中文 | English
  • Current Issue
  • Online First
  • Archive
  • Accept
  • Most Downloaded

    Editorial Office of Journal of China Pharmaceutical University  Volume 54,2023 Issue 6

    专栏：生物质谱技术前沿进展及其在药物研发中的应用
    Original Articles
    Monograph
    Select AllDeselectExport
    Display Method:
    专栏：生物质谱技术前沿进展及其在药物研发中的应用
    Recent advances in mass spectrometry imaging and its application in drug research
    WANG Songkai, ZOU Yuchen, SUN Shipeng, YAN Zhiye, TANG Weiwei, LI Ping, LI Bin
    2023,54(6):653-661. DOI: 10.11665/j.issn.1000-5048.2023091901
    [Abstract] (627) [HTML] (418) [PDF 1.05 M] (3386)
    Abstract:
    Mass spectrometry imaging (MSI), a label-free molecular imaging technique, has been applied widely in the spatial localization of small molecule metabolites, lipids, peptides, and proteins, with its unique advantage of high spatial resolving power compared to traditional liquid chromatography-mass spectrometry (LC-MS).With the nonstop advancement of its achievable sensitivity and spatial resolution, MSI technique has been providing novel perspectives into the preclinical studies of drugs, such as in vivo localization of drugs and their metabolites, visualization of drug metabolism, and drug delivery tracking.This review introduces the basics of MSI techniques, including basic principles, key features, technical advantages, and limitations, with particular highlight of the recent applications of MSI in drug efficacy and safety evaluation, drug distribution research, drug delivery research, and analysis of Chinese medicine from recent publications, aiming to promote the utilization and further expansion of MSI in the research and development of drugs.
    Progresses of mass spectrometry-based analysis of N-glycoproteins
    TIAN Zhixin
    2023,54(6):662-673. DOI: 10.11665/j.issn.1000-5048.2023062701
    [Abstract] (258) [HTML] (303) [PDF 2.90 M] (2467)
    Abstract:
    N-linked glycosylation is a common post-translational modification on proteins, which exhibits the same macro-heterogeneity of modification site as other small molecule modifications (such as methylation, acetylation, phosphorylation), i.e., the amino acid sequence of a protein has multiple putative modification sites. However, compared to small molecule modifications with single structures, N-glycosylation modification have tens of thousands of structures from multiple structural dimensions such as different monosaccharide compositions, sequence structures, linking structures, isomerism, and three-dimensional conformation.This results in additional micro-heterogeneity of modification site of N-glycosylation, i.e., the same N-glycosylation site can be modified with different glycans with a certain stoichiometric ratio.N-glycosylation modification regulates the structure and function of N-glycoproteins in a site- and structure-specific manner, and differential expression of N-glycosylation under disease conditions needs to be characterized through site- and structure-specific quantitative analysis.This article mainly introduces the latest development of mass spectrometry-based site- and structure-specific quantitative N-glycoproteomics and its applications in biomedical fields.
    Recent progress of protein glycosylation characterization utilizing native conformer-resolved mass spectrometry
    JIA Yifei, WANG Yamei, LI Gongyu
    2023,54(6):674-681. DOI: 10.11665/j.issn.1000-5048.2023060901
    [Abstract] (423) [HTML] (243) [PDF 1.36 M] (1766)
    Abstract:
    Glycosylation of proteins, one of the most prevalent and complex post-translational modifications occurring in nature, plays a crucial role in regulating protein net charge, conformation, binding properties and, ultimately, biological function.Traditional structural techniques are not amenable for glycoproteins due to the inherent heterogeneity of oligosaccharides.With the advances in analytical technique, mass spectrometry displays an increasingly crucial role in elucidating the structure of glycoproteins.Mass spectrometry-based proteomic technique can dissect the chemical composition and site information of low-abundance glycosylation at the peptide level.Instead, native mass spectrometry (nMS) can analyze intact glycoproteins while maintaining the information for glycan heterogeneity, and the insights into the regulatory effects of glycosylation on protein higher order structures and interactions with other proteins or ligands.As a representative structural mass spectrometry tool, ion mobility-based nMS strategy is powered by its conformer-resolving capability and by the feasibility of conformer manipulation through collision-induced unfolding.Consequently, native IM-MS analysis can provide rich information of dynamic protein conformations, allowing for the rapid identification and differentiation of protein isoforms in an unprecedented manner.In this review, we briefly introduced two emerging native IM-MS analytical modes, dynamic conformer-resolving mode and glycoform-resolving mode.Besides, we also discussed the recent progress of conformational and topological characterization of intact glycoproteins with three typical model systems based on two above-mentioned emerging modes of native IM-MS.
