Synthesis of metabolites and enantiomers of prolintane]

The synthesis of 15 possible metabolites of prolintane (1) (Katovit) which is used in the treatment of blood pressure disregulations is described. Furthermore, the preparation of the enantiomers of 1 is reported, starting with R-(+)- and S-(-)-phenylalaninol respectively.     

pH指示剂吸收度比值法测定盐酸乙胺丁醇的含量

本文报道pH指示剂吸收度比值法测定盐酸乙胺丁醇的含量。该法采用指示剂为0.05%茜素黄R,测定波长374nm和500nm;标准液为0.1mol/L NaOH;仪器为WFZ-800D_2型分光光度计。测得三批盐酸乙胺丁醇的含量分别为99.5±0.04%,99.4±0.05%和99.6±0.03%.同时与药典法比较,结果一致。     

益气平喘丸的药理研究

本实验结果表明,益气平喘丸具有明显的平喘止咳祛痰作用,并能显著增加免疫低下小鼠的免疫器官重量及碳粒廓清速率,使正常大鼠血清皮质醇浓度显著升高及肾上腺内维C 含量明显降低。     

New posture equilibrometer for the diagnosis of vestibular disease

Summary The vestibulospinal level of vestibular function is commonly neglected in the evaluation of vertiginous patients. We have now developed a new posture equilibrometer. A transducer is placed on the head of the subject being tested. With this meter we can record body swaying, X (left-right) and Y (fore-aft) components of angular displacement, angular velocity, and angular acceleration. A detailed analysis of the data can be made by having patients keep their eyes either open or closed during the Romberg test. The head is turned left or right in this test, while the eyes are opened and closed in the Mann test. The posture equilibrometer has enabled us to evaluate more precisely vestibulospinal function and sensory interactions. Offprint request to: N. C. Zhong     

Establishment of a prostatic hyperplasia model with beagle dogs

Objective: To establish a prostatic hyperplasia model with beagle dogs. Methods: Twenty-four male beagle dogs, 2 years of age, were divided into the treatment and control groups at random and were administrated testosterone propionate (TP) i.m. two months after castration. Three treatment groups were set with the doses of TP at 0.8 mg/kg, 2.5 mg/kg and 7.5 mg/kg, respectively, and the control was given the same volume of vehicle. Two months later, half of the animals were killed and sera samples were obtained. The wet weight and volume of prostate were measured. The dihydro testosterone (DHT) level of the serum and prostate were determined with the commercial radioimmunoassay (RIA) kit. The prostate was sectioned, fixed and stained with hematoxylin and eosin. Pictures were taken with a digital camera under the microscope and were analyzed with a computer for the epithelial cell height and the acinar luminal area with micro image analysis software. The prostate volume was measured with ultrasonic diagnost     

肝硬化病人施行胆道手术35例分析

本文对我院近10年来收治的肝硬化病人施行胆道手术35例进行分析，术前漏诊肝硬化12例，占3O％以上，死亡5例，有3例死于胆囊床大出血与术前漏诊有关。作者就术前漏诊原因、术前准备和手术处理体会进行讨论。     

Anti-leukemia effect of perillyl alcohol in Bcr/Abl-transformed cells indirectly inhibits signaling through Mek in a Ras- and Raf-independent fashion.

