高压氧治疗与血脑屏障通透性的实验研究

目的探讨常规治疗压力（0．25MPa）的高压氧增强血脑屏障开放、促进神经保护剂（神经节苷脂，GM-1）进入脑组织的作用。方法30只Wistar雄性大鼠，随机分为对照组、实验-1组、实验-2组、实验-3组、实验-4组；利用HPD 1700流体撞击仪，建立颅脑损伤动物模型，经毛细管电泳仪测定各组脑组织匀浆中GM-1相对浓度。结果各HBO治疗实验组GM-1浓度较无HBO治疗组和对照组有一定程度的提高，但对照组与各实验组、各实验组之间q检验均没有显著差异（P〉0．05）。结论常规治疗压力的高压氧无明显促进BBB通透性作用，但有增加BBB开放的趋势，促进神经保护剂进入脑组织。     

BRL 8242 (2-[2-benzimidazolyl]-amino-2-imidazoline dihydrochloride), a new inhibitor of dopamine-beta-hydroxylase with antihypertensive activity.

BRL 8242 (2-[2-benzimidazolyl]-amino-2-imidazoline dihydrochloride) was found to inhibit dopamine-beta-hydroxylase in vitro and in vivo and to have antihypertensive activity. The effect on dopamine-beta-hydroxylase in vitro was shown by inhibition of the conversion of phenylethylamine to phenylethanolamine, using enzyme extracted from rat adrenals. In vivo, BRL 8242 inhibited 3H-noradrenaline but not 3H-dopamine biosynthesis from 3H-L-dopa in rat brain. Furthermore, the compound lowered endogenous noradrenaline levels in both rat brain and heart whilst increasing the concentration of brain dopamine. In both metacorticoid hypertensive and normotensive rats, BRL 8242 lowered blood pressure. This response was dose related and correlated well with the reduction of endogenous noradrenaline in the tissues examined. It is therefore suggested that the inhibition of dopamine-beta-hydroxylase by BRL 8242 may account for its blood pressure lowering activity.     

Sensitivity of anticancer agents on human gastric cancers transplanted into nude mice

In the chemotherapy for gastric cancer, the most sensitive anticancer agent against individual tumors should be prescribed. The establishment of a sensitivity test using nude mice as anin vivo model is urgently awaited by clinicians and researchers alike. Seventy-three tumors derived from human gastric cancer were transplanted subcutaneously into nude mice and these mice were then treated intraperitoneally with anticancer agents. Mitomycin C (MMC), 5-fluorouracil (5-FU) and cyclophosphamide (CPM) were used. The doses given were 3 mg/kg of MMC, 75 mg/kg of 5-FU and 200 mg/kg of CPM. In 52 of the 73 cancers, chemosensitivity was evaluated by the microscopic changes in the tumors. The rate of positive sensitivity against gastric cancer was 44.2% in MMC, 34.6% in 5-FU and 30.8% in CPM, respectively. The sensitivity of each agent tested by this method indicated a good correlation with the clinical therapeutic effects. Our results suggest the feasibility of evaluation of the sensitivity of various agents from the microscopic changes on tumors transplanted into nude mice.     

非甾体抗生育药物的研究 Ⅱ.对-羟基苯丙烯酸衍生物的合成及其抗生育活性

据报道,对-羟基本丙烯酸(Ⅰ)对小鼠有很好的抗生育作用。鉴于芳基取代的苯乙烯美化合物亦有不同程度的抗生育活性,我们在对-羟基苯丙烯酸的α位,用芳基取代,合成了24个衍生物。初步药理筛选结果表明,化合物Ⅱ_(1,3,7,23)对小鼠有抗早孕作用(P<0.05～0.001),其中以化合物Ⅱ_1为显著(P<0.001)。     

Determination of a Novel Antiarrhythmic Agent ACC-9358 in Human Plasma by High-Performance Liquid Chromatography

A liquid chromatographic method for the determination of ACC-9358, an antiarrhythmic agent, in human plasma is described. ACC-9358 was extracted from plasma into chloroform and back extracted into 0.01 N hydrochloric acid. ACC-9358 in the acidic extract was eluted from a Novapak C18 column using a 87:13:0.1 (by volume) mixture of phosphate buffer (pH 3.0), acetonitrile, and triethylamine as the mobile phase and measured at 280 nm. The average extraction recoveries were 78.4 and 85.4% at the 0.5- and 5-µg/ml level, respectively. Standard curves were linear and reproducible over the concentration range of 0.01–10 µg/ml, with coefficients of determination better than 0.999. Coefficients of variation for both within-day and day-to-day analysis were less than 11%. The assay method is sensitive, reproducible, and suitable for disposition studies of ACC-9358 in humans.     

Bcl-2 prevents hippocampal cell death induced by the neuroleptic drug haloperidol

The proto-oncogene bcl-2 can rescue cells from apoptosis and necrosis and its mechanism of action may involve antioxidant activity. The possible involvement of free radicals in necrotic cell death induced by the neuroleptic drug haloperidol has led us to investigate the potential protective effect of Bcl-2 against haloperidol toxicity. We found that clonal mouse hippocampal cells stably transfected with the antioxidant Bcl-2 are protected against haloperidol toxicity. This data strongly supports the causative involvement of free radicals in haloperidol toxicity.     

PAOA对小鼠E花结形成的影响

本文观察了ＰＡＯＡ（玉竹提取物）腹腔注射，对小鼠Ｅ花结的形成率有明显抑制作用（Ｐ〈０．０１）。说明此药可能是一种新型的免疫抑制剂。     

丙戊酸镁治疗心律失常的疗效与剂量及血药浓度的关系

口服丙戊酸镁治疗各类心律失常33例,显效17例(51.5％),好转10例(30.3％)、总有效率81.8％。疗效分别与剂量及血药浓度呈正比。最适宜血药浓度为100—150μg/ml。起始剂量以每天1.8g为宜,若疗效欠佳可加大至每天2.4g。该药可使缺镁患者恢复镁正常水平。不良反应有恶心、呕吐、嗜睡及双手震颤等。     

脱硫催化剂的酸法制备及性能研究

对用酸法进行催化剂制备，酸法制备的最佳镁铝比，分散介质的优化，引入对脱催化剂的氧化性能和还原性能的影响。以及实验室的还原温度等诸方面进行了研究。