4-甲氧羰基芬太尼的4-N-丙酰基结构类似物的合成与镇痛活性

本文报道了4-甲氧羰基芬太尼4-N-丙酰基结构改变衍生物的合成及其镇痛活性。试验结果表明,该类衍生物均具有典型吗啡样作用的性质。多数化合物具有很强的镇痛活性。其中1379,1385和1387的镇痛活性强于先导物4-甲氧羰基芬太尼。     

Different Effects of Estrogen and Progesterone on K+ Currents Expressed in Xenopus Oocytes

Estrogen has received considerable attention recently as a potential therapeutic agent in vascular pathophysiological states such as stroke. The mechanisms by which estrogen influences cerebral arteries are incompletely understood. The present study was to examine the effect of ovariectomy and chronic estrogen or tamoxifen treatment on vascular reactivity in rat posterior communicating cerebral arteries with intact endothelium. Changes in vascular tension were measured by microvessel myograph. Ovariectomy significantly enhanced the constricting responses to endothelin I, but not to phenylephrine. Chronic treatment with estrogen or tamoxifen partially reversed or abolished the effect of ovariectomy. The contraction induced by high K⁺ solution was also enhanced in the ovariectomized rats and this enhancement was abolished by estrogen or tamoxifen treatment. Ovariectomy potentiated the relaxant response to nicardipine but not NS 1619. Estrogen but not tamoxifen reversed the effect of ovariectomy. The present results indicate that chronic tamoxifen may not act as an antagonist of estrogen, instead, chronic treatment with estrogen and tamoxifen has similar effect in inhibiting the increased vascular tension induced by ovariectomy. This study suggests the influence of physiological level of estrogen on vascular contractility. It is at present unknown what may have caused increased relaxant effect of nicardipine, a L-type Ca²⁺ channel blocker. More experiments are needed to show the role of endothelium in the altered vascular contractility in the ovariectomized and estrogen-treated rats. (supported by UPGC Direct Grant).     

Multi-quadrant biopsy technique improves diagnostic ability in large heterogeneous renal masses. Abel EJ,Heckman JE,Hinshaw L,Best S,Lubner M,Jarrard DF,Downs TM,Nakada SY,Lee FT Jr,Huang W,Ziemlewicz T.J Urol. 2015 Oct;194(4):886-91. [Epub 2015 Mar 30]. doi: 10.1016/j.juro.2015.03.106.

Purpose

Percutaneous biopsy obtained from a single location is prone to sampling error in large heterogeneous renal masses, leading to nondiagnostic results or failure to detect poor prognostic features. We evaluated the accuracy of percutaneous biopsy for large renal masses using a modified multi-quadrant technique vs. a standard biopsy technique.

Are peripheral and neuraxial blocks with ultrasound guidance more effective and safe in children?

Background and aims:  The efficacy and safety of ultrasound guided (USG) pediatric peripheral nerve and neuraxial blocks in children have not been evaluated. In this review, we have looked at the success rate, efficacy and complications with USG peripheral nerve blocks and compared with nerve stimulation or anatomical landmark based techniques in children.
Methods:  All suitable studies in MEDLINE, EMBASE Drugs and Cochrane Evidence Based Medicine Reviews: Cochrane Database of Systemic Reviews databases were identified. In addition, citation review and hand search of recent pediatric anesthesia and surgical journals were done. All three authors read all selected articles independently and a consensus was achieved. All randomized controlled trials (RCTs) comparing USG peripheral and neuraxial blocks with other techniques in children were included.
Results:  Ultrasound guidance has been demonstrated to improve block characteristics in children including shorter block performance time, higher success rates, shorter onset time, longer block duration, less volume of local anesthetic agents and visibility of neuraxial structures.
Conclusion:  Clinical studies in children suggest that US guidance has some advantages over more traditional nerve stimulation–based techniques for regional block. However, the advantage of US guidance on safety over traditional has not been adequately demonstrated in children except ilio-inguinal blocks.     

<Emphasis Type="Italic">Streptobacillus moniliformis</Emphasis> septic arthritis: a clinical entity distinct from rat-bite fever?

Background  

Streptobacillus moniliformis is a zoonotic agent associated with rodent contacts. Although it is more commonly reported to cause rat-bite fever with reactive arthritides, it can also lead to pyogenic infection of the joints.     

Risk factors in the occurrence of molar–incisor hypomineralization amongst a group of Iraqi children

International Journal of Paediatric Dentistry 2013; 23: 197–206 Background. Despite the worldwide increasing interest in the prevalence studies of molar–incisor hypomineralization (MIH), there is still insufficient evidence to verify the aetiological factors of this condition. Aims. To investigate risk factors involved in the development of MIH in a group of school‐aged Iraqi children. Design. Seven‐ to nine‐year‐old school children (823 of 1000 eligible, response rate of 82.3%) had their first permanent molars and incisors evaluated using the European Academy of Paediatric Dentistry evaluation criteria for MIH. Mothers completed a medical history questionnaire‐based interview performed in the schools by a trained examiner. Results. For children with MIH, 6% reported no relevant medical history; the remaining 94% reported various medical conditions putatively associated with MIH compared with 70% for the non‐affected group. Post‐natal medical conditions (33.3%) were most frequently reported. When data were split into the possible risk effect groups, maternal psychological stress (OR, 3.24), frequent exposure to ultrasonic scans during the last gestational trimester (OR, 2.51) and birth order as a fourth sibling or later (OR, 3.17 and 5.73, respectively) were previously unreported significant risk factors and postulated as contributing to, or causing the defect. Conclusions. Children with MIH had experienced a greater number of medical conditions than their unaffected peers with no single health event identified as a risk factor.     

