Journal of Chinese Pharmaceutical Sciences

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2013, 22(1): 1-6.

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GLP-1 biology and GLP-1 based antidiabetic therapy

Fan Yi, Dong Li, Weizhi Ma, Quan Du^*

2013, 22(1): 7-27. DOI: 10.5246/jcps.2013.01.001

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Environmental and lifestyle factors together account for the dramatic increase of type 2 diabetes in the past decades, in which defective insulin secretion emerges as the major culprit. Glucagon-like peptide 1 (GLP-1) is a peptide secreted from the intestine in response to nutrient ingestion, and plays an essential role in the regulation of blood glucose level by stimulating glucoses-dependent insulin secretion. Recently, GLP-1 develops to be a viable therapeutic target for the treatment of type 2 diabetes, by means of GLP-1 receptor agonists and dipeptidyl peptidase-4 inhibitors. Stemmed from its potent physiological activities, GLP-1-based therapies are clinically efficient and safe for both early and late stages of the disease, with low risk of adverse events. In this review, a comprehensive understanding of GLP-1 biology and the recent development of GLP-1-based antidiabetic therapy are summarized.

Four natural epothilone derivatives isolated from Sorangium cellulosum strain So0157-2

Chunhua Lu, Lin Zhao, Yuezhong Li, Yuemao Shen^*

2013, 22(1): 28-31. DOI: 10.5246/jcps.2013.01.002

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Four natural epothilone analogues, including two 14-membered epothilones L (1), L1 (2) and two epoxide opened epothilones A (3) and B (4), were isolated from the extract of fermentation adsorber resin of Sorangium cellulosum strain So0157-2. Their structures were elucidated on the basis of comprehensive NMR and MS data. They are all isolated from the wild type S. cellulosum strain So0157-2 as natural products for the first time.

A new 3, 11-cyclotaxane diterpenoid from Taxus media Rehd. cv. Hicksii

Rong Yang, Kehui Xie, Tianzhi Cai, Hongzheng Fu^*

2013, 22(1): 32-35. DOI: 10.5246/jcps.2013.01.003

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The aim of current study was to investigate the chemical constituents of the needles of Taxus media. The isolation and purification of components were achieved by a series of chromatography including silica gel, Sephadex LH-20, MCI and reversed-phase HPLC. Their structures were indentified based on 1D, 2D NMR, and mass spectral analysis. Seven taxane diterpenoids were isolated and identified as 1β,2α,9α,10β-tetrahydroxy-5α-cinnamoyloxy-3,11-cyclotaxa-4(20)-en-13-one (1), 2α, 7β, 9α, 10β, 13α-pentaacetoxytaxa-4(20), 11-dien-5α-ol (2), 2-deacetoxy-5-decinnamoyltaxinine J (3), taxuspine F (4), taxuspinanane K (5), taxchin A (6), and baccatin IV (7). Among them, 1 is a new compound and compounds 2, 5, 6 and 7 are isolated from Taxus media for the first time.

Isolation of flavonoids from the aerial parts of Polygala tenuifolia Willd. and their antioxidant activities

Tianxing Shi, Yuguang Li, Yong Jiang^*, Pengfei Tu

2013, 22(1): 36-39. DOI: 10.5246/jcps.2013.01.004

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The aim of this study was to isolate the chemical constituents of the aerial parts of Polygala tenuifolia Willd. and to determine their antioxidant activities. Ten flavonoids were isolated and purified by silica gel, Sephadex LH-20, and ODS column chromatography, and semi-preparative HPLC. Their structures were elucidated by spectroscopic analysis and identified as isorhamnetin-3-O-β-D-glucopyranoside (1), isorhamnetin-3-O-β-D-galactopyranoside (2), quercetin-3-O-β-D-glucopyranosyl (1→2)-β-D-galactopyranoside (3), quercetin-3-O-β-D-glucopyranosyl (1→2)-β-D-glucopyranoside (4), linarin (5), quercetin-3-O-β-D-glucopyranoside (6), 5,7-dihydroxy-8-methxoyflavone-7-O-β-D-glucuronoside (7), isorhamnetin (8), kaempferol (9) and quercetin (10). All these compounds were isolated from this plant for the first time, and compounds 1-5 and 7 were isolated from the genus of Polygala for the first time. The antioxidant activities of the isolated compounds were evaluated by DPPH free radical scavenging assay, and compounds 3, 4, 6, 8, 9 and 10 showed potent antioxidant activities.

