Administration of the antitumor drug mitoguazone protects normal thymocytes against spontaneous and etoposide-induced apoptosis

The suggestion has been made that polyamines may be involved in the control of cell death, since exceedingly high or low levels induce apoptosis in different cell systems. For a deeper insight into the relationship between apoptosis and polyamine metabolism, we investigated in vitro the effect on rat thymocytes of mitoguazone (MGBG, which inhibits S-adenosylmethionine decarboxylase, i.e. a key enzyme in the polyamine biosynthetic pathway). Thymocytes were selected as an especially suitable model system, since they undergo spontaneous apoptosis in vivo and can be easily induced to apoptose in vitro by etoposide, used here as an apoptogenic agent. MGBG protected thymocytes from both spontaneous and drug-induced apoptosis, and this protective effect was associated with a decrease in polyamine oxidase activity and total polyamine levels.Received 7 July 2004; received after revision 2 September 2004; accepted 9 September 2004     

CE与EP方案治疗小细胞肺癌的临床疗效评价

为观察CE与EP方案治疗小细胞肺癌的近期疗效和毒副反应,对52例小细胞肺癌患者按住院先后顺序,随机分为CE组(卡铂+足叶乙甙)和EP组(顺铂+足叶乙甙),化疗2周期后评价疗效。结果近期疗效方面,CE组CR6例,PR14例,总有效20例(76.9%);EP组CR5例,PR13例,总有效18例(69.2%),两组比较无差别(P>0.05)。在毒副反应方面,CE与EP两组发生Ⅱ度以上的胃肠道反应及骨髓抑制无差别,患者均能耐受。说明CE与EP方案治疗小细胞肺癌均有效,且近期疗效无差别,毒副反应均能耐受,均可作为小细胞肺癌一线化疗方案。     

顺铂、足叶乙甙腹腔灌注治疗癌性腹水35例疗效观察

癌性腹水 35例 ,采用腹腔穿刺抽液后 ,向腹腔内注入顺铂及足叶乙甙 ,观察其疗效及毒副作用。根据国际卫生组织 (WHO)癌性渗液疗效评定标准 ,完全缓解 15例 ,占 4 2 .9% ;部分缓解 7例 ,占 2 0 % ;总有效率 6 2 .9%。可见顺铂、足叶乙甙腹腔灌注治疗癌性腹水效果较好 ,副作用少 ,是一种较为安全有效的方法     

草药物与人血白蛋白相互作用的分光光度法研究

以曙红Y为光谱探针,采用分光光度法探讨抗癌药物足叶乙甙对人血白蛋白中曙红Y的竞争结合规律,研究足叶乙甙与人血白蛋白的相互作用及结合.结果表明,曙红Y与人血白蛋白以静电作用力为主进行结合,形成电子转移配合物.曙红Y与人血白蛋白结合后,药物足叶乙甙的加入对这种结合产生破坏,争夺并占据人血白蛋白的结合点位,使曙红Y从结合态变成游离态,同时生成新的更为稳定的结合体—人血白蛋白与药物足叶乙甙复合物,其结合比约为7.93molVp16/molHSA.由此说明:足叶乙甙不仅与人血白蛋白存在有效的结合点位,而且具有较好的结合强度和结合容量.这些既是足叶乙甙在人体内贮存和运输的条件,也是其产生抗癌活性的药理基础.     

依托泊苷纳米混合胶束的制备及其理化性质

为提高依托泊苷制剂的水溶性和稳定性,采用星点设计-效应面法优化依托泊苷纳米混合胶束(ETP mPEG-PLA/P123)的处方工艺.在单因素试验基础上,以投药量、mPEG-PLA所占质量比和水化体积为自变量,以依托泊苷包封率、载药量以及粒径为因变量,进行3因素5水平的星点设计-效应面法实验,采用荧光探针法测定临界胶束浓...     

氨基酸—琥珀酸依托泊甙盐的制备

从依托泊甙出发合成得到琥珀酸依托泊甙，琥珀酸依托泊甙与氨基酸相结合形成复盐，从而得到依托泊甙的新水溶性抗肿瘤前体药物．化合物Ｃ，Ｄ１，Ｄ２，Ｄ３均为首次合成