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Table of Content

    28 April 2014, Volume 23 Issue 4
    Contents
    Graphical contents list
    Journal of Chinese Pharmaceutical Sciences
    2014, 23(4):  211-214. 
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    Original articles
    Serum stability enhancement of siRNA caused by peptide conjugation at 3'-terminus of sense strand
    Lang Zou, Ye Huang, Xiaofeng Wang, Yuan Ma, Yang Liu, Zhu Guan, Lihe Zhang, Zhenjun Yang
    2014, 23(4):  215-219.  DOI: 10.5246/jcps.2014.04.029
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    RNA interference has been widely used for gene therapy of various infectious diseases and malignant tumors.However, its poor stability in serum has limited further clinic application. Here, we found that stability of siRNA in serumenhanced obviously when 3'-terminus of sense strand (siRNA-pS) was conjugated with peptide, while same conjugation at 3'-terminus of antisense strand brought no such effects. And it was also found that only the peptide residue in siRNA-pS could be cut off by RNase A. All these results indicated that nucleases in serum prefer to invade siRNA duplex through the 3'-end of sense strand.

    Route improvement of 3-substituted-4-(2-methylcyclohexyloxy)-6-phenethylpyridinone
    Xiangyi Liu, Yuanyuan Cao, Yu Zhang, Quanzhi Yang, Xiaowei Wang, Junyi Liu
    2014, 23(4):  220-224.  DOI: 10.5246/jcps.2014.04.030
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    trans-3-Isopropyl-4-(2-methylcyclohexyloxy)-6-phenethylpyridin-2(1H)-one, as reverse transcriptase (NNRTIs), exhibited significant potent activity not only against wild-type HIV-1 strains but also on mutant strains. For furthering study this compound, the original synthetic route should be shorten to improve the total yield. In this report, we designed an efficient synthetic strategy to obtain the target compound with higher yield.

    Simultaneous quantification of eighteen constituents in traditional Chinese medicine XiaoShuanTongLuo by UPLC-MS/MS  
    Yan Zhao, Min Liu, Zhao Yang, Shaohua Wang, Yang Li, Guanhua Du
    2014, 23(4):  225-232.  DOI: 10.5246/jcps.2014.04.031
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    XiaoShuanTongLuo (XSTL) is an important multi-herbal formula widely used as a traditional Chinese medicine (TCM). Inthis paper, an ultra-performance liquid chromatography-electrospray ionization tandem mass spectrometric method (UPLC-ESI-MS/MS) was developed for the simultaneous identification and quantification of18chemical constituents in the extract of XSTL.The analysis was performed in multiple-reaction monitoring (MRM) mode using positive and negative electrospray ionization (ESI). A BEH C18 (2.1 mm×100 mm, 1.7 μm) column with a gradient mobile phaseof methanol–0.1% aqueous formic acid solution at a flow rate of 0.2 mL/min was used for separation. The standard curves of most components showed good linearity over the concentration range of 0.0010.5 μg/mL withr = 0.98960.9996. The relative standard deviations (RSD) of intra-day and inter-day precision were all lower than 15% at low, middle, and high concentration levels. The RSD of stability analysis in 24 h were also lower than 15%. The validated method was employed to quantify 18 active components simultaneously in four different commercial brands of XSTL products in various dosage forms. The developed method was rapid, accurate, sensitive, and reproducible for the quality control of XSTL.
