Dasatinib_COA_11930_MedChemExpress
高效液相色谱法测定磺达肝癸钠注射液清洁验证残留物含量
高效液相色谱法测定磺达肝癸钠注射液清洁验证残留物含量发布时间：2021-01-13T14:11:07.717Z 来源：《医师在线》2020年9月18期作者：吴萍黄皆竣石小磊蒋红梅[导读] 采用高效液相色谱法测定磺达肝癸钠注射液清洁验证残留物含量吴萍黄皆竣石小磊蒋红梅（扬子江药业集团江苏紫龙药业有限公司；江苏常州213000）摘要目的：采用高效液相色谱法测定磺达肝癸钠注射液清洁验证残留物含量方法：色谱柱：Dionex CarboPacTM PA1预柱，Dionex CarboPacTM PA1色谱柱，4×250mm；柱温：25℃；1.0ml/min；检测波长：210nm；进样量：100μl；流动相：流动相A为二甲亚砜磷酸盐缓冲液溶液【1000ml磷酸盐缓冲液中加入约15±10μl二甲亚砜，如基线产生正相漂移，则增加二甲亚砜的用量，反之则减少二甲亚砜的用量，二甲亚砜的实际用量为5~25μl不等】；流动相B为2.0mol/L氯化钠磷酸盐缓冲液溶液【取0.210g磷酸二氢钠二水物和0.650g磷酸氢二钠二水物用水溶解，然后稀释至1000ml，用磷酸调节溶液pH约为7.3】。
结果：磺达肝癸钠注射液清洁验证残留物磺达肝癸钠在12.9088μg/ml -161.36μg/ml范围内线性关系良好，不锈钢板的平均回收率在70%，RSD值为18%。
结论：本方法稳定、简便、准确，灵敏度高，适用于磺达肝癸钠注射液清洁验证残留物的含量测定。
正文：磺达肝癸钠注射液，西药名。
为抗血栓形成药。
用于进行下肢重大骨科手术如髋关节骨折、重大膝关节手术或者髋关节置换术等患者，预防静脉血栓栓塞事件的发生等。
在药品生产过程中，为防止污染与交叉污染，需对涉及的生产设备进行清洁，为保证清洁的有效性，需对设备表面化学残留物进行检测，本文建立了高效液相色谱法测定磺达肝癸钠注射液清洁验证残留量。
1 仪器和试药Agilent Infinity II 生物惰性色谱仪磺达肝癸钠对照品（WSFS-191201，5.0425mg/ml）；二甲亚砜（20181205，99.8%）；磷酸二氢钠（20190116，99.0%）；磷酸氢二钠（20170401，99.0%）；氯化钠（K5072204913）；2 方法与结果2.1 溶液的配制2.1.1 对照品溶液的制备取磺达肝癸鈉对照品一支（标定浓度约5mg/ml），精密量取0.4ml，置25.0ml量瓶中，加水溶解并稀释至刻度，摇匀，作为对照品溶液。
Toceranib_SDS_MedChemExpress
Inhibitors, Agonists, Screening LibrariesSafety Data Sheet Revision Date:Jun.-08-2017Print Date:Jun.-08-20171. PRODUCT AND COMPANY IDENTIFICATION1.1 Product identifierProduct name :ToceranibCatalog No. :HY-10330CAS No. :356068-94-51.2 Relevant identified uses of the substance or mixture and uses advised againstIdentified uses :Laboratory chemicals, manufacture of substances.1.3 Details of the supplier of the safety data sheetCompany:MedChemExpress USATel:609-228-6898Fax:609-228-5909E-mail:sales@1.4 Emergency telephone numberEmergency Phone #:609-228-68982. HAZARDS IDENTIFICATION2.1 Classification of the substance or mixtureNot a hazardous substance or mixture.2.2 GHS Label elements, including precautionary statementsNot a hazardous substance or mixture.2.3 Other hazardsNone.3. COMPOSITION/INFORMATION ON INGREDIENTS3.1 SubstancesSynonyms:SU 11654; PHA 291639; SU11654; SU–11654; PHA–291639; PHA291639Formula:C22H25FN4O2Molecular Weight:396.46CAS No. :356068-94-54. FIRST AID MEASURES4.1 Description of first aid measuresEye contactRemove any contact lenses, locate eye-wash station, and flush eyes immediately with large amounts of water. Separate eyelids with fingers to ensure adequate flushing. Promptly call a physician.Skin contactRinse skin thoroughly with large amounts of water. Remove contaminated clothing and shoes and call a physician.InhalationImmediately relocate self or casualty to fresh air. If breathing is difficult, give cardiopulmonary resuscitation (CPR). Avoid mouth-to-mouth resuscitation.IngestionWash out mouth with water; Do NOT induce vomiting; call a physician.4.2 Most important symptoms and effects, both acute and delayedThe most important known symptoms and effects are described in the labelling (see section 2.2).4.3 Indication of any immediate