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Table of Content

    31 July 2019, Volume 28 Issue 7
    Review
    Microfluidic models in liver drug metabolism research
    Lin Zhao, Yong Jiang, Pengfei Tu, Xiaoni Ai, Xiaoyu Guo
    2019, 28(7):  449-467.  DOI: 10.5246/jcps.2019.07.044
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    In pre-clinical phase of new drug development, it is particularly important to establish an in vitro model to mimic the metabolism situation of human body. The aim of the in vitro model is to reduce the usage of experimental animals and to make a more accurate prediction of the drug metabolism in vivo. Microfluidic chip is an emerging technology to establish predictive models. By integrating subcellular fractions, hepatocytes or liver tissue in the microfluidic chips, more predictive in vitro metabolismmodels can be established for drug development. The microfluidic platform offers dynamic and controlled fluids, as well as sophisticated liver tissue assembly to remodel the physiological and pathological microenvironment of liver in the human body. This review updates the microfluidic-based liver drug metabolism models since 2011, and summarizes the development of different models based on different chip vectors (subcellular components, primary hepatocytes, and tissue sections). It serves as a guide for newcomers to this dynamic field.
    Original articles
    Chemical constituents from the aerial parts of Waltheria indica Linn.
    Yiming Hua, Xiaowen Zhang, Kewu Zeng, Qingying Zhang, Pengfei Tu
    2019, 28(7):  468-475.  DOI: 10.5246/jcps.2019.07.045
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    A phytochemical investigation on the aerial parts of Waltheria indica Linn. led to the isolation of 16 compounds,including five terpenoids (15), four coumarins (69), six flavonoids (1015), and one phenylpropanoid glycoside (16). The structuresof these compounds were identified by spectroscopic data analysis and comparison with those reported in the literatures. Except for12 and 15, all the compounds were isolated from W. indica for the first time. Moreover, coumarins were firstly reported to be obtained from this herb. The NO production inhibitory activities of all the isolated compounds in LPS-induced BV-2 cells were also presented.
    Interferon-liposomes prepared to make macroglia maintain M1 phenotype
    Yitian Du, Lu Zhang, Yin Zhan, Xinyu Chai, Kaisen Li, Xianrong Qi
    2019, 28(7):  476-483.  DOI: 10.5246/jcps.2019.07.046
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    Macroglia is a crucial macrophage only existing in the central nervous system. During the development of glioma, it can be activated as M2 anti-inflammatory type to promote glioma growth. Interferon-γ (IFN-γ) is an important immunomodulator inglioma microenvironment, which can also activate macroglia as M1 pro-inflammatory type to enhance anti-tumor immune responseand lead to inhibition of glioma growth. Therefore, we utilized IFN-γ to make macroglia maintain M1 phenotype, so that prospectively achieving anti-tumor immunity for glioma therapy. We prepared interferon-γ-liposomes (IFN-Lp) to protect IFN-γ from elimination. IFN-Lp was proved to have strong capability to be phagocytosed and accumulate in macroglia (BV2 cells) to achieve long-term effect. In addition, IFN-Lp could allow BV2 cells to maintain M1 phenotype, showing no impact on its cell viability. These findings will offer new opportunities to achieve enhanced immunotherapy of glioma.
    Molecular basis for rational construction of RVGP modified liposomal delivery system targeting to brain
    Bo Deng, Wei Cui, Shuang Ma, Xiaona Liu, Zhan Zhang, Baiyi Yan, Kun Chen, Ying Xie
    2019, 28(7):  484-501.  DOI: 10.5246/jcps.2019.07.047
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    The rational construction of active targeting liposomes will provide an important structural support for its effective brain targeting. However, there is no clear understanding of the structure-activity relationship of active targeting liposomes. Combining multiscale computational simulation and experimental verification, we established a computational model of RVGP modified PEGylated liposomes (RVGP-PEG-L) and investigated the role of PEG and molecular interaction mechanism of carrier-ligand-receptor. The result indicated that the complex network conformation formed by PEG with 42 monomers (42PEG) above the density of 8% was the molecular basis for PEG-L to achieve long-circulation function. The lowest monomer number of PEG linker to ensure the targeting ability of RVGP was 42. However, the pose of RVGP binding to nAChR changed after it was linked with PEG-L due to the restraint of PEG chain, leading to a decrease of binding free energy. Increasing the monomer number of PEG linker or improving the non-polarity of polymers was a potential strategy to enhance the combination of RVGP-PEG-L with nAChR on the targeting cell. 
