Table of Content

    29 March 2015, Volume 24 Issue 3
    Advances of bacterial transferase MraY and its inhibitors
    Yuanyuan Jin, Juanjuan Liu, Xiaozhou Feng, Yadong Li, Wan Sun, Kangyou Wang, Xifeng Tian, Zhaoyong Yang
    2015, 24(3):  137-147.  DOI: 10.5246/jcps.2015.03.017
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    The phospho-murNAc-pentapeptide translocase (MraY, translocase I) is a good target for the development of new antibiotics as it is ubiquitous and essential for bacterial growth. Furthermore, several inhibitors targeting towards this enzyme have been discovered. Recently, the crystal structure of MraY has been presented by Chung et al. Combination of the crystal structure and structure-activity relationship studies on these inhibitors could lead to the identification of active pharmacophores, and insight into their mechanisms of action. In this review, we described the structure and inhibitors of MraY. In addition, we also discussed the structure-activity relationship of these inhibitors and prospects of MraY as an antibacterial target.

    Original articles
    Stability, cytotoxicity, and saturation effect of the free radical-scavenging cinnamic acid-dopamine hybrid antioxidants
    Fenfen Yin, Zhengrong Wu, Lifang Zheng, Hongyu Li, Beining Chen
    2015, 24(3):  148-155.  DOI: 10.5246/jcps.2015.03.018
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    Hybrid antioxidants cinnamoyldopamine (2a), p-coumaroyldopamine (2b), caffeoyldopamine (2c), feruloyldopamine (2d) and sinapoyldopamine (2e) were synthesized by conjugation of dopamine (DA) and hydroxycinnamic acids (HCAs). The stabilities were studied in buffers at pH 1.3, pH 5.0, and pH 7.4 including the human plasma. All the compounds were found highly stable at acidic pH, but underwent hydrolysis at neutral pH. Furthermore, the hydrolysis proceeded much faster in plasma in the following order as indicated by half-life values (t1/2), 2c (1.21 h)<2e (1.52 h)<2d (1.85 h)<2b (3.38 h)<2a (3.88 h), correlating with the number of electron-donating groups. It has been proven by UV spectrum that 2c, 2d, and 2e displayed red shift of more than 50 nm as compared to 2a and 2b, because of the presence of OH and OCH3 groups. In addition, the compounds (2be) showed no cytotoxicity on normal HUVEC cells as DA, although 2a displayed a 16% inhibition of proliferation at 40 μM following 48 h incubation. Their free radical-scavenging activities were evaluated using ABTS•+ and superoxide anion assays and the mechanisms were proposed. It was found that they all exhibited higher activities than trolox, a recognized antioxidant. Amazingly, in the case of the hybrids (2ae), their activity was higher than that of HCAs while lower or comparable to that of DA, suggesting that there may be a “saturation effect” with the hybrid molecules in the antioxidant activities.

    Interaction study between Ocimum sanctum and Glimepiride (sulfonylurea derivative) in diabetic rats
    Mohd Fasih Ahmad, Raj K. Keservani, D J Mani Babu
    2015, 24(3):  156-163.  DOI: 10.5246/jcps.2015.03.019
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    The present study was intended to discover the interaction between Ocimum sanctum (O. sanctum) and Glimepiride, a sulfonylurea derivative used in the treatment of type-2 diabetes, in diabetic rats to suggest an alteration in the dose of Glimepiride in case of hypoglycaemia. LD50 studies for the aqueous extract of O. sanctum leaf were carried out in albino mice up to the dose level of 2000 mg/kg. O. sanctum atlow, medium and high doses (100, 200 and 400 mg/kg, per oral), respectively and Glimepiride ½ (half) therapeutic dose, therapeutic dose and 2 time therapeutic dose (0.036, 0.072 and 0.144 mg/200 g, per oral) were selected. After the treatment with O. sanctum and Glimepiride as single doses and in various combinations of these two drugs in streptozotocin-induced diabetic rats serum glucose levels in all the groups were analysed by the glucose oxidase-peroxidasemethod. When administered alone as single doses both aqueous extract of O. sanctum leaf and Glimepiride produced a significant anti-diabetic effect in diabetic rats. The anti-diabetic effect observed with combination of aqueous extract of O. sanctum leaf and Glimepiride was significant and more when compared to either of the drugs given alone. There was a definite interaction that necessitates dose readjustment of Glimepiride and further glucose levels are to be frequently monitored to avoid complication of hypoglycemic condition with aqueous extract of O. sanctum leaf and Glimepiride combination.

    Effect of 5-HMF on protection of hydrogen peroxide-induced injury in human umbilical vein endothelial cells
    Yafen Shen, Xin Wu, Gang Cao, Hao Cai
    2015, 24(3):  164-168.  DOI: 10.5246/jcps.2015.03.020
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    The protective effect of 5-hydroxymethylfurfural (5-HMF) against hydrogen peroxide (H2O2)-induced injured in human umbilical vein endothelial cells (HUVECs) was examined. Treatment of HUVECs with 5-HMF significantly increased their viability, decreased cell apoptosis induced by H2O2, accompanied by the decreased nitric oxide level. Western blotting analysis demonstrated that Bcl-2 expression was increased whereas Caspase-3 and NF-κB expression was decreased in 5-HMF groups. In conclusion, the results showed that 5-HMF could prevent endothelial dysfunction and related complications caused by oxidative stress.

