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Table of Content

    15 September 2013, Volume 22 Issue 5
    Contents

    Graphical contents list

    Journal of Chinese Pharmaceutical Sciences

    2013, 22(5):  381-384. 
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    Review
    Phytosomes: an effective approach to enhance the oral bioavailability of active constituents extracted from plants
    Haijun Hao*, Youzhi Jia, Ru Han
    2013, 22(5):  385-392.  DOI: 10.5246/jcps.2013.05.056
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    Many active constituents from herbal plants have well-established pharmacological effects in vitro. But they demonstrate less or no activities in vivo due to various problems of themselves, which severely restricts their clinical applications. After forming phytosomes with phospholipids in aprotic solvent, the active constituents exhibit different physicochemical properties from the free form. In particular, the bioavailability of the active constituent-phytosomes is enhanced greatly due to the improved capacity to cross the biomembrane and reach circulation. Therefore, increasing attention has been attracted to the use of phytosomes in recent years. Based on the published reports, we reviewed the recent progress in the research of phytosomes including preparation, characterization, structure verification and clinical applications.
    Original articles
    Pharmacophore identification and validation for human nAChR α7 agonists
    Bo Yu, Hongwei Jin, Liangren Zhang*, Chao Wang*
    2013, 22(5):  393-402.  DOI: 10.5246/jcps.2013.05.057
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    Human nAChR α7 is the potential target for schizophrenia cognitive disorders, and it is meaningful to develop selective human nAChR α7 agonists for the clinical treatment of the disease. Because the crystal structure of α7 receptor has not been resolved, ligand-based drug design strategy was took in this work. A 3D QSAR pharmacophore model was built by HypoGen method, and its quality was evaluated by cost function. Furthermore, the pharmacophore model was validated with activity prediction of test set and was cross-validated based on Fisher’s Randomization Method. By Enrichment Factor and AU-ROC analysis, the final pharmacophore, which is consisted of one HBA, two Hydrophobic and one PosIonizable, was selected and it fitted well with the docking result of α7 homology model and the ligand. The pharmacophore is expected for the following virtual screening and lead optimization of human nAChR α7 agonists, which is important for the development and discovery of novel antipsychotics.
    Combination of vitamin C and zinc gluconate prevented vanadium-induced tight junction leakage of MDCK cell monolayer
    Zhihan Xu, Xinyi Wang, Ruyue Xiao, Xiaoda Yang*
    2013, 22(5):  403-408.  DOI: 10.5246/jcps.2013.05.058
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    The tight junction disorder plays an important role in the pathological process of many chronic diseases, and is becoming a major concern for the clinical application of metal drugs, i.e. anti-diabetic vanadium compounds. The development of novel tight junction protecting agents has thus been a major research focus. Since oxidative stress is the primary cause for vanadium toxicity, the present work tested the protective effects of zinc gluconate (Zn2+) alone and when combined with vitamin C (VC) on the vanadium compound (VO(acac))-mediated paracellular leakage of MDCK cells. The experimental results showed that VO(acac) treatment significantly increased the paracellular permeability of MDCK monolayer. Zn2+ alone showed no protective effects and VC ameliorated tight junction leakage of MDCK cells when given in the basal chamber. Interestingly, unilateral treatment with the combination of Zn2+ and VC effectively prevented the increase of paracellular permeability. In addition, the combination of zinc and VC down-regulated the levels of reactive oxygen species in both the control and VO(acac)2-treated MDCK cells and caused the elevation of intracellular Ca2+; both effects were beneficial for the maintenance of integrity of intercellular tight junction. Our results provided a simple but very effective method of preventing the metal toxicity for clinical application of anti-diabetic vanadium compounds.
