Synthesis and antitumor activity of iodo-bridged binuclear platinum complex

来源 :Chinese Science Bulletin | 被引量 : 0次 | 上传用户:JK0803_zhoukaijun
下载到本地 , 更方便阅读
声明 : 本文档内容版权归属内容提供方 , 如果您对本文有版权争议 , 可与客服联系进行内容授权或下架
论文部分内容阅读
Iodo-bridged binuclear platinum(II) com- plex[Pt( -NH2)I2]2(BPA) has been synthesized and characterized by elemental analysis, conductivity, differential thermal analysis, IR, UV and 1HNMR spectra techniques. The cytotoxicity of the complex was tested by MTT and SRB assays. The results show that complex BPA demonstrates better cyto-toxicity than that of the clinically established cisplatin against EJ, HCT-8, BGC-823, HL-60 and MCF-7 cell lines. The complex BPA at concentrations of 1.00 and 2.00 μmol/L induces G1 cell cycle arrest in HL-60 cells. The level of total platinum bound to DNA in HL-60 cells is significantly higher than that of cisplatin under the same experimental conditions. Acute tox-icity experimental results indiacte that LD50 of BPA is 815.3 mg/kg by intraperitoneal administration. BPA at dose of 12 mg/kg significantly inhibits the growth of nude mice implanted by human A2780 and HCT-116 carcinomas, and inhibition rate is similar to that of cisplatin at dose of 4 mg/kg by intraperitoneal admini-stration. BPA at dose of 20 mg/kg inhibits the growth of nude mice implanted by human A549 carcinomas, but there was no significant statistical difference. Iodo-bridged binuclear platinum (II) com- plex [Pt (-NH2) I2] 2 (BPA) has been synthesized and characterized by elemental analysis, conductivity, differential thermal analysis, IR, UV and 1H NMR spectra techniques. The cytotoxicity of the complex was tested by MTT and SRB assays. The results show that complex BPA demonstrates better cyto-toxicity than that of the clinically established cisplatin against EJ, HCT-8, BGC-823, HL-60 and MCF-7 cell lines. The complex BPA at concentrations of 1.00 and 2.00 μmol / L induces G1 cell cycle arrest in HL-60 cells. The level of total platinum bound to DNA in HL-60 cells is significantly higher than that of cisplatin under the same experimental conditions. Acute tox- icity experimental results indiacte that LD50 of BPA is 815.3 mg / kg by intraperitoneal administration. BPA at dose of 12 mg / kg significantly inhibits the growth of nude mice implanted by human A2780 and HCT-116 carcinomas, and inhibition rate is similar to that of cisplatin at dose of 4 mg / kg by intraperitoneal admini-stration. BPA at dose of 20 mg / kg inhibits the growth of nude mice implanted by human A549 carcinomas, but there was no significant statistical difference.
其他文献
WTO不仅是一个多边贸易体系的国际组织,同时,WTO还是一种制度体系。中国加入WTO后,就必须按照WTO的规则办事,由从前的政策型开放向制度型开放转变。在这一过程中,对外开放将
目前高职院校学生信息管理系统化、网络化是目前学生信息管理的主流,校方可以利用信息管理软件的相关算法高效的对学生的信息进行筛选管理、为学生服务、记录学生的课业、学
目的 观察去甲长春碱持续静脉输注加顺铂治疗非小细胞肺癌的疗效及毒性作用.方法对去甲长春碱持续静脉输注组(改良NP组)与常规去甲长春碱加顺铂方案组(NP方案组)临床资料进行分析比较.结果改良NP组有效率为46.42%,NP方案组有效率为44.44%,两组差异无统计学意义(P>0.05),毒性作用两组主要为骨髓抑制,白细胞减少发生率分别为50.00%和81.48%,两者比较差异有统计学意义(P<0.0
随着计算机技术的发展数字三维动画的日益成熟,三维动画片也深受观众喜爱。因为市场的需要,所以各高校也纷纷开设了三维动画制作这门课程,但是数字三维动画的学科体系建设毕
目的 观察以去甲长春碱(NVB)为主的化疗方案对晚期非小细胞肺癌(NSCLC)的疗效.方法选择20例晚期NSCLC患者接受以NVB为主的化疗方案,其中10例接受DDP+NVB两药联合化疗方案,其他10例接受DDP+NVB+IFO(或VM26)三药联合化疗方案,根据每位患者治疗前后X线胸片、胸部CT检查对肺内肿块或纵隔淋巴结进行对比,并评价疗效.结果20例病例中,无CR病例,PR8例,SD9例,PD
Multicentric reticulohistiocytosis (MRH) is a rare histocytic disease characterized by destructive arthritis in association with classic skin findings. Although
省政协把“推动高等职业教育发展”列入2015年重点协商议题,开展全面的专题调研,充分体现了对我省职业教育工作的高度重视和热情关心。我厅在工作中充分吸纳省政协的建议,会
边境贸易是一种特殊的贸易形式 ,它对边境地区的经济发展具有重要意义 ,我国加入WTO以后 ,边境贸易与WTO规则具有不相符之处 ,我们要充分利用发展中国家的身份 ,利用缓冲期 ,
新世纪的市场营销 ,决胜在思想。历史给思想以食粮和驿站 ,中国传统文化中蕴含着颇具特色的营销思想遗产 ,范蠡、白圭关于市场预测的思想认识和司马迁有关选择市场机会的理论
癌症术后静脉血栓栓塞(VTE)的流行病学是以临床上使用静脉造影筛查深静脉血栓形成(DVT)来预防VTE为基础的。然而,临床上无症状患者静脉造影发现DVT的关联性仍然未知,且这些临床研究的人群并不足以代表全部癌症手术的人群。为评价在接受过手术的癌症患者中临床症状明显的VTE的发生率,确定VTE的风险因子,意大利的Agnelli等近期开展了一项名为@RISTOS的前瞻性观测性研究,并将结果刊登在Ann