Table of Content

Volume 16 Issue 12
26 December 2011

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Study on the relationship between pharmacokinetics and pharmacodynamics for statins in hyperlipidemia model in rats

LI Jing-yuan, CAI Jia-li, DAI Ren-ke, XIE Shui-lin, DENG Ji-feng, LU Pei-feng, LI Ren-shu, SUN He, LIU Yan-huai

2011, 16(12):  1321-1325. 

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AIM: To explore the relationship between exposure level (such as pharmacokinetics parameters) and pharmacodynamics for statins in hyperlipidemia model in rats.METHODS: The hyper- lipidemia rat model was established with the method of diet-induced, and the rats were given different does of statins to treat. The pharmacokinetics and pharmacodynamics parameters were determined, and the value of PK/PD were calculated, and their correlations were analyzed.RESULTS: TG-AUC showed a good linear relationship at the range of 0-10.96 folds, Y=0.01036X-7.6445 (γ=0.9599), the intermediate data such as CHOL-AUC, LDL-C-AUC, HDL-C-AUC were on the low side, which resulted large deviation, so there was an extremely weak linear correlation in these groups.CONCLUSION: There was a good linear relationship between TG and AUC in the range of AUC (0-10.96 folds), it could be efficaciously used to predicted the pharmacodynamics upon the related datas for AUC.

Effect of Ginkgo biloba talbes on the pharmacokinetics of intragastrically administered losartan in rats

PAN Pei, WANG Shi-ming, GUO Zhu-ying, YUAN Yong-fang

2011, 16(12):  1326-1331. 

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AIM: To investigate the possible effect of ginkgo biloba tablets which were prepared by Ginkgo biloba extracts (GBE) on the pharmacokinetics of losartan by intragastrically administering in rats.METHODS: SD rats were randomly divided into two groups (losartan group and GBE+losartan group).Rats in GBE+losartan group were administered with GBE 100 mg/kg from day 1 to 14. On day 15, Rats in the losatan group were administered with losartan 10 mg/kg, and Rats in the GBE+losartan group were added with GBE 100 mg/kg.Blood samples were collected from the angulus oculi veins at 0.5,1,2,3,4,6,8,10,12,24 h.The blood plasma concentration of losartan and EXP3174 were determined by HPLC.Main pharmacokinetic parameters were calculated and compared by statistical analysis.RESULTS: After co-administrating with GBE, there were no significantly different pharmacokinetic parameters of losartan were found.However, the t_max of EXP3174 was markedly decreased (P<0.05). The C_max,AUC_{0-8 h}, AUC_0-∞ of EXP3174 were significantly increase (P<0.01). And the CL of EXP3174 was markedly decreased (P<0.01).There was no significantly changed of t_1/2 and MRT about EXP3174.CONCLUSION: GBE can affect the metabolism of EXP3174, which were no significantly different on the pharmacokinetics of losartan.

Effects of hemp seed oil on learning and memory performances in senile mice induced by D-galactose

SU Jing, HE Hai-bo, SHI Meng-qiong, XIONG Xing-jun, CHEN Liang-jin, LU Xun-cong

2011, 16(12):  1332-1339. 

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AIM: To research the effects of hemp seed oil on learning and memory performances in senile mice induced by D-galactose and its mechanisms.METHODS: By using the D-galactose-induced aging mice, learning and memory performances were tested with step down, water maze and Morris water maze test, and determined the activities of total antioxidant capacity (T-AOC), superoxide dismutase (SOD), glutathione peroxidase (GSH-Px) and content of malonaldehyde (MDA) in brain tissue, determined the content of acetylcholine (Ach) and activities of acetylcholine esterase (AchE), choline acetyltransferase (ChAT) in cerebral cortex and hippocampus; analyzed brain tissue histopathological examination simultaneously.RESULTS: Hemp seed oil (3, 6, 12 mL/kg) could significantly prolong the latency, reduce the error frequency in step down test, reduce the reaching time and error frequency in water maze test, obviously shorten the escape latency and reaching primary platform time, increase passing through primary platform frequency and resided time in Morris water maze test. It could obviously reduce the content of MDA, increase activities of T-AOC, SOD, GSH-Px in brain tissue, remarkably increase the content of Ach and activities of AchE, ChAT in cerebral cortex and hippocampus and reduce the brain tissue injury.CONCLUSION: Hemp seed oil improves the learning and memory performances of the D-galactose-induced aging mice. The mechanism may be related to increased activity of antioxidation and scavenge of free radicals, improved function of the central cholinesterase system.