    Application of biological mass spectrometry in quality control of adeno-associated virus carrier preparations
    LI Mengxiao, LI Huilin
    2023,54(6):682-694. DOI: 10.11665/j.issn.1000-5048.2023062901
    [Abstract] (177) [HTML] (279) [PDF 2.59 M] (1121)
    Abstract:
    Adeno-associated virus (AAV) is a common viral vector used in gene therapy.Because of its high safety and its ability to target a variety of cells, it has been widely used in preclinical and clinical studies.However, during the design and production, AAV vectors have many key quality attributes that affect their safety and efficacy.The development and application of biological mass spectrometry technology provides a convenient platform for the research on biological macromolecules, especially in the aspects of protein sequence, structure and interaction.For AAV vectors, mass spectrometry can facilitate the determination or characterization of capsid protein ratio, post-translational modification, serotype, and empty capsid ratio, thus assisting in the quality control of AAV vectors.Compared with the existing methods, mass spectrometry has the advantages of smaller amount of sample size, faster and more sensitive analysis, being more suitable for the analysis of complete AAV vectors with higher mass resolution, and can distinguish empty capsids, full capsids and partial capsids.In the future, mass spectrometry technology is expected to play a more important role in the design and production of AAV vectors through the coupling of more efficient protein separation technology with mass spectrometry, the development of new information processing software platforms and new mass spectrometry detection techniques.
    Microfluidic chip and mass spectrometry-based detection of bacterial antimicrobial resistance and study of antimicrobial resistance mechanism
    ZHANG Dongxue, QIAO Liang
    2023,54(6):695-705. DOI: 10.11665/j.issn.1000-5048.2023060203
    [Abstract] (264) [HTML] (176) [PDF 938.62 K] (1290)
    Abstract:
    Bacterial antimicrobial resistance (AMR) is a globally serious problem that threatens public health security.Misuse and abuse of antibiotics cannot achieve the effect of treating bacterial infectious diseases, but will trigger the SOS response of bacteria, exacerbating the evolution of bacterial AMR and the spread of resistant bacteria.This article focuses on antibiotic-resistant bacteria, briefly introduces the pathogenesis of bacterial AMR and SOS response, and systematically summarizes the determination and mechanism study of bacterial AMR based on microfluidics and mass spectrometry.This article provides theoretical basis for AMR-related drug target mining and new drug development, aiming to develop new methods for rapid detection of bacterial AMR and new methods for bacteria inhibition, and promote the diagnosis and treatment of clinical bacteria infectious diseases.
    Advances in mass-encoded probes for multiplex mass spectrometric detection
    YIN Hao, WANG Wei, MIN Qianhao
    2023,54(6):706-717. DOI: 10.11665/j.issn.1000-5048.2023062902
    [Abstract] (145) [HTML] (212) [PDF 2.79 M] (951)
    Abstract:
    Mass-encoded probe is a probing tool that specifically identifies target molecules and thus outputs their characteristic ion signals with mass tags.It plays an important role in multiplex assay of disease markers, drug target screening and other biomedical applications.Based on various mass spectrometric methods, researchers have developed an array of mass tag-encoded probes with different structures and functions, providing powerful technical tools for multiplex detection of biomolecules in physiological environments and for mass spectrometry imaging of tissue samples.This review introduces the latest research progress of mass tag-encoded probes in multiplex mass spectrometric detection from three aspects, i.e. structural composition of the probes, mass spectrometric methods and their application in biochemical analysis, with a prospect of the future development of mass tag-encoded probes.
    An emerging analytical tool for highly sensitive quantitative analysis based on liquid chromatography-multiple-reaction monitoring cubed (MRM3)
    LI Ting, ZHANG Ke, LI Jun, WANG Shengpeng, SONG Yuelin
    2023,54(6):718-728. DOI: 10.11665/j.issn.1000-5048.2023062801
    [Abstract] (168) [HTML] (201) [PDF 914.23 K] (1942)
    Abstract:
    Liquid chromatography-multiple-reaction monitoring (LC-MRM) has been widely recognized as the golden standard for multiple components-targeted quantitative analysis of complicated matrices,with extensive applications for analysis in such fields as chemical drugs, traditional Chinese medicines and foods.Unfortunately, when facing the task of quantitatively analyzing trace chemical components in complex matrices, MRM suffers dramatically from the background noise or matrix interference, leading to undesirable sensitivity and selectivity in terms of the lower limits of quantification (LOQ) and detection (LOD).In recent years, MRM cubed (MRM3), also known as MS3 scan, has received much attention because of its unique ability to significantly improve detection selectivity and sensitivity attributing to the successive ion filtering function, enabling LC-MRM3 as an emerging analytical tool.In this review,our attention is devoted to: 1) the illustration of the principle for MRM3; 2) parameter settings; and 3) the application progress of LC-MRM3 in such fields as the pursuit of biomarkers, pharmaceutical analysis, forensic analysis, toxicological analysis, food chemistry, and environmental analysis, aiming to provide a promising analytical tool of LC-MRM3 advantageous in the quantification analysis of trace chemical components in complex matrices.
