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Table of Content

    20 May 2015, Volume 24 Issue 5
    Review
    Reversal of multidrug resistance in cancer treatment by regulating multidrug resistance gene1: focus on nuclear receptors and epigenetics
    Tingting Li, Zhijun Wang, Haiyan Liu, Huiru Xie, Xuehua Jiang, Ling Wang
    2015, 24(5):  273-284.  DOI: 10.5246/jcps.2015.05.036
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    Overexpression of P-glycoprotein (P-gp) encoded by the multidrug resistance gene-1 (MDR-1) is the main mechanism responsible for multidrug resistance (MDR) in a majority of cancer cells. However, the mechanism by which cancer cells acquire high levels of P-gp has not been well defined. Accumulating evidence suggests that nuclear receptors (NRs), especially human pregnane X receptor (PXR), play a crucial role in multidrug resistance. It has been shown that chemotherapeutic drug activates PXR and then enhances P-gp expression. Genetic knockdown or pharmacologic inhibition of PXR led to attenuation of drug-inducedMDR1 over expression, implying that NRs may be an effective target to reverse multidrug resistance. Recent investigations suggested that transcriptional activity of NRs is mediated by methylases, the important enzymes involved in epigenetic regulation. Other epigenetic modifications, such as promoter methylation, histone deacetylases and microRNAs, were also found to be involved in activation of MDR1 promoter, though the underlying mechanisms are not thoroughly known. In this review, we summarized recent researches in the regulation of P-gp expression, with particular focus on NRs and epigenetics, aiming to provide references and options to reverse and/or prevent MDR in cancer treatment.

    Original articles
    Microbial transformation of isoangustone A by Mucor hiemalis CGMCC 3.14114
    Jin Feng, Wenfei Liang, Shuai Ji, Xue Qiao, Yingtao Zhang, Siwang Yu, Min Ye
    2015, 24(5):  285-291.  DOI: 10.5246/jcps.2015.05.037
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    Isoangustone A (1) is an isoprenylated flavonoid isolated from licorice. It has been reported to possess anti-microbial, anti-oxidative, anti-inflammatory, and anti-tumor activities. In order to increase its structural diversity, microbial transformation of 1 was conducted by Mucor hiemalis CGMCC 3.14114 to obtain three new compounds. By extensive NMR and MS spectroscopicanalyses, their structures were identified as isoangustone A 7-O-glucoside (2), isoangustone A 7-O-glucoside-4'-O-sulfate (3), and isoangustone A 7,3'-di-O-glucoside (4), respectively. The major biotransformation reaction was glycosylation at C-7. Sulfation is rare for microbial transformation.

    Phytochemical screening and wound healing potential of Cuscuta reflexa
    Tapsya Gautam, Surya Prakash Gautam, Raj K. Keservani, Anil Kumar Sharma
    2015, 24(5):  292-302.  DOI: 10.5246/jcps.2015.05.038
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    The present study was to investigate pharmacognostical, phytochemical and pharmacological properties of extracts from stem of Cuscuta reflexa Roxb.Standard procedures have been followed to evaluate the pharmacognostical properties and preliminary screening of phytochemicals of Cuscuta reflexa Roxb. Albino Wistar rats (either sex) weighing 150200 g were taken and made to acclimatize by providing them with the appropriate room conditions in the experimental room. Excision wound model has been selected for analgesic and wound healing activity for evaluating potential of the water-extract and ethanolicextract from the stem of Cuscuta reflexa Roxb. The macroscopic and microscopic studies showed the various characteristic features of stems. Preliminary screening of phytochemicals reveled that alkaloids, glycosides, flavonoids were the major groups of phytochemicals present in the successive extracts. Water and ethanolic extracts from stem of Cuscuta reflexa Roxb at 200 mg/kg and 400 mg/kg were able to alleviate pain and wounds. It is concluded that the stems of Cuscuta reflexa Roxb have a markedly therapeutic potential to heal wound and may provide the pharmacological basis for its folk uses.