medical attention and special treatment neededTreat symptomatically.5. FIRE FIGHTING MEASURES5.1 Extinguishing mediaSuitable extinguishing mediaUse water spray, dry chemical, foam, and carbon dioxide fire extinguisher.5.2 Special hazards arising from the substance or mixtureDuring combustion, may emit irritant fumes.5.3 Advice for firefightersWear self-contained breathing apparatus and protective clothing.6. ACCIDENTAL RELEASE MEASURES6.1 Personal precautions, protective equipment and emergency proceduresUse full personal protective equipment. Avoid breathing vapors, mist, dust or gas. Ensure adequate ventilation. Evacuate personnel to safe areas.Refer to protective measures listed in sections 8.6.2 Environmental precautionsTry to prevent further leakage or spillage. Keep the product away from drains or water courses.6.3 Methods and materials for containment and cleaning upAbsorb solutions with finely-powdered liquid-binding material (diatomite, universal binders); Decontaminate surfaces and equipment by scrubbing with alcohol; Dispose of contaminated material according to Section 13.7. HANDLING AND STORAGE7.1 Precautions for safe handlingAvoid inhalation, contact with eyes and skin. Avoid dust and aerosol formation. Use only in areas with appropriate exhaust ventilation.7.2 Conditions for safe storage, including any incompatibilitiesKeep container tightly sealed in cool, well-ventilated area. Keep away from direct sunlight and sources of ignition.Recommended storage temperature:Powder-20°C 3 years4°C 2 yearsIn solvent-80°C 6 months-20°C 1 monthShipping at room temperature if less than 2 weeks.7.3 Specific end use(s)No data available.8. EXPOSURE CONTROLS/PERSONAL PROTECTION8.1 Control parametersComponents with workplace control parametersThis product contains no substances with occupational exposure limit values.8.2 Exposure controlsEngineering controlsEnsure adequate ventilation. Provide accessible safety shower and eye wash station.Personal protective equipmentEye protection Safety goggles with side-shields.Hand protection Protective gloves.Skin and body protection Impervious clothing.Respiratory protection Suitable respirator.Environmental exposure controls Keep the product away from drains, water courses or the soil. Cleanspillages in a safe way as soon as possible.9. PHYSICAL AND CHEMICAL PROPERTIES9.1 Information on basic physical and chemical propertiesAppearance Light yellow to yellow (Solid)Odor No data availableOdor threshold No data availablepH No data availableMelting/freezing point No data availableBoiling point/range No data availableFlash point No data availableEvaporation rate No data availableFlammability (solid, gas)No data availableUpper/lower flammability or explosive limits No data availableVapor pressure No data availableVapor density No data availableRelative density No data availableWater Solubility No data availablePartition coefficient