。
  • 【直接客户护理期间临床讲师的教学活动: 一项定性调查。】 复制标题 收藏 收藏
    DOI:10.1111/j.1365-2648.1991.tb01534.x 复制DOI
    作者列表:Morgan SA
    BACKGROUND & AIMS: :The lack of substantial research in the area of clinical teaching would suggest that this 'heart' of the nursing student's professional education has long been neglected. Employing a qualitative descriptive methodology, this study explored the teaching activities that nine clinical instructors said they implemented during the direct client care period and the teaching activities that these nine clinical instructors said they would implement in response to a specific scenario of a clinical teaching event. The unstructured interviews revealed that clinical instructors: (a) noted role modelling the greatest number of times as a teaching activity but implemented it less frequently; (b) used verbalizations in the form of telling, asking, saying, discussing or talking as the primary teaching activity in the clinical area and in response to the specific scenario; (c) do not have opportunities to see other clinical instructors teaching in the clinical area; (d) have difficulty separating teaching activities and evaluation activities; (e) are eclectic in their use of learning theories; and (f) find articulating teaching activities that they implement during the direct client care period to be a complex task.
    背景与目标: : 在临床教学领域缺乏实质性的研究表明,长期以来一直忽略了护生专业教育的 “心脏”。本研究采用定性描述性方法,探讨了九名临床讲师表示他们在直接客户护理期间实施的教学活动,以及这九名临床讲师表示他们将针对临床教学事件的特定场景实施的教学活动。非结构化访谈显示,临床讲师 :( a) 注意到角色建模作为教学活动的次数最多,但实施频率较低; (b) 以讲述,询问,说,讨论或谈话作为临床领域的主要教学活动,并针对具体情况; (c) 没有机会看到临床领域的其他临床讲师教学; (d) 难以分离教学活动和评估活动; (e) 在学习理论的使用上不拘一格; (f) 发现他们在直接服务客户期间实施的明确教学活动是一项复杂的任务。
  • 【对低收入少数民族青少年病态肥胖的多学科治疗的长期评估: 拉拉比达儿童医院的FitMatters计划。】 复制标题 收藏 收藏
    DOI:10.1016/j.jadohealth.2006.02.007 复制DOI
    作者列表:Germann JN,Kirschenbaum DS,Rich BH,O'Koon JC
    BACKGROUND & AIMS: PURPOSE:Long-term evaluation of an empirically based program for the treatment of morbidly obese, low-income, minority adolescents. METHODS:In the first year, 150 participants received cognitive-behavior therapy, nutritional education, medical monitoring, and structured exercise training. Weights and heights were collected at follow-up. Successful and Less Successful groups were delineated based on change in body mass index z-scores. Medical record review provided weight and height data one year before treatment for a subset of participants (comparison group). Analyses of variance examined differences between groups. Discriminant function analyses examined predictors of success in the domains of socioeconomic status, individual factors and psychological functioning, family factors, and prior weight loss behaviors. Correlates of success were explored. RESULTS:Eighty-three adolescents participated in the follow-up, on average 23 months (SD = 3.8) after initial assessment. Nineteen (23%) participants achieved clinically meaningful weight change (-.70 z-scores or better). Discriminant function analyses, correlations, and direct comparisons showed that the Successful group, compared with the Less Successful group, on average, attended 50% more sessions over 84% more weeks, were heavier initially, had somewhat better critical weight control skills (e.g., self-monitoring) before and during the program, and were somewhat more psychologically and intellectually challenged before treatment. CONCLUSION:Although some of these very high risk adolescents made clinically significant progress, more intensive treatments, like long-term residential treatments and bariatric surgery, may produce even more favorable outcomes.
