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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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    Cancer cell membrane camouflaged biomimetic gelatin-based nanogel for tumor inhibition

    Yuanzheng WangChen ZhangShuyan HanXiaoli Kong...
    389-394页
    查看更多>>摘要：Enhancing the active tumor targeting ability and decreasing the clearance of reticuloendothelial system(RES)are important issues for drug delivery systems(DDSs)in cancer therapy.In recent years,cell mem-brane camouflage,as one of the biomimetic modification strategies,has shown huge potential.Many nat-ural properties of source cells can be inherited,allowing the DDSs to successfully avoid phagocytosis by macrophages,prolong circulation time,and achieve homologous targeting to lesion tissue.In this study,a cancer cell membrane camouflaged nanoplatform based on gelatin with a typical core-shell structure was developed for cancer chemotherapy.Doxorubicin(DOX)loaded gelatin nanogel(NG@DOX)acted as the inner core,and 4T1(mouse breast carcinoma cell)membrane was set as the outer shell(M-NG@DOX).The M-NG platform enhanced the ability of homologous targeting due to the surface protein of cell mem-brane being completely retained,which could promote the cell uptake of homotypic cells,avoid phagocy-tosis by RAW264.7 macrophages,and therefore increase accumulation in tumor tissue.Meanwhile,due to the better controlled drug release capability of M-NG@DOX,premature release of DOX in circulation could be reduced,minimizing side effects in common chemotherapy.As a result,the biomimetic nanoplatform in this study,obtained by a cancer cell membrane camouflaged drug delivery system,efficiently reached desirable tumor elimination,providing a significant strategy for effective targeted therapy and specific carcinoma therapy.
      原文链接:
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    Ion-interferential cell cycle arrest for melanoma treatment based on magnetocaloric bimetallic-ion sustained release hydrogel

    Zheyi LiXiaoyang LiangZitong QiuZimeng Liu...
    395-401页
    查看更多>>摘要：Melanoma treatment has been revolutionized with the development of targeted therapies and im-munotherapies,which shows a positive influence on the patients.However,the long-term efficaciousness of such therapy is restricted by side effects,limited clinical effects as well as quick resistance to treat-ment.In this work,we prepared magnetocaloric carrier-free bimetallic hydrogels,named manganese-iron oxide nanocubes@polyethylene glycol-hydrogels(MFO@PEG-Gels),to realize ion-interferential cell cycle arrest for melanoma treatment.In detail,the tumor site was exposed to alternating magnetic field(AMF)after intratumorally injected MFO@PEG-Gels,which generated hyperthermia and promoted the sol-gel phase transition for MFO sustained release.Under the tumor microenvironment,hydrogen peroxide trig-gered MFO degradation to induce Mn2+and Fe3+release.On one hand,Mn2+blocked G1/S phase through the activation of p27 pathway.On the other hand,Fe3+could arrest the G2/M phase by upregulating the polo-like kinase 4(PLK4)expression as well as inhibiting autolysosome formation to achieve the en-hanced cell cycle arrest,thereby promoting the apoptosis of melanoma cells.In summary,this study pro-posed ion-interferential cell cycle arrest strategy by a multifunctional and injectable magnetic bimetallic hydrogel for melanoma treatment,which provided a secure and sustainable regimen for enhancing anti-tumor efficacy.
      原文链接:
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    A β-lactamase-activatable photosensitizer for the treatment of resistant bacterial infections

