Table of Content

15 May 2010, Volume 19 Issue 3

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Contents

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Journal of Chinese Pharmaceutical Sciences

2010, 19(3):  159-162. 

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Review

Drug efficacy and pharmacological action of an organoselenium compound ethaselen, a novel antitumor drug

Jia-Ning Fu, Jing-Yu Wang, Li-Hui Wang, Lei Wang, Wan-Chen Tang, Gao-Xiong Cai, Mi Liu, Hui-Hui Zeng^*

2010, 19(3):  163-168. 

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Ethaselen, an organoselenium compound designed and synthesized in the School of Pharmaceutical Sciences, Peking University, has been entitled to independent intellectual property rights both at home and abroad. As one of the novel antitumor drugs, ethaselen has been extensively studied in Phase I clinical trial, and its biological target is thioredoxin reductase. In this review, we focus on the ethaselen’s efficacy and pharmacological actions, including antitumor effects both in vitro and in vivo, and immunologic functions. These research findings not only provide the theoretical basis for the anticancer study of ethaselen, but also guide the clinical trial of ethaselen.

Solutions to improve the quality management of medical gas pipeline systems in China

Shuo Lin^*, Hélène van den Brink, Eric Fouassier, Alejandro Berardi

2010, 19(3):  169-176. 

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Gases have long been used for medical applications across the world. Medical oxygen, one of the most important medical gases, has been widely applied both in hospitals and at home. It is defined as a drug and its pipeline distribution systems are medical devices whose quality and management should conform to specific standards. In China, several deficiencies relating to the distribution and use of medical oxygen, which may lead to a number of fatal accidents like gas pipeline explosion and cause illicit product use, have been revealed in health facilities. They are the result of a lack of the relevant standards, management and practical experiences. To overcome these failures, it might be interesting to refer to the experience and regulations of other countries, for example, those of France.

Full Papers

Inhibition of angiogenesis by DADAG in vivo and in vitro

Jing-Tao Liu, Bo Xu, Min Li, Ying Zhou, Jing-Rong Cui^*

2010, 19(3):  177-185. 

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1,2,5,6-Dianhydro-3,4-diacetyl-galactitol (DADAG), an alkylating sugar alcohol derivative, has been shown effective against tumor growth. In this research, we explored the effect of DADAG on angiogenesis in chick chorioallantoic membrane (CAM) model and on the proliferation and migration of human umbilical vein endothelial cells (HUVECs). We also studied the possible mechanism of the anti-angiogenesis effect of DADAG. The results showed that DADAG (100, 500 and 1000 μmol/L) inhibited angiogenesis in CAM model dose-dependently. Sulforhodamine B (SRB) assay indicated that DADAG (45, 90, 135, 180 and 225 μmol/L) suppressed HUVECs proliferation in a dose-dependent and time-dependent manner. High Content Screening (HCS, Cellomics) assay, in which the influence of cell proliferation on migration could be excluded, indicated that DADAG (45, 135 and 225 μmol/L) directly inhibited the motility of HUVECs. Immunofluorescence assay suggested that DADAG inhibited angiogenesis possibly by decreasing vascular endothelial growth factor (VEGF) expression in HUVECs. Our findings reveal that DADAG show anti-angiogenic activity in vivo and in vitro, which is related to the downregulation of VEGF expression in endothelial cells.

Cardioprotective effects of Chinese herbal medicine Braintone on myocardial infarction in rats

Han Zhong, Hong Xin, Yi-Zhun Zhu^*

2010, 19(3):  186-194. 

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Recently, we reported the unique effects of cerebral protection of the Chinese herbal medicine-Braintone (a formulation containing Radix Rhodiola, Folium Ginkgo, Radix Notoginseng and Rhizoma Ligustici Chuanxiong), also known as Remembrance. In the present study, we tested the hypothesis that Braintone may extend cardioprotective effects on ischemic myocardium in Wistar rats. Animal model was created by ligating of left descending coronary artery. Mortality rate and infarct volume were assessed. In addition, capillary density, antioxidant enzymes, apoptosis modulators and VEGF, eNOS mRNA expression level were investigated to reveal the underlying mechanisms. Treatment with Braintone reduced mortality rate from 41.7% to 22.2% associate with notable diminished infarct volume (30.4%±9.0% vs 18.0%±3.0%). Braintone also acted as antioxidant agent for preserving the activities of catalase (13.07±0.48 U vs 9.71±0.44 U in vehicle, P<0.01). Furthermore, Braintone dramatically boosted the expression levels of anti-apoptotic genes Bcl-2 and Bcl-xl (1.43-, 2.30-fold, P<0.01) as compared to vehicle group and significantly down-regulated the expression level of pro-apoptotic gene Bax (0.84-fold, P<0.01) while slightly inhibited Caspase-9 and Caspase-3 signals. Moreover, higher mRNA expression levels of VEGF and eNOS were observed in Braintone group consisting with a remarkable raise of capillary density (46.0±13.3 vs 27.4±12.6, P<0.01) in myocardium. The findings indicated that Braintone markedly attenuate myocardial damage induced by ischemic insults in vivo. Braintone may confer cardioprotection via scavenging free radicals, inhibiting cardiomyocytes apoptosis and promoting angiogenesis in ischemic region.