Effects of compound decotion on activity and expression of nitric oxide and neuronal nitric oxide synthase in the brain of traumatic brain injury rat model

MIAO Jing-kun, CHEN Qi-xiong, WU Xiao-mei, LIU Zhen-qiu, ZHANG Xiao-ping

2011, 16(12):  1340-1346. 

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AIM: To explore the possible mechanism of the neuroprotective effect of compound decotion on traumatic brain injury model.METHODS: The traumatic brain injury rat model was induced by improved Feeneys fall weight method and divided into sham operation group, TBI model group and compound decotion treatment group, compound decotion treatment group rats were intragastrically administered with compound decotion at 10 g·kg^-1·d^-1. Sham operation group and TBI model group were treated with same dose of normal saline, twice per day for seven days. The brains were taken out at 24, 72 h and one week after injury, respectively. The morphological changes were observed by HE staining in the cerebral cortex. The NO and NOS concentration and neuronal nitric oxide synthase (nNOS) activity were detected by neurochemistry stain method. nNOS expression were detected by immunohistochemical method. nNOS-mRNA expression were detected by in situ hybridization.RESULTS: In TBI model group, the concentration of NO and NOS and the activity and expression of nNOS and the expression of nNOS- mRNA were markedly elevated at different degrees at different time point and especially 24 hours after injury and still higher than those of sham operation group one week after injury. However, compared with the TBI model group, the concentration of NO and NOS and the activity and expression of nNOS and the expression of nNOS-mRNA in compound decotion treatment group were obviously decreased and reach normal level one week after injury (P＜0.05).CONCLUSION: NO and nNOS play an important role in the pathophysiological process of TBI. Inhibition of activated NO and nNOS and mitigate secondary brain injury may represent a potential neuroprotective mechanism for the treatment of TBI with compound decotion.

Effects of Ginkgo biloba extract on cell proliferation in human Tenon's capsule fibroblasts stimulated by TGF-β₁ and its potential mechanism

LING Jiao-jiao, LI Ping-hua

2011, 16(12):  1347-1351. 

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AIM: To investigate the effects of Ginkgo biloba extract on cell proliferation in cultured human Tenon's capsule fibroblasts and its potential mechanism.METHODS: Human Tenon's capsule fibroblasts were cultured in vitro, the subcultured cells were identified by morphology observation and Vimentin staning. Untreated cells were acted as normal control group,TGF-β₁ as the stimulating factor, the cells were treated with GBE with concentrations of 0,25,50,100 and 200 mg/L. Cell proliferation was observed by MTT assay, flow cytometry tested cell cycle, the expression of α-smooth muscle-actin (α-SMA) was detected by immunocytochemistry, the mRNA level of connective tissue growth factor (CTGF) was measured by RT-PCR.RESULTS: TGF-β₁ markedly increased the cell proliferation, GBE effectively inhibited the proliferation in a concentration-time dependent way. The S phase of cells in TGF-β₁ group were gradually increased, the expression of α-SMA and CTGF were also markedly increased induced by TGF-β₁, which was partly attenuated by GBE.CONCLUSION: Ginkgo biloba extract can inhibit HTCFs proliferation and down regulation the TGF-β₁ induced α-SMA and CTGF mRNA overexpression.

Protective effect of Resveratrol on LPS-inducing mice acute lung inflammation

JIN Wan-bing

2011, 16(12):  1352-1356. 

