Table of Content

Volume 5 Issue 2
26 June 2000

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Protective effects of al lopregnanolone against differentseizuremodels in mice

YU Rong, YAO Ming-Hui

2000, 5(2):  97-100. 

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Aim To examine the protective effects of allopreg nanolone against seizureon different animal models.Methods The protective Effects of allopreg nanolone against maximal electrical seizure(MES)and picrotoxin-induced seizurewerestudiedin C 57 mice 15 minutes after vehicle or drug intraperitoneal administration.Results In the MEStest, we found that pretreatment with the phenobarbital or allopregnanolone produced a dose-dependent protective Effect against seizure.The potency(ED₅₀ value)of phenobarbital in the MEStest was 2.40 mg· kg^-1, with 95 % confidence interval range from 1.22 to 4.72 mg· kg^-1.The potency(ED₅₀ value)of allopregnanolone in the MEStest was 0.086 mg·kg^-1, with 95 % confidence interval range from 0.037 to 0.201 mg· kg^-1, which was significantly higher than that of phenobarbital (P < 0.01).The combination study of half ED₅₀ values of phenobarbital and allopreg nanoloneresultedin a 80 % of protective effectin MEStest, which was higher than 50 % produced by either phenobarbital or allopreg nanolone at their ED₅₀ values respectively. This resultindicated that therewas a synerg ismbetween phenobarbital and allopregnanolone in theiranticonvulsant activities.In the picrotoxin test, we found that pretrea tment with the allopreg nanolone alsoproduced a dose-dependent protective effect against picrotoxin-induced seizure.The potencyof allopregnanolone in the picro toxin seizuretest was 0.123 mg· kg^-1, with 95 % confidence interval range from 0.058 to 0.263 mg· kg^-1.Conclusion Allopregnanolone(ip)could protect differentseizures in a dose-dependent manner, had a higher potencythan phenobarbital, and had synerg ismwith phenobarbital in the MEStest.

Anovel animal model ofintra-abdominal adhesion and quantitative evaluation with relatedindices¹

ZHENG Qing-Shan, GUI Chang-Qing, SUN Rui-Yuan, WANG Ming

2000, 5(2):  101-105. 

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Aim To set up a novel animal model ofintra-abdominal adhesion and tode termine whether the tissue plasminogen activator activity (PAA)in exudate can be taken as an indicator to judge the formation of the adhesion.Methods Rats wererandomly dividedinto 2 groups. Each animal in both groups was opened the abdominal cavity via midline laparo tomy witho ut any disinfectant measures.2-cm section from the cecal end was clamped and lig ated, 1-cm cecum of the section was cut, and another 1-cm end from the ligated site was kept.After the contentin the end was extruded, the cecum was put back without using any antibacterial agent.Beforethe skin closure, an Effective combination AMD (allantoin, metronidazole and dexamethasone in combination), was g iven (ip)according to 1.5 ml per 100 g body weight (60.6 mg·kg^-1).The control group was injected (ip)the samevolumeof normal saline. After 6 h, the exudate was extracted from drainage-tube, with therats varying posture, and after 1 kw, therats werekilled forexamining the intra-abdominal adhesion.The values of PAA of exudate in both groups wereanaly zed by therelative operating characteristic curve (ROC).Results In the control group, all 20 rats formed the adhesions, the amo unt of exudate = (1.25±0.09)ml, the numberof WBC(×103) = (23.1±6.6)mm³ and PAA = (0.9±0.4)IU·ml^-1 in the exudate of abdominal cavity.In AMD group, however, therewas not the adhesion formations (0/20), the amount of exuade was (0.52±0.04)ml (P<0.01), the numberof WBC (×103)(10.6±4.2)mm³ (P<0.01), and PAA (23.1±6.6) IU·ml^-1(P<0.01)in exuade.ROCanalysis indicated thati f PAA >1.24 IU·ml^-1 in the exuade, the adhesion was difficult toform, and vice versa.Conclusion This animal model can be taken as an effective to olto evaluate the human adhesion related to multi-links on the pathog enesis, and the PAA in exudate an indicator to judge intra-abdominal adhesion formation.

