Phase II study of 10-ethyl-10-deaza-aminopterin (10-EdAM; CGP 30 694) for stage IIIB or IV non-small cell lung cancer

Summary Thirty-one patients with stage IIIB or IV non-small cell lung cancer (NSCLC) were treated with intravenous 10-EdAM on a weekly basis. The starting dose was 80 mg/m², with subsequent doses adjusted depending on evidence of toxicity. There were 20 men and 11 women with a median age of 58 years (range, 33–75). Response was evaluated in 30 patients, 5 with evaluable but not measurable tumors and 25 with measurable indicator lesions. There were no complete remissions; 3 patients achieved partial remission. Nine patients had a minor response, 6 showed no change, and 12 had progressive disease. Median survival for all 31 patients was 43 weeks (range, 12–65+). During the first 3-week period, the 10-EdAM dose was reduced or withheld in 19 patients (because of stomatitis in 12, SGPT elevation in 3, skin rash in 2, and granulocytopenia in 2), escalated in 11 patients, and unchanged in 1 patient. A mean of 34–88 mg/m²of 10-EdAM (median, 50) was given per week during the first 5-week period. Myelotoxicity was infrequent and there was no significant nephrotoxicity. Considering the modest side effects of this treatment and the conservative dose-modification schedule which mandated substantial dose reductions, we conclude that 10-EdAM is a promising antitumor agent for NSCLC.     

用化学发光自显影技术快速检测鸭沙门氏菌

应用我室建立的化学发光自显影技术检测鸭沙门氏菌。用酶标抗体与硝酸纤维素膜上固定的细菌结合,再同发光底物溶液作用,使X线胶片感光,根据胶片上的黑斑进行半定量,可检出100个菌。其检测特异性好,约2小时即可出报告。     

Juvenile Xanthogranuloma on the Palm

Abstract: Juvenile xanthogranuloma is a xanthomatous and granulomatous condition that frequently arises before 1 year of age and mainly occurs on the head and trunk. We report a rare solitary juvenile xanthogranuloma on the right palm of a 10-year-old girl, present for one year. This solitary involvement of the palm has been reported only twice before.     

消化道肿瘤血浆胃动素测定及其意义

作者报告经病理诊断消化道恶性肿瘤患者30例及手术切除肿瘤患者15例的血浆胃动素水平,并以健康成人31例作为对照。消化道恶性肿瘤的胃动素水平373.4±123.7ng/L,显著高于正常对照组(162.3±52.3ng/L,P<0.001),而消化道恶性肿瘤患者术前及术后胃动素水平无显著差异。消化道恶性肿瘤患者胃动素水平增高的原因可能是肿瘤刺激神经所致。胃癌和结肠癌细胞可产生胃泌素样物质,它可刺激胃动素的释放。     

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)。     

对居民使用液化气健康效应的初步探讨

对液化气燃烧后室内空气污染进行了流行病学调查，结果显示，液化气燃烧可造成ＳＯ＿２、ＮＯ＿２、空气总悬浮颗粒物和总烃类的室内空气污染。小鼠接触三个月出现Ｔ淋巴细胞计数降低、睡眠时间延长、骨髓嗜多染红细胞微核率增加、肺组织匀浆Ａｍｅｓ试验阳性率增高、雄性小鼠精子畸形率增加，并有明显的剂量－反应关系。对接触５年以上的人群调查发现，呼吸道、鼻和眼的自觉症状明显增加，咽炎、鼻炎、结膜炎患病率增高。人群尿液浓缩物Ａｍｅｓ试验和外周血红细胞微核率检出阳性结果，可能与液化气燃烧废气中含有致突变污染物有关。     

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。