Table of Content

Volume 16 Issue 4
26 April 2011

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Inhibitory effect of ginsenoside Rg1 on BGC-823 human gastric cancer cell line

ZHAO Bao-sheng, LIU Yang, XU Tun-hai

2011, 16(4):  361-365. 

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AIM: To observe the influences of Ginsenoside Rg1 on the activity, proliferation, the expression of Bax-2 and caspase-3 and morphology of BGC-823 gastric cancer cell line, and investigate its pharmacological mechanisms. METHODS: Cells which were stayed in logarithmic growth were used for the experiments, the cells were interfered with different concentration of Ginsenoside Rg1, the methods of growth curve, M'IT assay, protein content assay Real-time PCR and morphological observation were used to investigate the effects of Ginsenoside Rg1 on BGC-823 cells. RESULTS: Ginsenoside Rg1 had potent inhibitory effect on BGC-823 cell line in a dose-dependent and time-dependent manner. Ginsenoside Rg1 had significant cytotoxic effect to BGC-823 cells, and its half maximal inhibitory concentration (IC₅₀) is 29.56 mg/L. Ginsenoside Rg1 decreased the amount of protein in BGC-823 cells, improved the expression of Bax-2、caspase-3, and caused the shrinkage of cells, the cytoplasm decreased, and the color was salmon pink; the chromatin condensed and the color was intense violet; the cellular nucleuses were condensed or broken into round granules. CONCLUSION: Ginsenoside Rg1 obviously inhibited the cell proliferation, decreased its activity, showed conspicuous anti-tumor effect on BGC-823 cells. The anti-tumor effect may be related to the inhibition effect to tumor cell protein synthesis, and promote the apoptosis of BGC-823 cells.

Protective effect of qiye xinkang capsule on cerebral ischemia-reperfusion injury in rats

SU Mei, CUI Tao, YANG He-jin, YANG Hong-bo, ZHAO Chun-mei, BAO Guang-lei, WANG Zuo-xiang

2011, 16(4):  366-370. 

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AIM: To study the influence of qiye xinkang capsule (QXC) on the cerebral ischemia-reperfusion injury in rats. METHODS: Aften the model of cerebral ischemia-reperfusion injury in rats was simulated successfully by string occlusion, protective effect of QXC on cerebral ischemia-reperfusion injury was evaluated by neurofunctional score, red tetrazoline (TTC) and weighing method.The mechanism was investigated by determining the activity of superoxide dismutase (SOD), glutathione peroxidase (GSH-Px), nitric oxide (NO) and malondialdehyde (MDA) from rat hippocampus homogenate. RESULTS: The rats replicated successfully were orally administered with QXC for four times: 1 h for the first time, 12 h for the second time, 24 h for the third time and 36 h for the forth time.The neurological deficit and brain infarction area resulted from cerebral ischemia in rats were improved significantly,meanwhile the water content and content of MDA and NO were decreased significantly and the activity of SOD and GSH-Px was increased significantly in the tissue of cerebral ischemia in dose of 271.3 and 135.6 mg/kg. CONCLUSION: QXC had notable protective effect on cerebral inchemia-reperfusion injury in rats, which might be related with inhabiting the lipid peroxidation of the brain tissue and reducing the generate of the NO.

Empirical study of total flavonoids of selaginella moellendorfii hieron on hepatic fibrosis rat

WANG Fu-gen,ZHUANG Rang-xiao,FANG Hong-ying,ZHANG Yi-qi,XI Jian-jun

2011, 16(4):  371-373. 

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AIM: To explore the protective effect of Selaginella moellendorfii Hieron on experimental hepatic fbrosis rat. METHODS: Hepatic fibrosis model was made by subcutaneous injection 50% carbon tetrachloride (CCl₄) for 8 weeks,and then were intragastric administered with total flavonoids of Selaginella moellendorfii Hieron suspension(15,30,60 mg/kg),silybin was experimental control group.All rats were killed after 8 weeks,the score of hepatic fibrosis and the index in liver tissue and serum were evaluated. RESULTS: The result showed that the hepatic fibrosis was in III-IV stage. Compared with the model group,total flavonoids of Selaginella moellendorfii Hieron could significantly decrease the levels of ALT,AST in serum,and the MDA in liver tissue,and increase the level of SOD.The pathomorphology of hepatic fibrosis rat was improved. CONCLUSION: Total flavonoids of Selaginella moellendorfii Hieron have a better protective effect on rat hepatic fibrosis induced by CCl₄.

