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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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    Lidocaine hydrochloride loaded isomaltulose microneedles for efficient local anesthesia of the skin

    Xuebing JiangSiyi WangLi ZhangXian Jiang...
    298-302页
    查看更多>>摘要：Lidocaine hydrochloride(LIDH)as an anesthetic is widely used in local anesthesia.Dissolving micronee-dles(MNs)have great application value in the field of skin anesthesia.However,the limited drug-loading of dissolving MNs is an existing challenge that affects clinical use.In this study,we have screened isomal-tulose(ISO)as the proper matrix material for the MNs by using molecular dynamics(MD)simulation.Our findings indicate that ISO has good compatibility with LIDH,and the LIDH-loaded ISO MNs(LI-MNs)have high drug-loading capacity.The drug-loading capacity of LI-MNs could reach 80％,and it could effectively puncture the skin.In addition,the preparation method of customized LI-MNs was established based on three-dimensional(3D)printing technology.It was shown that the administration time of LI-MNs could be controlled within 3 min.Also,the LI-MNs were able to provide the local anesthetic efficacy within 2 min and sustained for more than 2 h.Significantly,LI-MNs had more efficient drug efficacy compared to the topical creams and the majority of existing LIDH-loaded dissolving MNs.They even provided a longer duration of action than the injections.Overall,the LI-MNs with high drug-loading have a promis-ing application prospect.
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    Scalable production of mesoporous titanium nanoparticles through sequential flash nanocomplexation

    Feng CuiFangman ChenXiaochun XieChenyang Guo...
    303-309页
    查看更多>>摘要：Mesoporous titanium nanoparticles(MTNs)have emerged as an important porous semiconductor owning to their large surface area and unique electronic/optical properties.However,the fundamental research for rational manufacturing MTNs in a highly scalable manner remains a challenge.In this study,we report a two-step flash nanocomplexation(FNC)approach to large-scalable generate MTNs through the sequen-tial combination of two multi-inlet vortex mixers.By optimizing the concentrated titanium precursor,polyethylene glycol(PEG)-functionalized silane amount and pH,we have been able to produce MTNs with small particle size(31.5 nm),larger surface area(416.9 m2/g)and pore volume(0.59 cm3/g).Different from the traditional MTNs bulk,FNC-produced MTNs exhibited well-controlled manner and exceptional photo-catalytic and antibacterial properties.Importantly,the optimized MTNs outperformed commercial P25 not only in protecting ultraviolet A(UVA)-exposed skin,but also in treating P.aeruginosa-infected wound.We believe that the high controllability and scalability of sequential flash nanocomplexation method offers great opportunities in enhancing the performance of mesoporous titanium nanoparticles.
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    Intermolecular hydrogen-bonding as a robust tool toward significantly improving the photothermal conversion efficiency of a NIR-Ⅱsquaraine dye

    Songtao CaiLiuying WuYuan LiSoham Samanta...
    310-315页
    查看更多>>摘要：The photothermal therapy(PTT)has come across as a promising noninvasive therapeutic strategy for tu-mor treatment.However,low photothermal conversion efficiency(PCE)and hydrophobicity may impede the therapeutic efficacy of organic photothermal agents and an efficient PTT-agent must overcome these two major challenges.In this work,we developed a new strategy to promote higher PCE wherein the intermolecular hydrogen-bonding interaction between the single dye molecule and water facilitated the transformation of the absorbed energy into the heat.A hydrophilic squaraine dye(SCy1)with the sec-ond near-infrared region(NIR-Ⅱ)absorption and extremely low emission were designed to exhibit much higher PCE than that of the analogues of pentamethine-dyes(PCy1,PCy2).The presence of the'-O-'at middle of squaric cycle enabled the intermolecular H-bonding formation between the SCy1 and water to promote the energy dissipation channel.Moreover,the introduction of long-chain phenylsulfonate groups helped in to improve the water solubility apart from serving as an additional means of further enhancing PCE through fluorescence quenching.Therefore,SCy1 with a squaraine backbone and long-chain sulfonate moieties revealed outstanding photothermal stability and anti-aggregation activity apart from showing exceptionally high PCE(74％)in water.SCy1 demonstrated excellent therapeutic efficacy when applied in the PTT treatment of tumor-bearing mice under a laser irradiation of 915 nm.
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    Heavy-atom engineered hypoxia-responsive probes for precisive photoacoustic imaging and cancer therapy

    Ling-Ling WuXiangchuan MengQingyang ZhangXiaowan Han...
    316-320页
    查看更多>>摘要：Photoacoustic agents combining photodynamic therapy(PDT)and photothermal therapy(PTT)functions have emerged as potent theranostic agents for combating cancer.The molecular approaches for enhancing the near-infrared(NIR)-absorption and maximizing non-radiative energy transfer are essential for effec-tive photoacoustic imaging(PAI)and therapy applications.In addition,such molecules with high speci-ficity and affinity to cancer cells are urgently needed,which would further decrease the side effect during treatments.In this study,we applied a heavy-atom engineering strategy and introduced p-aminophenol,-thio,and-seleno moieties into NIR heptamethine cyanine(Cy7)skeleton(Cy7-X-NH2,X=O,S,Se)to sig-nificantly increase photothermal conversion efficiency for PTT and promote intersystem crossing for PDT.Additionally,we designed a series of nitroreductase(NTR)-activated photoacoustic probes(Cy7-X-NO2,X=O,S,Se),and target hypoxic tumors with NTR overexpression.Our prostate cancer targeting probe,Cy7-Se-NO2-KUE,exhibited specific tumor photoacoustic signals and effective tumor killing through out-standing synergistic PTT/PDT in vivo.These findings highlighted a versatile strategy for cancer photoa-coustic diagnosis and enhanced phototherapy.
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    Water-soluble and polarity-sensitive near-infrared fluorescent probe for long-time specific cancer cell membranes imaging and C.Elegans label