Chromatographic fingerprint analysis of Bupleuri Radix by HPLC-ELSD

Yong Zhou, Yanliang Wang, Zhiqiao Ma, Bin Wang, Hong Liang, Yuying Zhao, Qingying Zhang^*

2013, 22(1): 40-46. DOI: 10.5246/jcps.2013.01.005

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To facilitate the species identification and quality assessment of Chaihu (Bupleuri Radix), a simple and valid chromatographic fingerprint method was developed. The method uses high-performance liquid chromatography coupled with evaporative light scattering detector (HPLC-ELSD) and the data analysis is assisted by professional analytical software recommended by the State Food and Drug Administration (SFDA). The results indicate that Nan Chaihu raw materials and Chaihu decoction pieces vary markedly in chemical quality, while Bei Chaihu raw materials are relatively more stable. Furthermore, it is obvious that Nan Chaihu is chemically very different from Bei Chaihu, suggesting that Nan Chaihu may not be suitable for medicinal use. In addition, the obvious differences between the chromatograms of decoction pieces and raw materials, especially the peaks between 30 and 40 min and after 45 min, indicate possible effects of the processing procedures on the chemicals. By analyzing the fingerprints of all samples, 12 main saponin-like fingerprint peaks, of which at least three are characteristic peaks of saikosaponins a, c, and d, are proposed to be considered for further characterization and quality evaluation of Chaihu.

Simultaneous determination of 15 bioactive compounds in Fufang Zhenzhu Tiaozhi capsules by HPLC-DAD-ELSD

Hui Fan, Jiao Guo^*, Yuanyuan Chen

2013, 22(1): 47-54. DOI: 10.5246/jcps.2013.01.006

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Fufang Zhenzhu Tiaozhi capsules (FTZc), which is consisted of eight traditional Chinese herbal medicines and contains multiple bioactive ingredients, is a patented and clinically approved herbal formulation for the treatment of dyslipidemia. A feasible HPLC-DAD-ELSD method was developed to simultaneously determine 15 bioactive compounds (salidroside, specneuzhenide, magnoflorine, rosmarinic acid, salvianolic acid B, columbamine, jatrorrhizine, epiberberine, coptisine, palmatine, berberine, 5,7-dimethoxycoumarin, ginsenoside Rg1, ginsenoside Rb1 and oleanic acid ) in FTZc for its quality control. The multiple wavelength detection mode of DAD was used. The chromatographic separation was performed on an Ultimate XB C18 column with gradient elution. The mobile phase A (acetonitrile) and B (0.25% glacial acetic acid and 0.13% triethylamine in water, v/v) were run at a flow rate of 0.8 mL/min. The developed method showed good precision and accuracy with overall intra- and inter-day variations of 0.7%-1.9% and 0.6%-3.0%, respectively. The recoveries measured at three concentration levels, varied from 95.5% to 103.8%. The validated method was successfully applied for the simultaneous determination of 15 bioactive compounds in three batches of FTZc. The results suggested that the developed method was convenient and reliable, particularly suitable for the routine quality control of FTZc.

Fingerprint analysis of Ophiopogonis Radix by HPLC-UV-ELSD coupled with chemometrics methods

Ning Li, Yanyun Che, Liang Zhang, Jiayu Zhang, Yuan Zhou, Yong Jiang, Pengfei Tu^*

2013, 22(1): 55-63. DOI: 10.5246/jcps.2013.01.007

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A new, simple and reliable method using HPLC-UV-ELSD was developed to generate the fingerprint of Ophiopogonis Radix. Homoisoflavonoids and steroidal saponins were determined simultaneously in a single run. A total of 27 Ophiopogonis Radix samples were analyzed, and 18 reference substances were used for the identification of the common peaks. The fingerprint was further analyzed by chemometrics methods including similarity analysis (SA), hierarchical clustering analysis (HCA) and principal component analysis (PCA). The results indicated that the combination of chromatographic fingerprint and chemometrics analysis could be used for the geographical differentiation and quality evaluation of Ophiopogonis Radix.