    Zhipeng LiQincong FengJianliang Shen
    402-405页
    查看更多>>摘要：Antibacterial agent of activatable photosensitizer not only has the advantages of traditional photosensi-tizers,such as good curative effect and low resistance,but also has better selectivity for bacteria and lower toxicity to normal tissues.Limited reports of activatable photosensitizer can be used to treat drug-resistant bacteria.In order to meet this challenge,we designed and synthesized an activatable photo-sensitizer(Ce-OHOA),which can not only selectively identify methicillin-resistant Staphylococcus aureus(MRSA)with high expression of β-lactamase by fluorescence imaging,but also kill MRSA with less than 10 times the concentration and 10 times the irradiation dose of CySG-2 reported.Ce-OHOA not only com-bines the dual functions of fluorescence diagnosis and photodynamic therapy,but also selectively acts on bacteria with high expression of β-lactamase and has little toxicity to normal cells.We expect that the study of this activating photosensitizer will provide a new solution for antibacterial photodynamic ther-apy(aPDT)of drug-resistant bacteria.
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    Tetrahedron DNA nanostructure/iron-based nanomaterials for combined tumor therapy

    Jiangshan XuWeifei ZhangZhengwen CaiYong Li...
    406-412页
    查看更多>>摘要：Triple-negative breast cancer,due to its aggressive nature and lack of targeted treatment,faces serious challenges in breast cancer treatment.Conventional therapies,such as chemotherapy,are encumbered by a range of limitations,and there is an urgent need for more effective treatment strategies.Ferroptosis,as an iron-dependent form of cell death,has exhibited promising potential in cancer treatment.Combining ferroptosis with other cancer therapies offers new avenues for treatment.Tetrahedral DNA nanostruc-ture(TDN),a novel DNA-based three-dimensional(3D)nanomaterial,is promising drug delivery vehicle and can be utilized for functionalizing inorganic nanomaterials.In this work,we have demonstrated the preparation of Fe3O4-PEI@TDN-DOX nanocomposites and elucidated their antitumor mechanism.The TDN facilitated the enhanced cellular uptake of polyetherimide(PEI)-modified Fe3O4,and the delivery of the chemotherapeutic drug doxorubicin(DOX)further augmented their anti-tumor effect.This novel strategy can destroy the tumor redox homeostasis and produce overwhelming lipid peroxides,consequently sen-sitizing the tumor to ferroptosis.The integration of ferroptosis with other cancer therapies opens up new possibilities for treatment.This research provides valuable mechanistic insights and practical strategies for leveraging nanotechnology to induce ferroptosis and amplify its impact on tumor cells.
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    Fe(Ⅲ)-juglone nanoscale coordination polymers for cascade chemodynamic therapy through synergistic ferroptosis and apoptosis strategy

    Zhendong LiuSainan LiuBin LiuQi Meng...
    413-418页
    查看更多>>摘要：Chemodynamic therapy(CDT)relying on the transformation of endogenous hydrogen peroxide(H2O2)into cytotoxic hydroxyl radicals(·OH)based on the catalysis of Fenton/Fenton-type reactions exhibits great potentiality for cancer treatment.However,the inadequate H2O2 supply and intricate redox home-ostasis in tumor microenvironment(TME)severely impair the efficacy of CDT.Herein,we design self-assembled 1,2-distearoyl-sn-glycero-3-phosphoethanolamine conjugated polyethylene glycol(DSPE-PEG)-modified Fe(Ⅲ)-juglone nanoscale coordination polymers(FJP NCPs)as redox homeostasis disruptors for juglone-enhanced CDT.Responding to glutathione(GSH)-rich and acidic TME,the Fe2+/Fe3+-guided CDT and GSH consumption by Fe3+are activated,resulting in·OH downstream and up-regulation of lipid per-oxidation(LPO).In addition,the released juglone not only depletes GSH through Michael addition,but also elevates intracellular H2O2 level for achieving·OH further bursting.With the impressive efficiency of GSH exhaustion and reactive oxygen species(ROS)storm generation,ferroptosis and apoptosis are sig-nificantly enhanced by FJP NCPs in vivo.In brief,this facile and efficient design for versatile nanoscale coordination polymers presents a novel paradigm for effectively elevating CDT efficiency and tumor syn-ergistic therapy.
      原文链接:
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    • 维普

    Penetrating efficiency of supramolecular hydrogel eye drops:Electrostatic interaction surpasses ligand-receptor interaction

