Table of Content

Volume 11 Issue 4
26 April 2006

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Neuronal nicotinic acetylcholine receptor-mediated Ca²⁺ signals and regulation

HU Jun, HU Gang, WU Jie

2006, 11(4):  361-365. 

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Neuronal nicotinic acetylcholine receptors (nAChRs) are widely distributed in the central nervous system, and they participate in complex neuronal signal transduction and regulation in the brain.The high Ca²⁺ permeability of nAChRs, plays a pivotal role in shaping nAChRs-induced neuromodulatory effects.The nAChRsmediated Ca²⁺ signals may regulate diverse neuronal activities such as the improvement of learning and memory, and are closely related to drug addiction or neuroprotection mechanism.

Progress on inflammatory reaction mechanism of ischemia/reperfusion injury

PENG Xin, DONG Zhi

2006, 11(4):  366-368. 

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The mechanism and pathophysiological progress of ischemia/reperfusion are complicated, and all the factors influence each other.This article summarized recent development on the related factors of inflammatory reaction mechanism.

Some problems on clinical trails evalution of herbs medicine for insomnia

LI Tao

2006, 11(4):  375-378. 

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The clinical trails of Traditional Chinese Medicine Herbs in treating insomnia need to pay attention to the adaptation and the symptoms change after stopping the herb medicines.It is recomnendated that the placebo control, sleep diary have to be a base for the result evaluation, the week is basic duration of evaluation and the insomnia symptom score is the major index.

Study on in vitro models of drug absorption

ZHOU Xin

2006, 11(4):  379-384. 

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This article summarized some in vitro models of drug absorption, whose shortcomings and virtues were compared in order to be convenient for researchers to know and select optimal model.

Use of trimetazidine in ischemic heart disease

Acharya Dhan Kumar, DANG Yu-hua

2006, 11(4):  385-391. 

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Ischemic heart disease (IHD) is characterized pathologically by the atheromatous plaque which may induce stenosis or obstruction of the coronary arterial lumen leading to myocardial ischemia, experienced by the patients as chest pain.Plaque rupture provides a focus for platelet deposition and thrombosis, and results in unstable angina or myocardial infarction.Stable angina pectoris is treated conventionally by using beta blockers, nitrates and calcium channel blockers (CCB), all of which act by either increasing the supply or decreasing the demand of oxygen in myocardium.In recent years a group of drugs known as metabolic modulators have been particularly shown to be beneficial in protecting the myocardium.Trimetazidine has been a special target in this group.It has been found that in ischemic myocardium there is high rate of fatty acid (FA) oxidation and subsequent inhibition of glucose oxidation.This drug is thought to have direct cytoprotective action in ischemic myocardium through inhibition of the oxidation of FA.Numerous studies are still being carried out to further clarify its roles in various other conditions related directly or indirectly with IHD.The purpose of the review was to assimilate the results of various trials done all over the world in the recent years to find out the role in IHD and the exact mechanism of action, in order to know its true worth in myocardial protection.

Genetic polymorghism of CYP2D6 and drug interactions

LI Qin, WANG Rui

2006, 11(4):  369-374. 

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As one of major cytochrome P450s, CYP2D6 is responsible for many important drugs' metabolism.The genetic polymorphism of CYP2D6 is the basis of significant individual variability in the metabolism of drugs.Meanwhile, many drugs can influence the activity of CYP2D6 by competitive inhibition or induction, which is easy to cause interaction in coadministration.So we will investigate the relations of genetic polymorphism of CYP2D6 to drug interactions from such aspects as phenotype, competitive inhibition of substrates, induction or inhibition of CYP2D6.

CPU86017 and its enantiomers inhibit abnormal gene expression of calcineurin and NFκB in rat cardiomyopathy induced by L-thyroxin

QI Min-you, XIA Hui-jing, DAI De-zai, TANG Xiao-yun, SU Wei, ZHANG Can

2006, 11(4):  392-397. 