    Lixian FuYiyun TanYue DingWeixia Qing...
    321-323页
    查看更多>>摘要：A novel D-π-A structure and near-infrared fluorescent probe(DCITT)with high polarity sensitivity and membrane targeting was reported.The fluorescent spectra of DCITT were polarity dependent and Stokes shift was greater than 300 nm.Due to its high fluorescence quantum yield,low cytotoxicity and photosta-bility,DCITT could be used as a labeling probe in multicellular organisms.In particular,DCITT effectively distinguished tumor cells from normal cells because it could specifically light up the cancer cells mem-brane based on strong red fluorescence for a long time.On this basis,a polar-sensitive cell membrane probe is developed to differentiate tumor cells from normal cells,which provides an idea and method for the early diagnosis of tumor at cellular level.
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    Activatable photoacoustic bioprobe for visual detection of aging in vivo

    Zihong LiJie ChengPing HuangGuoliang Wu...
    324-329页
    查看更多>>摘要：Aging is a natural physiological process with various challenges,related to the loss of homeostasis within the organism,which is not a disease,but a significantly strong risk factor for multiple diseases,including myocardial infarction,stroke,some age-related cancers,macular degeneration,osteoarthritis,neurode-generation,and many others.In the body,the main manifestation of aging is cellular aging,which exists within tissues and has a local or global impact on tissue function.However,the lack of effective aging detection tools has always been an issue that cannot be ignored in the field of aging research.Therefore,it is necessary to construct a non-invasive tool for in vivo detection of aging.Here,we show that the photoacoustic probe(LGAL),which has peak excitation and emission wavelengths in the near-infrared optical window,binds in vivo and at high contrast to the hallmark of aging,and allows for the micro-scopic imaging of aging through the intact mice.Firstly,this tool LGAL has been successfully applied to detect senescence in cells,displaying stronger photoacoustic signals than normal cells.Then,by using the photoacoustic probe,the blood vessels and tissues inside the mice can be visualized.Young and elderly mice exhibit varying intensities of photoacoustic signals,marking the first time a probe has been used to explore the aging of blood vessels and tissues inside the mice.Finally,we monitored the changes in the degree of aging during tumor treatment under photoacoustic(PA)imaging for the first time.As the treatment time increased,the degree of aging of the tumor gradually deepened.We expect the powerful tool could be a noninvasive and powerful tool for the study of aging biology.
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    Oxidative cyclization of allyl compounds and isocyanide:A facile entry to polysubstituted 2-cyanopyrroles

    Yaping ZhangWei ZhouMingchun GaoTianqi Liu...
    330-335页
    查看更多>>摘要：A facile TfOH-catalyzed oxidative cyclization of allyl compounds and isocyanide has been developed with the assistance of DDQ,where isocyanide is used as the crucial"N"and"CN"sources.Highly function-alized 2-cyanopyrroles are constructed efficiently through a new formal[3+2]mode,demonstrating di-verse reactivity and synthetic utility in organic chemistry.2-Cyanopyrrole is converted into a nucleobase analogue of Remdesivir and 5H-pyrrolo[2,1-a]isoindole through a three-step or a two-step sequence,re-spectively.This protocol features broad substrate scope,operational simplicity and good functional group tolerance.
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    Total synthesis of a putative yuzurimine-type Daphniphyllum alkaloid C14-epi-deoxycalyciphylline H

    Jingping HuJing Xu
    336-339页
    查看更多>>摘要：One of the largest subfamilies within the famous Daphniphyllum alkaloid family is made up of the yuzurimine-type(or macrodaphniphyllamine-type)alkaloids.Their complex aza-polycyclic caged struc-tures,several contiguous stereogenic centers,and vicinal all-carbon quaternary centers make these al-kaloids formidable challenge for synthetic chemists.Recently,synthesis of these alkaloids has received extensive attention from our community.Herein,we wish to report the total synthesis of C14-epi-deoxycalyciphylline H,a putative member of yuzurimine-type alkaloid subfamily.Key transformations employed in our approach include an intramolecular Prins reaction and a Pd-catalyzed enyne cycloiso-merization.In addition,synthesis of a daphnezomine L-type alkaloid,paxdaphnidine A,was also studied.
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    Electrochemical construction of 2,5-diaryloxazoles via N-H and C(sp3)-H functionalization

    Tong LiLeping PanYan ZhangJihu Su...
    340-345页
    查看更多>>摘要：An efficient N-H and C(sp3)-H functionalization of aryl ketones with benzylamines/amino acids was developed under mild conditions by virtue of anodic oxidation.A variety of functionalized 2,5-diaryloxazoles were obtained with good to excellent yields.Moreover,some important natural products can be prepared by this method.The reaction features a broad substrate scope,scalability,metal-free and chemical oxidant-free.
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    Phenylhydrazone anions excitation for the photochemical carbonylation of aryl iodides with aldehydes

    Lei ShenYang ZhangLinlin ZhangChuanwang Liu...
    346-351页
    查看更多>>摘要：Spectroscopic investigations discovered that the in-situ generated phenylhydrazone anion was signifi-cantly bathochromically shifted to visible light region for photoactivation under irradiation.The photoex-cited phenylhydrazone anion was potential to reduce aryl iodides via single electron transfer process for the subsequent radical chain reaction.A redox-neutral photochemical carbonylation of aryl iodides was developed on basis of the special spectroscopic features of phenylhydrazone anion.This protocol pro-vided a convenient and efficient synthetic tool for accessing carbonylation products under redox neutral conditions without the need of transition-metals.
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