    Drug administration and clinical pharmacy column
    The efficacy and safety of three types of combination therapies in patients with moderate to very severe COPD: a systematic review and meta-analysis
    Ruirui Zhou, Liqun Wang, Tong Sun, Ziyang Wu, Xiaohui Xie
    2019, 28(7):  502-518.  DOI: 10.5246/jcps.2019.07.048
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    Inhaled drugs, including long-acting muscarinic antagonists (LAMAs), long-acting β2-agonists (LABAs) and inhaled corticosteroids (ICSs), are the main therapeutic options for patients with chronic obstructive pulmonary disease (COPD). We conducted a systematic review and meta-analysis to compare the efficacy and safety of LAMA+LABA+ICS, LAMA+LABA and LABA+ICS therapies. The Pubmed, Embase and Cochrane Library databases were searched for randomized controlled trials (RCTs) comparing the efficacy (moderate-to-severe exacerbations, lung function and quality of life) and safety (adverse events (AEs), severe adverse events (SAEs), withdrawals due to AEs, deaths and pneumonia) of LAMA+LABA+ICS, LAMA+LABA and LABA+ICS in COPD patients. Two investigators independently searched eligible studies and extracted relevant information. The data were analyzed using the Review Manager software, and the quality of included studies was assessed using the Cochrane risk of bias tool. A total of 27 studies were included, and majority of the studies showed low risk of bias. Moderate­to­severe exacerbations were lower after LAMA+LABA+ICS therapy compared with the LABA+ICS (RR = 0.66; 95% CI: 0.590.74) and LAMA+LABA therapies (RR = 0.88; 95% CI: 0.820.94). Lung function was significantly improved after LAMA+LABA+ICS compared with LAMA+ICS treatment. FEV1, peak FEV1 and trough FEV1 were significantly increased by 100 mL, 150 mL and 120 mL, respectively, in LAMA+LABA+ICS therapy compared with LAMA+ICS. In addition, LAMA+LABA therapy resulted in increased FEV1, peak FEV1 and trough FEV1 by 80 mL, 90 mL and 70 mL, respectively, compared with LAMA+ICS. SGRQ-total score was used to assess quality of life of COPD patients, which indicated that LAMA+LABA+ICS therapy was associated with slightly greater decrease compared with LABA+ICS (MD = 1.33; 95% CI: –2.35 to –0.30). No significant differences were found across all three treatment combinations in term of AEs, SAEs, withdrawals due to AEs and deaths. However, the risk of pneumonia was higher in the triple therapy group than that in the LABA+ICS (RR = 1.16; 95% CI: 1.011.33) or LAMA+LABA (RR = 1.31; 95% CI: 1.061.62) groups, and significantly lower in the LAMA+LABA group compared with LABA+ICS (RR = 0.64; 95% CI: 0.540.76). LAMA+LABA+ICS therapy offered greater efficacy and comparable safety compared with the LAMA+LABAor LABA+ICS therapies. However, triple therapy could increase the risk of pneumonia compared with LAMA+LABA or LABA+ICS therapies. People who have higher risk of pneumonia should carefully consider the use of triple therapy. LAMA+LABA therapy offered greater efficacy and lower risk of pneumonia to LABA+ICS therapy. Collectively, LAMA+LABA therapy might be a better choice than LABA+ICS.            
    The others
    Management of electron paramagnetic resonance spectrometer in a university core laboratory
    Yingli Xu, Guangcan Bai, Jingfen Lu
    2019, 28(7):  519-526.  DOI: 10.5246/jcps.2019.07.049
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    Electron Paramagnetic Resonance (EPR) is the only spectral method for direct detection of paramagnetic substances. EPR technology can be used for the qualitative and quantitative analysis of free radicals and transition metals in solid, liquid, gas, cell and living samples. It is widely used in chemistry, material science, life science, quantum physics and other researches. This report discusses the basic principle, instrument structure, common problem solving, daily maintenance, and management model of the electron paramagnetic resonance spectrometer (German Bruker A-200) in the State Key Laboratory of Natural and Biomimetic Drugs of Peking University Health Science Center, so that the instrument can be fully used for various scientific researches.