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AIM: To investigate the CPU86017 and its enantiomers inhibit abnormal gene expression of calcineurin and NFκB in rat cardiomyopathy induced by L-thyroxin and compare the effect of CPU86017 (racemate) with its 4 enantiomers:(7S, 13R), (7S, 13S), (7R, 13S), and (7R, 13R)-CPU86017 in this model. METHODS: The animals were randomly divided into 7 groups.The rat hypertrophied model was produced by treatment with L-thyroxin 0.2 mg·kg ^-1 ·d ^-1, sc for 10 d and treated with CPU86017 or its enantiomers 4 mg·kg ^-1 ·d ^-1, sc from d 6 to d 10.The changes in left ventricular (LV) weight index, redox system, and the NO and iNOS activity in the myocardium were investigated.The expression of mRNA of calcineurin 、NF-κB in the left ventricle was measured.RESULTS: There were significant cardiac hypertrophy and oxidative stress in rats treated by L-thyroxin.The expression of calcineurin, NFκB mRNA were upregulated (P <0.05, compared with that of control).After treatment with CPU86017 (racemate and enantiomers), LV remodeling and the redox system were improved.CPU86017 and (7S, 13R)-CPU86017 showed a better improvement on LV remodeling and the redox than the other isomers and restored the normal expression of calcineurin, NF-κB (P <0.05, P <0.01), respectively.CONCLUSION: It suggested that an up-regulation of calcineurin and NFκB possibly related to the altered intracellular calcium handling system plays a role in the progression of L-thyroxin induced cardiomyopathy and CPU-86017 and its 7S, 13R-CPU86017 enantiomer effectively inhibit the abnormal expression of calcineurin and NFκB genes, the NOS enzyme and oxidant stress in the cardiomyopathy.

Diazoxide increases glutamate uptake by astrocytes via activating mitochondrial ATP-sensitive potassium channels

DAI Cui-ping, ZENG Xiao-ning, SUN Xiu-lan, DING Jian-hua, HU Gang

2006, 11(4):  398-401. 

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AIM: To demonstrate the effect of mitochondrial ATP-sensitive potassium channel opener, Diazoxide, on glutamate uptake activity of astrocyte. METHODS: Primary astrocytic cultures were prepared from cerebral cortices of rats within 3 days old.Glutamate uptake activity of astrocytes was measured using isotopic techniques to detect intracellular [³H]-labeled D, L-glutamate concentration.RESULTS: Diazoxide increased [³H]-glutamate uptake in a concentration-dependent manner, and could significantly reverse MPP⁺-induced glutamate uptake inhibition.The above effects of Diazoxide were blocked by 5-hydroxydecanoate, a selective mitochondrial ATP-sensitive potassium channel blocker. CONCLUSION: Diazoxide increase the activity of glutamate transporters in astrocytes by opening mitochondrial ATP-sensitive potassium channel.

Effect of compoud 5F isolated from Pteris Semipinnata L on cell cycle and synthesis of DNA and RNA of SPCA-1 cells

DAI Bin, CUI Liao, WU Tie, DENG Yi-feng, WU Ke-feng

2006, 11(4):  402-405. 

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AIM: To study the effects of compound 5F, one of the diterpenoids extracted from Pteris Semipinnata L, on cell cycle and synthesis of DNA and RNA of SPC-A-1 cells.METHODS: Cytotoxicity was determined by MTT test, the cell cycle was analysed by flowcytometry (FCM) and the synthesis of DNA and RNA was observed by the [³H]-TdR and [³H]-UTP incorporation.RESULTS: Compound 5F strongly inhibited the growth of SPC-A-1cells, FCM analysis revealed that 5F could increase the percentage of cells in G2 and S phase and decrease those in G1 phase after 24 h treatment.The assays of [³H]-TdR and [³H]-UTP incorporation into DNA and RNA respectively showed obvious inhibition dose-dependent after exposure to 5F for 24 h.CONCLUSION: Compound 5F obviously inhibits SPC-A-1cells proliferation, arrests SPC-A-1cells in G2 and S phase and inhibits the synthesis of DNA and RNA.

Determination of PMEA-Na in dog plasma by liquid chromatography and tandem mass spectrometry and its pharmacokinetic study

WANG Wen-yan, SHEN Zi-long, WANG Shi-bing, YAO Quan-sheng

2006, 11(4):  406-409. 