    Original Articles
    Synthesis and antitumor activity evaluation of glycoconjugates derived from natural product harmine
    LIU Xiaohan, TAN Yunying, LI Qiang, CHEN Xu, FU Junjie, YIN Jian
    2023,54(6):729-742. DOI: 10.11665/j.issn.1000-5048.2023041101
    [Abstract] (185) [HTML] (153) [PDF 3.67 M] (829)
    Abstract:
    Based on our previous work, the study herein designed and synthesized eight glycoconjugates of natural product harmine (14a-14h)by introducing a cyclohexylmethyloxyl group at its C7 position and coupling a methyl-2-amino-β-D-glucopyranoside to the N9 position through different lengths of alkyl chains.In vitro anti-tumor activity screening and structure-activity relationship studies showed that the antitumor activity of the conjugates increased with the lengthening of the alkyl chain in the linker.Compound 14h exhibited significantly better proliferative inhibitory activity against MDA-MB-231 breast cancer cells than harmine.As compared to harmine, the introduction of the carbohydrate moiety improved the water solubility of compound 14h and enhanced its tumor cell selectivity through the Warburg effect.Mechanism of action studies revealed that compound 14h induced apoptosis and G0/G1 cell cycle arrest in MDA-MB-231 cells, and inhibited tumor cell migration by interfering with epithelial-mesenchymal transition process.This study provides a new approach for the development of antitumor drugs based on harmine.
    In vitro release of paclitaxel derivative liposome by paddle membrane binding assay
    ZHENG Yuting, HONG Tao, XU Kehui, WEN Minghao, YANG Jixue, WU Mengying, HANG Taijun, SONG Min
    2023,54(6):743-748. DOI: 10.11665/j.issn.1000-5048.2023041803
    [Abstract] (144) [HTML] (141) [PDF 942.12 K] (916)
    Abstract:
    The in vitro release is an important index to evaluate the quality of liposome formulation.Currently, there is no evaluation method for the in vitro release of liposome in pharmacopoeia of various countries, which leads to the lack of unified standard and safety guarantee for the quality evaluation of liposome formulation.Taking the self-made paclitaxel derivative liposomes as an example, the paddle membrane binding method established by optimizing external release conditions was used to simulate the complete release of paclitaxel derivative drugs in 12 hours under physiological conditions.The results showed that using 0.5% SDS-HEPES as the release medium and a dialysis bag with a molecular weight cutoff of 1 000 kD to release the liposome solution met the requirements and had discrimination ability, providing a reference for the development of drug-loaded liposomes release methods in vitro.
    Chromatographic fingerprint and quality consistency of colistimethate sodium
    LI Xuan, HUANG Minwen, ZHOU Jie, YUAN Yaozuo, HANG Taijun
    2023,54(6):749-756. DOI: 10.11665/j.issn.1000-5048.2023071903
    [Abstract] (165) [HTML] (199) [PDF 2.30 M] (1000)
    Abstract:
    The UPLC fingerprint of colistimethate sodium was established for the study of quality consistency.The chromatographic column was Acquity UPLC? Peptide CSH C18 (2.1 mm × 150 mm, 1.7 μm).The mobile phase A was phosphate buffer-acetonitrile (19∶1), and the mobile phase B was phosphate buffer-acetonitrile (1∶1).The mobile phase was in gradient elution at a flow rate of 0.3 mL/min.The column temperature was set at 30 °C and the detection wavelength was 210 nm.The similarity of the fingerprints was analyzed with the Similarity Evaluation System for Chromatographic Fingerprint of Tradition Chinese Medicine (Version 2012) in combination with content determination of multiple index components to evaluate the quality consistency of imported and domestic bulk drugs.The result showed that both the original and generic bulk drugs met the specified limit requirements in the European Pharmacopoeia standards, and that their UPLC fingerprints were highly similar, indicating that the quality of the two substances was consistent.Establishing a fingerprint for similarity evaluation and combining it with the results of indicator component content determination as a comprehensive evaluation method for the study of drug quality consistency of complex components has the characteristics of fast, accurate, and comprehensive, which is helpful for drug quality evaluation and provides ideas for the evaluation of antibiotic quality consistency of complex components.
