Table of Content

Volume 5 Issue 1
26 March 2000

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Expression ofμandκopiate receptor in spinal cord and brainstem during morphine withdrawal in rats

LIU Hui-Fen, XIE Xiao-Hu, ZHOU Wen-Hua, YANG Guo-Dong

2000, 5(1):  1-5. 

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Aim To observe the gene expression ofμandκopiate receptor in spinal cord and brainstem,and the effects of muscarinic receptor antagonist,NMDA receptor antagonists and inhibitor of nitricoxide synthase on the expression of these genes during morphine withdrawal in rats.Methods The mRNA levels ofμandκopiate receptor mRNA were assayed by reverse transcription polymerase chain reaction (RT-PCR)with the beta-actin mRNA as an internal control.Results Theμopiate receptor mRNA levels were increased significantly in spinal cord and brainstem during morphine dependence,and decreased after injection of naloxone during morphine withdrawal in rats.Theκopiate receptor mRNA levels in spinal cord and brainstem were changed conversely compared with theμopiate receptor mRNA levels during morphine dependence and withdrawal.Theμandκopiate receptor mRNA levels in spinal cord and brainstem were decreased by administration of either Rp-cAMPs or calyculin A while these levels were not changed by Sp-cAMPs at half hour before injection of naloxone in morphine dependent rats.Administration of l-N-nitric arginine methylester(10mg·kg^-1)resulted in a decrease ofμopiate receptor andκopiate receptor levels in spinal cord,andμopiate receptor levels in spinal cord andκopiate receptor levels in brainstem were dedcreased by pretreatment with methyl-scopolamine (0.5mg·kg^-1)during morphine withdrawal.However,theμandκopiate receptor levels in both spinal cord and brainstem were not different from those of morphine withdrawal rats pretreated with either MK801 (0.125mg·kg^-1)or pirezenpine(10mg·kg^-1).In adddition,β-actin mRNA levels were not different in each group.Conclusion The expression ofμopiate receptor andκopiate receptor mRNA plays an important role in mediating the process of morphine dependence and withdrawal,and the expression ofμopiate receptor andκopiate receptor mRNA in spinal cord and brainstem could be inhibited by block of muscarinic receptor or inhibition of nitric oxide production.

Comparison of anxiolytic effects of allopregnanolone and diazepam on the elevated plus-maze in mice

YU Rong , LU Ying-Qing, SHENG Mei-Ping, SHI Nian-Ci, YAO Ming-Hui

2000, 5(1):  6-9. 

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Aim To compare the anxiolytic effects of reduced metabolite of progesterone and benzodi-azepine.Methods The effects of allopregnanolone and diazepam on spontaneous locomotor activity and on exploration in the elevated plus-maze were studied in C57 mice 20 min after vehicle or drug intraperitoneal administration.Results Allopregnanolone (0.1mg·kg^-1,ip)elicited marked anxiolytic effects in terms of significantly reducing the latency to enter the open arm from (31.30±8.39)s to (8.80±6.00)s,(P<0.001),and significantly increasing both the number of open arm entries from 1.20±0.42 to 4.80±1.75,(P<0.001)and the proportion of total time spent on the open arm from 7.13%to 32.50%,(P<0.001).Mean-while,the diazepam (0.25mg·kg^-1)produced a lower anxiolytic effect comparing to that of the allopregnanolone.Analysis of spontaneous locomotor activity showed while 0.5mg·kg^-1of diazepam decreased the locomotor activity (P<0.01),neither 0.1mg·kg^-1of allopreg-nanolonenor 0.25mg·kg^-1of diazepam affect the locomotor activity score.Conclusion Together,these results provide evidence for differential behavioral actions of the neurosteroids and benzodiazepines.Since the allopregnanolone produce a selective anxiolytic effect without affecting the spontaneous locomotor activity,the allopregnanolone may be a better alternative for diazepam in treating anxiety.

Effect of anti-digoxin antiserum on endogenous digitalis-like factor and membrane ATPase activity in hypoxic injury myocardium¹

KE Yong-Sheng, YANG Hao, YANG Ting, CHENG Guang-Hua, WANG You-Xia

2000, 5(1):  10-12. 

