• 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>Life sciences >Studies on the antitumor activity and biochemical actions of cyclopentenyl cytosine against human colon carcinoma HT-29 in vitro and in vivo.
【24h】

Studies on the antitumor activity and biochemical actions of cyclopentenyl cytosine against human colon carcinoma HT-29 in vitro and in vivo.

机译：环戊烯基胞嘧啶在体外和体内对人结肠癌HT-29的抗肿瘤活性和生化作用的研究。

获取原文
获取原文并翻译 | 示例
           
页面导航
  • 摘要
  • 著录项
  • 相似文献
  • 相关主题

摘要

Cyclopentenyl cytosine (CPEC) is cytotoxic to several tumor cell lines. CPEC inhibits CTP synthesis resulting in depletion of cytidylate pools. The aim of this study was to examine CPEC's cytotoxic and antitumor activity in vitro and in vivo against human colon carcinoma HT-29, and to relate its action on CTP synthesis. CPEC exhibits potent cytotoxicity in vitro to HT-29 cells with an LC50 (concentration that is lethal to the survival of 50% cell colonies) of 2.4 microM and 0.46 microM following 2 h and 24 h exposure, respectively. Incubation of cells with CPEC for 2 h resulted in a dose-dependent decrease in cytidylate pools. The in vivo antitumor activity of CPEC in athymic mice transplanted subcutaneously (s.c.) with 3 million HT-29 cells was examined. Antitumor activity of CPEC was elucidated in early-staged tumor, wherein CPEC (1.5 mg/kg, QD x 9 or 3 mg/kg, QOD x 9) was administered intraperitoneally (i.p.) 24 h after tumor implantation and it resulted in a significant reduction in tumor weight to 48% of control. The effect of CPEC on established solid tumors in vivo was examined in athymic mice transplanted s.c. 14 days earlier with HT-29 cells and treated i.p. with 1.5 mg/kg CPEC, QD x 5 for 4 courses, with a 10 day-interval between courses. This treatment resulted in a significant reduction in tumor weight (72%) in the treated group. HPLC analysis of HT-29 tumor obtained from mice after treatment with CPEC showed a depletion of the CTP concentration reaching a nadir at 8 h. In conclusion, the present studies demonstrate potent antitumor activity of CPEC against freshly transplanted and established human colon carcinoma which can be corroborated with the drug's biochemical actions.
机译：环戊烯基胞嘧啶（CPEC）对几种肿瘤细胞系具有细胞毒性。 CPEC抑制CTP合成，从而导致胞苷酸池消耗。这项研究的目的是检查CPEC在体外和体内对人结肠癌HT-29的细胞毒性和抗肿瘤活性，并探讨其对CTP合成的作用。 CPEC在体外对HT-29细胞表现出强力的细胞毒性，暴露2 h和24 h后的LC50（对50％细胞集落的存活具有致命性的浓度）分别为2.4 microM和0.46 microM。用CPEC将细胞孵育2小时会导致胞嘧啶库的剂量依赖性降低。检查了CPEC在皮下移植了300万HT-29细胞的无胸腺小鼠体内的抗肿瘤活性。阐明了CPEC在早期肿瘤中的抗肿瘤活性，其中在肿瘤植入后24 h腹膜内（ip）施用CPEC（1.5 mg / kg，QD x 9或3 mg / kg，QOD x 9）。肿瘤重量减少至对照组​​的48％。在经皮下移植的无胸腺小鼠中检查了CPEC对体内已建立的实体瘤的作用。用HT-29细胞提前14天并经腹膜内处理。用1.5 mg / kg CPEC，QD x 5进行4个疗程，疗程之间间隔10天。这种治疗导致治疗组的肿瘤重量显着减少（72％）。经CPEC治疗后从小鼠获得的HT-29肿瘤的HPLC分析表明，CTP浓度在8小时达到最低点。总而言之，本研究证明了CPEC对新鲜移植和建立的人结肠癌具有有效的抗肿瘤活性，这一点可与该药物的生化作用相证实。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱：kefu@zhangqiaokeyan.com

京公网安备：11010802029741号 ICP备案号：京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有

  • 客服微信

  • 服务号