High glucose-induced apoptosis of H9c2 cells is closely related to GAPDH nuclear translocation

SUN Chuan-bo,GAO Jing-hong, HU Liang, ZHANG Jing-wen, WEI Li, LI Qing-ping

2011, 16(4):  374-379. 

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AIM: To investigate whether high glucose induces GAPDH nuclear translocation and whether the GAPDH nuclear translocation is related to high glucose-induced apoptosis of H9c2 cells. METHODS: H9c2 cells were cultured for 48 h in high glucose condition, and then cells were collected for apoptosis determination. The generation of reactive oxygen species (ROS) was determined. The expression of GAPDH and iNOS was measured by western blotting. The translocation of GAPDH was determined by immunofluorescence. RESULTS: High glucose induced apoptosis of H9c2 cells. High glucose induced oxidative stress in H9c2 cells and translocation of GAPDH to nucleus. Rotenone and iNOS inhibitor 1400W protected H9c2 cells from death by inhibiting GAPDH translocation to nucleus. CONCLUSION: High glucose induces GAPDH translocation from cytoplasm to nucleus. The inhibition of high glucose-induced apoptosis of H9c2 cells is closely related to GAPDH nuclear translocation.

Spinal cord deformity effect of cyclophosphamide on fetal

HU Wen-juan, DENG Xiao-hua, JIN Hui, WU Jian-hui, LIU Xiang-yun, SUN Zu-yue

2011, 16(4):  380-384. 

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AIM: To observe the apoptotic cells of fetal spinal cord and define apoptosis of spinal cord by cyclophosphamide and make initial investigation in mechanism. METHODS: During the embryo-fetal development toxicity test, the CP experimental group was injected with CP 7.2 mg/kg and 9.0 mg/kg in the morning of day 10 of gestation;dissected pregnant rats on the day 20 of gestation for fetal spinal cord which were made HE staining and immunohistochemistry. RESULTS: A great quantity of apoptosis cells were observed in experimental group. Compared with negative control physiologic saline group, Bax expression in thoracic cord and isthmus cord anterior horn cell of low-dose CP group increased significantly (P<0.01), and Bcl-2 expression in thoracic cord and isthmus cord anterior horn cell of low-dose CP group are lower (P<0.05). CONCLUSION: These findings suggested that rats injected with CP 7.2 mg/kg in the morning of day 10 of gestation which can aggravate the apoptosis of fetuses' spinal nerves.

Methodology establishment for determination the effective components in quan tianma capsule by liquid chromatography-electrospray ionization mass spectrometry and its application

BAI Qiu-xiang

2011, 16(4):  385-388. 

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AIM: To establish a liquid chromatography-electrospray ionization mass spectrometry (LC-ESI-MS) method for determination the effective components in Quan Tianma capsule. METHODS: A Kromasil C₁₈ column (150 mm×2.00 mm, 3.5 μm) was used as the analytical column,while a mixture of acetonitrile and ammonium chloride solution was used as the mobile phase.The molecules [M+Cl] - at m/z 321 was used, and the injection volume was 10 μL. RESULTS: There was a good linear relationship in the range of 0.05- 2.00 μg/mL for gastrodin (r=0.9990) , the average recovery rate was 97.76%(RSD was 1.44%). CONCLUSION: The method is accurate, convenient, and can be used for the quantitative analysis of Tianma capsule. Mass spectrogram technology will be used for the effective components identification and quality control of the commonly used drugs in clinic.

