桃仁提取物对小鼠急性肝损伤的保护作用

目的:研究桃仁乙醇提取物对四氯化碳(CCl4)和乙醇所致小鼠急性肝损伤的保护作用。方法:采用CCl4和乙醇制备小鼠急性肝损伤模型,观察桃仁乙醇提取物对小鼠血清和肝匀浆谷丙氨酸氨基转移酶(ALT)、天冬氨酸氨基转移酶(AST)活性;肝匀浆超氧化物歧化酶(SOD)活性、丙二醛(MDA)和谷胱甘肽(GSH)含量的影响。结果:桃仁乙醇提取物能降低急性肝损伤小鼠血清中ALT、AST活性;降低肝匀浆AST活性和MDA含量;提高SOD活性和GSH含量。结论:桃仁乙醇提取物对急性肝损伤有一定的保护作用,其机制可能与抗脂质过氧化作用有关。     

保心微丸中肉桂酸大鼠体内的药代动力学研究

目的研究保心微丸中肉桂酸在大鼠体内的药代动力学.方法采用高效液相色谱法测定肉桂酸血药浓度,色谱柱HypersilODSC18,150mm×4.6mm,5μm,柱温30C.流动相甲醇-1%醋酸(4555)流速0.5mL/min;检测波长273nm;进样量10μL.结果与结论建立了用高效液相色谱法测定肉桂酸血药浓度的方法,肉桂酸的峰面积(y)与浓度(X)之间的回归方程为y=4973.5348+42867.96678X,相关系数r=0.9998.肉桂酸在血浆中的回收率为97.5%,RSD为1.33%.检测限为0.15ng,大鼠血浆中最低检测浓度为75ng/mL.肉桂酸口服吸收在大鼠体内的药时过程为线性动力学过程,符合一级吸收一级消除的开放式室模型,t1/2(K.)为7.12min,tmax为53.29min,Cmax为0.20μg/mL,t1/2,2(Ke)为340.74min.该药代动力学参数可能是保心微丸中肉桂酸及有关成分等多种成分在大鼠体内的综合体现.     

Use of the 3-nitro-2-pyridine sulfenyl protecting group to introduce Nε-branching at lysine during solid-phase peptide synthesis I. Application to the synthesis of a peptide template containing two addressable sites

TASPs (template-assembled synthetic peptides) are generated by the covalent attachment of linear peptides to a common peptide backbone, thus generating larger synthetic peptides/proteins with prefolded structure. In this work we present a strategy for the synthesis of a heterotemplate-assembled synthetic peptide containing two addressable sites. This orthogonal protection strategy would allow the selective introduction of different peptide chains via the ε-amino functions of template lysines being protected by either fluorenylmethoxycarbonyl (Fmoc) or 3-nitro-2-pyridine sulfenyl (Npys) groups. The N^α-Boc-N^ε-Npys-l -lysine required for solid-phase peptide synthesis (SPPS) is not readily available at a reasonable cost. To facilitate the more widespread use of this reagent we have compared the two published procedures for synthesizing this protected amino acid and evaluated the suitability of the products for SPPS. Two resin-bound peptides, a tripeptide Ac-G-K-Npys)-G-resin and an octapeptide template Ac-P₁-K₂-K₃-L₄-K_s-K₆-P₇-G₈-resin, were synthesized by SPPS. The ε-amino functions of lysines K₂ & K₆ and K₃ & K₅ of the octapeptide were protected by Fmoc and Npys groups, respectively. Secondly, these peptides were used to evaluate various reagents and reaction conditions for the deprotection of the ε-amino function of lysines bearing the N_ε-Npys protecting group. A procedure for the optimized selective and quantitative deprotection of the Npys group from the ε-amino function of lysine in a resin-bound peptide using 2-mercaptopyridine-N-oxide is described. © Munksgaard 1995.     

Mast cell protecting effects of shilajit and its constituents

The effects of shilajit and the combined effects of its main constituents, fulvic acids (FAs), 4′-methoxy-6-carbomethoxybiphenyl (MCB) and 3,8-dihydroxy-dibenzo-α-pyrone (DDP), were studied in relation to the degranulation and disruption of mast cells against noxious stimuli. Shilajit and different combinations of FAs, MCB and DDP provided statistically significant protection to antigen-induced degranulation of sensitized mast cells, markedly inhibited the antigen-induced spasm of sensitized guinea-pig ileum, and prevented mast cell disruption induced by compound 48/80. The findings are appraised in view of the clinical use of shilajit in the treatment of allergic disorders in Ayurvedic medicine.     

