Evaluation ofin vitro drug screening leads using experimental models of human ovarian cancer

Summary Five compounds which were identified as potential new anticancer drugs inin vitro screening with the human tumor colony forming assay were selected for further evaluation usingin vitro andin vivo models of human ovarian cancer. Three of five compounds were found to inhibitin vitro colony formation of ovarian cancer cell lines derived from both untreated and combination chemotherapy refractory patients. One compound was also found to prolong survival in a human ovarian carcinoma xenograft model system. This compound, chloroquinoxaline sulfonamide, was selected for development and has shown preliminary indication of activity in phase I clinical testing.     

乳癌根治术后并发臂丛神经损伤

乳癌根治术是治疗乳腺癌的主要手段,但并发臂丛神经损伤的报道却很少,总结从1989年10月～1991年2月华山医院诊治的9例,3例门诊治疗,6例住院治疗。其中5例行神经松解后,皮瓣或肌皮瓣转移覆盖神经瘢痕区。随访到8例,疼痛改善3例,感觉和运动改善2例,疗效不理想,认为寻找预防措施是减少乳癌根治术后臂丛损伤的根本办法。     

胃癌腹腔脱落细胞检查及临床意义

腹膜转移是胃癌常见的转移形式。为在肉眼可见转移前发现亚临床的转移现象,自1981年3月至1982年4月,我们共对胃癌病人142例进行了腹腔脱落细胞检查及临床随诊,发现有腹腔脱落细胞阳性者76例(53.5％)。5年随诊结果发现,腹腔脱落细胞阳性者无一例生存>3年;而腹腔脱落细胞阴性的66例中生存5年者有11例。可见,腹腔脱落细胞检查,对胃癌的诊断,治疗和预后判断有一定价值。     

Presence of antibodies reacting specifically with structural proteins of mouse mammary tumor virus (MMTV) among antibodies composing circulating immune complexes in breast cancer patients

All-Union Oncologic Scientific Center, Academy of Medical Sciences of the USSR, Moscow. (Presented by Academician of the Academy of Medical Sciences of the USSR N. N. Trapeznikov.) Translated from Byulleten' Éksperimental'noi Biologii i Meditsiny, Vol. 105, No. 4, pp. 475–477, April, 1988.     

Epirubicin as a single agent therapy for the treatment of breast cancer — A pharmacokinetic and clinical study

Sixty women with breast cancer (mean age: 61 years; range 36-78 years) were treated with Epirubicin (4’epi-Dox-orubicin), 60 mg m^-2 , as single drug therapy. The drug was administered as 2 hours’ constant rate infusions. The pharmacokinetics of the drug during the first course of treatment was evaluated by measurements of the plasma concentration of Epirubicin at the end of the infusion period. There was a five-fold inter-individual variation of the dose-normalized maximum plasma concentration, which increased with increasing age of the patients. There was no correlation between this pharmacokinetic parameter and degree of obesity.     

UROLOGICAL TUMOURS: RECENT CHANGES

The principles of urology and all surgical disciplines were, not too long ago, considered to be rigidly and permanently established. In this exciting era of change, the foundations of urology are now set on shifting sands rather than the bedrock of the past. The pertinent issue clinically is making discriminating evaluations of new developments so that, where appropriate. they are able to be incorporated into treatment practices to improve patient care. In this overview, a personal appreciation of the more important practical and conceptual changes relating to prostatic. urothelial and renal carcinoma during the past 5 to 10 years is presented.     

支气管动脉灌注化疗联合直线加速器放射治疗Ⅲa期非小细胞肺癌

目的　研究支气管动脉灌注化疗联合直线加速器放射治疗Ⅲa期非小细胞肺癌 (NSCLC)的可行性及临床价值。方法　 76例NSCLC患者随机分成A、B 2组 ,A组先行 2次支气管动脉灌注化疗 (BAI) ,第 2次BAI 1～ 2周后再行直线加速器放射治疗 (RT) ;B组单纯行 2次BAI (对照组 )。结果　临床疗效 ,A组 (BAI RT)和B组 (BAI)分别为 89.47%和 60 .5 3% (Ρ <0 .0 1) ;1、3年生存率 ,A、B组分别为 81.5 8%、5 0 .0 0 %和 60 .5 3%、2 1.0 5 % ( 0 .0 1<Ρ <0 .0 5 )。结论　支气管动脉灌注化疗联合直线加速器放射治疗Ⅲa期非小细胞肺癌的临床疗效和患者 1、3年生存率均显著提高     

Characterization of high-affinity receptors for bombesin/gastrin releasing peptide on the human prostate cancer cell lines PC-3 and DU-145: Internalization of receptor bound 125I-(Tyr4) bombesin by tumor cells

Specific receptors for bombesin/gastrin releasing peptide (GRP) on the androgen-independent human prostate cancer cell lines PC-3 and DU-145 were characterized. No specific binding of ¹²⁵I-[Tyr⁴]-bombesin to the androgen-dependent human prostate cancer cell line LNCaP was detectable. The binding of ¹²⁵I-[Tyr⁴]-bombesin to PC-3 and DU-145 cells was found to be time- and temperature-dependent, saturable, and reversible. Scatchard analysis revealed a single class of binding sites with high affinity (K_d 9.8 × 10^?11 M for PC-3, and 9.1 × 10-¹¹ M for DU-145 cells at 25°C) and with a binding capacity of 44,000 binding sites/cell and 19,000 binding sites/cell, respectively. Bound ¹²⁵I-[Tyr⁴]-bombesin was rapidly internalized by PC-3 cells. The nonhydrolyzable GTP analog GTP-gamma-S caused a dose-dependent inhibition of ¹²⁵I-[Tyr⁴]-bombesin binding to PC-3 and DU-145 cells, indicating that a G-protein (guanine nucleotide-binding protein) couples the bombesin receptor to intracellular effector systems. Bombesin and GRP(14-27) inhibited the binding of ¹²⁵I-[Tyr⁴]-bombesin to both cell lines in a dose-dependent manner with inhibition constants (K_i of 0.5 nM and 0.4 nM, respectively. Both cell lines express the bombesin/GRP preferring bombesin receptor subtype, since, in displacement studies, neuromedin B was more than 200 times less potent than bombesin and GRP(14-27) in inhibiting the binding of ¹²⁵I-[Tyr⁴]-bombesin. Two synthetic bombesin/GRP antagonists, RC-3095 and RC-3110, powerfully inhibited the specific binding of ¹²⁵I-[Tyr⁴]-bombesin with K_i 0.92 nM and 0.26 nM on PC-3 cells, and 3.3 nM and 0.89 nM on DU-145 cells, respectively. These findings indicate that the PC-3 and DU-145 human prostate cancer cell lines possess specific high-affinity receptors for bombesin/GRP, and are suitable models for the evaluation of the antineoplastic activity of new bombesin/GRP antagonists in the treatment of androgen-independent prostate cancer. © 1994 Wiley-Liss, Inc.