    Norcantharidin induces apoptosis through autophagosome accumulation in breast cancer MDA-MB-231 cells
    XIA Yuan, JIANG Qingling, WANG Xiaoting, LI Minjing, ZHENG Qiusheng, LI Defang
    2023,54(6):757-768. DOI: 10.11665/j.issn.1000-5048.2023033004
    [Abstract] (182) [HTML] (112) [PDF 3.84 M] (644)
    Abstract:
    The aim of this study was to investigate the effect of norcantharidin (NCTD) on the proliferation and apoptosis of triple-negative breast cancer cell line MDA-MB-231.Western blot was used to detect the effect of NCTD on the expression levels of apoptosis-related proteins Bax/Bcl-2, cleaved-PARP/PARP/PARP, cleved-caspase-9, cleaved-caspase-3 and MCL-1 in MDA-MB-231 cells.Also, the expression levels of autophagy-related proteins LC3-II/LC3-I, Parkin and PINK1 in MDA-MB-231 cells were measured by Western blot.Flow cytometry was used to measure the effect of NCTD on the changes of mitochondrial membrane potential and mitochondrial reactive oxygen species (ROS).The effect of NCTD on autophagy flow in cells expressing mCherry-EGFP-LC3 was detected by a confocal microscope.Moreover, the effects of NCTD combined with chloroquine (CQ) or 3-methyladenine (3-MA) on the apoptosis of MDA-MB-231 cells were detected by flow cytometry.The results showed that NCTD significantly increased the expression levels of Bax/Bcl-2, cleaved-PARP/PARP, cleaved-caspase-9, cleasved-caspase-3 and LC3-II/LC3-I proteins, and promoted the mitochondrial translocation of Parkin, and blocked the autophagic flow in MDA-MB-231 cells. Moreover, NCTD combined with CQ accelerated apoptosis, while NCTD combined with 3-MA decreased apoptosis.These results suggest that NCTD can induce autophagy accumulation and lead to apoptosis of MDA-MB-231 cells.
    Monograph
    Reflection on the construction of pharmacy and traditional Chinese pharmacy disciplines based on patent information analysis: taking “double first-class” universities as an example
    WANG Wei, DING Zuoqi
    2023,54(6):769-776. DOI: 10.11665/j.issn.1000-5048.2023051201
    [Abstract] (130) [HTML] (96) [PDF 1.79 M] (960)
    Abstract:
    Among the second round of “double first-class” construction universities, 12 universities are in the process of building first-class pharmaceutical and traditional Chinese medicine disciplines.The aim is to explore the innovative development trend of these 12 universities, based on their information related to pharmacy and traditional Chinese medicine in the past five years.The study used the PatSnap global patent database to search for pharmaceutical related patents applied by 12 universities from 2018 to 2022, and analyzed the information from perspectives such as application and authorization volume, technical themes, transfer and licensing status, and international patent situation.The results reveal that comprehensive universities and China Pharmaceutical University are superior to other pharmaceutical universities in terms of patent application volume and licensing rate.From the perspective of patent classification, most of the relevant patents involve the effective ingredients of drugs.Comprehensive universities and China Pharmaceutical University pay more attention to the research of anti-tumor drugs.Among all authorized patents, the quantity is insufficient, and most of them are exclusive licenses.The transfer of relevant rights mostly occurs between universities and enterprises.In terms of international patent applications, comprehensive universities dominate in terms of quantity, but the total amount is still insufficient.In the future innovation and development process of “double first-class” universities, it is necessary to improve the awareness of patent protection and layout, attract relevant talents, give full play to the advantages of university intellectual property information service centers, and promote the transformation of university achievements.
    Select AllDeselectExport
    Display Method:
    Select AllDeselectExport
    Display Method:
    Select AllDeselectExport
    Display Method:
    Advances of Hedgehog pathway in tumor resistance
    HUANG Shaoliang, ZHAO Li, GUO Qinglong, WU Yulin
    2016,47(3):259-266. DOI: 10.11665/j.issn.1000-5048.20160302
    [Abstract] (4082) [HTML] (0) [PDF 1.56 M] (44153)
    Abstract:
    Hedgehog pathway regulates the physiological process of tumor cells, including proliferation, cycle, invasion and metastasis, and maintains tumorigenesis and development. With abnomal activation of Hedgehog pathway, most tumors response poorly to chemotherapy, which is mediated by Hedgehog pathway through activation of target gene and crosstalk with other pathways. Herein, Hedgehog pathway has been an important target for reversing resistance. In this study, the Hedgehog pathway and role of Hedgehog-mediated resistance in recent years are reviewed.