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AIM: To established an HPLC/MS/MS method for the study of pharmcokinetics of PMEA-Na (the mono-sodium salts of 9-[2-(phosphonomethoxy) ethyl] adenine) in beagle dogs.METHODS: PMEA-Na and internal standard 9-(3-phosphony-methoxypropyl) adenine were isolated from plasma by protein precipitation with methanol, and then analyzed adopting multiple reaction monitoring (MRM) mode.Using Xterra MS column, the mobile phases consisted of methanol:water:formic acid (25:75:0.5) at a flow rate of 0.25 ml·min ^-1.Beagle dogs received the intravenous dosage of PMEA-Na at 1.0, 3.0 and 6.0 mg·kg ^-1.Pharmacokinetic parameters were obtained from concentration-time curves by non-linear least-squares regression using the program DAS.RESULTS: The linear calibration curve was obtained in the concentration range of 0.02 to 20 mg·L ^-1 (r =0.999), and the limit of quantitition was 20 μg·L ^-1.The withinday and internal-day precisions (RSD) were less than 6.5 % and 10.8 %, respectively.The accuracy was 97.1 %～ 107.3 %.After a single dose studies in dogs the AUC were 2.3 ±0.5, 8.2 ±1.3 and 18.5 ±1.3 mg·L ^-1·h;the t_1/2 were 3.9 ±1.8, 8.4 ±1.5 and 8.9 ±0.6 h;the CL were 0.44 ±0.09, 0.35 ±0.05 and 0.31 ±0.03 ml·h ^-1 ·kg ^-1 at the dose level of 1.0, 3.0 and 6.0 mg·kg ^-1 respectively.CONCLUSION: The analytical method is sensitive and specific for investigation the pharmacokintics of PMEA-Na in beagle dogs.

Effects of Ropivacaine and Bupivacaine on glutamate-evoked currents in cultured rat hippocampal neurons

JIANG Yu-ge, MI Wei-dong, XU Long-he, ZHANG Hong

2006, 11(4):  410-413. 

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AIM: To observe and compare the effects of Ropivacaine and Bupivacaine on glutamate-evoked currents in cultured rat hippocampus neurons.METHODS: Rat hippocampal neurons were dissociated and cultured. Glutamate-evoked currents were recorded by whole cell patch clamp recording.Effects of Ropivacaine and Bupivacaine on glutamate-evoked currents were observed.Drugs were given by pressure ejection or applicated in the bath. RESULTS: Glutamate (100mmol·L ^-1) can activate inward currents in cultured rat hippocampus neurons and this currents could be locked by non-NMDA antagonists DNQX.At concentrations of 10, 50, 100 mmol·L ^-1, both Bupivacaine and Ropivacaine could obviously decrease glutamate-evoked currents in cultured rat hippocampus neurons.At higher concentration of 50 and 100 mmol·L ^-1, the reduced amplitude of glutamate-evoked currents by Ropivacaine was larger than that of by Bupivacaine(P <0.01).CONCLUSION: Ropivacaine and Bupivacaine have obviously inhibition effect on glutamateevoked currents in cultured rat hippocampus neurons.The inhibition effect of Ropivacaine on glutamate-evoked currents is stronger than that of Bupivacaine.

Effects of Centalla asiatica combining emodin on complement C3 in glomerular mesangial cells stimulated by Tumor Necrosis Factor α

ZHU Xiao-ling, WANG Yong-jun, ZHANG Ying-hua, YANG Ru-chun, BO Shuang-shan

2006, 11(4):  414-417. 

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AIM: To investigate the effects of Centalla asiatica combining emodin on complement C3 mRNA and protein expression in BALB/C mice glomerular mesangial cells (MsC)stimulated by Tumor Necrosis Factor α(TNFα).METHODS: Cultured mice MsC from thirdfifth generation were exposed to TNFα5 ng·ml ^-1 and Centella asiatica (1, 2 and 4 μg·ml ^-1)combining emodin (0.1, 0.2 and 0.4 μg·ml ^-1) for 24 h.The transcriptase-polymerase chain reaction (RT-PCR)and enzyme-linked immunosorbent assay (ELISA)were performed to analysis complement C3 mRNA and protein expression. RESULTS: TNFαup-regulated C3 expression by MsC. This effect was inhibited by different concentrations of Centalla asiatica combining emodin in a dose-dependent manner.CONCLUSION: Centalla asiatica combining emodin inhibits C3 expression stimulated by TNFαin source of kidney local.It can protect function of kidney and delay development of nephropathic process.

