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Table of Content

    10 July 2013, Volume 22 Issue 4
    Contents

    Graphical contents list

    Journal of Chinese Pharmaceutical Sciences

    2013, 22(4):  289-292. 
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    Reviews
    Development of new solid phase extraction techniques in the last ten years
    Huixia Fan, Zhipeng Deng, Hao Zhong, Qingqiang Yao*
    2013, 22(4):  293-302.  DOI: 10.5246/jcps.2013.04.043
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    Solid phase extraction (SPE) is a widely used sample pretreatment method for separation, purification and enrichment, which has been established due to its significant advantages of time-saving, low consumption of solvent, high enrichment factor, high accuracy, etc. In recent years, a variety of new SPE methods such as molecularly imprinted solid phase extraction (MISPE), magnetic solid phase extraction (MSPE), solid phase micro-extraction (SPME), etc., which are superior to the conventional SPE, have been developed and been widely applied to food, drugs, and environmental monitoring. In this paper, the basic principles and methods of SPE and its new applications in different areas are reviewed.
    Tailoring active compounds across biological membranes by cubosomal technology: an updated review
    Vinod K.R.*, Sravya K., Sandhya S., David Banji, Anbazhagan S., Prameela Rani A.
    2013, 22(4):  303-313.  DOI: 10.5246/jcps.2013.04.044
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    It is challenging for many drugs to be transported across various biological membranes. Furthermore, development of many drugs gets thwarted owing to their hydrophilic nature. The bioavailability of such drugs, which is the function of their ability to cross the membrane, tends to be low and exhibit high intra and inter subject variability. At present, formulation scientists are pursuing many projects for transdermal, nasal, target delivery of many active compounds, and it is prudent to explore alternative possibilities. Cubosomes offer transportation and tailoring of active compounds intended for both systemic and dermal delivery. Cubosomes are dispersed, self-assembled nanoparticles of bicontinuous cubic liquid crystalline phase formed from lipid and surfactant systems. Monoolein, poloxamer 407 and polyvinyl alcohol are the mostly used ingredients in the formulation of cubosomes. The adjustment in lipid composition can control the internal and structural changes of cubosomes. Based on the nodal surfaces, three structures of cubosomes proposed are Pn3m, Ia3d and Im3m. Top-down and bottom-up techniques are widely considered in the formulation process of extreme viscous bulk phase and aggregate from a precursor respectively. This article gives a bird’s eye view about the engineering, characterization and evaluation of cubosomes, covering researches and applications of cubosomes done till date.
    Original articles
    Synthesis and the anti-HIV activity of novel dinucleotides containing
    L-isonucleosides
    Meng Wang, Lei Xing, Shifang Lu, Zhu Guan*, Zhenjun Yang, Lihe Zhang
    2013, 22(4):  314-318.  DOI: 10.5246/jcps.2013.04.045
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    Three dinucleotides containing L-isonucleosides at 5'-end were synthesized by an elegant phosphoramidite one-pot method. Their binding modes with HIV integrase were simulated and their anti-HIV activities in pseudotyped virus system were examined.
    Identification of major parent compounds and metabolites in bile, plasma and urine of rats after oral administration of Radix Scutellariae extract by UFLC-IT-TOF/MS
    Zhengwei Chen, Ling Tong, Shuming Li, Dongxiang Li, Xiaolin Liu, Li Ding*, Yonghong Zhu, Shuiping Zhou, He Sun
    2013, 22(4):  319-328.  DOI: 10.5246/jcps.2013.04.046
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    Flavonoids are the main bioactive components of Radix Scutellariae, a well-known traditional Chinese medicine. After oral administration of Radix Scutellariae extract (RSE), the bile, plasma and urine of rats were analyzed to identify the absorbed parent components and metabolites by ultra-fast liquid chromatography coupled with ion trap time-of-flight mass spectrometry (UFLC-IT-TOF/MS). A total of 36 different flavonoids, including 13 new metabolites, were identified or tentatively characterized in bile, plasma and urine of rats based on their fragmentation patterns. Among them, 16 flavonoids were identified in RSE in vitro, 25 flavonoids in rat bile, 15 flavonoids in rat plasma, and 14 flavonoids in rat urine. The results indicated that glucuronidation, sulfation and methylation were the major metabolic pathways of flavonoids. It is the first time that the metabolism of RSE was studied comprehensively.
