Home Latest Articles
Latest Articles
  • Meng-ru LI, Yu-zhi ZHOU, Jian-xin CHAI, Qiang CHEN, Li GAO, Guan-hua DU, Xue-mei QIN
    Acta Pharmaceutica Sinica. 2020, 55(11): 2702-2712.

    The effects of alcohol extracts from roots, stems, leaves, and flowers of Scutellaria Baicalensis Georgi (SBG) on endogenous metabolism in D-gal-induced aging-model rats were investigated by 1H NMR metabolomics. Results showed that 32 endogenous metabolites were identified in the urine. Combined with the VIP value and t-test, 14 different metabolites were found by multivariate statistical analysis of the spectrum. Compared with the control group, the content of α-ketoglutaric acid, hippuric acid and 3-hydroxybutyrate in the urine of rats in the model group was significantly decreased (P < 0.05) and the content of trimethylamine oxide, glycine, alanine, lactic acid, dimethylglycine, acetate, pyruvate, taurine, allantoin, betaine, N-acetylated glycoprotein was significantly increased (P < 0.05). The metabolites were mainly derived from taurine and hypo-taurine metabolism; glycine, serine and threonine metabolism; pyruvate metabolism; glycolysis/gluconeogenesis; glyoxylic acid and dicarboxylic acid metabolism; and the tricarboxylic acid cycle. The content of differential metabolites in urine samples was altered by the alcohol extracts from the different parts of SBG. Leaves extracts of SBG had the greatest effect on urine metabolites, and mainly affected taurine and hypo-taurine metabolism; glycine, serine and threonine metabolism; and pyruvate metabolism. This study provides a reliable experimental basis for the future development of SBG. This animal experiment was approved by the Committee on the Ethics of Animal Experiments of Shanxi University (SXULL2016036).

  • Lei TAO, Lei YU, You-xue DING, Hua BI, Chun-ming RAO
    Acta Pharmaceutica Sinica. 2020, 55(11): 2713-2718.

    The glycosylation heterogeneity of recombinant human pro-urokinase (pro-UK) was assessed using ultra-performance liquid chromatography-mass spectrometry (UPLC-MS). Firstly, the source of heterogeneity was determined by measuring the Mr of intact protein before and after N-deglycosylation. Glycosylation sites and the proportion of O-glycopeptides then were determined at the peptide level. Finally, the N-glycans were confirmed and quantified using the N-glycan profile. Results show that the structural heterogeneity of pro-UK is mainly caused by glycosylation. All T18 were fucosylated, and 6.4% of S138/139 was O-glycosylated with two kinds of oligosaccharides with a ratio of 6.0% and 0.4% respectively. All N302 positions were N-glycosylated by more than ten types of glycans, among which A2F and A3F accounted for 80% of the total. The assessment of glycosylation heterogeneity of pro-UK will provide a reference for quality standardization.

  • Bo-shi LIU, Zeng-ming WANG, Hui ZHANG, Jing GAO, Nan LIU, Xiang GAO, Meng LI, Ai-ping ZHENG
    Acta Pharmaceutica Sinica. 2020, 55(11): 2719-2727.

    The aim of this study is to prepare acetaminophen sustained-release tablets by hot melt extrusion 3D printing technology based on the concept of "Quality by Design" (QbD). Firstly, the failure mode and effect analysis (FMEA) was used to determine the critical process parameters (CPPs), then full-factor experimental design was used to analyze the critical quality attributes (CQAs) and to establish the design space. The results showed that the content of plasticizer, the path spacing and the shell numbers are independent variable for the experimental design. The design space was concluded to be plasticizer content:9%, and the shell number:3-5, the path spacing:1.05-1.2 mm. In this study, 3D printing technology was used to prepare acetaminophen sustained-release tablets in accordance with the concept of QbD, which improved the durability of the process and ensured the uniform and controllable quality of the preparation and also provided experimental basis for personalised medicine.

