目的 探索疫情期间药物化学专业研究生教育模式.方法 使用在线教育模式.鉴于不同阶段的研究生在知识储备、实验操作能力、学习能力及培养目标方面都有显著差异,因此同时进行差异性教育.结果 于在线教育模式的基础之上,结合药物化学学科特点,对不同阶段的研究生在教育内容、教育方式及考核方式上采取差异性培养方案,取得了与疫情之前线下教育相当的研究生培养质量,并为未来的研究生在线教育积累宝贵的经验.结论 疫情期间合理使用线上教学模式可以达到与疫情前相当的研究生培养质量.

大型精密仪器是高等院校创新人才培养和科学研究的重要支撑条件,能否把大型精密仪器有效应用于本科实验教学,对于提高本科生的科研素养和创新能力具有重要作用.结合郑州大学药学院的大型仪器平台情况,针对大型仪器设备的使用现状及存在的问题提出可能的解决方案.通过加快仪器实验教材更新速度、采用开放式实验教学模式、加强对大型仪器管理人员的培训、加强对本科生使用大型仪器的培训、完善药物化学实验教学内容等,进一步提高大型精密仪器在药物化学实验中的使用率,激发本科生学习和使用大型精密仪器的兴趣,培养学生的科研素养和创新能力.

目的 为培养适应社会发展需求的高层次药学人才,探索与应用药物化学立体教材.方法 通过优化电子教案,制作微课视频,建立交流平台等方式,将教材立体化、形象化,给学生提供更多的学习资源和学习手段.结果 学生学习积极性提高,成绩提升,对专业知识的理解和领悟能力明显加强.结论 药物化学立体化教材的建设具有很好的实践意义,为"双一流"建设背景下探索药学类创新人才培养模式奠定良好的基础.

Aim:To clone the key enzyme gene,CYP6003A1,which was involved in the reaction of fusariumoxysporum,which could transform drospirenone into an important intermediate(7α,15α-diOH-DHEA).Methods:Primers were designed according to the CYP gene of fusariumoxysporum.The total RNA of fusariumoxysporum was extracted by the method of Trizol extraction from fusariumoxysporum induced by DHEA for 48 h,and the CYP gene of fusariumoxysporum was amplified by PCR and sequenced.The bioinformatics were analyzed.Results:A full-length cDNA fragment of 3 459 bp was successfully amplified.After sequencing,the amino acid sequence of the CYP6003A1 gene was screened by BLAST on NCBI.The results showed that the first 10 genes were similar to CYP6003A1,among them,three were CYP gene,and the others were genes related to CYP gene.The result of bioinformatics analysis showed that the gene fragment encoded 691 amino acids polypeptide.Conclusion:CYP6003A1 gene has been successfully cloned from fusariumoxysporum and analyzed by bioinformatics.

目的:从本地土壤中筛选出一株对炔雌醇有转化能力的真菌,经形态观察,鉴定为镰刀属真菌,利用该菌株对炔雌醇进行微生物转化研究.方法:转化产物经柱层析分离后,利用质谱、二维核磁图谱等分析方法,确定了产物的结构.结果:底物炔雌醇被LZ0202菌株转化为6α-羟基-17α-乙炔基雌二醇.结论:化合物是炔雌醇衍生物类避孕药的一种重要的中间体,也是其相关研究中的重要参考指标和对照品,本研究为炔雌醇及其衍生物的进一步研究提供了物质条件和理论基础.

Dihydroepiandrosterone(DHEA) is one important bioactivity compound and one important intermediate of steroid drugs.It is for the first time to report the biotransformation of DHEA by Mucor circinelloides and two products was obtained.Furthermore,the 16-benzylidene derivatives were synthesized by Claison-Schimidt reaction.The cytotoxic evaluation showed that these derivatives had better activity than the parent compound.

为提高教学质量、培养创新性药学人才,以药物化学学科建设为中心,以教研室为基础,组建了药物化学教学团队,将学科优势转化为教学优势,为培养复合型创新性药学人才做出积极贡献。

随着社会经济的发展和人民生活水平的提高,对医药行业提出了新的要求,培养高素质的高等药学人才是推动药学领域发展的关键。通过本课题的探索研究,对课程体系、教学内容和方法进行改革,改变传统的培养药学人才模式,构建合理的教学方案,形成一套复合型药学人才培养模式。

<正>高校教育的根本任务是培养适应社会发展的需要的人才,我国正处于经济高速发展与转型时期,而随着中国的日渐国际化,对高等药学人才的要求也越来越高,旧的"灌输型"的教学模式已不适应发展的需要,为了培养高素质的药学人才,进行药物化学教学的改革工作刻不容缓。

