毛鸡骨草的研究进展

毛鸡骨草是一种常用民间中药,用于治疗多种疾病.本文从化学成分、药理活性、质量分析等方面对毛鸡骨草的研究进行综述,为其进一步开发提供参考.     

过岗龙化学成分、药理活性及质量控制研究进展

摘要：过岗龙为我国传统中药,其主要化学成分为三萜类、黄酮类、酚酸类、甾醇类化合物等,具有抗炎、镇痛、抗菌、抗氧化、抗补体等药理活性。本文综述了过岗龙的化学成分、药理活性及质量控制的研究现状与进展,为过岗龙的进一步开发与利用提供参考依据。     

天精草的化学成分及药理研究进展

天精草为一味重要的中药,含有黄酮类化合物、生物碱、多糖、多种氨基酸、维生素以及多种微量元素等活性化学成分。现代药理研究表明其具有降血糖、降血脂、抗氧化、抗疲劳、耐低温、抗肿瘤等作用。通过查阅大量文献,综述了夭精草的化学成分及药理活性研究概况,为进一步研究天精草提供科学依据。     

杜鹃花属植物的化学成分及药理研究进展

目的:对中药杜鹃花属植物的化学成分和药理活性作用进行综述.方法:查阅近30年的相关文献.结果:杜鹃属植物主要合有黄酮类、二萜类等有效成分.药理研究证明其在祛痰、止咳平喘、心血管系统、神经系统、抗炎镇痛、免疫、杀虫等方面具有药理活性.结论:杜鹃属植物在我国分布较广,对其进行进一步的化学和药理学研究具有重要的意义.     

苍耳子的主要化学成分及药理活性研究进展

目的:总结、归纳苍耳子的主要化学成分和药理活性研究进展,为其进一步研究提供参考。方法:以"苍耳子""化学成分""药理活性""倍半萜内酯""Xanthium""Xanthii fructus"等为关键词,组合查询2006年1月-2015年5月Pub Med、Science Direct、中国知网、维普、万方等数据库中有关苍耳子主要化学成分及药理活性的研究文献,并对其进行综述。结果与结论:共查阅到相关文献106篇,其中有效文献38篇。经整理,苍耳子中所含化学成分主要有酚酸类、水溶性苷类、倍半萜内酯类以及挥发油、脂肪酸、噻嗪二酮和生物碱等;其药理作用广泛,具有抗肿瘤、抑菌、抗炎镇痛、降血糖等作用。加强对其化学成分和药理活性研究,有利于更好地开发、利用这一传统中药。     

桃仁化学成分与药理活性研究进展

摘 要：桃仁又名桃核仁,含有多种营养成分和生物活性物质,既是益智食品,也是传统的活血化瘀中药,并且临床疗效显著。目前对桃仁的化学成分和药理活性研究不够深入,已经分得脂肪酸、蛋白质、甾醇及其糖苷类、黄酮类、酚酸类等化合物,证明其具有抗凝血、抗血栓、预防肝纤维化和增强免疫力等药理作用。综述了近年来对桃仁的化学成分与药理活性研究进展,为进一步研究和临床应用提供依据。     

桔梗科中药特性及化学成分和药理活性的研究进展

桔梗科中药在我国分布广泛,临床普遍应用。通过对桔梗科中药的文献研究,从四气五味、归经、化学成分、药理活性等方面的研究进展进行综述,以期在系统研究中药方面有所启发,为寻找新药源及有效药物的代用品等方面奠定基础。本文就桔梗科中药特性、化学成分、药理活性做一综述。     

枸杞子的化学成分和药理研究概况

枸杞子为一传统滋补中药,经含有枸杞多糖（ＬＢＰ）、氨基酸、微量元素、维生素等多种化学成分,近年来在免疫、抗衰老、抗肿瘤等方面表现出广阔的应用前景。对枸杞子的化学成分及其药理研究方面作一概述。     

