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中国化学快报（英文版）
中国化学快报（英文版）

梁晓天

月刊

1001-8417

cclbj@imm.ac.cn

010-63165638

100050

北京市先农坛街1号

中国化学快报（英文版）/Journal Chinese Chemical LettersCSCDCSTPCD北大核心SCI
查看更多>>本刊是由中国科协主管、中国化学会主办、中国医学科学院药物所承办的学术期刊，是由著名化学家梁晓天院士主编。是中国化学界通向世界的窗口，内容覆盖化学全领域。本刊的办刊宗旨是“新、快、准”，我们将坚持这个宗旨，力求及时反映化学研究中各个相关领域内的最新进展及热点问题，主要读者群是科研人员、研究生、大学教师。现已被国内外多家数据库收录，如SCI　Search、Chemical Abstract、Research Alert、Chemistry Citation Index、《日本科技文献速报》、万方数据数字化期刊群、中国学术期刊过刊全文数据库、中国学术期刊（光盘版）、中国学术期刊文摘、中文期刊全文数据库、俄罗斯Рж期刊源等。
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    CoFe2O4 decorated graphene/C18-functionalized mesoporous silica nanocomposites prepared for magnetic enrichment and electrochemical detection of promethazine in beef

    Xingdong YangShi-Ming YingSen ZhangJinxia Dai...
    208-213页
    查看更多>>摘要：Promethazine(PHZ)is used as a sedative in veterinary medicine,and its residue can threaten the health of human.The electrochemical detection of PHZ is suitable method for application in the field.However,the traditional electroanalysis is difficult to perform directly in meat samples due to matrix interfer-ence.This work integrates magnetic solid-phase extraction and differential pulse voltammetry for highly sensitive and selective determination of PHZ in beef and beef liver for the first time.CoFe2O4/graphene coated with C18-functionalized mesoporous silica(MG@mSiO2-C18)is synthesized as dispersed magnetic adsorbent to extract PHZ.Magnetic glassy carbon electrode modified with nitrogen-doped hollow carbon microspheres(HCM)attracts the MG@mSiO2-C18 with PHZ,and directly detects the PHZ without elution procedure.MG@mSiO2-C18 can separate PHZ to avoid the interference of impurities on following detec-tion,and also concentrate PHZ on magnetic electrode.Additionally,the electrode modification with HCM can amplify the electrochemical signal of PHZ.Finally,the integrated PHZ determination method exhibits a wide linear range from 0.08 μmol/L to 300 μmol/L with a low limit of detection of 9.8 nmol/L.The beef sample analysis presents excellent recovery,demonstrating that this protocol is promising for the rapid and onsite detection of PHZ in real meat samples
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    Rationally designed synthetic peptide as versatile calibrant to improve the accuracy of protein sequence analysis using MALDI mass spectrometry

    Lingpeng ZhanYanyi HuangGuanbo Wang
    214-220页
    查看更多>>摘要：Matrix-assisted laser desorption/ionization(MALDI)mass spectrometry(MS)plays an indispensable role in analyzing protein covalent structures.The reliable identification of amino acid residues and modifi-cations relies on the mass accuracy,which is highly dependent on calibration.However,the accuracy provided by the currently available calibrants still needs further improvement in terms of compatibility with multiple tandem MS modes or ion polarity modes,calibratable range,and minimizing suppression of and interference with analyte signals.Here aiming at developing a versatile calibrant to solve these problem,we designed a synthetic peptide format of calibrant Rx(GDPn)m(referred to as"Gly-Asp-Pro,GDP")according to the chemical natures of amino acids and polypeptide fragmentation rules in tandem MS.With four types of amino acid residues selected and arranged through rational designs,a GDP pep-tide produces highly regulated fragments that give rise to evenly spaced signals in each tandem MS mode and is compatible with both positive and negative ion modes.In internal calibration,its regulated frag-mentation pattern minimizes interference with analyte signals,and using a single peptide as the input minimizes suppression of the analyte signals.As demonstrated by analyses of proteins including mono-clonal antibody and Aβ-42,these features allowed significant increase of the mass accuracy and precision,which improved sequence coverage and sequence resolution in sequence analyses(including de novo se-quencing).This rational design strategy may also inspire further development of synthetic calibrants that benefit structural analysis of biomolecules.
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    Resolving the geometric structure of trastuzumab by mobility capillary electrophoresis and native mass spectrometry