Ojbective:To study the effects of erythromycin treatment to endotoxin-induced ALI(acute lung injury) in rat model.Methods: The rat model of ALI was made by injecting lipopolysaccharide(LPS) with a dose of 4mg/kg into vena caudalis.54 male SD rats were randomly divided into three groups: control group(NC),experiment group(LPS) and treatment group(EY),18 rats every group.In control group physiologic saline was injected,in experiment group LPS was injected,in treatment group LPS was injected as time as erythromycin injectable powder intraperitoneal injection(50 mg/kg).Measured the levels of IL-1β,IL-6,TNF-α,IL-8,IL-10 in serum and alveolar wash liquid of 54 rats by enzyme-linked immunosorbent assay(ELISA).Results:Compare treatment group with experiment group,PaO2 and pH stepped up,PaCO2 stepped down,lung coefficient was(0.62±0.07 vs 0.96±0.13,P0.05),lung water content(85.76±0.56 vs 82.88±0.47,P0.05),lung permeability index(7.41±0.61 vs 12.26±0.58,P0.05),all decreased significantly,IL-1β,IL-6,IL-8 and TNF-α in serum and alveolar wash liquid stepped down,however,IL-10 stepped up significantly.The lesion of lung tissue in treatment group was lighter than that in experiment group through pathology observing.Conclusion: Erythromycin can

Aim: To design and synthesize new azasteroids with potential bioactivities.Methods:Dehydroepiandrosterone was transformed to its 17a-aza derivative through 3 reaction steps including acetylation,oximation and Beckmann re-arrangement.The 17a-aza derivative was then transformed by fungus of Mucor circinelloides lusitanicus.Results and conclusion:17a-aza derivative of dehydroepiandrosterone was obtained with 78% yield by improving the synthesis method.The fungus could transform this kind of compound by hydrolyzing the ester and 7α-hydroxylation.All of the compounds were identified by IR,NMR and MS spectrum.

OBJECTIVE To prepare betaxolol hydrochloride-resin complexes with bath method and study its in vitro drug release.METHODS The factors effecting exchange reaction kinetics of betaxolol hydrochloride were studied with different temperature and betaxolol's concentration.The drug release were investigated in different releasing media (deionic water,0.5 mol·L-1, 1.0 mol·L-1,2.0 mol·L-1NaCl,0.5 mol·L-1 HCl and 0.5 mol·L-1 KCl).RESULTS The exchange rates and drug-loading increased with increasing in temperatures and concentration.The release rate increased with increase of ionic strength of the medium.CONCLUSION Betaxolol hydrochloride-resin can be prepared and excellent release was suitable for new dosage forms.

2004年5月至2006年3月,南阳市中心医院肿瘤科分别采用利血生加升血小板胶囊、国产重组人白细胞介素-11(rhIL-11)治疗恶性肿瘤放化疗后血小板减少症患者52例,并比较2者的疗效,现报道如下.

AIM: To observe the alterations of all kinds of pathophysiological and biochemical markers in rat model with endotoxin-induced acute lung injury (ALI) after pentoxifylline (PTX)treatment so as to approach the intervention effect of PTX treatment on ALI. METHODS: The rat model of ALI was made by injecting lipopolysacharide (LPS) at a dose of 4 mg/kg into vena caudalis. Seventy-two male SD rats with matched month age and weight were randomly divided into 3 groups: control group (NS), experimental group (LPS) and PTX treatment group, 24 rats each group. In control group physiologic saline was injected into vena caudalis; in experimental group 4 mg/kg LPS was injected into vena caudalis; in treatment group 0.036 mol/L PTX (10 mg/kg) was intraperitoneally (ip) injected 1 h before LPS injection into vena caudalis. Instantly after ALI rat modes were established successfully in erperimental group, 10 mg/kg PTX was injected ip, totally for 5 times, at an interval of 1 h; in the other 2 groups, same-volume physiologic saline was given in the same way. We determined PaO2, pH, PaCO2, lung coefficient, lung water content, lung permeability index, and detected the percentages of neutrocyte and macrophage in bronchoalveolar lavage fluid, the levels of malondialdehyde(MDA), superoxide dismutase(SOD), nitric oxide(NO) and inducible nitric oxide synthase(iNOS), and observed the pathomorphology of lung tissue. RESULTS: In treatment group compared with experimental group, PaO2 and pH stepped up, PaCO2 stepped down, lung coefficient (0.59±0.17 vs 0.92±0.11, P<0.05), lung water content(84.46±0.39 vs 80.22±0.37, P<0.05), lung permeability index(7.28±0.54 vs 12.32±0.28, P<0.05) were all decreased significantly, the percentage of neutrocyte in bronchoalveolar lavage fluid was reduced, NO and iNOS were depressed significantly, and SOD was improved significantly(P<0.05). The lesion of lung tissue in treatment group was lighter than that in experiment group through pathological observation. CONCLUSION: PTX can improve energy metabolism and reduce the cytotoxicity in LPS-induced ALI rats. PTX plays a role in intervening and preventing the development of ALI.

