Table of Content

13 March 2014, Volume 23 Issue 3

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Journal of Chinese Pharmaceutical Sciences

2014, 23(3):  141-144. 

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Original articles

Preparation and evaluation of lipid-matrix nanocarrier co-delivery gene and sensibilizer to elevate docetaxel antitumor

Tingting Meng, Jingquan Li, Xianrong Qi

2014, 23(3):  145-152.  DOI: 10.5246/jcps.2014.03.018

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It is a promising treatment strategy to use a nanoparticle-based drug delivery system for cancer patients, which can simultaneously deliver multiple drugs or genes in combination with therapy to induce synergistic effects and suppress drug resistanceto the tumor. In this study, cationic nanostructured lipid carriers (cNLC) for co-loading anionic small-interfering RNAs (siRNA) and chemotherapeutic docetaxel (DTX) were prepared from different cationic lipids based on particle distribution and loading efficiency. In order to increase the cNLC's positive targeting capacity, a novel peptide SP94 was bound to the surface of cNLC (SP94-cNLC). The cNLC showed good efficiency in loading siRNA and DTX. The SP94-cNLC revealed a better cytotoxicity compared with cNLC and Taxotere^®, indicating that SP94 could successfully enhance the internalization capacity of nanoparticles to the liver cancer cells. This new type of cNLC is a potential vehicle when using in co-delivery of chemotherapeuticsand siRNAs. The curcumin (CUR)/DTX co-delivery NLC could load both CUR and DTX in high efficiency and showed a sensibilization to DTX chemotherapy. The sensibilization was more obvious when it was used in the aggressive and resistant cancer cells. This CUR/DTX co-delivery system had good potential in treating cancer cells when chemotherapy drug showed little effect alone.



Development of high-performance liquid chromatography assay for pharmacokinetic analysis of KCNQ/M-channel opener QO58-lysin in rat plasma  

Tianyang Ma, Bochuan Teng, Jinlong Qi, Hailin Zhang, KeWei Wang

2014, 23(3):  153-158.  DOI: 10.5246/jcps.2014.03.019

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A simple, reliable and efficient assay for quantitative analysis of a novel Kv7/KCNQ/M-channel opener QO58-lysin in rat plasma was developed using high-performance liquid chromatography (HPLC) with UV detection. Separation of compound QO58-lysin from plasma was achieved using a reverse-phase C₁₈ column with a mobile phase of 0.2 M ammonium acetate in H₂O–acetonitrile (40:60, v/v) with nitrendipine used as an internal standard (IS). The retention times of QO58-lysin and the IS in rat plasma were 3.8 and 5.4 min, respectively. Calibration curve was linear ranging from 0.1 to 120 μg/mL with correlation coefficient (r²) of 0.9996. The lower limit of quantification was 0.1 μg/mL. Accuracy, precision, recovery as well as stability were all within acceptable criteria according to Food and Drug Administration (FDA) guidelines. This validated assay wassuccessfully applied to determine the pharmacokinetics of QO58-lysin administered intravenously (10 mg/kg) in SD rats. The distribution and elimination half-life of QO58-lysin in plasma was (0.25±0.16) h and (2.15±0.12) h, respectively.



Liquid chromatography electrospray ionization tandem mass spectrometry (LC/ESI-MS/MS) method for quantitative estimation of moxifloxacin in human plasma