PURPOSE: Perillyl alcohol (POH) displays preventive and therapeutic activity against a wide variety of tumor models, and it has been suggested that this might be associated with the ability of POH to interfere with Ras prenylation. POH also selectively induces G(1) arrest and apoptosis in Bcr/Abl-transformed hematopoietic cells. Because signaling through Ras is necessary for Bcr/Abl transformation, we examined whether POH induces its anti-leukemia effect by inhibiting Ras signaling. EXPERIMENTAL DESIGN: The ability of POH to inhibit posttranslational farnesylation and signaling from Ras as well as signaling through the Raf-Mek-Erk cascade was examined in Bcr/Abl-transformed and mock-transformed cells and related to the anti-leukemia effect of POH. RESULTS: POH does not affect Ras prenylation or Ras activity, but it blocks signaling downstream of Ras by reversing the state of activation of the Erk kinase, Mek. POH affects Mek activity only when it is added to intact cells. Treatment of either cell lysates or of purified Mek with POH has no effect on Mek activity. Inhibition of the Mek-Erk pathway seems to be related to the POH anti-leukemia effect for the following reasons: (a) the concentration of POH needed to block the Erk pathway, as well the kinetics with which POH inhibits this signaling cascade, both correlate with the anti-leukemia effect of POH; (b) both U0126 (a specific Mek inhibitor) and POH induce similar anti-leukemia effects; and (c) mock-transformed hematopoietic cells are simultaneously resistant to POH anti-leukemia effects and inhibition of the Mek-Erk pathway. CONCLUSION: Blocking Mek is sufficient to induce growth arrest and apoptosis in Bcr/Abl-transformed cells; therefore, POH represents a novel small molecule inhibitor of Mek that might be effective for treating Bcr/Abl leukemias.     

大鼠延髓腹外侧区在可乐定心血管效应中的作用

目的：探讨大鼠延髓腹外侧区（VLM）在介导可乐定心血管效应中的作用。方法：氨基甲酸乙酯麻醉SD大鼠，应用微量注射和细胞外记录等方法观察尾端延髓腹外侧区（CVLM）和头端延髓腹外侧区（RVLM）内局部给予可乐定导致的心血管活动变化。结果：单侧CVLM微量注射可乐定（5nmol/100nl,n=10)不仅能明显升主动脉血压（AP）和增加心率（HR）（P＜0．01），而且能增加同侧RVLM压力敏感性神经元（n=80)的放电频率（P＜0．01），而单侧RVLM微量注射可乐定（5nmol/100nl,n=9)，明显降低AP和HR（P＜0．01）。结论：RVLM和CVLM在介导可乐定的心血管效应中具有不同的作用。     

大剂量甲基强的松龙冲击治疗急性脊髓损伤疗效分析

目的研究大剂量甲基强的松龙(MP)治疗急性脊髓损伤的临床效果.方法对87例急性脊髓损伤患者进行回顾性研究,根据伤后时间并按自愿选择用药原则分为应用MP治疗组(MP组,45例)和未应用MP治疗组(对照组,42例),以ASIA分级标准进行分级,并比较疗效和并发症.结果两组患者在治疗前后感觉及运动功能均有明显改善(P＜0.05).但MP组的感觉及运动功能恢复均优于对照组(P＜0.05).MP治疗组中24h治疗组(A组)与48h治疗组(B组)并发症发生率比较无显著性差异(P＞0.05),而MP组与对照组比较并发症的发生率明显增加,有显著性差异(P＜0.05).结论早期应用MP大剂量冲击治疗急性脊髓损伤是一项有效措施,但会显著增加患者治疗中并发症的发生率.     

糖尿病雄性大鼠性腺5α-还原酶Ⅱ型活性变化

目的 :探讨大鼠青春期和成年期糖尿病时性腺 5α 还原酶Ⅱ型的活性变化。　方法 :取 4 0d和 90d龄雄性Wistar大鼠各 30只 ,分别分为对照组 (C)、糖尿病组 (D)和胰岛素治疗糖尿病组 (ID)。采用薄层层析法测定各组附睾头、附睾尾、前列腺和睾丸组织内 5α 还原酶 Ⅱ型的活性。　结果 :①青春期大鼠性腺的各部位内 ,5α 还原酶 Ⅱ 型的活性D组均明显低于C组 (P <0 .0 1) ,而ID组明显高于D组 (P <0 .0 1) ;②成年期大鼠性腺的各部位内 ,5α 还原酶 Ⅱ型的活性在C、D和ID组各组间差异无显著性 (P均 >0 .0 5 )。　结论 :青春期大鼠性腺内 5α 还原酶 Ⅱ型的活性更易受代谢环境、激素水平及局部特异性因素的影响 ,而成年期大鼠性腺内 5α 还原酶Ⅱ 型的活性相对稳定