人卵促性腺激素释放肽（hF－GRP）及其类似物合成和生物活性初探

用固相法合成了ｈＦ－ＧＲＰ及其１５个类似物。全部裂解均用三氟甲磺酸完成。产物总收率６０％～８０％。对所有合成肽进行了影响离体的小鼠垂体分泌ＬＨ的活性筛选。结果表明，当合成肽的浓度为０．０５ｍｍｏｌ／Ｌ时：（１）将ｈＦ－ＧＲＰ的Ｃ端ＣＯＯＨ变成ＣＯＮＨ２，活性变化不大；（２）Ｃ端残基Ａｓｎ１４被Ｐｈｅ替换后刺激垂体分泌ＬＨ的活性明显高于ｈＦ－ＧＲＰ；（３）Ｔｈｒ３被Ｔｙｒ替换后片段ｈＦ－ＧＲＰ（３～１３）有抑制ＬＨ分泌的活性；（４）其余类似物与空白对照相似。     

盐酸苯乙哌啶和dl-15甲基PGF_(2α)甲酯对大鼠卵巢黄体细胞的影响

盐酸苯乙哌啶(R1132)10μg/ml或dl-15甲基PGF_(2α)甲酯(PG05)5或10μg/ml在体外能明显抑制黄体细胞对hCG的反应性,使孕酮分泌下降。假孕大鼠po R1132 10 mg/kg或Sc PG 05 5.1 mg/kg不影响卵巢孕酮分泌,合并给药后却能使其降低。R1132无抗孕酮作用。卵巢分泌孕酮减少可能是抗早孕的主要原因.假孕大鼠po R1132 50 mg/kg或sc PG050.5 mg/kg可抑制卵巢腺苷环化酶的活性.该酶可能是R1132或PG05在大鼠抗早孕作用的重要靶酶。     

Inhibitory activity of xanthine oxidase by fractions Crateva adansonii

ObjectiveTo study the inhibitory effect of various extracts from Crateva adansonii (C. adansonii) used traditionally against several inflammatory diseases such as rheumatism, arthritis, and gout, was investigated on purified bovine milk xanthine oxidase (XO) activity.MethodsXanthine oxidase inhibitory activity was assayed spectrophotometrically and the degree of enzyme inhibition was determined by measuring the increase in absorbance at 295 nm associated with uric acid formation. Enzyme kinetics was carried out using Lineweaver-Burk plots using xanthine as the substrate.ResultsAmong the fractions tested, the chloroform fraction exhibited highest potency (IC₅₀ 20.2±1.6 μg/mL) followed by the petroleum ether (IC₅₀ 30.1±2.2 μg/mL), ethyl acetate (IC₅₀ 43.9±1.4 μg/mL) and residual (IC₅₀ 98.0±3.3 μg/mL) fractions. The IC₅₀ value of allopurinol used, as the standard was 5.7±0.3 μg/mL.ConclusionsEnzyme inhibition mechanism indicated that the mode of inhibition was of a mixed type. Our findings suggest that the therapeutic use of these plants may be due to the observed Xanthine oxidase inhibition, thereby supporting their use in traditional folk medicine against inflammatory-related diseases, in particular, gout.     

联合术式治疗女性出口处梗阻性便秘57例

1临床资料我们1999-06/2004-10收治女性出口处梗阻性便秘176例,其中耻骨直肠肌肥厚、直肠黏膜内脱垂、直肠前突三者并存57例,占32.4%,均为经产妇;年龄26～76岁,分娩1～5胎;病程1～32 a.合理的肠道及阴道准备,体位为膀胱截石位.用络合碘消毒阴道及肛管直肠腔.     

氯化四乙基铵及维拉帕米对家兔缺血心肌不应期的影响

实验比较了K⁺通道阻断剂氯化四乙基铵(TEA)及Ca²⁺通道阻断剂维拉帕米(verapamil,Ver)对家兔缺血性心室肌不应期(ERP)的影响。结果表明,阻断冠脉10min及30min后,缺血中心区(CIZ)和缺血边缘区(BIZ)心肌ERP比缺血前均明显缩短,而TEA和Ver均能延长急性缺血性心肌的ERP,可能对心肌缺血引起的心律失常有预防作用。     

重症监护病房革兰阴性菌耐药现状研究

目的：了解我院重症监护病房分离菌株对常用抗生素的耐药现状。方法：采用琼脂双倍稀释法测定从我院重症监护病房分离的230株革兰阴性菌的最低抑菌浓度（MIC），并采用抑制剂增强的纸片扩散法测定大肠埃希菌和肺炎克雷伯菌超广谱β－内酰胺酶（ESBLs)。结果：50株肺炎克雷伯菌和17株大肠埃希菌中ESBLs阳性率为62．1％。阴沟肠杆菌、产ESBLs的大肠埃希菌和肺炎克雷伯菌对三代头孢、庆大霉素、阿米卡星的耐药率≥50％。而对碳青霉烯类非常敏感。铜绿假单胞菌对各种抗菌药物均有一定的耐药性。嗜麦芽寡养单胞菌对碳青霉烯类耐药率达100％。结论：受试的230株革兰阴性菌对三代头孢、复合青霉素、氨基糖苷类和环丙沙星的总耐药率≥30％。CPZ／SB和头孢吡肟、碳青霉烯类耐药率较低。     

硝基甘油对狗缺血区冠脉循环的作用

用实验性犬冠脉狭窄模型,冠脉内恒流灌注硝基甘油0.5μg/kg.min^-1,使冠脉血流量(CBF)增加、远端小动脉压(DCP)、冠脉血管总阻力(R_T)、小冠脉血管阻力(R_S)及冠状静脉低切血粘(η_b)减少;而主动脉压和心率无明显变化。恒流灌注硝基甘油1μg/kg.min^-1时,在开始5min内冠脉循环的变化同上,并伴大冠脉血管阻力(R_L)减少,10 min后出现CBF减少和R_T,R_{L及ηb增加。结果提示,硝基甘油有缓解和加重心肌缺血的双重作用,其作用可能与剂量张扩张远端小动脉压的程度有关。}