Research of relationship between protein kinase and ATP-sensitive potassium current¹

ZHAO Ming-Gao, ZHAO De-Hua, ZHANG Yan-Feng, XIONG Xiao-Yun, YAO Xiu-Juan

2000, 5(2):  106-107. 

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Aim To observe the effects of protein kinase A (PKA), protein kinase C(PKC)inhibitorand dephosphory lating agent on ATP-sensitive potassium current($I_{KATP}$)of rat ventricularcardiomy ocytes andinvestiga te the mechanismof cromakalim opening $I_{KATP}$.Methods Whole-cell patch-clamp was used torecord $I_{KATP}$.Results Cromakalim (1 μmol·L^-1)was shown to induce $I_{KATP}$ at the holding potential of 10 mV, 37 ℃.When added to the pipet tesolution, the PKA inhibitor PKI(6 ~ 22)amide (1 μmol·L^-1)caused production of $I_{KATP}$, just as cromakalim did, whilethe PKC inhibitor calphostic C(1 μmol·L^-1)showed no Effect.Moreover, addition of the dephosphory lating agent, butanedione monoxime(5 mmol·L^-1), to the bath also stimulated $I_{KATP}$.Conclusion The mechanismof cromakalim opening $I_{KATP}$ is due to the inhibition of PKA (not PKC).

Inhibition of midazolam on macroscopic sodium currents in ratsympathetic neurons

ZHENG Ji-Jian, ZHUANG Xin-Liang, LIU Bao-Gang, DU Dong-Ping, XU Guo-Hui

2000, 5(2):  108-111. 

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Aim The effects of midazolam on the whole-cell sodium currents in ratsympathetic neurons werestudied to explorethe mechanisms whereby midazolam mediates hypotension.Methods Whole-cell patch-clamprecordings wereperformed on enzymatically isolated ratsuperior cervical sympathetic neurons.Results Midazolam do se-dependent ly blocked the whole-cell sodiumcurrents evoked by a voltagestep to 0 mV from a holding potential of-80 mV with a mean drug concentration required toproduce 50 % currentinhibition (IC₅₀)values of 18.35 μmol·L^-1; Clinically relevant concentration of midazolam(0.3 μmol·L^-1)reduced sodium peak cur rents by 19.98%(P<0.05);3 μmol·L^-1 midazolam didn't affect the shape of I-V curves of sodium cur rents, butreduced the peak values by 21.75%.Similarly, 3 μmol·L^-1 midazolam didn't cause significantshif tin the voltage-dependence of activation curve either.However, 3 μmol·L^-1 midazolam caused a substantial hyperpolari zingshif t of the steady-state inactivation curve (7.75 mV, P<0.05), thatis the conditioning pulse potential at whih half-max imal channel is inactiva ted (V 1/2)was changed from-40.39 mV to-48.14 mV.Conclusion Clinically relevant concentration of midazolam has significantinhibition on sympathetic neurons.This inhibition is dose-dependent and relavant to the inactivation of sodium channel.The circulation depression of midazolam may berelevant to the di rectsuppresion of sympathetic neurons.

Theoretical study on electronic structures and medical properties of Pt complexes as antitumor drugs¹

HAN Ju-Guang, PANG Wen-Min, SHI Yun-Yu

2000, 5(2):  112-116. 

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Aim To theoretically study on therelation between electronic structures and its medical properties.Methods The theoretical study of the electronic structures andits interaction micromechanismof Pt compounds was carried out by density functional method.Results and Conclusion The computational results indicated that the exchange dy namic equilibrium ofinteraction be tween first g eneration or second generation medical molecule and DNA could berepresented by the interaction streng th of Pt-Cl bond.The order is DDPC<Pt(en)₂CL₂<PtC₄N₃H₁₃Cl<DDPB<DDPA.The toxic-side Effect and antitumour do sage wereanalyzed successfully.Our theoretical results werein go od agreement with the experimental results. The equilibrium geometry was optimized and the stability was discussed.The electronic affinity, ionization potential and Mulliken populations werealsocalculatedin this article.