    Biotransformation of naringin by human intestinal flora
    Li Ran, Shuai Wu, Wei Xu, Youbo Zhang, Xiuwei Yang*
    2013, 22(4):  329-333.  DOI: 10.5246/jcps.2013.04.047
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    Naringin (1), the highest-content flavanone glycoside in sour oranges, was incubated with human intestinal flora, and four biotransformation products (2-5) were obtained from the incubated mixture by chromatographic methods. The chemical structures of the four products were elucidated as naringin-6"-acetate (2), naringenin (3), phloretic acid (4), and phloroglucinol (5) on the basis of their spectroscopic data. Naringin-6"-acetate was specifically formed by acetylation at C6-OH of glucosyl group of 1. The result obtained in the present research could account for the lower bioavailability of 1 after oral administration, suggesting that some biological properties of 1 in vivo may be mediated by its intestinal flora converted product 3. The biotransformation of 1 by intestinal flora leading to their systemic absorption deserves further attention and may provide valuable insights into pre-systemic drug metabolism, delivery or toxicity.
    Qualitative and quantitative analysis of four different polarity fractions
    from Huang-Lian-Jie-Du-Decoction by HPLC-DAD-ESI-MS/MS and their related neuroprotective effects
    Yang Yang, Haiyu Zhao, Hongjie Wang, Jianfang Song, Jian Yang, Nan Si, Baolin Bian*
    2013, 22(4):  334-341.  DOI: 10.5246/jcps.2013.04.048
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    Huang-Lian-Jie-Du-Decoction (HLJDD) has been widely used for the treatment of Alzheimer’s disease (AD) in clinic. However, the relationship between its chemical profile and neuroprotective bioactivity was not clearly clarified yet. In present study, the water extract of HLJDD and subsequent three polarity fractions divided by different reagents were investigated. A total of 17 chromatographic peaks were confirmed by comparison with standards and their UV, MS spectra. Among them, 11 major compounds were determined by HPLC-DAD method with good linear regression relationship (r2, 0.9994-0.9999), precisions (inter-day precision RSD, 0.79%-1.07%; intra-day precision RSD, 1.59%-2.10%), repeatability (RSD, 1.66%-3.67%), stability (RSD, 1.26%-4.77%) and recovery (95.24%-105.41%, RSD, 0.29%-2.69%). Furthermore, PC12 cells and primary neurons cells were used for the neuroprotective effective assessment of aforementioned four samples from HLJDD. The total aqueous extract and n-butanol extract of HLJDD presented more significant effects than the other two parts. According to their quality and quantity determination results, iridoids and alkaloids have a positive correlation with the neuroprotective effectiveness of HLJDD.
    In vivo antioxidant activity and its protective effects of green tea extract
    on acute myocardial infarction
    Rinkiko Suguro, Bo Wei, Ying Wang, Renqiang Li, Sheng Xiong*
    2013, 22(4):  342-347.  DOI: 10.5246/jcps.2013.04.049
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    The antioxidant activity and its protective effects of Green Tea Extract (GTE) from a Chinese green tea, Hangzhou Longjing, on acute myocardial infarction (AMI) were investigated in rats. Blood, liver and heart were collected to perform DNA damage test, hepatic antioxidant test, gene expression as well as capillary distribution study. A well-known angiotensin II type 1 receptor antagonist, Losartan was used as control. It was found there were significant reductions in certain DNA damage products' levels in GTE and Losartan treated groups compared to saline-treated group. In addition, significant increases in antioxidant enzyme activities and antioxidant gene expressions were observed in GTE and Losartan treated groups. Morphological study also demonstrated the cardioprotective effects of GTE on AMI. In conclusion, GTE has potent and similar cardioprotective effect as Losartan that may due to its ability to scavenge free radicals.