Study of hemodynamics variation of cirrhosis by Compound Danshen pill

JIANG Feng

2006, 11(4):  418-420. 

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AIM: To study the variation of portal hemodynamic of cirrhosis using Compound Danshen pills. METHODS: 27 cases of compensated cirrhosis group (CCG) and 13 cases of decompensated cirrhosis group (DCCG) were treated with Compound Danshen pills.The diameter of portal vein (D_pv), cross section square of portal vein(S_pv), blood velocity of portal vein (V_pv), congestion index of portal vein(I_pv =S_pv/V_pv), and blood quantity of portal vein(Q_pv) were measured with Colored Doppler before and after the treatment.RESULTS: D_pv 、S_pv 、I_pv 、V_pv 、Q_pv were changed remarkably in CCG and DCCG after the treatment(P <0.05 or 0.01). CONCLUSION: Compound Danshen pills can obviously change the portal hemodynamic of cirrhosis.

Changes of Bcl-2 expression in apoptosis induced by resveratrol in K562 cells

WEN Zhi-zhen, YU Bao-hai, SU Hai-xiang, WEI Hu-lai, HAO Chun-yan

2006, 11(4):  421-423. 

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AIM: To observe the apoptosis of K562 cells induced by resveratrol and to explore its possible mechanisms.METHODS: MTT assay, light microscopy and electron microscopy were used to examine apoptosis in K562 cells.Expression levels of Bcl-2 and P53 antigens were mesured by FCM.Colorimetric assay was employed to detect the activation of Caspase-3.RESULTS: Resveratrol could inhibit growth of K562 cells.Typical morphological changes of apoptosis were observed through light microscopy and electron microcopy.Expression of Bcl-2 significantly decreased after application of resveratrol.Caspase-3 could also be activated by resveratrol. CONCLUSION: Resveratrol induces apoptosis in K562 cells by activating Caspase-3 via a Bcl-2-dependent pathway.

Effect of IFN-γ on A549 cell proliferation and expression of P21

XIA Hui, YU Chang-hai, YU Jian-qi, LI Jie, ZHANG Bao-shi, LI Ying-jie

2006, 11(4):  424-426. 

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AIM: To observe the effect of IFN-γ on the A549 cell proliferation and the expression of P21 protein. METHODS: A549 cells were cultured and incubated with IFN-γ.MTT colorimetric method was used to observe the effect of IFN-γ on the A549 cell proliferation, and the change of P21 protein expression was observed by the immunocytochemistry.RESULTS: Compared with those of control group, the results of MTT showed that IFN-γ could reduce the A549 cell proliferation.From the experiment of immunocytochemistry, the expression of P21 protein increased significantly after treatment with IFN-γ.CONCLUSION: IFN-γ can induce the expression of P21 protein and inhibit the A549 cell proliferation and maybe provide the new idea for the therapy of lung cancer.

Role of bradykinin B₂ receptor in AT₁ antagonist inhibition of Ang Ⅱ-induced cardiomyocyte hypertrophy in neonatal rats

ZHAO Yan-feng, XU Jiang, ZHENG Ya-ping, WANG Hong, QU Xue-ju

2006, 11(4):  427-431. 