    背景与目标:
  • 【在日常活动中测量姿势和运动的新型活动监视器的验证。】 复制标题 收藏 收藏
    DOI:10.1136/bjsm.2006.030262 复制DOI
    作者列表:Grant PM,Ryan CG,Tigbe WW,Granat MH
    BACKGROUND & AIMS: BACKGROUND:Accurate measurement of physical activity patterns can be used to identify sedentary behaviour and may facilitate interventions aimed at reducing inactivity. OBJECTIVE:To evaluate the activPAL physical activity monitor as a measure of posture and motion in everyday activities using observational analysis as the criterion standard. METHODS:Wearing three activPAL monitors, 10 healthy participants performed a range of randomly assigned everyday tasks incorporating walking, standing and sitting. Each trial was captured on a digital camera and the recordings were synchronised with the activPAL. The time spent in different postures was visually classified and this was compared with the activPAL output. RESULTS:Intraclass correlation coefficients (ICC 2,1) for interdevice reliability ranged from 0.79 to 0.99. Using the Bland and Altman method, the mean percentage difference between the activPAL monitor and observation for total time spent sitting was 0.19% (limits of agreement -0.68% to 1.06%) and for total time spent upright was -0.27% (limits of agreement -1.38% to 0.84%). The mean difference for total time spent standing was 1.4% (limits of agreement -6.2% to 9.1%) and for total time spent walking was -2.0% (limits of agreement -16.1% to 12.1%). A second-by-second analysis between observer and monitor found an overall agreement of 95.9%. CONCLUSION:The activPAL activity monitor is a valid and reliable measure of posture and motion during everyday physical activities.
    背景与目标:
  • 【综合继续医学教育 (CME) 和质量改进 (QI) 计划对放射肿瘤学家 (RO) 临床实践的有效性。】 复制标题 收藏 收藏
    DOI:10.1016/j.ijrobp.2006.07.018 复制DOI
    作者列表:Leong CN,Shakespeare TP,Mukherjee RK,Back MF,Lee KM,Lu JJ,Wynne CJ,Lim K,Tang J,Zhang X
    BACKGROUND & AIMS: PURPOSE:There has been little radiation oncologist (RO)-specific research in continuing medical education (CME) or quality improvement (QI) program efficacy. Our aim was to evaluate a CME/QI program for changes in RO behavior, performance, and adherence to department protocols/studies over the first 12 months of the program. METHODS AND MATERIALS:The CME/QI program combined chart audit with feedback (C-AWF), simulation review AWF (SR-AWF), reminder checklists, and targeted CME tutorials. Between April 2003 and March 2004, management of 75 patients was evaluated by chart audit with feedback (C-AWF) and 178 patients via simulation review audit (SR-AWF) using a validated instrument. Scores were presented, and case management was discussed with individualized educational feedback. RO behavior and performance was compared over the first year of the program. RESULTS:Comparing the first and second 6 months, there was a significant improvement in mean behavior (12.7-13.6 of 14, p = 0.0005) and RO performance (7.6-7.9 of 8, p = 0.018) scores. Protocol/study adherence significantly improved from 90.3% to 96.6% (p = 0.005). A total of 50 actions were generated, including the identification of learning needs to direct CME tutorials, the systematic change of suboptimal RO practice, and the alteration of deficient management of 3% of patients audited during the program. CONCLUSION:An integrated CME/QI program combining C-AWF, SR-AWF, QI reminders, and targeted CME tutorials effectively improved targeted RO behavior and performance over a 12-month period. There was a corresponding increase in departmental protocol and study adherence.
    背景与目标:
  • 【Α-硫辛酸抑制糖尿病大鼠P2X受体活性和内脏对结直肠扩张的超敏反应。】 复制标题 收藏 收藏
    DOI:10.1038/s41598-017-04283-7 复制DOI
    作者列表:Hu J,Qin X,Song ZY,Yang PP,Feng Y,Sun Q,Xu GY,Zhang HH
    BACKGROUND & AIMS: :The present study was designed to investigate the roles of P2X3 receptors in dorsal root ganglion (DRG) neurons in colonic hypersensitivity and the effects of alpha-lipoic acid (ALA) on P2X3 receptor activity and colonic hypersensitivity of diabetic rats. Streptozotocin (STZ) was used to induce diabetic model. Abdominal withdrawal reflex (AWR) responding to colorectal distention (CRD) was recorded as colonic sensitivity. ATP-induced current density of colon-specific DRG (T13-L2 DRGs) neurons was measured with whole-cell patch clamp. The expression of P2X3Rs of T13-L2 DRGs was measured by western blot analysis. The results showed that AWR scores significantly increased after STZ injection. P2X3R expression and ATP current density of T13-L2 DRG neurons were enhanced in diabetic rats. Intraperitoneal injection with ALA once a day for 1 week remarkably reduced P2X3R expression and ATP current density in diabetic rats. Importantly, ALA treatment attenuated colonic hypersensitivity in diabetic rats. Our data suggest that STZ injection increases expression and function of P2X3 receptors of colon-specific DRG neurons, thus contributing to colonic hypersensitivity in diabetic rats. Administration of ALA attenuates diabetic colonic hypersensitivity, which is most likely mediated by suppressing expression and function of P2X3 receptors in DRGs of diabetic rats.
