Antitumor activity of five new platinum complexes having a glycolate leaving ligand.

In an attempt to develop a new anticancer platinum complex with greater or equivalent antitumor activity but reduced side effects compared with cisplatin (CDDP), a series of new platinum complexes having a glycolate leaving ligand was synthesized. Among them, five complexes were selected for further development on the basis of adequate water solubility, low nephrotoxicity and high antitumor activity in a murine system. The chemosensitivity of these five complexes was examined in MTT assay against two human pulmonary adenocarcinoma cell lines, PC-9 and PC-14, and two human stomach adenocarcinoma cell lines, MKN-45 and KATO III. Their IC50 and relative antitumor activity (RAA) values were compared with those of CDDP and 254-S, a second-generation platinum complex with a glycolate leaving ligand under phase III clinical trial. The lowest mean IC50 value was observed in CDDP, followed by SKI 2034R and SKI 2033R. In this study, the antitumor activity was evaluated in terms of RAA values and SKI 2034R showed the highest RAA value. The order of RAA values was SKI 2034R > CDDP > SKI 2032R > SKI 2033R > SKI 2030R > SKI 2029R > 254-S. Based on the RAA order, we have recommended SKI 2034R as the most promising candidate for further development of a clinically useful platinum complex.     

子宫颈癌手术前放疗28例临床分析

我院１９８９年至１９９４年共行子宫颈癌广泛切除术和盆腔淋巴结清扫术３９例，其中２８例行术前放射治疗，１９例临床诊断为Ⅱｂ，随着手术技术的提高和术前放射治疗的配合，子宫颈癌的手术适应症的选择，可以扩大至Ⅱｂ，不增加手术的并发症，并具有一定的优点。     

Quantitative structure-activity relationships in MAO-inhibitory 2-phenylcyclopropylamines: Insights into the topography of MAO-A and MAO-B

Ten (E)-and (Z)-isomers of 2-phenylcyclopropylamine (PCA), 1-Me-PCA, 2-Me-PCA, N-Me-PCA, and N, N-diMe-PCA and fifteeno ⁻, m⁻, p⁻ isomers of (E)-PCA with substituents of Me, Cl, F, OMe, OH were synthesized in this laboratory and tested for the inhibition of rat brain mitochondrial MAO-A and MAO-B. The effects of substituents, their positions, and stereochemistry on the inhibition were assessed for the compounds with substituents at cyclopropyl and amino groups and QSAR analyses were performed using the potency data of ring-substituted compounds. The best correlated QSAR equations are as follows: pI₅₀=0.804 Π² Blo−1.069 Blm+0.334 Lp−1.709 HDp+7.897 (r=0.945, s=0.211, F=16.691, p=0.000) for the inhibition of MAO-A; pI₅₀=1.815 π-0.825 Π² R+0.900 Es²+0.869 Es³+0.796 Es⁴−0.992 HDp+0.562 HAo+3.893 (r=0.982, s=0.178, F=23.351, p=0.000) for the inhibition of MAO-B. Based on the potency difference between stereoisomers of cyclopropylamine-modified compounds and on QSAR results, it is proposed that the active sites of MAO-A are composed of one deep hydrophobic cavity near para position, two hydrophobic cavities interacting with Me group, a hydrophobic area accomodating phenyl and cyclopropyl backbone, steric boundaries, a hydrogen-acceptor site near para position, and an amino group binding site and that in addition to the same two hydrophobic cavities, hydrophobic area, steric boundaries, hydrogen-acceptor site, and amino group binding site, another steric boundary near para position and a hydrogen donating site near ortho position constitute active sites of MAO-B.     

股骨颈骨折几种闭合复位方法的评价(译文)

在股骨颈移位骨折的治疗中,试用了7种不同的闭合复位方法。其中Whitman's法在骨折床台上进行,正常肢体外展,患肢由屈曲牵引至完全伸直位后,维持牵引并外展到与对侧肢体相称位,单髋人字石膏外固定(1914年)。 Leadbetter's法也在骨折床台上进行。将患肢髋部屈曲90°,沿大腿轴线行手法牵引。同时股骨干稍内收,患肢缓慢行环形活动至外展、内旋位,患肢向下降至骨折床台面时,行跟掌试验以验证是否完全复位(1933年)。 Bozan's法利用骨折床台使双下肢维持在伸直位,大绷带放置在患肢髂嵴部位,小绷带放置在患肢腹股沟皱襞最高点处实施牵引。然后整个患肢极度内旋,在维持侧方牵引的同时,患肢外展并轻度过牵(1934年)。     

