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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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    Synthesis of photostable near-infrared sulfone-rhodamines for photoacoustic imaging-guided photothermal therapy

    Huiyu SiDongjuan WangXianfa DuXin Zhou...
    369-372页
    查看更多>>摘要：Photothermal therapy(PTT)is a cutting-edge cancer treatment that can kill cancer cells in hypoxic en-vironments without relying on oxygen.Seeking of the ideal photothermal agents with a high absorption coefficient in the near-infrared region,and a high excellent photothermal conversion efficiency is of great significance.Sulfone-Rhodanmine dye has showed an impressive absorption wavelength over 700 nm,but suffered from a stability issue.In this study,we synthesized five sulfone rhodamines and investigated the substitution effects on stability.S02R2 showed high stability and strong absorbance at 714 nm with an excellent photothermal conversion efficiency of 53.06％,making it suitable for accurate photoacoustic imaging-guided photothermal therapy in vivo.
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    Easy-to-perform organic-solvent-free synthesis of carbon dots with strong green photoluminescence

    Jiazhuang GuoYifeng ChenPan ZhangGe Li...
    373-378页
    查看更多>>摘要：Carbon dots(CDs)have been extensively studied owing to their fascinating optical properties and wide potential applications.Here,we report an easy-to-perform and organic-solvent-free synthesis strategy for green-emissive CDs(G-CDs)possessing high photoluminescence(PL)quantum yield(QY).The G-CDs are synthesized by heating the homogeneous precursors of citric acid and cyanamide in an open ves-sel,circumventing the use of organic solvents,complex operations,high-pressure reactors,and expensive instruments in the synthesis process.The effect of various reaction variables on the formation and the op-tical properties of G-CDs are systematically investigated.The resultant G-CDs show bright PL emission at 521 nm with PL QY up to 73％.Then a white light-emitting diode(LED)with Commission Internationable de L'Eclairage(CIE)coordinates of(0.33,0.34)and color rendering index(CRI)of 92 is constructed based on G-CDs/thermoplastic polyurethane(TPU)composite.Moreover,a visual microfluidic detection plat-form is designed by using G-CDs as fluorescent probes for rapid quantitative detection of Fe3+,Cu2+,and Mn2+metal ions,which can realize synchronized testing of multiple samples.This study might promote the development and preparation methods of high-performance CDs with various optical applications.
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    Acatulides A-G,neuroprotective macrolides from Acaulium album H-JQSF

    Zhi-Wu TongTing-Ting WangPei YangJia-Lin Sun...
    379-383页
    查看更多>>摘要：Fungal symbionts co-evolve with hosts and microbial co-inhabitants to acquire an unpredictable poten-tial for producing novel bioactive metabolites,but the knowledge about the topic remains patchy and superficial.Here we present the chemical characterization of acatulides A-G(1-7)as architecturally un-precedented macrolides from the solid-state culture of Acaulium album H-JQSF,an arthropod-associated fungus.The acatulide structures were elucidated by spectroscopic analysis,modified Mosher's method and single-crystal X-ray diffraction.The plausible biosynthetic pathways for compounds 1-4 are pro-posed.Interestingly,acatulides B-D(2-4)and G(7)were demonstrated to be neuroprotective against the 1-methyl-4-phenylpyridinium(MPP+)-induced damage to SH-SY5Y cells and nematode Caenorhabdi-tis elegans(C.elegans).
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    Screened peptides from one-bead one-compound technique extend half-life of peptide drugs in circulation through binding to albumin

    Yi-Jing LiLingze ZhangMing-Hao PangPei-Pei Yang...
    384-388页
    查看更多>>摘要：Peptide drugs are known for their high biological safety.However,compared with small molecule drugs,peptide drugs are easily oxidized and hydrolyzed as well as short in half-life.Herein,inspired by the long circulation of albumin in blood,we screened albumin binding peptides(ABPs)from a one-bead one-compound(OBOC)peptide library to increase the half-life of peptide drugs.Beads displaying random peptides were screened using fluorescent labeled human serum albumin.Fluorescent beads with specific binding to albumin were isolated for sequencing.The selected ABPs can effectively bind to albumin,thus possessing the long circulation of albumin.The dissociation constant(KD)of ABPs to albumin is up to 1 x 10-8 mol/L.Once one of ABPs(ABP2)was coupled to triptorelin,the circulation half-life of triptorelin in mice was significantly prolonged to 263.50 h much longer than that of triptorelin alone(179.07 h).In addition,the combination therapy using ABP-conjugated triptorelin and doxorubicin(DOX)can effectively inhibit the proliferation of tumor cells in mice.The OBOC screening strategy and resulting ABPs showed great potential for enhancing the delivery efficiency of peptide drugs.
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    De novo design of highly efficient type-Ⅰ photosensitizer based onπ-conjugated oligomer for photodynamic eradication of multidrug-resistant bacterial infections