Improved method for the synthesis of Nα-9-fluorenylmethyloxycarbonyl-Nδ,ω bis-adamantyloxycarbonyl-L-arginine

A modified method is reported for the prepartion of N^α-9-fluorenylmethyloxycarbonyl-N^δ,ω bis-adamantyloxycarbonyl-L-arginine, giving an overall yield of 60% over three steps based on N^α-benzyloxycarbonyl-L-arginine. Commercially available adamantyl fluoroformate for guanidine function protection of N^α benzyloxycarbonyl-L-arginine, catalytic transfer hydrogenation with formic acid on palladium black for removal of the benzyloxycarbonyl protecting group, and fluorenylmethylsuccinimidyl carbonate for the final synthesis, were introduced to simplify and reduce the cost of preparation of this arginine derivative. The reaction conditions have been accurately studied at each step in order to optimize the yields.     

Experimental Observation on the Effects of Different Chitosan on Preventing Traumatic Peritoneal Adhesion in Rats

objective： The effects of different chitosan on preventing traumatic peritoneal adhesion in rats was studied in this paper. METHODS ： 96 SD rats with injured vermiform process were randomly divided into 4 groups as follows： group A without any treatment as control, group B treated with chitosan gel, group C treated with pure chitosan film and group D treated with chiston film containing 50% gelatin. 2 and 4 weeks after surgery, 12 rats in each group were respectively belly opened to observe chitosan degradation and evaluate peritoneal adhesion, and the adhesive vermiform processes tissues were histopathologically observed. RESULTS： 1. Degradation in the group D was faster than that in the group C but slower than that in the group B. 2. 2 weeks after surgery the adhesion in the group B was milder than that in the control group（goup A） （P〈0. 05）, but that in the group C and D （both P〈0. 05） were more severe than that in the control group. 3. 4 weeks after surgery , the adhesion in the group B was milder than that in the control group （P〈0. 05）, but that in the group C and D （both P〈0. 05） were more severe than that in the control group , whereas, there was no significant difference between adhesion in the group C and group D （P〉0. 05）. 4. Histopathological examinaiton indicated that： 2 weeks after surgery ,inflammatory cell infiltration and fibroplastic proliferation dominated in local lesion and the response was most severe on the serous coat, furthermore, the response in the control group was more severe than that in the group B, but milder than that in the group C and D; 4 weeks after surgery, fibroplastic proliferation dominated in local lesion in each group , moreover, the response in the control group was more severe than that in the group B but milder than that in the group C and D. What＇s more, integrated fibrous membrane formed around implanted materials in the group C and D, and the fibrous membranes were thinner in the group C than that in the group D. CONCLUSION： 1.Chitosan gel has perfect effect in protecting traumatic peritoneal adhesion in rats. 2. Pure chitosan film could exacerbate peritoneal adhesion and chitosan containing gelatin could exacerbate peritoneal adhesion further.     

鸡骨草的化学成分、药理作用及临床应用研究进展

鸡骨草是豆科植物相思子属植物,在我国广东、广西等地均有分布。鸡骨草在我国有着悠久的用药历史,常以全株入药,具有利湿退黄、清热解毒、舒肝止痛等功效。通过查阅中国知网,万方,维普,Science Direct,FMRS,Pubmed等国内外多个数据库,对近年来关于鸡骨草植物化学成分、药理作用及临床应用的相关文献进行归纳和总结,经全面分析后,分类归纳成综述。经调研大量相关的文献发现,鸡骨草含有大量丰富的化学成分,如白桦酸等三萜类成分,儿茶素等黄酮类成分,相思子碱等生物碱类成分,大黄酚等蒽醌类成分以及无机元素。鸡骨草丰富的物质基础使其具有广泛的药理作用,鸡骨草作为民间传统药材,临床上常用于湿热黄疸,胁肋不舒,胃脘胀痛,乳痈肿痛,脂肪性肝病、肝炎和跌打内伤的治疗。此外,鸡骨草还具有抗肿瘤、抗氧化、抗菌、抗病毒、抗炎镇痛、促进伤口愈合、免疫调节等多种药理作用。目前,临床上有鸡骨草单味药或与中药复方联用,其中以与中药复方联用为主,鸡骨草通过与其他药材配伍更好地发挥药效。鸡骨草广泛的药理作用,加之廉价易栽培的特点,使其具有极高的经济价值和社会效益,有着巨大的开发潜力和广阔的市场前景。基于近30年来国内外对鸡骨草的研究,本文从化学成分、生物活性及临床应用等方面对鸡骨草的研究现状进行了综述,以期能为进一步合理开发和综合利用鸡骨草的药用资源提供参考。     

