胡须刺激对大鼠桶状皮质局灶性脑缺血的神经保护作用

目的:研究胡须刺激对大鼠桶状皮质局灶性脑缺血的神经保护作用及可能机制。方法 :18只雄性SD大鼠先行胡须依赖实验,训练达标后随机分为假手术组、模型组和胡须刺激组。在显微镜下结扎右侧大脑中动脉2~3根分支构建大鼠胡须桶状皮质局灶性脑缺血模型,胡须刺激组于缺血3 d后开始刺激大鼠左侧胡须。造模成功后3组大鼠再次行胡须依赖实验直至再次达标,记录各组所需实验次数,并于术后14 d应用超声多普勒检测缺血区周围的血流量,HE染色观察缺血脑组织形态结构变化,免疫组化检测缺血区周围CD34的表达情况并测量微血管密度。结果:与模型组相比,胡须刺激组能显著减少胡须依赖实验再次达标所需次数(P<0.01),提高缺血区血流量(P<0.01),改善病理组织学,提高缺血区周围CD34阳性细胞的表达,微血管密度增多(P<0.01)。结论:胡须刺激对大鼠桶状皮质局灶性脑缺血有保护作用,其机制之一可能与诱导CD34的表达上调,改善脑缺血区的血流灌注有关。     

Radioiodinated Hypericin: Its Biodistribution, Necrosis Avidity and Therapeutic Efficacy are Influenced by Formulation

Purpose

To study whether formulation influences biodistribution, necrosis avidity and tumoricidal effects of the radioiodinated hypericin, a necrosis avid agent for a dual-targeting anticancer radiotherapy.

Methods

Iodine-123- and 131-labeled hypericin (¹²³I-Hyp and ¹³¹I-Hyp) were prepared with Iodogen as oxidant, and formulated in dimethyl sulfoxide (DMSO)/PEG400 (polyethylene glycol 400)/water (25/60/15, v/v/v) or DMSO/saline (20:80, v/v). The formulations with excessive Hyp were optically characterized. Biodistribution, necrosis avidity and tumoricidal effects were studied in rats (n?=?42) without and with reperfused liver infarction and implanted rhabdomyosarcomas (R1). To induce tumor necrosis, R1-rats were pre-treated with a vascular disrupting agent. Magnetic resonance imaging, tissue-gamma counting, autoradiography and histology were used.

Results

The two formulations differed significantly in fluorescence and precipitation. ¹²³I-Hyp/Hyp in DMSO/PEG400/water exhibited high uptake in necrosis but lower concentration in the lung, spleen and liver (p?<?0.01). Tumor volumes of 0.9?±?0.3 cm³ with high radioactivity (3.1?±?0.3% ID/g) were detected 6 days post-treatment. By contrast, ¹³¹I-Hyp/Hypin DMSO/saline showed low uptake in necrosis but high retention in the spleen and liver (p?<?0.01). Tumor volumes reached 2.6?±?0.7 cm³ with low tracer accumulation (0.1?±?0.04%ID/g).

Conclusions

The formulation of radioiodinated hypericin/hypericin appears crucial for its physical property, biodistribution, necrosis avidity and tumoricidal effects.     

不同厂家炙朝鲜淫羊藿饮片主成分含量比较

目的:对不同厂家炙朝鲜淫羊藿饮片主成分进行比较。方法:以反相高效液相色谱(PR-HPLC)法同时测定炙朝鲜淫羊藿饮片中5种主要黄酮类成分朝藿定A、朝藿定B、朝藿定C、淫羊藿苷和宝藿苷I的含量。结果:朝藿定A以亳州千草药业有限公司的炙朝鲜淫羊藿饮片含量最高;朝藿定B、朝藿定C以药都集团茗都中药饮片有限公司的炙朝鲜淫羊藿饮片含量最高;淫羊藿苷、宝藿苷I以安徽滕王药业有限公司的炙朝鲜淫羊藿饮片含量最高。结论:建立多种成分的含量测定方法可全面控制炙朝鲜淫羊藿饮片质量。     

胃安宁颗粒质量标准研究

目的:建立胃安宁颗粒的质量标准。方法:采用薄层色谱(TLC)法对方中黄芪、白花蛇舌草、苦参进行定性鉴别;采用高效液相色谱-蒸发光散射检测法测定黄芪甲苷的含量。结果:TLC鉴别斑点清晰,分离度良好。黄芪甲苷进样量在2.567～12.840μg范围内的对数值与峰面积对数值呈良好线性关系(r=0.9996);平均回收率为99.63%,RSD=4.69%(n=6)。结论:所建标准可用于胃安宁颗粒的质量控制。     

挤出滚圆法制备中药复方当归补血微丸及其性质考察*

目的：应用挤出滚圆法制备中药复方当归补血微丸，研究微丸制备的最佳工艺和处方。方法：用新型的挤出滚圆造粒机制备当归补血微丸；采用单因素考察和正交设计筛选最优处方和工艺条件；考察了微丸的粉体学性质、收率和体外溶出效果。结果：用挤出滚圆技术制备的当归补血微丸圆整度好，大小均匀，收率高，体外溶出迅速。结论：挤出滚圆法可以制备中药微丸。该工艺简便易行，制得的微丸质量好。     

