环烯醚萜类化合物防治骨质疏松症作用机制的研究进展

骨质疏松已是全球健康问题，因此寻找安全、有效、不良反应少的抗骨质疏松症药物是社会所关注的问题。环烯醚萜类化合物在植物界分布较广，具有多种药理活性。环烯醚萜类化合物可通过多种途径促进成骨功能、抑制破骨功能，发挥抗骨质疏松作用。归纳了环烯醚萜类化合物抗骨质疏松症的作用机制，为开发新型抗骨疏松症药物提供参考。     

巴戟天属植物中环烯醚萜类化合物研究进展

摘要：环烯醚萜类化合物广泛存在于巴戟天属植物中,具有抗抑郁、镇痛抗炎、骨保护、抗衰老、抗肿瘤、保护心血管和抗菌等作用。本文总结了巴戟天属植物中环烯醚萜类化合物的种类、结构、药理活性及含量检测方法,对分析巴戟天属植物中环烯醚萜类成分的物质基础和作用机制具有重要的意义。     

环烯醚萜类化合物的结构和生物学活性研究进展

目的：详细综述了新发现的、具有较新结构特点的环烯醚萜类化合物及生物学活性研究,为环烯醚萜类化合物的结构活性研究提供新的思路。方法：查阅总结近30年国内外发表的关于环烯醚萜新化合物的文献,总结结构和活性的研究概况。结果：环烯醚萜的主要结构类型环烯醚萜苷类、裂环环烯醚萜和环烯醚萜酯。环烯醚萜类化合物主要临床生物活性具有神经系统的保护作用、抗肿瘤作用和保肝作用等。结论：环烯醚萜类化合物的分布广泛,具有较大的药用价值。通过对环烯醚萜类化合物结构和生物学活性的总结和分析,探讨环烯醚萜化合物结构与活性之间的关系,为药物开发和利用提供文献和数据支持。     

环烯醚萜类化合物近年研究进展

目的 介绍环烯醚萜类化合物研究概况和近年研究进展。方法 以近年来国内外发表的文献为依据,从结构分类、半合成及生物活性方面综述环烯醚萜类化合物近年研究进展。结果 环烯醚萜类化合物具有多种生物活性。结论 环烯醚萜是一类很有研究价值的化合物。     

蜘蛛香环烯醚萜类成分的研究进展

蜘蛛香环烯醚萜类化合物是一类具有广泛生物活性的天然化合物,因其药用价值显著而备受重视。文中综述了国内外有关蜘蛛香环烯醚萜类化合物的研究,介绍了蜘蛛香环烯醚萜类化合物的理化性质、提取分离研究和含量测定方法,同时对蜘蛛香环烯醚萜类化合物几种明确的药理作用及作用机制做了较详细介绍,以期为该类化合物的进一步研究开发及应用提供参考。     

筋骨草属植物化学成分与药理活性

综述了筋骨草属植物中二萜类、环烯醚萜类、植物蜕皮甾酮类、黄酮类等化学成分的结构及其药理活性。     

忍冬属植物化学成分及药理活性

综述了对忍冬属植物中的黄酮类、三萜类和环烯醚萜类等化学成分及药理活性方面的研究进展。     

环烯醚萜类化合物的研究进展

以近5 a来国内外发表的文献为依据,从结构分类和生物活性两方面综述环烯醚萜类化合物的研究进展.环烯醚萜类化合物结构繁多,具有多种生物活性. 环烯醚萜化合物具有很高的研究价值.     

地黄中环烯醚萜类成分及其氢谱碳谱规律

我们对现有的600多个环烯醚萜类化合物进行比较,认为依据母核的不同,将环烯醚萜类化合物分为5大类便 加合理,地黄中已分得的环烯醚萜类化合物共32个,均属母核为9个碳,且C－10接在C－8上的第Ⅲ类骨架的化合物,本文试图结合已从其它植物中分得的第Ⅲ类骨架的环烯醚萜类化合物的^1H-NMR和^13C-NMR数据,对地黄中所分得的环烯萜类化合物的^1H-NMR和^13C-NMR规律作一总结。     

白毛夏枯草及其复方次生代谢产物含量与抑菌活性相关性研究

目的 比较白毛夏枯草饮片及其2种复方汤剂的次生代谢产物含量与抑菌活性的相关性,为合理配伍提供依据。方法 采用牛津杯琼脂扩散法测定抑菌圈大小,利用分光光度法测定次生代谢产物(总黄酮、总皂苷、环烯醚萜类和总生物碱)含量,并进行抑菌活性相关性和通径分析,确定目标化合物。结果 总黄酮、总皂苷和环烯醚萜类含量：复方1>复方2>单方,总生物碱含量：复方2>单方≈复方1。2种复方抑菌强度基本相同且显著高于单方,4种次生代谢产物对金黄色葡萄球菌的抑菌活性均起正相关作用,总环烯醚萜直接通径系数最大。结论 白毛夏枯草复方次生代谢产物含量和抑菌活性均高于单方,影响其抑菌活性的成分主要是环烯醚萜类与皂苷类。     

Quantitative in vivo and in vitro sex differences in artemisinin metabolism in rat

