Studies on the Synthesis of GHK and eptifibatide

蛋白质是生物体内最重要的物质之一，而氨基酸序列较短的多肽虽然在生物体内含量很少，却能发挥巨大生理作用。由于生物提取材料来源困难,而基因技术运用在小分子肽上表达量低等问题,使化学法合成多肽独具优势。本论文分别采用液相法和固相法合成了具有药用价值的三肽GHK及八肽Eptifibatide，研究了多肽合成过程中缩合剂及纯化等问题。GHK是存在于人类血浆中的一种三肽，研究表明它能促进纤维原细胞，巨噬细胞等多种细胞及组织的生长。采用液相合成法合成了三肽GHK，对甘氨酸的氨基、组氨酸的咪唑基、赖氨酸的侧链氨基进行保护，得到中间体Boc-Gly、His(trt)和Lys(Boc)；接肽反应以DMF为反应溶剂...Peptide is a type of bioactive substance that participates in normal functioning of a living organism. Isolation and purification of the peptide from natural sources has not been very successful; the use of recombinant DNA techniques has a problem of lower yield; so, chemical synthesis of peptide in the laboratory appears to be an efficient method. In this thesis, the tripeptide GHK has been synth...学位：理学硕士院系专业：生命科学学院生物学系_细胞生物学学号：20042607

SHRSP.Z-Leprfa/IzmDmcr rats における24 時間血圧概日リズムの週齢変化についての基礎的検討

Twenty-four hour ambulatory blood pressure monitoring has focused on the incidence of hypertension-related end organ damage. This study intends to measure 24-hour blood pressure in SHRSP.Z-Leprfa/IzmDmcr rats（SHRSPZF）at the age of 12 and 20 weeks. This 24-hour blood pressure monitoring was conducted using a telemetry system. Each rat at 12 and 20 weeks of age was used for 24-hour blood pressure monitoring for 7 days. Twenty-four-hour systolic and diastolic blood pressures in 20-week-old SHRSPZF was significantly higher than in 12-week-old SHRSPZF, but the heart rate did not change between them. Systolic blood pressure standard deviation as a marker of short-term blood pressure variability in 20-week-old SHRSPZF was significantly increased than in 12-week-old SHRSPZF during night and day time. From these results, the short-term blood pressure variability in 24-hour ambulatory blood pressure of 20-week-old SHRSPZF was significantly higher than those in 12-week-old SHRSPZF possibly due to marked hypertension. The development of renal damage in SHRSPZF may be related to this short-term blood pressure variability change in SHRSPZF at the age of 20 weeks

浮世絵で見るイケメンと美女

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救急外来に常駐する薬剤師によるタスクシフティングの現状調査

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Analgesic overlapped therapy for acute pain after orthopedic surgery

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Practical Report on "Graduation Research" 2018

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St. Luke's Booklet 1

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Fmoc Solid-phase Synthesis and Purification of Eptifibatide

Eptifibatide是一种血小板糖蛋白GPⅡb/Ⅲa受体拮抗剂,临床研究结果显示其医用上的产业前景良好.采用Rink-Am-Resin树脂作为固相载体,Fmoc为保护策略固相合成了Eptifibatide.以DMF为反应溶剂,Piperidine-DMF脱去Fmoc保护基团,以TBTU/HOBt/DIEA作为肽键缩合试剂进行接肽反应,用TFA/EDT/TIS/H2O定量地从树脂上切除,制备型高效液相色谱分离纯化粗肽.同时对产品进行色谱分析和质谱鉴定.实验结果表明Fmoc合成策略中各步的缩合率均在95%以上,多数在99%以上.粗肽纯度为86.8%,产率为55%.分离纯化后的产物纯度达到98.5%,MOLDI-TOF质谱测得的m/z与理论值相符.为化学合成Eptifibatide及其分离纯化提供了一条切实可行的路线.Eptifibatide is the receptor antagonist of platelet glycoprotein GPⅡb/Ⅲa,Clinical study showed that it has the advantage of potent effect.In the present work,a strategy for the synthesis and purification of Eptifibatide was presented.Eptifibatide has been synthesized by solid-phase method using the base-labile Fmoc group for protecting the α-amino acid.The peptide was assembled on Rink-Am-Resin.DMF is used as the coupling solvent;Piperidine-DMF to removed the Fmoc group;TBTU/HOBt/DIEA as the activation system,and TFA/EDT/TIS/H_2O as the cleavage condition.The synthetic product was purified by prepared reversed-phase high performance liquid chromatography and identified on MALDI-TOF-MS and HPLC.The experimental result shows that the ratio of the coupling synthesis of each amino acid is over 95 %,most of them are over 99 %.After cleavage of peptide resin,the purity of rude Eptifibatide was about 86.8%,and the yield of it is 55 %.The final purity of our product was found more than(98.5)%.The molecular mass of the product is correspond to molecular mass of the Eptifibatide.This synthetic strategy is practicable for chemical synthesis and purification of Eptifibatide