    Zhibin RenShan LiXiaoying LiuGuanghao Lv...
    419-422页
    查看更多>>摘要：The low drug bioavailability of eye drops challenges the therapy of ocular disorders with high efficacy.One of solutions is to extend the corneal retention and enhance the penetration of drug into cornea.Here we synthesize two fluorophore-conjugated peptide based analogs rich in positive charges(i.e.,NBD-FFKK)and with a specific ligand(i.e.,NBD-FFRGD),respectively,to visualize their performances in vitro and in vivo.The peptides both can self-assemble into supramolecular hydrogels with the microstructure of nanofibers.The in vitro experiments exhibit that two peptides are both uniformly distributed in cyto-plasm,and the intracellular amount of peptide rich in positive charges is significantly larger than that of peptide with a specific ligand.The living corneal fluorescence shows that two peptides enter the corneal stroma within 15 min,and the peptide rich in positive charges is accumulated more extensively through-out the entire cornea,revealing that the supramolecular hydrogel eye drops penetrate the cornea more efficiently via electrostatic interaction than that via ligand-receptor interaction.This work,as a compara-tive study of supramolecular hydrogel eye drops on penetrating efficiency,indicates a possible direction for the design of eye drops with efficient corneal penetration.
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    Penicillin G acylase-responsive near-infrared fluorescent probe:Unravelling biofilm regulation and combating bacterial infections

    Yang LiuLeilei ZhangKaixuan LiuLing-Ling Wu...
    423-429页
    查看更多>>摘要：Antibiotic resistance poses a critical threat to human healthcare,largely driven by bacterial biofilms.These biofilms resist the immune system and antibiotics,rendering enclosed microbial cells 10-1000 times more antibiotic-resistant than planktonic cells,leading to severe infections.Therefore,there is an urgent need to develop innovative tools for investigating biofilm regulators and devising novel antibacte-rial strategies.In this study,we developed Cy-NEO-PA,a near-infrared(NIR)fluorescent probe responsive to penicillin G acylase(PGA),with bacteria-targeting ability.This probe was designed to visualize the influence of environmental factors on biofilm formation in Acinetobacter baumannii(A.baumannii).Our findings demonstrated that glucose suppressed PGA production,leading to enhanced biofilm formation,whereas phenylacetic acid(PAA)stimulated PGA production and inhibited biofilm formation in A.bau-mannii.These observations highlight the remarkable capability of Cy-NEO-PA to accurately measure PGA dynamics,shedding light on the critical role of PGA in biofilm development.Additionally,Cy-NEO-PA ex-hibited excellent biocompatibility,potent reactive oxygen species(ROS)generation,efficient photothermal conversion,and bacteria-targeting abilities,making it a promising agent for combating bacterial infections and promoting wound healing through photothermal(PTT)/photodynamic(PDT)therapy.These discover-ies emphasize the significant role of PGA in antibacterial therapy and offer valuable insights for the design of effective strategies targeting PGA to combat biofilm-associated infections.
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    Design,synthesis and evaluation of the first DYRK1A degrader for promoting the proliferation of pancreatic β-cells

    Yueying YangHuiru XieXinbo YuYang Liu...
    430-434页
    查看更多>>摘要：Dual-specificity tyrosine-phosphorylation-regulated kinase 1A(DYRK1A)is the most promising target for diabetes treatment by promoting β-cell proliferation.The desmethylbellidifolin(DMB)as a DYRK1A in-hibitor could facilitate β-cell proliferation in vivo and in vitro.However,DMB has the problem of weak binding affinity to DYRK1A,which means that continuous high concentration administration of DMB is effective for the diabetes.In order to solve this problem,we designed and synthesized a series of DMB-based proteolysis targeting chimeras(PROTACs)by taking advantage of the property of PROTAC that in-duce protein degradation in a cycle-catalytic manner.MDM2-based PROTAC X1-4P-MDM2 was identified as the most active PROTAC molecule.Mechanism research showed that X1-4P-MDM2 formed a ternary complex with DYRK1A and murine double minute 2(MDM2),and induced the degradation of DYRK1A through the ubiquitin-proteasome system pathway.At a dose much lower than that of DMB,X1-4P-MDM2 still significantly enhanced β-cell proliferation by inhibiting transforming growth factor beta(TGF-β)and promoting the mitogen-activated protein kinases/extracellular signal-regulated kinase(MAPK/ERK)signaling pathway,which may provide a new strategy for the application of DMB in diabetes.
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    Discovery of an enantiopure N-[2-hydroxy-3-phenyl piperazine propyl]-aromatic carboxamide derivative as highly selectiveα1D/1A-adrenoceptor antagonist and homology modelling