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AIM: To study the protective effect of Resveratrol on the acute lung inflammation in experimental mice and its mechanism of action.METHODS: The acute lung inflammation model was established in mice and mice were i.p. treated with Resveratro or vehicle in 4 d. The curative effect of Resveratrol were observed, as well as the changes of differential leukocytes count in bronchoalveolar lavage fluid, the expression of TNF-α IL-1β and IL-6 after treatment.RESULTS: The results showed that Resveratrol could significantly relieve the clinical symptoms of acute lung inflammation and could reduce the numbers and percentages of leukocytes in the bronchoalveolar lavage fluid. The activation of TNF-α IL-1β and IL-6 were inhibited by Resveratrol.CONCLUSION: These findings indicated that Resveratrol possessed reliable curative effect for acute lung inflammation, in which the inhibition of inflammatory factors, especially TNF-α, IL-1β and IL-6 was a potential antiphlogistic mechanism.

Protective effect of 18-α isomer of glycyrrhizin on human hepatocytes injured by D-galactosamine and carbon tetrachloride

ZHANG Qun, WU Pei, ZHANG Jian-jun

2011, 16(12):  1357-1360. 

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AIM: To investigate the effects of 18-α isomer of glycyrrhizin (magnesium isoglycyrrhizinate,MI) in protecting human hepatocytes (L-02) injured by D-galactosamine (D-GalN) and carbon tetrachloride (CCl₄),and research MI in protecting human hepatocytes deeply.METHODS: The cultured L-02 were pre-treated MI,respectively, for protecting these cells from the injury made with CCl₄ or D-GalN. Then, the final product of nitrogen (NO_x), and the cellular mitochondrial membrane potentials were measured .All the values above were analyzed to research the protective effects of the MI.RESULTS: At the concentration of 1 mg/mL, the MI could improve the survival rate of cells, and significantly reduced NO_x releasing from the D-GaLN or CCl₄ injured cells(P＜0.05), and could increase the decreased cell mitochondrial membrane potential caused by D-GalN.CONCLUSION: At the concentration of 1 mg/mL, the MI have protective effects on the D-GalN or CCl₄ injured human hepatocytes. The mechanism of these protective effects may be related to the inhibition of NO_x release and related to the improvement of the cellular mitochondrial membrane potentia.

Relationship between the expression of LAT1,CD98hc and clinical pathological characteristics of gastric carcinoma

SHI Liang-hui, ZHANG Cai-quan, PENG Xiao-zhuang

2011, 16(12):  1361-1366. 

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AIM: To investigate the expression of L-type amino acid transporter-1(LAT1), CD98hc in gastric carcinoma and elucidate the relationship between their overexpression and clinical pathological characteristics.METHODS: The expression of LAT1, CD98hc and Ki67 in 45 cases of gastric cancer, 45 cases of adjacent normal gastric tissue were detected by using semiquantitative reverse transcription polymerase chain reaction (RT-PCR) and immunohistochemistry.RESULTS: RT-PCR analysis showed that the expression of LAT1, CD98hc mRNA in gastric carcinoma tissues were significantly higher than those in adjacent normal gastric tissues(P<0.05). Immunohistochemistry showed that the positive rate of LAT1 accounted for 64.4% (29/45) in gastric carcinoma, and 6.67% in adjacent normal gastric tissues (P<0.01). The positive expression rate of CD98hc was 60.0% in gastric carcinoma tissues, and 22.2% in adjacent normal gastric tissues (P<0.01). The expression of LAT1, CD98hc in poorly differentiated gastric carcinoma, stage Ⅲ-Ⅳ were significantly higher those in well differentiated gastric carcinoma, stage Ⅰ-Ⅱ(P<0.05). In gastric cancer with lymph metastasis, tumor size ≥5 cm, their expression were significantly higher than that in gastric cancer without lymph metastasis, tumor size ＜5 cm(P<0.05). The higher expression of LAT1, CD98hc were positive correlated to Ki67 in gastric carcinoma (P<0.01).CONCLUSION: LAT1, CD98hc specifically highly express in gastric carcinoma. The abnormal expression may play an important role in the carcinogenesis and metastasis of gastric carcinoma.

