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Table of Content

    15 September 2009, Volume 18 Issue 3
    Contents

    Graphical contents list

    Journal of Chinese Pharmaceutical Sciences
    2009, 18(3):  197-200. 
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    Review
    New progress in the study of poly (L-glutamic acid)-paclitaxel conjugates for cancer treatment
    Yi-Ning Song, Shuang-Qing Zhang*, Zhen-Qing Zhang*
    2009, 18(3):  201-207. 
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    The preparation of polymer-anticancer drug conjugates is an effective way to improve the efficacy and decrease the toxicity of anticancer drugs. Polymer-drug conjugates, which were made by combining a suitable polymeric carrier, a biodegradable linker and a bioactive anticancer agent, could form the basis of a new generation of anticancer agents. Poly (L-glutamic acid)-paclitaxel conjugate is a polymer-drug conjugate that links anticancer agent paclitaxel (PTX) to poly (L-glutamic acid) (PG). PG-PTX conjugate can improve the anticancer activity, enhance the safety and efficacy, and improve the pharmacokinetic properties of PTX. Therefore, the application of PG-PTX facilitates the clinical therapy of a variety of human cancers.
    Research progress on the chemical constituents and pharmacological activities of Fructus corni
    Gang Cao1, Yu Zhang1, Xiao-Dong Cong1, Hao Cai1, Bao-Chang Cai1, 2*
    2009, 18(3):  208-213. 
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    Fructus corni is the dried sarcocarp of Cornus officinalis Sieb. et Zucc. It has been used as an important traditional Chinese medicine. Its action is to protect liver and kidney and regulate the essence of human body. In this paper, the research progress on the chemical ingredients and pharmacological activities of Fructus corni are reviewed. According to its pharmacological activities, some suggestions for future research and development have been made.

    Full Papers
    Synthesis of S-linked tumor-associated carbohydrate antigen STn
    Chang-Xin Huo, Xin-Shan Ye*
    2009, 18(3):  214-217. 
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    Modified tumor-associated carbohydrate antigens could be used to develop anti-cancer vaccines. Carbohydrate antigens in which thioglycosidic linkages are used instead of O-glycosidic linkages may be more immunogenic and may stimulate the production of antibodies capable of recognizing naturally occurring carbohydrates due to their enhanced resistance to endogenous glycosidases and their inherent non-self antigen character. For this purpose, a new S-linked tumor-associated carbohydrate antigen STn has been successfully synthesized for the first time.
    Enhancement of fluorescence of terbium and transferrin-bound diterbium by HEPES
    Ping Du1, Lan Yuan2*, Hou-Nan Wu2, Ke-Ning Xu3, Xiao-Gai Yang1*
    2009, 18(3):  218-224. 
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    Terbium (Tb) has been extensively used as a fluorescence probe for the identification of calcium-binding sites in proteins and for fluorometric analysis of organic ligands. In the current study, we reported that HEPES, a commonly used pH buffer reagent, significantly enhanced the characteristic emission of Tb at 585 nm. The maximum emission of Tb at 490 nm and 549 nm were also enhanced by HEPES to a less extent. Thus, cautions should be taken when quantitative analysis is performed based on the fluorescence emission of Tb at 549 nm, since the emission may vary due to the buffer reagents. Additionally, the fluorescence intensity at 585 nm was proportional to the concentration of both HEPES and terbium ions, which might be utilized to develop new fluorometric analytical methods.
    Quercetin and green tea polyphenols inhibit the mitochondrial damages and cytotoxicity induced by VO(acac)2
    Yue-Bin Zhao, Zhe Shi, Li-Hua Ye, Hui-Xue Liu*, Xiao-Da Yang*, Kui Wang
    2009, 18(3):  225-231. 
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    Vanadium compounds are promising therapeutic agents for the treatment of diabetes and cancer. However, vanadium toxicity has been a great concern. Many works suggested that vanadium-induced oxidative stress is a major reason of vanadium toxicity. Quercetin and green tea polyphenols (GTP) are well-known antioxidants that play important roles in the prevention of many oxidative stress-related diseases. In this study, we investigated the protective effects of quercetin and GTP against damages caused by VO(acac)2 on isolated mitochondria and whole cells. The experimental results demonstrated that quercetin and GTP could significantly inhibit mitochondrial dysfunctions induced by VO(acac)2, such as mitochondrial swelling, depolarization of the inner mitochondrial membrane potential (Δψm), and increased release of reactive oxygen species (ROS). Moreover, they also reduce cytotoxicity in Hep G2 cells. These results indicated that use of natural antioxidants to control the metal toxicity of vanadium compounds may be a promising strategy for developing metal-based therapeutic agents.
