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  • Qian Li, Xiaoyun Lu
    Chinese Chemical Letters. 2020, 31(6): 1357-1365.

    With the emergence of multidrug-resistant tuberculosis and extensive drug-resistant tuberculosis strains, there is an urgent need to develop novel drugs for the treatment of tuberculosis. The respiratory chain is a promising target for the development of new antimycobacterial agents, and a growing number of compounds have been reported and some have entered clinical trials. In this review, we summarize the main features and the electron transfer process of the mycobacterial respiratory chain, and the recent progress in the search for new small molecule inhibitors targeting the three main potential targets in the respiratory chain of Mycrobacterium tuberculosis. Our emphasis is on the optimization strategy of QcrB inhibitors and the challenges of developing QcrB inhibitors as antituberculosis drugs due to the alternate bd-type oxidase oxidative compensation pathway are discussed.

  • Wenqi Yu, Shevtsov Maxim, Xianchun Chen, Huile Gao
    Chinese Chemical Letters. 2020, 31(6): 1366-1374.

    Recent days, aggregatable nanoparticles, which can specifically respond to certain stimulus, have shown great potential in tumor-targeted drug delivery with prolonged retention and deeper penetration. In this review, we summarize recent advances in design of aggregatable nanoparticles by different stimuli. Internal (pH and enzyme) and external (light, temperature and ROS) stimuli are introduced for a comprehensive description. Moreover, the aggregated nanoparticles usually exhibit photothermal, photoacoustic, PET and enhanced MRI contrast, which is also described. In the end, we discuss about the potential applications and challenges for the future clinical translation.

  • Hu Chen, Hongwei Cheng, Wenying Wu, Dengfeng Li, Jingsong Mao, Chengchao Chu, Gang Liu
    Chinese Chemical Letters. 2020, 31(6): 1375-1381.

    Transcatheter hepatic artery chemoembolization (TACE) is a universal treatment for patients with hepatocellular carcinoma (HCC) that inhibits tumor growth by cutting off the blood supply and provides chemotherapeutics locally to the tumor. The strategy of combining TACE formulation with image-guided ablation holds tremendous potential, but patient tolerance and undesired toxicity/immunosuppression remains a challenge. The application of nanotechnology in TACE opens new doors for the treatment of HCC. Strikingly, nanomaterials or nano-drugs dispersed in the TACE formulation can effectively improve the delivery efficiency of drugs by achieving both controlled and continuous release. In addition, the utilization of multifunctional nanoparticles can provide guidance and monitoring for various advanced imaging methods for TACE treatment, and can realize the combination therapy of thermal ablation, microwave ablation, in situ radiotherapy, and other therapies, greatly expanding the therapeutic strategies available for HCC treatment. Here, the current exploration of nanotechnology in TACE of HCC is briefly summarized and the challenges of TACE with nanoformulations for clinical translation are comprehensively discussed.

  • Hui Zhou, Shanshan Li, Xiaodong Zeng, Mengxian Zhang, Lin Tang, Qianqian Li, Deliang Chen, Xianli Meng, Xuechuan Hong
    Chinese Chemical Letters. 2020, 31(6): 1382-1386.

    Fluorescence imaging in the second near-infrared window (NIR-II, 1000-1700 nm) is a promising modality for real-time imaging of cancer and image-guided surgery with superior in vivo optical properties. So far, very few NIR-II fluorophores have been reported for in vivo biomedical imaging of chemically-induced spontaneous breast carcinoma. Herein, a NIR-II fluorescent probe CH1055-F3 with the nucleolin-targeted tumor-homing peptide F3 was demonstrated to preferentially accumulate in 4T1 tumors. More importantly, CH1055-F3 exhibited specific NIR-II signals with high spatial and temporal resolution, strong tumor uptake, and remarkable NIR-II image-guided surgery in dimethylbenzan-thracene (DMBA)-induced spontaneous breast tumor rats. This report presents the first tumor-homing peptide-based NIR-II probe to diagnose transplantable and spontaneous breast tumors by the active targeting.

  • Yingxue Li, Bo Zeng, Yujie Yang, Huageng Liang, Yanbing Yang, Quan Yuan
    Chinese Chemical Letters. 2020, 31(6): 1387-1391.

    Bladder cancer is the most common malignant tumor in the urinary system, with high morbidity, mortality and recurrence after surgery. However, current bladder cancer urine diagnosis methods are limited by the low accuracy and specificity due to the low abundance of bladder cancer biomarkers in the urine with complex biological environments. Herein, we present a high stability indium gallium zinc oxide field effect transistor (IGZO-FET) biosensor for efficient identification of bladder cancer biomarkers from human urine samples. The recognition molecular functionalized IGZO-FET biosensor exhibits stable electronic and sensing performance due to the large-area fabrication of IGZO thin-film FET. Owing to the excellent electrical performance of IGZO-FET, the IGZO-FET biosensor exhibits high sensitivity and extremely low detection limit (2.7 amol/L) towards bladder cancer biomarkers. The IGZO-FET biosensor is also able to directly detect bladder tumor biomarker in human urine with high sensitivity and specificity, and could differentiate bladder cancer patients' urine samples from healthy donors effectively. These results indicate that our designed high-performance biosensor shows great potential in the application of portable digital bladder cancer diagnosis devices.

  • Ge Song, Zonglin Yi, Lijing Xie, Zhihong Bi, Qian Li, Jingpeng Chen, Qingqiang Kong, Chengmeng Chen
    Chinese Chemical Letters. 2020, 31(6): 1392-1397.