No data availableAuto-ignition temperature No data availableDecomposition temperature No data availableViscosity No data availableExplosive properties No data availableOxidizing properties No data available9.2 Other safety informationNo data available.10. STABILITY AND REACTIVITY10.1 ReactivityNo data available.10.2 Chemical stabilityStable under recommended storage conditions.10.3 Possibility of hazardous reactionsNo data available.10.4 Conditions to avoidNo data available.10.5 Incompatible materialsStrong acids/alkalis, strong oxidising/reducing agents.10.6 Hazardous decomposition productsUnder fire conditions, may decompose and emit toxic fumes.Other decomposition products - no data available.11.TOXICOLOGICAL INFORMATION11.1 Information on toxicological effectsAcute toxicityClassified based on available data. For more details, see section 2Skin corrosion/irritationClassified based on available data. For more details, see section 2Serious eye damage/irritationClassified based on available data. For more details, see section 2Respiratory or skin sensitizationClassified based on available data. For more details, see section 2Germ cell mutagenicityClassified based on available data. For more details, see section 2CarcinogenicityIARC: No component of this product present at a level equal to or greater than 0.1% is identified as probable, possible or confirmed human carcinogen by IARC.ACGIH: No component of this product present at a level equal to or greater than 0.1% is identified as a potential or confirmed carcinogen by ACGIH.NTP: No component of this product present at a level equal to or greater than 0.1% is identified as a anticipated or confirmed carcinogen by NTP.OSHA: No component of this product present at a level equal to or greater than 0.1% is identified as a potential or confirmed carcinogen by OSHA.Reproductive toxicityClassified based on available data. For more details, see section 2Specific target organ toxicity - single exposureClassified based on available data. For more details, see section 2Specific target organ toxicity - repeated exposureClassified based on available data. For more details, see section 2Aspiration hazardClassified based on available data. For more details, see section 212. ECOLOGICAL INFORMATION12.1 ToxicityNo data available.12.2 Persistence and degradabilityNo data available.12.3 Bioaccumlative potentialNo data available.12.4 Mobility in soilNo data available.12.5 Results of PBT and vPvB assessmentPBT/vPvB assessment unavailable as chemical safety assessment not required or not conducted.12.6 Other adverse effectsNo data available.13. DISPOSAL CONSIDERATIONS13.1 Waste treatment methodsProductDispose substance in accordance with prevailing country, federal, state and local regulations.Contaminated packagingConduct recycling or disposal in accordance with prevailing country, federal, state and local regulations.14. TRANSPORT