Perifosine inhibits growth of rapamycin resistant cells through activating GSK3β

DONG Guang-hui, LUO Xuan, ZHAI Su-lan, LI Ping, WANG Xue-rong

2011, 16(4):  389-392. 

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AIM: To investigate the effects and mechanisms of perifosine on the growth of rapamcyin resistant NSCLC cells. METHODS: The growth inhibitory effects of perfisoine with or without LiCl on NSCLC cells were detected by SRB assay. The regulatory effects of perifosine on Akt, GSK3β singaling were detected by Western blotting. RESULTS: Perifosine had similar inhibitory effects on the growth of rapamycin resistant and sensitive cells. Perifosine inhibited phosphorylation of GSK3β without significant alteration of Akt phosphorylation, and thus activated GSK3β in rapamycin resistant cells. The inhibitor of GSK3β- LiCl blocked perifosine's inhibitory effects on the growth of rapamycin resistant cells. CONCLUSION: Perifosine inhibits growth of rapamycin resistant NSCLC cells through activating GSK3β.

Pharmacokinetics of compound olmesartan medoxomil and hydrochlorothiazide tablets in Chinese healthy volunteers

WAN Qian, HUANG Yuan-yuan, FU Zhi-min, TAN Hong-yi, PEI Qi HUANG Zhi-jun, YANG Guo-ping

2011, 16(4):  393-399. 

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AIM: To study the pharmacokinetics of compound olmesartan medoxomil and hydrochlorothiazide tablets after multiple oral dose administration in Chinese healthy volunteers. METHODS: In a randomized, open, single-center study, 12 Chinese healthy volunteers were randomized to administer a single dose of compound olmesartan medoxomil and hydrochlorothiazide tablets (20 mg/12.5 mg) on day 1 and day 3 to day 9. The concentration in human plasma was determined by LC-MS/MS method and its pharmacokinetic parameters were calculated and analysed by DAS 2.0 and SPSS 13.0. RESULTS: The main pharmacokinetic parameters of olmesartan medoxomil after a single dose and multiple-dose were as follows: C_max were (489±122) μg/L and (531±125) μg/L; AUC_0→t were (3468±869 ) μg·L^-1·h and (3557±1209) μg·L^-1·h; t_max were (2.6±0.5) h and (2.3±0.8) h; t_1/2 were (7.3±4.0) h and (8.3±3.6) h, respectively. The main pharmacokinetic parameters of hydrochlorothiazide after a single dose and multiple-dose were as follows: C_max were (122±34) μg /L and (182±38) μg /L; AUC_0→t were (764±211) μg·L^-1·h and (1079±361 ) μg ·L^-1·h; t_max were (2.2±0.7) h and (1.6±0.6) h; t_1/2 were (6.8±2.3) h and (7.1±1.6) h, respectively. CONCLUSION: There is no significant difference in pharmacokinetic parameters of compound Olmesartan medoxomil and hydrochlorothiazide tablets (20 mg/12.5 mg) between single and multiple administration,no accumulation after administration.

LC-MS/MS determination of flunarizine in human plasma and application in bioequivalence evaluation

CHEN Yao, TAN Zhi-rong, WANG Yi-cheng, LI Hui, LI Ling, DENG Xiao-lan, ZHANG Wei, ZHOU Hong-hao

2011, 16(4):  400-406. 

