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Table of Content

    21 January 2020, Volume 29 Issue 1
    Review
    Emodin and shikonin (quinones): an overview of their chemistry, plant sources, pharmacology and cytotoxic activities against lung cancer
    Eric Wei Chiang Chan, Chen Wai Wong, Siu Kuin Wong, Yew Woh Hui, Joash Ban Lee T
    2020, 29(1):  1-12.  DOI: 10.5246/jcps.2020.01.001
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    Emodin and shikonin are quinones that are commonly found in the roots of plant species of the families Polygonaceae and Boraginceae, respectively. They have a wide spectrum of bioactivities, including anti-cancer properties. This overview on the cytotoxic properties of emodin and shikonin is focused on lung cancer, the leading cause of cancer death in the world. In emodin, the −OH groups at C1 and C3 positions, while in shikonin, the −OH groups of the naphthazarin moiety and chiral side-chain, are important for their anti-tumour functions. Studies have shown that emodin and shikonin inhibit the growth of lung cancer cells by inducing apoptosis, autophagy, necrosis and early senescence, and by inhibiting proliferation, invasion, migration and metastasis. The cytotoxic activities are involved multiple molecular targets and signalling pathways. A clinical trial using shikonin to treat patients with late-stage lung cancer has been presented. Some future perspectives and research needs are suggested. Sources of information are from Google Scholar, PubMed, Science Direct, J-Stage, PubChem and CNKI. 
    Original articles
    Application of proteomic approaches to assess the effect of anti-epileptic drug on seizure foci
    Yujing Song, Xuyang Zhao, Qian Chen, Yan Song, Wanyu Lei, Yuxin Yin, Weining Ma, Zhuo Huang
    2020, 29(1):  13-28.  DOI: 10.5246/jcps.2020.01.002
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    Epilepsy is one of the most common neurological disorders characterized by epileptic seizures. The anti-epileptic drugs (AEDs) are the main form of treatment for people with epilepsy. Classically, people thought that AEDs modify the activities of ion channels to suppress epileptic seizures. However, accumulating evidence suggests that targeting at ion channels cannot completely account for the numerous effects of the AEDs on its broad clinical activity in epileptic patients. In our study, proteomic methods were used to quantify the proteome of hippocampal tissues from patients who were treated or not treated by AEDs (Carbamazepine). Further bioinformatics methods, including Gene Ontology (GO) annotation and Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway enrichment analysis, were utilized to analyze the differences between two patient groups. We found that more than 400 proteins, including metabolism and immune related proteins, had a higher expression level in the carbamazepine-treated group compared with the controls. These altered proteins were considered to be involved in many different biological pathways. Among these pathways, immune-system related pathway modulated by complement C3 and microglia was highly remarkable, which regulated the synapses elimination in physiological condition. In epilepsy, the carbamazepine induced up-regulation of complement C3 might decrease the abnormal synaptic connections between neurons and thus contribute to the therapeutic role of carbamazepine. The results of our study suggested that apart from ion channels, carbamazepine exerted numerous effects on human epileptic foci, which might be the fundamental mechanisms of AEDs for treatment, adverse-effects and pharmacoresistance of epilepsy.
    Design, synthesis and evaluation of carbamate-containing sialyltransferase inhibitors
    Wanjun Yan, Wenming Li, Decai Xiong, Xinshan Ye
    2020, 29(1):  29-44.  DOI: 10.5246/jcps.2020.01.003
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    A series of carbamate-containing sialyltransferase inhibitors were designed and synthesized to simulate phosphate-linkedCMP-Neu5Ac. Their inhibitory activities were assayed against recombinant human ST3Gal I and ST6Gal I by using the Schmidt’sHPLC-based assay. The synthetic compound 15g showed moderate inhibitory activity. These findings implied that carbamate might serve as a bioisosteric replacement for a phosphate group in sialyltransferase inhibitor design to improve the membrane permeability.                   
    Pharmacodynamic model of dopamine D1 receptor agonists in the treatment of breast cancer lung metastasis
    Liang Yang, Ye Yao, Yaoyao Feng, Wei Lu, Tianyan Zhou
    2020, 29(1):  45-54.  DOI: 10.5246/jcps.2020.01.004
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    Previous study has shown that dopamine D1 receptor (D1DR) agonists, fenoldopam (FEN) and l-stepholidine (l-SPD), have inhibitory effects on breast cancer lung metastasis. To quantitatively describe and predict the pharmacodynamic (PD) properties of FEN and l-SPD and to explore the PD model structure of cancer metastasis treating drugs, we used the data of lung metastasis in 4T1 breast cancer mice under the treatment of either FEN or l-SPD, and established a PD model. The PD model assumed an exponential growth for both primary tumor and metastasis. The primary tumor emitted cells to form metastases, and the cell emitting rate was proportional to power form of the primary tumor weight. The total number of lung metastasis was set as the target value. D1DR agonists inhibited metastasis by inhibiting cell emitting rate instead of the growth rate of primary tumor or metastasis. The model results showed that the decrease in the number of lung metastases was roughly proportional to the square of the drug dose. The values of PD coefficient reflected the inhibitory ability of the drugs, and that of l-SPD (0.274 kg/mg) was greater than that of FEN (0.0393 kg/mg). This PD model can quantitatively describe the effects of FEN and l-SPD on the progression of lung metastasis in 4T1 primary breast cancer mice and can predict the time course of drug efficacy at multiple doses, providing a reference for PD model structure of other drugs for cancer metastasis indication.
    Study on solubility improvement of lidocaine by ternary solid dispersion
    Wenling Fan, Yan Xu, Xinyi Zhang, Liuqing Di, Lei Li
    2020, 29(1):  55-65.  DOI: 10.5246/jcps.2020.01.005
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    In the present study, we aimed to probe the possibility of using mixed poloxamers as carriers to prepare ternary solid dispersion (SD) that facilitated solubility and dissolution rate of the poorly water soluble drug and compare with binary SD with single poloxamer. Lidocaine (LIC) was selected as a model drug, and poloxamer 188 (P188) and poloxamer 407 (P407) were utilized as single and mixed carriers. Depending on DSC and the dissolution testing, the appropriate ratio of SD prepared by melting method was optimized. Ternary and binary SD was characterized by DSC, XRD, SEM and FTIR. In vitro dissolution study, phase solubility study and saturated solubility study were performed to clarify solubilization from apparent phenomena and inherent reason. Moreover, stability study under different relative humidity (RH) was investigated. Physical characterizations of binary and ternary SD exhibited the formation of eutectic mixture and the presence of molecular interaction. Compared with the pure LIC, the dissolution rate and solubility of LIC in binary and ternary SDs were enhanced. The phase solubility study revealed an AL-type curve. Furthermore, the stability test indicated that ternary and binary SD was stable. The results of this study demonstrated that SD with mixed poloxamers could improve dissolution rate and solubility of poorly water-soluble drug.
    The others
    Information for Authors
    Journal of Chinese Pharmaceutical Sciences
    2020, 29(1):  66-75. 
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    Professor Zhang Qiang’s team won the 2019 National Science and Technology Progress Awards
    Shuxiang Song
    2020, 29(1):  76-78. 
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    Professor Zhang Qiang’s team won the 2019 National Science and Technology Progress Awards.