Synthesis and Purine P2X Receptor Antagonist Activity of Thiazole Derivatives

The ability of 12 new thiazole derivatives to influence the muscle contractility mediated by purine P2X receptors has been studied in vitro using isolated tissues of rats and guinea pigs. Most of the synthesized compounds did not cause significant effects, but two compounds exhibited pronounced antagonism with respect to P2X-mediated contractility response. These compounds offer a good starting point for the synthesis of new effective antagonists of P2 receptors. __________ Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 39, No. 6, pp. 22 – 25, June, 2005.     

Effect of kanamycin on the cochleas in guinea pigs

Kanamycin (400 mg/kg) was injected daily for 5 days in guinea pigs, the changes in CM and AP responses were recorded. The CM threshold was elevated in 34.5% of the animals and the CM amplitude was reduced when compared with normal animals (P less than 0.005). The AP threshold was elevated in 13.8%. The latency of N1 was increased (P less than 0.001) and the amplitude of N1 reduced at 80 dB (S-L) (P less than 0.001).cAMP and cGMP levels in the organ of Corti and stria vascularis spiral ligament decreased, and the decrease correlated with the changes in auditory function. We consider the reduction of cyclic nucleotides in the cochlea may be important in kanamycin ototoxicity.     

关于我国体外诊断试剂监督管理改革的建议

本文综述了美国、欧盟、日本、中国目前对体外诊断产品（试剂）监督管理的现状以及我国存在的问题。并根据我国具体情况提出了对体外诊断试剂监督管理的改革建议。     

Freiberg’s Infraction in Identical Twins: A Case Report

Freiberg's infraction is an ostechondrosis of a lesser metatarsal head resulting in degeneration of the metatarsophalangeal joint. Several mechanisms have been suggested in its pathenogenesis. Freiberg first described the entity and believed single impact trauma was the underlying cause. Repetitive biomechanical microtrauma is the most widely accepted etiologic theory. Other factors contributing to its development include aseptic necrosis, ischemia, and a congenital predisposition. We present a case report of Freiberg's infraction occurring in identical twins involving multiple metatarsals in various stages of degeneration. One of the twins was affected unilaterally whereas the other twin was affected bilaterally. Both twins had involvement of the second metatarsal on the same side extremity. The occurrence of Freiberg's infraction in identical twins suggests that an underlying congenital predisposition to the condition may play more of a role than previously considered.     

神经化组织工程骨构建的初步观察

目的评估两种组织工程骨体内神经化重建方法的成骨效果,研究神经化与成骨的相互关系。方法26只新西兰大白兔,其中24只随机分成四组:组织工程骨组(A组),感觉神经束植入组(B组),运动神经束植入组(C组),血管束植入组(D组);另2只为空白对照组。每只动物均制备左侧股骨长1.5cm的段缺性骨与骨膜缺损,钢板固定后骨缺损处分别植入用四种方法制备的组织工程骨。植入的神经分别是隐神经和股神经肌支。术后4、8、12周摄股骨正位X线片,用放射影像学评分和X线阻射影分析比较骨缺损修复情况。结果在组织工程骨中植入感觉神经束后,比单纯组织工程骨和运动神经束植入的修复效果均有明显提高,而在组织工程骨中植入运动神经束与单纯组织工程骨修复骨缺损的效果相比较无明显差异,感觉神经束植入与血管束植入的成骨效果比较无明显差异,血管束植入组的成骨效果优于其它两组。结论利用感觉神经束植入的方法可以提高组织工程骨的成骨作用,而植入运动神经束却无此作用。     

Effect of nuclear factor-κB p65 ASOND on I typ collagen expression and rat hepatic stellate cells proliferation

Objective Sstudy effect of nuclear factor-κB ASOND on I type collagen expression and rat hepatic stellate cells(HSC)proliferation.Methods Rat HSCs were separated by affusing and digestingof Ⅳ type collagenenzyme and density acentric method.Lipid-mediated NF-κB p65 ASOND(0.001,0.01,0.1,1μmol/L)Was transferred into rat HSCs.Toxicity of HSCs caused by NF-κB p65 ASOND and activity of LDH were determined by trypan blue staining.Proliferation affection of transferring NF-κB p65 ASOND into HSCs was determined by MTT.In different concentration NF-κB p65 ASOND.expression of Ⅰ type collagen stimulated by 1mg/L TNF-αwas determined by RT-PCR and ELISA.Results After transfection of NF-κB p65 ASODN,expression of NF-κB protein in HSCs was decreasing.Toxicity experiment indicated that NF-κB p65 ASOND of different concentration(0.001,0.01,0.1 and 1.0 μmol/L)had no effect on HSCs livability and LDH activity(P<0.05).Four different concentration NF-κ B p65 ASOND could restrain HSCs proliferation stimulated by 1 mg/L TNF-α.The expression of I type collagen and mRNA stimulated by 1mg/LTNF-αwas increased,and had a positive correlation with concentration(P>0.05).Conclusion NF-κB p65 ASOND may depress NF-κB activity to restrain HSCs proliferation and Ⅰ type collagen expression,and reduce extracellular matrix.     

Crohn病的CT表现

目的探讨Crohn病的CT表现特点。方法回顾性分析经病理证实的18例Crohn病的CT征象，大多数病例采用螺旋CT或多层螺旋CT扫描。结果所有病例均有节段性肠壁增厚，CT增强有7例表现为肠壁均匀增厚，缺乏层次，同时肠壁强化不明显；有11例表现为黏膜增厚和分层形成“靶征”和“双环征”，肠壁厚度多在5～10mm；有9例表现为病变段肠管周围纤维脂肪成分增多，蜂窝织炎及肠周或肠系膜血管增多增粗。有5例CT首先考虑为其他疾病，1例考虑为闭攀性肠梗阻，1例首先考虑为肠结核，2例回盲部病变怀疑为癌，1例肠穿孔形成脓肿仅诊为化脓性感染。结论cT不但能准确显示Crohn病肠壁、肠系膜及周围结构的异常，增强CT还能区分活动性与非活动性病变，有助于临床采取合理而积极的治疗方案。     

三康胶囊对高原移居者运动后NO乳酸及血氨的影响

目的探讨三康胶囊对高原人体运动后一氧化氮(NO)及其合酶(NOS)、乳酸(BLA)、血氨(Ammo)的影响.方法选择进驻海拔3 700 m高原1年的10名健康青年,口服三康胶囊15 d,在服药前后分别采用功量自行车进行渐增负荷运动,测定其血清 NO、NOS、BLA及Ammo含量.结果服药后较服药前运动后NO水平[(101.02±6.49) Vs (77.10±8.11)]和NOS活性[(71.40±7.23) Vs (56.29±6.28)]均增高, BLA[(7.58±0.79)Vs (6.13±0.74)]和Ammo[(80.11±9.44)Vs (69.38±8.86)]降低,有非常显著性差异(P＜0.01).结论 三康胶囊能增强高原移居者运动后NOS活性,加速乳酸清除,减缓运动疲劳的发生.