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AIM: To establish a LC-MS/MS method for determination of flunarizine in human plasma, and to study the relative bioequivalence of flunarizine hydrochloride made by Yangtze River Pharmaceutical Group Co., Ltd. METHODS: Thermo Hypurity C₁₈ column (150 mm×2.1 mm, 5 μm) was used in the experiment.Acetonitrile-10 mmol/L ammonium formate (including 0.1% formic acid) (65∶35, V/V) was used as mobile phase and the flow rate was 0.3 mL/min and the injection volume was 10 μL.The column temperature was set at 40 ℃,the sample room temperature was set at 15℃.A single oral dose of 20 mg flunarizine hydrochloride and its contrastive drug were given to 18 healthy volunteers in an open randomized two way crossover design.The plasma concentrations were determined by LC-MS/MS method at the different time points. RESULTS: Flunarizine was linear in the range of 0.38-196 ng/mL, the limitation of detection for flunarizine was 0.1 ng/mL,the method was high sensitivity, stability and specificity. The main pharmacokinetic parameters of flunarizine were as follows: C_max was (86±36) and (82±34 )ng/mL;t_max was 2.5 h(1-3 h) and 3 h(2-5 h);AUC_0-24 was (725±338) and (709±320) ng·mL^-1·h;AUC_0-∞ was (811±375) and (780±330) ng·mL^-1·h.The reference drug and the test drug of flunarizine are bioequivalent. CONCLUSION: The method is simple, accurate and repetitive for the determination of flunarizine in human plasma and successfully applied to the bioequivalence evaluation of flunarizine hydrochloride in human.

Effect of Modified Xiaoyao pill on the activity of CYP2C19

ZHAO Gang-tao, YANG Fan, Xu Qian, DING Yuan-yuan,Zheng Fei, XU Jing-feng

2011, 16(4):  407-411. 

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AIM: To investigate the effect of Modified Xiaoyao pill on CYP2C19, and provide foundation for clinical drug using. METHODS: Twenty volunteers were divided into two groups according to CYP2C19^*2 gene type, ten for WW gene type and ten for MM gene type. Omeprazole used as probe drug of CYP2C19, the effect of Modified Xiaoyao pill on the activity of CYP2C19 were investigated. Genetic classification was fulfilled by pyrosequencing method, and the blood concentration of probe drug and its metabolic product were determined by HPLC-MS/MS. RESULTS: The volunteers took Modified Xiaoyao pill for two weeks, AUC_0-12 was used as the standard of the activity of CYP2C19. The activity value was 5.7±1.6 before drug and 6.0±1.7 after drug using. So the activity of CYP2C19 was increased after drug using, t-test was used for comparison, there was no remarkable difference between the data. CONCLUSION: Modified Xiaoyao pill has no obvious affection on the activity of CYP2C19.

Phase Ⅰ clinical tolerability trial of (S)-ornidazole tablets

XIE An-yun, CHENG Ze-neng, OU-YANG Dong-sheng, GUO Xin, HUANG Zhi-jun, ZHANG Gui-xiang, LIU Chang,TAN Hong-yi,YANG Li, YANG Guo-ping

2011, 16(4):  412-416. 

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AIM: To evaluate the tolerability of (S)-ornidazole in healthy volunteers. METHODS: It is a randomized, blinded, placebo-controlled single-center clinical study. Fowrty-eight healthy volunteers enrolled the study. Thirty-eight healthy volunteers were randomly divided into four groups to attend single-dose tolerability trial (250, 500, 1000, 1500 mg, respectively). Ten healthy volunteers entered multi-dose tolerability trial for 7 days [1000 mg (S)-ornidazole, Qd]. Two healthy volunteers of each group were given placebo.Vital signs, electrocardiogram and serum biochemical indicators were observed before and after (S)-ornidazole administration and adverse effects were recorded. RESULTS: In the study, there were no abnormal findings in vital signs, electrocardiogram and serum biochemical indicators.20 healthy volunteers experienced mild adverse effects of dizziness, fatigue, drowsiness nausea and so on. CONCLUSION: (S)-ornidazole tablet is safe for healthy volunteers at daily dose of 250 to 1000 mg

Usage of equivalent numerical method based on entropy weight in evaluating comprehensively the promoting effect of transdermal enhancers

LI Zhi-ping, LIN Yan-qiong,WANG Hui, LIANG Qing

2011, 16(4):  417-422. 