Vipul. M. Vaghela, Prajesh Prajapati, Hetal K. Patel

2014, 23(3):  159-164.  DOI: 10.5246/jcps.2014.03.020

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A rapid and sensitive liquid chromatography tandem mass spectrometry (LC-MS/MS) method has been developed and validated for the determination of moxifloxacin (MOXI) in human plasma. After a simple protein precipitation using acetonitrile, the post treatment samples were analysed on a C₁₈ column interfaced with a Triple Quadropole Tandem Mass Spectrometer. Positive electrosprayionization was employed as the ionization source. The mobile phase consisted of 0.1% formic acid–acetonitrile (60:40, v/v). Ciprofloxacin (CIPRO) was used as an internal standard. The analyte and internal standard (CIPRO) were monitored in the multiple reaction monitoring mode (MRM). The mass transition ion-pair has been followed as m/z 402→358.2 for MOXI and 332→288.1 for CIPRO. The method was linear in the concentration range of 25–5000 ng/mL. The lower limit of quantification was 25 ng/mL. The intra- and inter-day precision (relative standard deviation) and accuracy (relative error) values were within 12.4%. Each plasma sample was analyzed within 3 min.



Chemical constituents from the stems of Homalium ceylanicum

Yuan Cao, Lei Liu, Zhiqin Guo, Qiang Guo, Yong Jiang, Xingyun Chai, Pengfei Tu

2014, 23(3):  165-169.  DOI: 10.5246/jcps.2014.03.021

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By means of solvent extraction and repeated chromatography on silica gel, Sephadex LH-20, HPLC, and preparative TLC, the ethanol extract of the stems of Homalium ceylanicum (Flacourtiaceae/Salicaceae sensu lato) was chemically investigated, which led to the isolation of 13 constituents, including five lignans (1–5) and three isocoumarins (6–8). Based on the spectroscopic analysis and comparison of its ¹H NMR and ¹³C NMR data with those in literatures, their structures were identified as (–)-5'-methoxyisolariciresinol 3α-O-β-D-glucopyranoside (1), (+)-lyoniresinol 3α-O-β-D-glucopyranoside (2), (+)-isolarisiresinol 3α-O-β-D-glucopyranoside (3), (–)-isolarisiresinol 3α-O-β-D-glucopyranoside (4), icariside E5 (5), 3-phenylisocoumarin (6), homalicine (7), (–)-dihydrohomalicine (8), friedelin (9), 4-hydroxybenzoic acid (10), catechol (11), methyl-α-arabinofuranoside (12), and uridine (13). All isolates except compounds 6–8 were described from this genus for the first time. Compound 6 was isolated from this species for the first time.



Simultaneous determination of eight flavonoids in Polygonum aviculare L. by RP-HPLC-UV

Qingrong Fu, Shujuan Liu, Hong Wang, Shizhong Chen

2014, 23(3):  170-176.  DOI: 10.5246/jcps.2014.03.022

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A reliable high performance liquid chromatography method was developed for the quality evaluation of Polygonum aviculare L. Eight marker flavonoids were identified and simultaneously quantified, which included myricitrin, hyperoside, galuteolin, avicularin, quercitrin, quercetin, luteolin, and kaempferol. The analysis was performed on an Inertsil ODS-4 column (4.6 mm×150 mm, 5 µm) with gradient elution. The mobile phases were 0.5% aqueous phosphoric acid and acetonitrile. The detection wavelength was 360 nm. The eight marker flavonoids were separated well with good linearity (r²>0.9991), precision, stability and repeatability. The recovery rate was 95.58%–102.65%. Cluster analysis was employed to analyze 28 batches of samples. The result indicated that this method provides an efficient way to perform quality control as well as a scientific rationale for the Geo-authentication of Polygonum aviculare L.



A new furostanol glycoside from Reineckia carnea 

Yanwei Hu, Xuan Wang, Kehui Xie, Guangzhong Tu, Dan Yuan, Hongzheng Fu

2014, 23(3):  177-181.  DOI: 10.5246/jcps.2014.03.023

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Phytochemical investigations of the aerial parts of Reineckia carnea, collected in Yunnan Province of China, were conducted to explore new chemical constituents. A series of chromatographic and spectroscopic procedures were utilized on the aqueous solution after partitioned with ethyl acetate, which resulted in the separation of a new furostanol-type glycoside and four known compounds. The structures of the isolated compounds were elucidated on the basis of spectroscopic techniques (1D and 2D NMR, IR, HRESIMS) as 26-O-β-D-glucopyranosyl-(25S)-5β-furost-20(22)-en-1α,3β,26-triol-1-O-α-L-arabinopyranosyl-(1→2)-[α-L-rhamnopyranos-yl]-3-O-α-L-rhamnopyranoside (1), (1β,3β,16β,22S)-cholest-5-en-1,3,16,22-tetrol-1,16-di-(β-D-glucopyranoside) (2), diosgenin (3), β-sitosterol (4), ecdysterone (5).



