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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。
正式出版
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    Oligomeric donor with appropriate crystallinity for organic solar cells

    Kaiming YangMin LvYanhong ChangKun Lu...
    289-294页
    查看更多>>摘要：Improving the performance of all-small-molecule organic solar cells(ASM-OSCs)largely depends on the design and application of novel donors with appropriate crystallinity.Extending molecular conju-gation is an effective method for regulating molecular stacking and crystallinity.In this work,we suc-cessfully designed and synthesized two novel acceptor-donor-donor-donor-acceptor(A-D-D-D-A)type oligomeric donors with three dithieno[2,3-d:2',3'-d']benzo[1,2-b:4,5-b']dithiophene(DTBDT)as the cen-tral unit,named as 3DTBDT-Cl and 3DTBDT,depending on with and without chlorine substitution on the thiophene side chains.We found that the introduction of chlorine atoms makes the blend films display stronger crystallinity but with large-scale phase separation morphology and more defects,which eventu-ally leads to a power conversion efficiency(PCE)of only 10.83％,whereas the blend films based 3DTBDT with appropriate crystallinity achieved 13.74％PCE.Compared with 3DTBDT-Cl/L8-BO,the 3DTBDT/L8-BO films exhibited a nanoscale bi-continuous interpenetrating network morphology with a smaller do-main size and more suitable crystallinity,which guarantees the corresponding devices obtained more ef-ficient exciton dissociation,efficient charge transport,reduced bimolecular recombination,and performed more balanced carrier mobility.These results demonstrated that regulating the crystallinity of oligomeric donors to obtain the desired phase separation morphology in the blend films could facilitate further im-proving the performance of ASM-OSCs.
      原文链接:
    • 万方数据
    • 维普

    A nanoagent for concurrent therapy of breast cancer bone metastasis and cancer-induced bone pain through SLC7A11 interruption and photodynamic therapy

    Qi FuZhongming LianMengya NiuYaru Huang...
    295-299页
    查看更多>>摘要：Bone metastasis,a life-threatening complication of advanced breast cancer,is often accompanied by debilitating pain(cancer-induced bone pain,CIBP)that severely impairs life quality and survival.The concurrent treatment of bone metastases and CIBP remains a clinical challenge because the therapeu-tic options are limited.In this study,we construct a near-infrared light-activated nano-therapeutic sys-tem to meet this conundrum.In detail,sorafenib(SRF)and photosensitizer(chlorin e6,Ce6)are encap-sulated into mesoporous hydroxyapatite nanoparticles(HANPs),which are further functionalized with hyaluronic acid(HA)to obtain HA-SRF/Ce6@HANPs system.The designed nanoplatform destroys tumor cells in vitro and in vivo via the synergism of SRF(interrupting the exchange of cystine/glutamate by inhibiting SLC7A11)and photodynamic therapy(PDT,inducing reactive oxygen species generation).The decrease in tumor burden and reduction of extracellular glutamate significantly attenuate CIBP in mice model with developing bone cancer.Moreover,the combination of HA-SRF/Ce6@HANPs and PDT inhibit osteoclasts activation,promote osteoblast differentiation and accelerate bone repair.Overall,the nanoa-gent with good biocompatibility may provide an effective therapy method for the concurrent treatment of breast cancer bone metastasis and CIBP.
      原文链接:
    • 万方数据
    • 维普

    Automated screening of primary cell-based aptamers for targeting and therapy of pancreatic cancer