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AIM: To investigate the use of equivalent numerical method based on entropy weight in evaluating comprehensively the promoting effect of transdermal enhancers. METHODS: Using paracetamol as model drug, the promoting effects of azone, menthol, camphor, oleic acid, clove oil, nepeta oil, patchouli oil were detected by transdermal absorption experimentation in rabbit skin in vitro, indexes such as cumulative permeation quantity, penetrating rates, enhancement ratio and lag time were calculated, finally the equivalent numerical method based on entropy weight was used to evaluate the promoting effects of those transdermal enhancers. RESULTS: The promoting effect of 2% camphor and 2% cloves promoted paracetamol was best, 1% Azone, 2% nepeta oil, 2% menthol, 2% oleic acid in sequence,2% patchouli oil was worst. CONCLUSION: The equivalent numerical method based on entropy weight could evaluate the promoting effect of transdermal enhancers objectively and fairly.

Control study of Sulpiride and Olanzapine in the treatment of anorexia nervosa

ZHONG Zhi-yong,WU Xiao-li ,CHEN Min-feng,ZHANG Jin-bei

2011, 16(4):  423-426. 

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AIM: To compare the difference of effect and side effects of Sulpiride with Paroxetine and Olanzapine with Paroxetine in the treatment of anorexia nervosa. METHODS: 57 anorexia vervosa patients were involved in the research, including 25 cases of Sulpiride group,32 cases of Olanzapine group, before and after the treatment, body weight, body mass index (BMI), Hamilton anxiety scale (HAMA), Hamilton depression rating scale (HAMD) and Treatment emergent side-effect scale (TESS) were used to evaluate the curative effect and the adverse drug reactions. RESULTS: After 8 weeks treatment ,the indexes of body weight, BMI, HAMA,HAMD were obviously better than those of before treatment (P<0.05). The indexes of body weight and BMI of Olanzapine group were better than those in Sulpiride group after 8 weeks treatment (P<0.05), but there were no difference of HAMA,HAMD and TESS between two groups(P>0.05) . CONCLUSION: After analysis of the indexes as body weight, BMI, HAMA, HAMD and TESS, the following conclusions are made: the two methods are both effective to the treatment of anorexia noversa, but the Olanzapine with Paroxetine is better than Sulpiride with Paroxetine in improving the body weight and the BMI. The difference of the adverse drug reactions is not found in the two groups.

Effects of dexmedetomidine on severity of emergence pain and agitation in children undergoing adenoidectomy

JIANG Zong-ming, ZHONG Jun-feng, CHEN Zhong-hua

2011, 16(4):  427-431. 

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AIM: To observe the effects of dexmedetomidine on severity of emergence pain and agitation in children undergoing adenoidectomy. METHODS: 88 patients scheduled for adenoidectomy, ages 4 to 12 years, were enrolled and randomly allocated into control group(n=44, group C) and dexmedetomidine group(n=44, group D).Group C were received intravenous fentanyl bolus 2 g/kg after anesthesia induction with sevoflurane ,whereas in group D were received intravenous dexmedetomidine bolus 1 g/kg over 10 minutes , followed by 0.5 g·kg^-1·h. Fentanyl bolus 1 g/kg was administered to patients in both groups in the presence of an increase in heart rate or systolic blood pressure 30% above precision values that continued for 3 minutes. Pain severity was evaluated and recorded in the postanesthesia care unit on arrival, at 5 minutes ,at 15minutes ,then every 15 minutes for 90 minutes. Emergence agitation was assessed using scale exclusive for child. Fentanyl bolus 0.5 g/kg was given for pain(score above 4) or severe agitation lasting for more than 3 minutes. RESULTS: Atropine and ephedrine were not used in both groups in an attempt to control bradycardia and hypotension. As for heart rate , there was lower rate in group D than that in group C, but no statistical significance was observed in systolic blood pressure between two groups. Time of spontaneous awake and endotracheal extubation were significantly shorter than those in group C(P<0.05,P<0.01). The amount of salvage fentanyl use during peri-operation and in post-anesthetic care unit in group D were lower than that in group C(P<0.01). The frequency of severe emergence agitation on arrival in the post-anesthetic care unit(0 min) was 18% in group D and 47% in group C (P<0.01); at 5 minutes and at 15 minutes, it was lower in group D. The duration of agitation on the scale was statistically lower in group D. In group D, 15% of patients and 42% in group C had an episode of pulse oximetry below 95% (P<0.01) . CONCLUSION: The incidence and duration of severe emergence agitation was lower with fewer patients having desaturation occurrence. An intraoperative infusion of dexmedetomidine combined with inhalation anesthetics provided satisfactory perioperative conditions for adenoidectomy without adverse hemodynamic effects.

