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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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    Design,synthesis,and biological evaluation of benzo[4,5]thieno[2,3-d]pyrimidine derivatives as novel HIV-1 NNRTIs

    Bairu MengZongji ZhuoHan YuSining Tao...
    344-348页
    查看更多>>摘要：Inspired by our previous studies to discover novel human immunodeficiency virus-1(HIV-1)non-nucleoside reverse transcriptase inhibitors(NNRTIs)by targeting the tolerant region Ⅱ of the NNRTIs binding pocket(NNIBP),a series of novel benzo[4,5]thieno[2,3-d]pyrimidine derivatives were designed through structure-based drug design as novel potent HIV-1 NNRTIs.The results showed that compound 16b was the most active inhibitor,exhibiting 50％effective concentration(EC50)values from 0.021 μmol/L to 0.298 μmol/L against wild-type(WT)and a panel of NNRTIs-resistant HIV-1 strains.Moreover,16b was demonstrated with a significantly low 50％cytotoxicity concentration(CC50)value(＞200μmol/L)and high selectivity index(SI)values.In addition,16b yielded moderate reverse transcriptase(RT)enzyme inhibi-tion with a 50％inhibition concentration(IC50)value of 0.183 μmol/L,which demonstrated that it acted as HIV-1 NNRTIs.The binding mode of 16b with RT was also illustrated via molecular docking.Overall,this work provided a novel lead compound for developing potent HIV-1 NNRTIs.
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    Development of functional dye with redshifted absorption based on Knoevenagel condensation at 1-site in phenyl[b]-fused BODIPY

    Tianze WangJunyi RenDongxiang ZhangHuan Wang...
    349-352页
    查看更多>>摘要：Integrating ring-fused modification with π-conjugated extension is an effective approach for designing,synthesizing,and application for novel borondipyrromethene(BODIPY)structures.In this work,based on phenyl[b]-fused BODIPY,we made reasonable modification of the methyl group at 1-site to gener-ate dye NBDP.NBDP possessed near-infrared region(NIR)absorption and emission properties,and the intramolecular charge transfer(ICT)resulted in low fluorescence.Whereas,heat energy is evidently re-leased in the presence of light,which can be exploited for intracellular photothermal therapy via the cell apoptosis process,reducing the inflammatory side-effects induced by necrosis.This research provides a crucial foundation for the novel molecule via BODIPY multi-directional alteration and its potential appli-cation in anti-tumor phototherapy.
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    Discovery of unusual phloroglucinol-triterpenoid adducts from Leptospermum scoparium and Xanthostemon chrysanthus by building blocks-based molecular networking

    Jinyan ZhangFen LiuQian JinXueyi Li...
    353-357页
    查看更多>>摘要：The first phloroglucinol-triterpenoid hybrids,myrtphlotritins A-E(1-5),were rapidly recognized and iso-lated from two species of Myrtaceae by employing the building blocks-based molecular network(BBMN)strategy.Compounds 1-5 featured new carbon skeletons in which phloroglucinol derivatives were cou-pled with lupane-and dammarane-type triterpenoids through different linkage patterns.Their structures and absolute configurations were elucidated by comprehensive analysis of spectroscopic data and quan-tum chemical calculations.Biosynthetic pathways for compounds 1-5 were proposed on the basis of the coexisting precursors.Guided by the biogenetic pathways,the biomimetic synthesis of compound 1 was also achieved.Additionally,compounds 2,3,and 5 exhibited potent antiviral activities against herpes simplex virus type-1(HSV-1)infection,and compounds 2 and 5 displayed significant anti-inflammatory activities on RAW264.7 cells.
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    Drug-loading ZIF-8 for modification of microporous bone scaffold to promote vascularized bone regeneration