    Zhukang GuoBaijiang JinYile FangLian Jin...
    300-304页
    查看更多>>摘要：Although it has been developed for many years,nucleic acid aptamer screening technology still fails to be widely used,a considerable part of it is due to the variability of tumor cell morphology,which leads to the use of immortalized cell lines in the laboratory to screen nucleic acid aptamers for recognition ability of tumor cells in the diseased body.To address this,primary cells that can be stably passaged were iso-lated and extracted from spontaneous tumors of genetically engineered pancreatic ductal adenocarcinoma model mice in this study.Next,an automated screening instrument for nucleic acid aptamers developed autonomously by our group was used to perform efficient aptamer screening using a limited number of cells,and the obtained nucleic acid aptamers were affinity verified at the cellular level.Finally,to an-swer the question of the cell growth environment difference on the recognition ability of nucleic acid aptamers,we verified its targeting ability to tumors in vivo on a nude mice xenograft tumor model,and further used a common antitumor drug doxorubicin combined with nucleic acid aptamers to verify the drug loading ability of this aptamer combined with the targeting therapeutic ability.
      原文链接:
    • 万方数据
    • 维普

    Tumor-targeted self-assembled micelles reducing PD-L1 expression combined with ICIs to enhance chemo-immunotherapy of TNBC

    Hongda ZhuKai MaRui RuanChaobo Yang...
    305-310页
    查看更多>>摘要：Immune checkpoint inhibitors(ICls)therapy targeting programmed cell death ligand 1(PD-L1)and pro-grammed death protein 1(PD-1)had exhibited significant clinical benefits for cancer treatment such as triple negative breast cancer(TNBC).However,the relatively low anti-tumor immune response rate and ICIs drug resistance highlight the necessity of developing ICIs combination therapy strategies to improve the anti-tumor effect of immunotherapy.Herein,the immunomodulator epigallocatechin gallate palmitate(PEGCG)and the immunoadjuvant metformin(MET)self-assembled into tumor-targeted micelles via hy-drogen bond and electrostatic interaction,which encapsulated the therapeutic agents doxorubicin(DOX)-loaded PEGCG-MET micelles(PMD)and combined with ICIs(anti-PD-1 antibody)as therapeutic strategy to reduce the endogenous expression of PD-L1 and improve the tumor immunosuppressive microenvi-ronment.The results presented that PMD integrated chemotherapy and immunotherapy to enhance an-titumor efficacy in vitro and in vivo,compared with DOX or anti-PD-1 antibody for the therapy of TNBC.PMD micelles might be a potential candidate,which could remedy the shortcomings of antibody-based ICIs and provide synergistic effect to enhance the antitumor effects of ICIs in tumor therapy.
      原文链接:
    • 万方数据
    • 维普

    Evaluation of erastin synergized cisplatin anti-nasopharyngeal carcinoma effect with a glutathione-activated near-infrared fluorescent probe

    Rong HeDandan TangNingge XuHeng Liu...
    311-316页
    查看更多>>摘要：Nasopharyngeal carcinoma(NPC),a malignant tumor originating from the nasopharynx,is one of the common malignant tumors of the head and neck.There are significant geographical differences in the incidence of nasopharyngeal carcinoma,with a high incidence in China and Southeast Asian countries.Herein,we designed and synthesized a novel near-infrared fluorescent(NIRF)probe to detect glutathione(GSH)in cellular and tumor environments using semi-naphthofluorescein(SNAFL)as the fluorescent molecular backbone and 2-fluoro-4-nitrobenzenesulfonate as the recognition moiety.Upon reaction with GSH,SNAFL-GSH emitted a fluorescence signal,and its emission wavelength at 650 nm was remark-ably enhanced.The results of selectivity experiments indicated that SNAFL-GSH was able to discriminate GSH from Cys,Hcy,and H2S.Moreover,SNAFL-GSH could image both endogenous and exogenous GSH and distinguish normal and cancer cells by fluorescence signal difference.At the cellular level,cisplatin(DDP)-induced ferroptosis and inhibition of proliferation of various NPC cell lines(CNE2,CNE1,5-8F cells)by erastin combined with DDP were visualized with the help of SNAFL-GSH.In a mouse tumor xenograft model,we successfully employed SNAFL-GSH for the evaluation of the efficacy of erastin combined with DDP in the treatment of NPC.More importantly,the probe could image cancerous tissue sections from NPC patients with an imaging depth of approximately 80 μm.It was foreseen that SNAFL-GSH offered great potential for application in the diagnosis and evaluation of the therapeutic efficacy of NPC,and these results would also provide new ideas for the clinical treatment of NPC.
      原文链接:
    • 万方数据
    • 维普