  • Yu LUO, Fei WU, Lan SHEN, Xiao LIN, Yi FENG
    Acta Pharmaceutica Sinica. 2020, 55(11): 2728-2735.

    This paper aimed to study the effect of combined co-processing of coating and pore forming on the tableting and tablet properties of traditional Chinese medicine (TCM) extracts together with its applicability. Four TCM extracts were co-processed using fluid bed with hydroxypropyl methyl cellulose (HPMC) as coating agent and ammonium bicarbonate (NH4HCO3) as pore-forming agent. Powder properties (such as particle size and size distribution, bulk density, tap density, moisture content) and tablet properties (including tensile strength, compaction ratio, fast elastic stretch, and disintegration time) were measured and compared among the powders. Scanning electron microscopy (SEM) was applied to characterize the surface of particles and tablets. Results showed that the particle size, flowability, and compactibility of the composite particles with HPMC were superior to the parent powders of TCM extracts. These properties of the porous particles with HPMC and NH4HCO3 showed further improvements. In addition, the addition of HPMC prolonged the disintegration time of tablets, whereas the pore-forming effect of NH4HCO3 could shorten the disintegration time. SEM revealed the changes in the morphology of the composite particles and the pores on the surface of the porous particles and tablets. In conclusion, co-processing with HPMC and NH4HCO3 could improve the powder and tablet properties of TCM extract powders, and this method shows certain applicability, which provides a feasible choice for improving the tableting properties of some TCM extract powders.

  • Jia-peng YANG, Zi-le ZHU, Ya-juan FAN, Fei ZHU, Yue-jun CHEN, Zhi-tao NIU, Xiao-yu DING
    Acta Pharmaceutica Sinica. 2020, 55(11): 2736-2745.

    Bulbophyllum orchids are popular for its ornamental appearance and great medicinal values. However, there is still a lack of research on phylogenetic relationship and species identification for this genus. In this study, the plastome sequences of three medicinal Bulbophyllum orchids (Bulbophyllum affine, Bulbophyllum pectinatum, Bulbophyllum funingense) were sequenced and analyzed. After assembly and annotation, it was found that the plastomes of Bulbophyllum plants encoded a total of 108 genes, including 74 protein-coding genes, 30 tRNA genes and 4 rRNA genes. Based on the analysis of mVISTA and comparison between junctions, it was found that the plastome structure of Bulbophyllum orchids was relatively conserved, and the variation mainly existed in the non-coding regions. Phylogenetic analysis showed that Bulbophyllum orchids were closely related to Dendrobium orchids. SSR analysis of Bulbophyllum showed that most SSRs were located in the intergenic spacer and had the most single nucleotide repeats. In addition, based on the comparative analysis of non-coding sequences, a total of 10 high-variability sequences were screened out, among which the combination of five non-coding region sequences, including psbI-trnS, psbC-trnS, clpP-ex1-psbB, psaJ-rpl33, rpl33-rps18, had the highest sequence variability and could be used in the species identification study of medicinal plants of Bulbophyllum. In conclusion, this study provides a theoretical basis for phylogenetic relationship and species identification of Bulbophyllum orchids through the comparative analysis of plastome sequences of three medicinal plants of the genus Bulbophyllum.

  • Lu-yao QIAO, Xiao-wei ZHANG
    Acta Pharmaceutica Sinica. 2020, 55(10): 2243-2255.

    Liver fibrosis is a critical pathological structural basis of a variety of chronic liver diseases such as alcoholic liver disease, viral hepatitis and nodular cirrhosis, while liver regeneration is the key mechanism for protecting liver against multiple injuries, promoting inflammation resolution and reversing liver fibrosis. When fibrosis occurs after liver injuries, the alternation of liver regeneration status in fibrosis usually plays an essential role in the outcome of diverse liver diseases. In this review, the differences between "homeostatic regeneration", "normal regeneration" and "aberrant regeneration" were identified in terms of the occurrence conditions, the basic state of the liver, the effects on liver repair, the types of cells involved and the pathogenesis. Emphatically, we not only summarize the differences of mechanisms between "aberrant regeneration" and "normal regeneration" in the pathogenesis of liver fibrosis, but also elucidate the features of "aberrant regeneration" in various liver fibrosis models, as well as the therapeutic strategies for the treatment of liver fibrosis based on "aberrant regeneration", expecting to provide evidence and clues for considering the risks and proposing possible solutions in clinical treatment of liver fibrosis.

