Luminescent Biological Probes Derived from Ruthenium(II) Estradiol Polypyridine Complexes

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• 作者：Kenneth Kam-Wing Lo ; Terence Kwok-Ming Lee ; Jason Shing-Yip Lau ; Wing-Lin Poon ; Shuk-Han Cheng
• 刊名：Inorganic Chemistry
• 出版年：2008
• 出版时间：January 7, 2008
• 年：2008
• 卷：47
• 期：1
• 页码：200 - 208
• 全文大小：320K
• 年卷期：v.47,no.1(January 7, 2008)
• ISSN：1520-510X

文摘

Four luminescent ruthenium(II) polypyridine estradiol complexes [Ru(NN)₂(bpy-estradiol)](PF₆)₂ (NN = 2,2'-bipyridine(bpy), 4,7-diphenyl-1,10-phenanthroline (Ph₂-phen); bpy-estradiol = 5-(4-(17-ethynylestradiolyl)phenyl)-2,2'-bipyridine(bpy-ph-est), 4-(N-(6-(4-(17-ethynylestradiolyl)benzoylamino)hexyl)aminomethyl)-4'-methyl-2,2'-bipyridine (mbpy-C6-est)) have been designed as new luminescent biological probes. The lipophilicity and photophysical andelectrochemical properties of these complexes have been investigated. Upon photoexcitation, all the complexesexhibited intense and long-lived triplet metal-to-ligand charge-transfer (³MLCT) (d(Ru) *(diimine)) emission influid solutions at 298 K and in low-temperature glass. The binding of the complexes to estrogen receptor- (ER)has been studied by emission titrations. The Ph₂-phen complexes showed emission enhancement and increasedlifetimes upon binding to the protein. Additionally, the cytotoxicity of the complexes toward the HeLa cell line hasbeen examined by the 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyltetrazolium bromide (MTT) assay and the IC₅₀ valuesranged from 83.1 to 166.6 M (cisplatin showed an IC₅₀ value of 34.3 M under the same experimental conditions).Furthermore, the cellular uptake of the complexes has been investigated by flow cytometry and laser-scanningconfocal microscopy.