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  • Haoyuan Lv, Shuai Ma, Zhenbo Wang, Xiaoting Ji, Shaoping Lv, Caifeng Ding
    Chinese Chemical Letters. 2021, 32(5): 1765-1769.

    Nanomaterial based drug delivery system have received great attention in clinical application due to their high therapeutic efficacy and lower side effects than classical method, multi-functional nanomaterial also have shown the excellent performance at cancer theranostic and durg tracking in vivo and in vitro. However, most of these works are influenced by the bio-toxicity of applied nanomaterials, which could influence the diagnostic results and treatment effect. Therefore, we have prepared a high biocompatibility porous carbon nanospheres (PCNs) based nano-system (PCN-siRNA-DOX-FA) for targeted drug delivery and theranostic. The surface modifications have increased dispersion and stability of the PCNs, and folic acid (FA) had enhanced the active target ability for FA receptor positive cell lines. Moreover, through the siRNA structure and doxorubicin (DOX) loading, biological and chemical combined multi-therapy was achieved in cancerous cells. This constructed nano-system could positively improve the biotoxicity problem of nanomaterial and provide a potential platform for clinical cancer theranostic applications.

  • Hui Liu, Xi Xiang, Jianbo Huang, Bihui Zhu, Liyun Wang, Yuanjiao Tang, Fangxue Du, Ling Li, Feng Yan, Lang Ma, Li Qiu
    Chinese Chemical Letters. 2021, 32(5): 1759-1764.

    The increasing incidence of osteoarthritis (OA) seriously affects life quality, posing a huge socioeconomic burden. Tissue engineering technology has become a hot topic in articular cartilage repair as one of the key treatment methods to alleviate OA. Hydrogel, one of the most commonly used scaffold materials, can provide a good extracellular matrix microenvironment for seed cells such as bone marrow mesenchymal stem cells (BMSCs), which can promote cartilage regeneration. However, the low homing rate of stem cells severely limits their role in promoting articular cartilage regeneration. Stromal cell-derived factor- 1α (SDF-1α) plays a crucial role in the activation, mobilization, homing, and migration of MSCs. Herein, a novel injectable chemotaxis hydrogel, composed of chitosan-based injectable hydrogel and embedding SDF-1α-loaded nanodroplets (PFP@NDs-PEG-SDF-1α) was designed and fabricated. The ultrasound was then used to augment the injectable chemotaxis hydrogel and promote the homing migration of BMSCs for OA cartilage repair. The effect of ultrasound augmenting injectable PFP@NDs-PEG-SDF-1α/hydrogel on the migration of BMSCs was verified in vitro and in vivo, which remarkably promotes stem cell homing and the repair of cartilage in the OA model. Therefore, the treatment strategy of ultrasound augmenting injectable chemotaxis hydrogel has a bright potential for OA articular cartilage repair.

  • Tianlu Zhang, Zhiguo Lu, Jianze Wang, Jie Shen, Qiulian Hao, Yan Li, Jun Yang, Yunwei Niu, Zuobing Xiao, Lei Chen, Xin Zhang
    Chinese Chemical Letters. 2021, 32(5): 1755-1758.

    Fragrances are frequently added to a variety of products, including food, cosmetics and health products. However, the high volatility and instability of essence limit its application in some fields. In this study, mesoporous silica nanoparticles (MSNs) were prepared to encapsulate eugenol, which could reduce the volatilization of the fragrance molecules. A facile approach was presented to synthesize MSNs with three different pore diameters for encapsulating eugenol. In addition, the properties of MSNs including mean particle size, morphology, encapsulating efficiency and release tendency were characterized. Results showed that the larger the pore diameters of MSNs, the more aromatic molecules were adsorbed. Furthermore, the release mechanism was described as the smaller the pore diameters of MSNs, the slower the release of eugenol.

  • Lei He, Rongrong Huang, Pengfeng Xiao, Yuan Liu, Lian Jin, Hongna Liu, Song Li, Yan Deng, Zhu Chen, Zhiyang Li, Nongyue He
    Chinese Chemical Letters. 2021, 32(5): 1593-1602.

    Due to their high specificity and affinity towards various targets, along with other unique advantages such as stability and low cost, aptamers are widely applied in analytical techniques. A typical aptamer-based electrochemical biosensor is composed of a aptamer as the biological recognition element and transducer converting the biologic interaction into electrical signals for the quantitative measurement of targets. Improvement of the sensitivity of a biosensor is significantly important in order to achieve the detection of biomolecules with low abundance, and different amplification strategies have been explored. The strategies either employ nanomaterials such as gold nanoparticles to construct electrodes which can transfer the biological reactions more efficiently, or attempt to obtain enhanced signal through multi-labeled carriers or utilize enzyme mimics to catalyze redox cycling. This review discusses recent advances in signal amplification methods and their applications. Critical assessment of each method is also considered.

  • Chunying Li, Yifan Zhang, Yilin Wan, Jingle Wang, Jing Lin, Zhiming Li, Peng Huang
    Chinese Chemical Letters. 2021, 32(5): 1615-1625.