从土样中筛选到1株能转化甾体的菌株,经形态观察,鉴定为总枝状毛霉(Mucor racemoosus).利用该茵株对去氢表雄酮进行生物转化研究,转化产物分离后,通过红外、质谱和二维核磁波谱分析,确定了化学结构.研究结果表明转化产物是7α-羟基去氢表雄酮和7β-羟基去氢表雄酮.

Objective In order to contrast the therapeutic outcome of omeprazole and mosapride treating reflux esophagitis and to summarize and evaluate the curative effects and applicable scope of the two,24-hours esophageal pH monitoring combined with clinical symptom and endoscopic observation was used.Methods 72 patients with reflux esophagitis identified and dignosed by endoscopic were collected in Hospital of Anyang Iron Steel Group from Jan.2002 to Dec.2005.The patients were divided into three groups randomly: associated-dose group(24 cases)/ omeprazole group(24 cases)/ mosapride group(24 cases),observing their corresponding therapuatic effects.Associated-dose group: treated with omeprazole 20mg qd every morning,and mosapride 5mg tid,30 minutes before every meal;omeprazole group: treated with omeprazole 20mg qd every morning;mosapride group: treated with mosapride 5mg tid,30 minutes before every meal.The period of treatment was 4 weeks,observed markers such as pyrosis,spontaneous esophageal chest pain,regurgitation,acid reflux,belching clinical symptom,dysphagia,the detect data for the pH of esophagus in 24-hours esophageal pH monitoring,and countercheck endoscopic results for 4 weeks after treatment were taken as criteria for comparison.Results The symptom control rates in associated-dose group,omeprazole group and mosapride group for 2 weeks after treatment were 83.33%,70.83% and 54.17%,respectively(P0.05);for 4 weeks after treatment were 95.83%,91.67% and 79.17%,respectively(P0.05);the endoscopic efficiency was 95.83%,83.33% and 62.50%,respectively(P0.05);the data for pH detect in esophagus were improved.Those in omeprazole group were similar with that in mosapride group.However,for the group with grade Ⅱ～Ⅳ esophagitis,the endoscopic effects and the improvement for pH detect in omeprazole group were better than those in mosapride group,but the therapeutic effects in omeprazole group and mosapride group were not as good as those in associated-dose group.Conclusion Omeprazole and mosapride have good theraputic efftcts for reflux esophagitis.For the reflux esophagitis above grade Ⅱ,treating patients with only omeprazole is better than mosapride,but both of their therapeutic effiency are not as good as those treated by combining omeprazole with mosapride.Above all,the research shows that it is very reasonable and meaningful to treat reflux esophagitis corresponding their grades.

The effect of potassium borohydride on ester and carboxylic acid reduction was introduced.It was pointed out that the effect was not properly explained in the present textbooks.A better understanding of the effect was achieved in this paper.

Objective To observe the effects of pentoxifylline(PTX) on newborn rats with hypoxic-ischemic encephalopathy(HIE). Methods Models of 7-day-old newborn Wistar rats with HIE were established and 72 rats were randomly divided into sham operation group,HIE model group and PTX group.72h after hypoxic-ischemic operation the left side brains were taken out and the water content,intracellular calcium content(%) and the level of SOD,MDA,NOS,NO were measured. Results Compared with HIE model group,the content of water and calcium and the level of MDA,NOS,NO were markedly reduced(P0.05,0.01,0.05,0.05,0.05),while the levels of SOD were increased significantly(P0.05). Conclusion PTX could protect brain of neonatal rat against hypoxic-ischemic damage,which might be the result of the improvement of energy metabolism and the removal of local cytotoxic substance.

Aim: To obtain the hydroxylated derivatives of 4-pregnen-3,20-dione. Methods and Results: 4-pregnen-3,20-dione was transformed by microorganism with Macor racemosus and the resultant was identified to be 14β-hydroxy-pregnen-3,20-dione and 7β,14β-dihydroxy-pregnen-3,20-dione by testing the point of fusion,infrared rays,NMR and mass spectrometry analysis. Conclusion: With the method of microorganism transformation, steroidal derivatives which is prepared difficultly by chemical methods can be easily obtained.

药学英语的目的是培养学生阅读有关英语专业材料的能力,即掌握必要的词汇,为本专业的语言交流(口语和写作)打下坚实的基础.药学英语水平不仅是文化素质的重要组成,而且在很大程度上也是能力的补充和延伸.所以,教好药学英语,对于药学专业学生综合素质的培养至关重要.