1.Protective effects of allopregnanolone against different seizure models in mice
Chinese Journal of Clinical Pharmacology and Therapeutics 2000;5(2):97-100
Aim To examine the protective effects of allopregnanolone against seizure on different animal models.Methods The protective effects of allopregnanolone against maximal electrical seizure (MES) and picrotoxin-induced seizure were studied in C57 mice 15 minutes after vehicle or drug intraperitoneal administration.Results In the MES test, 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 MES test 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 MES test 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 allopregnanolone resulted in a 80% of protective effect in MES test, which was higher than 50% produced by either phenobarbital or allopregnanolone at their ED50 values respectively. This result indicated that there was a synergism between phenobarbital and allopregnanolone in their anticonvulsant activities. In the picrotoxin test, we found that pretreatment with the allopregnanolone also produced a dose-dependent protective effect against picrotoxin-induced seizure. The potency of allopregnanolone in the picrotoxin seizure test 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 different seizures in a dose-dependent manner,had a higher potency than phenobarbital,and had synergism with phenobarbital in the MES test.
2.Comparison of vasoconstrictive effect of histamine on the isolated rabbit central and peripheral arteries in vitro and its mechanism
Huijing WANG ; Aizhen WU ; Minghui YAO ;
Chinese Journal of Clinical Pharmacology and Therapeutics 1999;0(04):-
AIM: To compare the effects of histamine and its antagonists on tension of isolated rabbit basilar and mesenteric artery in vitro, and to observe the role of Ca 2+ in histamine induced response. METHODS: The dose response curves induced by histamine were recorded on the isolated rabbit central and peripheral arteries in different doses of diphenhydramine, cimitidine, and nifidipine. RESULTS: Histamine could cause contraction of basilar and mesenteric isolated arteries. Diphenhydramine and nifidipine antagonized these effects, while cimitidine enhanced this effect. CONCLUSION: There may be different receptors densities in different rabbit arteries; histamine shows the vasoconstrictive effect on both brain and mesenteric arteries; and the vasoconstrictive effect mainly produces via Ca 2+ inflax.
3.Protective effects and mechanisms of salidroside on cerebral ischemia-reperfusion injury
Jingye WANG ; Rong YU ; Minghui YAO
China Journal of Traditional Chinese Medicine and Pharmacy 2005;0(03):-
Objective:To explore the protective effects and mechanisms of salidroside on cerebral ischemia-reperfusion injury in middle cerebral artery occlusive(MCAO)rats.Methods:Focal cerebral ischemia in rats was produced by 1.5 h occlusion of the middle cerebral artery and 24 h reperfusion.Salidroside was administered intravenously immediately after occlusion and reperfusion respectively.The neurologic deficit scores were investigated according to Zea-Longa's Standard.The infarct areas were assessed with software Imagepro Plus 6.0 after TTC staining.And the activities of inducible nitric oxide synthase(iNOS)as well as glutathione peroxidase(GSH-Px)were determined by specific kit.The levels of B cell lymphoma/lewkmia-2(Bcl-2)and Bcl-2 assaciated X protein(Bax)in central neutral system were assessed by western blot.Results:Compared with the model group,salidroside could decrease the neurologic deficit score,reduced the infarct areas of the brain in MCAO-I/R rats,increased the activity of GSH-Px and decreased the activity of iNOS,enhanced the expression of Bcl-2,depressed the expression of Bax.Conclusion:Salidroside has a protective effect on cerebral ischemia-reperfusion injury and this effect is related to attenuating lipid peroxidation,enhancing the expression of Bcl-2 and diminishing Bax expression.