Limitations of the use of MTT assay for screening in drug discovery

Mei Han^*, Jin-Feng Li, Qi Tan, Yuan-Yuan Sun, Yong-Yan Wang

2010, 19(3):  195-200. 

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The 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay is a routine cell viability assay for cell proliferation and cytotoxicity, which is widely used in many fields, especially in screening for drug discovery. However, this assay exhibits limitations in the presence of particular compounds and under certain assay conditions, which may yield false screening results. For example, polyphenols that are extracted from natural sources can react with MTT in the absence of living cells and thus interfere with the screening results. We measured the absorbance of 15 polyphenols extracted from green tea and showed that the phenolic hydroxyl groups in the polyphenols are responsible for the reduction of MTT to formazan. When three or more phenolic hydroxyl groups were present on a conjugated polyphenol, a significantly increased MTT reduction was observed. Moreover, the type of medium also had an effect on the absorbance value, in the following order: α-MEM + 10% FBS> α-MEM>DMEM/F12>PBS. The absorbance of the MTT assay recorded at 570 nm is more sensitive than that measured at 595 nm. These results will improve the cell-based assay of polyphenols and clarify the limitations of the MTT assay as a method of screening in drug discovery.

Involvement of pro-inflammatory and anti-inflammatory cytokines in the anti-inflammatory activity of Rubus idaeus L. on LPS-treated RAW 264.7 cells

Fei Xiao, Jiang Zhu, Lei Zhao, Guo-Hua Zheng, An-Shu Yang, Jun-Yan Tao^*, Bao-Hui Zhang, Zhi-Jun Huang, Fu-Liang Xiong

2010, 19(3):  201-208. 

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Anti-inflammatory activity of Rubus idaeus L. and possible mechanisms involved were explored in lipopolysaccharide (LPS)-treated RAW 264.7 cells. The effects of ethanol extract of R. idaeus on the levels of pro-inflammatory cytokines, including tumor necrosis factor-alfa (TNF-α), interleukin-6 (IL-6) and interleukin-1 beta (IL-1β), as well as pro-inflammatory mediators, such as nitric oxide (NO), inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) were studied by Sandwich ELISA, real-time PCR, and Western blot analysis. Moreover, the effects of ethanol extract of R. idaeus on anti-inflammatory cytokine interleukin-10 (IL-10) and anti-inflammatory mediator heme oxygenase-1 (HO-1) were also investigated using the same methods. Furthermore, nuclear factor-κB (NF-κB) level was assayed by immunocytochemistry. The results showed that the production of IL-1β, IL-6, NO, TNF-α and COX-2 in LPS-treated cells could be significantly inhibited (P<0.01 or P<0.05) by ethanol extract of R. idaeus compared with that in the cells treated with LPS only. Meanwhile, the production of NF-κB was also inhibited by the extract. Based on these results, the anti-inflammatory activity of R. idaeus was attributed to the down-regulation of IL-6, IL-1β and TNF-α levels as well as gene expression of iNOS and COX-2 through the suppression of NF-κB activation, and induction of anti-inflammatory cytokine IL-10 and anti-inflammatory mediator HO-1.

Quantitative determination of ganoderic acid T in rat plasma by a sensitive
RP-HPLC method and its application in pharmacokinetic studies

Xiang Chen, Shao-Lin Tao, Feng Gao*, Ying-Bo Li, Jian-Jiang Zhong

2010, 19(3):  209-213. 

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A selective and sensitive HPLC method has been developed and validated for the quantification of ganoderic acid T in rat plasma. A reverse-phase column was used with UV detection at 245 nm. The mobile phase consisted of methanol-water-acetic acid (95.5:4.5:0.5, v/v/v) run at a flow rate of 1 mL/min. Testosterone propionate was used as the internal standard. The standard curve was linear over the range of 0.05-50 μg/mL in rat plasma with a linear correlation coefficient greater than 0.999. The lower limit of quantification of this assay was 20 ng/mL. The recoveries of samples at 0.05, 2 and 40 μg/mL were 97.6%, 98.4% and 103.2%, respectively. The relative standard deviations of intra- and inter-day assay variations were less than 8.2%. The usefulness of the assay was confirmed by the successful analysis of plasma samples from a pharmacokinetics study in rats. Following a single dose of ganoderic acid T (5 mg/kg for i.v. or 14 mg/kg for p.o.), the main pharmacokinetic parameters by intravenous injection were: t1/2α: (5.46±1.25) min; t1/2β: (227.18±11.40) min; CL: (1.09±0.16) mL/(kg·min); AUC0–12 h: (3939.13±311.14) μg·min/mL; AUC0–∞: (4681.96±710.70) μg·min/mL and the absolute bioavailability was 41.98%±2.40%. This method is simple, sensitive, and accurate. It is suitable for pharmacokinetic studies of ganoderic acid in rats.

