盐生肉苁蓉栽培品中苯乙醇苷类的指纹图谱研究

  目的 为规范化种植盐生肉苁蓉药材的质量研究提供基础研究资料。 方法 选择 RP-HPLC 建立盐生肉苁蓉补肾助阳功能特征成分的指纹图谱，并进行栽培品与野生品、不同生长期、不同药用部位指纹图谱的比较研究，采用计算机辅助相似度评价软件分析了相似度。 结果 种植基地药材的指纹图谱具有较高的相似度，其化学组成相似，相对比例也基本稳定。不同生长期和不同部位药材的指纹图谱也具有较好的一致性，但特征峰的含量存在明显差异。 结论 利用 RP-HPLC 指纹图谱可以较为全面地反映盐生肉苁蓉补肾助阳功能整体特征成分的内在质量，方法重现性好。     

大粒车前子中苯乙醇苷类化合物对树突状细胞的调控研究

目的:探讨大粒车前子中苯乙醇苷类化合物对小鼠骨髓来源树突状细胞(DCs)功能调节的影响,为进一步阐明大粒车前子的免疫调节活性提供依据.方法:采用细胞因子诱导法,从Balb/cj小鼠骨髓细胞贴壁分离获得单核细胞,加入含10%胎牛血清、10μg·L~(-1)重组小鼠粒细胞巨噬细胞集落刺激因子(rmGM-CSF)及重组小鼠白细胞介素_4(rmIL-4)的RPMI1640完全培养基培养,在培养第6天,实验组加入车前子苯乙醇苷类化合物(10,50,100 mg·L(-1)),对照组加入RPMI 1640或LPS(1mg·L~(-1)),流式细胞仪检测DCs表面分子CD11c,CD86,MHC Ⅱ和CD80的表达以及各组DCs吞噬功能的变化.结果:车前子毛蕊花苷和异毛蕊花苷能够提高DCs表面分子CD11c,CD86,MHC Ⅱ和CD80的表达;空白组DCs的吞噬功能很强(45.39%),车前子毛蕊花苷和异毛蕊花苷组DCs吞噬功能都明显下降(分别为37.27%,30.40%,33.45%和40.15%,37.59%,31.07%).结论:车前子苯乙醇苷类化合物能促进小鼠骨髓来源的DCs表型及功能的成熟.     

福参的苷类成分

目的 从福参Angelica morii提取分离活性成分。方法 采用乙醇提取，溶剂萃取，大孔树脂、聚酰胺、硅胶柱层析，LH-20、重结晶等纯化，对福参饮片进行系统提取分离；运用波谱学方法及理化常数对照进行结构鉴定。结果 从正丁醇和水部分分离到6个苷类化合物，分别为升麻索苷(prim-O-glucosylcimifugin，Ⅰ)、紫花前胡苷(marmesinin，Ⅱ)、芹菜素7-O-β-D-葡萄糖苷(apigenin 7-O0-β-D-glucoside，Ⅲ)、木犀草素7-O-β-D-葡萄糖苷(1ute—olin 7-O-β-D-glucoside，Ⅳ)，umbeliferone 7-apiosylglucoside(V)和胡萝卜苷(daucosterol，Ⅵ)。结论 6个化合物均为首次该植物中分得；化合物Ⅲ首次从当归属中分得。     

Plant cardiac glycosides and digoxin Fab antibody

The potential application of the Digoxin Fab antibody (Wellcome Digibind) in the clinical management of plant poisoning was investigated. The cardiac glycoside contents of various Australian plants were studied using immunoassay techniques. The cross-reactions of the Fab antibody and two digoxin assay antibodies against extracts of these plants were also studied. Results obtained indicated that the Digibind antibody cross-reacted with a wide range of glycosides contained in Australian plants and therefore could be of use in the treatment of life-threatening plant poisoning.     

Ovariectomy in the rat induces a rapid increase in the urinary excretion of hydroxylysine glycosides and non-reducible crosslink residues

The ovariectomized rat is the most commonly used animal model of human postmenopausal osteoporosis, exhibiting a high rate of bone turnover with resorption exceeding formation. At present, bone turnover is quantified directly by dynamic histomorphometry. The aim of the present study was to determine whether the measurement of the urinary output of some specific bone collagen catabolites — pyridinolines and hydroxylysine glycosides — could be used to indirectly monitor the initial phase of bone turnover increase in ovariectomized 90-day-old rats. Ninety-day-old female rats were randomly divided into three groups (n=6): ovariectomized, sham-operated and non-treated controls. Urine samples (24 h) were collected 6 days before surgery and twice weekly for the 4 weeks following ovariectomy. Urinary excretion of pyridinoline (PYD), deoxypyridinoline (DPD), glucosyl-galactosyl-hydroxylysine (GGHYL) and galactosyl-hydroxylysine (GHYL) were measured. As expected, ovariectomy was associated with a significant decrease in bone mineral density in both the proximal tibial and distal femoral metaphysis. Compared with both sham-operated and control animals, ovariectomized rats showed significant increases in PYD, GGHYL and GHYL urinary output 8 days after surgery and in DPD output after 15 days. These changes were maintained throughout the study. The results confirm that measurement of the urinary excretion of pyridinolines and hydroxylysine glycosides represents a powerful tool for detecting the onset of bone turnover in ovariectomized 90-day-old rats.     