Experiment study of Guanxinshu capsule attenuates anoxia/reoxygenation injury in neonatal rat cardiomyocytes by partial formulation analysis

HE Huan, HOU Li, HUANG Huang, WANG Jing-qian, FAN Mei-mei, HE Ming

2011, 16(12):  1367-1373. 

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AIM: To investigate the protective effect of guanxinshu capsule on cardiomyocytes after anoxia-reoxygenation(A/R) injury, partial formulation experiment was executed by orthogonal design in order to obtain the best ratio of Guanxinshu.METHODS: Based on the effective site and the basic ratio isolated from original chemical formulation of salvia miltiorrhiza, panax pseudo-ginseng, lignum acronylchiae, orthogonal table was designed.The primarily neonatal rat ventricular cardiomyocytes were randomly divided into 18 groups: (1)control group; (2)A/R group; (3)-(18) experimental groups treated with different ratio; Cell viability, SOD, Catalase, GPx activities, MDA contents and LDH activitied were detected.Best ratio of program was obtained by analysis of integrated equilibrium and then verificated.RESULTS: These groups treated with different ratio of Guanxinshu elevated cell viability and SOD, Catalase, GPx activity, whereas LDH activities and MDA contents reduced(P<0.01 or P<0.05); Panax pseudo-ginseng saponins and salvia miltiorrhiza phenolic acid have played an important role of protection of cardiomyocyte and increased ability of attenuation lipid peroxidation; The best ratio of Guanxinshu is: A3B3C2D4.CONCLUSION: The different ratio of Guanxinshu have protected cardiomyocyte against A/R injury, the mechanism may be relative with attenuation lipid peroxidation.The best ratio of Guanxinshu is: salvia miltiorrhiza total phenolic acid 0.027 mg, Panax pseudo-ginseng total saponins 0.048 mg, lignum acronylchiae oil 0.002625 mg, lignum acronylchiae total flavonoids 0.01326 mg.

Activation of group I metabotropic glutamate receptors modulates descending activation of spinal cord motoneurons

ZHENG Yong, WANG Meng-ya

2011, 16(12):  1374-1378. 

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AIM: To evaluate the modulatory action of group I metabotropic glutamate receptors (mGluRs) on descending activation of spinal cord motoneurons (MNs) in vitro.METHODS: The intracellular recordings were made in MNs of spinal cord slices isolated from neonatal rats (7-14 days old), and excitatory postsynaptic potential (EPSP) was evoked by ipsilateral ventrolateral funiculus (iVLF) stimulation, i.e. iVLF-EPSP.By superfusion of (S)-3,5-dihydroxyphenylglycine hydrate (DHPG), an agonist of group I mGluRs, the modulatory action was observed on the MN membrane electrical properties, as well as on the iVLF-EPSP.RESULTS: Application of DHPG (5 μmol/L) significantly depolarized the motoneuron membrane (n=7, P<0.01), reduced time constant (n=7, P<0.05), and extended the half-width of the spike potential (n=5, P<0.05). The amplitude of iVLF-EPSPs in 7 tested MNs was reversibly and concentration-dependently suppressed by superfusion of DHPG (5-10 μmol/L,P<0.01).CONCLUSION: Activation of group I mGluRs by DHPG may inhibit the descending activation of spinal cord MNs in vitro.

Acetyl-L-carnitine prevents and reduces oxaliplation-evoked painful peripheral neuropathy

LIU Guo-kai, Gary Bennett

2011, 16(12):  1379-1382. 

