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合成了一种碘桥双核铂配合物二(μ-碘)·af-二碘·二(环己胺)合二铂(Ⅱ)(BPA),用元素分析、摩尔电导、差热热重分析、红外光谱、紫外光谱和1H核磁共振谱对配合物进行了表征.体外抗肿瘤活性研究表明,其对人膀胱癌细胞EJ,人结肠癌细胞HCT-8,人胃癌细胞BGC-823,人急性早幼粒白血病细胞HL-60和人乳腺癌细胞MCF-7五种肿瘤细胞的活性明显好于顺铂;浓度为1.00和2.00μmol/L的该配合物可以阻止HL-60细胞周期G1→S的进行;相同条件下,其与HL-60细胞的DNA键合量明显高于顺铂;急性毒性实验表明,腹腔注射BPA的半数致死量LD50为815.3mg/kg;体内药效学研究表明,腹腔注射BPA,12mg/kg的BPA明显抑制人卵巢癌A2780及人结肠癌HCT-116裸鼠异体移植性肿瘤的生长,而且作用强度与阳性对照药4mg/kg的顺铂相近;20mg/kg的BPA可在一定程度上对人肺腺癌A549裸鼠异体移植性肿瘤的生长有一定的抑制作用,但统计学上无显著差异.
A bis (μ-iodine) · af-diiodo · di (cyclohexylamine) platinum (Ⅱ) (BPA) complex was synthesized and characterized by elemental analysis, molar conductance and differential thermal gravimetric analysis , IR, 1H-NMR and 1H nuclear magnetic resonance spectroscopy. The antitumor activity in vitro showed that the complex has good cytotoxicity against human bladder cancer cell EJ, human colon cancer cell HCT-8, human gastric cancer cell BGC-823, human acute The activity of HL-60 cells and MCF-7 cells was significantly higher than that of cisplatin. The concentrations of 1.00 and 2.00μmol / L could prevent the cell cycle G1 → S The DNA binding of HL-60 cells was significantly higher than that of cisplatin under the same conditions. The acute toxicity test showed that the LD50 of intraperitoneal injection of BPA was 815.3 mg / kg. In vivo pharmacodynamic studies showed that intraperitoneal injection BPA and BPA at 12 mg / kg significantly inhibited the growth of xenografted tumors in human ovarian cancer A2780 and human colon cancer HCT-116 nude mice, and the intensity of BPA was similar to that of positive control 4 mg / kg cisplatin. BPA 20 mg / kg To some extent, the growth of human lung adenocarcinoma A549 xenografted tumors in a certain extent, but statistics No significant difference in learning.