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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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    A lateral-immobilization zebrafish microfluidic chip-based system for in vivo real-time evaluation of antithrombotic agents

    Lijuan HeHongxia DuYi YangZhihua Guan...
    312-315页
    查看更多>>摘要：Thrombosis remains a major global health concern mainly characterized by high rates of morbidity and mortality.Animal models serve as an indispensable tool to understand the underlying pathogenesis of thrombosis and assess the efficacy of novel antithrombotic drugs.Currently,zebrafish has emerged as a valuable model organism for thrombosis research.However,the traditional method of studying zebrafish thrombosis requires a laborious and time-consuming procedure,including anesthesia and manual im-mobilization of zebrafish.In this study,based on hydrodynamic force,a lateral-immobilization zebrafish microfluidic chip(LIZMC)was designed to evaluate the cardiovascular system of multiple larvae within a single microscope field of view.Specifically,coupling with microscope imaging,real-time monitoring of the peripheral blood circulation in the tail of phenylhydrazine(PHZ)-induced zebrafish thrombosis was enabled.Furthermore,the reliability of LIZMC for in vivo evaluation of antithrombotic agents in zebrafish was verified using aspirin.Collectively,this novel LIZMC-based system can be used for in vivo zebrafish thrombosis studies and rapid screening of antithrombotic agents.
      原文链接:
    • NETL
    • NSTL
    • 万方数据

    Applying dynamic light scattering to investigate the self-assembly process of DNA nanostructures

    Wei YuanGui-Zhi DongHui NingXiang-Xiang Guan...
    316-320页
    查看更多>>摘要：Understanding the dynamic assembly process of DNA nanostructures is important for developing novel strategy to design and construct functional devices.In this work,temperature-controlled dynamic light scattering(DLS)strategy has been applied to study the global assembly process of DNA origami and DNA bricks.Through the temperature dependent size and intensity profiles,the self-assembly process of various DNA nanostructures with different morphologies have been well-studied and the temperature transition ranges could be observed.Taking advantage of the DLS information,rapid preparation of the DNA origami and the brick assembly has been realized through a constant temperature annealing.Our results demonstrate that the DLS-based strategy provides a convenient and robust tool to study the dy-namic process of forming hieratical DNA structures,which will benefit understanding the mechanism of self-assembly of DNA nanostructures.
      原文链接:
    • NETL
    • NSTL
    • 万方数据

    Chalcone derivatives as novel,potent and selective inhibitors against human Notum:Structure-activity relationships and biological evaluations

    Jin-Hui ShiBei ZhaoLi-Lin SongYu-Qing Song...
    321-325页
    查看更多>>摘要：Human Notum(hNotum)inhibitors could be used for treating Wnt signalling-associated diseases includ-ing colorectal cancer.Herein,two series of chalcone derivatives were designed and synthesized aiming to find selective and potent hNotum inhibitors.Structure-activity relationship(SAR)studies showed that 2-methoxyl and 5-bromine substitutions on A-ring significantly enhanced anti-hNotum effect,while 4'-ethoxyl and 3'-alkyl substitutions on B-ring were beneficial for hNotum inhibition.Among all tested chalcones,B11 displayed the most potent anti-Notum effect(IC50=3.6nmol/L),good selectivity,excel-lent chemical stability and suitable metabolic stability.Further investigations showed that B11 acted as a competitive inhibitor of hNotum,while this agent(5 μmol/L)significantly weaken the migration abilities of colorectal cancer cells.Collectively,this study deciphers the SARs of chalcones as hNotum inhibitors and reports a novel and potent hNotum inhibitor with the anti-migration effect on colorectal cancer cells,which offers a promising lead compound to develop novel anti-cancer agents.
      原文链接:
    • NETL
    • NSTL
    • 万方数据

    Design,synthesis,and biological evaluation of 1,2,4-triazole derivatives as potent antitubercular agents

    Yu WenShichun LunYuxue JiaoWei Zhang...
    326-331页
    查看更多>>摘要：Inhibition of mycobacterial membrane protein large 3(MmpL3)thereby affecting the mycolic acid biosyn-thetic pathway has been proven to be an effective strategy for developing antitubercular drugs.Based on the X-ray crystal structure of MmpL3 inhibitor complexes,a series of novel 1,2,4-triazole derivatives were designed,synthesized and evaluated antitubercular activity against Mtb strain H37Rv.Comprehen-sive structure-activity relationship exploration resulted in the identification of compounds 21 and 28,which possess potent antitubercular activity against Mtb strain H37Rv[minimum inhibitory concentration(MIC)=0.03-0.13 μg/mL]and the clinical isolates of multidrug resistance(MDR)and extensive drug resis-tance(XDR)tuberculosis(MIC=0.06-1.O μg/mL).Moreover,compounds 21 and 28 showed neglectable cytotoxicity(IC50 ≥ 32 μg/mL)to the mammalian Vero cells and favorable physicochemical and pharma-cokinetic properties according to the in silico absorption,distribution,metabolism and excretion(ADME)prediction.Finally,the potential target of representative 1,2,4-triazole 28 was identified to be MmpL3 using a microscale thermophoresis(MST)assay.
      原文链接:
    • NETL
    • NSTL
    • 万方数据