Lanthanum chloride promotes proliferation of NIH 3T3 cells via cell cycle machinery

Xin Pan, Jinxia Li, Faqin Dong, Jianjun Deng, Lan Yuan, Kui Wang, Siwang Yu^*

2013, 22(1): 64-70. DOI: 10.5246/jcps.2013.01.008

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Lanthanum ions (La³⁺) have been reported to exert profound effects on the proliferation of NIH 3T3 mouse embryonic fibroblasts. In the present studies, the pro-proliferative effect of La³⁺ on NIH 3T3 cells was further characterized, and its impacts on the cell cycle kinetics were analyzed in detail by cell cycle arrest-and-release and pulse BrdU-labeling and chasing experiments. The results show that La³⁺ promoted the proliferation of NIH 3T3 cells after 12 h and the EC50 was 2.4 μM after 48 h. Such effect was also confirmed by enhanced BrdU incorporation. La³⁺ stimulated more cells to pass through the G1/S checkpoint into S phase, but did not change the length of cell cycle. Furthermore, La³⁺-treatment increased the protein levels and nuclear localization of cyclin D1 and c-Myc, two key regulators of G1/S checkpoint, as demonstrated by immunostaining. The pro-proliferative effects of La³⁺ share striking similarity with that of Gd³⁺, and provided new information regarding the cellular biological activities of lanthanides.

Gadolinium-promoted angiogenesis involves the activation of PKCα/β2 and MAPKs in human umbilical vein endothelial cells

Xiao Wan, Baodi Gou^*, Kui Wang^*

2013, 22(1): 71-76. DOI: 10.5246/jcps.2013.01.009

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Gadolinium has been widely used as a contrast agent for magnetic resonance imaging in clinical practice. Recently, it was reported that gadolinium is involved in nephrogenic systemic fibrosis, although the exact mechanism by which gadolinium triggers nephrogenic systemic fibrosis remains unclear. In this study, we show that gadolinium chloride (GdCl₃) induced human umbilical vein endothelial cells (HUVECs) to migrate in Matrigel and tubulogenesis during wound healing. Chick chorioallantoic membrane assay confirmed that GdCl₃ stimulates angiogenesis. Under the optimal angiogenic concentration of GdCl₃ (10 μM), intracellular calcium concentration and reactive oxygen species generation were elevated. Moreover, western blotting results indicate that in cells treated with GdCl₃, Ca²⁺-dependent PKCα/β₂ was phosphorylated, and MAPKs pathways were also activated. Taken together, GdCl₃ has a potential effect on angiogenesis in HUVECs, and the possible mechanisms may involve oxidative stress and calcium-related signaling pathways.

Mitochondria as the main source of vanadyl acetylacetonate-induced reactive oxygen species generation in renal epithelial cell lines

Congcong Hou, Gang Wang, Xiaogai Yang^*

2013, 22(1): 77-80. DOI: 10.5246/jcps.2013.01.010

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In this study, we aimed to clarify the source of the reactive oxygen species (ROS) generation induced by vanadium compounds. We used vanadyl acetylacetonate (VO(acac)₂), a highly effective agent in controlling hyperglycemia, to determine the source of ROS generation in two renal cell lines LLC-PK₁ and MDCK. Four commonly fluorescent dyes were used to assess VO(acac)₂-induced H₂O₂ and ·O₂^- production and their location. It demonstrated that VO(acac)₂can induce significant ROS generation in both LLC-PK₁ and MDCK cells, which were primarily derived from mitochondria. The results obtained in this study raised the possibility to reduce ROS level induced by vanadium compounds locally and thus avoid affecting its activity.

