1.Anticonvulsant activity of allopregnanolone against pentylenetetrazol- induced seizures in rodents
Chinese Journal of Tissue Engineering Research 2001;05(1):155,157-
Objective To examine the protective effects of allopregnanolone against pentylenetetrazol- induced seizures. Methods The protective effects of allopregnanolone against pentylenetetrazol- induced seizures were studied in C57 mice and SD rats 15 minutes after vehicle or drug intraperitoneal (ip) administration. Results The pretreatment with the allopregnanolone produced a dose- dependent protective effect against pentylenetetrazol- induced seizures. The potencies (ED50 values) were 4.7 mg/kg and 9.8 mg/kg for mice and rats, respectively. Conclusion Allopregnanolone has anticonvulsant activity against pentylenetetrazol- induced seizures in rodents.
2.Molecular mechanism of protective effects of estrogen on cerebral ischemia
Chinese Journal of Clinical Pharmacology and Therapeutics 2000;0(02):-
Estrogen has the protective effect on cerebral ischemia in v ar ious ways. It not only can improve the regional cerebral blood flow during ische mia and rescue the remaining neurons alive, but also can reduce the injury of is chemia-reperfusion. In this article, we enumerate at the molecular level that e strogen has the properties of inhibiting the expression of VCAM and cytokines li ke TNF-? in the ischemia region, educing the overload of calcium and cytotoxic ity of EAA by modulating the calcium channels, and regulating related genes expr ession and anti-apoptosis. It is crucial for estrogen replacement therapy as a neutoprotectant clinically.
3.Discourse on the development and reform of medical education in 21'st century:Flexner Report'inspiration
Chinese Journal of Medical Education Research 2011;10(1):36-39
The famous Abraham Flexner's 1910 report to the Carnegie Foundation launched the modern medical educmion.The report'S focus on the medical education standards and the curricula frameworks was laudable and appropriate.At the centennial of this report.we were still able to get a lot of inspiration and the direction of development and reforms of medical education by reviewing Flexner'd Report.
4.On the Concept of Clinical Thinking
Chinese Journal of Medical Education Research 2002;0(01):-
At present the concept of clinical thinking is reviewed at the narrow senses and there are many limitations.So it is very necessary to understand the concept of clinical thinking at the broad senses.
5.The synthesis and metabolism of neurosteroids and the effects on the nervous system
Dan WANG ; Yingqing LU ; Rong YU
Chinese Journal of Clinical Pharmacology and Therapeutics 2004;0(07):-
Neurosteroids exist in central and peripheral nervous system, independence of peripheral glands, including pregnenolone, progesterone, allopregnanolone, and dehydroepiandrosterone, etc. They can be synthesized in the nervous system from sterol or sterol precursors catalyzed by certain enzymes. They play roles by interacting with GABAA, NMDA or?receptors, and have effects on memory, sleep, convulsion, cellular excitability, etc.
6.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.
7.Novel small-molecule CDK2-cyclinA2 inhibitors: design, synthesis, and biological evaluation
Yingqing WEI ; Lu ZHANG ; Yutong HU ; Jian ZHANG ; Ying SHEN
Journal of Shanghai Jiaotong University(Medical Science) 2017;37(3):330-336
Objective · To design and synthesize a series of benzenesulfonamide derivatives, test their inhibitory activity to CDK2-cyclinA2 kinase, and investigate the structure-activity relationship. Methods · Virtual screening was executed via computer-aided drug design according to the ATP binding site in CDK2-cyclinA2 protein crystal. A series of benzenesulfonamide derivatives were designed and synthesized on the basis of the interaction modes between the lead compound and the CDK2-cyclinA2. The biological evaluation of compounds was made through the CDK2-cyclinA2 in-vitro kinase activity detection system. Results · Twenty-nine new benzenesulfonamide compounds were prepared, and their inhibitory activity to CDK2-cyclinA2 was elicited. WZ-026 had the highest inhibitory parameter, which half maximal inhibitory concentration (IC50) was 3.81 μmol/L. Conclusion · By multipurpose utilization of virtual screening, chemical synthesis, and biological activity test, a benzenesulfonamide compound WZ-026 was found, which has great inhibitory activity towards CDK2-cyclinA2. Preliminary structure-activity relationship of compounds was obtained.
8.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.
9.The Reliability and Item Quality of Ten Medical Academic-courses From Two Angles
Yong ZENG ; Xueshan FENG ; Gang CHEN ; Yingqing LU
Chinese Journal of Medical Education Research 2003;0(04):-
Underlying both the angles of norm-referenced test and criterion-referenced test, the qualitative or(and)quantitative analysis and evaluation were made on the tests of 10 medical academic courses in recent 4 years in reliabil-ity and item quality. From the angle of norm-referenced test, 67.4 percent of the items had good quality, 60 percent ofthe tests could differentiate the classes and 12.5 percent of the papers could differentiate the individual person accord-ing to their reliability. However, from the angle of criterion-referenced test, approximately 90 percent of the items werequalified; 87.5% had high reliability to determine whether an examinee passes the test or not.[
10.Reformation and Exploration of Contents and Methods in Teaching Pharmacology for the Students in Major of Basic Medical Science
Surong YANG ; Minghui YAO ; Yiqun YANG ; Yingqing LU
Chinese Journal of Medical Education Research 2003;0(02):-
Directing at the cultivating aims of the students in major of basic medical science,the article expounds some instruction innovations in teaching pharmacology.We introduce some social practical problems and some research fields which evolve rapidly to the teaching class by compiling the teaching materials,conducting lectures and giving discussion lessons.In addition,we incorporate the cultivation of students' capability of doing scientific research to the teaching work through guiding them how to read references,directing them to finish independently the project of experiment designed by themselves and operating group activities instructed by their supervisors in the department of pharmacology.