Novel azapeptide inhibitors of cathepsins B and K. Structural background to increased specificity for cathepsin B

Abstract: We have designed and synthesized a new series of azapeptides which act as potential inhibitors of cathepsin B and/or cathepsin K. Their structures are based upon the inhibitory sites of natural cysteine protease inhibitors, cystatins. For the synthesized azapeptides, the equilibrium constants for dissociation of inhibitor–enzyme complex, K_i, were determined. Comparison of these values indicated that all of the azainhibitors act much stronger toward cathepsin B. Z‐Arg‐Leu‐His‐Agly‐Ile‐Val‐OMe ( 7 ) proved to be approximately 500 times more potent for cathepsin B than for cathepsin K. To be able to explain the obtained experimental values we used the molecular dynamics procedures to analyze the interactions between cathepsin B and compound 7 . We also determined the structure of the most potent and selective cathepsin B azainhibitor by means of NMR studies and theoretical calculations. In this report, we describe SAR studies of azapeptide inhibitors indicating the influence of the conformational flexibility of the examined compounds on inhibition of cathepsins B and K.     

Treatment of horizontal root‐fractured maxillary incisors – a case report

Abstract – Traumatic dental injuries often occur to the teeth and their supporting tissues and they are the main reasons for emergency visit to a dental clinic. Management of a fracture depends on its position and the extent of root involvement. Horizontal root fractures are not seen frequently and the treatment consists of reduction and long‐term rigid fixation of the coronal segment. The present case demonstrates the successful management of two horizontally fractured maxillary central incisors with a follow‐up period of 9 months.     

上胸椎骨折手术治疗方法的探讨

目的 探讨上胸椎骨折的特点及治疗。方法 15例病人按AO分型，A型2例、B型10例、C型3例。均经后路切开复位、脊髓减压、长节段内固定、取髂骨植骨融合术治疗。结果 随访18-24个月，后路长节段固定随访时无一例失败，完全瘫的患者9例中有1例神经功能改善I级．不完全瘫的5例均有Ⅲ级改善，1例无神经损伤。结论 上胸椎骨折损伤严重，后路长节段固定技术是一种合理的有效治疗方法。     

雌激素及其受体与胆囊癌关系的研究现状及进展

目的:探讨并讨论雌激素及其抗体与胆囊癌的关系.方法:阅读关于雌激素和胆囊癌方面的文献并进行总结.结果:雌激素在胆囊癌转变过程中起极为重要的作用.结论:研究胆囊癌患者血清中的雌激素水平对胆囊癌的发生、发展、预后及指导相应临床内分泌治疗具有重要的理论意义.     

精神病人与正常人戒烟前后焦虑抑郁症状的对照研究

目的　了解精神病人和正常人戒烟前后精神状况的变化及差异性 ,探讨戒烟措施。方法　对 71例精神病人和 5 0例正常人戒烟前及戒烟后 1周分别应用汉密顿焦虑量表 (HAMA)、汉密顿抑郁量表 (HAMD)、焦虑自评量表 (SAS)、抑郁自评量表 (SDS)、简明精神病量表 (BPRS )进行测评。结果　精神病人强制性戒烟前HAMA、HAMD、SAS、SDS、BPRS分值分别为 (8.2 1± 6 .4 1)、(7.6 4± 5 .71)、(36 .81± 7.14 )、(33.71± 7.1)、(2 9.4 5± 8.4 7) ;戒烟后HAMA、HAMD、SAS、SDS、BPRS分值分别为 (16 .4 5± 6 .34)、(19.73± 8.71)、(5 8.1± 12 .12 )、(5 6 .31± 11.4 )、(37.32± 7.95 ) ;戒烟前后 5种量表分值变化与正常人戒烟前后分值变化比较有极显著性差异(P <0 .0 1)。结论　对精神病人强制性戒烟可引起明显的情绪反应 ,应适宜控制病人吸烟 ,建立一个合理的管理制度     

输尿管上段结石的微创手术治疗

目的：探讨输尿管上段结石的治疗方法。方法：回顾性分析输尿管镜下气压弹道碎石(URSL），后腹腔镜输尿管切开取石(RLU)、经皮肾穿刺取石(PCNL)治疗输尿管上段结石患者的临床资料。其中URSL组25例，RLU组20例。PCNL组9例。结果：URSL组碎石成功18例；7例不成功，其中3例改为开放手术，1例改为后腹腔镜取石。2例行ESWL术，1例仅留置双J管。术后1个月拔管后自行排出。2例并发输尿管穿孔。RLU组取石成功18例，2例滑入肾内，经配合输尿管镜和腹腔镜直视下经皮肾穿刺取石成功，术后15例有伤口漏尿。PCNL组成功9例，无并发症。结论：USRL创伤小。术后恢复快。是治疗输尿管上段结石的较为满意的治疗方法。PCNL创伤小，取石成功率高，在结石靠近肾盂、儿童输尿管上段结石并同侧肾结石和结石以下输尿管狭窄时应优先考虑。但技术难度较大。RLU可作为URSL不成功后的辅助治疗方法。     

ISOLATION OF VIRULENT TREPONEMA PALLIDUM FRQM HUMAN AORTA THIRTY-TWO HOURS AFTER DEATH FROM CARDIOVASCULAR SYPHILIS

After a comprehensive rernew of the literature on syphilitic aortitis, Longcope, (1) stated in 1913; ": . . . the presence of spiro: chetes in these lesions, as might be expected, cannot by any means be constantly demonstrated with Levaaiti stain. . . . . . . That these organisms are ''Treponema pallidum seems almost certain thouS:h actual proof of such by culture from the arterial lesions, a most difficult task, or direct inoculation into animals, has not as yet been accomplished."