    A new linear monoterpene from the Chinese mangrove plant Cerbera manghas L.
    Xia Yu1, Min-Juan Xu1, Zhi-Wei Deng2, Wen-Han Lin1*
    2009, 18(3):  232-235. 
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    The current study aimed to investigate the chemical components of the Chinese mangrove plant Cerbera manghas L., collected in Hainan Island. Repeated column chromatography was performed for the isolation and purification. Compounds were identified by the analysis of their 1D and 2D NMR data as well as IR and MS spectral data. A new linear monoterpene, named (2E,6S)-8-hydroxy-2-hydroxymethyl-6-methyl-2-octenoic acid (1), together with cerbinal (2), cerberidol (3), 2α,3β,24-trihydroxyolea-12en-28oic acid (4), 4,4',9,7'-tetrahydroxy-3,3'-dimethoxy-7,9'-epoxylignan (5), (-)-olovil (6), (+)-cycloolivil (7), naringenin-7-glucoside (8), aromadendrin (9), naringenine (10), and (+)-dihydroquercetin (11) were isolated from the EtOH and CH2Cl2 extracts. Compounds 4, 5, 8-11 were isolated from this plant for the first time.
    Liposoluble chemical constituents from the fibrous root of Ophiopogon japonicas
    Chang-Ling Duan1,2, Yu Jiang3, Yong Jiang1, Cheng-Ren Lin2, Jian-Xun Liu2, Peng-Fei Tu1*
    2009, 18(3):  236-239. 
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    We investigated the chemical constituents of the fibrous root of Ophiopogon japonicus and their cytotoxicities against Hela and Hep2 cells. Ten compounds were purified by various chromatographic techniques. Their structures were identified as 2'-hydroxylophiopogonone A (1), 5,8-dimethoxy-6-methyl-7-hydroxy-3-(2'-hydroxy-4'-methoxybenzyl) chroman-4-one (2), 5,7-dihydroxy-6,8-dimethyl-3-(4'-hydroxybenzyl) chroman-4-one (3), 7,4'-dihydroxy-5-methoxyflavanone (4), N-trans-coumaroyltyramine (5), N-trans-coumaroyloctopamine (6), N-trans-feruloyltyramine (7), 4-hydroxycinnamic acid (8), caffeic acid (9), and ferulic acid (10) on the basis of spectroscopic analyses. Compounds 4, 6, 7, 9, 10 were obtained from this genus for the first time. The cytotoxic activities of 1, 2, 4, 5, 6, 7, 9 and 10 against Hela and Hep2 cells are described.
    Chemical composition and antimicrobial activities of the essential oil of Aconitum tanguticum
    Chun-Jiang Zhang1, Chun-Mei Liu2, Tian Yun1, Hong-Yu Li1*
    2009, 18(3):  240-244. 
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    The composition and antimicrobial activities of the essential oil of Aconitum tanguticum from the southern part of Gansu Province of China were investigated. The essential oil of aerial parts was obtained by hydrodistillation with a 0.7% (v/w) yield. The chemical composition of the essential oil was analyzed by gas chromatography-mass spectrometry (GC-MS) method. Thirty-five compounds were characterized in the oil, which were mainly monoterpenoids (41.7%) and sequiterpenoids (12.7%). The main compounds in the oil were (-)-tran-pinecarvyl acetate (15.6%), heptane (14.88%), cineole (6.82%), 3-pinanone (3.64%), pinocamphone (3.34%), cadinol (2.93%), and cubenol (2.33%). These compounds are identified for the first time in Aconitum tanguticum. The antimicrobial activities of the oil were evaluated against 9 bacteria strains, 1 yeast strain and 3 fungi strains using agar diffusion and broth microdilution methods. It showed strong inhibition against Fusarium semitectum and methicillin-resistant Staphlococcus aureus, low activity against Escherichia coli, but no effect against Epidermophyton floccosum. Its MIC values ranged from 0.125-5.000 mg/mL. Thirty-five compounds are newly identified in Aconitum tanguticum.