    Determination of fexofenadine in human plasma by LC-MS/MS and its application in pharmacokinetic study
    Yenan Chen, Hsinyi Chou, Wenkuei Chang, Kuangyang Hsu*
    2013, 22(5):  409-414.  DOI: 10.5246/jcps.2013.05.059
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    This study presented a simple, rapid, and sensitive liquid chromatography analytical method employing tandem mass spectrometry (LC-MS/MS) to determine fexofenadine in human plasma. After the de-proteination procedure with acetonitrile, chromatographic separation of fexofenadine was performed using a reversed-phase Eclipse XDB-C8 column with a mobile phase consisted of 1 mmol/L ammonium acetate buffer solution containing 0.2% formic acid-methanol (45:55, v/v). Fexofenadine was quantified using tandem mass detection in the electrospray ionization (ESI) positive ion mode. The flow rate of the mobile phase was 1 mL/min, and the retention times of fexofenadine and the internal standard (IS, losartan) were 1.76 min and 2.65 min, respectively. The calibration curve was linear over the plasma concentration range of 1-1000 ng/mL. The relative standard deviations of intra- and inter-batches were less than 10.4% and 15.4%, respectively. The LC-MS/MS method reported in this study showed higher sensitivity for the quantification of fexofenadine in human plasma than that shown by previously described analytical methods. Lastly, the method was successfully applied to the pharmacokinetic of fexofenadine in healthy Taiwan volunteers.
    Development of a novel quality standard of Indigoplant
    Shanshan Xu, Qing Li, Xinli Wang, Lu Li, Kaishun Bi*
    2013, 22(5):  415-419.  DOI: 10.5246/jcps.2013.05.060
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    Traditional Chinese medicine (TCM) has been widely used in China for thousands of years, and has received more and more recognition worldwide. Indigoplant (Folium Polygoni Tinctorii), a TCM, has been used in various diseases. In our study, we established a quality standard of Indigoplant according to the European Pharmacopoeia, and this standard has passed the early audit stages of the European Pharmacopoeia Commission. The Indigoplant samples were identified with high performance thin layer chromatography (HPTLC), qualified with RP-HPLC quantitation, and analyzed with a series of quality tests. An accurate, reliable and robust HPLC method with gradient elution for quantitation was developed and validated with a one-variable-at-a-time (OVAT) robustness approach. Several tests, including the loss on drying, total ash and ash insoluble in hydrochloric acid of Indigoplant, were performed for quality analysis. Furthermore, six batches of the Indigoplant samples were appraised with this quality standard. In conclusion, the established quality standard was more internationally normative and applicable for the quality control of Indigoplant in practical application.
    Quantification and structural identification of related phenolic compounds in the raw medicinal material honokiol
    Baobao Zhang, Hong Wang, Shizhong Chen*
    2013, 22(5):  420-426.  DOI: 10.5246/jcps.2013.05.061
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    High-performance liquid chromatography (HPLC) was used to quantify magnaldehyde B (6), magnaldehyde E (4) and 8',9'-dihydroxyhonokiol (7) simultaneously in the raw Chinese medicinal material honokiol. The separation was performed on a reversed-phase C18 column by using a gradient elution with mobile phases of water (A) and methanol (B). The mobile phase gradient was run from 40% B to 56.5% B in 55 min, 55-67 min from 56.5% to 51.5%, 67-80 min from 51.5% to 70%, 80-170 min at 70%. The elution was carried out at a flow rate of 1.0 mL/min at the column temperature of 35 оC with the UV detection wavelength at 256 nm. Magnaldehyde B, magnaldehyde E and 8',9'-dihydroxyhonokiol showed good linear relationships with peak areas in the range of 0.00864 to 0.07776 mg/mL, 0.01488 to 0.13392 mg/mL and 0.01568 to 0.10976 mg/mL, respectively. Their corresponding average recoveries were 100.30%, 99.63% and 98.29%, respectively. Our results showed that the established method is simple, rapid, and accurate with good reproducibility for evaluating the quality of raw Chinese medicinal material honokiol. Moreover, another five phenolic compounds, namely erythro-7-O-methylhonokitriol (1), threo-7-O-methylhonokitriol (2), 7-O-ethylhonokitriol (3), magnaldehyde C (5), honokiol (8), together with compounds 4, 6 and 7, were isolated and purified from the remaining substance in the process of preparing the raw material honokiol by silica gel column and semi-preparative HPLC. Their structures were characterized by 1D and 2D NMR spectroscopy. Among them, compounds 1 and 2 were reported to have common planar structures and their relative configurations were identified for the first time. Compounds 3 and 7 were not only obtained from the raw medicinal material for the first time but also novel compounds.