    Supramolecular complex glycoconjugate vaccine generates self-enhancement effects for carbohydrate antigen delivery

    Han LinYanchun LiKun ZhouDan Li...
    317-322页
    查看更多>>摘要：Targeting delivery of tumor-associated carbohydrate antigen(TACA)-based vaccine to antigen-presenting cells(APCs)mediated by endogenous antibodies can improve the immunogenicity of TACA.However,an essential requirement of this approach is to generate high titers of endogenous antibodies in vivo through pre-immunization,which complicates the immunization procedure and may cause side effects.Herein,we report a new generation of APC-targeting TACA-based supramolecular complex vaccine,as-sembled by sialyl Thomsen-nouveau-bovine serum albumin-adamantine(sTn-BSA-Ada)and heptavalent rhamnose(Rha)-modified β-cyclodextrin(β-CD)via host-guest interaction.The complex vaccine re-tained anti-Rha antibodies recruiting capability and facilitated the APCs uptake of the vaccine via the interaction of the Fc-domain with the Fc receptors on APCs.We demonstrate that direct immuniza-tion of complex vaccine elicited anti-Rha and anti-sTn specific immune response synchronously,gen-erating a novel self-enhancement effect that can improve the antigen delivery to APCs in high efficacy.The structure-activity relationship(SAR)study proved that complex vaccine 4 with polyethylene glycol 6(PEG6)linker in host molecule provoked a robust and specific sTn immune response comparable to the pre-immunization approach.The antisera induced by complex vaccine,either through direct immuniza-tion or pre-immunization,exhibited equal potency of cytotoxicity against the sTn expression cancer cells.This study provides a general platform for TACA-based vaccines with self-enhancement effects without the need for pre-immunization.
      原文链接:
    • 万方数据
    • 维普

    Elaborately engineering of lipid nanoparticle for targeting delivery of siRNA and suppressing acute liver injury

    Qiu WangQikun JiangDan LiZimeng Yang...
    323-328页
    查看更多>>摘要：Small interfering RNA(siRNA)-based gene silencing has been considered as a potential therapy modality against inflammatory diseases.Nevertheless,the effective delivery of siRNA to desired destination still re-mains challenging due to poor stability,high molecular weight and negative charge.Currently,ionizable lipid nanoparticle(LNP)has been extensively used as vector for effective delivery of siRNA.Herein,we re-port a mannose-modified LNP(M-MC3 LNP@TNFα)loading tumor necrosis factor α(TNFα)siRNA for tar-geting liver macrophages,achieving effectively inhibit acute liver injury.The M-MC3 LNP@TNFα not only increases the internalization of LNP by macrophages,but also enhances the gene silencing efficiency of TNFα in vitro.Additionally,the M-MC3 LNP@TNFα exhibits higher accumulation in liver of healthy mice than that of MC3 LNP@TNFα(un-modified LNP)owing to the targeting effect of mannose.As expected,the M-MC3 LNP@TNFα significantly suppresses the expression of TNFα and ameliorates liver damage in acute liver injury model.Such a LNP targeting siRNA delivery holds great potential for the treatment of diseases associated with liver in the future.
      原文链接:
    • 万方数据
    • 维普

    Remodeling the tumor microenvironment by vascular normalization and GSH-depletion for augmenting tumor immunotherapy