    Analysis of the constituents in Semen Descurainiae by UPLC/Q-TOF-MS/MS
    Zuohuan Meng, Li Qiao, Zongquan Wang, Zhensi Ma, Jiming Jia, Qingxian Chang, Wenlie Li
    2015, 24(5):  303-309.  DOI: 10.5246/jcps.2015.05.039
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    A UPLC/Q-TOF-MS/MS method was developed for identifying the constituents in the Chinese herb Semen Descurainiae. A total of 14 compounds were identified or tentatively characterized based on their mass spectra, including 9 flavonoids, 4 fatty acids and 1 cardiac glycoside. Among them, quercetin-3-O-β-D-[6-O-sinnapoyl-2-O-β-D-glucopyranosyl]-glucopyranoside was identified in Semen Descurainiae for the first time.

    Qualitative and quantitative analysis of HPLC fingerprint of Wuji gastric floating sustained-release tablets
    Zhongfen Chen, Wen Liu, Daye Chen, Xiaowei Shi, Qun Wang
    2015, 24(5):  310-317.  DOI: 10.5246/jcps.2015.05.040
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    A qualitative and quantitative test method of fingerprint of Wuji gastric floating sustained-release tablets was established. High performance liquid chromatography (HPLC) was adopted, using Agilent ZORBAX SB-C18 column (250 mm×4.6 mm, 5 μm) as the chromatographic column, and acetonitrile0.05 mol/L potassium dihydrogen phosphate solution as the mobile phase in a gradient elution with the flow rate of 1.0 mL/min. Sample solution (10 μL) was injected and was tested at the wavelength of 225 nm for 75 min at the column temperature of 30 ºC. Fingerprint similarity software (2004A version) was used to conduct data analysis. A total of 11 batches of Wuji gastric floating sustained-release tablets were tested and analyzed with HPLC fingerprint. Seventeen common peaks were found and the similarity of the 11 batches of agents was greater than 0.9, indicating that the production process of the agent is stable and feasible. The method is operable and could effectively control the quality of Wuji gastric floating sustained-release tablets.

    Simultaneous determination of four saponins in Shugan Quzhi Capsule by UHPLC-MS/MS
    Zhiyan Lin, Rongfu Yang, Yuenian Tang, Huaiping Tian, Xinzhu Liu, Xiaotong Lu
    2015, 24(5):  318-325.  DOI: 10.5246/jcps.2015.05.041
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    Shugan Quzhi capsule is a hospital preparation of Xinhua Hospital affiliated to School of Medicine, Shanghai Jiaotong University. It has been used for the treatment of adult patients with fatty liver caused by obesity, high cholesterol and other factors. In the present study, we established an ultra-high pressure liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS) method to simultaneously determine 4 saponiningredients including Notoginsenoside R1, Ginsenoside Rb1, Ginsenoside Re and Ginsenoside Rg1 present in Shugan Quzhi capsule. The chromatographic separation was conducted on ZORBAX SB-C18 (2.1 mm×50 mm, 1.8 μm). The mobile phase was composed of acetonitrile and aqueous solution consisted of 0.05% formic acid and 5 mM ammonium acetate. Gradient elution rate was 0.3 mL/min, the column temperature was 40 ºC; MS was conducted using electrospray ionisation (ESI) and multiple reaction monitoring (MRM) coupled with positive and negative scanning switch. With which, Ginsenoside Re and Ginsenoside Rg1 were detected using negative ion mode detection while Notoginsenoside R1, Ginsenoside Rb1 and internal standard (Ginsenoside F1) were detected using positive ion mode detection. The limits of quantification (LOQ) for Notoginsenoside R1, Ginsenoside Rb1, Ginsenoside Re and Ginsenoside Rg1 were 6.54×10–4, 2.57×10–4, 0.11 and 6.91×10–3 ng/mL, respectively. The limits of detection (LOD) for these compounds were 1.96×10–4, 7.70×10–5, 3.45×10–2, and 2.07×10–3 ng/mL, respectively. All calibration curves showed a good linearity (r2>0.9633) within the test range. The intra- and inter-day precisions (relative standard deviation, RSD) were lower than 5% and the average recoveries were in the range of 80%–120%. With this method, four kinds of saponins were separated and detected in 6 min. This method is simple, rapid and shows high sensitivity and accuracy.