    Pharmaceutical cocrystals and salts
    MA Kun, GAO Jing, MA Lei
    2012,43(5):475-480. DOI:
    [Abstract] (4350) [HTML] (0) [PDF 947.09 K] (15411)
    Abstract:
    New solid forms with modified physicochemical and biopharmaceutical properties can be obtained by introducing different guest molecules to form cocrystals or salts.This approach appears to be an advantageous alternative for pharmaceutical research and development.Inspired by the newly released Guidance for Industry：Regulatory Classification of Pharmaceutical Cocrystals,we reviewed the differences between cocrystals and salts in their definition,structure,characterization,regulatory issues and physicochemical properties such as solubility,stability as well as bioavailability.In addition,some newly developed techniques for characterizing cocrystals or salts are also introduced.
    Research progress of prostaglandin receptors and related drugs
    徐 红, 孙宏斌
    2010,41(5):385-394. DOI:
    [Abstract] (5961) [HTML] (0) [PDF 1.18 M] (14895)
    Abstract:
    Prostaglandins is a kind of endogenous compounds with extensive physiological activities,and more than twenty kinds of natural prostaglandins have been found,while about two thousand prostanoid have been synthetized.These compounds have been developed as therapic agents,which are used in alimentary system,cardiovascular system, genital system and anti-glaucoma.Numerous types of prostaglandin receptors exist in organism,belonging to G-protein-coupled receptor superfamily,mediate multiple physiological and pathological processes,such as asthma,pain and inflammation.This review summarizes the properties of each type of prostaglandin receptor,and the clinical applications and research progress of drugs targeting their corresponding prostaglandin receptors.
    Transcription factors as new targets for cancer therapy
    刘楠, 陈依军
    2010,41(2):97-103. DOI:
    [Abstract] (6180) [HTML] (0) [PDF 539.59 K] (13278)
    Abstract:
    Mechanism studies in the gene regulation in the eukaryotic cells is one of the momentous areas in molecular biology.Regulation at transcription level is a complex progress with multiple steps with the presence of the gene functions.There exist ubiquitous occurrence of transcription factors in mammalian tissues and biodiversity in the factors.These transcription factors are found to relate closely to various carcinogeneses，including cell proliferation，apoptosis，invasion and angiogenesis.Understanding of transcription factors and their action mechanisms,through the activation and inhibition of transcription factors, would potentially lead to the discovery of new entities in the targeting treatment and prevention of the cancer diseases.
    Application progress of fullerene and its derivatives in medicine
    LIU Zeyuan, GUO Liangliang, ZHANG Jing
    2018,49(2):136-146. DOI: 10.11665/j.issn.1000-5048.20180202
    [Abstract] (2059) [HTML] (0) [PDF 2.90 M] (12517)
    Abstract:
    Fullerene is an effective free radical scavenger and antioxidant. The fullerene derivatives obtained by chemical modification of fullerene have good water solubility and biological activities. Fullerene and its derivatives have many advantages in cell protection and antioxidant properties, antibacterial activity, antiviral activity, photodynamic activity, drug delivery and anti-tumor activities, playing an important role in the field of medicine. In recent years, great progress has been made in this field. In this review, we summarized the latest research progress and applications of fullerene and its derivatives in medicine field at home and abroad from four aspects of regulating tumor microenvironment, drug delivery, photodynamic therapy and anti-oxidative stress. At last, the future development and application of fullerene and its derivatives in the domain of medicine are prospected.
    Advances of mesoporous silica nanoparticles as drug delivery system
    TANG Yue, KE Xue
    2012,43(6):567-572. DOI:
    [Abstract] (2403) [HTML] (0) [PDF 1.38 M] (12139)
    Abstract:
    Mesoporous silica nanoparticles(MSNs) is a new inorganic material which has attracted extensive attention as drug nanocarriers in recent years.In this review,we summarized the current investigations about the preparation,biocompatibility,drug loading and drug delivery applications of MSNs.