    Junjun HuangRan ChenYajian HuangHang Zhang...
    435-441页
    查看更多>>摘要：α1-Adrenergic receptor(AR)blockers can be effective for the treatment of benign prostatic hyperpla-sia/lower urinary tract symptoms(BPH/LUTS),their usage is limited by cardiovascular-related side ef-fects that are caused by the subtype nonselective nature or low selectivity of many current drugs.We previously reported that phenylpiperazine analogues with amide and propane linker were moder-ate α1D/1A adrenoceptor antagonists and exhibited better anti-BPH effect than lead compound naftopidil(NAF)in vivo,however,with modest α1D/1A-subtype selectivity.Herein,we replaced propane moiety with 2-hydroxypropanol linker and synthesized twenty-seven racemic derivatives with modified aromatic and hetero aromatic groups.Of these new compounds,quinoline surrogate 17 exhibited extremely weak an-tagonistic affinity on α1B in both cell-based calcium assay and tissue-based functional assay,so that elicited significant α1A/1B and α1D/1B selectivity.Intriguingly,the R enantiomer of 17 preferentially dis-played superior anti-BPH effect in rat model compared with S-17,supporting ligand regulates the receptor in a highly stereospecific manner.Finally,the computer-aided modelling research was also performed in order to deeply understand the unique binding mode of R-17 in complex with α 1A and the subtype recep-tor selectivity for R-17 was also rationalized in this study.Taken together,our work enriched the diversity of phenylpiperazines for the treatment of BPH/LUTS,and provided a basis for discovery of α1D/1A-selective ligands.
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    Rationally engineered IR-783 octanoate as an enzyme-activatable fluorogenic tool for functional imaging of hNotum in living systems

    Lilin SongMengru SunYuqing SongFeng Zhang...
    442-447页
    查看更多>>摘要：As a vital negative regulator of Wnt signaling pathway,human Notum(hNotum)plays a crucial regula-tory role in the progression of many human diseases.Deciphering the relevance of hNotum to human diseases requires practical and reliable tools for visualizing hNotum activity in living systems.Herein,an enzyme-activatable fluorogenic tool(IR-783 octanoate)was rationally engineered for sensing and imag-ing hNotum activity in living systems by integrating computer-aided molecular design and biochemical assays.IR-783 octanoate showed good optical properties,excellent specificity and high binding-affinity towards hNotum(Km=0.98 pmol/L).IR-783 octanoate could be well up-taken into the cancerous cells or tumors that over-expressed organic anion transporting polypeptides(OATPs),and then hydrolyzed by cellular hNotum to release free IR-783 ketone,which created brightly fluorescent signals around 646 nm.Further investigations showed that IR-783 octanoate achieved a good performance for in-situ functional imaging of hNotum in both living cells,cancerous tissues and organs.It was also found that some SW620 cells with multipolar spindles could be stained by IR-783 octanoate to emit extremely bright signals,suggesting that this agent could be used as a novel visualizing tool for tracing the cells undergoing ab-normal cell mitoses.Collectively,this study devises a highly specific fluorogenic tool for in-situ functional imaging of hNotum in living systems,which offers a practical and reliable tool to dynamically track the changes in hNotum activity under various conditions.
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