中国药学（英文版）杂志
Journal of Chinese Pharmaceutical Sciences 중국약학（영문판）
- 论文标题 期刊级别 审稿状态
-
新型溶栓蛋白的设计、制备及其活性评价
rPA作为溶栓药物之一,仍存在血浆半衰期短和颅内出血等问题.将rPA分子中PAI-1的水解部位突变,并与具有不同溶栓机制的NR3进行融合,再引入RGD序列,可能延长半衰期、增强溶栓作用、减轻出血副作用.据此,本研究克隆、表达和纯化了两个新型蛋白mrPA和mrPA-NR3,并进行活性评价.通过PCR扩增编码mrPA和mrPA-NR3的DNA片段,并克隆到pET-30a中构建重组质粒pET30a-mrPA和pET30a-mrPA-NR3,随后转化大肠杆菌E.coli BL21(DE3).通过异丙基β-D-1-硫代吡喃半乳糖苷(IPTG)诱导重组蛋白的包涵体表达,使用镍(Ni)亲和层析纯化,经过复性后用BCA法进行蛋白定量.分别对mrPA和mrPA-NR3的体内和体外溶栓活性及出血副作用进行了评价,结果发现:mrPA和mrPA-NR3均有明显的体外溶栓活性,在高浓度时,mrPA-NR3溶栓效果强于mrPA.mrPA和mrPA-NR3也具有明显的体内溶栓活性,在高剂量时,mrPA-NR3具有比mrPA更强的溶栓效果;二者的尾出血时间明显低于模型组,接近正常组.这些结果可能为提高溶栓药的药效和减轻出血副作用提供了新的思路,为进一步研究奠定了基础.
-
高效液相色谱法同时测定山蜡梅叶中的l-洋蜡梅碱、槲皮素和山奈酚的含量
运用高效液相色谱法,对江西道地药材山蜡梅叶中l-洋蜡梅碱、槲皮素和山奈酚3种成分进行含量测定,采用Agilent HC-C18色谱柱(250 mm×4.6 mm,5μm);流动相为甲醇-磷酸盐水溶液(10:90,v/v)至(90:10,v/v)梯度洗脱;柱温:25℃;流速1.0 mL/min;检测波长0-15 min为239 nm,16-45 min为365 nm;三个主要成分分离度良好,在测试范围内呈良好的线性关系,R2≥0.9991;精密度、重复性、稳定性良好;平均加样回收率在97.47％-98.26％之间,RSD平均值小于2.27％.利用该方法对不同采收时间的山蜡梅药材进行了生物碱和黄酮成分的定量测定,结果表明4～7月份药材中生物碱含量随月份推后不断增加,而黄酮成分在4、5月份的含量高,这与民间选择春季采药的习惯相匹配.该方法具有准确、快速、简便的特点,为山蜡梅药材的质量控制方法研究提供了实验数据,对于保证其质量和临床疗效具有重要的意义.
-
LC-MS/MS法测定大鼠血浆中PAC-1的新型抗癌衍生物的浓度及其药物动力学研究
本研究建立了一个新的、灵敏的液相色谱-串联质谱法用于测定大鼠血浆中SM-1的浓度.在简单的蛋白沉淀处理后,用乙腈-甲醇-10mM乙酸铵溶液(37.5∶37.5∶25,v/v/v)作为流动相,在C18反相色谱柱(50 mm×4.6 mm,3.5 μm)上分离SM-1和内标(吉非替尼).质谱检测使用三重四级杆串联质谱,电喷雾正离子模式、质谱多反应监测技术对待测物SM-1和内标物分别在质核比为407.3→203.4和447.3→128.3处进行检测.方法学验证的线性范围为30至6000 ng/mL,批内和批间的精密度都小于4.7％.平均回收率在98.7％-104.1％之间.在样品制备和分析程序中SM-1都是稳定的.测定结果均符合FDA生物分析方法指导原则的要求.该方法已成功地应用于测定单次口服50、100、200 mg/kg剂量后,大鼠血浆中SM-1的浓度.