INFORMATIONDOT (US)This substance is considered to be non-hazardous for transport.IMDGThis substance is considered to be non-hazardous for transport.IATAThis substance is considered to be non-hazardous for transport.15. REGULATORY INFORMATIONSARA 302 Components:No chemicals in this material are subject to the reporting requirements of SARA Title III, Section 302.SARA 313 Components:This material does not contain any chemical components with known CAS numbers that exceed the threshold (De Minimis) reporting levels established by SARA Title III, Section 313.SARA 311/312 Hazards:No SARA Hazards.Massachusetts Right To Know Components:No components are subject to the Massachusetts Right to Know Act.Pennsylvania Right To Know Components:No components are subject to the Pennsylvania Right to Know Act.New Jersey Right To Know Components:No components are subject to the New Jersey Right to Know Act.California Prop. 65 Components:This product does not contain any chemicals known to State of California to cause cancer, birth defects, or anyother reproductive harm.16. OTHER INFORMATIONCopyright 2017 MedChemExpress. The above information is correct to the best of our present knowledge but does not purport to be all inclusive and should be used only as a guide. The product is for research use only and for experienced personnel. It must only be handled by suitably qualified experienced scientists in appropriately equipped and authorized facilities. The burden of safe use of this material rests entirely with the user. MedChemExpress disclaims all liability for any damage resulting from handling or from contact with this product.Caution: Product has not been fully validated for medical applications. For research use only.Tel: 609-228-6898 Fax: 609-228-5909 E-mail: tech@Address: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA。
Dasatinib_hydrochloride_DataSheet_MedChemExpress
Inhibitors, Agonists, Screening Libraries Data SheetBIOLOGICAL ACTIVITY:Dasatinib hydrochloride is a potent and dual Abl WT /Src inhibitor IC 50 of 0.6 nM/0.8 nM respectively; also inhibits c–Kit WT /c–Kit D816V with IC 50 of 79 nM/37 nM.IC50 & Target: IC50: 0.6 nM/0.8 nM (Abl WT /Src)[1]IC50: 79 nM/37 nM (c–Kit WT /c–Kit D816V )[2]In Vitro: Dasatinib potently inhibits wild–type Abl kinase and all mutants except T315I over a narrow range (IC 50≤1.7 nM). Dasatinib (IC 50: 0.8 nM) displays 325–fold greater potency compared with Imatinib against cells expressing wild–type Bcr–Abl in Ba/F3 cells [1].In Vivo: Daily treatment with Dasatinib (50 mg/kg) is initiated on day 10. Using this approach, a significant inhibition of BCPAP orthotopic tumor growth is observed 6 days after treatment (day 16, P=0.014), which is sustained through days 23 and 29(P=0.0003), compared with vehicle–treated mice [3]. Metabolism studies of Dasatinib (50 mg/kg) in rat suggested that Dasatinib is the major circulating component, whereas