    Advances in analytical techniques for the determination of genotoxic impurities in pharmaceuticals
    RUAN Xiaoling, ZHENG Xiangyuan, XU Jie, DING Li, ZHENG Feng
    2016,47(3):267-274. DOI: 10.11665/j.issn.1000-5048.20160303
    [Abstract] (2796) [HTML] (0) [PDF 1.07 M] (11771)
    Abstract:
    Genotoxic or potentially genotoxic impurities seriously threaten people′s health, therefore, it is necessary to identify and quantify these impurities in pharmaceutical materials even at trace levels. Due to the special requirements on the sensitivity, selectivity, analyte stability and matrix effect, development of analytical methods is a challenge for the determination of genotoxic impurities. This paper reviews the recent advances in analytical methods for trace levels of commonly encountered genotoxic or potentially genotoxic impurities, including alkyl halides, alkyl sulfonates, hydrazines, epoxides and acyl halides, which would be helpful to control these impurities.
    Comparative pharmacokinetics of aconitine, mesaconitine and hypaconitine in rats after oral administration of four decoctions composed with Radix Aconiti Lateralis
    何雷萍, 狄 斌, 杜迎翔, 严 方, 刘华清
    2010,41(1):55-59. DOI:
    [Abstract] (5320) [HTML] (0) [PDF 969.51 K] (11609)
    Abstract:
    Aim：To study pharmacokinetics of aconitine，mesaconitine and hypaconitine in rats after single oral administration of decoctions composed with Radix Aconiti Lateralis.Methods：Four groups of rats were orally administered four decoctions including decoction a(Sini decoction)，decoction b（decoction composed with Radix Aconiti Lateralis)，decoction c(decoction composed with Radix Aconiti Laterali and Radix et Rhizoma Glycyrrhizae Praeparata Cum Melle) and decoction d(decoction composed with Radix Aconiti Laterali and Rhizoma Zingiberis)，respectively.Quantitative analysis of aconitine，mesaconitine and hypaconitine in rat plasma was achieved using a liquid chromatography-electrospray ionization/tandem mass spectrometry method.Pharmacokinetic parameters were estimated using DAS 2.0.Results：Pharmacokinetic parameters of aconitine，mesaconitine and hypaconitine were different after oral administration of four decoctions according to Radix Aconiti Laterali combined with different herbal medicines.Multiple peaks were observed in plasma concentration-time curve after oral administration of the decoction of herb couple Radix Aconiti Laterali and Radix et Rhizoma Glycyrrhizae Praeparata Cum Melle，and the results showed a delay in tmax and a prolonger in MRT0-t compared with the decoction of Radix Aconiti Lateralis.When Radix Aconiti Lateralis was combined with Radix et Rhizoma Glycyrrhizae Praeparata Cum Melle and Rhizoma Zingiberis at the same time in Sini decoction，tmaxwas delayed too but MRT0-t was shorten than that of the group of Radix Aconiti Lateralis.Conclusion：The pharmacokinetic parameters of the three compounds obtained in this work shows that the pharmacokinetics of aconitine，mesaconitine and hypaconitine were influenced diversely when Radix Aconiti Laterali was combined with different herbal medicines.
    Advances on novel drug delivery system
    WU Qu, HUO Meirong, ZHOU Jianping
    2013,44(2):97-104. DOI: 10.11665/j.issn.1000-5048.20130201
    [Abstract] (2820) [HTML] (0) [PDF 1.03 M] (11173)
    Abstract:
    Modern pharmaceutics has undergone a rapid development in recent years.For the significance of reducing adverse drug reaction,improving drug efficiency and ensuring safety of drugs,novel drug delivery system (DDS) shows expansive foreground.The latest advances on modern pharmaceutics including organic drug DDS,inorganic drug DDS and biopharmaceutics DDS,are reviewed in this paper.
    Advances in research on the modulation of autophagy by Ras/Raf/MEK/ERK signaling pathway
    WANG Xue, ZHANG Pinghu
    2017,48(1):110-116. DOI: 10.11665/j.issn.1000-5048.20170117
    [Abstract] (1683) [HTML] (0) [PDF 1.00 M] (11008)
    Abstract:
    Autophagy is a conserved self-defense mechanism of organism, degrading the necrotic organelles and excess protein into small molecules for recycling. Autophagy plays a role in both physiological and pathological condition, influencing the expression of intracellular substance through multiple signaling pathways. Although it has been demonstrated that Ras/Raf/MEK/ERK signaling pathway was not only extensively involved in the regulation of cell growth, proliferation, differentiation and apoptosis, but was also implicated in autophagy and autophagic cell death, though its detailed mechanisms involved in regulation of autophagy has not been fully elucidated yet. This review focused on the advances of autophagy induced by Ras/Raf/MEK/ERK signaling pathway, to better understand the role of Ras/Raf/MEK/ERK signaling pathway in regulation of autophagy.