    Investigation of the redox status in H22 hepatocellular carcinoma xenografts treated by a novel anticancer drug——ethaselen
    Li-Hui Wang1,2, Hui-Hui Zeng1,2*
    2009, 18(3):  245-251. 
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    We investigated the redox status of H22 hepatocellular carcinoma xenografts treated with various doses of ethaselen, a novel anticancer drug targeting thioredoxin reductase (TrxR). The concentrations of low molecular weight antioxidant glutathione (GSH) and malondialdehyde (MDA), a product of lipid peroxidation, as well as the activities of important antioxidant enzymes were measured for elucidating the redox status of H22 tumor tissues. We found that the decreased GSH level, decreased thioredoxin reductase and superoxide dismutase (SOD) activities as well as increased MDA content were closely related to the tumor growth inhibition and ethaselen doses. Glutathione peroxidase (GPx) and glutathione reductase (GR) activities are also affected by ethaselen treatment. However, the catalase (CAT) activity remains unchanged. Finally, we studied the relationship of tumor growth inhibition caused by ethaselen with these redox factors. This study showed that ethaselen could elevate the oxidative stress to suppress the H22 tumor growth in mice model.
    The effects of pinellia total alkaloids on the amino acid concentration and the GABAA receptor expression in hippocampus region of epileptic rats
    Yan-Ting Gu, Yong-Gang Ma, Ming-Zheng Wang*, Xin-Feng Wang, Yi Xiao
    2009, 18(3):  252-256. 
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    The antiepileptic effect of pinellia total alkaloids (PTA) on penicillin (PNC) chronically kindled rats was investigated. We investigated the effects of PTA on Glu, Asp, Gly and γ-aminobutyric acid (GABA) concentrations and the expression level of cerebral GABAA receptor in hippocampus. The influence of PTA on epilepsy seizure latency and degree in PNC chronically kindled rats were observed. High performance liquid chromatography (HPLC) was adopted to measure the concentrations of Glu, Asp, Gly and GABA in hippocampus. Reverse transcriptase-polymerase chain reaction (RT-PCR) was used to determine the expression of cerebral GABAA receptor mRNA. Compared with normal rats, the levels of GABA and Gly decreased obviously while the level of Glu and Asp increased significantly in model rats. The cerebral GABAA receptor mRNA level was also decreased at the same time. The difference was statistically different compared to the control group. PTA could prolong the latent period of the penicillin induced seizure and weaken the extent of seizure, compared with the model group without PTA treatment. Moreover, PTA increased the level of GABA and the expression level of GABAA receptor, while decreased the level of Glu significantly. However, it had no obvious effect on the level of Gly and Asp. Pre-treatment of PTA can also increase the GABAA receptor mRNA level. In conclusion, PTA could alleviate the PNC chronically kindled rat seizure. It increased the GABA level and the expression of GABAA receptor, and it decreased the Glu concentration.
    Antitumor efficacy of doxorubicin encapsulated in neovasculature targeting liposomes
    Song Zhuang, Xian-Rong Qi*
    2009, 18(3):  257-260. 
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    It was reported that a 5-amino acid peptide Ala-Pro-Arg-Pro-Gly (APRPG) could specifically bind to the tumor angiogenic site. We investigated the antitumor efficacy of doxorubicin (DOX) encapsulated in APRPG modified liposome (APRPG-LP) compared with DOX encapsulated in non-APRPG modified liposomes (LP) and DOX solution (free DOX) on Lewis lung carcinoma (LLC) bearing mice. APRPG-LP could efficiently suppress the tumor growth of the experimental mice, compared with LP (P<0.001), free DOX (P<0.001) and saline of negative control (P<0.001). The present results demonstrated that the APRPG modified liposomes exhibited a much better therapeutic efficacy over the non-modified liposomes and the DOX solution, because of the effect of targeted tumor angiogenesis disruption. Thus, APRPG-LP could be a promising active-targeting drug carrier to tumor angiogenic site.
    Determination of montelukast in human plasma by LC-ESI-MS and its application in pharmacokinetic study
    Yao Huang1, Li Ding1*, Yuan-Yuan Liu1, He-Ying Liu1, Ai-Dong Wen2, Lin Yang2
    2009, 18(3):  261-266. 