4.Anticonvulsant action of L-histidine in mice
Aizhen WU ; Huijing WANG ; Minghui YAO
Chinese Journal of Clinical Pharmacology and Therapeutics 2000;0(01):-
AIM: To observe the anticonvulsant action of L-histidine in mice. METHODS: The anticonvulsant effect of L-histidine, and the antagonism of dl-chlorpheniramine to L-histidine were observed in convulsion mice induced by pentylenetetrazole (PTZ) and electric stimulation. RESULTS: L-histidine exerted remarkable anticonvulsant action with dose-response relationship in convulsion mice induced by pentylenetetrazole and electric stimulation, and the action was partly antagonized by dl-chlorpheniramine. CONCLUSION: L-histidine has anticonvulsant effect, and the action was partly antagonized by dl-chlorpheniramine, suggesting that L-histidine can pass the BBS and enter the central nervous system.
5.Antitumor effects of novel thymidylate synthase inhibitor ZD1694 in vitro and in vivo
Ling LI ; Surong YANG ; Minghui YAO
Chinese Journal of Clinical Pharmacology and Therapeutics 2002;0(06):-
10 mg?kg -1?d -1? 5 d. The inhibitory rate of ZD1694( 0.001- 1 000 mmol?L -1)on SGC-7901 cells were increased in concentration and time-dependent manner. The cell numbers in G_0-G_1 phase in SGC-7901 cells were raised by ZD1694 as well. CONCLUSION: ZD1694 can take obvious antitumor effects on S180-bearing mice. The antitumor rate of ZD1694 is in a dose-dependent manner, and it is higher when the total dosage is administered in one day than that the total dosage was divided into 5 consecutive days. ZD1694 can inhibit the growth of SGC-7901 cells and block the cells in G_1 phase in vitro.
6.Follow-up survey on general practitioners after residency training in Shanghai
Minghui PENG ; Xiangjie ZHANG ; Yao LIU ; Hui LI ; Sunfang JIANG
Chinese Journal of General Practitioners 2016;15(6):430-433
Objective To survey the current working status of general practitioners (GPs) who received residency training in Shanghai.Methods The current status of general practitioners,who completed residency training in Shanghai from 2013 to 2014,was surveyed with self-designed questionnaire by e-mail.The survey items included current employers,job specification,clinical practice,teaching,scientific research and so on.Results Three hundred and thirteen out of 377 GPs,who completed residency training from 2007 to 2012,participated in the survey (83.0%),including 85 males and 228 females with a mean age of (31.2 ± 2.6) years.Among all participants,298 (95.2%) worked in community health service centers,12.8% (40/313) of them were involved in general practice teaching,9.9% (31/313) undertook management,9.3% (29/313) did academic research in community,and 7.7% (24/313) had chance for overseas study.The survey also showed that 134 person/times received various commendations and awards.Conclusion Most GPs who completed residency training are undertaking clinical practice in community health service centers,and they are also well involved in management,teaching,and research.
7.Effect of soybean isoflavones on ventricular remodeling induced by myocardial infarction in rats
Yue LI ; Minghui YAO ; Yingqing LU ; Qinyan GONG
Chinese Journal of New Drugs and Clinical Remedies 2006;25(4):241-247
AIM: To investigate the effect of soybean isoflavones (SI) on ventricular remodeling induced by myocardial infarction (MI). METHODS: MI was induced by permanent ligation of the left anterior descending coronary artery (LAD) in male Sprague-Dawley (SD)rats. Rats were randomly divided into six groups: shamThree hours after the operation, the drugs or solvent were administrated ig qd for 35 d. Twenty-four hours after the last administration, heart rate (HR), left ventricular end-diastolic pressure (LVEDP), peak systolic left ventricular pressure (Peak), maximal rate of left ventricular pressure rising (+dp/dtmax), maximal rate of left ventricular pressure declining (-dp/dtmax) and myocardial maximal shortening velocity (Vmax) were measured. After above hemodynamic parameters were measured, hearts were extracted. The ratio of total ventricle weight to body weight(TVW/BW) was calculated. Myocardial collagen was shown with the collagen-specific picrosirius red stain,myocardial interstitial collagen volume fraction(ICVF), perivascular collagen volume fraction(PCVF), infarct size,septal thickness (ST) and left ventricular diameter (LVD) were measured by image analysis system. RESULTS:(31 ± 5) %, respectively, all of which were significantly smaller than that in MI group (( 38.9 ± 2.9) %, P < 0.01 ).In MI group, TVW/BW, LVD, ICVF and PCVF were remarkably increased compared with those in sham group (P < 0.01 ). The increased TVW/BW, LVD, ICVF and PCVF were significantly reduced by treatment with eaprats in MI group was significantly decreased than that in sham group (P < 0.01 ). The reduced ST could be in-dp/dtmax and Vmax were decreased (P < 0.01 ), while LVEDP was increased (P < 0.01 ), significantly. The reSION: SI can improve cardiac function and ventricular remodeling induced by myocardial infarction in the rat.