    Antitumor activity and biodistribution of DHA-NLC formulation in sarcoma 180-bearing mice
    Xiaoyun Zhang*, Hua Qiao, Peng Zhao, Jingman Ni, Yanbin Shi
    2013, 22(4):  348-354.  DOI: 10.5246/jcps.2013.04.050
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    Lipid nanoparticles have become attractive for its prominent properties recent years. In this paper, in vivo anti-tumor efficacy of nanostructured lipid carrier of dihydroartemisinin (DHA-NLC) were evaluated in sarcoma 180-bearing mice model through intraperitoneal (i.p.) administration. In vivo biodistribution was also investigated in Kunming mice bearing S180. Results demonstrated that the intraperitoneally injected DHA-NLC could significantly inhibit tumor growth at the dose levels of 20, 40 and 80 mg/kg, and their inhibition rates were 71.24%, 79.20% and 85.74%, respectively. The biodistribution of DHA after intraperitoneal injection of DHA-NLC in S180-bearing mice is remarkably different from the DHA solution. Therefore, DHA encapsulated in NLC does demonstrate superior anticancer effect to DHA suspension on S180-bearing mice at the same dose and displayed a dose-dependent antitumor efficacy.
    Methoxyl methyl ether isoamylene quercetin, a quercetin derivative, protects rat aorta endothelial cells against oxidation and apoptosis
    Xiumei Liu, Xiaoyan Liu, Yinye Wang*
    2013, 22(4):  355-360.  DOI: 10.5246/jcps.2013.04.051
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    Methoxyl methyl ether isoamylene quercetin (MIAQ) is one of the newly synthesized quercetin derivatives. The present study investigated the effect of MIAQ on rat aorta endothelial cells (RAECs) injured by hydrogen peroxide (H2O2), as well as the potential mechanisms. We observed that MIAQ at 2.5-10 μmol/L significantly enhanced the viability of injured RAECs, and the effect was more potent than quercetin and α-tocopherol. However, MIAQ at the same concentration failed to show anti-oxidant activity in a cell-free system. In H2O2-injured endothelial cells treated with MIAQ (5-10 μmol/L), the level of nitric oxide (NO) and malondialdehyde was decreased, and the activities of superoxide dismutase and glutathione peroxidase was enhanced. In addition, RAECs treated with MIAQ (2.5-10 μmol/L) exhibited significant inhibiting apoptosis. In conclusion, MIAQ had protective effect on RAECs, possibly through increasing NO production and antioxidases activities, as well as inhibiting apoptosis. These findings suggest that MIAQ is possibly beneficial in the prevention of atherosclerosis and other diseases related to endothelial injury.
    A high performance liquid chromatography method for the quantitative
    determination of ribavirin in human plasma and its application in a pharmacokinetics study
    Hua Zhang, Guiling Wang, Kexin Li, Xuan Zhang*, Qiang Zhang
    2013, 22(4):  361-364.  DOI: 10.5246/jcps.2013.04.052
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    The clinical pharmacokinetics of ribavirin after a single oral dose of 600 mg ribavirin tablets in healthy Chinese volunteers was studied. A rapid and simple high performance liquid chromatography (HPLC) method was developed to determine the ribavirin concentration in human plasma. C18 column was used for separation with a column temperature of 25 °C, the mobile phase was ultrapure water adjusted to pH 3 with acetic acid at the flow rate of 1 mL/min, and the detection wavelength was set at 207 nm. The linear range of the standard curves was 50.4-2016.0 ng/mL and the lower limit of quantification (LLOQ) was 50.4 ng/mL. The relative recoveries of ribavirin were more than 90% in plasma. The RSD of the intra-day precision was less than 10% and that of inter-day was less than 15%. The pharmacokinetic parameters of ribavirin were calculated by WinNonlin. Results indicated that the two-compartment model was a better model for describing the pharmacokinetics profile of ribavirin than one-compartment model. The AUC0-t was 10807.8 h∙ng/mL, the CL/F was 64879.5 mL, and the Cmax was 525.1 ng/mL. These results provided the experimental data for the development of ribavirin dosage form.