山茱萸的文献研究综述

综述了近十几年来中药山茱萸在炮制、化学成分、药理活性和现代临床研究等方面的研究进展,并对山茱萸的应用前景进行了展望,为山茱萸的进一步开发提供参考。     

龙葵的化学成分及抗肿瘤药理活性研究进展

目的:综述中药龙葵的化学成分和抗肿瘤药理活性,为龙葵抗肿瘤药物的进一步开发利用提供理论参考。方法:以"龙葵""化学成分""抗肿瘤""Nightshade""Chemical composition""Anti tumor activity"等为关键词,检索2004-2014年中国知网、万方、Pub Med数据库中的相关文献,对龙葵化学成分和抗肿瘤药理活性进行归纳和总结。结果:根据文献来源筛选及剔除重复文献后共检索到相关文献50余条,其中有效文献38条。研究显示,已从龙葵中分离得到约87个化学成分,大多为甾体类(甾体皂苷和甾体生物碱),也含有少量的有机酸、木脂素等成分;龙葵具有抗肝癌、宫颈癌、结肠癌、乳腺癌等药理活性,其药效物质主要为生物碱类、皂苷类及糖蛋白等。结论:龙葵有多种抗肿瘤活性,具有较大开发价值。建议对其水溶性成分进行深入研究,为开发抗肿瘤新药提供理论依据。     

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.     

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.     

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     

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。     

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.     

Changes in angiopoietin expression in glomeruli involved in glomerulosclerosis in rats with daunorubicin-induced nephrosis

AIM: To study the potential pathological role of endogenous angiopoietins in daunorubicin-induced progressive glomerulosclerosis in rats. METHODS: Seventy male Wistar rats were allocated randomly into a daunorubicin group (DRB; n=40) or a control group (n=30). The rats in the DRB group were injected with DRB (15 mg/kg), in their tails. Subsequently, at intervals of 1, 2, 4, 6, 8, and 12 weeks, 5 male Wistar rats in each group were chosen randomly for 24 h urinary protein quantitative measurements (24 h UPQM), and determination of plasma tumor necrosis factor alpha (TNF-alpha), angiopoietin-1 (Ang1), and angiopoietin-2 (Ang2) levels. Kidney sections were examined by electron microscopy, Periodic Acid Schiff (PAS) staining, immunohistochemical staining and in situ hybridization histochemistry. RESULTS: As glomerulosclerosis progressed in the DRB group, expression of Ang1 mRNA and protein in glomeruli decreased and expression of TNF-alpha protein, Ang2 mRNA and protein in glomeruli increased. Expression of Ang1 mRNA and protein in glomeruli were negatively correlated with 24 h UPQM, Fn protein expression, and mean area of extracellular matrix (MAECM). In comparison, expression of Ang2 mRNA and protein in glomeruli were positively correlated with 24 h UPQM, Fn protein expression and MAECM; furthermore, there was a positive correlation between plasma Ang2 and 24 h UPQM. Plasma TNF-alpha and expression of TNF-alpha in glomeruli were positively correlated with expression of Ang2 mRNA and protein in glomeruli. There was a negative correlation between Ang1 protein expression and Ang2 protein expression in glomeruli. CONCLUSION: During DRB-induced glomerulosclerosis, podocyte injury led to a shift in the balance of Ang1 and Ang2 in glomeruli. Increased TNF-alpha in plasma and glomeruli may upregulate Ang2 expression in glomeruli. Elevated Ang2 in both plasma and glomeruli may mediate protein permeability through the glomerular filtration barrier. Moreover, local expression of Ang2 may facilitate the progress of glomerulosclerosis by upregulating a component expression of extracellular matrix.     

Hyperkalaemia in patients in hospital

A survey of all laboratory blood specimens with a plasma potassium concentration greater than or equal to 5.5 mmol/L was conducted over a three month period. Of 331 specimens with hyperkalaemia, 71 were excluded because the specimens was haemolysed, old or contaminated. The laboratory served a population of 348,561 and during this time measured the plasma potassium on 25,016 occasions. Sixty-six outpatients and 20 neonates were not evaluated. The survey was undertaken on 86 of 102 inpatients (46 males), 48 of whom were over 66 years of age. Fifty-seven patients were admitted under a medical service and 29 under a surgical service. Fifty-nine had a single episode of hyperkalaemia. Thirty-two underwent a surgical procedure. The commonest contributing factor was impaired renal function which was present in 71 (83%) patients. Although a definitive causative role for drugs could be identified in only five patients, in 52 (60%) patients drugs were a contributing factor (potassium supplements 24, ACE inhibitors 16, nonsteroidal antiinflammatory drugs 12). Thirty-five of the 86 (41%) patients died during their hospital admission. Nineteen of the 35 deaths occurred within three days of the hyperkalaemia being recorded. A normal plasma potassium was eventually documented in 50 of the 86 patients. Of the remaining 36 patients, 25 (69%) subsequently died. In general the treatment of patients with hyperkalaemia focused on identifying and treating the underlying cause. Hyperkalaemia must always be considered seriously and regard given to the overall clinical status of the patient, with particular attention to drug therapy, renal and cardiac function, acid base status and the possibility of sepsis.