    Wenjing ZhangJie HongLei YangZuqiang Xu...
    221-225页
    查看更多>>摘要：Available online Immunoglobulins G(IgGs)are Y-shaped globular proteins,however,their high flexibility and heterogeneity pose great challenges to their structure and conformation determinations.Geometric structure of IgG closely correlates to its biofunctions,such as the antibody escape of human immun-odeficiency virus(HIV)could attribute to the distance mismatch between the ends of two Fab arms(antigen-binding sites)and envelope glycoprotein spikes on virion surface.Herein,we report the first use of mobility capillary electrophoresis(MCE)and native mass spectrometry(nMS)to resolve the in-ternal geometric structure and conformation of an IgG(trastuzumab)in solution phase.After proteoly-sis,the ellipsoid dimensions of IgG and its subunits were measured by MCE-nMS experiments.IgG was then reconstructed,in which the sizes and relative positions of these three subunits in three-dimensional space were characterized.It was found that the two Fab arms have an angle of～102.1° and a distance of～11.0 nm between the two antigen-binding sites under native condition,and the Fc arm was tilted～16.0° towards one of the Fab arms.Fc was not on the plane of Fab-Fab,but has an angle of no larger than 103.1°.Under acidic environment(pH 3.0),each subunit of the IgG would unfold into larger di-mensions,and the angles between these subunits also change.With great potential for tumor imaging and therapy,the structure of F(ab')2 fragments was also measured and validated by molecular dynamic simulation.It was found that the electrostatic force among these three subunits and steric hindrance stemming from Fc help maintaining the angle between two Fab arms.
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    TCP-1,a novel peptide to diagnose early colon cancer

    Hang YuBaoying WenMin HuangRu Feng...
    226-233页
    查看更多>>摘要：A nine cyclic peptide(TCP-1)showed excellent specificity for colon cancer.TCP-1 binds with human tu-mor tissues at early stages and mice tumor with diameters of 1-4 mm,suggesting that TCP-1 may be used for early diagnosis of colon cancer.The mechanism of the targeted binding of TCP-1 to colon cancer was also studied using immunoprecipitation,LC-MS and bioinformatics.After screening and identifying of the possible binding target proteins of TCP-1,keratin,type Ⅱ cytoskeletal 5 was speculated to be the specific binding target protein of TCP-1 in human tumor tissue.Pharmacokinetics studies were conducted to investigate the target-mediated drug disposition of the new tumor-specific peptide by LC-MS/MS.The tissue distribution study showed that TCP-1 was found only in colon tumors(the target site)in tumor mice did not bind to any other tissues.Conjugating TCP-1 to tumor markedly increased its removal rate from blood circulation but mildly extended its staying time in vivo.In tumor mice,a lower AUC of TCP-1(reduced by almost 35％)and 2-fold higher clearance were found compared to that of normal mice.The proposed metabolic pathway of TCP-1 in the kidney was also determined using LC-MS"-IT-TOF.The high specificity and low toxicity of the peptide may be caused by its extremely tight binding to the targets.Potential applications for future clinical use,including MRI and PET/CT were also explored,and this re-search may promote the development of colon cancer diagnostic technology research and provide new ideas and technical routes for tumor diagnostic technology.
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    Divergent total synthesis of marine meroterpenoids(+)-dysidavarones A-C

    Qunlong ZhangYang KuangLe ChangJingyi Kang...
    234-238页
    查看更多>>摘要：Here,we report a concise and divergent enantioselective total synthesis of marine sesquiterpene quinone meroterpenoids(+)-dysidavarones A-C(1-3)using predysidavarone 6 as a key common intermediate.The highly strained and bridged eight-membered carbocycle of predysidavarone 6 was constructed by a one-pot intermolecular alkylation and intramolecular arylation of Wieland-Miescher ketone derivative 11 and benzyl bromide 12.The total synthesis of(+)-dysidavarones A-C(1-3)was achieved from predysi-davarone 6 in a divergent manner by a late-stage introduction of the ethoxy group,which reveals the possible source of the ethoxy group within(+)-dysidavarones A-C(1-3)and provides a late-stage modi-fiable route for the synthesis of dysidavarone analogs for further anti-cancer activity evaluation.
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    Copper-catalyzed conjugate addition of allene-derived nucleophiles to alkenyl-substituted carboxamides