8.Effect of genistein on c-myc mRNA expression induced by low density lipoprotein in endothelial cells
Jin LIU ; Minghui YAO ; Qinyan GONG ; Rong YU ; Yingqing LU
Chinese Journal of New Drugs and Clinical Remedies 2003;22(1):5-8
AIM: To study the effect of genistein on c-myc mRNA expression induced by oxidized low density lipoprotein (ox-LDL) in human vascular endothelial cells (ECV304). METHODS: LDL were isolated from healthy human plasma by gradient ultracentrifugation and oxidized by CuSO4. ECV304 cells were exposed to ox-LDL 200 mg*L-1 in the presence or absence of genistein 100 μmol*L-1 for 1, 2, and 4 h in vitro. Northern blot was employed to measure c-myc mRNA levels of ECV304. RESULTS: In response to ox-LDL 200 mg*L-1, c-myc mRNA expression in ECV304 increased by 3 fold for 1h and 3.3 fold for 2 h and decreased below the control level at 4 h. Expressions of c-myc stimulated by ox-LDL in the presence of genistein 100 μmol*L-1 for 1 h and 2 h were separately 80 percent and 60 percent of that in the absence of genistein 100 μmol*L-1. CONCLUSION: Genistein can effectively inhibit c-myc mRNA expression in ECV304 induced by ox-LDL.
9.Comparison of anxiolytic effects of allopregnanolone and diazepam on the elevated plus-maze in mice
Rong YU ; Yingqing LU ; Meiping SHENG ; Nianci SHI ; Minghui YAO
Chinese Journal of Clinical Pharmacology and Therapeutics 2000;5(1):6-9
To compare the anxiolytic effects of reduced metabolite of progesterone and benzodiazepine.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 (0.1 mg.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).Meanwhile,the diazepam (0.25 mg·kg-1) produced a lower anxiolytic effect comparing to that of the allopregnanolone.Analysis of spontaneous locomotor activity showed while 0.5 mg·kg-1 of diazepam decreased the locomotor activity (P<0.01),neither 0.1 mg·kg-1 of allopregnanolone nor 0.25 mg·kg-1 of 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.
10.Inhibitory effect of domestic leuprorelin acetate microspheres on experimentally induced endometriosis in rats
Xinhong XU ; Linghong GUO ; Qinyan GONG ; Linai CHEN ; Minghui YAO ;
Chinese Journal of Clinical Pharmacology and Therapeutics 2000;0(03):-
Aim To study the effect of leuprorelin acetate microspheres (LE ms) on endometriosis in rats, and compare the efficacy of material drug (LE), domestic and imported LE ms (enanton). Methods Endometriosis was induced by endometrial implant in rats. Then the animals were treated with LE (20 ?g?kg -1 ?d -1 ? 28 d ,sc), enanton(20 ?g?kg -1 ?d -1 ,sc)and domestic LE ms ( 2,20,200 ?g?kg -1 ?d -1 ,sc). Results Implants in control group continued to grow, while those in groups treated with drugs shrinked significantly, and domestic LE ms could produce dose dependent inhibitory effect on the growth of endometrial implant in rats. Conclusion The domestic LE ms at the single dose of 20 ?g?kg -1 ?d -1 has the same effectiveness as enanton and routine injection with the same does of LE for 28 days.