    Effect of parecoxib on remifentanil-induced hyperalgesia after ambulatory surgery
    Dongliang Mu, Dongxin Wang*, Yuan Qu, Chunjing Li
    2013, 22(4):  365-369.  DOI: 10.5246/jcps.2013.04.053
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    In previous human studies, pretreatment with parecoxib can effectively relieve hyperalgesia after short-term infusion of remifentanil. In this study, we aim to investigate the effect of parecoxib on hyperalgesia after short-term infusion of remifentanil in clinical practice. Totally, 120 patients who underwent ambulatory surgery were randomly divided into four groups. All patients received either parecoxib (40 mg) or normal saline (as placebo) 30 min before induction of anesthesia. Group A (placebo + propofol) and Group B (parecoxib + propofol) received only propofol for anesthesia, while Group C (placebo + propofol + remifentanil) and Group D (parecoxib + propofol + remifentanil) received both propofol and remifentanil for anesthesia. Visual analogue score (VAS) was used to evaluate pain score at various time points, including the time of birth date recollection and 30, 60, 90, 120, 180, 240, and 300 min after surgery, respectively. During the phase from discontinuation of anesthesia to 240 min after surgery, there is significant difference in the severity of pain among four groups with the order of: Group B <Group A <Group D <Group C (P<0.001). Compared with patients in Groups A and B, patients in Group C suffered significantly higher pain score. After administration of parecoxib, patients in Groups B and D experienced similar low pain score with comparison to Groups A and C (P<0.001). Patients in Groups B and D experienced shorter recovery time to eye opening on verbal command and recollection of birth date among the four groups (P<0.001). Groups B and D also had significantly improved satisfaction of pain management (P<0.001). In conclusion, short-term infusion of remifentanil can induce significant hyperalgesia in clinical practice, while pretreatment with parecoxib at 40 mg is effective in relieving such remifentani-induced hyperalgesia. In addition, we also found that pretreatment with parecoxib could significantly improve patients' satisfaction of pain management.
    Analysis of antihypertensive regimens and their intended patients from
    three hospitals in Beijing
    Kai Zheng, Yingqi Sun, Yanhong Wei, Wei Yang, Weihua Kong, Hong Shao*, Tiansheng Wang
    2013, 22(4):  370-376.  DOI: 10.5246/jcps.2013.04.054
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    This study aimed to investigate various regimens of antihypertensive agents for different groups of patients and the outcomes in the real world. We retrospectively collected 974 prescriptions for hypertension from three hospitals in Beijing, along with medical records of 219 hypertensive patients from one of the hospitals to study the regimens and their effects on patients. The antihypertensive regimens were classified by different combinations of subclasses of antihypertensive agents. Nearly all prescriptions can be classified into 11 different antihypertensive regimens, and most of them are combination therapy. Grade III hypertension patients significantly (P<0.001) tend to be treated with regimens containing calcium channel blocker (CCB) and RAAS inhibitors, angiotensin II receptor blocker (ARB) or angiotensin-converting enzyme inhibitor (ACEI). β-Blockers are more likely to be combined with CCB than with other categories of antihypertensive agents. Hydrochlorothiazide is less widely used than recommended.
    Anti-neuroinflammatory constituents from Artemisia argyi
    Shu Wang, Yong Jiang, Kewu Zeng, Jingrong Cui, Pengfei Tu*
    2013, 22(4):  377-380.  DOI: 10.5246/jcps.2013.04.055
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    Chemical constituents of the leaves of Artemisia argyi were investigated. By using a variety of chromatographic techniques and spectroscopic methods, six compounds were isolated and identified as follows: clemaphenol A (1), aurantiamide acetate (2), camelliagenin A (3), japonica acid (4), labd-13(E)-ene-8α,15-diol (5), and 3β-acetoxy-20-oxo-21-nordammaran-23-oic acid (6). Among these products, compounds 1 and 3-6 were obtained from the genus Artemisia for the first time and compound 2 was firstly reported from the species. Additionally, compound 5 displayed an inhibitory effect against the lipopolysaccharide (LPS)-induced nitric oxide (NO) production in BV-2 microglial cells with an IC50 value of 6.68 μM.