multiple metabolites contributed to the remaining 40–60% of the sample radioactivity at 4 h post dose [4].PROTOCOL (Extracted from published papers and Only for reference)Kinase Assay:[1]Kinase assays using wild–type and mutant glutathione S–transferase (GST)–Abl fusion proteins (c–Abl amino acids 220–498) are done with minor alterations. GST–Abl fusion proteins are released from glutathione–Sepharose beads before use; the concentration of ATP is 5 μM. Immediately before use in kinase autophosphorylation and in vitro peptide substrate phosphorylation assays, GST–Abl kinase domain fusion proteins are treated with LAR tyrosine phosphatase. After 1–hour incubation at 30°C, LAR phosphatase is inactivated by addition of sodium vanadate (1 mM). Immunoblot analysis comparing untreated GST–Abl kinase to dephosphorylated GST–Abl kinase is routinely done using phosphotyrosine–specific antibody 4G10 to confirm complete (>95%)dephosphorylation of tyrosine residues and c–Abl antibody CST 2862 to confirm equal loading of GST–Abl kinase. The inhibitor concentration ranges for IC 50 determinations are 0 to 5,000 nM (Imatinib and AMN107) or 0 to 32 nM (Dasatinib). The Dasatinib concentration range is extended to 1,000 nM for mutant T315I. These same inhibitor concentrations are used for the in vitro peptide substrate phosphorylation assays. The three inhibitors are tested over these same concentration ranges against GST–Src kinase and GST–Lyn kinase.Cell Assay: Dasatinib is dissolved in DMSO (10 mM) and stored, and then diluted with appropriate media before use [1].[1]Ba/F3 cell lines are plated in triplicate and incubated with escalating concentrations of Imatinib, AMN107, or Dasatinib for 72 hours.Proliferation is measured using a methanethiosulfonate–based viability assay (CellTiter96 Aqueous One Solution Reagent). IC 50 and IC 90 values are reported as the mean of three independent experiments done in quadruplicate. The inhibitor concentration ranges for IC 50 and IC 90determinations are 0 to 2,000 nM (Imatinib and AMN107) or 0 to 32 nM (Dasatinib). The imatinibconcentration range is extended to 6,400 nM for mutants with IC 50>2,000 nM. The Dasatinib concentration range is extended to 200Product Name:Dasatinib (hydrochloride)Cat. No.:HY-10181A CAS No.:854001-07-3Molecular Formula:C 22H 27Cl 2N 7O 2S Molecular Weight:524.47Target:Src; Bcr–Abl; Autophagy Pathway:Protein Tyrosine Kinase/RTK; Protein Tyrosine Kinase/RTK;Autophagy Solubility:DMSO: 15 mg/mLnM for mutant T315I.Animal Administration: Dasatinib is prepared in 80 mM sodium citrate buffer, pH 3.0 (Mice)[3].Dasatinib is prepared in 0.5% methylcellulose (Rat)[4].