    背景与目标: 本研究旨在研究背根神经节 (DRG) 神经元中P2X3受体在结肠超敏反应中的作用以及 α-硫辛酸 (ALA) 对糖尿病大鼠P2X3受体活性和结肠超敏反应的影响。链脲佐菌素 (STZ) 用于诱导糖尿病模型。对结直肠扩张 (CRD) 反应的腹部撤药反射 (AWR) 被记录为结肠敏感性。用全细胞膜片钳测量ATP诱导的结肠特异性DRG (T13-L2 DRGs) 神经元的电流密度。通过蛋白质印迹分析测量T13-L2 DRGs中P2X3Rs的表达。结果显示,注射STZ后AWR评分明显升高。糖尿病大鼠T13-L2 DRG神经元P2X3R表达和ATP电流密度增强。每天一次腹腔注射ALA,持续1周,可显着降低糖尿病大鼠的P2X3R表达和ATP电流密度。重要的是,ALA治疗可减轻糖尿病大鼠的结肠超敏反应。我们的数据表明,STZ注射可增加结肠特异性DRG神经元的P2X3受体的表达和功能,从而导致糖尿病大鼠的结肠超敏反应。ALA的给药可减轻糖尿病结肠超敏反应,这很可能是通过抑制糖尿病大鼠DRGs中P2X3受体的表达和功能来介导的。
  • 【州和地方卫生部门自愿国家认证计划的最终建议: 指导委员会报告。】 复制标题 收藏 收藏
    DOI:10.1097/01.PHH.0000278026.49196.40 复制DOI
    作者列表:Bender K,Benjamin G,Carden J,Fallon M,Gorenflo G,Hardy GE Jr,Jarris PE,Libbey PM,Nolan PA
    BACKGROUND & AIMS: :A recently released report of the Exploring Accreditation Project affirmatively answered the questions regarding the desirability and feasibility of establishing a national voluntary public health accreditation program. The report's recommendations were made after 10 months of inquiry from public health experts, elected officials, the general public health workforce, academicians, and other interested parties, more than 650 public health professionals in all. Recommendations regarding how such a program might be implemented insofar as its governance, principles for standards development, financing and incentives, and evaluation were included. The report provides a blueprint for establishing a national voluntary public health accreditation program. This article describes key aspects of the Steering Committee recommendations, with limited linkage to implementation strategies where relevant, in the four areas in which the project was designed. Details are provided in the final reports of the Steering Committee (www.exploringaccreditation.org) and in other articles in this issue.
    背景与目标: : 最近发布的 “探索认证项目” 报告肯定地回答了有关建立国家自愿公共卫生认证计划的可取性和可行性的问题。该报告的建议是在公共卫生专家,民选官员,一般公共卫生工作人员,院士和其他有关方面,共有650多名公共卫生专业人员进行了10个月的调查后提出的。包括了关于如何实施此类计划的建议,包括其治理,标准制定原则,融资和激励措施以及评估。该报告提供了建立国家自愿公共卫生认证计划的蓝图。本文介绍了指导委员会建议的关键方面,在设计项目的四个领域中,与相关实施战略的联系有限。指导委员会的最终报告 (www.exploringaccreditation.org) 和本期的其他文章提供了详细信息。
  • 【线粒体: 氧化还原活动和细胞窘迫控制的枢纽。】 复制标题 收藏 收藏
    DOI:10.1007/s11010-007-9520-8 复制DOI
    作者列表:Kakkar P,Singh BK
    BACKGROUND & AIMS: :In their reductionist approach in unraveling phenomena inside the cell, scientists in recent times have focused attention to mitochondria. An organelle with peculiar evolutionary history and organization, it is turning out to be an important cell survival switch. Besides controlling bioenergetics of a cell it also has its own genetic machinery which codes 37 genes. It is a major source of generation of reactive oxygen species, acts as a safety device against toxic increases of cytosolic Ca2+ and its membrane permeability transition is a critical control point in cell death. Redox status of mitochondria is important in combating oxidative stress and maintaining membrane permeability. Importance of mitochondria in deciding the response of cell to multiplicity of physiological and genetic stresses, inter-organelle communication, and ultimate cell survival is constantly being unraveled and discussed in this review. Mitochondrial events involved in apoptosis and necrotic cell death, such as activation of Bcl-2 family proteins, formation of permeability transition pore, release of cytochrome c and apoptosis inducing factors, activation of caspase cascade, and ultimate cell death is the focus of attention not only for cell biologists, but also for toxicologists in unraveling stress responses. Mutations caused by ROS to mitochondrial DNA, its inability to repair it completely and creation of a vicious cycle of mutations along with role of Bcl-2 family genes and proteins has been implicated in many diseases where mitochondrial dysfunctions play a key role. New therapeutic approaches toward targeting low molecular weight compounds to mitochondria, including antioxidants is a step toward nipping the stress in the bud.