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Aim To evaluate the protective effect of anti-digoxin antiserum on hypoxic injury my-ocardium and its mechanism.Methods It was observed that different concentration an-ti-digoxin antiserum effect on endogenous digitalis-like factor and cell membrane ATPase ac-tivity in hypoxic myocardium model.Results The level of endogenous digitalis-like factor was remarkably higher,cell membrane ATPase activity were remarkably lower in hypoxic group than those of normal group;anti-digoxin antiserum can resume membrane ATPase ac-tivity.Conclusion Rise of endogenous digitalis-like factor was basic of molecular biology of myocardial damage during myocardial hypoxia.Anti-digoxin antiserum has lightened my-ocardial injury and has protective effect on hypoxic myocardium by against effect of endoge-nous digitalis-like factor.

Adrenomedullin abolish the vasoconstrictive effect of norepinephrine and endothelin

YAN Xiao-Wei, Christoph Schalcher, Wolfgang Kiowski

2000, 5(1):  14-17. 

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Aim Adrenomelullin is a novel vasodilator with a potent hemodynamic effect on human arterioals.The interaction of adrenomedulling with vasoconstrictors in normal volunteers have not been investigated.Methods 14 normal volunteers were divided into two groups randomly with a double blind manner.Group A (n =7) were treated with ADM or/and norepinephrine and group B(n =7),ADM or/and endothelin,through brachial artery infu-sion of different doses.Forearm blood flow were observed (with plethysmography)before,during and after durg administration.Results Intraarterial infusion of ADM resulted a three-fold increase of forearm blood flow.The vasodilation effect of ADM disappeared 40 minutes after drug discontinuation.Intraarterial infusion of norepinephrine and endothelin resulted 61%and 73%decrease of FBF,respectively.Combined infusion of low dose ADM with high dose norepinephine or endothelin could abolish the vasoconstrictive effects of pre-mentioned vasoconstristors.Conclusion ADM is a potent vasodilator.Its vasodila-tion effect lasts 40 min after discontinuation of infusion.In forearm resistance arteries,ADM can abolish the vasoconstrictive effects of high dose norepinephrine or endothelin.

Anoxia-reoxygenation damage to rat ventricular myocytes and protective effects of tetramethylpyrazine¹

CHEN Jiang-Bin, JIANG Hong, SUN Xiao-Mei, LI Geng-Shan, HUANG Cong-Xin, XU Jia-Li, TANG Qi-Zhu

2000, 5(1):  18-20. 

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Aim To observe anoxia-reoxygenation damage to ventricular myocytes and the protective effects of tetramethylpyrazine on the damage in rats.Methods T he myocytes viability,intracellular K⁺/Na⁺,intracellular free calcium concentration were detected in different tetramethylpyrazine concentration groups and control group in the anoxia-reoxygenation damage condition.Results Anoxia-reoxygenation had done harm to the rat ventricular myocytes.Tetramethylpyrazine inhibited the myocyte contracture,increased the cell via-bility,inhibited the fall of intracellular K⁺/Na⁺,and increased intracellular free calcium concentration in the dose of 4μmol·L^-1or more.And the more the dose is,the better the salutary effects are.Conclusions Tetramethylpyrazine has protective effect during anoxia-reoxygenation on the ventricular myocytes of rats.

Effect of ligustrazine on pulmonary arterial pressure and thromboxane A 2 and prostacyclin in chronic hypoxic hypercapnic rats¹

WANG Liang-Xing, CHENG Shao-Xian, XU Zheng-Jie, YU Lin-Sheng, XIE Yu-Peng, CHENG Yan-Fan, WANG Wen

2000, 5(1):  21-24. 

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Aim To investigate the effect of ligustrazine on pulmonary arterial pressure,thromboxane A₂(TXA₂)and prostacyclin(PGI₂)in chronic hypoxic hypercapnic rats.Methods Thirty rats were randomly divided into control group(A),hypoxic hypercapnic group(B)and hypoxic hypercapnia+ligustrazine (lig)group(C).Results The mPAP in group B was significantly higher than that in group A(P<0.01)and group C(P<0.01).Differences of mCAP among groups were not significant (P>0.05);The specific value of WA/TA(vessel wall area/total area) and SMC (the density of medial smooth muscle cells)were significantly higher in group B than that in group A(P<0.01)and group C(P<0.01).Electron microscopy showed the proliferation of medial smooth muscle cells and collageous fibers of pulmonary ar-terioles in ratsof group B and ligustrazine could invert the changes mentioned above.Plasma TXB₂ concentration and TXB_2/6-keto-PGF 1αwere significantly higher in ratsof group B than that of group A(P<0.01)and group C (P<0.01).Differences of 6-keto-PGF_1α were not significant among groups(P>0.05).Conclusion Ligustrazine can inhibit pulmonary hyper-tension and structural remodeling of pulmonary artery in chronic hypoxic hypercapnic rats by inhibiting synthesis of TXA₂.