[3][4]Mice[3]Male athymic nude mice (25 grams; 5–week old) are used. Dasatinib (50 mg/kg) is prepared for daily oral gavage (5 d/wk) in 80 mM sodium citrate buffer, pH 3.0. For the orthotopic murine model, mice are randomized on day 10 based on bioluminescence activity to receive drug or vehicle. In the metastatic murine model, mice receives dasatinib or vehicle, as described earlier, starting 2 days before intracardiac injection (pretreatment), or on day 11 following randomization (posttreatment).Rat[4]Dasatinib is dosed to male Wistar–Han (WH) rats at 50 mg/kg orally in 0.5% methylcellulose. The automated rat blood collection device is programmed to collect 200 μL of blood at predetermined intervals. At each time point, the accusampler is programmed to directly spot 20 μL of blood twice (two spots) onto the DBS card. The remaining 160 μL of liquid blood is collected into sodium EDTA–containing tubes. Plasma samples are obtained after immediate centrifugation of blood at 11,000 rpm for 5 min. The plasma samples are stored at -80°C until analyses. The DBS samples are dried under room temperature for a minimum of 2 h and stored in a plastic bag in the dessicator until sample analysis.References:[1]. O'Hare T, et al. In vitro activity of Bcr–Abl inhibitors AMN107 and BMS–354825 against clinically relevant imatinib–resistant Abl kinase domain mutants. Cancer Res. 2005 Jun 1;65(11):4500–5.[2]. Shah NP, et al. Dasatinib (BMS–354825) inhibits KITD816V, an imatinib–resistant activating mutation that triggers neoplastic growth in most patients with systemic mastocytosis. Blood. 2006 Jul 1;108(1):286–91.[3]. Chan CM, et al. Targeted inhibition of Src kinase with dasatinib blocks thyroid cancer growth and metastasis. Clin Cancer Res. 2012 Jul 1;18(13):3580–91.[4]. Shen Z, et al. Metabolite profiling of dasatinib dosed to Wistar Han rats using automated dried blood spot collection. J Pharm Biomed Anal. 2012Aug–Sep;67–68:92–7.Caution: Product has not been fully validated for medical applications. For research use only.Tel: 609-228-6898 Fax: 609-228-5909 E-mail: tech@Address: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA。
BCA蛋白浓度测定试剂盒
BCA蛋白浓度测定试剂盒产品编号产品名称包装价格P0012 BCA蛋白浓度测定试剂盒 500次 258.00 元O 碧云天生产的BCA蛋白浓度测定试剂盒是根据目前世界上最常用的两种蛋白浓度检测方法之一BCA法研制而成，实现了蛋白浓度测定的简单，高稳定性，高灵敏度和高兼容性。
O 灵敏度高，检测浓度下限达到25微克/毫升，最小检测蛋白量达到0.5微克，待测样品体积为1-20微升。
O 在50-2000微克/毫升浓度范围内有较好的线性关系。
O BCA法测定蛋白浓度不受绝大部分样品中的化学物质的影响，可以兼容样品中高达5%的SDS，5%的Triton X-100，5%的Tween20, 60, 80。
但受螯合剂和略高浓度的还原剂的影响，需确保EDTA低于10mM，无EGTA，二硫苏糖醇低于1mM，β-巯基乙醇低于1mM。
不适用BCA法时建议使用碧云天Bradford蛋白浓度测定试剂盒。
O BCA蛋白浓度测定试剂盒对样品中各种物质详细的兼容性表，参见BCA蛋白浓度测定兼容性表。
O 每个试剂盒可以检测500个样品。
包装清单:BCA试剂 A 100 mlBCA试剂 B 3 ml蛋白标准(5mg/ml BSA) 1 ml说明书 1 份保存条件:BCA试剂A和B室温保存，蛋白标准请-20?冻存。
本试剂盒自订购之日起一年注意事项: O 需酶标仪一台，测定波长为540-595nm之间，562nm最佳。
需96孔板。
如果没有酶标仪，也可以使用普通的分光光度计测定，但是测定蛋白浓度时，需根据测定吸光度的杯子的体积，按比例调整A液,B液和样品的体积。
使用分光光度计测定蛋白浓度时，每个试剂盒可以测定的样品数量可能会显著减少。
O 如发现样品稀释液或裂解液本身就有较高背景，请试用Bradford蛋白浓度测定试剂盒。
O 为了加快BCA法测定蛋白浓度的速度可以适当用微波炉加热，但是切勿过热。
O EDTA浓度必需小于10mM，不兼容EGTA。
以肽为基础的治疗动脉粥样硬化的免疫疗法,和以肽为基础的用于确
专利名称：以肽为基础的治疗动脉粥样硬化的免疫疗法，和以肽为基础的用于确定针对氧化低密度脂蛋白的免疫
反应的检测方法
专利类型：发明专利
发明人：扬·尼尔森,普里迪曼·K·沙赫
申请号：CN200910009565.5
申请日：20020405
公开号：CN101486766A
公开日：
20090722