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AIM: To investigate the role of the bradykinin (BK) B₂ receptor in the inhibitory effect of valsartan on angiotensin Ⅱ (Ang Ⅱ)-induced cardiomyocyte hypertrophy.METHODS: Neonatal rat cardiomyocytes were randomly divided into 6 groups:control, Ang Ⅱ, valsartan, Ang Ⅱ +valsartan, Hoe-140 (a specific BK B₂ receptor antagonist) and Ang Ⅱ +valsartan +Hoe-140. Flow cytometry (FCM) was used to evaluate the size and protein content of cardiomyocytes.Nitric oxide (NO) and intracellular cyclic GMP (cGMP) were measured by colorimetry and radioimmunoassay. RESULTS: 10 ^-7 mol·L ^-1 Ang Ⅱ significantly increased the size and protein content of cardiomyocytes compared to control (P < 0.01 for both), which was inhibited by 10 ^-5 mol·L ^-1 valsartan (P <0.01).10 ^-6 mol·L ^-1 Hoe-140 partially blocked the inhibitory effects of valsartan (P <0.05 or P <0.01 vs.Ang Ⅱ +valsartan, respectively).In the Ang Ⅱgroup, NO was markedly decreased (P <0.01 vs. control);valsartan significantly increased NO and intracellular cGMP compared to the Ang Ⅱgroup (P <0.01 for both), and the effect of valsartan was attenuated by Hoe-140 (P <0.01 or P <0.05 vs.Ang Ⅱ +valsartan, respectively).CONCLUSION: The BK B₂ receptor may partially mediate the antihypertrophic action of valsartan in Ang Ⅱ-induced cardiomyocyte hypertrophy, and the elevation of NO and cGMP may contribute to the cardioprotective effects of BK.

Protective effects of genistein against intestinal ischemia-reperfusion injury in rats

ZHAN Gong-hao, LI Xing-wang, ZHANG Bing, SHANG You

2006, 11(4):  432-435. 

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AIM: To investigate the effects of genistein on intestinal ischemia-reperfusion injury in rats and the possible mechanism.METHODS: Twenty-four Wistar rats were randomly divided into three groups (n = 8):sham operation group, intestinal ischemia-reperfusion injury group(model group) and genistein group.In model group, intestinal damage was induced in rats by clamping the superior mesenteric artery for 1 h, followed by 2 h of reperfusion.Genistein group received genistein 1.0 mg·kg ^-1 i.v.5 min before intestinal ischemia.In genistein group the superior mesenteric artery was o exposured without other treatment.At 2 h of reperfusion, blood samples were collected to measure plasma level of D-lactate and intestines were removed to assay histopathological changes, wet-to-dry weight (W/D) ratio, myeloperoxidase (MPO) activity and intercellular adhesion molecule-1 (ICAM-1) protein expression.RESULTS: W/D ratio, MPO activity, expression of ICAM-1 protein in the intestine tissues and D-lactate level in plasmawere significantly higher in model and genistein group than those in sham operation group (P <0.05 or 0.01).All these indices were significantly lower in genistein group than those in model group (P <0.05 or 0.01).The morphology of lung tissues in sham operation group was basically normal, that in model group was markedly damaged, and that in genistein group was lightly damaged. CONCLUSION: Genistein has protective effect on intestinal ischemia-reperfusion injury in rats.The underlying mechanism may involve an inhibition of neutrophilic recruitment and activity in intestine caused by a down-regulation of ICAM-1 expression.

Protective effects of zafirlukast on focal cerebral ischemia-reperfusion injury in rats

LIU Ying, YU Juan, XU Lin, CHEN Chong-hong

2006, 11(4):  436-439. 

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AIM: To study the protective effects of a leukotriene receptor antagonist zafirlukast on focal cerebral ischemia reperfusion injury (CIRI) in rats and its possible mechanisms.METHODS: Reversible middle cerebral artery occlusion(MCAO) model was produced by intraluminal suture technique, and reperfusion was begun after 2 h of occlusion.Zafirlukast was intragastrically administrated at 0 and 12 h of the reperfusion.After 24 h reperfusion the infarct volume of the brain, the cerebral edema degree and the permeability of blood brain barrier were estimated.The activity of myeloperoxidase (MPO), the contents of maleic dialdehyde (MDA), glutathione peroxidase (GSH-PX), nitric oxide (NO) and inducible nitric oxide synthase (iNOS) in the brain tissue were measured. RESULTS: Zafirlukast could decrease the infarct volume of the brain, lessen the degree of cerebral edema and reduce permeability of blood brain barrier.It could also decrease the content of MDA, the level of NO, the activity of iNOS and increase the activity of GSH-PX in the brain tissue significantly.The 40 mg·kg ^-1 dose of zafirlukast could reduce the activity of MPO.CONCLUSION: The highly selective leukotriene receptor antagonist zafirlukast can prevent cerebral ischemia reperfusion injury by depressing permeability of the blood brain barrier, inhibiting inflammation reaction, decreaseing lipid peroxidation and reducing toxic action of NO.