  • Yi-kai LIAN, Wei-dong ZHOU
    Acta Pharmaceutica Sinica. 2020, 55(10): 2256-2263.

    Polycystic ovary syndrome (PCOS) is a common reproductive endocrine disease, which is mainly characterized by hyperandrogenemia, rare or anovulation, and polycystic ovarian changes. PCOS is seriously harmful and its causes are complex, which has not yet been clarified. Studies have shown that non-coding RNAs play important roles in the development of PCOS, including the regulation of hormone metabolism and follicle development. Exosomes are natural nano-scale membrane vesicles that contain cell-specific proteins, lipids, nucleic acids, and other biologically active molecules. Exosomes are important mediators for intercellular communication and new targets for disease diagnosis and treatment. Recent studies have shown that as an important component of follicle microenvironment, exosome is closely related to the pathogenesis of PCOS. Exosome and exosomal non-coding RNAs are expected to serve as potential new diagnostic and therapeutic targets for PCOS. In this review, we will summarize the function of exosome and exosomal non-coding RNA in the pathogenesis, diagnosis, and treatment of PCOS.

  • Sen ZHANG, Xiao-yue ZHAO, Yu LIANG, Sha LI, Guan-hua DU
    Acta Pharmaceutica Sinica. 2020, 55(10): 2264-2272.

    Parkinson's disease (PD) is the second most common neurodegenerative disease of the central nervous system. It is currently believed that PD is related to factors such as age, gender, family inheritance, gene mutation and environment. The pathogenesis of PD is complex and is related to dysfunction and loss of dopaminergic neurons, involving accumulation of α-synuclein, neuroinflammation, oxidative stress, mitochondrial dysfunction and excessive accumulation of neuromelanin. In many ways, various factors act both independently and through cross-promotion, resulting in an ongoing pattern of brain tissue damage and progressing PD pathology. This article reviews the recent research on the pathogenic factors and pathogenesis of PD and explores new ideas and potential targets for PD treatment and drug development.

  • Qing-hua WANG, Ting-ting DU, Zhi-hui ZHANG, Ming JI, Hai-yu HU, Xiao-guang CHEN
    Acta Pharmaceutica Sinica. 2020, 55(10): 2273-2280.

    In recent years, with rapid advances in chlorogenic acid (CGA) research, it has become widely used in medicine, the chemical industry and health care products, with the potential for broad application. CGA is a water-soluble phenolic natural product and is extensively distributed in a variety of plants. Numerous studies have shown that CGA has strong biological activities including antibacterial, antiviral, antitumor, antioxidative, anti-inflammatory and metabolic regulatory activities. This review summarizes the pharmacological effects as well as the underlying mechanisms of CGA, providing an important theoretical basis for further research on CGA drug targets and potential mechanisms.

  • Yu-hua MA, Yu FANG, Yi BAO, Peng-cheng LIN, Guo-qing PAN, Xiang-yun GAI
    Acta Pharmaceutica Sinica. 2020, 55(10): 2281-2290.

    The technology of lipid-drug conjugates is developed on the basis of prodrug principle, which overcomes some drawbacks of drugs via increasing the lipophilicity of hydrophilic or poorly soluble drugs to promote the absorption of drugs and enhance the curative effect. This article sums up the research progress of lipid-drug conjugates from the chemical synthesis methods of conjugates, the types of conjugates, the influence on biological activity of drugs, the application in nanoparticles for drug delivery and the mechanism of absorption and degradation.