人参皂苷Re促进自然衰老大鼠学习记忆作用及其机理的研究

目的研究人参皂苷Re对自然衰老大鼠学习记忆功能的影响,并初步探讨其作用机制。方法采用Morris水迷宫法观察人参皂苷Re对大鼠学习记忆功能的影响,同时采用电生理学方法观察人参皂苷Re对大鼠突触长时程增强(LTP)的作用。结果人参皂苷Re能显著对抗自然衰老引起的记忆获得障碍,对麻醉大鼠海马齿状回基础突触传递有增强作用,且能形成突触长时程增强形象。结论人参皂苷Re有改善大鼠学习记忆障碍的作用,该作用可能与其增强基础突触传递、促进LTP形成有关。     

痫宁片的质量标准研究

采用TLC法对痫宁片中黄芪、三七、白芍及柴胡进行了定性鉴别;并采用薄层扫描法测定黄芪甲甙及人参皂甙Rg1的含量,其平均回收率分别为97.55%、97.30%;RSD分别为3.22%、2.96%.     

红金消结片的制备与质量控制

目的:研究红金消结片的制备及其质量控制方法.方法:鉴别采用薄层色谱法,用高效液相色谱法测定人参皂苷Rg1含量.色谱柱为Cmsmosil C18(200mm×4.6mm,5μm),乙腈-0.05%磷酸溶液(21:79)为流动相;检测波长为203nm,柱温为25℃.结果:红金消结片中人参皂苷Rg1在0.7～6.3μg呈良好线性关系,r=0.999 2.结论:红金消结片制备工艺简单,质量控制方法可靠,重现性好.     

人参皂苷Rb1抑制β淀粉样蛋白25-35诱导的皮层神经元tau蛋白过度磷酸化

目的探讨人参皂苷Rb1对凝聚态β-AP_25-35诱导的胎鼠皮层神经元tau蛋白过度磷酸化的影响及其可能的作用机制。方法通过蛋白免疫印迹法和免疫细胞化学染色法检测神经元tau蛋白磷酸化水平、总tau蛋白水平和糖原合成酶3β(GSK-3β)的蛋白表达水平。结果凝聚态β-AP_25-35(20 μmol·L^-1)作用于皮层神经元12 h，tau蛋白磷酸化水平和总tau蛋白水平均增高，同时GSK-3β蛋白表达也增多。用人参皂苷Rb1或GSK-3β特异性抑制剂氯化锂预处理后，凝聚态β-AP_25-35诱导的tau蛋白的过度磷酸化受到明显抑制，同时GSK-3β的表达也降低。结论人参皂苷Rb1可通过抑制GSK-3β的表达来抑制凝聚态β-AP_25-35诱导的皮层神经元tau蛋白的过度磷酸化。     

Proposal of a Parameter for OATP1B1 Inhibition Screening at the Early Drug Discovery Stage

It is known that potent inhibition of organic-anion-transporting polypeptide (OATP)1B1 increases exposure to statins, leading to severe adverse effects. The aim of this study was to propose a parameter and its criteria in OATP1B1 inhibition assay at the early drug discovery stage to avoid compounds with the risk of statin-related adverse effects. According to drug label information, most compounds classified as “contraindicated” or “should be avoided” when administered concomitantly with statins increased their AUCs more than 4-fold. Generally, R values where R = 1 + plasma unbound fraction (fu) × maximum inhibitor concentration at the inlet to the liver/IC₅₀ are used to evaluate the extent of clinical drug interaction. However, clinical doses and C_max cannot be determined at the screening stage. Therefore, we estimated the correlations between change in AUC of statins concomitantly administered with OATP1B1 inhibitors and various parameters including fu/IC₅₀. Cyclosporin A, rifampicin, and telaprevir increased the AUC of statins more than 4-fold and fu/IC₅₀ of these compounds was >0.1 L/μmol. On the other hand, fu/IC₅₀ of other compounds was ≤0.03 L/μmol. This study indicates that fu/IC₅₀ is a useful parameter to avoid compounds that seriously affect statin potency through interaction with OATP1B1 at the screening stage.     