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    A liquid chromatography-electrospray ionization-mass spectrometry (LC-ESI-MS) method was developed for the determination of montelukast in human plasma. After precipitation of plasma proteins, the plasma samples were separated on a C18 column with a mobile phase consisted of 20 mmol/L ammonium acetate buffer solution containing 0.2% formic acid-methanol (12:88, v/v). LC-ESI-MS was performed in the selected-ion monitoring (SIM) mode using target ions [M+H]+ at m/z 586.2 for montelukast and m/z 515.2 for telmisartan, the internal standard (IS). The calibration curve was linear over the plasma concentration range of 1 ng/mL-1000 ng/mL. The lower limit of quantification (LLOQ) was 1 ng/mL for montelukast. The relative standard deviations of intra- and inter-batches were less than 5.9% and 10.0%, respectively. The method was successfully applied to study the pharmacokinetics of montelukast sodium tablets in healthy Chinese volunteers.
    Effects of pegylated cationic liposomes on siRNA transfection
    Li-Juan Yang, Ting Yang, Juan Jiang, Zhen-Zhong Xu, Jian-Cheng Wang*, Qiang Zhang
    2009, 18(3):  267-272. 
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    This study aimed to investigate the effects of cationic liposomes containing different cationic lipids (DC-Chol and DOTAP) and different pegylation ratios on siRNA transfection in human U251 glioma cells. The data showed that the transfection efficiency of DOTAP was much higher than that of DC-Chol and PEG at 2 mol% enhanced cellular uptake of siRNA. Cationic liposome-siRNA complexes with particle size around 100 nm were prepared. PEG modification could efficiently stabilize the liposome in the presence of serum, which might protect the siRNA from serum degradation and prolong the circulation time in vivo. Efficient intracellular uptake and lysosome release of siRNA in human U251 glioma cells were observed for pegylated DOTAP-based lipososomes compared with the control transfection reagent lipofectamine 2000. The results demonstrated that this cationic liposome might be a potential vehicle for the in vivo delivery of siRNA.
    Pharmacokinetics of diclazuril after oral administration of clinical doses to rabbits
    Lian-Dong Hu1*, Ci Liu1, Wen Xu2
    2009, 18(3):  273-277. 
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    The purpose of this study was to evaluate the pharmacokinetic parameters and bioavailability of the solid dispersion formulation of diclazuril after oral administration in rabbits in comparison with its known premix form with feed additive. Plasma concentrations were determined by high-performance liquid chromatography (HPLC). The areas under the plasma concentration curves (AUC0–∞) of diclazuril in solid dispersion and premix were 247.8±18.1 μg/h/mL and 145.4±12.6 μg/h/mL, respectively. The Cmax of diclazuril in solid dispersion and premix were 33.72±4.75 μg/mL and 16.42±3.48 μg/mL, respectively. The t1/2 were 9.53±1.37 and 9.23±1.20 min, respectively. The oral bioavailability of drug solid dispersion was 1.7-fold higher than that of premix. From these data we concluded that diclazuril solid dispersion may be used as a potential anticoccidial preparation.
    Exploratory research on drug safety in China
    Xiao-Wu Huang1, Yi-Lin Lv2, Lu-Wen Shi3, Bin Jiang2,3*
    2009, 18(3):  278-282. 
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    The article defines the concept of drug safety, summarizes the problems and causes in the area of drug safety in China, and proposes relevant measures to solve the problems.
    Impact of pharmaceutical intervention on the rational use of antibiotics in primary hospital
    Ying Cao1,2, Wei Yang1, Xiao-Wen Lin1, Hong Shao1*
    2009, 18(3):  283-286. 
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    Evidence based pharmaceutical interventions focusing on the characteristics of antibiotics use in primary hospitals were investigated to optimize the use of antibiotics. Four pharmaceutical interventions were set up in this study: 1) different levels of antibiotic management system were developed; 2) usage of antibiotics was reported in a monthly journal for the entire hospital; 3) early antibiotics warning system was started; 4) communication between pharmacists and physicians was strengthened. Use of antibiotics in 2007 (before intervention) and 2008 (after intervention) in department of respiratory medicine was analyzed. Significant differences (P<0.01) in antibiotics use before and after intervention were observed. Use of antibiotics was changed from focusing on one category of drugs to a rotation of a wide range of agents. Evidence based, sound pharmaceutical interventions were effective means to ensure the rational use of antibiotics.
    Others
    General information and subscription
    Journal of Chinese Pharmaceutical Sciences
    2009, 18(3):  287-287. 
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    Brief introduction of School of Pharmacy, Fudan University
    2009, 18(3):  288-288. 
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