Clinical observation on the treatment of puerperal mastitis with purple swelling Plaster

GU Jia-fu, QI Mei-ying

2011, 16(4):  432-434. 

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AIM: To study the therapeutic effect of puerperal mastitis with purple swelling plaster and joint anti-infection treatment. METHODS: 180 cases patients of puerperal mastitis were randomly divided into two groups,observation group and control group(n=90,each group).Observation group used purple swelling plaster by local application, control group used 25% magnesium sulfate solution with local hot compress, both groups used antimicrobial drugs and symptomatic treatment, efficacy was compared after 3 d. RESULTS: The total effective rate, effective time,course of treatment in observation group were better than those in control group,there is statistical significance (P<0.01). CONCLUSION: Purple swelling plaster combined with anti-infection treatment is effective to puerperal mastitis.

Analysis of therapeutic effect of 80 cases patients with pelvic inflammation disease treated with Kangfu anti-inflammatory suppository combined with antibiotics

CHEN Lin-hai

2011, 16(4):  435-438. 

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AIM: To evaluate the efficacy of treated pelvic inflammatory disease with Kangfu anti-inflammatory suppository and tinidazole. METHODS: 152 patients were diagnosed as pelvic inflammatory disease, who were divided into treated group(n=80)and control group(n=72). Treated group was treated with Kangfu anti-inflammatory suppository by rectal administration and oral tinidazole; Control group took tinidazole and amoxicillin orally or given an intravenous injection twice a day with ampicillin/sulbactam 3.0 g and metronidazole injection 100 mL. After three courses of treatment,the curative effect were compared between treated group and control group. RESULTS: The curative effect was good with Kangfu anti-inflammatory suppository combined with tinidazole treated pelvic inflammatory disease. The total effective rate were 97.5%,87.5%, respectively in treated group and control group.There was no statistical difference between the two groups. CONCLUSION: There is significant curative effect and less side effect on pelvic inflammatory disease treated with Kangfu anti-inflammatory suppository combined with tinidazole,which deserves the clinical expansion application.

Progress of metabonomic study on various metabolic diseases

ZHAO Chun-yan, A Ji-ye, CAO Bei, LIU Lin-sheng, WANG Xin-wen, LI Meng-jie, SHI Jian, WANG Guang-ji

2011, 16(4):  439-446. 

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Changes of modern living style and food structure greatly challenge biochemical metabolism of our body. Consequently, there appears an increasing rate of the metabolic diseases, such as hypertension, diabetes, dyslipidemia, tumor and so on, which do seriously harm to public health. Although substantial evidences have proved that metabolic diseases are tight associated with metabolic disorders, the underlying pathogenic mechanism is poorly known. By quantitative measuring of the in vivo molecules, metabonomics enables a dynamic profile of metabolic response of living systems to pathologic, genetic and environmental stimuli, and provides metabolic data for further exploring these diseases. Recently metabonomic studies have gained fruitful achievements, which show that in vivo biochemical metabolism is perturbed during the development of these diseases, including energy metabolism, lipids metabolism and amino acids turn over. Additionally, metabololism of fatty acids are possible to build the interchangeable association among hypertension, diabetes, and dyslipidemia,both oxidative stress and insulin resistance are deeply involved in their linkage. This article reviews recent studies of metabonomics on the metabolic diseases, aiming at clarifying the association between metabolic diseases and metabolic disorders, and providing potential strategy for the prevention and management of metabolic diseases.

Drug-drug interaction mediated by UGT

ZHANG Yan, HAO Hai-ping, WANG Guang-ji

2011, 16(4):  447-454. 