白细胞介素-10诱导的大鼠树突状细胞体外免疫功能的研究

目的　研究白细胞介素 10 (IL 10 )诱导的大鼠未成熟树突状细胞 (imDCs)体外诱导免疫耐受的可行性。方法　在经典诱导方案的基础上 ,应用IL 10 ( 10 μg/L)抑制大鼠骨髓来源DCs的成熟 (IL 10组 ,10例 ) ,并设对照组 (IL 4组 ,10例 )。培养期间观察DCs形态 ,检测DCs表型、摄取抗原能力、体外免疫功能及培养上清细胞因子水平。结果　与IL 4组比较 ,IL 10组DCs细胞表面CD80 、CD86及OX6低度表达 ( 2 5 .3 %、42 .4%、3 2 .3 % ) ,吞噬能力较强 ( 81.9) ,刺激同种异体淋巴细胞增殖能力下降 ,该淋巴细胞具有抗原特异性低反应性 ;培养上清中IL 12水平 ( 4 0 6.5pg/L)及初次MLR培养上清IL 2水平 ( 2 45 .4ng/L)均较低 ,差异有非常显著性 (P <0 .0 1)。 结论　IL 10作用的大鼠imDCs具有诱导免疫耐受的应用价值。     

福州市区蚊虫孳生习性调查分析

目的:探讨福州城区蚊虫孳生习性与分布现状。方法:调查不同环境孳生地种类与分布,捕捞幼虫计数密度（条/勺）,以人工小时诱捕蚊数计算刺叮率（只/h.m）。结果:调查各类水体 33种 16257处,发现阳性水体32种45522处,阳性率27.8％。建筑工地、高层建筑地下层积水池、开放式排水沟和下水道口等环境积水是城区致倦库蚊的主要孳生环境,建筑工地积水池最高幼虫密度1065～2342条/勺,成蚊刺叮率141.5只/h.m,是普通居民区的16.2倍。白纹伊蚊的孳生环境多达28种,主要为建筑工地和高层建筑地下层水泥池、阳台积水和水缸、桶类、轮胎等容器型积水。结论:城市蚊虫孳生环境与50～60年代明显不同,建筑工地、高层建筑地下层、阳台等建筑类积水和花圃蓄水缸成为现代都市蚊虫重要的孳生环境。     

小剂量氯化汞对小鼠脂质过氧化物的影响

本观察小剂量１ｍｇ／ｋｇ）ＨｇＣｌ２对小鼠肝，脑组织中脂质过氧化物（ＬＰＯ）的影响，发现小剂量ＨｇＣｌ２可使肝组织中ＬＰＯ含量明显增高，与对照组比，差异有显性（Ｐ〈０．０２５），而脑组织中ＬＰＯ含量未见明显影响（Ｐ〉０．０５）。     

玻璃体腔内注气治疗黄斑裂孔视网膜脱离

采用玻璃体腔内注气治疗黄斑裂孔视网膜脱离４９例（５３只眼），视风膜复位４２只眼（７９．２％），其中术后视力增进２９只眼（６９％），讨论了注气的适应征和影响视网膜复位的因素。     

Ag—NOR计数在区分良恶性甲状腺病变中的意义

随机选择经长期随访证实的滤泡性甲状腺癌和腺瘤各10例,正常甲状腺组织5例作为对照。按Ploton的染色方法和Crocker推荐的计数方法分别计算三组每例各50个细胞的Ag-NOR嗜银颗粒平均数,再算出三组各自的AgNOR均数,经统计学检验三者有极显著性差异。可望成为甲状腺滤泡性肿瘤良恶鉴别的一项辅助指标。     

Statistical MUNE: A comparison of two methods of setting recording windows in healthy subjects and ALS patients

OBJECTIVE: To address the issue as to how best to perform statistical MUNE, we applied two different approaches and compared results in healthy subjects and ALS patients. METHODS: Twelve normal subjects (women 8, mean age 52years) and 11 ALS patients (women 4, mean age 54years) underwent two consecutive MUNE studies, which differed in terms of setting and modifying the recording window. These are referred to as the 'expansion' and 'narrowing' methods, respectively. Size-weighted average (Av) SMUP and MUNE values were obtained using the two methods, and compared in control and patient groups. RESULTS: Expansion method-derived Av SMUP sizes and MUNE values differed only slightly from those obtained using the narrowing method in healthy subjects, whereas the narrowing method resulted in significantly larger Av SMUP sizes and smaller MUNE values than the expansion method in ALS patients (Wilcoxon signed ranks test, p=0.003). The sizes of tested areas (mean+/-SD) were significantly larger for the narrowing method than the expansion method in both subject groups with much greater difference in ALS patients; 9.6+/-3.1% vs. 7.9+/-1.7% in healthy subjects and 16.1+/-5.1% vs. 11.2+/-3.0% in ALS patients (Student t-test, p<0.01). CONCLUSIONS: The present study shows, unlike that found in normal subjects, that the results of statistical MUNE in ALS patients are heavily dependent on the approach used to set and modify recording windows. SIGNIFICANCE: The expansion method using a 10%-sized window is likely to suffer from systemic errors due to the ceiling effect and the sampling of artifactually small motor units in ALS patients. The authors recommend that the narrowing method be considered as an alternative that avoids these problems.