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Table of Content

    26 June 2015, Volume 24 Issue 6
    Original articles
    Efficient and convenient total synthesis of mycothiol on a large scale
    Zijie Liu, Youzhen Wu, Gang Liu
    2015, 24(6):  347-355.  DOI: 10.5246/jcps.2015.06.045
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    Mycothiol (MSH) is the major low molecular weight thiol in most actinomycetes. Chemical synthesis of MSH is of value for enzymology and inhibitor screening assays, but is hampered by difficulties in large scale sysnthesis. We achieved the totalsynthesis of MSH by linking 2-camphanoyl-3,4,5,6-tetra-O-benzyl-D-myo-inositol (D-1) and 2-deoxy-2-azido-3,4,6-tri-O-benzyl-1-p-toluene-thio-D-glucoside (2) first, followed by coupling with N-Boc-S-acetyl-L-cysteine (3). This route of synthesis allowed the efficient and convenient synthesis of mycothiol on a large scale.

    Synthesis of N(OMe)-linked TF antigen analogue
    Shuang Sun, Yanyan Liu, Yafei Cao, Youhong Niu, Qin Li, Xin-Shan Ye
    2015, 24(6):  356-363.  DOI: 10.5246/jcps.2015.06.046
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    Tumor-associated carbohydrate antigens (TACAs), important molecular markers on tumor cells, are major targets for the development of anti-cancer vaccines. However, due to the immunotolerance and weak immunogenicity, native TACAs cannotinduce powerful immune response. The use of modified TACAs such as N-glycosides could be an alternative strategy to overcomethis problem. Herein, the synthesis of N(OMe)-linked analogue of tumor-associated disaccharide antigen Thomsen-Friedenreich (TF) by the glycosylation reaction is described.

    Rapid determination of eight aristolochic acid analogues in five Aristolochiaceae plants by ultra-high performance liquid chromatography quadrupole/time-of-flight mass spectrometry
    Deqiang Kong, Huiyuan Gao, Xin Li, Jincai Lu, Dan Yuan
    2015, 24(6):  364-375.  DOI: 10.5246/jcps.2015.06.047
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    Aristolochic acids (AAs) and aristololactams (ALs) are commonly found in some Aristolochiaceae plants, and they have been reported to be AA nephropathy (AAN), nephrotoxicity and carcinogenicity. In the present study, we established an ultra high performance liquid chromatography (UHPLC) coupled with quadrupole/time-of-flight mass spectrometry (Q/TOF-MS) method for the rapid analysis of eight AA analogues in 19 samples originated from the five Aristolochiaceae plants, the roots and rhizomes of Asarum sieboldii Miq. var. seoulense Nakai, the fruits of Aristolochia contorta Bunge or A. debilis Sieb. et Zucc., the roots of Aristolochia debilisSieb. et Zucc., the stems of Aristolochia manshuriensis Kom., and the roots of Aristolochia fangchi Y. C. Wu ex L. D. Chou et S. M. Hwang. A total of five AAs and three ALs were identified by co-chromatography of sample extract and comparing the retention time, UV spectra, and characteristic molecular ions and fragment ions with those of authentic standards, or tentatively identified by MS/MS determination along with Mass Fragment software. Moreover, the method was validated for the simultaneous quantification or semi-quantification of them. The samples significantly differed in the quality and quantity of AA analogues, which allowed the possibility of showing their chemical distinctness, and it might be helpful in their standardization and quality control. Furthermore, in order to holistically compare the difference between the five Aristolochiaceaeplants, dataset obtained from UHPLC-Q/TOF-MS was processed with principal component analysis (PCA) and orthogonal partial least squared discriminant analysis (OPLS-DA).

    Simultaneous quantification of eight active compounds in Sinopodophyllum hexandrum by HPLC-DAD
    Aihua Wang, Yue Kong, Mingying Shang, Rongyun You, Guangxue Liu, Feng Xu, Shaoqing Cai
    2015, 24(6):  376-382.  DOI: 10.5246/jcps.2015.06.048
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    Sinopodophylli Fructus is the commonly used traditional Tibetan medicinal herb. In the present study, we established a reversed-phase high performance liquid chromatography method to simultaneously determine three lignans and five flavonoid constituents, namely podophyllotoxin, desoxypodophyllotoxin, 4′-demethyldesoxypodophyllotoxin, 8-prenylkaemferol, quercetin, kaempferol, 8,2'-diprenylquercetin 3-methylether and 8-prenylquercetin, in Sinopodophylli Fructus. The chromatographic separationwas achieved on a C18 analytical column with a gradient mobile phase consisting of acetonitrile and 0.05% phosphoric acid at a flowrate of 1.0 mL/min. UV detection was set at 290 nm and 370 nm, and the column oven was set at 35 °C. This method provided a good reproducibility, and its overall intra- and inter-day precision was less than 3% and 4%, respectively. The recovery of the method was 98.29%101.60%, and a good linearity (R2≥0.9992) was obtained for all the analytes over a relatively wide range of concentration. A total of 17 samples of S. hexandrum (12 fruits, 5 roots and rhizomes) were collected from different areas and then successfully quantified. The results indicated that the contents of eight compounds significantly varied (the sum content rangedfrom 16.90 to 55.68 mg/g), and prenylated flavonoids could be used as marker constituents in the identification and quality control of Sinopodophylli Fructus.