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AIM: To examine the potential efficacy of acetyl-L-carnitine (ALCAR) to prevent and treat oxaliplation-evoked pain.METHODS: 20 adult male Sprague-Dawley rats (150-200 g) were randomly divided into two groups, ALCAR group and control group. Each group had 10 rats. A stock solution of oxaliplatin is diluted to 2 mg/mL with 5% dextrose in distilled water and injected IP at 2 mg/kg on five consecutive days (d 0-d 4) in a volume of 1.0 mL/kg. ALCAR (100 mg/kg; p.o.) or vehicle was given daily starting on day 0 (the day of the first oxaliplatin injection) and continuing until day 21 (i.e.,15 days after the last oxaliplatin injection. Mechano-allodynia and mechano-hyperalgesia were assessed using von Frey hairs with bending forces of 4 g and 15 g, respectively, on d 8, d 22, d 27, d 35, and d 41 postoperatively. Withdrawal responses were counted and expressed as an overall percentage response.RESULTS: Mechano-allodynia (4 g) and mechano-hyperalgesia (15 g) of the rats in ALCAR group were significantly and persistently reduced (P<0.01) on d 8, d 22, d 27, d 35, and d 41 postoperatively in comparison with control group.CONCLUSION: It is concluded that ALCAR may be useful in the prevention and treatment of oxaliplatin-induced painful peripheral neuropathy.

Population pharmacokinetics of amlodipine in healthy Chinese adult male volunteers

HUANG Xiao-hui, HUANG Ji-han, LI Lu-jin, WANG Kun, YANG Juan, ZHENG Qing-shan

2011, 16(12):  1383-1390. 

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Amlodipine is a third-generation dihydropyridine calcium channel blocker that is indicated for treatment of hypertension and angina in adults. The population pharmacokinetics of amlodipine was evaluated in 60 healthy volunteers enrolled in three bioequivalence studies. These data, along with a set of covariates, were the subject of a nonlinear mixed-effect modeling analysis using the NONMEM program. A two-compartment model with first order absorption was fitted to the serum amlodipine concentration data. No significant covariates were found in the model-building. The intraindividual (residual) variability expressed as coefficient of variation was 18.7%, whereas the interindividual variability of CL, V₂,V₃ and K_a,was 27.3%, 26.6%, 49.9% and 65.7%, respectively. The relatively high (>40%) interindividual variability for V₃ and K_a parameters, observed under the controlled experimental settings of bioequivalence trials in healthy volunteers, may result from genetic variability of the processes involved in amlodipine absorption and disposition.

Association of polymorphism in CRP gene with metabolic syndrome

JIN Yue-long, HE Lian-ping, CHEN Jin-feng, WANG Bin-bin, SHEN Chong, YAO Ying-shui

2011, 16(12):  1391-1396. 

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AIM: To investigate the association of rs6677719 polymorphism in the C-reactive protein gene with metabolic syndrome.METHODS: Stratified cluster sampling method was conducted to select 301 cases of metabolic syndrome and 547 healthy individuals who were matched with cases for age and gender from a community based population.Questionnaire was managed, and physical examination and blood biomarkers tests were conducted, and rs6677719 locus was detected by the method of polymerase chain reaction-restriction fragment length polymorphism (RFLP).The distributions of TT, TC and CC genotype frequencies between cases and controls were compared and the association of rs6677719 polymorphism with serum glucose, blood pressure and blood lipids were analyzed.RESULTS: The results of association analysis indicated that rs6677719 variation had significant correlation with MS, and additive and dominant models presented statistical significances, odds ratios (OR) and corresponding 95% confidence interval (CI) were 0.785 (0.640-0.862) and 0.659 (0.489-0.889) ,respectively.The TG level of TC genotype carrier was significantly lower than that of TT genotype carrier in control group.Furthermore, the HDL-C and LDL-C levels of individuals presented significant linear trend in TT, TC and CC genotypes.CONCLUSION: The results in the present study suggest that rs6677719 polymorphism in CRP gene is associated with MS and the genetic variation significantly affects the TG, HDL-C and LDL-C of metabolisms in general population.