    Xin ZhangJunyu ChenXiang PeiLinxin Yang...
    358-364页
    查看更多>>摘要：Surface modification of microporous bone scaffolds using nanoparticles has been broadly studied in bone tissue engineering.Aiming at improving vascularized bone regeneration(VBR),zeolitic imidazo-late framework-8(ZIF-8)was encapsulated with dimethyloxallyl glycine(DMOG)and the drug-carrying nanoparticles(D@Z)could be uniformly coated onto the surface of the bone scaffold.The osteogenic and angiogenic actions of D@Z are closely correlated with the amount of slowly released DMOG,and in general,exhibited a favorable association.Then,the D7.5@Z group,which showed the greatest capacity to induce in vitro osteogenesis-angiogenesis coupling,was utilized for surface modification of the bone scaffold.Biological processes including phosphate-containing compound metabolic process,cell differen-tiation,cell proliferation and cell motility might contribute to enhanced ability to induce VBR by the coated scaffold and signaling pathways such as Rap1,Ras,phosphatidylinositol 3-kinase/protein kinase B(PI3K-AKT)and vascular endothelial growth factor(VEGF)signaling pathways participated in these pro-cesses.Finally,as depicted by in vitro real time-polymerase chain reaction(RT-PCR),Western blot(WB)and in vivo cranial bone defect model,the microporous scaffold coated with nano-D7.5@Z greatly pro-moted VBR.To conclude,nano-D@Z has significant promise for practical application in modification of microporous bone scaffolds to enhance VBR,and DMOG loading quantity has a beneficial influence on D@Z to improve osteogenesis-angiogenesis coupling.
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    A lipid droplets-targetable fluorescent probe for polarity detection in cells of iron death,inflammation and fatty liver tissue

    Xing TianDi WuWanheng WeiGuifu Dai...
    365-369页
    查看更多>>摘要：Abnormal accumulation and metabolism of lipid droplets can lead to a variety of diseases.Polarity,a key parameter of the microenvironment,is closely associated with many diseases and dysfunctions in the body.It is important to elucidate the relationship between the physiological activity of lipid droplets(LDs)and the polarity of the microenvironment.In this work,based on push-pull mechanism,a fluorescent probe(E)-3-(5-(4-(diphenylamino)phenyl)thiophen-2-yl)-1-(2-hydroxyphenyl)prop-2-en-1-one(PPTH)with aggregation-induced emission(AIE)properties for the detection of polarity changes in cells was synthesized.PPTH not only visualize intracellular polarity fluctuation of iron death and inflam-mation but also distinguish between normal and fatty liver tissue.
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    A mitochondria-targeted H2S-activatable fluorogenic probe for tracking hepatic ischemia-reperfusion injury

    Bin FangJiaqi YangLimin WangHaoqin Li...
    370-375页
    查看更多>>摘要：Hepatic ischemia-reperfusion injury(HIRI)is the cause of postoperative hepatic dysfunction and failure,and even death.As an important biological effector molecule,hydrogen sulfide(H2S)of mitochondria as a gasotransmitter that is usually used to protect against acute HIRI injury.However,the exact rela-tionship between HIRI and mitochondrial H2S remains tangled due to the lack of an effective analytical method.Herein,we have fabricated a mitochondria-targeted H2S-activatable fluorogenic probe(Mito-GW)to explore the stability of mitochondrial H2S and track the changes of mitochondrial H2S during the HIRI.By virtue of pyridinium electropositivity and its amphiphilicity,Mito-GW could accumulate in mitochon-dria.It goes through an analyte-prompted immolation when reacts with H2S,resulting in the releasing of the fluorophore(GW).Therefore,the extent of Mito-GW conversion to GW can be used to evaluate the changes of mitochondrial H2S level in living cells and tissues.As proof-of-principle,we have used Mito-GW to demonstrate the mitochondria H2S-levels increase and then decrease during HIRI in vitro and in vivo.Our research highlights the tremendous potential of Mito-GW as a mitochondrial H2S fluorogenic probe in elucidating the pathogenesis of HIRI,providing a powerful tool for promoting future research on hepatology.
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    An AIEgen nano-assembly for simultaneous detection of ATP and H2S

    Jia-Mei QinXue LiWei LangFu-Hao Zhang...
    376-379页
    查看更多>>摘要：A new aggregation-induced emission(AIE)-based fluorescence sensor,TPEPy-SS-C14,for simultaneous recognition of adenosine triphosphate(ATP)and hydrogen sulfide(H2S)has been reported via the aggregation-disaggregation mechanism.The probe self-assembles nano-structure aggregations in aqueous solution.It shows fluorescence turn-on response toward ATP for the complexation-enhanced aggregation,but leads to fluorescence quenching of H2S for cleavage the aggregations.
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    Five quinolizidine alkaloids with anti-tobacco mosaic virus activities from two species of Sophora