    Advances in targeted drug delivery system
    KE Xue
    2012,43(1):9-15. DOI:
    [Abstract] (3410) [HTML] (0) [PDF 1.31 M] (10705)
    Abstract:
    Targeted delivery system have been the important research fields in pharmaceutics,but the complicated physiological conditions hinder the targeting efficacy.The scientists took many strategies in designing the drug carriers to face the situation,including the intelligent delivery system and adaptive delivery system,which can navigate drug carriers through the blood hurdles,target to the specific cell,even the organelle.The review introduced these advances.
    Poly(ADP-ribose) polymerase inhibitors and synthetic lethality
    ZHAO Na, SUN Hong-bin
    2012,43(2):107-112. DOI:
    [Abstract] (4318) [HTML] (0) [PDF 1.10 M] (10528)
    Abstract:
    In recent years,some new anticancer strategies have been found with a growing understanding of the underlying biology of cancer.For example,molecular targeting cancer therapy,which is based on the oncogene addiction phenomenon,had proved to be a successful strategy in some specific cancer types.A more recent example came from synthetic lethality which is now showing great promise as a new direction of anticancer drug discovery.Previous research has shown that PARP-1 and BRCA have a relationship of synthetic lethality.We herein describe the rationale of this synthetic lethality and the potential applications of this interaction in anticancer therapy.
    Advances in the tumor microenvironment-responsive smart drug delivery nanosystem
    LIU Yanhong, ZHOU Jianping, HUO Meirong
    2016,47(2):125-133. DOI: 10.11665/j.issn.1000-5048.20160201
    [Abstract] (2590) [HTML] (0) [PDF 1.73 M] (10425)
    Abstract:
    With the rapid development of nanotechnology and in-depth understanding of tumor microenvironment, stimuli-responsive smart drug delivery nanosystem based on tumor microenvironment(TME)has received extensive attention. TME-responsive smart delivery nanosystem can transport antitumor drug in circulation stably, after arriving in tumor tissue or targeted cells, the structure of nanocarriers changes under the stimuli of TME. Improved drug concentrations in targeted site significantly increase the antitumor efficiency and reduce the side effects of drugs. The stimulating factors in the TME include pH, redox potential, enzyme, reactive oxygen species(ROS), adenosine-5′-triphosphate(ATP)and so on. This review mainly gives a comprehensive overview in the latest research and new development in TME-responsive smart drug delivery nanosystems for efficient tumor therapy, mainly based on pH response type, enzyme response, reduction response, ROS response, and ATP response smart drug delivery nanosystems. Moreover, research directions in the future are pointed out in this review.
    Advances of new antidiabetic drugs
    XU Si-sheng, ZHANG Hui-bin, ZHOU Jin-pei, HUANG Jian-jun
    2011,42(2):97-106. DOI:
    [Abstract] (6754) [HTML] (0) [PDF 1.12 M] (10417)
    Abstract:
    Diabetes mellitus,an epidemic metabolic disorder characterized by high blood glucose level associated with various microvascular complications,is one of the main causes of human suffering across the globe.With the advance of the pathogenesis of diabetic research,the study of anti-diabetic drugs has transformed from the traditional drugs to the current products with new targets and new mechanism.Some of these drugs are already marketed or still in clinical trials,e.g. GLP-1 activator,DPP-4 inhibitor,GPR119 activator,SGLT-2 inhibitor,11β-HSD1 inhibitor,PTP1B inhibitor and so on.In this article,the new antidiabetic drugs mentioned above are reviewed with regard to the therapeutic targets and mechanism.
    Tumor microenvironment：A novel target for antitumor activity of polysaccharides
    张 先, 高向东
    2010,41(1):1-10. DOI:
    [Abstract] (7746) [HTML] (0) [PDF 1.09 M] (10123)
    Abstract:
    Tumor microenvironment plays a crucial role in neoplastic evolution process as it may provide functional interactions between neoplastic and non-neoplastic cells involved in tumor invasion，metastasis and angiogenesis，which implies that it can be regarded as a novel target for the antitumor therapy of polysaccharides. This review focuses on the protumor variations existing in tumor microenvironment，such as growth factors，immunosuppressive factors，proteases，glycoproteins，etc.，which may offer possible mechanisms of polysaccharides on the regulation of their corresponding functions.