Exploration of the mechanisms of Aflatoxin B1 toxicity and the targets of Oltipraz by reverse docking

Yu Zhang, Limei Guo

2014, 23(3):  182-185.  DOI: 10.5246/jcps.2014.03.024

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Aflatoxin B1 toxicity is well known but the mechanism of this toxicity is still unclear. In addition, the target of the anti-aflatoxin chemopreventive drug Oltipraz remains to be identified. In this study, we employed computer aided reverse docking analysis to identify putative targets of Aflatoxin B1 (AFB) and Oltipraz. The results showed that the clinically known toxic effects of AFB are related to this molecule’s strong binding affinity for key proteins involved in cell apoptosis, hormone metabolism,immune suppression, and digestive organ function. In addition, virtual binding assay indicated that Oltipraz neutralizes the toxicity of AFB by inhibiting its biotransformation enzymes. In conclusion, the technique of reverse docking may be used to identify the specific targets of AFB and Oltipraz, and our findings could significantly accelerate the mechanistic studies of the two molecules and provide guidance for the development of anti-AFB drugs.



Study of the interactions between compound S009 and the extracellular loops of CC chemokine receptor 4 by capillary zone electrophoresis

Lu Yang, Pazilaiti Yakufu, Meina Li, Xiaomei Ling, Zhongjie Li, Ying Wang

2014, 23(3):  186-189.  DOI: 10.5246/jcps.2014.03.025

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CC chemokine receptor 4 (CCR4) is a G-protein-coupled receptor which plays a pivotal role in allergic inflammation. In the present study, three extracellular loops (EL1−3) of CCR4 were synthesized, and the interactions between the extracellular loops and compound S009 were investigated using capillary zone electrophoresis (CZE). Both qualitative and quantitative characterizations of the compound-peptide binding were carried out. The experimental data indicated that compound S009 exhibited interactions with EL3, and a binding constant of (12.5±0.19)×10⁴ M^-1 was determined using the Scatchard plot. Our study identified the specific domains of CCR4 that could be targeted by small molecules and provided insights for the discovery of novel CCR4 antagonists. 



Effect of amiodarone on the warfarin in different CYP2C9 and VKORC1 status of 207 inpatients

Yatong Zhang, Zihui Zheng, Xin Liang, Xin Hu, Kexin Li

2014, 23(3):  190-193.  DOI: 10.5246/jcps.2014.03.026

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Warfarin has been used as anticoagulant for the long-term treatment of thromboembolic disease, however, the wide spread use is limited by a wide inter-individual variation in dose requirement. Recent studies have demonstrated that amiodarone may interact with warfarin to potentiate the anticoagulant effects and lead to an elevated international normalized ratio (INR). In addition, genetic variation in the vitamin K epoxide reductase complex subunit 1 (VKORC1) and cytochrome P450 2C9 (CYP2C9) may also affect the dose of warfarin in single or combination therapy. In our study, we aim to examine the effect of amiodarone on the warfarin in different CYP2C9 and VKORC1 status. From September 2008 to November 2009, 207 patients from Beijing, China were enrolled in our study, including 34 patients on combination therapy of amiodarone and warfarin and 173 patients on warfarin therapy. VKORCl and CYP2C9 genotypes were examined using ligation detection reaction (LDR) method. We compared the stable dosage of warfarin and INR between patients on warfarin therapy and patients on warfarin-amiodaronetherapy when they are stratified with VKORC1 or CYP2C9 genotype. We did not observe significant difference in dosage or INR between these two groups. The difference in characteristics between these two groups, the blood collection time after amiodarone administration and the method for monitoring may all contribute to the negative finding. Large studies taking into account of these factors are needed to improve our understanding of the interaction between warfarin and amiodarone, as well as the effect of genotype in such interaction.