用正交试验法探讨芸杞补肾口服液的生产工艺

作者采用正文试验法，以水提醇沉法提取和分离酚戒类有效成分，并以苯乙醇成含量作为含量测定指标，考察了乙醇浓度、提取温度及煎煮时间三个因素对有效成分提取量的影响，从而筛选出芸杞补肾口服液的是佳生产工艺。     

肉苁蓉总苷对阿霉素所致小鼠心肌毒性的保护作用

目的：探讨肉苁蓉总苷（GCs)对阿霉素（Dox)所致小鼠心肌损害的保护作用及其机制。方法：选用NIH小鼠一次腹腔注射Dox(17.5mg/kg)造成急性心肌损伤模型，测定心肌超氧化物歧化酶（SOD）活性；硒－谷胱苷肽过氧化物酶（Se-GSH-Px)活性；丙二醛（MDA）含量及血清肌酸磷酸激酶（CPK）活性。电镜检查心肌细胞超微结构的改变。结果：腹腔注射Dox 48h后可致小鼠心肌明显损害，心肌SOD及Se-GSH-Px活性下降，MDA含量升高，血清中CPK的活性增强，同时出现心肌组织超微结构的损伤。GCs(62.5、125.0、250.0mg/kg）能增加心肌SOD、Se-GSH-Px活性，降低MDA含量，减少CPK释放，减轻心肌超微结构的损伤。结论：肉苁蓉总苷对阿霉素所致心肌损害有一定的保护作用，其机制可能与其保护心肌SOD及Se-GSH-Px活性及其清除自由基，防止脂质过氧化有关。     

Reversal of toxic and non-toxic effects of digoxin by digoxin-specific fab fragments in isolated human ventricular myocardium

Summary The time course of the reversal of toxic and nontoxic effects of digoxin by digoxin-specific antibody fragments (Fab) was measured in isolated human ventricular myocardium. A concentration of 2×10^–6 mol/l digoxin was used to produce positive inotropy followed by mechanical signs of toxicity. After addition of a 1.5-fold higher molar concentration of digoxin-specific Fab, signs of toxicity disappeared within 30 min and digoxin-induced force of contraction decayed with a monoexponential time course with a half-life of 52 min. This rate of decay was almost identical to that observed for the dissociation of the digoxin-(Na⁺+K⁺)-ATPase complex in human heart cell membranes. It is concluded that (a) digoxin-specific Fab are capable of completely removing digoxin from its binding sites, (b) the maximal rate of removal of digitalis glycosides from the (Na⁺+K⁺)-ATPase is limited by the dissociation rate constant, and (c) there is a close correlation between the degree of binding of digitalis glycosides to the (Na⁺+K⁺)-ATPase and the increase in force of contraction.Abbreviation Fab Fragment antibody binding (digitalis antidote)     

In-vivo quantification of myocardial Na-K pump rate during β-adrenergic stimulation of intact pig hearts

Maintenance of adequate electrical activity of the heart depends critically on the ability of the Na-K pump to compensate for normal passive sodium and potassium fluxes. Using sudden injections of [³H]ouabain into the left coronary artery in anaesthetized open-chest pigs, we monitored transient changes in myocardial potassium balance by PVC-valinomycin mini-electrodes. When related to the number of pumps blocked and fractional inhibition, these data provided estimates of total Na-K pump capacity as well as actual pump rate and perturbations of the Na-K balance. Experiments were performed in hearts with and without intracoronary isoprenaline infusion (2.5 nmol min^-1). After injection of 120 nmol [³H]ouabain into the left coronary artery, myocardial [³H]ouabain concentrations were 118 (74–178) and 103 (76–145) pmol g^-1 and total concentrations of [³H]oubain binding sites were 893 (752–1076) and 785 (691–877) pmol g^-1 (median, 95% confidence interval) in isoprenaline-treated and control hearts respectively (differences not significant). The [³H]ouabain injection caused a net potassium release of 81 (56–132) and 43 (23–75) μcool 100 g^-1 (median, 95% confidence interval) in isoprenaline-treated and control hearts respectively (n= 6–8; significance of difference, P= 0.03). Na–K pump rate estimated from mono-exponential release curves was 6363 (3942–10,858) K⁺ ions min^-1 site^-1 during β-adrenoceptor stimulation and 2514 (1380–4322) in control (significance of difference, P= 0.03). This corresponds to 40 and 16%, respectively, of the maximum possible pump rate determined from ATP hydrolysis. Comparison of accumulated potassium release and relative Na-K pump rate indicates that catecholamines enhance the sensitivity of the Na-K pump for intracellular sodium.