Effects of Taurine on dysfunction of myocardial nuclear calcium transport in rat myocardial injury induced with isoproterenol

WAN Fu-Sheng, ZENG Zhao-Jian, ZHAO Xiao-Man, LUO Da-Ya

2000, 5(1):  25-27. 

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Aim To observe the dysfunction of my ocardial nuclear calciumtransport in rat myocardial injury and effects of taurine on it.Methods The model of my ocardial damage was induced by subcutaneous injection of isoproterenol(ISO,5mg·kg^-1·d^-1).Myocardial nuclei were purified with Sucrose density cent rifuga tion and ident if iedzymolog ically.The activity of Ca²⁺-ATPase was measured zymolog ically and calcium uptake was assayed with⁴⁵Ca²⁺iso tope.Results Compared with the control,the Ca²⁺-ATPase activity of my ocardial nuclear in ischemia group was decreased by 18.1%(P<0.05),the nuclear⁴⁵Ca²⁺uptake was significant decreased and Vmax value was lowered by 54.6%.With the controlg roup Ca²⁺-A TPase activ ity and⁴⁵Ca²⁺uptake in the my ocardial nuclei of Taugroup showed nosignificant changes.Conclusion The above results indicated taurine has notable protective effects on dysfunction of nuclear calciumt ransport in rat my ocardium.

Effects of berberine on EEG and EEG power spectrum recorded in conscious rabbits

G UO Shu-Ren, WU Jun-Fang, LUO Wei-Feng, LIU Tian-Pei

2000, 5(1):  32-35. 

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Aim In order to study the mechanisms of underlying improving learning and memory in rodent,the effects of berberine (Ber)on EEG and EEG pow erspectrum were recorded in conscious rabbits.Methods EEG and EEG power spectrum were recorded in conscious rabbits with chronical implanted elect rodes.Results Ber at doses of 1~4mg·kg^-1iv showed to decrease dose-dependently the spect rum power of delta dominant frequency in cortical area and transfer the dominant frequency from delta to thetarhy thm in hippo campus.Under the same conditions,the effects of physostigmine 0.1mg·kg^-1iv on EEG were similar to Ber.Ber 2mg·kg^-1iv reversed significantly these effects of Ber 0.05 mg/rabbitivon EEG and power spectrum,but scopolamine butylbromide 0.4mg·kg^-1iv,which can not pass the blood-brain barrier,did not.Conclusion The effects of Ber are closely related to the action on the central cholinergic system.

Comparison of domestic and foreign simvastatin for the treatment of primary hypercholesterolemia

CHEN Shan, SHAN Jiang, JIN Hong-Yi, XIE Hai-Bao, Q ING Nan-Ping, LI Pei-Zhang, RUAN Zhou-Rong

2000, 5(1):  36-38. 

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Aim The efficacy and safety of the domestic simvastatin in the treatment of primary hypercho lesterolemia were compared with those of the imported simvastatin.Methods A controlled,multicenter,open-abel and randomized clinicaltrial was performed in 156 patients,of whom 56 received domestic simvastatin,56 took imported simvastatin and 44 in the open group,also took domestic simvastat in in a do se of 10mg·d^-1at night for 8weeks.Results In the domestic simvastatin group and the imported simvastatin group the serum total cholesterol(TC)was reduced by 26.73% and 25.62% respectively,and the low density lipoprotein cholesterol (LDL-C)by 40.47% and 36.41% respectively.The total efficacy of the two groups was 94.62% and 91.07% respectively.The side effects w ere mild in the discomfort of gast rointestine and the increase of CPK.The re was no significant difference between two groups about the efficacy and the safety.In the open group TC and LDL-C were reduced by 25.50% and 40.57% respectively,the overall efficacy was86.36%.Conclusion Domest icsimvastatin is one of the safe and effective drug s to treat the hypercho lesterolemia.

