红景天中8种成分体外抗氧化作用的比较

目的比较性研究红景天中8种苷及醇类化合物———芦丁苷、红景天苷、异槲皮苷、酪醇、络塞琳、熊果苷、络塞维、肉桂醇红景天的体外抗氧化作用。方法测定8种成分对DPPH自由基、超氧阴离子自由基、一氧化氮自由基、羟自由基的清除能力,以及总抗氧化能力和抑制脂质过氧化反应的能力。结果除清除羟自由基实验外,异槲皮苷和芦丁苷作用明显强于其他化合物,其中在清除DPPH、超氧阴离子能力和抑制脂质过氧化实验中的IC50分别为5.72和10.46,23.63和36.39,10.78和56.49 mg.L-1;而在清除羟自由基实验中,酪醇和红景天苷的作用则强于其他化合物,IC50分别为10.84和18.97 mg.L-1。结论红景天中苷及醇类成分对多种自由基具有清除作用,有良好的综合抗氧化性和开发应用前景。     

管花肉苁蓉中活性成分提取纯化工艺研究

目的考察从管花肉苁蓉中提取、纯化苯乙醇总苷类物质的最佳工艺和条件。方法通过正交试验优化管花肉苁蓉中苯乙醇总苷的提取工艺,并通过筛选大孔吸附树脂、洗脱液,选择最适树脂和最佳纯化条件。结果苯乙醇总苷的最佳提取工艺为:12倍60%乙醇,超声提取3次,每次30min,提取率95%以上,从8种大孔吸附树脂中选出纯化效果最佳的DM130树脂,最大静态吸附量为344.49mg/g,用60%乙醇洗脱,解析率达96%,纯度达97%。结论该方法简单易行,周期短,成本低,所得苯乙醇总苷纯度高,对工业生产具有指导意义。     

龙胆总苷胃漂浮微丸制备及其体外释药特性研究

目的 制备龙胆总苷胃漂浮微丸,并探讨其体外释药特性。方法 采用助漂剂十六醇-微晶纤维素（7∶3）,以离心造粒法制备空白丸芯（40～60目）;采用HPMC-K15M为骨架材料和龙胆总苷等量混合以粉末层积法滚丸（20～30目）;采用Eudragit NE 30D进行流化床包衣,制得龙胆总苷胃漂浮微丸;以龙胆苦苷为指标,《中国药典》2010年版二部附录XC“转篮法”和HPLC法,测定胃漂浮微丸12 h释放度,并用Higuchi等数学模型对释放度数据进行拟合,探讨龙胆总苷胃漂浮微丸释药特性。结果 在人工胃液（pH 1.2）中,龙胆总苷胃漂浮微丸具有良好的漂浮性能和良好的缓释效果。累积释放率数据用Ritger-Peppas模型拟合度最高,相关系数R²＞0.97,且0.43＜n＜0.85,说明龙胆总苷胃漂浮微丸释药过程是溶蚀与扩散协同作用。结论 龙胆总苷制备胃漂浮微丸工艺可行,且能够达到胃滞留缓释的效果。     

小叶锦鸡儿中异黄酮及其苷类化合物的体外抗肿瘤活性研究

目的研究小叶锦鸡儿中异黄酮及其苷类化合物的体外抗肿瘤细胞增殖作用。方法利用四唑盐比色法检测,观察小叶锦鸡儿中分离出的3种异黄酮及其苷类化合物:雁靛黄素(Ⅰ)、高丽槐树-7-O-β-D-吡喃葡萄糖苷(Ⅱ)和芒柄花素-7-O-β-D-吡喃葡萄糖苷(Ⅲ)对人乳腺癌细胞株、宫颈癌细胞株、人肝癌细胞株生长的影响。结果化合物Ⅰ对人乳腺癌细胞株、宫颈癌细胞株的增殖均有明显的抑制作用,IC50分别为20.2、16.9μg.mL-1;化合物Ⅱ对乳腺癌细胞株、肝癌细胞株均有不同强度的抑制作用,IC50分别为17.9、18.8μg.mL-1;化合物Ⅲ对乳腺癌细胞株的增殖有抑制作用,但不呈现浓度依赖关系,对其他两个细胞株的增殖不显示抑制活性。结论化合物Ⅰ、Ⅱ对两种细胞株有不同程度的抗肿瘤活性,化合物Ⅲ不具抗肿瘤活性。     

沙棘果中总黄酮苷类的提取工艺研究

目的探讨沙棘果实中总黄酮苷类的最佳提取工艺。方法采用单因素实验和正交实验结合的方法筛选,对乙醇浓度、提取温度、料液比、提取时间进行四因素三水平的正交试验。结果最佳工艺条件为70℃下采用60%的乙醇浸提,固液比1∶15,回流提取(0.5 h×3)。结论首次将水解后的沙棘总黄酮苷元作为沙棘总黄酮提取工艺的评价指标,在分析检测方法上不仅应测定水解前,还应考察测定水解后总黄酮苷元的含量。     

藤甲酰苷缓释片的制备及体外释药因素考察

目的制备藤甲酰苷缓释片并研究其体外药物释放行为。方法通过亲水凝胶骨架型缓释技术,以羟丙基甲基纤维素(HPMC)为缓释材料、乙基纤维素(EC)为凝胶骨架材料制备藤甲酰苷缓释片;考查了释放介质的pH值、骨架材料与其用量、致孔剂的类型与用量、压片压力等工艺因素和条件对藤甲酰苷缓释片体外药物释放行为的影响。结果药物的释药速率受骨架材料的规格和用量、致孔剂种类的影响;释放介质pH值、转速和压片压力对释药速率有一定影响。结论研制的藤甲酰苷缓释片处方合理,有较好的可控性和重现性。     