Acid sensitive doxorubicin-PAMAM with tumor targeting profile

Fei Peng, Pengchao Gao, Xiangtao Wang, Xin Hu^*

2013, 22(1): 81-88. DOI: 10.5246/jcps.2013.01.011

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Poly (amidoamine) dendrimers are emerging as versatile and derivatizable nano-scale drug delivery vehicles. In our study, cis-4,7,10,13,16,19-docosahexenoic acid and doxorubicin were conjugated to generation 2.5 PAMAM. The molecular architecture of the carrier was designed for optimized blood circulation and optimized drug release through the use of pH-sensitive hydrazone linkages. In vitro, DHA-PAMAM-DOX conjugates were able to release twice as much doxorubicin at pH 4.5 (lysosomal pH) as at pH 7.4, ensuring more pronounced antitumor activity. Upon intravenous administration to ICR mice, the DHA-PAMAM-DOX delivery systems resulted in more plasma exposure of doxorubicin than free doxorubicin solution. In efﬁcacy studies performed with B6D2F1 mice bearing B16 melanoma tumors, DHA-PAMAM-DOX was significantly more efficient in inhibiting tumor growth than free doxorubicin at the dose equivalent to 5 mg/kg doxorubicin. Our research provides evidence that DHA-PAMAM-DOX conjugates have the potential to enhance the effect of cancer therapy in the course of delivering anticancer drugs to their target sites.

Effects of compound 209 on colorectal cancer cell HT-29 in vivo and in vitro

Xiao Jiang, Xia Yuan, Mingming Chu, Wei Guo, Jingtao Liu, Fuxiang Ran, Zemei Ge, Runtao Li^*, Jingrong Cui^*

2013, 22(1): 89-94. DOI: 10.5246/jcps.2013.01.012

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Compound 209 is a newly synthesized dithiocarbamate derivative with antiproliferation activity in vitro, however, its antitumor effect in vivo and the underlying mechanisms have yet to be identified. We explored the antitumor effect of compound 209 and the possible mechanisms for its inhibition of the growth of HT-29 xenograft tumor and proliferation of HT-29 cells. Cell proliferation was evaluated with SRB assay in vitro. The results showed that compound 209 had significant antiproliferation activity on HT-29 cells. Furthermore, the xenograft HT-29 nude mouse model was used to study the antitumor effect of compound 209 in vivo. We found that compound 209 significantly inhibited tumor growth and did not cause loss of body weight or leukocytopenia. Analysis by flow cytometry indicated that compound 209 arrested HT-29 cell cycle in G₁ phase. Western blotting analysis suggested that compound 209 increased the expression of p27, cyclin E, CDK2, cyclin D1 and CDK4. These results demonstrated the antitumor effect of compound 209 and its potential use as an anticancer drug.

Analysis and comparison of two low-dosage warfarin regimens in Chinese patients

Guy-Armel Bounda^*, Cosette Ngarambe, Weihong Ge, Feng Yu

2013, 22(1): 95-100. DOI: 10.5246/jcps.2013.01.013

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Oral anticoagulation therapy with warfarin is used to prevent and treat venous and arterial thrombosis and embolism. Its narrow therapeutic index should be monitored carefully in order to reach the desired outcomes. The complexity of the pharmacokinetic and pharmacodynamics profile of warfarin makes it a challenge to use during treatment. Its manufacturing characteristics play a key role in its dosage. The aim of this study is to examine and evaluate the effect of two different warfarin regimens in Chinese patients. A cross-sectional study design was adopted. Medical records of all patients (n = 368) who received warfarin therapy in cardio-thoracic surgery wards between Sep. 2008 and Dec. 2009 were reviewed. Details of antithrombotic results of international normalized ratio (INR) monitoring were obtained. Statistical analysis was performed to assess factors predictive of INR therapeutic range at patients’ discharge time according to different warfarin regimens (2.5 mg in China and 3.0 mg in USA). The patients’ mean age was (48.23±12.96) years. The percentage of patients within the INR therapeutic range in the group treated with 2.5 mg warfarin (35.17%) was much lower than that in group treated with 3.0 mg warfarin (47.72%). Therefore, a significance difference was observed (P = 0.032<0.05). In this study, statistical values have shown that most of the patients were related to medical case requesting INR target range of 1.8-2.2 and 2.0-2.5, respectively. There was a statistically significant difference between the two groups. The study showed that the 2.5 mg-warfarin regimen was less suitable than the 3.0 mg-warfarin regimen. Medication regimen should be simplified as much as possible, especially during different treatment period.