    背景与目标: : 在揭示细胞内现象的还原论方法中,科学家们最近将注意力集中在线粒体上。细胞器具有独特的进化史和组织,被证明是重要的细胞存活开关。除了控制细胞的生物能学外,它还具有自己的遗传机制,可编码37个基因。它是产生活性氧的主要来源,可作为防止胞质Ca2毒性增加的安全装置,其膜通透性转变是细胞死亡的关键控制点。线粒体的氧化还原状态对于对抗氧化应激和维持膜通透性很重要。线粒体在决定细胞对多种生理和遗传压力,细胞器间通讯以及最终细胞存活的反应中的重要性一直在本文中讨论和讨论。参与细胞凋亡和坏死细胞死亡的线粒体事件,如Bcl-2家族蛋白的激活、通透性转换孔的形成、细胞色素c和凋亡诱导因子的释放、半胱天冬酶级联的激活以及最终的细胞死亡等不仅是细胞生物学家关注的焦点,但也适用于毒理学家揭示应激反应。由ROS引起的线粒体DNA突变,其无法完全修复以及突变的恶性循环以及Bcl-2家族基因和蛋白质的作用已与许多疾病有关,其中线粒体功能障碍起着关键作用。将低分子量化合物 (包括抗氧化剂) 靶向线粒体的新治疗方法是将压力抑制在芽中的一步。
  • 【Plantagiolides I和J,来自Tacca plantaginea的两种新的withanolide葡萄糖苷,具有核因子-kappaB抑制和过氧化物酶体增殖物激活的受体反式激活活性。】 复制标题 收藏 收藏
    DOI:10.1248/cpb.c12-00550 复制DOI
    作者列表:Quang TH,Ngan NT,Minh CV,Kiem PV,Yen PH,Tai BH,Nhiem NX,Thao NP,Anh Hle T,Luyen BT,Yang SY,Kim YH
    BACKGROUND & AIMS: :A novel withanolide glucoside, plantagiolide I (1), a new withanolide glucoside, plantagiolide J (2), and six known compounds (3-8) were isolated from the whole plant of Tacca plantaginea. Their structures were determined by spectroscopic and chemical methods. Compound 3 significantly inhibited tumor necrosis factor alpha (TNFα)-induced nuclear factor-kappaB (NF-κB) transcriptional activity in HepG2 cells in a dose-dependent manner, with IC(50) values of 9.0 µM. Compounds 1-8 enhanced the transcriptional activity of peroxisome proliferator-activated receptors (PPARs) in a dose-dependent manner, with EC(50) values ranging from 1.6 to 49.7 µM. In addition, the transactivational effects of compounds 1-8 on three individual PPAR subtypes, including PPARα, β(δ), and γ were evaluated. Compounds 1-8 significantly activated the transcriptional activity of PPARβ(δ), with EC(50) values in a ranging from 4.1 to 29.6 µM. These results provide scientific support for the use of T. plantaginea and its components for the prevention and treatment of inflammatory and metabolic diseases.