Amplified immune response by ginsenoside-based nanoparticles (ginsomes)

We describe here a novel adjuvant of ginsenoside-based nanoparticles (ginsomes) and its activity for up-regulation of immune response in mice. Ginsomes were assembled during removal of the detergent by dialysis in presence of ginseng saponins extracted from the root of Panax ginseng C.A. Meyer, cholesterol and phosphatidyl choline. The nanoparticles were spherical with diameters ranging from 70 to 107 nm, and contained ginsenosides Rb2, Rc, Rb1 and Rd. When co-administered with a model antigen ovalbumin (OVA) in ICR mice, ginsomes at a dose range from 10 to 250 μg promoted significantly higher IgG responses than OVA alone. Co-administration of ginsomes with OVA also significantly increased the levels of specific IgG1, IgG2a, IgG2b and IgG3, as well as T and B lymphocyte proliferation in response to Con A, LPS and OVA than when OVA was used alone. The enhanced IgG titer and subclass levels paralleled the increased production of IFN-γ (Th1 cytokine) and IL-5 (Th2 cytokine). Therefore, ginsomes as an adjuvant have up-regulated both Th1 and Th2 immune responses.     

Ocotillone—type Ginsenoside from Leaves of Pannax ginseng

An ocotillone-type ginsenoside,together with 2 known ginsenosids was isolated from leaves of Panax ginseng and identifed as psudoginsenoside-RT5 on the basis of chemical and physicohemical evidences.It has been so far the first example of ocotillone-type ginsenoside disicovered in Panax giunseng and its plausible biotransforrnation athway also discussed.     

肝郁调经颗粒质量标准研究

目的建立肝郁调经颗粒(白芍、佛手、郁金、玫瑰花、代代花等)质量标准。方法:用薄层色谱法鉴别白芍、佛手、牡丹皮、当归、香附;用高效液相色谱法测定芍药苷含量,采用μBondpackC18柱;以乙腈-0.2%磷酸水-四氢呋喃(8:92:5)为流动相,流速:1.0mL·min-1,检测波长230nm。结果:芍药苷含量在0.1912～1.912μg呈良好的线性关系,平均回收率100.55%,RSD为1.25%。结论:建立的定性定量方法简便、重复性好,可作为肝郁调经颗粒的质量控制。     

不同厂家参麦注射液人参皂苷含量比较

目的比较不同厂家参麦注射液中人参皂苷的含量。方法采用反相高效液相色谱法进行梯度洗脱,测定3个厂家生产的参麦注射液中人参皂苷Rg1、Re和Rb1的含量。色谱条件:汉邦L ichrospher C18色谱柱;流动相A为水,流动相B为乙腈;流速为1.2 mL/m in;检测波长为203nm;柱温为35℃。结果3个厂家生产的参麦注射液中人参皂苷Rg1、Re和Rb1的含量分别为12.36,4.26,93.80μg.mL-1;122.38,50.88,180.58μg.mL-1;153.24,58.73,115.38μg.mL-1。结论不同厂家参麦注射液中人参皂苷Rg1、Re和Rb1的含量差异较大。     

血栓通注射液治疗不稳定型心绞痛的临床观察

目的研究血栓通注射液治疗不稳定型心绞痛的临床疗效。方法将80例不稳定型心绞痛患者随机分为治疗组(40例)和对照组(40例)。两组患者常规给予西药抗心绞痛治疗,治疗组加用血栓通注射液。观察两组患者的心绞痛缓解、心电图ST-T改善情况,以及血脂、超敏C-反应蛋白等各项生化指标的变化。结果治疗组心绞痛缓解总有效率(97.5%,39/40)明显高于对照组(85.0%,34/40),两组比较,差异有统计学意义(P<0.01);两组治疗后心电图显示心肌缺血改善情况、血脂、超敏C-反应蛋白各指标比较,差异均有统计学意义(P<0.01)。结论血栓通注射液治疗不稳定型心绞痛疗效显著、安全可靠,具有较高的临床应用价值。