Determination of metadoxine in human serum by HPLC and its pharmacokinetic studies

YUAN Gui-yan, WANG Ben-jie, WEI Chun-min, GUO Rui-chen

2006, 11(4):  440-443. 

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AIM: To establish an HPLC method for determination of metadoxine in human serum and to study the pharmacokinetics of metadoxine in healthy Chinese volunteers.METHODS: The volunteer serum samples were deproteinized and separated on a Diamonsil C₁₈ column (250 mm ×4.6 mm, 5 μm), eluted with the mobile phase of methanol-5 mmol·L ^-1 ammonium acetate (14:86, v/v) at a flow rate of 1.0 ml·min ^-1 and detected at 286 nm.RESULTS: The linear range of the calibration curve for metadoxine was 0.2 ～ 12 μg·ml ^-1, and the low limit of quantitation (LLOQ) was 0.2 μg·ml ^-1.The absolute and relative recoveries were 73.31 %～ 82.00 % and 91.08 %～ 95.69 % respectively.Within-day RSD and between-day RSD were less than 6.3 % and 4.3 %.CONCLUSION: The assay method is simple, sensitive, accurate, and reproducible and was successfully applied for the pharmacokinetic study of metadoxine in healthy volunteers.

Measurement of recombinant human glucagon-like peptide-1 (7-36) concentration by ELISA kit methods

ZHENG Zhuan-jie, FANG Yi, WANG Rui

2006, 11(4):  444-447. 

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AIM: To qualitatively detect the concentration of recombinant human glucagon-like peptide-1 (7-36) [rhGLP-1(7-36)] in human blood.METHODS: RhGLP-1 (7-36) concentrations of standard and blood samples were detected by ELISA kits.RESULTS: The parameters of specificity, sensitivity, detection limits, reproducibiltiy and recovery can meet the requirements for pharmacokinetic studies.CONCLUSION: The concentrationmeasuring method of rhGLP-1(7-36) in blood samples using ELISA kit produced by LINCO company can meet the detection methods of biological production, which can be used as a measuring method of rhGLP-1(7-36) concentration and for its pharmacokinetic studies.

Effects of crocetin on formation of advanced glycation end products and expression of releptor for advanced glycation and prodmts protein in diabetic rats

XIANG Min, QIAN Zhi-yu, ZHOU Cheng-hua

2006, 11(4):  448-452. 

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AIM: To study the effect of crocetin on the formation of advanced glycation end products (AGEs) and receptor forAGEs (RAGE)protein expression in diabetic rats induced by streptozotocin (STZ).METHODS: Rats were injected STZ in tail vessel with a dose of 45 mg·kg ^-1.3 d later, the rats whose blood glucose were over 11.1 mmol·L ^-1 were regarded as diabetic rats, and were divided randomly into two groups:diabetic mellitus (DM)group, crocetin (50 mg·kg ^-1, po)group.At the same time, 8 normal rats were regarded as control group. After 21 d treatment, The levels of fasting blood glucose (FBG), serum fructosamine (FMN)and glycosylated hemoglobin (GHb)were measured.The contents of AGEs in aorta and mesenteric vessel were detected by fluorospectrophotometry.HE staining for mesenteric aorta was performed, and RAGE protein expression was studies with immunohistochemical method.RESULTS: Compared with DM group, crocetin did not decrease the level of FBG.However, it could decrease the levels of FMN and GHb in blood and AGEs in aorta and mesenteric vessel (P <0.01 or 0.05).HE staining demonstrated injure of mesenteric aorta attenuated and RAGE protein expression decreased after crocetin treatment.CONCLUSION: These results suggest that crocetin not only inhibit nonenzymatic glycation reaction but also reduce RAGE protein expression in diabetic rats, which may contribute to attenuate diabetic vascular complications.