Effect of CYP2C19 genetic polymorphism on pharmacokinetic characterstics and 5 - hydroxyl metabolic pathway of lansoprazole in Chinese volunteers

YAN Fei, XIA Chun-hua, XIONG Yu-qing

2011, 16(12):  1397-1401. 

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AIM: To investigate the effect of CYP2C19 polymorphism on pharmacokinetic characteristics and 5-hydroxyl metabolic pathway of lansoprazole in Chinese subjects.METHODS: Twelve healthy subjects were typed by using RFLP-PCR method. After intravenous drip 30 mg lansoprazole, the plasma concentrations of lansoprazole in subjects were determined by LC-MS method. The pharmacokinetic parameters of lansoprazole and AUC_LPZ/AUC_{5-OH LPZ} were calculated and compared between different groups.RESULTS: After all the subjects were given 30 mg lansoprazole, it found that the AUC_0-t, AUC_0-∞, CLz, (AUC_LPZ/AUC_5-OH)_0-t and (AUC_LPZ/AUC_5-OH)_0-∞ of the mutant types were equivalent to 2.381, 2.572, 0.428, 3.602 and 4.083-fold as those of the wild types, respectively.CONCLUSION: The CYP2C19 genetic polymorphism, which has significant influence on the pharmacokinetic characteristics of the lansoprazole in Chinese volunteers (P<0.05), has very significant influence on the 5-hydroxyl metabolic pathway of the lansoprazole (P<0.01). The result suggests that CYP2C19 genetic polymorphism is one of the important factors leading to individual concentration differences of the lansoprazole and has a better relevance with the 5-hydroxyl metabolic pathway.

Effect of intravenous lidocaine on bispectral index and stress reaction in patients undergo tracheal intubation

WANG Hong-zhu, CHEN Feng-lin, WANG Ming-cang

2011, 16(12):  1402-1405. 

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AIM: To observe the relationship between the level of catecholamine with bispectral index during endotracheal intubation with propofol anesthesia in order to investigate the mechanism of the preventing of endotracheal intubation response with lidocaine.METHODS: Sixty patients were randomly allocated into two groups:control group (Group C) and lidocaine group (Group L). The patients received lidocaine 1.5 mg/kg in Group L and saline in Group C before induction of anesthesia. Anesthesia was induced with propofol (2 mg/kg) and fentanyl (4 μg/kg) and tracheal intubation was facilitated with rocuronium (0.6mg/kg) in all patients. Bispectral index (BIS), systolic pressure(SP), diastolic pressure(DP)and heart rate(HR)were continuously monitored and recorded before induced of anesthesia(T₀), preintubation(T₁),immediately and 1,3 min after intubation (T_2-4). Arterial blood samples were obtained at T₀, T₁ and T₃ for determination of plasma concentration of adrenaline (Ad) and noradrenaline(NA).RESULTS: SP, DP,HR were significantly increased after intubation in Group C compared with baseline values at T₀(P<0.05),while plasma Ad and NA concentrations at T₃ were of no statistic significance(P>0.05). Compared with Group C, BIS value at T₁ to T₄ decreased significantly in Group L(P<0.05). Plasma Ad and NA were lower at T₃ in Group L than those in Group C and T₀(P<0.05).CONCLUSION: Lidocaine can further reduce BIS value and the plasma concentration of catecholamines during propofol anesthesia, indicating the sedative and anti-nocieptive effect of intravenous lidocaine. Lidocaine(1.5 mg/kg)can restrain the changes of BIS and reduce stress reaction caused by tracheal intubation.

Cost-effectiveness analysis of three treatment schemes for Insulin Aspart 30 Injection on type 2 diabetes mellitus

ZHU Lei, ZHANG Li-fang, XU Lan, WANG Juan, ZHANG Guo-dong, SHEN Ming-feng

2011, 16(12):  1406-1409. 

