|Title||Cytotoxicity of the traditional chinese medicine (TCM) plumbagin in its copper chemistry|
|Publication Type||Journal Article|
|Year of Publication||2009|
|Authors||Chen, ZF, Tan, MX, Liu, LM, Liu, YC, Wang, HS, Yang, B, Peng, Y, Liu, HG, Liang, H, Orvig, C|
|Type of Article||Article|
|Keywords||BIOLOGICAL-ACTIVITY, CALF-THYMUS DNA, CANCER-CELLS, CRYSTAL-STRUCTURE, DNA CLEAVAGE ACTIVITY, IRON(II) COMPLEXES, METAL-COMPLEXES, N-PROPYL-NORFLOXACIN, PLATINUM ANTICANCER AGENTS, TOPOISOMERASE-I|
The anticancer traditional Chinese medicine (TCM), plumbagin (PLN), was isolated from Plumbago Zeylanica. Reaction of plumbagin with Cu-II salt, afforded [Cu(PLN)(2)]center dot 2H(2)O (1). With 2,2’-bipyridine (bipy) as a co-ligand, PLN reacts with Cu-II to give [Cu(PLN)(bipy)(H2O)](2)(NO3)(2)center dot 4H(2)O (2). 1 and 2 were characterized by elemental analysis, IR, ESI-MS spectra. Their crystal structures were determined by single crystal X-ray diffraction methods. The in vitro cytotoxicity of PLN, 1 and 2 against seven human tumour cell lines was assayed. The metal-based compounds exhibit enhanced cytotoxicity vs. that of free PLN, suggesting that these compounds display synergy in the combination of metal ions with PLN. The binding properties of PLN, 1 and 2 to DNA were investigated through UV-vis, fluorescence, CD spectra, and gel mobility shift assay, which indicated that 1 and 2 were non-covalent binding and mainly intercalated the neighboring base pairs of DNA. PLN, 1 and 2 exhibit inhibition activity to topoisomerase I (TOPO I), but 1 and 2 were more effective than PLN.
|URL||<Go to ISI>://000272359900024|