Protective effects of penehyclidine hydrochloride on transient forebrain ischemia reperfusion injury in gerbils

MA Teng-fei, JIN Rong, ZHANG Jing, GU Shu-ling, DUAN Shi-ming

2006, 11(4):  453-457. 

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AIM: To study the protective effects of penehyclidine hydrochloride (PHC)on transient forebrain ischemia reperfusion injury in gerbils.METHODS: The model of transient forebrain ischemia reperfusion was established in gerbils by bilateral carotid artery clamping. The effects of PHC on neurological function scores and the morphous of hippocampal pyramidal neuron of gerbils were observed after receiving transient forebrain ischemia reper-fusion.SOD activities and contents of MDA in the hippocampus and cortex of gerbils were measured.RESULTS: In the groups of PHC 0.08, 0.24 mg·kg ^-1 and atropine, the stroke index was decreased, compared with the ischemia-reperfusion group after the gerbils received transient forebrain ischemia reperfusion for six hours. PHC could reduce the degree of injury in hippocampal pyramidal neuron after ischemia reperfusion for three days. CONCLUSION: PHC has protective effects on transient forebrain ischemia reperfusion injury in gerbils.

Tolerability and pharmacokinetics of multiple-dose Ceftriaxone Sulbactam (4:1) injection in Chinese health volunteers

WANG Jin, XIAO Yong-hong, LU Yuan, KANG Zi-sheng, ZHANG Ming, LIANG Jun, LIU Yan, ZHANG Man, LI Tian-yun

2006, 11(4):  458-463. 

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AIM: To evaluate the pharmacokinetics of multiple-dose Ceftriaxone/Sulbactam (4:1) injection in Chinese health volunteers.METHODS: The serum samples and urine samples of 12 healthy volunteers were collected after injecting 2.50 g Ceftriaxone/Sulbactam (4:1) injection for 7 days.RESULTS: All health volunteers were well tolerated.The pharmacokinetic parameters were calculated by DAS software.The average of C_max was 202.60 ±26.31 mg·L ^-1, C_av was 60.65 ±8.85 mg·L ^-1, AUC_ss was 1455.68 ±212.41 mg·L ^-1 ·h, DF was 3.36 %, FI was 96.77 %.The 72 h cumulative urinary excretion rate of Ceftriaxone was 43.61 %±10.23 % and the 12 h cumulative urinary excretion rate of Sulbactam was 71.61 %±10.06 %.CONCLUSION: 2.50 g multiple-dose Ceftriaxone Sulbactam (4:1) injection is well tolerated in the health volunteers.According to the results of pharmacokinetic parameters, there is no pharmacokinetic change between the two drugs from the compound preparation, and there is no drug interaction between them.

Effects of ST-1 against focal cerebral ischemia-reperfusion injury in rats

DU Wen-feng, ZHAO Lei, XU De-yi

2006, 11(4):  464-466. 

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AIM: To demonstrate the protective effects of ST-1 against focal cerebral ischemia-reperfusion injury in rats.METHODS: The model of focal ischemiareperfusion was induced by middle cerebral artery occlusion 2 h followed by reperfusion 22 h in rats.Neurological deficit scores were evaluated.Infarct size, malondialdehyde (MDA) content and superoxide dismutase (SOD) activity were measured, pathological changes of neurons in hippocampal CA1 region were observed.RESULTS: Compared with vehicle group ST-1 at dose of 10 and 20 mg·kg ^-1 could reduce the infarct size, MDA content, enhance SOD activity and relieve neurons injury in hippocampal CA1 region in dose-dependent way;ST-1 at dose of 20 mg·kg ^-1 could also improve neurological function. CONCLUSION: ST-1 can protect brain tissue from focal ischemia-reperfusion injury.

Changes in immune function of children patients with repeated respiratory infection and effect of treatment with nucleotide and casein injection

WU Lin, CUI Min-xian, XIA Xiao-qing

2006, 11(4):  467-469. 