    Bin FuYue ZhaoXiuping YuanYanfei Li...
    239-242页
    查看更多>>摘要：Catalytic Michael addition reaction represents a fundamental importance in organic synthetic chem-istry.Whereas corresponding conversions toward intrinsically low reactive enamide remains an ongoing challenging.We herein report a copper-catalyzed conjugate addition of allenes to β-substituted alkenyl amides,one of the most challenging Michael acceptors.The present method utilizes readily available al-lenes as the latent carbon-based nucleophiles and simple,common β-substituted alkenyl amides as start-ing materials,unlike previous methods that usually preinstall an activating group to improve the reac-tivity of amide or uses highly reactive stoichiometric quantities of organometallics.Hence,this approach shows good functional group compatibility and can be implemented under mild reaction conditions with excellent level of chemo-and regioselectivities.
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    Development of a cell-permeable adenine-derived probe for capture of nucleotide-binding proteins in living cells

    Lihong LiuRui ChenGang XueChenzhou Hao...
    243-246页
    查看更多>>摘要：Adenine is an essential building block of genetic material and a range of coenzymes.Chemical probes containing an adenine moiety have been used in kinase profiling studies in cell lysates.Here we report that adenine-derived small-molecule probes with an activated ester reactive group can covalently modify a conserved lysine residue of protein kinases and capture a number of nucleotide-binding proteins within living cells.
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    Copper(Ⅰ)-catalyzed interrupted click/radical relay:A four-component modular synthesis of triazole sulfones

    Pengfei SunFang WeiChen-Ho TungZhenghu Xu...
    247-251页
    查看更多>>摘要：A new,four component copper(l)-catalyzed interrupted click/radical relay cascade has been developed.This unprecedented interrupted click reaction provides a rapid modular synthesis of triazole sulfones,important privileged heterocyclic pharmacophores which cannot be accessed by a traditional click reac-tion.Radical interception of cuprate-triazole,the key reaction intermediate formed in situ,is an important feature of this process.
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    Phosphine-catalyzed acyl-transfer of heteroaryl ketones for the construction of N-fused heterocycles

    Yu ZhangDe-Rui HanDan YeHong Lu...
    252-256页
    查看更多>>摘要：An inexpensive phosphine catalyst was used effectively for a transition-metal-free acyl-transfer of N-containing heteroaryl ketones for the rapid synthesis of N-fused heterocycles.The key pre-aromatic spiro-cyclic intermediate initialized by the single electron transfer(SET)process of Togni's reagent Ⅱ promoted by the tertiary phosphine resulted in an intriguing and alternative tactic for the cleavage of C-C bonds.By using inexpensive tertiary phosphine as the catalyst,this skeleton-reorganizing approach of N-containing heteroaryl ketones allows a streamlined assembly of complex N-fused heterocycles with broad functional group tolerance.
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    Portable fluorogenic probe for monitoring of volatile amine vapour and food spoilage

    Jian-Hao ZhaoWen-Xing XuBin LiWei Xu...
    257-261页
    查看更多>>摘要：There are urgent needs of volatile amine gas sensors with high-performance in food quality control,dis-ease monitoring and environmental pollution.Thin-film fluorescent probe is suitable for amine vapour sensing due to its high sensitivity,high selectivity,and no polluting analyte.Herein,a novel fluorescent probe based on indacenodithiophene structure with π conjugated system was designed and synthesized.The experimental results show that the films prepared by this material exhibit rapid and distinct fluores-cence quenching after being exposed to saturated vapours of primary amine,secondary amine and ter-tiary amine represented by n-propylamine,diethylamine and trimethylamine,respectively.The quenching of fluorescence is 84％,87％and 96％,respectively,within 10 s.The detection mechanism of probe for pri-mary amine is based on specific chemical reaction,while the detection mechanism for secondary amine and tertiary amine is intramolecular charge transfer.Further experiments show that the detection limit of the fluorescent probe for trimethylamine,an important marker of food spoilage,could reach 4.610 ppt.On-site detection based on spoilage of small yellow croaker suggests the material possesses the potential for food freshness detection.This simple fluorogenic probe is an original approach to simplify real-time visual monitoring of volatile amine vapour.
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