Table of Content

Volume 5 Issue 4
26 December 2000

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Suppression of invasion and migration by 7-hydroxystaurosporine(UCN-01), a new ant i-tumor agent

MENG Qing-Hui, SHAO Rong-Guang, XU Jing-Wen, FAN Sai-Jun

2000, 5(4):  289-293. 

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Aim and Methods To investigate the effect of UCN-01(7-hydroxystaurosporine)on cell migration and invasion ability of DU-145, an invasive human pro state cancer cell line.Results It was found that UCN-01 at no n-cytotoxic doses (100 nmol·L^-1)significantly inhibited prostate cancer DU-145 cell invasion and migration behaviors.Moreover, this anti-invasion and migration activity of UCN-01 was associated with an up-regulation of cell adhesion molecule E-cadherin.Conclusion These results indicate for first time that UCN-01 inhibits the invasion and migration of human prostate cancer cells.Thus, clinical application of UCN-01 may contribute to the potential benefit for suppression of prostate cancer invasion and metastasis.

Protective effects of total extract of astragalus ( TEA) on primary rats hepatocytes injured by CCl₄ or H₂O₂

YANG Yan, CHEN Min-Zhu

2000, 5(4):  294-297. 

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Aim To study the protective effect of total extract of astragalus(TEA)on primary rat hepatocytes injured by CCl₄ or H₂O₂ and its mechanism.Methods The primary hepatocytes were isolated by Ⅳ collaganase and injured by CCl₄ or H₂O₂.The contents of malondialdehy de(MDA)and glutathione (GSH), glutathione peroxidase(GSHpx)activity of hepatocytes and the AST and or ALT level in cultural supernatant were determined by general methods. Results (1)The elevation of MDA content of hepatocytes and AST level in supernatant of cultural hepatocytes, and the loss of GSH content and GSHpx activity induced by CCl₄ were restored remarkably by TEA(5~80mg·L^-1);(2)The elevation of ALT level in the supernatant of hepatocytes and MDA content of hepatocytes, and the loss of GSH content and GSHpx activity induced by H₂O₂ were improved significantly by TEA( 5~80 mg·L^-1) treatment.Conclusion The results suggest that TEA possess direct protective action on primary hepatocyte in vitro injured by CCl₄ or H₂O₂.These might be associated with its anti-oxidative activity.

Anti-oxidative effect of total extract of astragalus(TEA)on aging mice

LEI Hong, WANG Bin, LI Wei-Ping, YANG Yan, ZHOU Ai-Wu, CHEN Min-Zhu

2000, 5(4):  298-301. 

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Aim To study the mechanism of the anti-aging effect of total extract of astragalus(TEA) in mice.Methods MDA content, the activities of Mn-SOD and GSH_px and the reduced to oxidized glutathione (GSH/GSSG)ratio in mitochondria of D-galactose(D-gal)treated mice and 17-month-old mice were measured.Results Treatment with TEA(40 mg·kg^-1·d^-1ig)for 10wk would lower the content of MDA and restore activities of Mn-SOD, GSH_px and GSH/GSSG ratio in mitochondria of D-gal treated mice.Treatment with TEA (40mg·kg^-1·d^-1 ig)for 3 mon had the same effect on 17-month-old mice.Conclusion TEA has anti-aging effect on D-gal treated mice and 17-month-old mice significantly, probably being related to its anti-oxidative effect.

Expertmental study of tiaxiongbushen oral liquid on the sexual vitality and aging in male drosophila melanogaster

LU Hui-Xiang, XU Shi-Kai, WU Guo-Zhong

2000, 5(4):  302-304. 

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Aim To observe the effects of tiaxiongbushen oral liquid(TOL)on the sexual vitality and aging in male Drosophila Melanogaster.Methods TOL in two dosages (0.5 %and 1 %)was fed to male Drosophila Melanogasters and the sexual vitality and life span were detected.Results It was found that the period of mating latency was shortened (P<0.05), the times of vibrating wings was increased (P<0.05), and the mating duration and the life span were prolonged significantly.Conclusion Tiaxiongbushen oral liquid is valuable in treatment of human impotence and prolongation of life span.