    A folic acid-decorated nanoparticles loaded JQ1 for oral squamous cell carcinoma therapy

    Dequan ZengZhongkai MaXin ZanTing Luo...
    332-336页
    查看更多>>摘要：Oral squamous cell carcinoma(OSCC)is known as one of the most malignant tumors with high recur-rence and fatality rate.The poor tumor-targeting ability of traditional chemotherapeutic drugs has been a grand challenge for anti-OSCC therapy.Beyond that,a large quantity of tumor associated macrophages in OSCC tissues further diminish the anti-tumor effects of these drugs.Therefore,we produced a therapeu-tic nano drug delivery system(FA-PEG-PLA-JQ1)through encapsulating JQ1[a small-molecule inhibitor of bromodomain containing protein 4(BRD4)]into the folic acid(FA)-modified nanoparticle(PEG-PLA),which could prolong the half-life of JQ1 and target the tumor tissues.And then,JQ1 released from this nanoparticle could prevent OSCC growth inducing tumor cell apoptosis,inhibiting tumor angiogenesis and the polarization of M2 type macrophages.In conclusion,our date demonstrated the therapeutic ben-efits of FA-PEG-PLA-JQ1 against OSCC in vivo or in vitro,which could be a novel treatment strategy for OSCC in coming days.
      原文链接:
    • NETL
    • NSTL
    • 万方数据

    Restoring cellular calcium homeostasis to rescue ER stress by 1,2-bis(2-aminophenoxy)ethane-N,N,N',N'-tetraacetic acid acetoxymethyl ester-loaded lipid-mPLGA hybrid-nanoparticles for acute kidney injury therapy

    Jingwen ZhangJiahui YanYanan WangHong Liu...
    337-345页
    查看更多>>摘要：Early pathogenesis of ischemia-reperfusion(I/R)-induced acute kidney injury(AKI)is dominated by in-tracellular calcium overload,which induces oxidative stress,intracellular energy metabolism disorder,in-flammatory activation,and a series of pathologic cascaded reactions that are closely intertwined with self-amplifying and interactive feedback loops,ultimately resulting in cell damage and kidney failure.Cur-rently,most nanomedicines originate from the perspective of antioxidant stress,which can only quench existing reactive oxide species(ROS)but cannot prevent the continuous production of ROS,resulting in insufficient efficacy.As a safe and promising drug,BAPTA-AM is hydrolyzed into BAPTA by intracel-lular esterase upon entering cells,which can rapidly chelate with overloaded Ca2+,restoring intracel-lular calcium homeostasis,thus inhibiting ROS regeneration at the source.Here,we designed a KTP-targeting peptide-modified yolk-shell structure of liposome-poly(ethylene glycol)methyl ether-block-poly(L-lactide-co-glycolic)(mPLGA)hybrid nanoparticles(＜100nm),with the characteristics of high encap-sulation rate,high colloid stability,facile modification,and prolonged blood circulation time.Once the BA/mPLGA@Lipo-KTP was targeted to the site of kidney injury,the cholesteryl hemisuccinate(CHEMS)in the phospholipid bilayer,as an acidic cholesterol ester,was protonated in the simulated inflamma-tory slightly acidic environment(pH 6.5),causing the liposomes to rupture and release the BA/mPLGA nanoparticles,which were then depolymerized by intracellular esterase.The BAPTA-AM was diffused and hydrolyzed to produce BAPTA,which can rapidly cut off the malignant loop of calcium overload/ROS gen-eration at its source,blocking the endoplasmic reticulum(ER)apoptosis pathway(ATF4-CHOP-Bax/Bcl-2,Casp-12-Casp-3)and the inflammatory pathway(TNF-α-NF-κB-IL-6 axes),thus alleviating patholog-ical changes in kidney tissue,thereby inhibiting the expression of renal tubular marker kidney injury molecule 1(Kim-1)(reduced by 82.9％)and also exhibiting prominent anti-apoptotic capability(TUNEL-positive ratio decreased from 40.2％to 8.3％),significantly restoring renal function.Overall,this research holds huge potential in the treatment of I/R injury-related diseases.
      原文链接:
    • NETL
    • NSTL
    • 万方数据

    Cocktail nano-adjuvant enhanced cancer immunotherapy based on NIR-Ⅱ-triggered in-situ tumor vaccination

