玳玳果黄酮降脂提取物体内组织分布规律及特征研究

目的：建立UPLC-MS/MS分析方法同时测定玳玳果黄酮降脂提取物效应组分新橙皮苷和柚皮苷在大鼠10种脏器组织中含量，分布规律及特征。方法：采用UPLC-MS/MS技术建立提取物效应组分新橙皮苷及柚皮苷在大鼠心、肝、脾、肺、肾、脑、胃、小肠、脂质、肌肉组织中的定量分析方法；大鼠给药后分别于0.33，0.67，1，4，8 h的5个时间点，分别摘取以上10种脏器组织，测定脏器组织及血液中效应组分的质量浓度，采用DAS（V 2.0）药动学软件对各样本的药物浓度-时间数据进行房室拟合，并计算不同组织效应组分的药-时曲线下面积（AUC）及平均滞留时间（MRT）。结果：所建立的UPLC-MS/MS定量分析方法具备良好的专属性、标准曲线及线性范围良好、方法准确度与精密度、定量下限均符合有关规定；玳玳果黄酮降脂提取物效应组分在血液中的分布符合一室模型，除肾脏及脑组织外，其余脏器中提取物效应组分的房室特征多为静脉注射的二室模型，柚皮苷在肾脏中的拟合结果为非静脉注射的二室模型，新橙皮苷在脑组织拟合结果为静脉注射的三室模型，给药后8 h各组织中效应组分新橙皮苷及柚皮苷AUC值大小顺序均为小肠 > 胃 > 肾 > 脂质 ≈ 脾脏 > 肺 > 肌肉 > 肝 > 心 > 脑，效应组分在各脏器中均无明显蓄积；效应组分在血液、肾脏、肝脏中的滞留时间较长，MRT均大于2 h，脂质最短，MRT不足1 h；各脏器中新橙皮苷的药-时曲线下面积约是柚皮苷的3倍，而心、肝、肾中则是3.5，2.1和3.4倍。结论：玳玳果黄酮降脂提取物效应组分在大鼠组织中分布迅速，达峰时间早于血液；效应组分在肠道内消除缓慢，给药8 h后在各脏器中的含量均显著下降且无特异的蓄积部位。研究结果揭示玳玳果黄酮降脂提取物效应组分在大鼠体内的分布特征及规律，为进一步理解玳玳果黄酮降脂提取物在体内的作用靶点及机制奠定了基础。     

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.     

钙和鸡冠花黄酮提取物对大鼠废用性骨质疏松的作用

目的探讨钙和鸡冠花黄酮提取物对废用性骨质疏松大鼠的作用,为骨质疏松的防治提供依据.方法选用健康SD大鼠40只,雄性.随机分为5组,第1、2组分别为正常对照和阳性对照,灌胃蒸馏水5 ml/(kg@d),第2～5组制造废用性骨质疏松大鼠模型,第3、4、5组为预防组,分别灌胃等量鸡冠花提取物,碳酸钙,鸡冠花提取物加钙溶液.实验8周后,测骨密度(BMD),股骨CT值,测血清MDA、SOD及24 h尿钙、羟脯氨酸(HOP)、尿肌酐含量等.结果阳性组与正常对照组比较股骨重、灰分重、CT值、血清钙下降,尿钙、尿HOP升高(P＜0.05或0.01),预防组与阳性组比较股骨重、CT值显著增加,碳酸钙组、鸡冠花加钙组灰分重显著增加(P＜0.05).与阳性组比较各预防组血清钙增加,尿钙、尿HOP减少(P＜0.05或＜0.01).鸡冠花组、鸡冠花加钙组与阳性组比较股骨BMD、血清SOD升高,MDA降低,单纯补钙组仅BMD升高(P＜0.05或＜0.01).结论鸡冠花提取物、钙对废用性骨质疏松大鼠骨质代谢均有促进作用,两者合用具有更好的预防效果,能延缓或减轻废用性骨质疏松的发生.     

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。     

舒血宁治疗脑衰弱综合征的双盲对照研究

１４３例脑衰弱综合征患者随机分成舒血宁组和对照组，进行双盲的前瞻性研究。通过脑衰弱量表，打洞试验，连线实验的回查，结果表明：应用舒血宁治疗脑衰弱综合征，整体疗效明显优于对照组，脑衰弱量表的总评分显著优于对照组，而且对脑衰弱量表各个症状都有显著改善，易激惹，烦恼两项症状降分幅度较大，打洞、连线试验表明舒血宁治疗后患者的注意力、记忆力都有明显的改善，而且没有发现明显副作用。作者认为舒血宁治疗脑衰弱综合征有显著的作用，作为一种治疗脑血管疾患伴发精神症状和早期预防脑血管痴呆的新药是可行的。     

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)