Influences of perindopril on pulmonary vascular remodeling in normobaric hypoxia-hypercapnia rats

YANG Peng-Lin, YU Lin-Sheng, GONG Yong-Sheng, ZHENG Lu-Zhen, WANG Wei, HU Liang-Gang

2000, 5(4):  305-308. 

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Aim To investigate the effect s of perindopril, an angiotensin converting enzyme inhibitor,on mean pulmonary arterial pressure(mPAP)and pulmonary vascular remodeling.Methods Using the normobaric hypoxia-hypercapnia rat model, the changes of plasma angiotensin Ⅱ(AngⅡ), mPAP and ultrastructure of pulmonary arteriolar wall were observed after administration of perindopril.Results The mPAP and AngⅡ were significantly greater and the ultrastructure of the small lung vessels had a more obvious change in the 4 weeks hypoxia-hypercapnia group than those in the control group.It was also found that perindopril decreased Ang Ⅱ, declined mPAP and amelio rated vascular ultrastructure change.But the change of ultrastructure was similar in the 8 weeks hypoxia-hypercapnia group and perindopril treatment group.Conclusion I t is suggested that chronic hypoxia-hypercapnia should induce the remodeling of pulmonary arteriolar structure via Ang Ⅱ and that perindopril could ease pulmonary vascular remodeling in early stage.

Preconditioning with desflurane, sevoflurane and isoflurane increase the preservation of adenosine triphosphate in anoxia-reoxygenation myocardial cells

YE Min, PENG Zhang-Long

2000, 5(4):  309-312. 

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Aim To study the effects of preconditioning with desflurane, sevoflurane and isoflurane on adenosine triphosphate (A TP)in anoxia-reoxygenation myocardial cells.Methods Rat ventricular myocytes, cultured for 4 ~ 5 days, were randomly allocated to five groups:Control group, anoxia-reoxygenation group and groups preconditioned with 1.5 MAC desflurane,sevoflurane or isoflurane follow inganoxia-reoxy genation.The content of intracellular ATP,the activities of lactic dehydrogenase(LDH)and creatine kinase(CK), and the cell viability were measured at the end of experiment.Results Preconditioning with 1.5 MAC desfllurane, sevoflurane or isoflurane significant lyattenuated the great reduction in ATP and cell viability and the increase of LDH and CK caused by anoxia-reoxygenation.There was a positive correlation ship between A TP and cell viability, and anegatiue correlation ship between LDH and CK (r was 0.83, -0.87 and -0.82 respectively, P<0.01).Conclusion sPreconditioning with desflurane, sevoflurane or isoflurane increases the preservation of ATP in anoxia-reoxygenation myocardial cells, which may be one of the mechanisms for myocardial protection.

Effects of rhomotoxin on electrophysiologic parameters in rabbit heart

LI Di-Jun, WANG Hai-Yu

2000, 5(4):  313-316. 

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Aim To study effect s of rhomotoxin (Rh)on electrophysiologic parameters in rabbit heart.Methods The rabbi t heart s in vivo were injected with Rh 12.5μg·kg^-1,25μg·kg^{- 1} or saline iv respectively and the isolated rabbit hearts were perfused by Krebs-Henseleit(K-H)perfusion liquid containing Rh 0.34 μmol·L^-1 or 0.68μmol·L^-1.The electrophysiologic parameters were observed before and after drug adminitration.Results At 20, 40, 60 and 80 min after inject ion of Rh 12.5μg·kg^-1 iv, the VDT,ERP and RRP had no significant changes ;but at 20, 40, 60 and 80 min after inject ion of Rh 25 μg ·kg^-1 iv a significant prolongation of ERP and (or)RRP was found (P<0.05).Perfusion gisolated heart with Rh 0.34 μmol·L^-1 prolonged ARRP and A ERP (P<0.05, P<0.01);while perfusion gisolated heart with Rh 0.68 μmol·L^-1 increased ADT and VDT(P<0.05, P<0.01)and pro longed ARRP, AERP,VRRP and VERP (P<0.05, P<0.01).Conclusion Rh might have an effect of increasing atrial and ventricular diastolic threshold, which prolongates atrial and ventricular refractory period by direct action on rabbits myocardial muscle.

