Table of Content

    27 October 2016, Volume 25 Issue 10
    The biological potentials of substituted 1,2-diazines: a review on versatile pyridazine derivatives
    Mohammad Asif
    2016, 25(10):  707-725.  DOI: 10.5246/jcps.2016.10.080
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    Many studies have been performed on the pyridazine (1,2-diazine) derivatives in the past decade. This heterocyclic nucleus possesses almost all types of pharmacological activities. This small and simple pyridazine nucleus is present in various compounds that are involved in the research aiming to evaluate new compounds with interesting biological activities, including anti-bacterial, anti-fungal, anti-viral, analgesic, anti-inflammatory, anti-platelets, anti-ulcer, anti-secretory, anti-depressants, anxiolytics, sedative-hypnotics, anti-convulsant, anti-tumor, anti-thrombotics, cardiotonics, vasodilatators, anti-arrhythmics, anti-diabetic, anti-tubercular agents and so on. This review focuses on the pyridazine derivatives with potential activities that have been developed. Pyridazine compounds draw attention of scientists and researchers because of their diverse biological activities as well as simple chemical and easy functionalization at various ring positions, making them attractive synthetic building blocks for designing and development of novel pyridazinone-based therapeutic agents.

    Original articles
    Design, synthesis and evaluation of novel non-ATP competitive CHK1 inhibitors as chemotherapy sensitizing agents
    Yuanxin Li, Zifei Han, Chao Tian, Zhili Zhang, Junyi Liu
    2016, 25(10):  726-736.  DOI: 10.5246/jcps.2016.10.081
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    A series of urea-based compounds containing purine moieties were designed and synthesized as novel non-ATP competitive CHK1 inhibitors. The biological evaluation showed that several target compounds exhibited more potent inhibitory effects against CHK1 than the lead compound. In addition, one particular compound displayed synergistic effects with gemcitabine against HT29 cells.

    A practical method to trace intracellular and transcellular transport pathways of gold nanoparticles via oral administration
    Dechun Liu, Dan Yang, Bing He, Wenbing Dai, Hua Zhang, Xueqing Wang, Lan Yuan, Qiang Zhang, Xing Tang
    2016, 25(10):  737-746.  DOI: 10.5246/jcps.2016.10.082
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    Oral nanoparticles play an important role in improving the bioavailability of poorly water-soluble drug. It is necessary to investigate the interaction of nanoparticles with intestinal epithelial cells. In general, nano-carriers labeled with fluorescent probes are always chosen. However, fluorescent dye via physical loading may leak in complex biological environment and lose its function to trace the transport behavior of nanoparticles. Fluorescent probes chemically coupled on the nanoparticles may alter the properties of nanoparticles. Therefore, a facile and exact detection method is required to trace intracellular and transcellular pathways of oral nano-medicines. In our study, gold nanoparticles were selected as nano-carriers owing to their unique characteristics of light scattering. The feasibility of gold nanoparticle detection through reflected light signal was tested in different situations, including gold nanoparticle solution, cell and animal level. As a result, high resolution image of gold nanoparticles could be detected through reflection mode by confocal laser scanning microscope (CLSM) when excited at a wavelength of 633 nm. The reflected light signal of gold nanoparticles could be clearly shown in different intestinal epithelial cells no matter when they were in fixed or in living state, and the intracellular trafficking and distribution of gold nanoparticles were clearly shown in three-dimensional image. Meanwhile, this method was also applied to rat small intestine in vivo. In conclusion, we believed that this technique was a convenient and precise way to explore the transport behavior of gold nanoparticles via oral administration without fluorescent dye.    

    Determination of gallic acid in the traditional Chinese medicine by high-performance capillary electrophoresis
    Yaya Gaoyang, Chenqi Zhu, Shuang Guo, Bailing Qiu, Di Wu, Ye Gao, Qihui Liang, Nanyin Han, Ping Zhang
    2016, 25(10):  747-753.  DOI: 10.5246/jcps.2016.10.083
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    Rhizoma Polygoni Bistortae has been widely used as an important medicinal herb in the Far East for a few thousand years, and it has gained more recognition in the last few decades. In the present study, we used a high-performance capillary electrophoresis (HPCE) method for determination of the gallic acid (GA) in Quanshen (QS) pieces. The analysis of GA in QS pieces was successfully achieved in less than 6 min by capillary electrophoresis with UV detection at a wavelength of 290 nm. The background electrolyte was 20 mmol/L sodium borate solution (pH 9.00). The separation was performed in an uncoated fused-silica capillary (52 cm×50 μm) with an effective length of 40 cm, and the applied voltage was 20 kV. Sample solutions were injected for 10 s at an atmospheric pressure of 5 KPa. The result showed good resolution and precision (the intra-day RSD was 0.37%). The calibration curves of the standard solutions were linear in the range of 0.22–2.25 mg/mL, with correlation coefficients greater than 0.9990. The recovery of the method ranged from 100.6% to 107.9%, and the average recovery of GA was 105.9% with an RSD of 3.63%. HPCE is a powerful technology, and it is the first time to successfully apply such a method for the determination of GA in the traditional Chinese medicine.  