    背景与目标: : 从Tacca plantaginea的整个植物中分离出一种新的withanolide葡萄糖苷,plantagiolide I (1),一种新的withanolide葡萄糖苷,plantagiolide J (2) 和六种已知化合物 (3-8)。它们的结构通过光谱和化学方法确定。化合物3以剂量依赖性方式显著抑制肿瘤坏死因子 α (tnf α) 诱导的HepG2细胞核因子 κ b (NF-κ b) 转录活性,IC(50) 值为9.0 µm µ m。化合物1-8以剂量依赖性方式增强过氧化物酶体增殖物激活受体 (ppar) 的转录活性,EC(50) 值范围为1.6至49.7 µm µ m。此外,还评估了化合物1-8对三种单独的PPAR亚型 (包括PPAR α,β(δ) 和 γ) 的反式激活作用。化合物1-8显著激活ppar β(δ) 的转录活性,EC(50) 值范围为4.1至29.6  µ m。这些结果为使用车前草及其成分预防和治疗炎症和代谢性疾病提供了科学支持。
  • 【尿尿利尿剂的研究。I.黄嘌呤氧乙酸和dihydrofuroxanthone-2-carboxylic的合成和活性。】 复制标题 收藏 收藏
    DOI:10.1248/cpb.38.1266 复制DOI
    作者列表:Sato H,Dan T,Onuma E,Tanaka H,Koga H
    BACKGROUND & AIMS: :A series of substituted xanthonyloxyacetic acids (5 and 6), 1,2-dihydrofuro[2,3-c]xanthone-2-carboxylic acids (7) and 2,3-dihydrofuro[3,2-b]xanthone-2-carboxylic acids (8) were synthesized and tested for diuretic and uricosuric activities in rats. Most of the xanthon-3-yloxyacetic acids (5) and 7 showed potent diuretic activities, while 8 had lower activities. Uricosuric activities were found in 5c, 5f, 5k, 5m, 5o, 5p, 5r, 7m, 7p and 8q.
    背景与目标: : 一系列取代的黄环氧乙酸 (5和6),1,2-二氢呋喃 [2,3-c]xanthone-2-carboxylic (7) 和2,3-二氢呋喃 [3,合成了2-b]xanthone-2-carboxylic酸 (8) 并测试了大鼠的利尿和尿尿活性。大多数xanthon-3-yloxyacetic酸 (5) 和7表现出强效的利尿活性,而8表现出较低的活性。在5c,5f,5k,5m,5o,5p中发现尿尿活性。5r、7m、7p和8q。
  • 【苄腺嘌呤对吸收的黑克子叶线粒体活性发展的影响。】 复制标题 收藏 收藏
    DOI:10.1016/S0176-1617(84)80093-0 复制DOI
    作者列表:Morohashi Y
    BACKGROUND & AIMS: :The development of mitochondria was followed in black gram cotyledons cultured on filter paper wetted with water or benzyladenine solution. Treatment with benzyladenine brought about an increase in activities of some mitochondrial enzymes and in respiratory activities of mitochondria. Cycloheximide did not inhibit the increase, although it almost completely inhibited the incorporation of (14)C-leucine into mitochondrial protein. It was inferred that the increase in mitochondrial activity by benzyladenine-treatment was not due to biogenesis of mitochondria but due to an acceleration of activation processes in pre-existing mitochondria. The respiratory control ratio of mitochondria from benzyladenine-treated cotyledons was lower than that of mitochondria from untreated ones. It was also suggested that benzyladenine brought about some qualitative changes in mitochondrial activities.
    背景与目标: : 在用水或苄基腺嘌呤溶液润湿的滤纸上培养的黑色革兰氏子叶中,跟踪线粒体的发育。用苄基腺嘌呤治疗可增加某些线粒体酶的活性和线粒体的呼吸活性。尽管环己酰亚胺几乎完全抑制了 (14)C-亮氨酸掺入线粒体蛋白中,但它并没有抑制这种增加。可以推断,苄基腺嘌呤处理引起的线粒体活性增加不是由于线粒体的生物发生,而是由于先前存在的线粒体中激活过程的加速。苄基腺嘌呤处理的子叶线粒体的呼吸控制率低于未处理的子叶线粒体的呼吸控制率。还建议苄基腺嘌呤在线粒体活性中引起一些质的变化。
  • 【非洲传统草药的促有丝分裂活性 (第二部分)。】 复制标题 收藏 收藏
    DOI:10.1016/S0944-7113(96)80078-X 复制DOI
    作者列表:Tachibana Y,Kato A,Nishiyama Y,Ikemi M,Ohoka K,Kawanishi K,Juma FD,Ngángá JN,Mathenge SG
    BACKGROUND & AIMS: :Mitogenic activities in African traditional herbal medicines were examined on human peripheral blood lymphocytes and mouse spleen cells using protein fractions obtained from their extracts by precipitation with ammonium sulfate. Target specificity for these mitogens was investigated by using isolated T cells and lymphocytes from athymic nude mice. Among 20 plants investigated, potent mitogenic activities for both human and mouse lymphocytes were found in 7 plants: Monanthotaxis sp. (Annonaceae), Uvaria lucida (Annonaceae), Maytenus buchananii (Celastraceae), Lonchocarpus bussei (Leguminosae), Phytolacca dodecandra (Phytolaccaceae), Phytolacca octandra (Phytolaccaceae), and Toddalia asiatica (Rutaceae). The U. lucida stem demonstrated the highest activity among all and induced mitogenesis both in human and mouse isolated T cells, but not in lymphocytes from athymic nude mice.
