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Cytotoxicity of the traditional chinese medicine (TCM) plumbagin in its copper chemistry

TitleCytotoxicity of the traditional chinese medicine (TCM) plumbagin in its copper chemistry
Publication TypeJournal Article
Year of Publication2009
AuthorsChen, ZF, Tan, MX, Liu, LM, Liu, YC, Wang, HS, Yang, B, Peng, Y, Liu, HG, Liang, H, Orvig, C
JournalDalton Transactions
Pagination10824-10833
Type of ArticleArticle
ISBN Number1477-9226
KeywordsBIOLOGICAL-ACTIVITY, CALF-THYMUS DNA, CANCER-CELLS, CRYSTAL-STRUCTURE, DNA CLEAVAGE ACTIVITY, IRON(II) COMPLEXES, METAL-COMPLEXES, N-PROPYL-NORFLOXACIN, PLATINUM ANTICANCER AGENTS, TOPOISOMERASE-I
Abstract

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.

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