Safety and tolerability of isradipine in Phase I trial in Chinese population 

Kongcai Zhu, Wei Xue, Panpan Xie, Aixin Shi, Xin Hu, Yang Li, Min Li, Bei Yan, Jiamin Chi, Fan Dong, Kang Li, Guoying Cao

2014, 23(3):  194-198.  DOI: 10.5246/jcps.2014.03.027

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Hypertension is one of the well-established risk factor for cardiovascular diseases. Calcium channel blockers (CCBs), chemicals that could block voltage-gated calcium channels (VGCCs) in cardiac muscle and blood vessels, has been widely used for the treatment of hypertension. Isradipine, a second-generation CCB with high affinity for voltage-operated calcium channels, has not been marked in China. The purpose of this study was to investigate the efficacy, safety and tolerability of isradipine in a phase I clinical trial including 31 healthy Chinese subjects. All subjects received different doses of isradipine at 2.5, 5.0 and 10.0 mg in single-dose study. When the test is completed, subjects treated with 5.0 mg isradipine stayed at the research center for multiple-dose study (5.0 mg isradipine twice daily for 9 d). Systolic blood pressure (SBP) and diastolic blood pressure (DBP) were measured pre-dose and post-dose (1, 2, 4, 6, 8, 12, 24, 36 and 48 h after isradipine treatment). Electrocardiography (ECG) and peripheral edema were monitored pre-dose and 4, 8, 24 and 48 h after isradipine treatment. SBP and DBP in single-dose study decreased after isradipine treatment. SBP reached the lowest values 8 h after dosing with a decrease of (7.0±9.7) mmHg (5.4%, P = 0.111) in 2.5 mg group, (7.0±6.9) mmHg (6.0%, P = 0.008) in 5.0 mg group, and (14.0±10.5) mmHg (12.7%, P = 0.005) for 10.0 mg group respectively. Similarly, DBP also reached the lowest values 8 h after dosing with a decrease of (10.0±7.9) mmHg (12.8%, P = 0.004) in 2.5 mg group, (6.0±7.0) mmHg (8.6%, P = 0.003) in 5.0 mg group, and (11.0±4.1) mmHg (15.1%, P = 0.000) in 10.0 mg group respectively. No significant changes of SBP and DBP were observed in multiple-dose study. We detected mild adverse events (AEs), such as increased transaminase and headache that resolved rapidly and spontaneously without intervention. No serious or potentially life-threatening AE was detected. Our results indicate that isradipin has a good safety and tolerability in Chinese healthy subjects. Long-term study with larger sample size is needed to confirm our conclusion.



Special subject

Raise the international status of Journal of Chinese Pharmaceutical Sciences under “the International Influence of Chinese Science and Technology Journals Promotion Plan”

Heqing Huang, Jingjing Zhang, Jian Han

2014, 23(3):  199-203.  DOI: 10.5246/jcps.2014.03.028

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Journal of Chinese Pharmaceutical Sciences (JCPS) has been published for 22 years. During this period,JCPS has progressed from a quarterly journal to monthly publication. Moreover, the qualities of manuscripts and editing are improving, and its influence and international status reaches a high level. Under “the International Influence of Chinese Science and Technology Journals Promotion Plan”, the development and internationalization of JCPS will be further promoted.



Editor profile

Lihe Zhang, travels on the pharmaceutical road

Donghong Fu, Huiyuan Wu, Shuxiang song

2014, 23(3):  204-209. 