Protective effect of taurine on myocardial ischemia and reperfusion injury in rats

YANG Jian, CAO Yong-An, JI Yue-E, SHI Wen-Yan

2000, 5(4):  317-319. 

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Aim To research the protective effect and mechanisms of taurine on myocardial ischemia and reperfusion injury in rats. Methods Myocardial ischemia reperfusion models were established in SD rats. The effects of taurine on the size of myocardial infarction and the changes of activity of SOD,and the levels of MDA and NO in myocardium and plasma of rats with myocardial ischemia and reperfusion injury were observed. Results In rats with myocardial ischemia and reperfusion injury, the taurine could reduce the size of my ocardial infarction (P<0.05,0.01), raise the activity of SOD (P<0.01) and decrease the levels MDA and NO (P<0.05,0.01) in myocardium and plasma. Conclusion The taurine has protective effect on myocardial ischemia and reperfusion injury in rats. It may be related to raising the activity of SOD and decreasing the levels of MDA and NO in myocardiun and plasma.

Effects of aspirin in combination with captopril on hemodynamics in anesthetized open chest dogs

SONG Yi-Min, ZHOU Li, GAO Er

2000, 5(4):  320-322. 

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Aim To observe the effects of aspirin in combination with captopril (Cap)on hemodynamics in anesthetized open chest dog s.Methods Tension time index(TTI), left ventricular work index(LVWI), mean arterial pressure (MAP), and total peripheral vascular resistance(T PV R), femoral artery blood f low(FBF), ventricular systolic pressure(LVSP), maximum of its first derivative(+dp/dt_max), left ventricular end diastolic pressure (LVEDP)and heart rate were recorded on polygraph and electromagnetic flower separately when aspirin was administered alone or in combination with captopril.Results The result showed that Asp 5, 10 mg ·kg^-1 had no marked effect on indices of hemodynamics.Cap 0.5mg·kg^-1 iv had no significant effect on LVSP, +dp/dt_max, LVEDP, HR and did not obviously increase cardiac index (CI), but distinctively decreased T TI, LVWI, MAP, TPVR, and significantly increased FBF.The effect of Asp in combination with Cap was similar to that of Cap alone.Conclusion The improvement of cardio vascular function caused by Cap is not changed in the presence of Asp.

Experiment study of the GLUT4 mRNA expression in the skeletal muscle and the relationship between GLUT4 mRNA expression and insulin secretion in NIDDM rats

QIAN Dong-Sheng, HE Min, LUO Lin, ZHU Yi-Fang, E Qun

2000, 5(4):  323-326. 

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Aim To observe the glucose transporter 4 (GLUT4)mRNA expression in the skeletal muscle and the relationship between GLU T4 mRNA expression and insulin secretion in non-insulin-dependent diabetes mellitus (NIDDM)rats.Methods The rat models of N IDDM were made.The GLUT 4 mRNA expression in skeletal muscle was observed with Northern blot method.The serum insulin was determined by radio immunoassay.The change of insulin positiveβcell in islet was observed by immunohistochemistry.Results The GLU T4 mRNA expression in skeletal muscle in NIDDM rats was decreased to 45 %of that in normal rats (P<0.01).The fast serum insulin level was normal, but in oral glucose test, the secretion of insulin was reduced markedly and a phenomenon of delayed secret ion was observed.Immunohistochemistry experiment displayed that the volume of islet in NIDDM rats was smaller than half of that in normal rats and the number of insulin positive β cells reduced markedly.Conclusion The present study showes that in NIDDM rats the GLUT 4 mRNA expression in skeletal muscle is lower and this response is considered to have some positive correlation with insulin secretion.