Effect of methyl polyglycoside on cardiachemodynamics in experimental heart failurecats

LUO Xue-Ya, YANG Yu-Mei, LUO Lin

2000, 5(2):  117-119. 

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Aim The effect of Methyl Polyg ly coside (MPG)on cardiachemody namics in experimental heart failurecats was studied.Methods Model of experimental heart failurewas establishedin anesthetized cats.MPG(100 mg·kg^-1, 200 mg·kg^-1, iv)was administered by intravenous infusion and cardiachemody namics parameters weremeasured by using polygraph and electromag netic f lowmeter.Results LVSP,±d p/d t max, CO, CI, LVWI and MAP wereobvio usly increased, LVEDP was decreased and TPVR was not markedly alteredin both low and high do se MPG group.HR was not obviously changedin low-dose group, butit was light ly quickenedin high-dose group.Conclusion MPG has the actions of enhancing myocardial contraction, improving my ocardial compliancyand left ventricularsy stolic and diostolic function andincreasing cardiacoutput and arterial blood pressurein heart failurecats caused by Pentobarbital sodium.These show MPG is beneficialtoreleasing heart failure.

Effect of total paeony glycoside(TPG) andits mechanismon calcium overloading injury in cultured PC12 cells

HE Li-Na, YANG Jun, HE Su-Bing

2000, 5(2):  120-122. 

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Aim The protective Effect and mechanismof TPG on PC 12 cells in calcium overloading injury models werestudied.Methods Two injury models induced by KCl and NMDA wereused to assay the action of TPG in cultured PC 12 cells.Results The morphological examination revealed that TPG possessed obvious protective effects on PC12 cells in injury models.MT T and LDH measurementindicated that TPG increased the numberof live cells and reduced the extent of cell injury significantly.TPG alsolessened the concentration of calcium ion in cytoplasm.Conclusion T PG protected rat PC 12 cells against twocalcium overloading injuries Effectively in vitro.I ts actions may deal with anti oxidation, inhibition of NO production and blocking of bothty pes of calcium channel.

Effect of extracts of astralus on learning, memory andimmune function in mice

ZHANG Yan, MING Liang, LI Wei-Ping, LI Jing-Pei, CHEN Min-Zhu

2000, 5(2):  124-126. 

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Aim The effect of extract s of astralus(EA)on learning, memory andimmune function of C TX treated mice was observed.Methods The step-down test was adopted to investiga te learning and memory in mice;the method of enveloping CRBC was adopted to explorethe function of macrophage in abdominal cavity;3H-TdR marking method was used to observe the prolifernation of Tlymphocytes and the method of ELISA was applied to measurethe concentration of IFN-γin blood.Results EA (25 mg·kg^-1, 50 mg·kg^-1, ig, 21 d)could boost learning and memory, enhance the phagocytic activity of monocytes and the proli feration of Tlymphocytes of C TX treated mice, andincrease the concentration of IFN-γin blood of CTX treated mice.Conclusion EAnot only promote learning and memory, butregulate immune function.

Effect of human placental extract on the lipoprotein-cholesterol metabol ism

CUI Wen-Ji, YANG Jing-Wen, LV Zhong-Zhi

2000, 5(2):  127-130. 