    Jin WangQingqing ZhangYanchen LiXiaoyan Pan...
    329-334页
    查看更多>>摘要：Remodeling tumor microenvironment(TME)is a very promising and effective strategy to enhance the effects of chemotherapy,photodynamic therapy,and immunotherapy.Normalization of tumor vasculature as well as depletion of glutathione(GSH)can improve the TME.Here,we developed a novel therapeutic nanoparticle functional enzyme ultra QDAU5 nanoparticles(FEUQ Nps)based on a fluorescence-on and releasable strategy by combining a vascular normalization inducer,a GSH depleting agent,and an acti-vated fluorophore.In which the cleavage of disulfide bonds releases active molecules that induce vascu-lar normalization and improve the hypoxic microenvironment.In addition,it may deplete GSH in cancer cells,thus inducing the production of reactive oxygen species(ROS)and lipid peroxide(LPO)and pro-moting iron toxicity.It may also lead to endoplasmic stress and release of calmodulin,which activates the immune system.Meanwhile,quenched fluorophores are turned on in the presence of galactosidase(GLU)for tumor-specific labeling.In summary,we developed novel therapeutic agent nanoparticles with the function of vascular normalization inducers to achieve specific labeling of hepatocellular carcinoma while exerting efficient antitumor effects in vivo.
      原文链接:
    • 万方数据
    • 维普

    Paclitaxel-lipid prodrug liposomes for improved drug delivery and breast carcinoma therapy

    Xin WuXinmei ChenXinyu WangHaisheng He...
    335-340页
    查看更多>>摘要：Paclitaxel(PTX)is widely applied for the treatment of unresectable and metastasis breast carcinoma as well as other cancers,whereas its efficacy is always impeded by poor solubility.Liposomes are one kind of the most successful drug carriers which are capable of solubilizing PTX and improving patients'tol-erance owing to excellent biocompatibility and biodegradability.However,poor compatibility between PTX and liposomes compromises the stability,drug loading and anti-tumor capacity of liposomal for-mulations.To address this issue,three lipids with various chain lengths,namely,myristic acid(MA,14C),palmitic acid(PA,16C)and stearic acid(SA,18C),were conjugated to PTX via ester bonds and the synthe-sized prodrugs with high lipophilicity were further formulated into liposomes,respectively.All liposomes show high stability and drug loadings,as well as sustained drug release.The chain lengths of lipids are negatively correlated with drug release and enzymatic conversion rates,which further impact the phar-macokinetics,tumor accumulation,and anti-tumor efficacy of liposomal PTX.Neither rapid nor slow drug release facilitates high tumor accumulation as well as anti-tumor efficacy of PTX.Among all liposomes,PTX-PA-loaded liposomes show the longest circulation and highest tumor accumulation of PTX and exert the most potent anti-tumor capacities in vivo,owing to its moderate drug release and enzymatic conver-sion rate.Witnessing its superior safety,PTX-PA liposomes hold potential for further clinical translation.
      原文链接:
    • 万方数据
    • 维普

    Natural polysaccharide-based smart CXCR4-targeted nano-system for magnified liver fibrosis therapy

    Liqiong SunXinping LuoChenxi ZhouZhanwei Zhou...
    341-346页
    查看更多>>摘要：Activated hepatic stellate cells(aHSCs),the main source of extracellular matrix deposition,are key targets in liver fibrosis.However,no effective drug specific to aHSCs has been clinically applied due to poor drug delivery efficiency.Herein,we designed a CXC chemokine receptor 4(CXCR4)-targeted reactive oxygen species(ROS)-responsive platform AMD-Dex-ROS-responsive-sorafenib(ARS)based on natural polysac-charide and thioctic acid frame,which can deliver anti-fibrosis drug represented by sorafenib specifically to aHSCs on account of CXCR4 over-expression on aHSCs,and smartly disassemble via ROS-responsive thioketal rupture relying on high intracellular ROS in HSCs,realized on-demand drug release and effec-tive liver fibrosis reversion.Notably,in this platform,the CXCR4 antagonist AMD3100 not only enhanced aHSCs targeting efficiency of sorafenib but also effectively magnified the aHSCs elimination of sorafenib by blocking stroma cell derived factor-1(SDF-1)/CXCR4-induced aHSCs protection,resulting in synergis-tic anti-fibrosis effect.The platform provided a new approach for drug delivery system design and liver fibrosis treatment.
      原文链接:
    • 万方数据
    • 维普