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AIM: To explore the changes in immune function children patients with repeated respiratory infection (RRI) and the influence of nucleotide and casein injection on it.METHODS: 45 patients with RRI were arranged in therapy group and were injected with nucleotide and casein injection.32 patients with acute respiratory infection were arranged in control group who were not injected with nucleotide and casein injection.The effect of treatment, change of IgA, IgG, IgM, T-lymphocyle subgroups and reaction intensity of PHA were observed.RESULTS: There were very significant decline of IgA and IgG level (P <0.01, P <0.05) in RRI children than those in control group.The IgA level in RRI increased obviously after treatment with nucleotide and casein injection (P <0.05).There were very significant decline of CD₄, CD₄/CD₈ and NK cells levels (P <0.05, P < 0.01) in RRI children than those in control group.The CD₄, NK cells levels in RRI obviously increased after treatment with nucleotide and casein injection (P < 0.05).The roseola diameter of PHA in RRI children declined significantly (P <0.05).There were obviously increase in roseola diameter of PHA after treatment with nucleotide and casein injection (P <0.05).CONCLUSION: Nucleotide and casein injection boosts and improves cell immunity and fluid immunity.

Clinical observation of Reduning injection in treatment of patients with acute upper respiratory tract infections

HUANG Xiao-min, LIU Yu-jie, HE Yu-zhou, CHEN Fang-fan, WANG Yun-kai

2006, 11(4):  470-473. 

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AIM: To evaluate the efficacy and safety of Reduning injection in treating acute upper respiratory tract infections.METHODS: Seventy-one patients were randomly assigned to two groups.Fifty-three patients in trial group were administrated with Redunimg injection 20 ml, iv gtt, qd, while the other in control group were administrated with Qingkailing injection 30ml, iv gtt, qd. The period of treatment was 3 d for each group.RESULTS: On d 3 after treatment, the total clinical effective rate were 98 % in the trial group and 94 % in the control group with significant difference between two groups (P <0.01), while the total effective rate of Chinese traditional medical symptoms were 98 % in the trial group and 94 % in the control group with significant difference between two groups (P <0.05).In trial and control groups no adverse reactions was found.CONCLUSION: Reduning injection is an effective and safe agent in treatment of patients with acute upper respiratory tract infections.

Change of decreasing blood pressure on pain threshold of spontaneously hypertensive rats

LIU Xiao-yu, WU Dang-fang, ZHOU Yan, LI Jie, ZHANG Yan-hai

2006, 11(4):  474-476. 

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AIM: To study the effect of decreasing blood pressure on mechanical and heat pain sensitivity in spontaneously hypertensive rats.METHODS: 15 SHRs were intramuscularly given reserpine (1 μg·kg ^-1·d ^-1) on day 4-11.Blood pressure, paw withdrawal mechanical threshold (PWMT) and paw withdrawal thermal latency (PWTL) were measured every day.RESULTS: After the therapy of reserpine in spontaneously hypertensive rats, blood pressure decreased by 50 mmHg, mechanical and heat pain threshold were both decreased (P < 0.05).CONCLUSION: Spontaneously hypertensive has reversible effect on spontaneously hypertensive rat nociceptive system.

Ethic review in clinical research:women and pregnant women

LIU Shen-lin, WANG Xiu-qin, XIONG Ning-ning, LI Qi-yi, JIANG Meng, LIU Fang, ZOU Jian-dong, GAO Wei-min, XUE Xue-kun

2006, 11(4):  477-480. 

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Ethics Committee need to have special consideration when reviewing clinical research involving pregnant women or women of reproductive age by the fact that it may present risks and potential benefits to the woman herself, the pregnancy, the fetus as well as to the person the fetus is destined to become.Special ethical concerns regarding clinical research involving women are as follow:The potential for becoming pregnant during a study should not, in itself, be used as a reason for precluding or limiting participation.However, a thorough discussion of risks to the pregnant woman and to her fetus is a prerequisite for the woman' s ability to make a rational decision to enroll in a clinical research.Special ethical concerns regarding clinical research involving pregnant women are as follow:Evaluation of risk-benefit ratio should be considered from two aspects (i.e., pregnant woman, the fetus), taking into account the categories of research as well.Research in this population should be performed only if it is relevant to the particular health needs of a pregnant woman or her fetus, or to the health needs of pregnant women in general, and, when appropriate, if it is supported by reliable evidence from animal experiments, particularly as to risks of teratogenicity and mutagenicity.