    Two-dimensional (2D) heterostructural Ni2P/rGO is successfully fabricated by in-situ phosphating selfassembled NiO/rGO composites and shows the enhanced electrochemical performances. In this design, the rGO sheets effectively reduce the lattice strain created during the phase transformation from NiO to Ni2P, thereby maintaining ultrathin nanostructures of Ni2P. The resulting Ni2P/rGO layered heterostructure gives the composite plenty of pores or channels, good electrical conductivity and well-exposed active sites. Density functional theory (DFT) calculation further demonstrates that the Fermi energy level and electron localize of near Ni atoms in Ni2P is higher than that of NiO, which endow Ni2P with faster and more reversible redox reactivity in dynamic. Benefiting from their structural and compositional merits, the as-synthesized Ni2P/rGO exhibits high specific discharge capacity and excellent rate performance. Furthermore, a hybrid supercapacitor built with Ni2P/rGO and activated carbon shows a high specific energy of 38. 6 Wh/kg at specific power of 375 W/kg.

  • Jiajia Chen, Huajian Gao, Zhihao Li, Yingxue Li, Quan Yuan
    Chinese Chemical Letters. 2020, 31(6): 1398-1401.

    Metalloenzymes which employ metal species and organic ligands as central active sites play significant roles in various biological activities. Development of artificial metalloenzymes can help to understand the related physiological mechanism and promote the applications of metalloenzymes in biosynthesis, energy conversion and biosensing. In this work, inspired by the active sites of ferriporphyrin-based metalloenzymes, Fe-MOFs by using ferric as the metal center and a porphyrin analog as the organic ligand were developed as an artificial metalloenzyme. The Fe-MOFs exhibit high peroxidase-like catalytic activity with excellent long-term stability. Moreover, highly sensitive biosensors were built to detect H2O2 and glucose based on the Fe-MOFs. Such MOFs-based artificial metalloenzyme offers an efficient strategy for the development of highly stable and efficient metalloenzymes, showing great potential in catalysis, energy transfer, biosensing and medical diagnosis.

  • Jianfang Cao, Wen Sun, Jiangli Fan
    Chinese Chemical Letters. 2020, 31(6): 1402-1405.

    A systematic spectral analysis was presented for bishemicyanine dyes (Hsd and D2) and monohemicyanine dyes (Hs and DSMI). The bishemicyanine dyes displayed long emission wavelengths, large Stokes shifts, low background quantum yields in aqueous solutions and high sensitivity in viscous environments. Better understanding of the structure-property relationships could benefit the design of improved dyes. Computational studies on these dyes revealed the three conjugated forms of bishemicyanines are in equilibrium due to two positive charges and a branched bulk substituent. Bishemicyanines possessed obviously lower rotating energy barrier of C-C bond rotation compared to the monohemicyanine dyes. Moreover, the synergetic effects of the rotation about the ϕ4 bond, ϕ5 bond and ϕ7 bond of the bishemicyanines (Hsd and D2) lead to lower fluorescence quantum yields in a free state and larger fluorescence quantum yield enhancements in viscous environment compared to that of monohemicyanine dyes (Hs and DSMI). The results demonstrate a foundation for interpretation of the behavior of the dyes, thus providing guidelines for future of new bishemicyanine fluorophores with specific applications.

  • Yingzi Tan, Zhikai Guo, Mengyue Zhu, Jing Shi, Wei Li, Ruihua Jiao, Renxiang Tan, Huiming Ge
    Chinese Chemical Letters. 2020, 31(6): 1406-1409.

    Spirobisnaphthalenes comprise a relatively rare family of natural products that are normally isolated from fungi and occasionally from plants. Here we reported the discovery of seven new preussomerintype spirobisnaphthalenes, preussomerins YT1-YT7 (1-7), and seven known ones (8-14), from the endophytic fungus Edenia gomezpompae, enriching the structural diversity of this family of natural products. Their structures were established by 1D and 2D NMR spectroscopy, HRESIMS analysis and comparison with previously reported compounds, with the absolute configurations of compounds 1 and 2 being further confirmed by single-crystal X-ray diffraction using Cu Kα radiation. The antiinflammatory activities of all isolates were assessed by measuring the production of NO in LPS-induced RAW264.7 macrophage cells. Among them, compounds 8 and 13 exhibited potent inhibitory activities on the production of NO, with IC50 values of 2.61 and 1.32 μmol/L, respectively.

  • Jiajia Liu, Xiaoxia Dai, Zhongbiao Wu, Xiaole Weng
    Chinese Chemical Letters. 2020, 31(6): 1410-1414.

    Since the discovery of polychlorinated dibenzo-p-dioxins and dibenzofurans (PCDD/Fs) in the process of municipal solid waste incineration (MSWI), a large number of researches have been conducted to reveal their formation mechanisms and emission characteristics. As one of national priority control pollutants, chlorinated organics are inclined to transfer into PCDD/Fs in the heterogeneously catalyzed process, which has been considered to be one of great challenges in environmental catalysis. However, so far direct evidences to support such a conversion process are insufficient, and the reaction mechanisms are lack of exploration. This study investigated the catalytic elimination of chlorobenzene (CBz) over a range of industrially applied active species including Pt, Ru, V, Ce and Mn oxides, and explored their reaction byproducts, chlorine adsorption/desorption behaviors and PCDD/F formations. We found that all of these species could generate the PCDD/Fs, amongst which, Mn species were the most active for PCDD/F formation. Approximately 140 ng I-TEQ g-1 PCDD/Fs were detected on the Mn-CNTsurface after ageing at 250 ℃ for 30 h. Even using the dichloromethane (DCM) as a precursor, significant PCDD/Fs were still detected. The Ru and V species were shown to generate much less polychlorinated byproducts and PCDD/Fs, owning to their sufficiently high abilities in Cl desorption, which were through the semi-Deacon and Brønsted H reactions, respectively.

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