Preparation and evaluation of docetaxel-loaded albumin nanoparticles for intravenous administration

Yi-Bo Wang, Jian-Cheng Wang^*, Meng Meng, Hua Zhang, Qiang Zhang

2010, 19(3):  214-222. 

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Docetaxel (DTX) was incorporated into albumin nanoparticles to form the docetaxel loaded nanoparticles (DTX-NPs) with a high-pressure homogenization method. The purpose of this procedure was to improve the solubility, stability and biocompatibility of DTX. In our study, particle size, zeta potential, size distribution, and encapsulation efficiency were investigated. The crystalloid state of DTX in nanoparticles was further determined by the X-ray diffraction technique. The hemolysis rate, pharmacokinetics and pharmacodynamics of the DTX-NPs were analyzed and compared with the injectable docetaxel solution (DTX-Sol), which was fabricated according to the formulation of the commercial Taxotere^®. It demonstrated that the DTX-NPs were prepared successfully with these properties, including the (193±4) nm size, (–30±1) mV zeta potential and 69%±2% encapsulation efficiency. Higher stability was achieved in the lyophilized nanoparticles compared to that in the nanoparticle suspension. Furthermore, less hemolysis effect was observed in the DTX-NPs than that in the DTX-Sol. The pharmacokinetic and pharmacodynamic behaviors of the DTX-NPs were similar as that of DTX-Sol based on the in vivo experiments. In conclusion, albumin nanoparticles may act as a useful and safe carrier for DTX.

Quantitative analysis of astragaloside IV in traditional Chinese medicine 'Huang-Qi-Si-Wu' Capsules by HPLC/UV

Yan-Li Zhang, Xing-Xin Yang, Xiao-Ni Li^*

2010, 19(3):  223-228. 

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A reliable and accurate HPLC/UV method was developed for the quantitative determination of astragaloside IV in 'Huang-Qi-Si-Wu' Capsules, a widely used prescription of traditional Chinese medicines (TCM). The chromatographic separation conditions employed for HPLC/UV were optimized using a Hypersil-ODS column (250 mm×4.6 mm, 5.0 μm) with isocratic elution. Acetonitrile–water (32:68, v/v) were used as the mobile phase pumped at a flow rate of 1.0 mL/min and a detection wavelength at 203 nm was used. The method was fully validated with respect to linearity, precision, accuracy, specificity and robustness. The validated method was applied successfully to the quantification of astragaloside IV in the extract of 'Huang-Qi-Si-Wu' Capsules from different production batches. The results indicate that the established HPLC/UV method is suitable for the quantitative analysis and quality control of 'Huang-Qi-Si-Wu' Capsules and other related botanical drugs.

Inappropriate use of empirical antibiotics in adults with acute infectious diarrhea in a large teaching hospital

Feng-Qin Hou, Xin-Ting Sun, Gui-Qiang Wang^*

2010, 19(3):  229-234. 

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Overuse of antibiotics for the treatment of acute diarrhea is very common. The aim of the current study was to investigate the inappropriate use of antibiotics in adults with acute infectious diarrhea and to evaluate the association between the use of antibiotics and clinical features. To achieve this aim, we reviewed 4891 patients’ medical records from Apr. 2008 to Oct. 2009. Of the total 4891 cases, 30.5% had clinical features of invasive bacterial diarrhea, 48.1% were prescribed with antibiotics, and 20.3% received inappropriate antibiotic treatment. Of note, 19% involved unnecessary antibiotic prescriptions in non-indicated cases, which accounted for 39.4% of all antibiotics prescribed in the total 4891 patients. There was no significant differences between physicians and medical trainees in the inappropriate use of antibiotics (P = 1.0). Logistic regression analysis demonstrated that except for body temperature, other clinical symptoms including abdominal pain, tenesmus, and faecal WBC count (>10 cells/HPF) were associated with the use of antibiotics. In addition, other clinical indicators including vomiting, stool frequency of 5–10 times/d, mucous stool, and fecal WBC count of 1-10 cells/HPF, which are not normally indicators for prescribing antibiotics, were also associated with the use of antibiotics. This might suggest that these symptoms were mistaken as features of invasive bacterial diarrhea, thus leading to the overuse of antibiotics.

Factors influencing job satisfaction of medical representatives in Pakistan

Mahmood Ahmad, Naveed Akhtar, Muhammad Bin Ibrahim, Ghulam Murtaza^*

2010, 19(3):  235-238. 

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The objective of this extensive study was to analyze the motivational problems of medical representatives (MRs) and to examine the effects of environment, job characteristics and personality variables on job satisfaction. The statistical analysis has revealed that MRs have a variety of different responses for working harder which is strictly required. An interesting job and satisfaction with various aspects of their work especially their position, task area and pay induce them to exert extra efforts. Over all, this study has provided evidence that in order to understand the factors influencing employer's satisfaction, researcher must examine the combined effects of above mentioned factors.