丹皮酚衍生物及其药理活性研究进展

丹皮酚具有广泛的药理活性,主要具有保护心脑血管系统、促进微循环、抗菌、抗炎、抗肿瘤、抗氧化、抗变态反应、增强免疫力以及治疗糖尿病、骨质疏松症等作用。近年来,为了提高丹皮酚生物利用度,不仅改进其人工合成的方法,还对丹皮酚进行了大量的结构修饰及改造,包括羰基、酚羟基、羰基α-氢、甲氧基以及苯环,生成了羧酸酯类、磺酸酯类、磷酸酯类、醚类、NO供体类、糖苷化类、丹皮酚钠盐、Schiff碱类、噻唑类、肟类、羟烷基化类、α,β-不饱和酮类、胺甲基化类、α-氢卤代类、去甲基化类、苯环卤代类16种丹皮酚衍生物。结合国内外有关丹皮酚衍生物的文献,对丹皮酚衍生物及其药理活性方面进行综述,为此类化合物的进一步研究提供参考。     

Synthesis of S‐thiomethyl MAG3, radiolabelling with technetium‐99m and biological evaluation

Protection of the thiolate function of the mercaptoacetyltriglycine (MAG₃) by S‐thiomethyl group allows automatic deprotection of the protecting group during technetium‐99m radiolabelling by transchelation using stannous chloride dihydrate as reductant. Protection of the thiolate group with S‐thiomethyl increases the stability of the ligand, desired complex of high radiochemical purity could be prepared under relatively mild labelling condition (at room temperature) omitting the aeration step. The complex prepared from the S‐thiomethyl protected MAG₃ ligand were chromatographically (HPLC) and biologically compared with the corresponding complex prepared from the S‐benzoylated MAG₃ precursor. This result suggests that technetium‐99m complex of MAG₃ could be prepared from S‐thiomethylated MAG₃ precursor in comparatively higher purity under relatively milder labelling condition and this method of radiolabelling could be used for the development of less cumbrous single vial MAG₃ kit. Copyright © 2012 John Wiley & Sons, Ltd.     

针刺保肝护脑对脑缺血再灌注 肝损伤大鼠CATmRNA表达的影响

目的:探讨针刺保肝护脑对脑缺血再灌注肝损伤大鼠CATmRNA表达的影响。方法:将40只SD雄性大鼠随机分为假手术组、模型组、针刺对照组、针刺保肝护脑组。线栓法制作缺血再灌注大鼠模型,测试大鼠行为学、血清谷丙转氨酶(ALT)、谷草转氨酶(AST)、过氧化氢酶(CAT)活性、肝组织CAT mRNA含量。结果:模型组、针刺对照组和针刺保肝护脑组缺血2 h(电针治疗前)时神经功能缺损评分无显著差异;经10次电针治疗结束后:与模型组相比,针刺对照组和针刺保肝护脑组神经功能缺损评分有极显著差异(P<0.01);与针刺对照组相比,针刺保肝护脑组神经功能缺损评分变化更为显著(P<0.05)。电针治疗前,与假手术组、针刺对照组和针刺保肝护脑组比较,模型组血清ALT、AST水平显著增高(P<0.01),而血清CAT、肝组织CATmRNA明显降低(P<0.01);经10次电针治疗结束后:与模型组相比,针刺对照组和保肝护脑针法组血清ALT、AST水平明显降低(P<0.01),同时血清CAT、肝组织CATmRNA显著升高(P<0.01);与针刺对照组相比,针刺保肝护脑组血清ALT、AST、CAT和肝组织CAT mRNA各项变化更为显著(P<0.05)。结论:针刺保肝护脑对脑缺血再灌注大鼠的治疗效果较单纯头穴针刺更为显著,其治疗机理与促进肝脏CATmRNA表达相关。