    Chemical constituents from Qianliang tea
    Qian Liu, Jun Li, Xingyun Chai, Yong Jiang, Pengfei Tu*
    2013, 22(5):  427-430.  DOI: 10.5246/jcps.2013.05.062
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    Ten compounds were isolated from Qianliang tea, a kind of dark tea fully fermented from the leaves of Camellia sinensis (L.) O. Kuntze var. sinensis, and identified as N-(2-hydroxyphenyl)-2-pyrrolidinone (1), p-hydroxyacetophenone (2), salicifoliol (3), (-)-3-hydroxy-β-ionone (4), p-hydroxy ethyl cinnamate (5), ethyl 4-(sulfooxy)benzoate (6), (+)-matairesinol (7), (-)-pinoresinol (8), (+)-lirioresinol-A (9), and caffeine (10), among which compound 1 was isolated as a new natural product, and compound 6 was isolated from Theaceae family for the first time. Compounds 3, 4, 5, 7, 8, and 9 were isolated from this species for the first time.
    Chemical constituents from the leaves of Premna microphylla Turcz
    Zhengxi Hu, Yongbo Xue, Guangmin Yao, Zengwei Luo, Yanyan Wang*, Yonghui Zhang*
    2013, 22(5):  431-434.  DOI: 10.5246/jcps.2013.05.063
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    Phytochemical investigation of the leaves of Premna microphylla Turcz led to the isolation of 13 known compounds. Based on spectroscopic and chemical evidences, their structures were identified as diosmetin (1), blumenol A (2), (3S,5R,6S,7E,9R)-5,6-epoxy-3,9-dihydroxy-7-megastigmene (3), 3β-hydroxy-5α,6α-epoxy-7-megastigmen-9-one (4), ixerol B (5), (-)-dehydrovomifoliol (6), 3S,5R-dihydroxy-6S,7-megastigmadien-9-one (7), loliotide (8), (+)-dehydrololiolide (9), (+)-medioresinol (10), 4-oxopinoresinol (11), tormentic acid (12), and indole-3-carboxylic acid (13). Compounds 213 described above were isolated from this genus for the first time.
    The protective effects of thalidomide derivative ZSN-12 on acute lung injury
    Xiaoli Gao, Xiangbao Meng, Yimin Jiang, Zhongjun Li*, Jia Ye*
    2013, 22(5):  435-440.  DOI: 10.5246/jcps.2013.05.064
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    The aim of this study was to evaluate the protective effect of thalidomide derivative ZSN-12 on acute lung injury induced by oleic acid in mice, and to investigate the possible mechanisms. The results showed that ZSN-12 (200 mg/kg) markedly improved the pathological changes of acute lung injury. The proportion of polymorphonuclear neutrophils (PMN) was reduced by 48% (P<0.01) and the content of nitric oxide (NO) in bronchoalveolar lavage fluid (BALF) was decreased by 33% (P<0.05). ZSN-12 produced significant anti-inflammatory effects in the models of xylene induced ear edema and carrageenan induced paw edema, in which ZSN-12 inhibited ear edema and paw swelling in a dose-dependent manner. The inhibition rates by ZSN-12 dosed at 200, 100, 50 mg/kg were 62%, 43%, and 30% in ear edema, respectively and 60%, 47%, and 33% in paw edema, respectively, at 3 h. Meanwhile, ZSN-12 (10, 5, 1 μmol/L) significantly restrained the ConA-induced T lymphocyte proliferation, with the inhibition rates of 33%, 30% and 22%, respectively (P<0.01). In conclusion, the present study showed that administration of thalidomide derivative ZSN-12 exerted significant protective effect in acute lung injury induced by oleic acid in mice, which may be related to its anti-inflammation effect. ZSN-12 inhibited the effusion of PMN, reduced the release of NO, and suppressed the proliferation of T lymphocyte.
