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 cyto...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.展开更多
A new polymeric demethylcantharidato （DCA） bridged copper（II） phenanthroline （phen） complex （[Cu（DCA）（phen）]n-nH20） has been synthesized and characterized by elemental analysis, IR and electronic spectra s...A new polymeric demethylcantharidato （DCA） bridged copper（II） phenanthroline （phen） complex （[Cu（DCA）（phen）]n-nH20） has been synthesized and characterized by elemental analysis, IR and electronic spectra studies, molar conductivity measure- ment, and single crystal X-ray diffraction. The complex crystallizes in the orthorhombic space group Pbca with crystallo- graphic data： a -- 12.4537（4）/~, b = 9.3897（5） A, c = 30.1264（10） A, and Z = 8. In the crystal structure, the octahedral coordi- nated copper（II） ions are bridged by demethylcantharidate ligands into a one-dimensional zigzag-like structure with the Cu＇＂Cu separation of 6.1719/~, along with phen ligands attached to both sides of the chain altematively. Interdigitation of the chelating phen ligands of two neighboring chains via hydrophobic interaction and van der Waals forces along ac plane forms two-dimensional polymeric bilayers with discrete water sandwich layer between the adjacent polymeric bilayers. The evalua- tion of the cytotoxic activity of the copper（II） complex against HCT-8 （colorectal carcinoma）, A549 （pulmonary carcinoma）, HeLa （cervical cancer）, HepG2 （hepatocarcinoma）, BGC-823 （gastric carcinoma）, and MCF-7 （breast adenocarcinoma） cell lines revealed that it is a potent cytotoxic agent, superior to Na2DCA and phen against HeLa, HepG2 and BGC-823 cells.展开更多
基金supported by the Natural Science Foundation of Zhejiang Province(Grant No.298068)the 0pening Foundation of State Key Laboratory of Natural and Biomimetic Drugs,Peking University.
文摘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.
基金supported by the Doctoral Fund of Ministry of Education of China (20110001110054)
文摘A new polymeric demethylcantharidato （DCA） bridged copper（II） phenanthroline （phen） complex （[Cu（DCA）（phen）]n-nH20） has been synthesized and characterized by elemental analysis, IR and electronic spectra studies, molar conductivity measure- ment, and single crystal X-ray diffraction. The complex crystallizes in the orthorhombic space group Pbca with crystallo- graphic data： a -- 12.4537（4）/~, b = 9.3897（5） A, c = 30.1264（10） A, and Z = 8. In the crystal structure, the octahedral coordi- nated copper（II） ions are bridged by demethylcantharidate ligands into a one-dimensional zigzag-like structure with the Cu＇＂Cu separation of 6.1719/~, along with phen ligands attached to both sides of the chain altematively. Interdigitation of the chelating phen ligands of two neighboring chains via hydrophobic interaction and van der Waals forces along ac plane forms two-dimensional polymeric bilayers with discrete water sandwich layer between the adjacent polymeric bilayers. The evalua- tion of the cytotoxic activity of the copper（II） complex against HCT-8 （colorectal carcinoma）, A549 （pulmonary carcinoma）, HeLa （cervical cancer）, HepG2 （hepatocarcinoma）, BGC-823 （gastric carcinoma）, and MCF-7 （breast adenocarcinoma） cell lines revealed that it is a potent cytotoxic agent, superior to Na2DCA and phen against HeLa, HepG2 and BGC-823 cells.