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Professor Lihe Zhang, Academician of the Chinese Academy, is the founder and research leader on nucleosides and nucleotides, and also a worldwide famous pharmaceutical chemist. Firstly, he served at School of Pharmaceutical Sciences, Peking University Health Science Center as Assistant and Lecturer. From 1981 to 1983, he worked as Research Associate in Department of Chemistry, University of Virginia, USA. Since 1985 he has become a professor and then was designated as Dean of School of Pharmaceutical Sciences, Director of Chemistry Department, National Natural Science Foundation of China, and Director of State Key Laboratory of Natural and Biomimetic Drugs, Peking University. 
      His research interests include Cyclic ADP-ribose (cADPR), a metabolite of NAD+, which is a signaling molecule to regulate calcium mobilization via ryanodine receptors (RyR) from intracellular stores in a wide variety of biological systems. A main approach to explore the molecular mechanism of calcium release is to investigate the relationship of the structure of cADPR and cADPR analogues with their respective biological activities. In addition to the structure activity relationship, such studies result in novel antagonists and agonists which serve as the tools for mechanistic studies in the complex cellular system or potential drug lead. This publication list contains more than 200 original research articles and review papers. For his outstanding works, a serial prizes was awarded to him, such as: National Natural Science Award, Second Prize, Ministry of Science and Technology, China; Millennium Pharmaceutical Scientist Award, FIP, San Francisco, USA; Nagai-Hisamitsu  Outstanding Science Award, Asia Pharmaceutical Association, Kyoto, Japan and so on.



Others

Academician Lihe Zhang and Professor Demin Zhou are invited to serve as Associate Editor-in-Chief of Eur. J. Med. Chem. and member of Editorial Board of J. Med. Chem., respectively

Journal of Chinese Pharmaceutical Sciences

2014, 23(3):  210-210. 

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Academician Lihe Zhang, Editor-in-chief of Journal of Chinese Pharmaceutical Sciences (JCPS), has been invited to serve as Associate Editor-in-Chief ofEuropean Journal of Medicinal Chemistry (Eur. J. Med. Chem.), which was founded in 1996, isan authoritative international pharmaceutical journal, and it reports all frontiers of pharmaceutical chemistry. This is the first Chinese scientist to receive such an honor.This appointment not only reflects the achievements of Academician Lihe Zhang inmedicinal chemistry researches, but also shows the increasing importance of drug researches in China.

In the mean time, Professor Demin Zhou, the Executive Editor-in-Chief of JCPS, has been invited to serve as a member of the EditorialBoard ofJournal of Medicinal Chemistry(J. Med. Chem.). Itis anauthoritative medicinal chemistry journal published by American Chemistry Society (ACS), and Professor Demin Zhou is the first member of Editor-in-Chief from Peking University.

The appointments of Academician Lihe Zhang and Professor Demin Zhou as the member of Editor-in-Chief of authoritativemedicinal chemistry journals will enhance the influence of manuscripts in pharmaceutical sciences from Peking University. It also provides a real-time interaction platform for the advancement of medicinal chemistryand related researches in our university. 



Professor Xinshan Ye is invited to serve as Co-Editor-in-Chief of Current Topics in Medicinal Chemistry

Journal of Chinese Pharmaceutical Sciences

2014, 23(3):  210-210. 

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Professor Xinshan Ye, the Associate Editor-in-Chief of Journal of Chinese Pharmaceutical Sciences (JCPS), has been invited to serve as the Co-Editor-in-Chief ofCurrent Topics in Medicinal Chemistry. Current Topics in Medicinal Chemistry, which was founded in 1996 and published by Bentham Science Publishing Group, is specialized in the reporting of reviews on recentprogresses in medicinal chemistry. Professor Xinshan Ye is the first Asian scientist to receive such an honor. It shows the attention by the international pharmaceutical community on the advancement of Chinese medicinal chemistry research. At the same time, Professor Xinshan Yehas also been invited to serve as an advisor ofChem Med Chem, which is another important academic journal in the medicinal chemistry field.