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Aim The Effect and mechanismof human placental extract(HPE) on the lipoprotein-c holesterol metabolism, peroxidation and the function of platelet agg reg ation in hyperlipaemiarats wereabserved.Methods Wistarrat with hyperlipaemia models weregiven each HPE 0.4 ml (100 g)^-1·d^-1 throug h lavage for 12 days.The serum levels of TG, TC, LDL-C, HDL-Cand HDL 2-C in its subgroup weremeasured.The activies of LPO and SOD in both blood and liver tissue weredeter mined.The Effect of HPE on lipidosis of liver wereabserved by fat dy eing.The levels of 6-keto-PG F1α, TXB 2 in plasma and maximum platelet agg regation rate were measured by ELASA.Result The levels of HDL-Cand HDL2-C wereincreased (P<0.01)whilethe levels of TG, TCand LDL-C weredecreased (P<0.01).The levels of LPO in serum and liver tissue decreased obviously and SOD activity increased (P<0.01).The lipidosis in liver was inhibited and adipose hollow spacereduced obviously.The levels of PG I2 in plasma increased (P<0.01), the level of T XB 2 was no t changed and platelet agg reg ation rate was decreased obviously.Conclusion HPE may improve the lipoprotein-cholesterol metabolism, enhance the antioxidation andinhibite platelet aggregation and the formation of lipidosis of liver in hyperlipemiarats.HPE is good for inhibition of the formation and development of atheoscleorsis.

Effect of triptolide on local stimulation

LIN Jian-Feng, ZHU Hui, ZHENG You-Lan

2000, 5(2):  131-133. 

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Aim The effect triptolide(Tri)on local stimulation was observed.Methods Trisolution in different concentrations was appliedin rabbits, rats and mice and therespenses wereobserved.Results 1.11, 2.22 and 4.44 mmol·L^-1 of Tri induced obviousery thema and edema on both intact skin andinjured skin of rabbits.The pathological histology revealed the evidentinf lammation in scarf skin and corium 2.22 mmol·L^-1 and 4.44 mmol·L^-1 of triptolide significantly induced swelling of auricle in mice.0.55 mmol·L^-1 and 1.11 mmol·L^-1 of Trisignificantly induced swelling of planta in rats.Theresponse ofinflammation reached topeak at the third day after hypodermic injection and lasted a week.Tri also significant ly induced pain reaction and enhanced the permeability of capillary after local injection in mice.Conclusion Tri has a local stimulation effect andinduces inflammation which can no t be antagoni zed by its anti-inflammation Effect.

Mornitoring of the enantiomers of (±)-trans tramadol andits active metabol ite in the serum of postoperative patients after differentintravenous doses of (±)-trans tramadol hydrochloride injection

LIU Hui-Chen, YANG Yan-Yan, HOU Yan-Ning, WANG Ya-Li

2000, 5(2):  134-137. 

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Aim To investig ate therelationship between the clinical actions and the serum concentrations of the enantiomers of (±)-trans tramadol andits active metabolite.Methods 20 postoperative patients weredividedinto two groups and given multiple intraveno us doses of (±)-trans tramadol hydrochloride injection, 400 mg·d^-1 (group A)or 300 mg·d^-1 (group B).The blood samples weretaken at 38 h after the initial dose.The concentrations of the enantiomers of (±)-trans tramadol andits active metabolite, (±)-trans O-demethy ltramadal weredetermined with high performance capillary electrophoresis(HPCE).Results The concentrations of the enantiomers of (±)-trans tramadol, the f requencyand serious level of adversereactions werehigher in group A than in group B.The concentrations of the enantiomers of (±)-trans O-d emethy ltramadal, the analgesic Effect weresimilarbetween group A and group B.Conclusion Thereis much closer relation between the analgesic Effect and the concentration of (+)-O-d emethy ltramadal.The f reque ncyand serious level of adversereactions may be at tributed to the higher concentrations of the enantiomers of (±)-trans tramadol, which arecaused by the saturated metabolism.

Relative bioavalability of hydrochloride eperisone granule in healthy volunteers

GUO Rui-Chen, WANG Ben-Jie, ZHANG Wen-Dong, LI Chao-Wu, LI Zhi-Li

2000, 5(2):  138-141. 