    Lilin FanYanwen FengJiang BianAnhong Chen...
    346-351页
    查看更多>>摘要：Second near-infrared(NIR-Ⅱ)light triggered in-situ tumor vaccination(ISTV)represents one of the most promising strategies in boosting the whole-body antitumor immunity.While most of previously devel-oped nano-adjuvants for NIR-Ⅱ-triggered ISTV are"all-in-one"formulations,which may indiscriminately damage both the tumor cells and the immune cells,limiting the overall effect of immune response.To overcome this obstacle,we designed a"cocktail"nano-adjuvant by physically mixing hyaluronidases(HAase)-decorated gold nanostars(HA)for NIR-Ⅱ light triggered in situ production of tumor-associated antigens and CpG functionalized gold nanospheres(CA)for immune cells activation.Compared to"all-in-one"formulation,the"cocktail"nano-adjuvants displayed a significantly stronger immune response on NIR-Ⅱ light induced dendritic cells(DCs)mutation and T cells differentiation,greater effect on tumor-growth inhibition,and higher efficacy in inhibition of pulmonary metastases.What is more,increasing the molar ratio of HA to CA led to an enhanced anticancer immune responses.This study highlight the nano-adjuvant formulation effects on the treatment of tumors with multiple targets.
      原文链接:
    • NETL
    • NSTL
    • 万方数据

    Cisplatin-appended BODIPY for near infrared Ⅱ fluorescent and photoacoustic imaging-guided synergistic phototherapy and chemotherapy of cancer

    Xuejian XingE PangShaojing ZhaoTangna Pan...
    352-357页
    查看更多>>摘要：Combining phototherapy and chemotherapy has been considered a promising modality for cancer ther-apy due to their synergistic effect.Herein,we developed three D-π-A-structured boron dipyrromethenes(BODIPYs)(named as B-B,B-C,and B-C-Pt).Due to their enlarged π-conjugated structure and high intramolecular charge transfer effect,the synthesized BODIPYs had photothermal conversion capability,and their absorption and fluorescence spectra were red-shifted.The cisplatin-appended BODIPY(B-C-Pt)exhibited good singlet oxygen(1O2)generation ability and near infrared(NIR)absorption and fluores-cence(λAbs=748 nm,λEm=947 nm).After being encapsulated by distearoyl phosphoethanolamine polyethyleneglycol 2000(DSPE-PEG-2000),which could inhibit the H-aggregation of B-C-Pt,the absorp-tion and fluorescence of the obtained B-C-Pt nanoparticles(NPs)were red-shifted to 762 and 985 nm,respectively.The 1O2 quantum yield and photothermal conversion efficiency of the B-C-Pt NPs were 4.0％and 40.6％,respectively.Moreover,B-C-Pt NPs had chemotherapeutic efficacy due to the presence of cis-platin.In vitro and in vivo studies further demonstrated that B-C-Pt NPs had synergistic therapeutic ef-ficacy.Together,B-C-Pt NPs could be employed in NIR Ⅱ fluorescent and photoacoustic imaging-guided synergistic phototherapy and chemotherapy for cancer treatment.
      原文链接:
    • NETL
    • NSTL
    • 万方数据

    High-throughput fluorescent screening of thioredoxin reductase inhibitors to inhibit Mycobacterium tuberculosis

    Fei YanXin ZhaoRuibo LiXiuyan Han...
    358-362页
    查看更多>>摘要：Tuberculosis(TB)is a chronic infectious disease,which is caused by the pathogen Mycobacterium tubercu-losis(Mtb)and reemerged as a global health risk with a significant proportion of multi-drug resistant and extensively drug resistant TB cases.It is very urgent to find some novel high-confidence drug targets in Mtb for discovering the effective anti-TB agents.Thioredoxin reductase(TrxR)has been identified to be a highly viable target for anti-TB drugs for its important role in protecting the pathogen from thiol-specific oxidizing stress,regulating intracellular dithiol/disulfide homeostasis and DNA replication and repair.In the present work,a near-infrared(NIR)fluorescent probe DDAT was developed for the detection of TrxR activity and used to high-throughput screen the TrxR inhibitors from natural products.Two screened TrxR inhibitors from Sappan Lignum and microbial metabolites that were further used to inhibit Mycobacterium tuberculosis.All the results indicate that DDAT is a practical fluorescent molecular tool for the discovery of potential anti-TB drugs.
      原文链接:
    • NETL
    • NSTL
    • 万方数据

    mtDNA-triggered pH response signal-amplified fluorescent probe for multiple cell discrimination

    Tianping XiaYanxian HouZhuoran XiaGengwen Chen...
    363-368页
    查看更多>>摘要：Developing fluorescence probes with multiple responses has vital significance but remains challeng-ing.Herein,for the first time,we present a mitochondrial DNA(mtDNA)-triggered pH response signal-amplified fluorescent probe(QCY-DBT)for multiple cell detection.The probe exhibited a large stokes shift(229 nm),excellent DNA selectivity over RNA,and ultrasensitivity of detection limit(DL;74.0ng/mL).Thus,QCY-DBT was successfully applied to analyze multiple human peripheral blood cells and visualize mtDNA in healthy and apoptotic cells.In the tumor acidic environment(pH6.0-7.0),the absorbance of QCY-DBT at 436 nm increased,and the fluorescence signal(665 nm)was amplified by mtDNA,which enabled the direct observation of tumor cells.Our study provides help in designing smart probes with multiple responses for efficient abnormal cell detection.
      原文链接:
    • NETL
    • NSTL
    • 万方数据