    The stimulator of interferon genes (STING) shows promising clinical activity in infectious diseases and tumors. However, the lack of targeting capability and intracellular stability of STING agonists severely limits the therapeutic efficacy. Recently, drug delivery systems (DDSs) overcome these delivery barriers of STING agonists via passive or active cell targeting, prolonged blood circulation and drug release, and lysosome escape, etc. In this review, we will describe in detail how existing DDSs are designed to overcome delivery barriers and activate the STING pathway, and the current biomedical applications of STING-activating DDSs in the treatments of infectious diseases and tumors. Finally, the prospects and challenges of DDSs in STING activation are discussed.

  • Ruoxi Li, Dazheng Ling, Tongke Tang, Zhenghui Huang, Manjiong Wang, Fei Mao, Jin Zhu, Lubin Jiang, Jian Li, Xiaokang Li
    Chinese Chemical Letters. 2021, 32(5): 1660-1664.

    Antimalarial chemotherapies endowed with effectiveness against drug-resistant parasites and good safety are urgently required in clinical. Our previous research revealed that clinical phase Ⅱ antitumor drug Quisinostat was a promising antimalarial prototype by inhibiting the activity of Plasmodium falciparum (P. falciparum) histone deacetylase (PfHDAC). Herein, 30 novel spirocyclic linker derivatives were designed and synthesized based on Quisinostat as lead compound, and then their antimalarial activities and cytotoxicity were systematically evaluated. Among them, compounds 8 and 27 could effectively eliminate wild-type and multi-drug resistant P. falciparum parasites, and display weakened cytotoxicity and good metabolic stability. Western blot assay demonstrated that they could inhibit PfHDAC activity like Quisinostat. In addition, both 8 and 27 showed certain antimalarial efficacy in rodent malaria model, and the animal toxicity of 8 was significantly improved compared with Quisinostat. Overall, 8 and 27 were structurally novel PfHDAC inhibitors and provided prospective prototype for further antimalarial drug research.

  • Junjie Yang, Junxian Qin, Ziyang Guo, Yun Hu, Xia Zhang
    Chinese Chemical Letters. 2021, 32(5): 1819-1822.

    A Zn-containing graphite carbon (Zn-GC) with uniform Zn metal sites and hierarchical pore structure was obtained by pyrolysis of Zn-based metal organic framework (MOF). Zn-GC exhibited excellent adsorption capacity and reproducibility for formaldehyde. The adsorption capacity of Zn-GC was 736 times that of commercial activated carbon and 5.6 times that of ZSM-5 adsorbents. The characterization and experimental results showed that the surface chemical characteristics of the adsorption material play an important role in the adsorption performance. The superior performance was attributed to Zn metal sites and oxygen-containing functional groups on the MOF derivative as well as hierarchical pore structure. The material showed a great potential in the field of organic pollutant removal.

  • Qiao Song, Yan Liu, Linlin Cai, Xinyu Cao, Shan Qian, Zhouyu Wang
    Chinese Chemical Letters. 2021, 32(5): 1713-1716.

    Fused indolizidines and quinolizidines are important skeletons in a variety of natural products and pharmacologically important compounds. A one-pot tandem route from amide to fused indolizidines and quinolizidines is disclosed. This method is conducted in mild conditions and shows well tolerance of functional groups. It is also easy to be scaled up to gram scale and can be applied smoothly to the total synthesis of alkaloids such as (±)-crispine A, (±)-xylopinine, (±)-desbromoarborescidine A, (±)-harmicine and other bioactive substances.

  • Kemei Jiang, Yanan Wu, Juan Chen, Mingqing Shi, Hong-Min Meng, Zhaohui Li
    Chinese Chemical Letters. 2021, 32(5): 1827-1830.

    Exosomes have attracted widespread interest due to their inherent advantages in tumor diagnosis and treatment monitoring. However, it is still a big challenge for highly sensitive and specific detection of exosome in real complexed samples. Herein, a molecular recognition triggered aptazyme cascade strategy was developed for ultrasensitive detection of cancer exosomes in clinical serum samples. In this design, one target exosome could capture a large quantity of aptazymes for the first-step signal amplification. And then the captured aptazyme was activated and recycled to release the fluorophore-abelled substrate strand for a cascaded signal amplification. Notably, the activation of aptazyme only occurs when it has bound with target exosome, ensuring a low background. The experimental results show that the limit of detection (LOD) and the limit of quantification (LOQ) are 3.5×103 particles/μL and 1.7×104 particles/μL, respectively, which is comparable to the results of most existed fluorescence-based exosome probes. Moreover, this assay possesses high specificity to distinguish exosomes derived from other cell lines. Furthermore, this fluorescence probe was utilized in cancer patient and healthy serum samples successfully, suggesting its great potential for clinical diagnosis and biological studies.

  • Wei-Min He, Xiuling Cui
    Chinese Chemical Letters. 2021, 32(5): 1589-1590.
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