雷公藤多甙联合泼尼松治疗成人紫癜性肾炎

目的探讨雷公藤多甙联合泼尼松治疗成人过敏性紫癜性肾炎(HSPN)的效果和安全性。方法选取60例明确诊断为HSPN的成人患者,随机分2组,观察组30例,采用雷公藤多甙联合泼尼松治疗,对照组常规激素治疗。治疗6个月观察疗效,追踪24h尿蛋白定量,血白蛋白等指标。也记录不良反应。结果治疗6个月后观察组尿蛋白较治疗前明显下降,差异有统计学意义(P<0.05)。两组治疗后比较差异有统计学意义(P<0.05)。治疗6个月后观察组血白蛋白较治疗前明显升高(P<0.05)。两组治疗后比较差异有统计学意义(P<0.05)。治疗组总有效率明显高于对照组(P<0.05)。两组未见严重不良反应发生。结论雷公藤多苷联合泼尼松治疗HSPN可有效降低尿蛋白,延缓紫癜性肾炎发展,疗效明显且安全可靠。     

Peony glycosides produce antidepressant-like action in mice exposed to chronic unpredictable mild stress: Effects on hypothalamic-pituitary-adrenal function and brain-derived neurotrophic factor

The root part of Paeonia lactiflora Pall. (Ranunculaceae), commonly known as peony, is a commonly used Chinese herb for the treatment of depression-like disorders. Previous studies in our laboratory have demonstrated that total glycosides of peony (TGP) produced antidepressant-like action in various mouse models of behavioral despair. The present study aimed to examine whether TGP could affect the chronic unpredictable mild stress (CUMS)-induced depression in mice. The mechanism(s) underlying the antidepressant-like action was investigated by measuring serum corticosterone level, glucocorticoid receptor (GR) and brain-derived neurotrophic factor (BDNF) mRNA levels in brain tissues. CUMS, being lasted for 6 weeks, caused depression-like behavior in mice, as indicated by the significant decrease in sucrose consumption and increase in immobility time in the forced swim test. Whereas serum corticosterone level was significantly increased in mice exposed to CUMS, expressions of GR mRNA in hippocampus, and BDNF mRNA in hippocampus and frontal cortex, were decreased in CUMS-treated mice. Daily intragastric administration of TGP (80 or 160 mg/kg/day) during the six weeks of CUMS significantly suppressed behavioral and biochemical changes induced by CUMS. The results suggest that the antidepressant-like action of TPG is likely mediated by modulating the function of hypothalamic-pituitary-adrenal axis and increasing the expression of BDNF in brain tissues.     

仙茅的酚苷和木脂素类成分的分离和鉴定

目的:分离鉴定仙茅Curculigo orchioides Gaertn.的酚苷和木脂素类成分.方法:利用硅胶和Sephadex LH-20凝胶柱层析,以及半制备HPLC方法分离化学成分,通过理化性质和光谱方法确定所分离化合物的结构.结果:仙茅乙醇提取物中得到5个酚苷类成分,1个木脂素类成分,1个甾醇类成分.经鉴定分别为2,6-二甲氧基苯甲酸(1)、仙茅苷(2)、仙茅苷乙(3)、仙茅素A(4)、2,4-二氯-5-羟基-3-甲基苯酚-1-O-β-D-吡喃葡萄糖-(1→6)-β-D-吡喃葡萄糖苷(5)、3,3′,5,5′-四甲氧基-7,9′7′,9-二环氧木脂素-4,4′-二-O-β-D-葡萄糖苷(6)、β-谷甾醇(7).结论:从仙茅乙醇提取物中分离出7个化合物,其中化合物(5)为一新的含氯酚类成分,命名为仙茅素D.     

Mechanistic insight into the functional and toxic effects of Strophanthidin in the failing human myocardium

BACKGROUND: Cardiac glycosides are characterized by a narrow therapeutic range with Ca2+-overload and arrhythmias occurring at higher concentrations. Data on cardiac glycosides in isolated failing human myocardium are scarce and the frequency-dependent actions and toxicity of Strophanthidin have not yet been characterized. AIMS: To determine inotropic responses and toxicity of Strophanthidin in failing human myocardium. METHODS AND RESULTS: Experiments were performed in trabeculae from 64 end-stage failing hearts. Developed force, and intracellular [Ca2+]i and [Na+]i were recorded with Strophanthidin (0.01 to 1 micromol/L; 37 degrees C, 1 Hz) and compared to interventions with distinct mechanisms of action (elevated [Ca2+]o, Isoproterenol, and EMD57033). The effects of Strophanthidin on force-frequency behaviour were also assessed. Strophanthidin exerted concentration-dependent positive inotropic effects. These were paralleled by increases in intracellular [Na+] as well as increasing [Ca2+]i-transients and SR-Ca2+-load. At high concentrations (>0.5 micromol/L), Strophanthidin caused afterglimmers and aftercontractions, with declining developed force despite further increasing [Ca2+]i-transients. The force-frequency-relationship and diastolic function at higher pacing rates was worsened by Strophanthidin in a concentration-dependent manner. CONCLUSIONS: Strophanthidin toxicity was dependent on concentration, calcium load, beating rate and beta-adrenergic receptor activation. Our data support the view that low doses, heart rate control and additional beta-adrenergic receptor blockade are essential in the use of cardiac glycosides in heart failure.