-
姜黄素类似物和多西紫杉醇对人前列腺癌细胞生长的协同作用
前列腺癌是发生于男性前列腺组织中的恶性肿瘤,近年来我国前列腺癌发病率迅速上升.本文以前列腺癌细胞PC-3细胞株为主要研究对象,联合姜黄素类似物E10和多西紫杉醇作用于前列腺癌细胞,比较其与单独给药的作用效果.结果显示低剂量的姜黄素类似物E10与低剂量的多西紫杉醇联合使用,比两种药物单独高剂量使用更能有效地抑制前列腺癌细胞生长,核转录因子NF-κB信号传导通路和Erk1/2传导通路具有协同作用的机制.研究结果表明联合姜黄素类似物E10和多西紫杉醇对抑制前列腺癌细胞具有一定的协同效应.
-
Synthesis and characterization of pyrimidines analogues as anti-Alzheimer's agents
Pyrimidine derivatives have been reported as neuroprotective agents useful for the treatment of various neurodegenerative disorders.In the present study,several pyrimidine analogues have been evaluated as neuroprotective agents in Morris water maze model.It was observed that pyrimidine derivatives 8-17 considerably improve learning,memory,and movement deficits in animal models.Biochemical estimations of brain serum of treated animals revealed suppression of oxidative and nitrosative stress,acetylcholinesterase activity,and other parameters which leads to neurodegeneration of brain.Of all the pyrimidine derivatives,thiomorpholine derivative 8 and piperazine ethanol derivative 17 were found to be the most active neuroprotective agents and produced effects comparable to standard drug rivastigmine in terms of behavioral,biochemical,and molecular aspects.
-
Alpinia zerumbet,a ginger plant with a multitude of medicinal properties:An update on its research findings
In this review,the botany and uses ofAlpinia zerumbet (yan shan jiang) are described,and the current knowledge of its phytochemistry,pharmacological properties,and clinical trials is summarized.An important ginger crop in East Asia,A.zerumbet has many uses,both medicinal and non-medicinal.Leaves are used to produce essential oils and herbal teas.Rhizomes are consumed as spices,and stem fibers are made into paper,fabrics,and handicrafts.In Brazil,tea from A.zerumbet leaves is believed to have hypotensive,diuretic,and anti-ulcerogenic properties.This species possesses many medicinal properties due to its chemical constituents,including flavonoids,phenolic acids,phenylpropanoids,kava pyrones,sterols,and terpenoids.Extracts of A.zerumbet display antioxidant,antimicrobial,insecticidal,anthelmintic,tyrosinase and melanogenesis inhibitory,anti-atherogenic,anti-aging,anti-glycation,integrase and neuraminidase inhibitory,lifespan prolongation,hair growth promotion,anticancer,antidepressant,anxiolytic,anti-obesity,analgesic,anti-inflammatory,hypolipidemic,anti-ulcerogenic,anti-platelet,osteoblastic,osteogenic,thrombolytic,and cardiac arrhythmogenic activities.Essential oils ofA.zerumbet leaves have antimicrobial,larvicidal,antinociceptive,hypotensive,vasorelaxant,myorelaxant,antispasmodic,antidepressant,anxiolytic,anti-neuraminidase,anti-atherogenic,anti-aging,anti-melanogenic,anti-tyrosinase,cytoprotective,cardiodepressive,antipsychotic,analgesic,anti-inflammatory,and tissue healing activities.Clinical trials conducted in Brazil showed that extracts of A.zerumbet have hypotensive and diuretic effects whereas topical application of the essential oil has positive therapeutic effects on patients with fibromyalgia.Spanning two continents of Asia and South America,A.zerumbet is truly a multi-purpose ginger plant with promising medicinal properties.
| 年 | 期数 |
| 2018 | 01 02 03 04 05 06 07 08 09 10 11 |
| 2017 | 01 02 03 04 05 06 07 08 09 10 11 12 |
| 2016 | 01 02 03 04 05 06 07 08 10 11 12 |
| 2015 | 01 02 03 04 05 06 07 08 09 10 11 12 |
| 2014 | 01 02 03 04 05 06 07 08 09 10 11 12 |
| 2013 | 01 02 03 04 05 06 |
| 2012 | 01 02 03 04 05 06 |
| 2011 | 01 02 03 04 05 06 |
| 2010 | 01 02 03 04 05 06 |
| 2009 | 01 02 03 04 |
| 2008 | 01 02 03 04 |
| 2007 | 01 02 03 04 |
| 2006 | 01 02 03 04 |
| 2005 | 01 02 03 04 |
| 2004 | 01 02 03 04 |
| 2003 | 01 02 03 04 |
| 2002 | 01 02 03 04 |
| 2001 | 01 02 03 04 |