1. The pharmacokinetics of the antimalarial compound artemisinin were compared in the male and female Sprague-Dawley rat after single dose i.v. (20 mg.kg) or i.p. (50 mg.kg) administration of an emulsion formulation. 2. Plasma clearance of artemisinin was 12.0 (95% confidence interval: 10.4, 13.0) l.h. kg in the male rat and 10.6 (95% CI: 7.5, 15.0) l.h. kg in the female rat suggesting high hepatic extraction in combination with erythrocyte uptake or clearance. Artemisinin half-life was 0.5 h after both routes of administration in both sexes. Values for plasma clearance and half-lives did not statistically differ between the sexes. 3. After i.p. administration artemisinin AUCs were 2-fold higher in the female compared with male rat (p 0.001). Artemisinin disappearance was 3.9-fold greater in microsomes from male compared with female livers and it was inhibited in male microsomes by goat or rabbit serum containing antibodies against CYP2C11 and CYP3A2 but not CYP2B1 or CYP2E1. 4. The unbound fraction of artemisinin in plasma was lower (p 0.001) in plasma obtained from the male (8.8 2.0%) compared with the female rat (11.7 2.2%). 5. The possibility of a marked sex difference, dependent on the route of administration, has to be taken into account in the design and interpretation of toxicological studies of artemisinin in this species.     

休克时血中氧自由基的变化

本实验测定10名休克患者血浆和红细胞的丙二醛(MDA)、血浆总抗的氧化活性(AOA)的含量。结果表明:休克病人红细胞膜和血浆 MDA 含量(4.298±0.722;5.348±0.834)与对照组(3.235±0.682;4.356±1.081)比较明显增高(P<0.05);血浆 AOA(39.65±7.858)与对照组(48.21±10.81)比较明显降低(P<0.01)。提示:休克时,患者机体内自由基反应增强是引起组织细胞损伤的原因之一。     

Quantitative in vivo and in vitro sex differences in artemisinin metabolism in rat

1. The pharmacokinetics of the antimalarial compound artemisinin were compared in the male and female Sprague-Dawley rat after single dose i.v. (20 mg x kg(-1)) or i.p. (50 mg x kg(-1)) administration of an emulsion formulation. 2. Plasma clearance of artemisinin was 12.0 (95% confidence interval: 10.4, 13.0) 1 x h(-1) x kg(-1) in the male rat and 10.6 (95% CI: 7.5, 15.0) 1 x h(-1) x kg(-1) in the female rat suggesting high hepatic extraction in combination with erythrocyte uptake or clearance. Artemisinin half-life was approximately 0.5 h after both routes of administration in both sexes. Values for plasma clearance and half-lives did not statistically differ between the sexes. 3. After i.p. administration artemisinin AUCs were 2-fold higher in the female compared with male rat (p < 0.001). Artemisinin disappearance was 3.9-fold greater in microsomes from male compared with female livers and it was inhibited in male microsomes by goat or rabbit serum containing antibodies against CYP2C11 and CYP3A2 but not CYP2B1 or CYP2E1. 4. The unbound fraction of artemisinin in plasma was lower (p < 0.001) in plasma obtained from the male (8.8 +/- 2.0%) compared with the female rat (11.7 +/- 2.2%). 5. The possibility of a marked sex difference, dependent on the route of administration, has to be taken into account in the design and interpretation of toxicological studies of artemisinin in this species.     

Interindividual variability in metabolic activation in humans in vivo

In assessing interindividual variability in metabolic activation, the toxic metabolite is often too unstable for conventional analysis. Possible alternatives include a stable product of the reactive metabolite e.g. cysteinyl derivatives of N-acetyl-4-benzoquinoneimine, the toxic metabolite of paracetamol, adducts with DNA or protein, and indirect measurement of the activity of the enzyme(s) producing the active metabolite. An example of the last approach is the use of furafylline, a highly specific inhibitor of human CYP1A2, to determine the extent of the metabolic activation of the cooked food mutagens PhIP and MeIQx. The extent of inhibition, determined from levels of unchanged amine in urine, is an indirect measure of the activity of the activation pathway. Further refinement of this approach, allied to improved measures of the biological process of interest should prove of value in evaluating interindividual variability and its role in the risk assessment process.     

Theophylline kinetics in peripheral tissues in vivo in humans

Several biochemical and cellular effects have been described for methylxanthines under in vitro conditions. However, it is unknown, whether threshold concentrations required to exert these effects are attained in target tissues in vivo. We therefore employed the microdialysis technique for measuring theophylline concentrations in peripheral tissues under in vivo conditions.Following in vitro and in vivo calibration, microdialysis probes were inserted into the medial vastus muscle and into the periumbilical subcutaneous adipose layer of healthy volunteers. Following single oral dose administration of 300 mg or i.v. infusion of 240 mg theophylline, in vivo time courses of theophylline concentrations were monitored in tissues and plasma. Major pharmacokinetic parameters (c_max, t_max, AUC) were calculated for plasma and tissue time courses. The mean AUC_tissue /AUC_plasma-ratio was 0.56 (p.o.) and 0.55 (i.v.) for muscle and 0.55 (p.o.) and 0.72 (i.v.) for subcutaneous adipose tissue.We conclude that microdialysis provides important information on the distribution and the tissue pharmacokinetics of theophylline.Abbreviations FPIA Fluorescence polarisation immuno assay - AUC Area under the curve - t_max Time to peak concentration - c_max Peak concentration     

Trichinellosis in immigrants in Switzerland

We describe a case of trichinellosis diagnosed at the Division of Infectious Diseases, Hospital of Lugano, in January 2009. This case was associated with a cluster of cases and was traced to the consumption of contaminated meat after a wild boar hunt in Bosnia.