    Application of UHPLC-MS/MS method in determining the content of multi-ingredient in hospital preparations
    Zhiyan Lin, Rongfu Yang, Yuenian Tang, Huaiping Tian, Jian Zhang
    2014, 23(4):  233-240.  DOI: 10.5246/jcps.2014.04.032
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    In the present study, we established an ultra-high pressure liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS) method to simultaneously determine 11 compounds in two hospital preparations(Shegan mixture and Gandi capsules), including ephedrine, caffeic acid, ferulic acid, rutin, scutellarin, belamcandin, baicalin, baicalein, astragaloside IV, irisflorentin and wogonin. The chromatographic separation was conducted on ZORBAX SB-C18 (2.1 mm×50 mm, 1.8 μm). Eleven analytes and IS were detected using ESI and MRM combined with positive and negative scanning switch. Caffeic acid, ferulic acid, scutellarin and belamcandin were detected using negative ion mode detection, whereas ephedrine, rutin, baicalin, baicalein, astragaloside IV, irisflorentin and wogonin were detected using positive ion mode detection. The quantification limits of ephedrine, caffeic acid, scutellarin, belamcandin, baicalin, baicalein, irisflorentin and wogonin were 4.90×10-3 ng/mL, 7.80 ng/mL, 6.8 ng/mL, 5.3×10-2 ng/mL, 4.20×10-3 ng/mL, 4.6×10-2 ng/mL, 1.44×10-4 ng/mL, 4.85 ng/mL, 0.23 ng/mL, 3.18×10-4 ng/mL and 2.95×10-4 ng/mL, respectively. The detection limits of these components were 2.90×10-4 ng/mL, 0.77 ng/mL, 2.0 ng/mL, 0.016 ng/mL, 1.3×10-3 ng/mL, 3.33×10-4 ng/mL, 4.32×10-5 ng/mL, 1.46 ng/mL, 0.07 ng/mL, 9.5×10-5 ng/mL and 8.84×10-5 ng/mL, respectively. All calibration curves showed good linearity (R2>0.99) within the test range. The RSD values of intra-day and inter-day precision were less than 5%, and the average recovery rates of the 11 components ranged from 80% to 120%. In conclusion, our newly developed method was simple, rapid, sensitive and accurate. It could be used to determineephedrine, caffeic acid, ferulic acid, rutin, scutellarin, belamcandin, baicalin, baicalein, astragaloside IV, irisflorentin and wogonin in Shegan mixture and Gandi capsules, which was helpful for the quality control of drugs.
    Biotransformation of malabaricone C by rat hepatic microsomes and cytotoxic activities against gastric cancer cells in vitro
    Ni Wu, Wei Xu, Youbo Zhang, Xiuwei Yang
    2014, 23(4):  241-245.  DOI: 10.5246/jcps.2014.04.033
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    Malabaricone C (1), isolated from the seeds of Myristica fragrans Houtt., belongs to a kind of diarylnonanoid compounds that are only found in Myristicaceae till now. In this study, biotransformation of 1 was investigated using rat hepatic microsomes for the first time and the main biotransformation product waselucidated as malabaricone B (2) according to the spectroscopic data. Further evaluation on human gastric cancer cell lines showed that the cytotoxic effects of malabaricone C and its metabolite malabaricone B were comparable to those of vinorelbine, with the values of IC50 of (42.62±3.10) and (19.80±1.70) μg/mL on NCI-N87, and (22.94±1.33) and (19.60±2.21) μg/mL on MGC803, respectively. Statistical analysis revealed that malabaricone B had significantly stronger cytotoxicity than the parent compound(P<0.01 on NCI-N87 and P<0.05 on MGC803), which may indicate a bioactivation of malabaricone C by hepatic microsomes. These results suggest that malabaricone C has a simple biotransformation pathway by hepatic microsomes and provide valuable information for further investigation on both the parent compound and its biotransformation product as anti-gastric cancer agents or lead compounds.
    A new triterpenoid saponin from Silene rubicunda Franch.
    Qiong Wu, Guangzhong Tu, Hongzheng Fu
    2014, 23(4):  246-250.  DOI: 10.5246/jcps.2014.04.034
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    A new triterpenoid saponin (compound 1), together with a known one (compound 2) was isolated from the roots of Silene rubicunda Franch. The isolation and purification were performed by a series of chromatographic techniques including silica gel, sephadex LH-20, and reversed-phase HPLC. Their structures were elucidated on the basis of combination of mass spectrometry and 1D, 2D NMR spectroscopy, and the new compound was identified as 3-O-{β-D-galactopyranosyl-(1→2)-[β-D-xylopyranosyl-(1→3)]-β-D-glucuronopyrannosyl}-28-O-{β-D-xylopyranosyl-(1→3)-β-D-xylopyranosyl-(1→4)-α-L-rhamnopyranosyl-(l→2)-[β-D-quinovopyranosyl-(1→4)]-β-D-fucopyranosyl} quillaic acid.