Therapeutic value of fosinopril in heart failure

CAI Heng, WANG Feng-Zhi, ZHANG Xue-E

2000, 5(4):  327-329. 

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Aim To investigate the therapeutic value of fosinopril in heart failure.Methods Thirty SD rats were divided into three groups at random.Rats in heart failure group and fosinopril group were given an 8 weeks overswimming exercise to induce heart failure and the heart failure rats in fosinogril group were treated with fosinopril orally (2 mg·kg·d^-1)for 6 weeks.14 weeks late r the hemodynamic indexes, myocardiac apoptosis rate, left ventricular mass index (LVM I)and myocardiac interstitial fibrosis were determined.Results The hemodynamic indexes in heart group were remarkably different from those in normal control group, while there was a significant improvement in fosinopril group (P<0.01).Left ventricular mass index in heart failure group was more increased than in the control(P<0.01), but it was significantly decreased in fosinopril group (P<0.01).Myocardiac apoptosis rats was highest in heart failure group, and it was decreased when treated with fosinopril(P<0.01).Conclusion Fosinopril could drop the myocardiac apoptosis rats.It suggests that fosinopril has protecting myocardium effect, andim proves prognosis of patients with heart failure.

Pharmacokinetics and relative bioavailability of domestic ibudilast sustained release capsules in healthy volunteers

YANG Yi-Mei, CHEN Shu-Juan, GU Shi-Fen, ZHANG Bin, DA I Zong-Shun, ZENG Fan-Dian

2000, 5(4):  330-332. 

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Aim The relative bioavailability of domestic ibudilast sustained release capsules in healthy volunteers was observed.Methods A single oral dose of 20 mg of imported and domestic ibudilast sustained release capsules and 10 mg of ibudilast raw material was separately given to 12 healthy volunteers in a randomized crossover study.Ibudilast concentration in plasma was determined by HPLC method.Results The C_max were (54.9±9.7), (60.7±9.1)and (62.2±11.5)μg·L^-1;the t_max were (3.8±0.8), (3.9±0.8)and (1.8±0.3)h; the t_1/2(ke) were (1.5±1.4), (12.1±1.0) and (3.5±0.5)h, and the A UC_(0~t) were (618.1±57.7), (588.1±66.6)and (233.0±46.4)μg·h ·L^-1 in imported capsule group, domestic capsule group and raw material group respectively.The relative bioavailability of domestic sustained release capsules of ibudilast is (95.6±11.0)%.Conclusion The results of statistical analysis demonstrate that the imported and domestic sustained capsules have significant character of significantly sustained release and are bioequivalent.

Relative bioavailability of levofloxacin hydrohloride capsule in healthy volunteers

MA Yue-Ming, ZHENG Zao-Ho ng, CHEN Bo, MAO Guo-Guang, ZHONG Qiu, YAN Wen-Kui, ZHA Xiao-Juan, SUN Rui-Yuan

2000, 5(4):  333-335. 

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Aim To investigate the pharmacokinetics and relative bioavailability of levofloxacin hydrochloride capsule.Methods A single 200 mg oral dose of either capsule or tablet was given to 12 healthy male volunteers in randomized self-crossover way.Plasma levofloxacin concentration was determined by high performance liquid chromatography.The concentration-time data of levofloxacin was fit ted to two-compartment model with first-order absorption and the bioequivalence of the two formulations were evaluated by the analysis of variance and the two one-sidedt-test.Results The pharmacokinetic parameters were as follows: capsule:C_max=(3.18±0.57)mg · L^-1, t_max=(0.83±0.33)h, AUC_0~24=(19.95±2.86)mg·h·L^-1, t_1/2(β)=(7.75±2.04)h ;tablet:C_max=(2.96±0.43)mg·L^-1, t_max=(0.96±0.33)h, AUC_0~24=(21.49±1.88)mg ·h·L^-1, t_1/2(β)=(6.82±0.84)h.Relative bioavailability of capsule was (93.0±11.8)% compared with tablet.Conclusion The two formulations are of bioequivalence.