    Hematological and pathological toxicity of anti-HER2/neu peptide mimetic modified paclitaxel bovine serum albumin nanoparticles
    Zhanzhang Wang, Zhenzhen Yang, Xianrong Qi*
    2013, 22(5):  441-448.  DOI: 10.5246/jcps.2013.05.065
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    Nanoparticles have been widely applied in diagnosis and therapy due to the high loading of insoluble drug, increased target accumulation and interaction with biological tissues. Recently, severe side effects of nanoparticles have been reported, but the underlying mechanism remains largely unknown. In our study, we aim to understand the safety of paclitaxel (PTX) loaded bovine albumin nanoparticles (BNPs) and active targeted PTX loaded BNPs to normal vital organ or tissue in vivo. The anti-human epidermal growth factor receptor 2 (HER2/neu) peptide mimetic (AHNP) was covalent bound to surface of BNPs (AHNP-BNPs) to exert selected delivery to HER2+ cells. In HER2+ tumor xenographs, saline (control), PTX traditional formula (medium of Cremophor EL-ethanol), BNPs, and AHNP-BNPs were administrated to evaluate the toxicity. There is no severe neutropenia or anemia with treatment of BNPs and AHNP-BNPs compared with traditional PTX injection. We also evaluated their damage on normal organs, including liver, kidney, spleen, lung and heart to fully estimate the safety of AHNP-BNPs and BNPs delivery systems. We observed similar toxicity in liver and lung in mice treated with BNPs or PTX injection, but decreased liver damage in mice treated with AHNP-BNPs. Further studies are required to confirm our conclusion.
    Design and evaluation of aceclofenac ocular inserts with special reference to cataracts and conjunctivitis
    Vivek Dave*, Sachdev Yadav, Sarvesh Paliwal, Swapnil Sharma, Dhirendra Kumar
    2013, 22(5):  449-455.  DOI: 10.5246/jcps.2013.05.066
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    The eyes present unique opportunities and challenges when it comes to the delivery of pharmaceuticals. While absorption by this route is bungling, there are a few side effects with conventional dosage forms. Ocular inserts were prepared with prolonged release of drug and minimum swelling within cul-de-sac using aceclofenac. The work focused on treatment of conjunctivitis and cataracts by formulating ocular inserts of different polymeric combination of aceclofenac using hydroxypropyl methyl cellulose (HPMC, 3% to 5%), chitosan (3% to 5%), poly vinyle alcohol (PVA, 3% to 5%), methyl cellulose (MC, 3% to 5%) as drug reservoir and ethyl cellulose (EC) polymer as rate controlling membrane by solvent casting technique with the objective of increasing contact time, achieving controlled release and greater therapeutic efficiency. The prepared ocular insert were then evaluated for physical appearances tensile strength, elongation at break (%), weight variation, uniformity of thickness, moisture absorption (%), pH, folding endurance, Fourier Transform Infrared spectroscopy, differential scanning calorimetry. Physicochemical characterization and in vitro transcorneal permeation studies reveals that, the prepared ocular insert formulations F2 and F8 containing HPMC and PVA had released their drug content, 98.54% and 96.24%, respectively, over an extended period of 24 h. Hence these formulations were selected as best optimized formulations. It can be concluded that hydroxy propyl methyl cellulose is a good film forming hydrophilic polymer which shows potential agent for ocular drug delivery system. Incorporation of polyethylene glycol enhances the permeability of aceclofenac ocular insert and has perfect zero order release, proving a promising controlled release delivery system.
    Economic evaluation of soft silicon foam dressings versus sterile gauze for the treatment of pressure ulcers in China
    Sheng Han, Kuan Wang, Run Pu, Luwen Shi*
    2013, 22(5):  456-460.  DOI: 10.5246/jcps.2013.05.067
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    The aim of this study was to evaluate the cost and effectiveness of soft silicone foam dressings (SSFD, Mepilex) on the treatment of pressure ulcers. We searched electronic databases and retrieved articles to make a systematic evaluation, and then make a cost-effectiveness analysis by decision tree model combined with data from clinical treatments. The result shows that compared with the common sterile gauze, SSFD possesses an apparent advantage. The effective ratio is 96.3% versus 77.3%, although the cost of SSFD is much higher than that of sterile gauze, Mepilex appears to be more cost-effectiveness for preventive use.
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