    Application of pharmacometrics in drug development and therapeutic drug monitoring
    尚德为, 王曦培, 邓晨辉, 毕姗姗, 管 峥, 周田彦, 卢 炜
    2010,41(1):91-96. DOI:
    [Abstract] (3227) [HTML] (0) [PDF 1.01 M] (9739)
    Abstract:
    Pharmacometrics，developed from the conventional pharmacokinetics，is the science of applying mathematical and statistical methods to characterize，understand，and predict a drug′s pharmacokinetic，pharmacodynamic，and biomarker-outcome behaviors.Pharmacometrics has been widely valued for its utility of modeling and simulation in drug research and development，therapeutic drug monitoring and individualized therapy.This paper reviewed the advances of pharmacometrics employed in new drug research and development and therapeutic drug monitoring both at home and abroad.
    Advances in indoleamine 2, 3-dioxygenase 1 inhibitors
    CHENG Yulan, MEN Jinxia, ZHOU Jinpei, ZHANG Huibin
    2017,48(3):361-370. DOI: 10.11665/j.issn.1000-5048.20170318
    [Abstract] (1737) [HTML] (0) [PDF 2.19 M] (9290)
    Abstract:
    Indoleamine 2, 3-dioxygenase 1(IDO1)is the rate-limiting enzyme which catalyses the metabolism of L-tryptophan(L-Trp)in the kynurenine pathway. It is overexpressed in many tumor cells and antigen presenting cells. This enzyme inhibits local immune response and supports tumor cells to evade immune surveillance by depleting L-Trp and producing kynurenine metabolites, thus, it is an important target for cancer immunotherapy. There are several IDO1 inhibitors with different scarfold under investigation, three of which have already entered clinical stage. The role of IDO1 in tumor immune tolerance and the research progress on IDO1 inhibitors in recent years are summarized in this paper.
    Effects of various autophagy modulators on the expression of autophagic markers LC3II and p62
    WEI Yanming, REN Jinhong, LUAN Zhihua, WANG Yonghui
    2018,49(3):341-347. DOI: 10.11665/j.issn.1000-5048.20180313
    [Abstract] (1613) [HTML] (0) [PDF 2.54 M] (9027)
    Abstract:
    Western blotting of autophagic markers LC3II and p62 are widely used for estimating autophagic activity. To compare the regulation of various autophagy modulators on LC3II and p62, HEK293 cells were treated separately with mTOR-dependent autophagy activator rapamycin or -independent autophagy activators trehalose, and autophagy inhibitors including 3-methyladenine(3-MA), bafilomycin A1 or E64d and pepstatin A that inhi-bited the initiation of autophagy, the fusion of autophagosome and lysosome, and the activities of lysosomal enzymes accordingly, and then LC3II and p62 levels were assessed. Western blot results demonstrated that rapamycin enhanced the conversion of LC3I to LC3II, promoted the degradation of p62 simultaneously, while trehalose merely increased the expression of LC3II with no influence on the p62 level. Moreover, inhibition of autophagy commonly led to accumulation of LC3II as well as blockage of p62 degradation in a concentration- and time- dependent manner. These results indicate that obvious differences exist in the regulation of LC3II and p62 by various modulators although both are autophagic markers.
    Progress in research on the determination of entrapment efficiency of liposomes
    ZHANG Yi, HANG Taijun, SONG Min
    2021,52(2):245-252. DOI: 10.11665/j.issn.1000-5048.20210214
    [Abstract] (1380) [HTML] (1356) [PDF 739.10 K] (8547)
    Abstract:
    Liposome, a new dosage form, has become important in improving in vivo behavior of drugs or realizing targeted drug delivery. Study and control of its critical processes and quality attributes are the main challenges in the current research on liposomes. The degree of encapsulation can determine drug''s effect in vivo directly, thus entrapment efficiency (EE) has turned into one of the critical quality attributes of liposome.In this paper some methods commonly used for the determination of EE and their characteristics are summarized and analyzed, and the main factors to be considered for the determination are discussed.
  • 中国药科大学学报
  • 主    编：王广基
  • 常务副主编：尤启冬
  • 副主编：孔令义 吴晓明 张奕华
  • 主    办：中国药科大学
  • 地    址：江苏省南京市童家巷24号
  • 电    话：025-83271566
  • 传    真：025-83271279
  • E-mail：xuebao@cpu.edu.cn
  • 刊    号：ISSN 1000-5048  
                    CN 32-1157/R

    • Download center

      • 扫一扫关注微信号

    External Links

    总访问量：


    版权所有：Editorial Office of Journal of China Pharmaceutical University   苏ICP备12050101号-2
    地址：24 Tongjiaxiang, Nanjing, Jiangsu Province, PRC 电话: 025-83271566 83271562 传真: 025-83271279 E-mail:cpuxuebao@sohu.com; cpuxuebao@yahoo.com.cn
    技术支持：北京勤云科技发展有限公司