    Increased risk of hyperglycemia associated with the use of everolimus in patients with cancer: a systematic review and meta-analysis
    Zihan Guo, Yuanyuan Jiao, Zhanmiao Yi, Ran Li, Yanhua Zhang
    2015, 24(5):  326-335.  DOI: 10.5246/jcps.2015.05.042
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    Everolimus is an orally administered rapamycin analogue that has been approved to treat several types of solid tumors. However, some patients develop hyperglycemia after being treated with everolimus. In this meta-analysis, we aimed to evaluate the incidence and risk of hyperglycemia in patients with cancer who received everolimus. We searched the medical literature, as index in the Cochrane Library, PubMed, EMBASE, and abstracts from the top scientific meetings (AACR, ASCO, and ESMO). Our meta-analysis included the randomly controlled trials published before November 2014. We calculated overall incidence, relative risk (RR) and 95% confidence intervals (CI) using fixed-effects or random-effects models, depending on the heterogeneity among the trials. A total of 3377 patients (everolimus: 1971; control: 1406) from 8 randomized clinical trials were included in the meta-analysis. In the everolimus groups, the incidence of all grades of hyperglycemia was 20.0% (95% CI: 11.0%–29.0%), while the incidence of high-grade hyperglycemia was 6.0% (95% CI: 3.0%–8.0%). Patients treated with everolimus had an increased risk of hyperglycemia as compared with that of controls (all-grade RR: 2.94, 95% CI: 2.34–3.70; high-grade RR: 4.66, 95% CI: 2.75–7.89). Everolimus significantly increased the risk of hyperglycemia. This risk may depend on the tumor type and the everolimus dosage.

    Pharmacokinetics of lipoic acid in healthy Chinese volunteers after single and multiple doses of Lipoic acid dispersible tablets
    Hengli Zhao, Ruoming Cao, Zengjun Fang, Haisheng Wang
    2015, 24(5):  336-341.  DOI: 10.5246/jcps.2015.05.043
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    This study aimedto evaluate the pharmacokinetics for lipoic acid (LA) after oral administration of 12 healthy Chinese volunteers with single and multiple-dose of lipoic acid dispersal tablets using a liquid chromatography-temdend mass spectrometry (LC-MS/MS) methods. In single-dose study, healthy Chinese male and female volunteers received three dose levels at 0.2, 0.3, and 0.4 g of LA dispersal tablets with a 3×3 Latina square design. In multiple-dose study, 12 healthy Chinese volunteers received orally a 0.1 g of LA dispersible tablet three times daily for 6 consecutive days and 0.3 g once on day 7. The results showed that pharmacokinetics of LA fitted a two-compartment open model. The values of area under the curve (AUC) increased proportionally within the range of 0.2–0.4 g, while the Vd/F, CL/F, MRT, t1/2 and tmax of LA were similar at three dose levels. The steady-state pharmacokinetic parameters of LA were similar to those following a single dose and no accumulation was found following multiple-dose of LA dispersal tablets.

    Short communication
    Development strategy for hospital preparations from a management view
    Haining Yu, Guochun Bao
    2015, 24(5):  342-345.  DOI: 10.5246/jcps.2015.05.044
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    With the development of medical environment, the development of hospital preparations is facing more and more difficulties, and the number of preparations is gradually shrinking. In this article, the authors reviewed the advantages of hospital preparations and analyzed the reasons that reduce hospital preparations from three aspects: the characteristics of hospital preparations, the innovation capacity and human resources and the quality of the preparations. Then the authors took a deep thought about the development strategy on current hospital preparations from the perspective of management. The purpose is to survey the developing trend of hospital preparations in China, and to serve the people’s health wholeheartedly.

    Editor profile
    Introduction of Professor Dean Guo
    Journal of Chinese Pharmaceutical Sciences
    2015, 24(5):  346-346. 
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    Dean Guo, principal investigator/leading scientist of Shanghai Institute of Materia Medica, Chinese Academy of Sciences, director of National Engineering Laboratory for TCM Standardization Technology, director of Research Center for Modernization of Traditional Chinese Medicine. Obtained his Ph. D of Pharmacognosy in Beijing Medical University in 1990. Worked as a postdoctor in Department of Chemistry and Biochemisty,Texas Tech University, USA from 1993 to 1996. Principal social concurrent posts include Member of Drug Evaluation Committee of SFDA, Member of the Executive Committee of the National Pharmacopoeia Committee, Expert Committee member of United States Pharmacopoeia, Board Memberand Advisor of Society for Medicinal Plant Research (GA), Advisor and Expert of Panel of the American Botanical Council (ABC). He also serves as Associate editor or Editorial Board member of 16 international journals such as Journal of Chinese Pharmaceutical Sciences, Journal of Ethnopharmacology, Planta Medica, and etc.