丹参对持续癫痫幼鼠脑损伤保护作用的实验研究

目的 探讨丹参对持续癫痫发作诱发幼鼠脑神经元损伤是否具有保护作用。方法 皮下及腹腔注射贝美格针诱发健康幼龄鼠癫痫持续状态发作。光镜下观察神经元病变情况；电镜观察海马神经元超微结构的改变。结果 持续癫痴组幼鼠脑组织光镜下可见明显的神经元病变。电镜下可见海马区神经元的超微结构病变。丹参治疗组神经元病变均轻于持续癫痴组；而正常对照组未见类似病变。结论 丹参在组织、细胞和亚细胞水平对持续癫病幼鼠脑神经元损伤具有一定的保护作用，为临床有效防治小儿惊厥性脑损伤提供了可靠的实验依据。     

腰椎管狭窄症术后下肢残留麻木的发生率及影响因素

[目的]探讨腰椎管狭窄症术后下肢残留麻木的发生率和影响因素。[方法]2001年1月～2003年2月手术治疗56例腰椎管狭窄症患者，术后随访10d，1、3个月、1年和2年，记录患者神经功能和残留症状。[结果]术前82．1％的患者有下肢麻木，术后10d，1、3个月、1年和2年分别有43．6％、39．I％、36．6％、35．3％和35．7％的患者下肢残留麻木，与病程、术前JOA评分和椎管狭窄类型有关，与年龄和神经根直径无关。[结论]腰椎管狭窄症患者术后1个月内下肢麻木恢复最快，术后1年和2年下肢麻木发生率为35．3％和35．7％，推测神经组织的潜在恢复能力影响下肢麻木的发生率。     

醋酸精氨酸对创烧伤患者预后的影响及安全性分析——86例多中心、随机、双盲、安慰剂对照试验

目的观察服用醋酸精氨酸对创烧伤患者预后的影响及可能出现的不良反应。方法采用多中心、随机、双盲、安慰剂平行对照的研究方法,将96例创烧伤患者(实际完成86例)随机分为治疗组和对照组,治疗组41例,服用醋酸精氨酸0．4 g·kg-1·d-1;对照组45例,服用安慰剂酪氨酸,剂量同前,均连用7 d。两组患者采用等氮、等热量的营养支持疗法。比较患者创面(切口)愈合时间、住院时间及不良反应发生情况。结果创伤患者治疗组(29例)创面(切口)愈合时间和住院时间分别为(11．1±2．8)、(19±6)d,明显短于对照组(13．2±5．5)、(22±6)d(33例,P< 0．05);烧伤患者治疗组(12例)创面愈合时间和住院时间各为(20±5)、(28±6)d,与对照组(22±8)、(29±8)d(12例)比较,差异无统计学意义(P>0．05)。在整个试验过程中,患者出现的不良反应为恶心、腹泻,其中治疗组1例占2．44％,对照组1例占2．22％,两组比较差异无统计学意义(P= 1．000)。以上不良反应停药后消失。结论服用醋酸精氨酸能显著促进创伤患者创面(切口)愈合,缩短住院时间,且无明显不良反应,但对烧伤患者的预后无明显改善,这可能与病例数较少有关,其确切疗效有待于通过大样本的临床试验予以确定。     

Therapeutic effect of antimicrobial drugs against experimental infections due toYersinia pestis in mice

Although there are effective antibacterial agents against plague, newer antibacterial agents have been developed which show more potent activity against other bacterial organisms, but have not been tested againstYersinia pestis. A strain ofYersinia pestis was selected (no. 22; National Institute of Infectious Diseases, Tokyo, Japan) that caused a systemic infection in mice.Y. pestis no. 22 was intraperitoneally inoculated into DDY-strain mice, and 13 oral or 6 injectable antibacterial drugs given to the infected mice at varying doses 1 and 24 hours after infection. Levofloxacin, sparfloxacin and ofloxacin were the most effective oral agents against the infection, and prulifloxacin and pazufloxacin were also effective but to a lesser extent. Also, gentamicin and arbekacin were the most potent injectable antibacterial agents againstY. pestis. These results suggest that there are several new drugs, both oral and injectable, which exert excellent in vivo antibacterial activity against a mouse infection model and may be useful for the clinical treatment of plague.     

