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
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Amavadin诱导大鼠肾线粒体通透性转换孔开放与活性氧生成无关
Amavadin是自然积累于毒蘑菇鹅膏菌中的小分子钒复合物.近年来amavadin在肿瘤治疗研究中显现出一定的活性,但是其毒理机制并不清楚.本工作研究amavadin作用于大鼠肾线粒体的毒性效应及其可能作用机制.该研究结果表明,amavadin显著诱导线粒体通透性转换孔(PTP)开放,该作用并非和ROS生成相关.以琥珀酸为呼吸底物时,amavadin浓度依赖地抑制ROS生成;以苹果酸为呼吸底物时,200 μMamavadin显著促进ROS的产生.在苹果酸呼吸底物中,线粒体复合体Ⅰ抑制剂鱼藤酮能够显著促进amavadin诱导的活性氧生成增加;在琥珀酸呼吸底物中,鱼藤酮对amavadin抑制ROS生成的效应没有影响.以上结果提示,amavadin可能作用于线粒体呼吸链鱼藤酮抑制位点下游,线粒体复合体Ⅰ末端的泛醌结合位点是有可能的作用靶点.
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RP-HPLC-DAD法同时测定毛冬青根中4种三萜皂苷和2种木脂素的含量
建立了反相高效液相色谱-二极管阵列检测法同时测定毛冬青根中的6种活性成分(tortoside A,(+)-丁香脂素,毛冬青皂苷B3,毛冬青皂苷A1,毛冬青皂苷B1,毛冬青素A)的含量.RP-HPLC分离用反相C18分析柱,流动相以乙腈-0.1％磷酸水体系梯度洗脱.流速1.0 mL/min,检测波长为210 nm.6个指标成分达到基线分离,标准曲线具有良好的线性(r2＞0.9996),精密度、稳定性和重复性符合分析方法学要求.加样回收率范围为99.00％-104.52％.后对15个批次的毛冬青药材含量测定结果进行了聚类分析.结果表明该方法不仅可以对毛冬青药材进行质量控制,而且也为毛冬青药材的道地性分析提供了科学依据.
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高效液相色谱-质谱联用技术对缬草三酯稳定性的研究
缬草三酯属于多酰基类环烯醚萜化合物.中国药典2010年版一部蜘蛛香项下收载缬草三酯作为质量控制对照品使用.然而,结构不稳定是该类对照品发放中亟待解决的问题.本文通过高效液相色谱-质谱联用的方法对缬草三酯的稳定性进行了研究.根据ICH导则要求,使用加速稳定性实验对缬草三酯适宜贮存条件、运输和实验条件进行研究.结果表明,缬草三酯在碱性和加热条件下不稳定,而在酸性、氧化和强光照射条件下保持相对稳定.实验中有九个缬草三酯降解产物被检出,其中N1-N4为碱性水解时产生,B1-B5为热降解中产生.研究结果为本对照品的稳定性分析提供了依据.本文还对缬草三酯的制备、贮藏和使用等条件进行研究,该对照品在避光低温(-20％C)条件下贮藏.通过长期稳定性研究,在拟定的贮藏条件下,缬草三酯在3年内可以保持稳定.
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3-苯亚甲基-2-吲哚酮衍生物几何异构体的合成分离与NMR分析
本文合成了一系列3-(4'取代苯亚甲基)-2-吲哚酮的E和Z几何异构体,并采用反相硅胶色谱的方法首次对所有异构体进行了成功分离.通过对E和Z异构体1H NMR特征的分析发现了E和Z异构体中处于取代苯环屏蔽区的质子实际受到较明显去屏蔽效应的反常现象并对这种现象进行了分析.
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Gastric ulcer healing effect of wild honey and its combination with Turmeric (Curcuma domestica Val.) Rhizome on male Wistar rats
Gastric ulcer is a common disorder in human at any ages.In this research,the antiulcer activity of wild honey produced by Apis dorsata,alone or in combination with Turmeric Rhizome,was evaluated in healing acute gastric ulcer.Male Wistar albino rats (150-250 g) were induced ulcers with aspirin at 405 mg/kg BW and ethanol.Antiulcer evaluation was done based on the gastric acidity,numbers and diameter of ulcers,ulcer index,healing ratio,histological examinations,and body weight.The results showed that the groups given honey alone,turmeric alone,and combination of turmeric-honey displayed significant ulcer healing compared to the control group.Ulcers in the group administered with combination of turmeric-wild honey was different significantly from the turmeric alone and wild honey alone groups with increased body weight in that group.The result showed that wild honey (2125 mg/kg BW) had the greatest activity in healing ulcers among other groups.The combination of turmeric-wild honey had a good activity in healing ulcers and increased the body weight of the group.