Quantification of the active ingredient quercetin of “Guangdong Wang-bu-liu-xing” by high-performance liquid chromatography with UV detection

Song Zeng, Xiuqi Han, Shuyuan Li^*

2013, 22(1): 101-105.

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High-performance liquid chromatography with UV detection was used for the quantification of the flavonoid quercetin, the active compound found in “Guangdong Wang-bu-liu-xing”. The method was developed and demonstrated to provide superior performance over other commonly documented methods. This HPLC assay achieved high specificity through the use of a reversed-phase C18 column eluted with a mobile phase of methanol-0.4% (v/v) phosphoric acid (50:50, v/v) over the course of 30 min. UV detection at 360 nm was used. This analytical method provided excellent precision and a mean recovery of 99%, demonstrated by repeated analysis of 11 sample groups. Because of its high performance and simplicity, this HPLC assay can be readily utilized as a practical method for the quality control of active compounds extracted from Guangdong Wang-bu-liu-xing.

Acetylcholinesterase inhibitory activities of 48 traditional Chinese medicinal herbs

Ping Chen, Peipei Wang, Guohua Shao, Lan Xiang^*

2013, 22(1): 106-109. DOI: 10.5246/jcps.2013.01.015

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Inhibition of acetylcholinesterase (AChE) is one of the approaches for the treatment of Alzheimer's disease (AD). In this paper the AChE inhibitory activities of ethanolic and aqueous extracts of 48 traditional Chinese medicinal herbs were evaluated. These traditional Chinese medicines have intelligence-promoting, anti-insomnia, sedative, neurotonic or tonic effects. Microplate assay indicated that ethanolic extracts of 28 traditional Chinese medicinal herbs and water extracts of 11 herbs showed AChE inhibitory activities. Among them, ethanolic extracts of Herba Moslae, Fructus Alpiniae Oxyphyllae, Radix Rehmanniae and Folium Nelumbinis showed most potent AChE inhibitory activities at the concentration of 0.1 mg/mL, with (68.63±1.12)%, (44.49±3.66)%, (43.78±4.76)%, and (42.63±8.31)% inhibition, respectively. The AChE inhibitory activities were also confirmed by TLC bioautographic assay. These results partially validate the traditional uses of some medicinal herbs for cognitive improvement.

Sensitive method for rapid estimation of Lornoxicam in bulk and its dosage form by RP-HPLC

Prajapati Prajesh^*, Vaghela Vipul, Baraiya Dharmendra

2013, 22(1): 110-113. DOI: 10.5246/jcps.2013.01.016

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Lornoxicam (6-chloro-4-hydroxy-2-methyl-N-2-pyridyl-2H-thieno-[2,3-e]-1,2-thiazine-3-carboxamide-1,1-dioxide) is persist as a non-steroidal anti-inflammatory drug of the oxicam class with analgesic, anti-inflammatory and antipyretic properties. A fast, accurate and sensitive chromatographic method for estimation of Lornoxicam was developed as no official method available for detection. The chromatographic separation employs isocratic elution by utilizing an inertsil ODS-C18, 250 mm×4.6 mm, 5 µm columns. Mobile phase consisting of solvent (40 mL acetonitrile and 60 mL 0.1 M phosphate buffer (pH 6.8 was adjusted with triethylamine)) endowed at a flow rate of 1.0 mL/min. The analyte was detected and quantified at 290 nm using UV detector. The method was validated according to ICH guidelines, illustrating to be accurate (recovery 99.08%-101.13%) and precise (intraday (0.27-1.32) and interday (0.59-1.59))within the corresponding linear range (10-60 µg/mL) with r² 0.9992.

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Journal of Chinese Pharmaceutical Sciences

2013, 22(1): 114-121.

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