中成药上市后“安全性信号”的识别与评价

上市后中药安全信号的识别与评价,是针对取得新药证书后的中成药实施常规药物警戒的主要手段,包括规范的药品不良反应／事件（ADR／ADE）报告的填写,报告的整理与归类,ADR病例组的概述及分析,应用数据挖掘识别药物一事件组合,重点关注的安全信号,计算报告率和发生率等6方面内容,用于ADR／ADE的日常监测,以便企业、药监部门、专家共同协作,针对“问题”品种采取进一步的深入研究。     

粪便内中短链脂肪酸柱前衍生化UHPLC-QTOF-MS/MS分析方法研究

建立柱前衍生化超高效液相色谱-串联四级杆飞行时间质谱(UHPLC-QTOF-MS/MS)定性、定量表征小鼠粪便内中短链脂肪酸的方法,并用于评价其在抗生素处置前后小鼠粪便样品中的变化。动物实验方案获得江苏省中医药研究院动物实验伦理委员会的批准。以3-硝基苯肼为衍生化试剂,对衍生化反应条件、色谱及质谱条件进行优化,建立了粪便中16个中短链脂肪酸的定性、定量方法。所有分析物在各自浓度范围内线性关系良好(R2>0.99),日内、日间精密度RSD均小于10%,重复性RSD小于6%,加样回收率介于80%～120%之间,样品36 h内稳定性RSD小于7%;联合抗生素处置后小鼠粪便内的中短链脂肪酸种类和含量均发生了明显改变。其中,甲酸、乙酸、丙酸、丁酸、异丁酸、戊酸、乳酸等含量明显降低,而庚酸和丁二酸的含量明显增加。该方法准确、可靠,可作为粪便内中短链脂肪酸的表征方法。     

硫磺熏蒸前后白芍HPLC-UV特征图谱的比较研究

目的:对白芍硫磺熏蒸前后的HPLC-UV特征图谱进行比较研究,为科学评价及有效控制其质量提供可靠方法。方法:采用RP-HPLC方法,使用Hypersil ODS C18(250 mm×4.6 mm,5μm)色谱柱,流动相为乙腈-0.5%醋酸水溶液,流速为1.0 mL·min-1,二元梯度洗脱,二极管阵列检测器,测定未经硫磺熏蒸和经硫磺熏蒸的白芍各10批,以芍药苷为参照物,检测波长为270 nm。结果:未经硫磺熏蒸的白芍中共有23个共有峰,经硫磺熏蒸的白芍中共有18个共有峰,通过与对照品的保留时间及紫外光谱比较,5、13、16、17号峰的归属分别为没食子酸、儿茶素、白芍苷、芍药苷。结论:白芍经硫磺熏蒸后,其成分发生了比较明显的变化,同时白芍在硫磺熏蒸前后,某些共有成分的含量也有不同程度的改变,硫磺熏蒸确实对白芍的质量有非常大的影响。     

冰片在不同贮存条件下稳定性的考察

目的：考察冰片在不同贮存条件下的稳定性,为冰片的贮存条件提供参考。方法：建立毛细管柱气相色谱法测定冰片中龙脑的含量,并系统考察在密闭条件下的光照、温度和空气对合成冰片稳定性的影响。结果：将冰片密闭贮存12月,其龙脑的含量仍大于55%,而樟脑的含量未检测;在低温、充氮和避光保存,其龙脑的含量比高温、不充氮和光照的含量高。结论：冰片经密闭贮存12月,龙脑的含量是保证的,且温度、空气和光照对冰片的稳定性有影响。     

The pharmacodynamic active components study of Tibetan medicine Gentianopsis paludosa on ulcerative colitis fibrosis

The current study focused on the pharmacodynamic activity components of Gentianopsis paludosa against ulcerative colitis (UC) fibrosis including symptoms of intestinal diarrhea and inflammatory. Trinitro-benzene-sulfonic acid induced UC model rats were gavaged with gradient polarity extracts respectively from ethanol-extract of Gentianopsis paludosa. Masson staining and qRT-PCR methods were respectively used to assess the degree of UC fibrosis and detect the mRNA expressions of collagen I, collagen III, a-smooth muscle actin (α-SMA) and E-cadherin in colon tissue. Separated by silica gel column chromatography, further screening was conducted until active components appeared. Infrared, nuclear magnetic resonance, mass spectroscopy and ultraviolet methods were applied to confirm active components' structures. The results indicated that the expression of collagen I, collagen III and α-SMA mRNA in the colon tissues of acetidin group rats was obviously depressed compared with control groups while E-cadherin displayed just opposite. Dyed in blue indicating UC fibrosis degree, the area of acetidin group was less than that other experimental groups. Four components: (1,8-Dihydroxy-3,7-Dimethoxyxanthones, 1-hydroxy-3,7,8-Trimethoxyxanthones, 1,7-Dihydroxy-3,8-Dimethoxyxanthones and 1-hydroxy-3,7-Dimethoxyxanthones), were obtained from acetidin group and all of which have a significant equivalence to Gentianopsis paludosa on the therapeutic effect of UC fibrosis. Our findings revealed the activity components for clinical application history of Gentianopsis paludosa and provided a preliminary foundation for further new drug research and exploitation.