专利内容由知识产权出版社提供
摘要：本发明涉及载脂蛋白B的片段，特别是由所述片段确定的肽，用于免疫治疗或治疗包括人类在内的哺乳动物所发生的缺血性心血管疾病，以及在ELISA(酶联免疫吸附试验)中使用一种或多种所述肽以确定是否存在与缺血性心血管疾病发生危险性升高或降低有关的抗体。
申请人：南方佛斯卡专利公司,赛达斯西奈医疗中心
地址：瑞典兰德市伊隆
国籍：SE
代理机构：北京中原华和知识产权代理有限责任公司
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美洲大蠊抗肝纤维化活性提取物ML-D中粘多糖的含量测定
ｆ ｒ ｏ ｍ Ｐ ｅ ｒ ｉ ｐｌ ａ ｎ ｅ ｔ ａ ａ ｍｅ ｒ ｉ ｃ ａ ｉ ｒ ａ ．Ｍ ｅ ｔ ｈ ｏ ｄ ｓ ：Ｐ ｈ ｅ ｎ ｏ ｌ — ｖ ｉ ｔ ｉ ｒ ｏ ｌ ｃ ｏ ｌ ｏ ｒ ｉ ｍｅ ｔ ｙ ｒ ｗａ ｓ ｕ ｓ ｅ ｄ ｆ ｏ ｒ ｄ ｅ ｔ ｅ ｍｉ ｒ ｎ ｉ ｎ ｇ ｃ ｏ ｎ ｔ ｅ ｎ ｔ ｏ ｆ ｙ ｃ ｏ ｓ ａ ｍｉ ｎ ｏ ｙ ｃ ａ ｎ ；ｏ ｒ ｔ ｈ ｏ ｇ ｏ ｎ ａ ｌ
美洲大蠊抗肝纤维化活性提取物Ｍ Ｌ — Ｄ 中粘多糖的含量测定
李夸巧 ， 李春艳 ， 杨 永寿 ， 陈丽娜 ， 肖培云
（ 大理 学院 药学与 化 学 学院 ， 云 南 大理 ６ ７ １ ０ ０ ０ ）
［ 摘要 ］目的 ： 建立美洲大蠊抗肝纤维化活性提 取物ＭＬ — Ｄ中粘 多糖的含量测定方法 。方法 ： 采用苯酚一 硫酸法测定粘多糖的含 量， 采用 正交试验设计考察ＭＬ — Ｄ中粘 多糖 的水解工 艺和 显色条件 ， 采用单 因素试验考察加热显色时间、 苯酚和硫酸的用量。结
ｄ ｅ ｓ ｉ ｇ ｎ ｋ（ ３ ４ ） ｗ ａ ｓ ａ ｄ ｏ ｐ ｔ ｅ ｄ ｔ ｏ ｉ ｎ ｖ ｅ ｓ ｔ ｉ ｇ ａ ｔ ｅ ｈ ｙ ｄ ｒ ｏ ｌ ｙ ｓ ｉ ｓ ｐ ｒ ｏ ｃ ｅ ｓ ｓ ｏ ｆ ｌ ｇ ｙ ｃ ｏ ｓ ａ ｍｉ ｎ ｏ ｇ ｌ ｙ ｃ ａ ｎ ｉ ｎ ＭＬ — Ｄ ； ｓ ｉ ｎ ｇ ｌ ｅ ｆ ａ ｃ ｔ ｏ ｒ ｅ ｘ ｐ ｅ ｉ ｒ ｍ ｅ ｎ ｔ ｗ ａ ｓ ｕ ｓ ｅ ｄ ｔ ｏ ｉ ｎ ｖ ｅ ｓ ｔ ｉ ｇ ａ ｔ ｅ
乙酰胆碱酯酶抑制剂
上海应用技术学院研究生课程《高等天然产物化学》试卷2014 / 2015 学年第1 学期课程代码：NX0702013论文题目：乙酰胆碱酯酶抑制剂的研究进展姓名：芮银146061414康满满146061409专业：制药工程学院：化工学院乙酰胆碱酯酶抑制剂的研究进展芮银，陈祎桐，康满满摘要：本文阐述了乙酰胆碱酯酶抑制剂(AChEI)的研究进展，介绍了用于药物治疗的乙酰胆碱酯酶抑制剂的各种来源如植物、微生物等，及其抑制乙酰胆碱的活性物质。
在此基础上，总结了几种现代分析技术，对AChEIs进行筛选，大大加快AD药物资源的开发利用进程。
这些方法主要有基于比色法的Ellman's法及相关的改进方法、薄层显色法、荧光显色法、电喷雾质谱法等。
但是，到目前为止，现代分析技术在AD药物资源中的应用还处在起步阶段。
关键词：乙酰胆碱酯酶抑制剂，筛选方法，薄层显色法，荧光显色法The progress of acetylcholinesteraseinhibitorsRui Yin, Chen Yitong, Kang ManmanAbstract：In this artical, the research elaborates progress of acetylcholinesterase inhibitors (AChEI), and introduces a variety of sources for drug treatment acetylcholinesterase inhibitors such as plants, microorganisms, and its active ingredients. On this basis, the review summarizes several modern analytic techniques such as Ellman's method which based on the colorimetric method, TLC chromogenic method, fluorescent color method, Electrospray ionization mass spectrometry and so on. However, at present, the application of modern analytic techniques in AD drug resources is still in infancy.Key word: Acetylcholinesterase inhibitors, Screening Methods, TLC chromogenic method, Fluorescent color method目录摘要.................................................................................................错误!未定义书签。
HPLC法测定达沙替尼含量及有关物质_黄玉
样，记录色谱图，依外标法计算（ 见表 2） 。精密称取达沙替尼 原料药适量，用缓冲液溶解配制成浓度为 200μg·mL － 1 的供 试品溶液； 精密移取供试品溶液适量，同法制得 2μg·mL － 1 的
对照品溶液。取对照品溶液进样，记录色谱图，调节检测灵敏
度使得 1 峰峰高约为满量程的 20% 。取供试品溶液进样，记
·药品检验与分析·
海峡药学 2013 年 第 25 卷 第 7 期
HPLC 法测定达沙替尼含量及有关物质
黄 玉，吕 华，陈建秋，严拯宇（ 中国药科大学分析化学教研室 南京 211198）
摘要： 目的 高效液相色谱法测定达沙替尼原料药的含量及其有关物质。方法 采用 YMC Pack Pro C18 色谱柱，以流动相 A〔50mM 醋酸铵溶
在 5 ～ 50μg·mL － 1 的浓度范围内线性关系良好。
2. 6 精 密 度、重 复 性 与 稳 定
性试验 取达沙替尼对照品
溶液，重 复 进 样 6 次，记 录 色
谱图，计算其峰面积的 ＲSD 为
0. 22% 。精密称取同批样品 6
图2
份，分别按 2. 1 项方法配制供
试品溶 液，进 样 测 定，按 外 标
图 1 达沙替尼和个中间体混合溶液的 HPLC 色谱图 1 达沙替尼 2 中间体Ⅰ 3 中间体Ⅱ 4 中间体Ⅲ
