几种常见天然化合物对ABCA1表达影响的研究进展

动脉粥样硬化是心血管疾病的主要病理基础,细胞内胆固醇蓄积引起的泡沫细胞形成是导致动脉粥样硬化发展的重要因素。三磷酸腺苷结合盒运转体A1(ABCA1)在胆固醇代谢中有着重要作用。许多天然化合物如葛根素、姜黄素、芍药醇等能够增加ABCA1的表达,促进胆固醇流出,减少细胞内胆固醇蓄积,抑制泡沫细胞形成。本文主要综述了天然化合物对ABCA1表达调控及动脉粥样硬化的影响,为心血管疾病的预防与治疗提供新的思路。     

复方银黄微型灌肠剂对发热大鼠下丘脑中COX-1、COX-2蛋白表达的影响

目的:研究复方银黄微型灌肠剂(compound of Yinhuang micro-enema,YHCE)对发热大鼠下丘脑中环氧化酶-1(cyclooxygenase,COX-1)、环氧化酶-2(cyclooxygenase,COX-2)蛋白表达的影响,探讨YHCE的解热作用机制.方法:用酵母混悬液复制发热大鼠模型,采用免疫组化ElivisionTM plus二步法观察下丘脑中COX-1、COX-2蛋白表达的情况.结果:YHCE能明显抑制发热大鼠的体温上升,且能抑制下丘脑中COX-2蛋白表达,而对下丘脑中COX-1蛋白表达无明显影响.结论:YHCE有明显的解热作用,其解热作用机制可能与抑制发热大鼠下丘脑中COX-2蛋白表达有关.     

肌苷衍生物的碱基核糖化研究

目的研究N1-核糖肌苷衍生物的合成反应。方法用丙叉保护肌苷2′,3′-OH,单甲氧基三苯甲基保护5′-OH,在碳酸钾、18-冠醚-6作用下与2,3,5-O-三苄基-1-溴代核糖反应。结果反应得到N1-核糖肌苷衍生物。结论用酰基做保护基易发生酰基重排反应,改用丙叉保护肌苷2′,3′-OH,再用单甲氧基三苯甲基保护5′-OH与2,3,5-O-三苄基-1-溴代核糖在碳酸钾18-冠醚-6作用下得到目的物N1-(2,3,5-O-三苄基-D-核糖)-2′,3′-O-异亚丙基-5′-O-单甲氧基三苯甲基肌苷。     

吸附澄清剂在HL颗粒中的应用

目的:考察吸附澄清剂在HL颗粒除杂工艺中的应用。方法:以黄芪甲苷的含量、干膏得率为指标,比较了乙醇沉淀与加澄清剂的除杂效果;并采用单因素实验优选了ZTC1+1-Ⅱ型吸附澄清剂除杂的工艺参数,包括ZTC1+1-Ⅱ型吸附澄清剂的加入量、加入顺序、药液浓度、搅拌速度等。结果:ZTC1+1-Ⅱ型吸附澄清剂处理对黄芪甲苷含量影响较小,且能明显降低出膏率,研究所得除杂工艺为:取提取液浓缩至药材重(g)与提取液体积(ml)为1:5时,先加入澄清剂B组分,后加入A组分,搅拌速度100～150 r/min。结论:澄清剂法比水醇法工艺简单,生产周期短,减少乙醇用量,节省能源,以ZTC1+1-Ⅱ型吸附澄清剂除杂能较好的保留黄芪甲苷,而且除杂效果明显。     

稳定剂和防灰雾剂对溴碘化银T-颗粒乳剂微晶体电性能的影响

利用Wagner极化法研究稳定剂和防灰雾剂对溴碘化银T-颗粒乳剂微晶体的电子电导率和空穴电导率的影响。实验结果表明:将乙基巯基四氮唑、吗啡啉-4-甲酸硫代-(1-苯基四氮唑-5)酯、苯并三氮唑甲酸苯酯、2-甲基巯基-4-羟基-6-甲基-1,3,3a,7-四氮茚等4种稳定剂和防灰雾剂用在溴碘化银T-颗粒乳剂中,对乳剂电性能都有一定的影响。其中,乙基巯基四氮唑防灰雾剂的影响最为显著。研究表明:添加了稳定剂和防灰雾剂的溴碘化银T-颗粒乳剂微晶体的电性能与其防灰雾性能具有较好的相关性。当稳定剂和防灰雾剂使溴碘化银T-颗粒乳剂微晶体的电子电导率和空穴电导率增大时,乳剂的稳定性和防灰雾性能就增强。     