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Glucuronidation catalyzed by UDP-glucuronosyltransferase (UGT) is often recognized as the main pathway of conjugative metabolism for a variety of endogenous substances and exogenous compounds. For the development of new drugs, the investigation of drug metabolism mediated by UGT and the evaluation of potential drug-drug interaction are essential. Drug-drug interactions have been extensively studied and attracted much attention from researchers worldwide. However, the area of drug-drug interaction mediated by UGTs has received less attention than CYPs. Therefore, it is important to enhance our understanding of the role UGTs play in metabolic drug interactions in light of the fact that many drugs and their metabolites undergo UGT-mediated conjugation reactions. This review summarizes latest studies of the drug-drug interaction mediated by UGT inhibition.

Effects of polymorphic gene on the pharmacokinetics and pharmacodynamics of amlodipine

YANG Xia-ling,YANG Jing-zhi, XIONG Yu-qing

2011, 16(4):  455-460. 

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Amlodipine, 1,4-Dihydropyridine calcium channel antagonists, prescribed in the management of angina and hypertension, act as substrates of CYP3A5, has a pharmacokinetic profile that differs from other dihydropyridines.It has been suggested that the CYP3A5^*3 allele contributes to the interindividual variability of CYP3A activity in vivo. This review aimed to summarize the clinical application of the amlodipine and the possible role of the genetic polymorphism CYP3A5 on the pharmacokinetics and pharmacodynamics of amlodipine and instruct the reasonable clinical application of amlodipine.

Research progresses of free radical scavengers treating with ischemic stroke

WANG Xiao-jin , SUN Jian-guo , PENG Ying , WANG Guang-ji

2011, 16(4):  461-467. 

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Ischemic stroke is the second leading cause of death worldwide. Plenty of studies supported that free radicals are generated in the brain during ischemic-reperfusion injury and these radicals play important roles in the injury processes. Several free radical scavengers have been developed and some of them have progressed into clinical trials. One of them, edaravone, has been approved by the regulatory authority in Japan for the treatment of stroke patients. The purpose of this article is to review the current development of the radical scavengers treating with cerebral ischemic, and discuss the problems encountered and look into the future development of the free radical scavengers in the treatment of ischemic stroke.

Study on pharmacokinetic features of Repaglinide and the influence of genetic polymorphisms on its pharmacokinetics and drug interactions

SUN Xu,YUAN Zhao,WEN Jin-hua,XIONG Yu-qing

2011, 16(4):  468-473. 

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Repaglinide is a novel non-sulfonylurea oral hypoglycemic agent by stimulating insulin secretion, with a structure of amino acid profile.Its action occurs rapidly and sustains shortly.By simulating the physiology secretion of insulin, it majors in controlling hyperglycemia and reduces the incident of hypoglycemia.In this paper,we will give a review about the pharmacokinetic features, genomics research progress, drug interaction of repaglinide,in order to lay down a solid theory foundation for the guidance in clinical usage of repaglinide, ensure the safety and effectiveness of clinical usage, achieving individualized therapy in its true sense.

Cytochrome P450s and the metabolism of vitamin A

WANG Ping, LIU Xiao-dong

2011, 16(4):  474-480. 

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Vitamin A, as a kind of fat-soluble vitamin, could be metabolized to retinal and retinoic acid, which exhibited higher bioactivities. Cytochrome P450s (CYP450s) participated in not only the metabolism of xenobiotics but also metabolism of endogenous chemicals, such as vitamin A. It was reported that CYP1, CYP2C, CYP2E, CYP3A and CYP26 families were the CYP450s that mainly mediated metabolism of vitamin A. However, expression and activities of CYP450s could also be regulated by retinoic acid binding to nuclear receptors (RARs, RXRs). Besides CYP450s, transcription of several lipid transporters gene was also under the regulation of retinoic acid. Here, we reviewed the relative importance of CYP450s on vitamin A metabolism and molecule mechanism that how retinoic acid modulated the expression and activities of CYP450s and lipid transporters, in order to provide some new ideas and new targets for the study of disease caused by the lipid metabolic disorder.