2. 4 专属性实验 将达沙替尼样品分别在强酸、强碱、高温、 强光照射和强氧化剂氧化破坏等情况下进行破坏，用溶剂定 容，制成 200μg·mL － 1 的溶液。然后分别进样，记录色谱图， 结果显示，达沙替尼对酸、碱、高温、光照均较稳定，氧化破坏 降解出一些杂质，各降解产物分离良好（ 见图 2） 。 2. 5 线 性 试 验 取 达 沙 替 尼 对 照 品 5mg，精 密 称 定。置 50mL 容量瓶中，用缓冲液溶解并定容，制得 100μg·mL － 1 的 对照品贮备液； 分别精密量取储备液 0. 5、1、2、3、4、5mL，各置 10mL 容量瓶中，用缓冲液定容，制得浓度为 5、10、20、30、40、 50μg·mL － 1 的系列浓度对照品溶液，分别进样，以浓度 c 为 横坐标，峰面积 A 为纵坐标，进行线性回归，得回归方程： A = 3. 9413 × 104 c + 3. 1547 × 104 ，r = 0. 9999。结果表明达沙替尼
生物科技-阿卡宁衍生物合成产物中乙酰胆碱酯酶抑制剂的筛选阿卡宁衍 精品
阿卡宁衍生物合成产物中乙酰胆碱酯酶抑制剂的筛选左娜娜马志玲*(中山大学化学学院分析化学研究所，广州，510275)摘要本文以合成得到的乙酰胆碱酯酶抑制剂混合物为研究对象，通过紫外分光光度法检测出混合物是否具有活性，进一步通过高效薄层色谱法（HPTLC）确定活性物质的个数以及位置，接着通过液相－质谱（LC-MS）联用等方法对活性物质定性分析。
混合物体系，通过本实验的方法，不经分离提纯即可测定各种化合物是否具有抑制能力以及抑制活力的大小，包括各种副产物，因而可以获得合成体系中有关抑制剂的最大的信息量。
关键词乙酰胆碱酯酶抑制剂筛选1 前言阿尔茨海默病（Alzheimer’s，AD）是一种多发生于老年人中的缓慢进行性、智能衰退性疾病，俗称老年性痴呆病。
AD的关键性症状主要是由胆碱能功能障碍所引起的，治疗AD 病的主要途径是寻找新的中枢拟胆碱药，乙酰胆碱酯酶抑制剂就是其中的一类治疗药物。
传统的药物筛选方法是定向合成再定向筛选，即首先通过化学预试寻找到药物先导物，接下来设计合成路线，对产物进行分离纯化，最后检验活性。
传统筛选方法有两个主要缺陷，一是传统活检只能应用于纯品，该方法只适用于易分离体系，对难分离混合物体系暂时没有解决办法；二是传统定向合成只关注主合成产物，无视副产物也可能会有活性等信息。
而在本方法中，合成产物不需经过分离和纯化，可以直接筛选出活性物质并对其定性。
本文以合成得到的乙酰胆碱酯酶抑制剂混合物为研究对象，通过紫外分光光度法检测出混合物是否具有活性，进一步通过高效薄层色谱法（HPTLC）确定活性物质的个数以及位置，接着通过高效液相色谱法（HPLC）以及液相－质谱（LC-MS）联用等方法对活性物质定性分析。
这种筛选方法，克服了传统筛选方法的弊端，讲求整体性，对任意的合成体系，可以判断出产物是否具有活性、活性物质的位置以及活性物质的结构，这对药物筛选有重要的指导意义。
基金项目：中山大学化学与化工学院第五届创新化学实验与研究基金项目资助第一作者左娜娜，女，中山大学化学与化工学院应用化学专业2001级指导老师马志玲，中山大学化学院，副教授，Email：cesmzl@.2实验部分2.1抑制剂混合物体系的合成反应步骤如下：在两个50ml圆底烧瓶中，分别加入50mg原料和5ml甲醇，搅拌溶解；分别加入2-氨基吡啶和2-氨基代苯骈噻唑50mg；室温状态下搅拌72h；用薄层色谱法监测反应的进行程度，必要时加入催化剂硼酸（催化量）；反应结束后，用氮气把溶剂吹干，再用三氯甲烷溶解；转入分液漏斗中，用水洗两次，每次5ml。
丝裂霉素C白蛋白磁性微球用于裸鼠人肝癌模型疗效观察
丝裂霉素C白蛋白磁性微球用于裸鼠人肝癌模型疗效观察干育红;张宁杲
【期刊名称】《中国肿瘤临床》
【年(卷),期】1998(025)009
【摘要】观察了自制丝裂霉素白蛋白磁性微球用于裸鼠人肝癌模型的疗效。
结果显示：ＭＭＣ白蛋白磁性微球不仅是安全的，而且在体外磁场作用下可较长时间内沉积于靶区。
分组试验显示：治疗组肿瘤体积缩小，与生理盐水对照组和ＭＭＣ对照组具有显著性差异；治疗组平均生存时间比上述两组对照组明显延长。
【总页数】3页(P675-677)
【作者】干育红;张宁杲
【作者单位】上海医科大学附属中山医院肝癌研究所;上海医科大学附属中山医院肝癌研究所
【正文语种】中文
【中图分类】R735.705
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2.索拉非尼对Bel-7402细胞裸鼠移植性肝癌模型的疗效观察 [J], 牛凯;成宇晶
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4.^(131)I-抗HBxAg人/鼠嵌合抗体在裸鼠人肝癌模型定位的初步研究 [J], 龚奕;
刘康达;周铬;薛琼;陈绍亮;汤钊猷
5.抗人AFP－R－LCA McAb在裸鼠人肝癌模型中放免显像及治疗 [J], 刘扬;吴孟超;钱光相;张柏和;陈传松
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乙酰肝素酶、硫酸乙酰肝素和多配体蛋白聚糖-1在肺癌患者血清中的表达及诊断价值
乙酰肝素酶、硫酸乙酰肝素和多配体蛋白聚糖-1在肺癌患者
血清中的表达及诊断价值
李涛;高萌;翟乃亮
【期刊名称】《滨州医学院学报》
【年(卷),期】2024(47)2
【摘要】目的探讨多配体蛋白聚糖-1(SDC-1)、硫酸乙酰肝素(HS)以及乙酰肝素
酶(HPA)在非小细胞肺癌(NSCLC)及小细胞肺癌(SCLC)患者血清中的水平及其对诊断及预后的预测价值。
方法收集10例健康对照组及76例肺癌患者的血清标本,通过ELISA方法检测血清中HS、SDC-1、HPA表达水平。
采用Mann-Whitney U 检验进行组间比较。
结果肺癌患者血清HS、SDC-1及HPA含量均高于健康对照
组(P<0.05);HS、HPA单因素用于诊断肺癌时的AUC分别为0.819和0.930,HS、SDC-1、HPA三者联合诊断肺癌时AUC为0.974。
结论HS、SDC-1、HPA三者联合检测对肺癌的诊断及预后具有较好的预测价值。
【总页数】4页(P122-125)
【作者】李涛;高萌;翟乃亮
【作者单位】滨州医学院附属医院呼吸与危重症医学科;烟台山医院呼吸与危重症
医学科
【正文语种】中文
【中图分类】R734.2
【相关文献】
1.硫酸乙酰肝素蛋白聚糖与增殖诱导配体在肺癌中的相关性研究
2.中老年卵巢癌患者硫酸乙酰肝素蛋白聚糖-1表达水平及与预后的关系
3.阿托伐他汀对大鼠心肌缺血再灌注损伤后硫酸乙酰肝素蛋白聚糖和多配体蛋白聚糖的干预作用
4.多配体蛋白聚糖-1/乙酰肝素酶轴在子宫腺肌病发生发展中的临床意义
5.乙酰肝素酶与多配体蛋白聚糖-1在恶性肿瘤中的研究进展
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