    Qi ZhaoGuangchao QingJie YuYing Liu...
    389-393页
    查看更多>>摘要：Traditional photosensitizers show limited singlet oxygen generation in hypoxic infection lesions,which greatly suppress their performance in antibacterial therapy.Meanwhile,there still is lack of feasible de-sign strategy for developing hypoxia-overcoming photosensitizers agents.Herein,radical generation of 7r-conjugated small molecules is efficiently manipulated by an individual selenium(Se)substituent.With this strategy,the first proof-of-concept study of a Se-anchored oligo(thienyl ethynylene)(OT-Se)with high-performance superoxide radical(O2·-)and hydroxyl radical('OH)generation capability is present,and achieves efficient antibacterial activities towards the clinically extracted multidrug-resistant bacteria methicillin-resistant S.aureus(MRSA)and carbapenem-resistant E.coli(CREC)at sub-micromolar con-centration under a low white light irradiation(30 mW/cm2).The water-dispersible OT-Se shows a good bacteria-anchoring capability,biocompatibility,and complete elimination of multidrug-resistant bacteria wound infection in vivo.This work offers a strategy to boost type-Ⅰ photodynamic therapy(PDT)perfor-mance for efficient antibacterial treatments,advancing the development of antibacterial agents.
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    A nonenzymatic electrochemical sensor for the detection of hydrogen peroxide in vitro and in vivo fibrosis models

    Hongyao LiuYan YuTaixiong XueCailing Gan...
    394-398页
    查看更多>>摘要：Fibrosis occurs due to the excessive deposition of extracellular matrix caused by cell injury.After various types of tissue injury,the dysregulation of the internal response can eventually lead to the destruction of organ structure and dysfunction.There is increasing evidence that oxidative stress,which is characterized by excessive production of hydrogen peroxide(H2O2),is an important cause of fibrosis.Therefore,we synthesized a biosensitive and efficient electrochemical H2O2 sensor based on PtNi nanoparticle-doped N-reduced graphene oxide(PtNi-N-rGO)to detect H2O2 released from transforming growth factor β1(TGFβ1)-induced myofibroblast.In addition,the sensor could easily detect changes in H2O2 in the lung and bronchoalveolar lavage fluid(BALF)of mice with pulmonary fibrosis.Furthermore,the sensor could also detect H2O2 in activated hepatic stellate cells and the liver of carbon tetrachloride(CCl4)-induced liver fibrosis.Moreover,the alterations in H2O2 detected by the sensor were consistent with nicotinamide adenine dinucleotide phosphate oxidase 4(NOX4)protein expression and the staining results of patho-logical sections.Taken together,these results highlight the use of H2O2 sensors for the rapid detection of fibrosis and facilitate the rapid evaluation of antifibrotic drug candidates.
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    Synthesis and potential osteogenic applications of Wnt3a-loaded ZIF-8 nanoparticles