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二甲双胍激活Nrf2信号并诱导抗氧化基因的表达
二甲双胍是一个一线抗糖尿病药物,然而其详细作用机制仍在研究中.Nrf2信号在保护细胞免受氧化性损伤中起着重要作用,近年来也成为干预糖尿病及其相关并发症的重要药物靶标.本研究在体内外实验中检测了二甲双胍对Nrf2信号的影响,并探究了其可能的机制.首先,二甲双胍激活AMPK和Nrf2信号,并以类似的浓度-和时间-依赖方式在小鼠骨骼肌细胞C2C 12中诱导抗氧化基因NQO1和γ-GCSm的表达.其次,过表达AMPK会显著提高基础的和二甲双胍诱导的ARE-萤光素酶报告基因的活性,说明AMPK参与了二甲双胍对Nrf2信号的激活.后,二甲双胍激活小鼠肝脏和骨骼肌组织中的Nrf2信号,诱导抗氧化基因HO-1和SOD的表达,导致GSH水平的增加.总之,我们的结果说明二甲双胍可以激活Nrf2信号和增强组织的抗氧化能力,并提供了二甲双胍作用的新机制.
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海藻酸包衣的季铵化壳聚糖纳米粒用于胰岛素口服给药的研究
本研究的目的是开发海藻酸包衣的壳聚糖纳米粒口服递送胰岛素.采用三聚磷酸钠(TPP)离子交联作用将N-[(2-羟基-3-三甲基铵)丙基]壳聚糖氯化物(HTCC)制备得到季铵化壳聚糖纳米粒(HTCC-T纳米粒),然后在温和搅拌条件下滴加入海藻酸钠溶液,进一步形成海藻酸包衣季铵化壳聚糖纳米粒(HTCC-A纳米粒).分别采用粒度仪、透射电镜和HPLC分析对HTCC-A纳米粒进行了粒径、zeta电位、表面形态、载药量和包封率的表征.结果表明,HTCC-A纳米粒为均匀的球形颗粒,大小为(322.2±8.5) nm,表面带有正电荷((14.1±0.6)mV).体外释放结果表明,在不同pH值的释放介质中,HTCC-A纳米粒的释放行为与HTCC-T纳米粒(未用海藻酸包衣)有很大的不同,这表明海藻酸包衣可以显著改善纳米粒中胰岛素的释放行为.同时,体外酶解试验和圆二色散图谱进一步证实,海藻酸包衣可以显著改善纳米粒中胰岛素结构稳定性.HTCC-A纳米粒十二指肠给药的相对药理生物利用度为8.0％±2.5％.与HTCC-T纳米粒口服给药相比,HTCC-A纳米粒的相对药理生物利用度显著增加(P＜0.05),是HTCC-T纳米粒的2.2倍.由此可见,海藻酸包衣季铵化壳聚糖纳米粒(HTCC-A纳米粒)将可能成为一种有效的口服递送载体系统用于提高胰岛素的体内口服吸收效果.
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Determination of the antioxidant activity based on the content changes in fatty acid methyl esters in vegetable oils
Free radicals,which are generated in several biochemical reactions in the body,have been implicated as mediators of many diseases,including cancer,atherosclerosis and heart diseases.Although the endogenous antioxidants can scavenge these free radicals,they are often insufficient to maintain the in vivo redox balance.The antioxidant activity (AOA) was examined by addition of each tested antioxidants [alpha-tocopherol (a-T),beta-tocopherol (β-T),gamma-tocopherol (γ-T),delta-tocopherol (δ-T),butylated hydroxyanisole (BHA),2,6-di-tert-butyl-4-methylphenol (BHT),and ascorbyle palmitate (AP)] to four types of different vegetable oils (sunflower oil,soybean oil,corn oil and olive oil).Moreover,content changes in fatty acids were then investigated every 3 months during the storage period.The results showed that the AOA was different among the tested antioxidants.The AOA for BHA was the most for different types of oil compared with other antioxidants,whereas the δ-T possessed the lowest AOA.
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Flavonoids:emerging trends and potential health benefits
Flavonoids are widely used in industry for the prevention of various diseases.In daily life we are directly in touch with flavonoids due to their presence in different beverages,fruits and vegetables.Flavonoids are mainly used as a coloring agent in plants,antioxidant and nutritional food for human.Flavonoids have explicit role in UV filtration,symbiotic nitrogen fixation and floral pigmentation.Flavonoids have potential for different biological activities like chelation of metals,decreasing platelets aggregation and cell signaling etc.
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