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Aim Therelative bio avalability of hydrochloride eperisone granule in 10 healthy volunteers was studied.Methods The time-p lasma concentrations of hydrochloride eperisone granule, as test drug, and my onal, as reference drug, weredetermined by GC-MS, with tolperisone senuingas internal standard.The pharmacokinetic parameters of both reference and test drug werecalculated and analyzed with two-one side test and confidential intervaltest.Results Theresults showed that the AUC^0-8, AUC^0-∞, C_max, T^peak, t^1/2 (α)and t^1/2(β) were(17.9±1.3)ng·h·ml^-1 and(18.6±1.6)ng·h·ml^-1, (19.1±1.2)ng·h·ml^-1 and (20.2±1.6)ng·h·ml^-1, (5.2±0.5)ng·ml^-1 and (5.4±0.5)ng·ml^-1, (1.05±0.18)h and (1.08±0.23)h, (0.78±0.13)h and (0.82±0.14)h, (1.8±0.3)h and (1.8±0.3)h, respectively.Therelative bioavalability of test drug was (105±5)%.Conclusion I t can be concluded that the test and reference arebioequivalented be tween individuals, preparations and periods.

Relative bioavailablity of cefacloreffervescent tablets in human volunteers

QIU Fu-Rong, JI Jin-Mei, CHENG Bo, ZENG Zhao-Hong, SUN Hua, MAO Guo-Guang

2000, 5(2):  142-144. 

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Aim To study relative bioavailablity of cefacloreffervescent tablets in healthy volunteers.Methods According to the crossover design, Avolunteers wereeach orally g iven a sing le does of the 0.75 g cefacloreffervescent tablets and cefaclor capsules with an interval of 5 days between the twoformulations.The plasma concentrations of the drug weredetermined by RP-HPLC.Pharmacokinetic parameters wereobtained by A TPK programe, and calculated on the basis of open sing le compartment model.Results After a single oral dose, the peak levels in plasma averaged C_max(31.27±5.81) μg·ml^-1 and(30.56±5.25) μg·ml^-1 at (0.58±0.12) h and(0.73±0.17) h and AUC_0~4(35.48±4.65) μg·h·ml^-1 and (35.89±2.90) μg·h·ml^-1 for tablet and capsule, respectively.Conclusion Theresult show s that twoformulations arebioequivalence.

Effect of baoxinbaofilm on plasma endothel in and nitricoxide levels in patients with stable angina pectoris

WANG An-Cai, CHA NG Bao-Hua, YANG Shan-Ying, NI Wei-Hua, YANG Hao, HUANG Jia-Sheng

2000, 5(2):  145-146. 

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Aim To study the Effect of Baoxinbaofilm on endothelin(ET)and nitricoxide(NO)secretion in patients with stable angina pectoris(SAP).Methods 76 patients with SAP wererandomly dividedinto two groups, with 40 cases in the baoxinbao group plastered with baoxinbaofilm and 36 cases in the isosorbide dinitrate groupreceiving isosorbide dinitrate. The levels of plasma E T and NO beforeand after treatment wereobserved.Results The concentrations of plasma E T wereincreased and plasma NO reduced significant ly in the SAP patients respectively, as compared with those in the control group(all P<0.01).After treatment the metabolic imbalance of ET and NO was improved markedly in both Baoxinbao andisosorbide groups(P<0.05, P<0.01), but the imbalance of ET and NO in the Baoxinbao group was improved moreobviously than thatin the isosorbide group(P<0.05).Conclusion Baoxinbaofilm can obviously improve the metabolic imbalance of ET and NO secretion,which results in the effective alleviation of angina pectoris in patients with SAP.

Powderedinjections of luotai protect against ISO-induced experimental myocardial ischemia model on rats

LEI Xiu-Ling, DONG Xue-Feng, LI Leng, CHEN Zhi-He

2000, 5(2):  147-149. 