睡眠剥夺对力竭运动大鼠胸腺谷胱甘肽、丙二醛、超氧化物歧化酶的影响

目的:观察不同睡眠剥夺时间后力竭运动对大鼠胸腺谷胱甘肽、丙二醛含量和超氧化物歧化酶活性的变化,探讨睡眠剥夺对大鼠抗氧化能力的影响。方法:实验于2006-04/05在湖南师范大学体育学院运动生物化学实验室完成。实验分组:选择10周龄健康雄性SD大鼠30只,按随机数字表法分为5组,每组6只:睡眠非运动组,睡眠 力竭运动组和睡眠剥夺24,48,72h 力竭运动组。实验方法:①采用轻柔刺激法制备大鼠睡眠剥夺模型。②睡眠非运动组和睡眠 力竭运动组不进行睡眠剥夺。③睡眠 力竭运动组和睡眠剥夺各组大鼠运动方案:跑台坡度为10°,速度为19.3m/min(相当于76%VO2max),所有大鼠运动至力竭(运动末期,大鼠先后滞留跑道后1/3处达3次以上,各种刺激驱赶均无效,停跑后体征表现为呼吸急促,神情倦怠,腹卧位,对刺激反应迟钝,捕捉时,逃避反应较运动前减弱)。实验评估:①大鼠一般状态。②力竭时间。③大鼠力竭后麻醉处死,测定胸腺谷胱甘肽、丙二醛含量和超氧化物歧化酶活性。结果:纳入大鼠30只,均进入结果分析。①大鼠一般状态:睡眠 力竭运动组大鼠表现为形态正常,活泼好动,皮毛光亮,眼睛有神;睡眠剥夺48,h 力竭运动组大鼠均出现神态倦怠,眼神黯淡,四肢亦有不同程度的红肿;睡眠剥夺24h 力竭运动组大72鼠介于以上两者之间。②睡眠 力竭运动组和睡眠剥夺24,7248,h组大鼠的力竭时间分别为(232.36±37.67),(269.19±38.61),(162.42±35.70),(141.07±28.56)。③谷胱甘肽含量、超氧化物歧化酶活性:睡眠 力竭运动组谷胱甘肽含量和超氧min化物歧化酶活性均低于睡眠非运动组[分别为(25.54±0.79),(27.09±1.31)mg/g;(±0.21),(±0.10)mkat/g],差异有显4.594.88著性意义(P<0.05);睡眠剥夺24h 力竭运动组谷胱甘肽含量和超氧化物歧化酶活性均高于睡眠非运动组[分别为(28.60±0.96),(27.09±1.31)mg/g;(±0.10),(±0.10)5.234.88mkat/g],差异有显著性意义(P<0.05),睡眠剥夺48,h 力竭运动组P72均低于睡眠非运动组[分别为(23.74±1.19),(22.43±0.52),(27.09±1.31)mg/g;(±0.14),(±0.18),(±0.10)mkat/g],4.523.354.88差异均有非常显著性意义(P<0.01);睡眠剥夺各组与睡眠 力竭运动组间谷胱甘肽含量和超氧化物歧化酶活性差异均有非常P显著性意义(P<0.01);睡眠剥夺各组间比较差异有显著性意义(P<0.05)。④丙二醛浓度:睡眠 力竭运动组丙二醛浓度高于P睡眠非运动组[分别为(±0.27),(±0.24)μmol/L],差异有非常显著性意义(P<0.01);睡眠剥夺各组与睡眠非运动组之间6.565.35P差异均有非常显著性意义(P<0.01);睡眠剥夺24,48,72h 力竭运动组丙二醛含量均高于睡眠 力竭运动组[分别为(±0.12),(±P7.398.850.72),(10.89±0.82),(±0.27)μmol/L],差异有显著性意义(P<0.05;P<0.01);睡眠剥夺各组间比较,睡眠剥夺48h与睡眠剥夺24h差6.56异无显著性意义(P>0.05),睡眠剥夺72h与睡眠剥夺24h、睡眠剥夺72h与睡眠剥夺48h间比较差异有非常显著性意义(P<0.01)。结论:①睡眠剥夺24h可引起大鼠胸腺氧化应激,使氧自由基能力有所增强。②睡眠剥夺48,72h力竭运动后氧自由基能力降低。     

Nuts and Cardiovascular Disease Prevention

Purpose of Review

We review recent epidemiological and clinical studies investigating the consumption of tree nuts and peanuts and cardiovascular disease (CVD) mortality as well as CVD risk factors.

Recent Findings

A greater consumption of tree nuts and peanuts is associated with a reduced risk of CVD mortality, as well as lower CVD events. Furthermore, risk factors associated with the development of CVD such as dyslipidemia, impaired vascular function, and hypertension are improved with regular tree nut and peanut consumption through a range of mechanism associated with their nutrient-rich profiles. There is weak inconsistent evidence for an effect of nut consumption on inflammation. There is emerging evidence that consuming tree nuts reduces the incidence of non-alcoholic fatty liver disease (NAFLD) and promotes diversity of gut microbiota, which in turn may improve CVD outcomes.

Summary

Evidence for CVD prevention is strong for some varieties of tree nuts, particularly walnuts, and length of supplementation and dose are important factors for consideration with recommendations.