Stereoselectivity of actions of the calcium sensitizer [+]-EMD 60263 and its enantiomer [-]-EMD 60264

The thiadiazinone derivative [+]-EMD 60263 ((+)-5-(1-(α-ethylimino-3,4-dimethoxybenzyl)-1,2,3,4- tetrahydroquinoline-6-yl)-6-methyl-3,6-dihydro-2H-1,3,4 -thiadiazine-2-on) is a Ca²⁺-sensitizing agent with only minor phosphodiesterase inhibitory activity. Our aim was to characterize the inotropic and electrophysiological effects of [+]-EMD 60263 and its enantiomer [-]-EMD 60264 in several cardiac muscle preparations. The Ca²⁺-sensitizing activity resided in the [+]-enantiomer only. [+]-EMD 60263 (3 μM) shifted the EC₅₀ of Ca²⁺ for contractile activation of skinned fibers of pig heart from 2.41 μM to 0.73 μM, whereas [-]-EMD 60264 (30 μM) was ineffective. In Langendorff-perfused guinea pig hearts, [+]-EMD 60263 and [-]-EMD 60264 induced concentration-dependent positive and negative inotropic effects, respectively; both enantiomers reduced spontaneous heart rate but did not influence perfusion pressure. The maximum increase in force of human atrial trabeculae was 35 % of pre-drug control with [+]-EMD 60263 in comparison to 113 % with forskolin. In guinea-pig papillary muscles, [+]-EMD 60263 and [-]-EMD 60264 had opposite inotropic responses, however, both agents similarly prolonged action potential duration. Both enantiomers concentration-dependently blocked the rapidly activating component I_Kr of the delayed rectifier in guinea-pig myocytes. The block saturated at potentials positive to +30 mV, closely resembling the effects of the antiarrhythmic agent E-4031 which had been originally used to define I_Kr. It is concluded, that the positive inotropic action of [+]-EMD 60263 can be explained by prevalence of the Ca²⁺-sensitizing effect. The accompanying prolongation in action potential duration is caused by block of the I_Kr component of the delayed rectifier. While the inotropic effects are stereoselective, most of the electrophysiological actions are clearly independent of sterical configuration. The combination of Ca²⁺-sensitizing with class-III antiarrhythmic action may provide an interesting pharmacological profile of potential therapeutic use. Received: 7 January 1997 / Accepted: 25 February 1997     

Dorsal and ventral dopaminergic innervation of the spinal cord: Functional implications

Several studies have demonstrated that a descending dopaminergic pathway innervates the dorsal and the intermediate gray matter of the spinal cord and have suggested that this pathway is involved in pain modulation and in the control of autonomie functions. Other studies have also demonstrated the presence of dopamine (DA) and DA metabolites as well as of DA receptors in the ventral cord. There is also evidence for the implication of DA in the control of motor functions at the spinal level. The occurrence of a dopaminergic innervation in the ventral horn has been, however, disputed until recently. But recent work has demonstrated that the motoneural cell groups in the ventral horn (lamina IX) are a target for descending dopaminergic fibers. In addition, the possibility that DA is a mediator of primary afferent fibers has also been postulated. Finally, the occurrence of dopaminergic cell bodies has been suggested in the spinal cord. This indicates that DA is probably implicated in a complex manner in spinal functions. In the present paper the possible involvement of DA in sensory and in motor functions at spinal level will be discussed in view of neurochemical observations made in polyarthritic rats, in which pain-related behavior and reduction of locomotor activity associated with a marked decrease in mobility, are observed.     