    背景与目标: : 使用通过硫酸铵沉淀从其提取物中获得的蛋白质级分,对人外周血淋巴细胞和小鼠脾细胞检查了非洲传统草药中的促有丝分裂活性。通过使用来自无胸腺裸鼠的分离的T细胞和淋巴细胞研究了这些有丝分裂原的靶特异性。在所调查的20种植物中,在7种植物中发现了人类和小鼠淋巴细胞的强效促有丝分裂活性: 单棘科 (Annonaceae),Uvaria lucida (Annonaceae),Maytenus buchananii (Celastraceae),Lonchocarpus bussei (豆科),Phytolacca dodecanandra (phtomacaceae),和Toddalia asiatica (芸香科)。U. lucida茎在人类和小鼠分离的T细胞中表现出最高的活性,并诱导了有丝分裂,但在无胸腺裸鼠的淋巴细胞中却没有。
  • 【从东方火腹蟾蜍 (Bombina orientalis) 的皮肤分泌物中发现了两种具有抗菌和抗癌活性的bombinin肽。】 复制标题 收藏 收藏
    DOI:10.1111/cbdd.13055 复制DOI
    作者列表:Zhou C,Wang Z,Peng X,Liu Y,Lin Y,Zhang Z,Qiu Y,Jin M,Wang R,Kong D
    BACKGROUND & AIMS: :Amphibian skin secretions are known to contain numerous peptides with a large array of biological activities. Bombinins are a group of amphibian-derived peptides with broad spectrum antimicrobial activities that have been only identified from the ancient toad species, Bombina. In this study, we described the identification and characterization of a novel bombinin precursor which encoded a bombinin-like peptide (BLP-7) and a novel bombinin H-type peptide (named as Bombinin H-BO) from the skin secretion of Oriental fire-bellied toad, Bombina orientalis. The primary structures of both mature peptides were determined by combinations of molecular cloning of peptide precursor-encoding cDNAs and mass spectrometry techniques. Secondary structure prediction revealed that both peptides had cationic amphipathic α-helical structural features. The synthetic replicate of BLP-7 displayed more potent antimicrobial activity than Bombinin H-BO against Gram-positive and Gram-negative bacteria and yeast. Also, in vitro antitumour assay showed that both peptides possessed obvious antiproliferative activity on three human hepatoma cells (Hep G2/SK-HEP-1/Huh7) at the non-toxic doses. These results indicate the peptide family of bombinins could be a potential source of drug candidates for anti-infection and anticancer therapy.
    背景与目标: 已知两栖动物皮肤分泌物含有大量具有大量生物活性的肽。Bombinins是一组具有广谱抗菌活性的两栖动物衍生肽,仅从古代蟾蜍物种Bombina中鉴定出。在这项研究中,我们描述了一种新的bombinin前体的鉴定和表征,该前体编码了一种bombinin样肽 (BLP-7) 和一种新的bombinin H型肽 (称为Bombinin H-BO),来自东方火腹蟾蜍的皮肤分泌物,东方Bombina。通过编码肽前体的cdna的分子克隆和质谱技术的组合确定了两种成熟肽的一级结构。二级结构预测表明,两种肽均具有阳离子两亲性 α-螺旋结构特征。BLP-7的合成复制比Bombinin H-BO对革兰氏阳性和革兰氏阴性细菌和酵母表现出更有效的抗菌活性。此外,体外抗肿瘤测定表明,两种肽在无毒剂量下对三种人肝癌细胞 (Hep G2/SK-HEP-1/Huh7) 具有明显的抗增殖活性。这些结果表明,bombinins的肽家族可能是抗感染和抗癌治疗的候选药物的潜在来源。

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