甘草次酸-氟尿嘧啶复合物对人肝癌Bel-7402细胞的抗癌活性

【摘要】目的探讨甘草次酸-氟尿嘧啶类复合物-18β-甘草次酸酮-N-羟甲基-5-氟尿嘧啶（GA-Fu）的体外抗癌活性及细胞毒性。方法利用人肝癌多药耐药株Bel．7402细胞株,用MTT法观察GA—Fu对肝癌细胞增殖的抑制活性;用正常肝细胞changliver测定GA-Fu对正常细胞的毒性,并与5．氟尿嘧啶进行对照。结果GA—Fu与5-氟尿嘧啶（5-Fu）在浓度为25～250μg／ml范围内对人肝癌Bel-7402细胞具有明显的抑制活性,其抑制率随浓度提高而增强,呈浓度依赖性。尤其在较高浓度（200～250斗g／m1）下,GA—Fu对人肝癌Bel-7402细胞的增殖的抑制率（46％-57％）明显高于对照物5．氟尿嘧啶（33％～39％）（P〈0．05）;而对正常肝细胞的毒性（最高可达9．96％）则明显低于5-氟尿嘧啶（18．50％）（P〈0．05）。结论甘草次酸与抗癌药5-氟尿嘧啶进行耦合可提高5-氟尿嘧啶的抗癌活性并降低其对正常细胞的毒性,这可能是产生抗癌协同及化疗增敏作用的结果。本研究为甘草次酸-氟尿嘧啶类偶合物中筛选新型肝靶向抗癌候选药物奠定了一定基础。     

Dipeptidyl peptidase IV of Streptococcus anginosus: purification and characterization

We found that N-unblocked nine p-nitroanilde derivatives of amino acids or peptides were hydrolyzed by the crude cell extracts of Streptococcus anginosus NCTC 10713. Then dipeptidyl peptidase IV was purified 323-fold by the procedures including ammonium sulfate concentration, anion exchange chromatography (twice), gel filtration (twice), hydrophobic interaction chromatography, and isoelectric focusing. The molecular weight was calculated as 84 kDa, and the isoelectric point was 4.9. The enzyme hydrolyzed mainly dipeptides containing proline residues at P1 position. It was strongly inhibited by serine enzyme inhibitors. General protease inhibitors, metal chelators, thiol alkylating agent, reducing agent, and several metal ions had no effect on the enzyme activity. Optimum pH for the activity was found at 7.0. The enzyme was mostly inactivated by heating at 50 degrees C for 15 min.     

Radiolabeling LyP-1 peptide and preliminary biodistribution evaluation in mice bearing MDA-MB-435 xenografts

Background Recent studies have shown the LyP-1 peptide can home to either tumor lymphatics or the tumor cells and be internalized by targeted cells.This study aimed to investigate the possibility of us...     

A clinical study of intubating conditions under vecuronium bromide.

The drug vecuronium bromide, a short acting, non-depolarising agent with little side-effects, has brought much promise in the field of muscle relaxants. Fifth healthy patients were induced with injection thiopentone sodium 4 mg/kg and vecuronium bromide, 0.1 mg/kg was given IV. The earliest time at which the largest percentage of patients could be intubated satisfactorily was noted. The intubating conditions were estimated by scoring method. The duration of clinical relaxation was decided from the time of IV injection of vecuronium bromide to the return of muscle power of the non-respiratory muscles requiring repeat dose of the drug. The ideal intubating condition was achieved at 120 seconds and the duration of clinical relaxation ranged from 11-15 minutes.     

桂麻合方对哮喘豚鼠引喘潜伏期及肺组织病理变化的影响

目的:探讨桂麻合方对哮喘豚鼠引喘潜伏期及肺组织病理变化的影响.方法:建立豚鼠哮喘模型,设立正常对照、哮喘模型、桂枝汤、麻黄汤、桂麻各半汤(先煎后合)、桂麻各半汤(先合后煎)、桂二麻一汤(先煎后合)、桂二麻一汤(先合后煎)共八组,分别测定豚鼠引喘潜伏期并在光镜下观察豚鼠肺组织的病理学改变.结果:桂麻合方六组皆能延长哮喘豚鼠的引喘潜伏期;且桂麻合方六组均可改善哮喘豚鼠肺组织的病理改变,但六组的作用强度不尽相同.结论:桂麻合方能减轻过敏性哮喘豚鼠肺内局部炎性反应,从而缓解哮喘发作.提示桂麻合方治疗哮喘可能是通过延长哮喘发作的潜伏期,减少肺组织炎性浸润而实现的.