大鼠不同脑区微量注射蝇蕈醇与氯苯氨丁酸镇痛作用比较

目的观察并比较GABAa受体激动剂蝇蕈醇及GABAb受体激动剂氯苯氨丁酸在大鼠不同脑区的镇痛作用。方法实验分侧脑室、室旁核和海马三组 ,每组又分成生理盐水对照组、蝇蕈醇组及氯苯氨丁酸组 ,分别经侧脑室、海马和室旁核”微量注射生理盐水或药物 ( 1× 1 0 - 3 mol·L- 1,1 μl) ,在大鼠甩尾测痛模型上”测定大鼠的痛阈。结果微量注射蝇蕈醇和氯苯氨丁酸在不同脑区均可不同程度地提高大鼠的痛阈 (与生理盐水对照组相比 ,P <0 .0 5或P <0 .0 1或P <0 .0 0 1 ) ,虽然蝇蕈醇与氯苯氨丁酸在侧脑室和室旁核的镇痛作用无显著性差异 (P >0 .0 5 ) ,但氯苯氨丁酸在海马的镇痛作用明显强于蝇蕈醇(P <0 .0 0 1 )。比较药物在不同脑区的镇痛作用发现 ,氯苯氨丁酸在海马和室旁核的镇痛作用无明显区别 ,但均强于侧脑室 ;而蝇蕈醇在室旁核最强 ,其次为海马、侧脑室。结论经侧脑室、海马或室旁核微量注射蝇蕈醇或氯苯氨丁酸均能降低大鼠对痛的感受性。氯苯氨丁酸在海马和室旁核可产生较强的镇痛作用 ,而蝇蕈醇在室旁核镇痛作用较明显 ,其次为海马     

复方华蟾胶囊抗小鼠肿中瘤作用的实验研究

目的了解复方华蟾胶囊抗小鼠移植性肿瘤的作用.方法以小鼠肝癌22(H22)、小鼠肉瘤180(S180)为瘤株,应用动物移植性肿瘤的体内试验法对药物进行抗癌药效学试验.结果复方华蟾胶囊灌胃4,2 g/kg@d,连续14 d,对小鼠移植性肝癌实体型生长有明显的抑制作用,抑瘤率分别为38.09%,30.95%.对小鼠移植性S180实体型生长有明显的抑制作用,抑瘤率分别为34.7%,30.08%.复方华蟾胶囊对荷瘤小鼠的胸腺和脾脏重量无影响.结论复方华蟾胶囊在试验条件下有一定抗肿瘤作用.     

苦碟子抗肿瘤作用的实验性研究

目的 研究苦碟子对动物移植性肿瘤的作用。方法 以小鼠移植性肉瘤180（S180)和艾氏腹水瘤（EAC）为模型，观察苦碟子的抗肿瘤作用，并分别计算出抑瘤率和生命延长率。结果 不同剂量的苦碟子对小鼠肉瘤S180的抑制率分别为39．86％，38．14％和35．73％（与对照组相比差异有显著性，P＜0．01），苦碟子也能延长荷艾氏腹水瘤（EAC）小鼠的存活期，生命的延长率分别为41．27％、29．79％和17．88％（高剂量组和中等剂量组与对照组相比差异有显著性，P＜0．01）。结论 苦碟子在动物体内可能具有抗肿瘤作用，可作为一种有前途的抗肿瘤药物进行研究。     

调整给药时间减轻顺铂肾毒性的研究

目的　观察不同给药时间对顺铂肾毒性的影响。　方法　 1 6例癌症患者分为两组各 8例 ,分别在上午 1 0时或下午 8时静滴 6 0mg m2 顺铂 ,3～ 4周后作第 2周期化疗时交换给药时间 ,以尿 β2 微球蛋白浓度作为肾小管功能改变的指标。　结果　治疗前两组的尿 β2 微球蛋白浓度均在 2 0 0 μg L以下。治疗后 ,上午 1 0时给药组的尿β2 微球蛋白浓度在第 1周期为 4 96± 6 6 μg L ,第 2周期为 5 0 4± 74 μg L ,下午 8时给药组分别为 2 77± 4 3μg L(t=3.6 6 ,P <0 .0 1 )和 2 83± 39μg L(t=3.6 3,P <0 .0 1 )。 　结论　不同时间给药对顺铂的肾毒性有显著影响 ,下午 8时给药可明显减轻顺铂的肾毒性。