硬膜外入路切除颅底中线部肿瘤的临床分析

目的探讨扩大额下硬膜外入路显微手术切除颅底中线部肿瘤的适应证和手术技巧.方法回顾总结经扩大额下硬膜外入路显微手术切除颅底中线部肿瘤16例的手术经验.结果肿瘤全切除13例,次全切除3例,术后未发生任何并发症,全部病例切口Ⅰ期愈合.结论扩大额下硬膜外入路,适应于切除前、中、后颅底中线部位硬膜外各类肿瘤,良好的显微技术、完整修复硬脑膜缺损和颅底重建是提高手术疗效的有效措施.     

喹诺酮类抗菌药物的体外抗菌活性测定和分析

测定１９９１年９月至１９９３年９月收集到的８９２株临床分离菌株对诺氟沙星，依诺沙星，氧氟沙星，洛美沙星及环丙沙星的敏感性，将结果进行归纳总结，并用部分菌株作体外抗菌活性测定，结果在８９２株菌中，对５种喹诺酮类药物敏感６７５株，耐药２１７株，耐药率为２４．３％，耐１种药者１６．９％耐２种药者４．７％，耐３种药者２．２％，耐４种药者０．４％，对５种喹诺酮类药物的耐药率分别为：诺氟沙星２９．９％，依诺沙     

Measurement of the bactericidal activity of fluoroquinolones against Streptococcus pneumoniae using the bactericidal index method

Kill curve analysis alone showed trovafloxacin to be more bactericidal than levofloxacin, grepafloxacin and moxifloxacin against four isolates of Streptococcus pneumoniae. However, using the bactericidal index (BI) method, levofloxacin was the most bactericidal fluoroquinolone using serum or lung biopsy concentration levels against the ofloxacin-susceptible strains and trovafloxacin was the most bactericidal against the ofloxacin-intermediate strain. None of the fluoroquinolones was bactericidal against the ofloxacin-resistant strain. With BIs using epithelial lining fluid or alveolar macrophage concentration levels, trovafloxacin or grepafloxacin was most bactericidal, respectively. These data illustrate that simple analysis of traditional kill curves may not be adequate in the evaluation of fluoroquinolone bactericidal activity. The results of this study suggest a need for further investigation to assess the role of tissue concentration and bactericidal activity in antimicrobial efficacy.     

C-3取代喹诺酮衍生物抗肿瘤活性的二维定量构效关系

目的 研究3位取代喹诺酮衍生物抗肿瘤活性的定量构效关系。方法 采用Hansch方法经计算机模拟与统计分析，获得定量构效关系方程。结果 3位取代基的生成热、最大负电荷、特殊极性、logP和零阶价分子连接性指数与活性有良好的线性关系，并提出3位取代基的一些设计原则。结论 获得较好的定量构效关系方程，并发现喹诺酮的抗菌与抗肿瘤作用机制存在差异。     

Synthesis and bactericidal activity of N-allyllactams

Translated from Khimiko-farmatsevticheskii Zhurnal, Vol. 25, No. 8, pp. 35–36, August, 1991.     

N-Chlorotaurine and ammonium chloride: an antiseptic preparation with strong bactericidal activity

The bactericidal activity of the endogenous antiseptic N-chlorotaurine (NCT) is significantly enhanced in the presence of ammonium chloride which induces the formation of monochloramine (NH(2)Cl) whose strong bactericidal activity is well known. In this study the properties of NCT plus ammonium chloride have been investigated. The reaction of active chlorine compounds like chloramine-T (N-chlorotoluene-sulfonamide sodium), chloroisocyanuric acid derivatives, hypochlorites (NaOCl, CaOCl(2)) with ammonium chloride did not stop at the stage of monochloramine, and the pungent smelling by-products di- and trichloramine, NHCl(2) and NCl(3), were also formed. This was not the case with NCT where only monochloramine was generated. The equilibrium constant of the reaction of NCT with ammonium was found to be [Formula: see text] , which allows to estimate the equilibrium concentration of monochloramine in aqueous solutions of NCT and ammonium chloride. At concentrations each ranging between 0.01% and 1.0% it comes to [NH(2)Cl]=3.5-254 ppm. As an unexpected result the monochloramine containing formulation turned out to be most stable in plain water without buffer additives. Quantitative killing assays revealed complete inactivation of 10(6) to 10(7)CFU/mL of seven bacterial strains by 0.1% NCT plus 0.1% ammonium chloride within 5 min, while with plain 0.1% NCT an incubation time of 2-4h was needed to achieve the same effect. The highly significant increase of bactericidal activity (200-300-fold) could be assigned to the presence of monochloramine which could be isolated by vacuum distillation. Aqueous solutions of NCT and ammonium chloride provide a highly effective and well tolerable antiseptic preparation appropriate to a treatment cycle of at least 1 month if stored in the refrigerator.     

Synthesis and bactericidal activity of quaternary ammonium compounds containing an asymmetric nitrogen atom

Translated from Khimiko-farmatsevticheskii Zhurnal, Vol. 24, No. 1, pp. 36–38, January, 1990.     

抗菌药物血清杀菌活性研究的临床意义

血清杀菌活性(SBA)是综合反映抗菌药物的药代动力学与药效学的重要参数,本文综述了SBA的定义、测定方法、临床意义及应用价值.     

Augmentation of serum bactericidal activity by paldimycin

At concentrations below the MIC, paldimycin induced changes in Staphylococcus aureus 502A (UC 9116, ATCC 28417) which increased its sensitivity to serum. The enhanced sensitivity to serum was concentration dependent with the maximal sensitivity found when bacteria were grown in approximately 1/10 MIC of paldimycin. Within an 1-hour incubation, S. aureus 502A typically grew 1.5-2-fold in serum. Following exposure to paldimycin, however, approximately 30-50% of the bacteria were killed in serum. The paldimycin treated bacteria were not more susceptible to phagocytosis and killing by polymorphonuclear leukocytes. At the concentrations utilized, the Staphylococci were enlarged and had thickened cell walls. The organisms were still viable and replicating, but irregularities in cell division were observed in transmission electron micrographs.     

Comparison of inhibitory effects of new quinolones on drug metabolizing activity in the liver

The effects of three new quinolones (enoxacin (ENX), norfloxacin (NFLX) and ofloxacin (OFLX] on acetaminophen-induced liver injury in rats were examined and compared with their effects on the elimination half-life (T1/2) of theophylline (in vivo) and on the 7-ethoxycoumarin (7-EC) O-deethylase activity in liver microsomes (in vitro). ENX, NFLX and OFLX (75 or 300 mg/kg) were administered orally to rats 1 hr before, simultaneously with, and 1 hr after the acetaminophen injection (800 mg/kg). Biochemical liver function tests, drug metabolizing activity in liver microsomes, the total glutathione content of the liver and histological changes were examined 5 hr after the acetaminophen injection. ENX markedly reduced acetaminophen-induced liver injury and NFLX slightly but significantly did so, but no protective effect was observed with OFLX treatment. ENX markedly and NFLX slightly prolonged the T1/2 of theophylline, but OFLX did not affect it. In addition, ENX markedly and NFLX slightly inhibited the 7-EC O-deethylase activity in liver microsomes, but OFLX again had no effect. These findings indicated that ENX markedly inhibited the activity of cytochrome P-450 in liver microsomes and NFLX did so slightly, while OFLX had no such effect. Slight variations in the structures of these quinolones might explain the differences in their effects on cytochrome P-450 activity.