    Preparation of monolithic osmotic tablet of quercetin loaded by solid dispersion
    Haijun Hao, Youzhi Jia, Hongqin Zhang, Ru Han, Xueping Wang, Limei Han, Jianxin Wang
    2015, 24(6):  383-392.  DOI: 10.5246/jcps.2015.06.049
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    The objective of this study was to prepare monolithic osmotic tablet of quercetin for controlled drug release. Quercetin-PVP solid dispersion was prepared to enhance its solubility and dissolution rate. Solid dispersion, suspending agents, osmotic agents and other conventional excipients were used as tablet core composition and cellulose acetate (CA) with plasticizer as release controlling membrane. Different formulation variables, the amounts of PEO (polyethylene oxide), NaCl, plasticizer, and coating weight gain were optimized to gain the optimum formulation. The mechanism of drug release from monolithic osmotic tablet was also discussed. The optimal monolithic osmotic pump tablet could deliver quercetin at the rate of approximate zero-order up to 12 h, and the cumulative release was 90.74%. The developed monolithic osmotic system for quercetin loaded by solid dispersion was found to be a promising approach for controlled release of poorly-water soluble drug candidates.

    Quantification of rhynchophylline in rabbit plasma by UPLC-MS/MS and its application in a pharmacokinetic study
    Lanlan Hu, Jianlin Tang, Shiwen Zhou
    2015, 24(6):  393-399.  DOI: 10.5246/jcps.2015.06.050
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    It was recently revealed thatRhynchophylline (Rhy), an important constituent of Uncaria rhynchophylla, possessed antihypertensive and neuroprotective effects. However, no information about the pharmacokinetics of Rhy in a herbivorous speciessuch as rabbit is available. Allometric scaling is valuable in designing human pharmacokinetic parameters from preclinical species. To investigate the characteristics of Rhy in vivo, a rapid and sensitive ultra performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method was developed and validated for the measurement of Rhy concentrations in rabbit plasma. The method was linear over the concentration range of 0.01–10.24 µg/mL. Intra-day and inter-day precision and accuracy were less than 8.0%. The recoveries were in the range of 94.17%–103.32%. Matrix effects (ME) were minor. After oral administration of Rhy at 20, 40 and 80 mg/kg, the mean elimination half-life (t1/2) for these doses were 1.19, 1.49 and 1.37 h in rabbits, respectively. There was a proportionate increase in the maximum concentration (Cmax) and the area under the blood concentration-time curve (AUC) for three doses. The developed method was suitable for the study on pharmacokinetics of Rhy after oral administration and it may provide a valuable basis for clinical application of such a bioactive compound of herbal medicines.

    Interactions of carrageenan or its degradation product with R15K by affinity capillary electrophoresis
    Zhongjie Li, Li Li, Xiaowei Wang, Junyi Liu, Xiaomei Ling
    2015, 24(6):  400-404.  DOI: 10.5246/jcps.2015.06.051
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    V3 loop of HIV-1 envelop protein gp120 plays a pivotal role in the entry process of HIV-1 into target cells. R15K, the relatively conserved region of V3 loop, can be used in binding studies instead of recombinant gp120 molecule. Polyanionic compounds, such as carrageenan, possess antiviral activity through disrupting gp120-CD4 interaction, and chemical modifications have been performed to improve such activity. In this work, we, for the first time, analyzed the interactions between carrageenan or its degradation and R15K by affinity capillary electrophoresis (ACE). Our results revealed that depolymerized carrageenan rather than carrageenan could bind to R15K. The binding constant of depolymerized carrageenan was (2.94±0.57)×106 mol/L. Our finding indicated that the depolymerized carrageenan could be R15K antagonist, and it might inhibit the infection of HIV-1 through the entry process.

    Risk management of drug products in FDA: the development and implication
    Baomin Wang, Linguang Zhou, Bin Li, Song Yang, Bin Jiang
    2015, 24(6):  405-411.  DOI: 10.5246/jcps.2015.06.052
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    This paper presented detailed information about the timeline of development of drug risk management in FDA. The time process was divided into three stages: the launch of laws and regulations of drug risk management, pre-market approval and post-market safety supervision, adverse drug reaction and risk communication. To address the problems existing in drug risk management in China, suggestions to further and improve the development of drug risk management are proposed.

    The impact of obesity in managing diabetes
    Xiaohui Xie, Fei Wang, Jiayu Cui
    2015, 24(6):  412-418.  DOI: 10.5246/jcps.2015.06.053
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    The epidemic of diabetes has been fueled by a parallel increase in the prevalence of overweight and obesity. Both diabetes and overweight/obesity have become major public health problems causing increased morbidity and mortality and are important risk factors for cardiovascular disease.Cardiovascular disease is the leading cause of death in China. Excess weight has been shown to be associated with increased prevalence of type 2 diabetes, hypertension, dyslipidemia, metabolic syndrome and certain cancers; while weight loss dramatically reduces these obesity-related diseases. Overweight and obesity are important modifiable risk factors for diabetes and cardiovascular disease. There has also been encouraging progress in treatments for obesity. In 2013, the American Medical Association declared obesity a “disease state”requiring a range of medical interventions to advance obesity treatment and prevention. Since 2012, four new drugs have been approved by the U.S. FDA for the treatment of obesity.