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AIM: To compare the clinical therapeutic effects and cost-effectiveness of Insulin Aspart 30 Injection(NovoMix30FlexPen) among different therapeutic regimens for diabetic patients.METHODS: A retrospective study was conducted in which a total of 135 cases with type 2 diabetes mellitus were divided into 3 groups by random(A: NovoMix30FlexPen for morning or night for 6 months; B: NovoMix30FlexPen prior three meals for 6 months; C: NovoMix30FlexPen for morning or night + Acarbose Tablets for 6 months).RESULTS: The effective rates of FBG were 84.4％ in Group A versus 86.7％ in Group B and 91.1％ in Group C (P>0.05), the effective rates of PBG2h were 91.1％, 91.1％ and 88.9％, and the effective rates of HbA1c were 75.6％, 80.0％, 77.8％ respectively.CONCLUSION: Blood sugar level can be controlled to an ideal level through the three treatment schemes; while Group C is better considering the cost-effectiveness ratios, and it has the clinical value of popularization.

Effection of Shenmai Injection for chemotherapy patients with cancer on blood tests and CD₄/CD₈ ratio

ZHOU Yue-fen , WU Min-hua, CHEN Xue-feng, YIN Xiao-li , XIE Yan-ru, WANG Yong-hui, LOU Jian

2011, 16(12):  1410-1413. 

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AIM: To study the effect of Shenmai Injection for gastrointestinal tumor patients after operation with oxaliplatin chemotherapy on blood tests and CD₄/CD₈ level.METHODS: Eighty cases of gastrointestinal tumor patients after operation with oxaliplatin chemotherapy were divided into single group and combined group, each 40 cases. The single group was administered by chemotherapy only while the combined group by chemotherapy and Shenmai Injection. After 6 cycle chemotherapy, TCM symptoms integral, neutrophils, CD₄/CD₈ ratio were compared between two groups.RESULTS: Compared with the single group, the TCM symptoms integral of the combined group was less (P<0.01). Compared with the single group, the neutrophils level of the combined group was less (P<0.05). Compared with the single group, the CD₄ level and CD₄/CD₈ ratio were more and statistically significant (P<0.05).CONCLUSION: Shenmai Injection can improve chemotherapy related symptoms and reduce bone marrow toxicity; it can also adjust chemotherapy patient's immune status and ensure chemotherapy smoothly.

Effectes of β₁-adrenergic receptor and CYP2D6 gene polymorphism on metoprolol antihypertension therapy

XU Cheng-hua, YANG Yu-wen, CAO Heng

2011, 16(12):  1414-1418. 

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AIM: To investigate effects of β₁-adrenergic receptor and CYP2D6 gene polymorphism on metoprolol antihypertension therapy.METHODS: 120 cases of patients with essential hypertension were detected by β₁-adrenergic receptor and CYP2D6 gene polymorphism,118 patients with Arg 389 allele in β₁- adrenergic receptor gene chosen from 120 essential hypertension patients were divided into three phenotype groups according to CYP2D6 gene mutations: the poor metabolism group(PM, 55 cases), intermediate metabolism group(IM, 36 cases)and extensive metabolism group(EM, 27 cases).The subjects of PM, IM and EM were administrated with metoprolol for the same dose(100 mg/d), taking orally twice a day. Blood pressures, heart rates and side effects were observed during 4-week following-up.RESULTS: Blood pressure and heart rate in group PM, IM and EM were decreased, especially, obviously decreased in group PM, however, the incidence of side effect was significantly increased in group PM.CONCLUSION: The genetic polymorphism of β₁- adrenergic receptor and CYP2D6 was associated with the efficiency of metoprolol antihypertension therapy.

Dosage research of serum 25-hydroxyvitamin D levels on different intervention treatments for children

ZHANG Xia-juan, BAO Li-fang, BAO Zhou-jun, WANG Yin, LI Yi-wei, WANG Ye-kai

2011, 16(12):  1419-1422. 