    Hengfei WangSong ChenZihan HeJunyu Chen...
    399-405页
    查看更多>>摘要：The Wnt signaling pathway plays a critical role in bone homeostasis,and the related protein therapy strategies have been reported to have great potential in osseointegration;however,they face formidable challenges such as complex external environments and unavoidable protein denaturation.In this work,we report a novel approach combining the synthesis of metal-organic frameworks(MOFs)and protein encapsulation in a one-pot process based on zeolitic imidazolate framework-8(ZIF-8)and Wnt3a protein,with improved biomechanical behavior and enhanced protein biological response.This combination was designed to enhance the Wnt3a protein function through the improved chemical stability provided by the ZIF-8 crystals.Additionally,the zinc ions contained in the ZIF-8 crystals induced bone homeostasis,further favoring the osteogenesis.The results showed that the Wnt3a protein-loaded ZIF-8 crystals served as efficient drug delivery vehicles to promote osteogenesis,preventing protein denaturation.In particular,Wnt3a-loaded ZIF-8 nanoparticles(Wnt3a@ZIF-8 NPs)had higher efficacy on bone marrow mesenchymal stem cells(BMSCs)than ZIF-8 NPs or Wnt3a proteins,contributing to the osteogenesis through ZIF-8 crystals and intracellular Wnt3a proteins released from Wnt3a@ZIF-8 NPs.Furthermore,polymerase chain reaction(PCR)analysis showed that the osteogenic pathways were upregulated.Overall,the present one-pot process can open up new avenues to develop signaling protein-delivery systems for applications in protein therapy strategies.
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    Combination losartan with hyaluronic acid modified diethyldithiocarbamate loaded hollow copper sulfide nanoparticles for the treatment of breast cancer and metastasis

    Haili HuWeiwei ZhangLei LeiFan Tong...
    406-414页
    查看更多>>摘要：The application of photothermal therapy(PTT)is greatly limited by the low accumulation of photother-mal agents,uneven photothermal distribution,and heat endurance of cancer cells.Worse still,despite PTT enhances immunogenicity,the anti-tumor immune efficacy is still unsatisfactory due to the ineffi-cient immunogenic cell death(ICD)induction and poor infiltration of immune cells.To solve the above problems of PTT,we developed hyaluronic acid(HA)modified hollow copper sulfide nanoparticles en-capsulating diethyldithiocarbamate(DDTC)to construct a breast tumor targeting and near infrared(NIR)photo-responsive drug delivery system(D-HCuS@HA),which further combined with losartan to improve the accumulation and penetration in the tumor site.Upon irradiation,D-HCuS@HA realized enhanced PTT and released cytotoxic Cu(DDTC)2 to eliminate heat endurance tumor cells,thereby enhancing anti-tumor effect and inducing effective ICD.Moreover,the combination with losartan could remodel the tu-mor microenvironment,allowing more T cells to infiltrate into the tumor,and significantly inhibiting the occurrence and development of metastatic tumors.In vitro/vivo results revealed the great potential of D-HCuS@HA combined with losartan,which provides a new paradigm for anti-tumor and anti-metastases.
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    Rearranged 19-nor-7,8-seco-labdane diterpenoids and Diels-Alder cycloadducts from the Chinese liverwort Pallavicinia ambigua:Structural elucidation,photoinduced rearrangement,and cytotoxic activity

    Chunyang ZhangYuelan LiZhaojun ChuShuangzhi Yuan...
    415-418页
    查看更多>>摘要：Two distinctive rearranged 19-nor-7,8-seco-labdane diterpenoids(1 and 2)with a novel tetracyclo[5.2.1.02,5.04,10]decane skeleton,a derivative of the open tetrahydrofuran ring(7),three dimeric compounds(8-10),and four revised homologs(3-6)were obtained from Chinese liverwort Pallavicinia ambigua.Their structures were identified via combined analysis of their spectroscopic data,single-crystal X-ray diffraction patterns,and ECD calculations.The light-driven conversion of compound 5 to compounds 1-4 demonstrated that photochemically induced postmodification involved in biosyn-thesis is an important way to diversify natural structures.A preliminary cytotoxicity assay revealed that compound 5 showed significant inhibition in the human prostate cancer(PC-3)cell line via an apoptotic pathway.
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    A metal-free coordination-insertion ring-opening polymerization of tetrahydrofuran by the central metalloid bis(pentafluorophenyl)(phenoxy)borane

    Cheng WuYixuan LiuChunsheng XiaoChenyang Hu...
    419-422页
    查看更多>>摘要：A new strategy for the metal-free coordination-insertion ring-opening polymerization of tetrahydrofuran by the central metalloid Boron has been first identified.Bis(pentafluorophenyl)(phenoxy)borane was used as a catalyst for the polymerization reaction system.And polytetrahydrofuran with high molecular weight and narrow molecular weight distribution could be obtained.The proposed mechanism was studied by MALDI-TOF,ESI-MS and O-18 isotope labeling analyses as a metal-free coordination insertion mechanism.
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