    Chemical constituents from Xiaoaiping injection
    Yirun Wang, Mingbo Zhao, Li Tang, Pengfei Tu
    2014, 23(4):  251-255.  DOI: 10.5246/jcps.2014.04.035
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    Xiaoaiping injection is a single-prescription of Marsdenia tenacissima. One newcompound, tenacigenoside L(1), along with ten known compounds were isolated from the CHCl3-soluble fraction of Xiaoaiping injection extractby silica gel, ODS, Sephadex LH-20 and semi-preparative HPLC chromatography. The new compound was characterized as 3-O-β-D-oleandropyranosyl-17β-tenacigenin B. The ten known compounds were identified as tenacigenin B (2), 17β-tenacigenin B (3), marsdenoside F (4), tenacissoside G (5),tenacissoside I(6), tenacissoside H (7), marsdenoside D(8), tenacigenin A (9), marsdenoside I (10), and tenacigenin C (11). The structures of 11 compounds were elucidated on the basis of extensive analyses of spectroscopic data including MS, 1D NMR and 2D NMR, and comparison of their spectroscopic data with those reported in the literatures.
    Sphingomyelin synthase activity measurement by the fluorescent product in cell culture medium or animal plasma
    Tingbo Ding, Jibin Dong, Bin Lou, Xian-Cheng Jiang
    2014, 23(4):  256-261.  DOI: 10.5246/jcps.2014.04.036
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    Sphingolipids, a new class of lipid mediators, are involved in a variety of important physiological and pathological processes. Sphingomyelin synthase (SMS) is an enzyme to convert the ceramide (Cer.) and phosphatidylcholine into sphingomyelin (SM) and diacylglycerol, which plays a key role in sphingolipid biosynthesis. Two SMS isoforms, SMS1 and SMS2, have been identified with different subcellular localizations and expression level in tissues. Previous studies have shown that SMS may serve as a potential therapeutic target for the treatment of various diseases, such as cardiovascular and metabolic diseases. Thus, there is an urgent need for a rapid and sensitive method for SMS activity analysis. In our study, we developed a novel method for SMS activity by monitoring the appearance of the product, NBD-SM, in the tissue culture medium or bloodand applied this method in cells and mice. In Huh7 cells, the interassay coefficient of variation of the SMS activity assay was (3.60±0.07)%. In wild type (WT) mice, we observed accumulation of NBD-SM in blood in a time dependent fashion. In SMS2 KO mice, NBD-SM in plasma collected at 5- (0%, P<0.01), 30- (16%, P<0.01), and 60 min (21%, P<0.01) after injection of fluorescence liposome solution was significantly decreased compared with WT mice. However, in SMS1 KO mice, NBD-SM in plasma collected 5- and 30 min is similar to that in WT mice. Our results suggest that this method could be used for SMS activity measurement in vitro and in vivo.
    Antihyperglycemic, insulin-sensitizing and antioxidant activities of the active fractions from Anoectochilus chapaensis
    Jinyan Cai, Lin Zhao, En Zhu, Chengxi Wang
    2014, 23(4):  262-267.  DOI: 10.5246/jcps.2014.04.037
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    Anoectochilus chapaensisGagnep. (Orchidaceae), an indigenous and valuable Chinese folk medicine, has been widely used in China to treat diabetes. However, few reports are available about its constituents and activity. The present experiment was conducted to investigate the active fractions from A. chapaensis in diabetic rat model induced by high-fat diet plus streptozotocin. The total EtOH extract from the whole herbs of A. chapaensis,half of which was partitioned in sequence with petrol ether (PE), ethyl acetate (EtOAc), n-BuOH and H2O, thus yielding four fractions, all of them were orally administered with an identical dose amount to 4 g/kg dried crude herbs once a day for consecutive two weeks to further investigate the antihyperglycemic activity. The EtOAc fraction caused a significant fall in the non-fasting blood glucose level of diabetic rats from (402.66±82.26) to (226.26±62.10) mg/dl, which may be attributed to ameliorating insulin resistance, modulating the activity of enzymatic antioxidants, reducing the content of NO, etc. Much more intact β cells in the islets of Langerhans in EtOAc fraction-treated groups than the negative control were observed, which greatly supported the morphological and functional elucidation. The OGTT evidencedthat EtOAc fraction could promote the endurance capacity of acute glucose increase in diabetic rats. The EtOAc fraction ofA. chapaensis contains some hypoglycemic and antioxidant principles with the potential to be developed further for the treatment of diabetes specifically associated with an insulin resistance state.
    Editor profile
    Demin Zhou, Xinshan Ye
    Journal of Chinese Pharmaceutical Sciences
    2014, 23(4):  268-270. 
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    Other
    Information from US FDA
    http://www.fda.com
    2014, 23(4):  271-274. 
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