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AIM: To explore the serum 25-hydroxyvitamin D levels effected by different intervention treatments.METHODS: 102 children with vitamin D deficiency were selected and divided as follows: Group A: VitD 150000 IU once; Group B: VitD 200000 IU once; Group C: VitD 300000 IU once; Group D: VitA 3600 IU+VitD 2000 IU per day, lasting for a month. A month later, their serum 25-hydroxyvitamin D levels were rechecked by electrochemistry method.RESULTS: The serum 25-hydroxyvitamin D levels after treated in Group A,B,C,D were significantly higher than that before treated(P＜0.01). The increased serum 25-hydroxyvitamin D levels in Group A,B and C were significantly higher than that in Group D(P＜0.01). The increased serum 25-hydroxyvitamin D levels in Group C was significantly higher than that in Group A and B(P＜0.01).CONCLUSION: VitD 150000-200000 IU once is a safe and effective intervention treatment for vitamin D deficiency.

Clinical research on botulinum toxin type A combining rehabilitation training for the treatment of children cerebral palsy

WU Su-ying

2011, 16(12):  1423-1425. 

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AIM: To observe the clinical effect of botulinum toxin type A combining rehabilitation for the treatment of children cerebral palsy.METHODS: Thirty-two cases of children cere bral palsy admitted to hospital from March 2009 to March 2011 were randomly divided into two groups, control group(n=16) and treatment group(n=16). The control group was given conventional rehabilitation training; the treatment group was also given injection of botulinum toxin A. The clinical effects in 2 groups were observed and compared.RESULTS: After treatment, the GMFM score in the treatment group was significantly higher than that in the control group (P<0.05). The Ashworth score in the treatment group was significantly lower than that in the control group (P<0.05); and the popliteal fossa angle, foot disaffection angle and abduction angle in the treatment group were superior to those in the control group(P<0.05).CONCLUSION: There is a significant clinical effect of botulinum toxin type A combining rehabilitation for the treatment of children cerebral palsy.

Progress of pharmacological effects and pharmacokinetics of stilbene glycoside from Polygonum multiflorum Thunb

WANG Jian-kun, ZHU Xuan-xuan, SUN Jian-guo

2011, 16(12):  1426-1430. 

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Stilbene glycosides, the special constituents in Polygonum multiflorum Thunb, were reported to be the active ingredients with various pharmacological effects. It is reviewed the research progress of the pharmacological effects of Stilbene glycoside (2,3,5,4'-tetrahydroxystilbene-2-O-β-D-glucoside) on antioxidant system, cardiovascular system, central nervous system and anti-tumor effects. The possible mechanism involved and its possible application are also discussed. Meanwhile, the advances in pharmacokinetics of stilbene glycoside such as absorption and metabolism are also summarized. Thus we can provide some new ideas and strategies for further in-depth research on stilbene glycosides.

Phytoestrogen-like effects of herbal saponins

XU Xian-xiang, WU Yang-zheng, SUN Ai-jing, DIAO Yong

2011, 16(12):  1431-1436. 

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Phytoestrogens (PEs) are defined as the plant compounds with structures or activities similarly to estrogen. Benefits of PEs to human health get universal attentions. Multifarious herbal components play the roles as phytoestrogen. Saponins, important natural products, exhibit remarkable pharmacological effects including anti-tumor, anti-oxidant, anti-inflammation, immunoregulation, anti-osteoporosis, antivirus, cardiovascular protection, neuroprotection, anti-aging and regulation of glucose and lipid metabolism.Saponins are clinically valuable for applications in hormone-related diseases like endometriosis, breast cancer, prostate cancer,osteoporosis and cardiovascular diseases. It is theoretically and practically significant to further elucidate phytoestrogen-like effects of saponins.

Written main contents of six sections of labeling for prescription drug and cautions

XIAO Hui-lai

2011, 16(12):  1437-1440. 

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Main contents of six sections of labeling for prescription drug, including warning, indication, dosage and administration, adverse reactions, overdosage, pharmacology and toxicology written when drafting according to the related rules and guidelines of China and USA are described. The cautions are provided based on the problems of drafts of labeling. It is expected to help to improve the quality and efficiency of drafting. The paper is also beneficial to reading and supervision of the labeling.