    Vanadyl complexes work with cinnamaldehyde in promoting cell viability under the β­amyloid burden in SH­SY5Y neural cells
    Xue Li, Lidan Bai, Yaqiong Dong, Qing Chang, Rui Wu, Jing Zhang, Xiaoda Yang
    2016, 25(10):  754-763.  DOI: 10.5246/jcps.2016.10.084
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    The Alzheimer’s disease (AD) is one of the common cognitive disorders in the elderly. AD shares some similar pathological characters with diabetes mellitus (DM), suggesting potential application of anti-diabetic agents, such as vanadyl complexes, in therapeutic treatment of AD. In the present work, we studied the effects of vanadyl acetylacetonate (VO(acac)2) and cinnamaldehyde (CA) on an AD model based on SH-SY5Y neural cells. The experimental results showed that VO(acac)2 at sub-micromolar concentrations could improve the viability of neural cells with or without increased β­amyloid (Aβ) burden; and the combination of VO(acac)2 and CA showed an additive cell protection effects. Further investigation revealed that for SH-SY5Y neural cells, VO(acac)2 could activate PPARγ-AMPK signal transduction and inhibit GSK 3β, one of the major kinases for Tau hyperphosphorylation. Meanwhile, CA could correct the abnormal mitochondrial morphology due to Aβ-induced excessive mitochondrial fission, thus restoring/enhancing the mitochondrial function. In addition, both VO(acac)2 and CA decreased intracellular reactive oxygen species (ROS) level and inhibited formation of toxic Aβ oligomers. Overall, VO(acac)2 might work with CA in improving the neural cell viability under the Aβ burden, suggesting application of vanadium metallodrugs in AD treatment.

    The chemical constituents in the decoction of Urtica fissa rhizomes 
    Mengyue Wang, Xiaoru Feng, Chengqin Zhang, Jun Cheng, Enjia Liu, Li'ang Sun, Xiaobo Li
    2016, 25(10):  764-770.  DOI: 10.5246/jcps.2016.10.085
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    Phytochemical investigation of the decoction of Urtica fissa rhizomes led to the isolation of 23 known compounds. Their structures were identified as medioresinol dimethyl ether (1), L-pyroglutamic acid methyl ester (2), nicotinic acid (3), L-pyroglutamic acid (4), erythritol (5), 6-methyl-2′-deoxy thymidine (6), 2-methyl-6-(2′,3′,4′-trihydroxybutyl)-pyrazine (7), 5-hydroxyl-2-hydroxymethyl pyridine (8) , adenine (9), uracil (10), thymine (11), adenosine (12), inosine (13), 2-deoxyadenosine (14), 2′-deoxyguanosine (15), 2′-deoxyinosine (16), uridine (17), n-butyl-O-β-D-fructopyranoside (18), di-D-fructose (19), β-D-fructofuranosyl-α-D-galactopyranoside (20), bis (5-formyl-furfuryl) ether (21), chlorogenic acid (22), and 5-hydroxymethyl furaldehyde (23) by spectroscopic methods. In addition, a total of 20 compounds (1–20) were isolated from U. fissa for the first time. Meanwhile, compounds 1, 6, 7, 8, 19 and 20 were isolated from the Urticaceae plants for the first time.  

    Two novel phorbol esters from Croton tiglium L.
    Wentong Dou, Yanping Hao, Junli Liu, Dan Yuan, Hongzheng Fu
    2016, 25(10):  771-778.  DOI: 10.5246/jcps.2016.10.086
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    To investigate the phytochemical constituents of aboveground parts of Croton tiglium L. (family Euphorbiaceae), its ingredients were isolated by repeated chromatography on silica gel, Sephadex LH-20, ODS and preparative HPLC. Their structures were identified based on 1D, 2D NMR and mass spectral analysis. A total of 10 phorbol esters were obtained. Among them, compound 1 (12-O-(2-methyl)butyryl-4α-deoxyphorbol-13-isobutyrate) and compound 10 (20-formyl-4α-deoxyphorbol-13-acetate) were two new compounds, and the other eight were known compounds.

    Drug administration column
    Implementation of NFS (2012) in Qingdao: from the perspective of public policy implementation
    Chan Chen, Bin Li, Dongsheng Yang, Bin Jiang
    2016, 25(10):  779-784.  DOI: 10.5246/jcps.2016.10.087
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    The lunch of the National Fee Schedule (2012) triggered a new round of medical service price adjustment. In China, Qingdao is one of the early birds with best effects in implementing the new policy. This article analyzed the process and experiences of price adjustment of medical service in Qingdao and suggested that local governments in the process of implementing the National Fee Schedule (2012) fully utilize various influencing factors such as tools, resources and environment of policy implementation in order to obtain better policy results.