Inhibition of motility of hamster spermatozoa by protein tyrosine kinase inhibitors

Genistein, tyrphostin and piceatannol, which are specific inhibitors of protein tyrosine kinase, were screened for their effects on the motility of intact and demembranated hamster spermatozoa. Of the three inhibitors only piceatannol inhibited the motility of intact spermatozoa. None of the inhibitors had any inhibitory effect on the reactivation of motility of demembranated hamster spermatozoa. Taken together these results indicated that a protein tyrosine kinase associated with the membrane of hamster spermatozoa was probably involved in sustenance of hamster sperm motility. Therefore in the present study a membrane-associated protein tyrosine kinase was purified from a detergent-soluble extract of plasma membranes of mature hamster spermatozoa. The purification involved cation exchange chromatography on fast protein liquid chromatography (FPLC) followed by affinity chromatography either on an antiphosphotyrosine antibody agarose or poly glu-tyr agarose column. The pure protein tyrosine kinase had an apparent molecular mass of 45 kDa. The enzyme was not inhibited by genistein or herbimycin but was inhibited by piceatannol. This is the first report on the purification of a sperm plasma membrane-associated protein tyrosine kinase, an enzyme which has also been implicated in hamster sperm motility.     

检测肾小球滤过功能的新方法——血清巯基蛋白酶抑制肽C

目的探讨测定血清巯基蛋白酶抑制肽C(CysC)的方法并评价其检测肾小球滤过功能的价值。方法对照组 2 1例、患者 10 7例 ,用全自动生化分析仪检测CysC、血清肌酐 (Scr)、尿肌酐 ,计算肌酐清除率 (Ccr)。根据Ccr将患者分成 4组。CysC用颗粒增强透射免疫比浊法 ,肌酐用肌氨酸氧化酶 PAP法测定。结果对照组CysC浓度为 1 2 5± 0 14mg/L ,患者组CysC随Ccr下降而升高 ,各组间差异显著 (P <0 0 0 1)。CysC与Ccr的相关性优于Scr与Ccr的相关性。CysC与性别、年龄无相关 ,而Scr男性显著高于女性 (P <0 0 0 1)。受试者工作特征 (ROC)曲线分析 ,CysC区别正常或异常肾功能的准确性较高 ,优于Scr。结论检测肾小球滤过功能CysC较Scr更好 ,不受年龄、性别的影响 ;本法可大批量、快速、准确测定 ,适于临床常规应用。     

血清Cystatin C对早期肾小球滤过功能受损的诊断价值

目的　评价CystatinC在反映早期肾小球滤过功能受损时的价值。方法　对 65例确诊有肾小球疾病患者同时测定血清CystatinC、β2 微球蛋白、BUN、Scr共 115例次 ,对其升高程度构成、浓度相关性、相对敏感性进行分析。结果　CystatinC浓度与BUN、Scr升高程度构成比较差异非常显著 (P <0 .0 1) ;CystatinC与 β2 微球蛋白、BUN、Scr浓度是正相关 (r 分别为 0 .90 7、0 .612、0 .419) ,并有显著意义 (P <0 .0 1) ,与CystatinC比较 ,β2 微球蛋白、BUN、Scr的相对敏感性分别为 95 %、43 %、3 1%。结论　血清CystatinC浓度可反映肾小球滤过功能受损的程度 ,可作为诊断早期肾小球滤过功能受损的敏感指标     

脂必妥胶囊对不稳定心绞痛患者C-反应蛋白的影响

目的　探讨脂必妥胶囊对不稳定心绞痛患者 C-反应蛋白的影响。方法　 86例 UA患者 CRP>3mg/ L ,分为两组 ,一组给予阿斯匹林、抵克立特、硝酸脂类药物常规治疗 ,一组在以上用药基础上再给予脂必妥胶囊 ,4～ 8周后再次检查 CRP浓度。结果　未服脂必妥胶囊组 CRP浓度变化无显著性 (P>0 .0 5 ) ,服用脂必妥胶囊组 CRP浓度下降显著 (P<0 .0 1)。结论　脂必妥胶囊具有降低 U A患者 CRP浓度的作用     

介入治疗对急性冠脉综合征血清C—反应蛋白的影响

目的：探讨经皮冠脉介入治疗术(PCI)对急性冠脉综合征患者C—反应蛋白(CBP)水平的影响。方法：94例急性冠脉综合征患者分为两组，观察组46例，行PCI；对照组48例，行冠脉造影。采用速率散射比浊法测定术前及术后血清CBP浓度。结果：观察组CBP浓度术后较术前明显增高(P＜0．05)；对照组CBP浓度术前术后无明显变化。结论：PCI术损伤血管内膜，可引起急性冠脉综合征患者血清CBP浓度升高。     

A new approach for 11C–C bond formation: Synthesis of 17α‐(3′‐[11C]prop‐1‐yn‐1‐yl)‐3‐methoxy‐3,17β‐estradiol

A new approach for ¹¹C–C bond formation via a Sonogashira‐like cross‐coupling reaction of terminal alkynes with [¹¹C]methyl iodide was exemplified by the synthesis of 17α‐(3′‐[¹¹C]prop‐1‐yn‐1‐yl)‐3‐methoxy‐3,17β‐estradiol. The LC‐purified title compound was obtained in decay‐corrected radiochemical yields of 27–47% (n=8) based on [¹¹C]methyl iodide within 21–27 min after EOB. In a typical synthesis starting from 9.6 GBq [¹¹C]methyl iodide, 1.87 GBq of 17α‐(3′‐[¹¹C]prop‐1‐yn‐1‐yl)‐3‐methoxy‐3,17β‐estradiol was synthesized in radiochemical purity >99%. The specific radioactivity ranged between 10 and 19 GBq/µmol, and the labeling position was verified by ¹³C‐NMR analysis of the corresponding ¹³C‐labeled compound. Copyright © 2003 John Wiley & Sons, Ltd.     

莫沙必利的核磁共振氢谱与碳谱指定

用一维和二维核磁共振技术(gCOSY，gNOESY，gHMQC，gHMBC)，对莫沙必利的核磁共振氢谱与碳谱进行了指定。计算机模拟的结果证明了我们对吗啉环优势构象的推测。     

巴豆属植物Croton hemiargyerius var.gymnodiscus中生物碱的研究

目的 从巴西巴豆属药用植物的一新变种复制Muel的叶中分离生物碱成分。方法 应用硅胶柱层析法分离和纯化，波谱分析与已知化合物的波谱和理化性质比较得以确定化合物结构。结果 分离得到12个生物碱，其中4个为新生物碱，命名为hemiargineA(1)，B(5)，C(6)和D(7)；8个已知生物碱为isocorydine(2)，corydine(3)，norcorydine(4)，salutaridine(8)，glaucine(9)，tetrahydropalmatrubine(10)，xylopinoine(11)和norlaudanosine(12)。结论 获得4种新化合物，除生物碱(8)，其余生物碱均为首次从该属植物中获得。