Investigation of increasing efficacy of aterial infusion of NaHCO₃ to solid malignant tumors in interventional chemotherapy

FAN Ping-Sheng, WAN Yu-Xiu, LI Ji-De, BEI Hu, FENG Ke-Hai, WANG Shi-Ceng, LI Xin-Min, LIU Ru-Hua, HU Li-Yuan

2000, 5(4):  336-337. 

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Aim To observe the effect of interventional therapy of 5-fluorouracil(5-Fu), mitomycin C(MMC)and adriamycin (ADM)on solid malignant turmors in association with aterial infusion of NaHCO₃.Methods Patients were randomly divided into two groups.With Seldinger technique, through the femoral atery to tumoratery.The patients in the control group were infused by anticarcinoma agents simply, and patient s in the treatment group were initially infused by NaHCO₃, and then by NS 30 ml and anticarcinoma agents seperately. Results Partial remission (PR)in the group treated with NaHCO₃ and anticarcinoma agents was significantly higher than in the group treated simply with anticarcinoma agents.Conclusion Aterial infusion of NaHCO₃ into malignant tumors can increase the efficacy of ADM,MMC and 5-Fu.

Influence of cisplatin cream on the production of skin granular cell

YAN Jun, QU Peng-Cheng, ZHANG Yu-Zhen, LI Chang-Sheng, LI Ying-Quan, LIU Shu-Ping

2000, 5(4):  338-339. 

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Aim To observe the influence of cisplatin cream on the production of skin granular cells and the body weight of mice.Methods The changes of body weight and skin pathology of mice were observed 18 days after external application of cisplatins.Results The experiment results showed that 0.1 % ~ 1 % cisplat in cream obviously enhanced the product ion of skin granular cells(P<0.01)and the effect on the growth of body weight of mice was less than the effect of tretinoin cream(P<0.01)and no obvious dermatic stimulation was found.Conclusion Cisplatin cream promeotes the product ion of skin granular cells.

Comparison of medical abortion, induced abort ion and medical with induced abortion in the termination of early pregnancy

XU Lan, ZHANG Yong-Feng, ZHENG Yan-Luan

2000, 5(4):  340-343. 

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Aim To compare the advantage of different methods of terminating early pregnancy. Methods 684 women in early pregnancy(≤49 d)were allocated into three groups according to their request:Group A (medical abortion, n=241), taking (po)mifepristone 25 mg every 12 h for three days and then taking misopostol 600 μg at 8:00 on the forthday;Group B (induced abortion, n=220), taking the routine intrauterine operation by vacuum aspirator and Group C (medical with induced abortion, n=223), inserting a Gongshuan suppository into rectum 0.5 ~ 2 h before induced abortion operation.Some indices w ere compared, including the efficacy, vaginal bleeding volume and time, side effects and acceptability of the three abortion methods.Results The abortion effects of Group C and B are better than that of Group A (P<0.01).The vaginal bleeding volume of Group C is the least, then is the Group B, and the last is Group A (P<0.01).The vaginal bleeding time of Group B and C is apparently shorter than that of Group A (P<0.01).The infection rate after abortion operation of Group B and C is lower, compared with Group A (P<0.01, P<0.05).The acceptability rate of medical with induced abort ion is higher than that of the other two groups (P<0.01).Conclusion The medical with induced abortion is a safe, fast, less painful and less side effects approach to terminate early pregnancy, and it is easily accepted by patients.