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Aim Pow deredinjections of luo tai consist of total saponins of panax notoginseng(PNS) which protect againstischemia injury from my ocardial reperfusion injury.Methods ISO-induced acute my ocardial ischemia model in rat was made, which decreased S-T sigments in ECG.Luotai after intravenous injection ororal can protect against S-T sigmentsignificantreduction and ΣS T after ISO induced acute my ocardial ischemia.Results Luotai 50 mg·kg^-1 and 100 mg·kg^-1 significantly inhibited S-T sigment decreases.Conclusion Luo tai protect ISO induced acute my ocardial ischemia and has dose-dependent Effect.T his ISO-induced acute my ocardial ischemia model in rat has somesignificant advantages, forexample, higher stability, good duplication, quickly filtrates, easily masters.

Effect of PNS on MCAO-induced cerebral ischemia

SHI Yi-Ju, NIE Heng-Huan, XING Guo-Qing, MENG Qing-Hua, LI Juan

2000, 5(2):  150-153. 

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Aim The Effect of panax notoginseng(PNS)andits monomers Rb₁ and Rg₁ on cerebral blood f low (CBF)in rats with middle cerebral artery occlusion(MCAO)was observed.Methods Sixty Wistarrats wererandomizedinto 7 groups, which weresubdividedinto 5 MCAO experimental groups and one MCAO control group operated via internal artery and one sham-operated(SO) control group undergone the samesurgical procedurebut without MCAO.3 MCAO experimental mental groups weregiven different drugs respectively in the doses of Rg₁ 20 μg·kg^-1 (iv);Rb₁ 20 μg·kg^-1 (iv)and nimodipine.Nim 5 μg·kg^-1 (iv)30 minutes beforeandimmediately after MCAO.Ano ther 2 MCAO groups weregiven PNS(200 mg·kg^-1 or 400 mg·kg^-1, po.)for 10 days and MCAO was observed 30 minutes after the final administration.Results CBF in Rb₁ group, Nim group and PNS group was increased signi ficantly (P<0.01), as compared with thatin the MCAO control group, whereas in Rg₁ group it was decreased obviously(P<0.05).Electron microscopic structural analysis indicated that Rb₁, Rg₁, PNS and Nim obviously alleviated brain injury and neuron necrosis caused by ischemia.The samedosage of PNScould markedly increase the action of superoxide dismutase (SOD)and decrease the concentration of nitrie oxide(NO).Conclusion Different from Rg₁, Rb₁ and PNScan increase CBF in MCAO region.Allthese drugs can lessen brain injury and neuron necrosis.The mechanismmay berelated to thereduction of Ca²⁺and NO contentin ischemic reg ion.

Clinical study of azithromycin and cefazol in in treatment of respiratory tractinfections

LI Xiu, ZHANG Ying, ZHANG Su-Ping, MENG Lei

2000, 5(2):  154-156. 

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Aim To evaluate the effect and safety of azithromycin injection producedin China and cefazolin in the treatment of respiratory tractinfections.Methods 50 patients with respiratory tractinfections weredivided randomly into two groups.Patients in the test grouprecieved azithromycin in the dosage of 250 mg·d^-1, qd for 5 div with double dosages at the fi rst timeand patients in the control grouprecieved cefazolin in the do sage of 2.0 g, bid, iv for 5 ~ 10 d.Results No statistical significant differences of overall clinical Effect wereobserved between two groups.The fully recovery, Effective and sidereaction rates for the test group were46.67 %, 90% and 3.3 %, respectively, and for control group the data were60 %, 95 %, and 0 %, respectively.Conclusion Azithromycin injection producedin China is effective and safe in the treatment of respiratory infections.

Appl ication of capillary zone electrophoresis in clinical pharmacology and therapeutics¹

CAO Cheng-Xi, HE You-Zhao, ZHOU Shu-Lin, QIAN Yi-Tai

2000, 5(2):  180-186. 

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