    Ji ZhangTong ZhangQiao AnPeng Zhang...
    380-384页
    查看更多>>摘要：Three novel matrine-type alkaloids(1-3)and two unprecedented aloperine-type alkaloids(4 and 5)were isolated from the root of Sophora tonkinensis and the seeds of Sophora alopecuroides respectively.Notably,compound 1 possessed an unprecedented 6/5/6 tricyclic skeleton,while compounds 2 and 3 characterized by rare 6/6/5/6 tetracyclic system and 6/6/6/6/6 pentacyclic system respectively.Moreover,compound 4 possessed an unprecedented 6/7/6/6 tetracyclic core,and compound 5 characterized by rare 6/6/6/6 tetracyclic skeleton.Their structures were elucidated by comprehensive spectroscopic data analysis and electronic circular dichroism(ECD)calculations.Biological tests indicated that compound 5 displayed sig-nificant anti-tobacco mosaic virus(TMV)activity compared with the positive control ningnanmycin.
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    Nanomedicine integrating the lipidic derivative of 5-fluorouracil,miriplatin and PD-L1 siRNA for enhancing tumor therapy

    An LuYuhao GuoYi YanLin Zhai...
    385-391页
    查看更多>>摘要：Immunosuppressive microenvironments present critical problems in clinical chemotherapy.To regulate the tumor immune microenvironment for enhancing antitumor effect,a combination of immune check-point inhibitors(ICIs)with chemotherapeutics has been applied clinically.In this study,miriplatin(MiPt),the lipidic derivative of 5-fluorouracil(Fu-OA),as well as the programmed death ligand 1(PD-L1)target siRNA(siPD-L1)were integrated into Lip-Pt/Fu@siPD-L1 nanoparticles(NPs)for chemo-immunotherapy.In vitro results showed that Lip-Pt/Fu@siPD-L1 NPs could exhibit effective siRNA gene silencing and pro-mote the phagocytosis of tumor cells by macrophages.Furthermore,in vivo results revealed that Lip-Pt/Fu@siPD-L1 NPs showed significantly higher anti-tumor efficiency than that of the physical mixing of MiPt,5-fluorouracil,and Lip@siPD-L1 NPs(delivery of siPD-L1 by liposomes).The best anti-tumor effi-ciency of Lip-Pt/Fu@siPD-L1 NPs resulted from the synergistic immunotherapeutic effects of MiPt and siPD-L1 based on the inhibition of CD47 expression and the downregulation of PD-L1 in tumor cells,which elicited a robust anti-tumor immune response through the activation of macrophage phagocyto-sis and immune checkpoint inhibition.The Lip-Pt/Fu@siPD-L1 NPs provide a potential strategy for tumor chemo-immunotherapy.
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    Reversing artemisinin resistance by leveraging thermo-responsive nanoplatform to downregulating GSH

    Yong-Dan ZhaoYidan WangRongrong WangLina Chen...
    392-397页
    查看更多>>摘要：Artemisinin(ART)resistance has been an emerging clinical problem,severely compromising antimalar-ial efficacy and threatening the global malaria elimination campaign.Albeit intensive studies about the molecular mechanism for ART resistance are under way,no effective therapeutic targets for reversing resistance have been applied.Here,we explore glutathione(GSH)as a therapeutic target to develop a thermo-responsive nanoplatform to specifically co-deliver ART and GSH synthesis inhibitor(L-buthionine sulfoximine,BSO)in a sustained manner,effectively reversing ART resistance in vivo.By combining with BSO,ART exerts increased antimalarial activity with reduced half-maximal inhibitory concentration(IC50)by 7.43-fold in ART-resistant strains.This work reveals that the GSH in ART-resistant parasites can be a promising therapeutic target for reversing ART resistance,paving the way for developing drug candidates and intelligent nanomedicines in malaria therapy.
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