    Triterpenoids from the stems of Uncaria macrophylla
    Yuding Wei, LianheYan, Hong Liang, Meixiao Zhu, Duanlu Ye, Qingying Zhang
    2015, 24(3):  169-176.  DOI: 10.5246/jcps.2015.03.021
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    Nineteen triterpenoids, including eleven ursane triterpenoids and eight olenane triterpenoids, were isolated from the stems of Uncaria macrophylla Wall. by comprehensive chromatographic methods. Structure elucidation of the compounds was succeeded by extensive spectroscopic analysis. Twelve compounds were obtained from this plant for the first time, among which six compounds were obtained from the genus Uncaria for the first time.

    An improved calibrated normalized resolution product (r*') and the application in HPLC fingerprints of soy isoflavone extract
    Weiyang Shen, Juan Bian, Feiye Liu, Shuifang Peng
    2015, 24(3):  177-184.  DOI: 10.5246/jcps.2015.03.022
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    In this paper, we proposed a novel resolution criterion (improved calibrated normalized resolution product, r*') to evaluate separation quality of fingerprints. By comparing with the calibrated normalized resolution product (r*) and the hierarchical chromatographic response function (HCRF), the validity of this criterion was demonstrated by experimental chromatograms. The soy isoflavone extract was selected as the analytical object. The initial and end percentages of methanol and elution time affectinggradient elution were tested by orthogonal design. The final optimized conditions were as follows. It was detected by UV absorbance at 254 nm, column temperature was maintained at 36 ºC, solvent A was 0.1% (v/v) acetic acid, solvent B was methanol, gradient elution was from 34% to 65% B in a linear gradient in 25 min, and the flow-rate was set at 1.0 mL/min. In addition, the main ingredients of the soy isoflavone extract were confirmed by LC-ESI/MS.

    Impact of GMP on pharmaceutical industry in China based on indicator system evaluation
    Zhe Chen, Menglu Qi, Guoqing Ye, Haopeng Qu, Bin Jiang
    2015, 24(3):  185-191.  DOI: 10.5246/jcps.2015.03.023
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    To evaluate the impact of GMP on Chinese pharmaceutical industry in a quantitative system, we referred to theories on policy evaluation and industrial organization, and conducted literature review, key person interview, multi­round Delphi and field investigation. We set up the principles to construct our indicator system, reviewed based on the policy objectives of the new GMP for drugs systematically, and analysed the influence path of the new GMP for pharmaceutical manufacturers. We proposed a three-dimensional “structure­conduct­performance” evaluation indicator system. Our evaluation indicator system is accepted by experts and relevant personnel, indicating the three-dimensional evaluation indicator system is feasible to evaluate the impact of the new GMP in Chinese pharmaceutical industry.

    Case report
    Atrial fibrillation associated with tiotropium in patients with pre-existing arrhythmia: a case report
    Yanhong Wei, Liping Yang, Yatong Zhang, Hong Shao
    2015, 24(3):  192-194.  DOI: 10.5246/jcps.2015.03.024
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    Inhaled anticholinergic agent tiotropium is widely used in the treatment of chronic obstructive pulmonary disease (COPD). However, it has pro-arrhythmic and pro-ischaemic effects, which can potentially increase the risk of serious cardiovascularevents, especially in patients with pre-existing arrhythmias. We presented a 79-year-old man with a medical history of arrhythmia, who developed atrial fibrillation after used tiotropium 18 μg daily for two weeks. We urge the caution of pro-arrhythmic effect of tiotropium. Healthcare professionals should be aware of the potential effect when prescribing tiotropium to patients with known cardiac rhythm disorders.

    Short communication
    Higher pharmaceutical education in China: evolution, current status and prospects
    Xiaoyuan Xu, Kaili Zhang, Wenbing Yao
    2015, 24(3):  195-199.  DOI: 10.5246/jcps.2015.03.025
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    Higher pharmaceutical education in China has developed for more than 100 years. More and more talented pharmacy professionals are required due to the rapid development of pharmaceutical industry and patients’ needs, leading to many challenges for the current higher pharmaceutical education system. This paper provided a retrospective review of the evolution of higher pharmaceutical education in China, which described its current status and future prospects of higher pharmaceutical education in China, and offered some suggestions on these challenges.

    Special subject
    The international impact of Chinese academic journals revealed by the "Annual Report for International Citation of Chinese Academic Journals"
    Heqing Huang, Jian Han, Jingjing Zhang
    2015, 24(3):  200-204.  DOI: 10.5246/jcps.2015.03.026
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    CNKI has published the “Annual Report for International Citation of Chinese Academic Journals” since 2012. In the past three years, it has provided comprehensive data on the international impact of Chinese academic journals. Using the clout index (CI) to rank the Chinese academic journals, “the Highest International Impact Academic Journals of China” and “ the Excellent International Impact Academic Journals of China” are announced every year. By introducing the rating criteria of the “Annual Report for International Citation of Chinese Academic Journals”, the characteristics of high impact journals are discussed. Especially, the status of the pharmaceutical journals is discussed. We found that there are increasing numbers of Chinese journals that are included in the SCI, and some of them are high impact journals. However, journals published in Chinese are still facing difficulties to be included in SCI, even though they show higher impact than journals published in other non-English languages. The Chinese Pharmaceutical journals need to enhance their international impact, but Journals on Chinese Medicine show high impact.