Bioavailability of ubiquinone 10 tablets in healthy volunteers

XIAO Shu-Hua, WEI Guang-Li, LU Rong, LIU Chang-Xiao

2000, 5(1):  39-41. 

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Aim To compare the bio availability of two ubiquinone tablets in healthy volunteers.Methods A HPLC method was used to determine the serum ubiquinone 10 concentrations at 0,1,2,3,4,6,8 and 12 h after oral administration for 7 day s (20 mg,tid)in a cross -over test.Results AUC,C_max and T_peak of the test tablets were (5.91±1.78)μg·h·ml^-1,(0.66±0.17)μg·ml^-1and (4.00±1.25)h,respectively,and these of the reference tablet s were (6.30±2.09)μg·h·ml^-1,(0.70±0.20)μg·ml^-1and (4.60±1.58)h,respectively.All of these parameters between the two kinds of tablets were not significantly different statistically.Conclusion The related bioavailability of the test tablet sversus the reference tablets is 93.9%.The two formulations of ubiquinone 10 are bioequivalent.

Chronic toxicity of tea polyphenols in dogs

ZHAO Ya-Nan, KE Yong-Sheng, ZHENG Qing-Shan, GUI Chang-Qing

2000, 5(1):  43-46. 

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Aim The chronic toxicity of tea polyphenols(TP)in dogs was observed.Methods 18 dogs were randomly divided into high,middle and low dose TP groups and one control group.When TP was given(po)by 650mg·kg^-1·d^-1,65mg·kg^-1·d^-1,6.5mg·kg^-1·d^-1re-spectively for 90 d and after TP was stopped for two weeks,the general conditions,ECG,blood routine,urine routine,serum lipids,blood sugar,coagulation time,and hepatic and kidney function were detected respectively.Results These mdices were not different from each other among the 4 groups before,during and after administration of TP.The level of serum total cholesterol was progressively decreased in TP groups.Conclusion TP has no toxic effect on dogs and can decrease the level of serum total cholesterol in normal dogs.

Ef fect of the all trans retinoic acid and Ara-con the telomerase activity of HL-60 cells

WU Xiang-Hua, YE Kai-He, HU Ai-Qun

2000, 5(1):  47-48. 

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Aim To investigate the possible mechanism of human promyelocytic leukemia cells differentiation and apoptosis induced by all trans-retinoic acid (ATRA)and A ra-c.Methods The effects of AT RA and Ara-c on the tolomerase activity of HL-60 cells were detected by PCR-E LISA.Results The tolome rase activity of HL-60 cells declined during the course of differentiation and apoptosis induced by AT RA and Ara-c.Conclusion These finding ssuggest that AT RA and Ara-c can inhibit tolomerase activity of HL-60 cells.It may be one of the important mechanisms of human promyelocytic leukemia cells differentiation and apo ptosis induced by ATRA and Ara-c.

ICAM-1 expression in experimental fibrosis tissue affected by Radis Astragali

WANG Yao-Jun, QUA N Qi-Zhen, SUN Zi -Qin, QI Feng, JIANG Xue-Liang, ZHANG Xiu-Li, WANG Dong

2000, 5(1):  49-51. 

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Aim To observe the antifibrotic effect of Radis Astragali and to explore the mechanism.Methods The fibrosis of animal model was induced with CCl₄,and the model animals were treated with Radis Astragal in treatment group and saline in control group respectively.Results The serum hyaluronic acid (HA),fibrosis score and ICAM-1-positive hepatocytes all the decreased in the treatment group as compared to those in the control group.Conclusion Radis Astragali has satisfactory effect on experimental fibrosis.The mechanism may be correlated with it saffection on ICAM-1 in livert issue.

Determination of homoharringtonine distribution in eyeball tissue of rabbit by high performance liquid chromatography method

YAN Fang, LIU Jin-Xiang, CHEN Chang-Song, LI Jun-Sheng

2000, 5(1):  52-53. 

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Aim To observe homoharring to nine(HHT)distribution in eyeball tissue of rabbit.Methods Harringtonine(HT)was used as internal standard.The chromatography consisted of Kromasil C₁₈ column with methanol0.01mol·L^-1(60∶40,pH_2.5)as the mobile phase at the flow rate of 0.8ml·min^-1.Results The chromatography retention time of HHT and HT were6.35min and 4.70min.The standard curve was linear in the concentration range of 5~200μg·L^-1in serum and the relation coefficient was 0.994.The recovery of spiked sample was(93.17±4.31)%.After injection of 2mg of HHT in side of rabbit eyeball,the contents in sclera,cornea,retina,vitreous body and crystalline lens were reduced progressively,but the eliminate rate w ere reduced in a proper order.Conclusion HHT can distribute to every eyeball tissue when it was injected in side of rabbit eyeball.

Analyses of the complex prescriptions of Luofendeine

FANG Zhi-Ping, LIU Xiao-Kang, XIAO Yi, SONG Xiao-Hong, LI Yu-Hong

2000, 5(1):  54-58. 

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Aim To study the actions of Luofendeine and its component.Methods LD50 tests of Luofendeine and its component,heat-board text and body-twisting test of mice were pertormed to learn its analgesic and antiinflammatory actions.Results The analgesic action and antiinflammatory action were increased when codamine was mixed with buluofen by the rate of 13∶200,without increasing its toxicity.Conclution The complex prescription of Luofendeine is rational and can increase the analgesic action obviously.

Nasal absorption of furosemide and promotion action of l-menthol

WANG Hui, XUE Man-Qing

2000, 5(1):  59-60. 

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Aim The nasal absorption of furosemide and promotion action of l-menthol was ex amined.Methods In situnasal recirculation methods was used to study the does-effect relationship of nasal absorption of furosemide and the effect of l-menthol on nasal absorptionof furosemide in rat s.Results When the concentration of furosemide in circulation liquid was respectively (4.66±0.33)、(9.76±0.45)and (18.83±1.89)μg·ml^-1,the absorption rate constant k (min^-1)of nasal insitu was correspondingly 0.0067±0.0011,0.0134±0.0024 and 0.0163±0.0037;and urine liquid appearing time was (73.33±1.53)、(52.67±7.02) and (47.00±4.58)min.But the larger the concentrationofl-menthol,the little the absorption rate constant k.Conclusion Furosemide can be absorbed through the nasal mucous,and l-menthol can promote its absorption.

Effect of alumina magnesia and simethicone tablet on gastric acid and pepsin activity in rats

LI Xing-Tian, GENG Li-Jian, DING Shu-Min

2000, 5(1):  62-64. 

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Aim To study the effects of alumina,magnesia,and simethicone tabeton the secretionof gastric acid and pepsin activity in rats.Methods The pharmacodynamic indices were measured by the secretion of gastric acid and pepsin activity.Results and Conclusion Compared with the controlgroup,alumina,magnesia,and simethicone inhibited gastricacid and increased pH of gastric juice.A significant decrease occurred in pepsin activity after a doses of 180mg·kg^-1and 600mg·kg^-1(P<0.05 and P<0.01,respectively)and a positive relationship between decreased pepsin activity and doses of alumina,magnesia,and simethicone(r =0.987).There are no influence on secretion of gastricjuice.

Release of anticancer doxorubicin-hydroxypatite(DOX-HAP)complex in rabbit liver

PENG Xiang-Xin, CAI Mei

2000, 5(1):  65-66. 

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Aim The release process of an anticancer agent,DOX-HAP in rabbit live r was observed.Methods DOX and DOX-HAP were separately injectoed into rabbit livers under the guide of Btypeultrasound.Dox concentrations in plasma and liver tissue of the rabbits in both groups were measured by fluorescent stectrophotometer and compared.Results The concentration of complex could existedin the liver tissue about 5 d(1 000 ng·g^-1)when it was given in a dose of 2mg·g^-1.At the 10 min the concentration in plasma would be reduced about 1/2 as compared with that in the control group.Conclusion sThe DOX-HAP complex not only could increase and insist in an effective concentration of DOX at the local injecting area of liver tissue,but also reduce its concerntration in the plasma.The refore,it could decrease the toxicity and side-effect of DOX.