Comparative Studies of the Cellular Uptake, Subcellular Localization, and Cytotoxic and Phototoxic Antitumor Properties of Ruthenium(II)鈥揚orphyrin Conjugates with Different Linkers

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• 作者：Jing-Xiang Zhang ; Jun-Wei Zhou ; Chi-Fai Chan ; Terrence Chi-Kong Lau ; Daniel W. J. Kwong ; Hoi-Lam Tam ; Nai-Ki Mak ; Ka-Leung Wong ; Wai-Kwok Wong
• 刊名：Bioconjugate Chemistry
• 出版年：2012
• 出版时间：August 15, 2012
• 年：2012
• 卷：23
• 期：8
• 页码：1623-1638
• 全文大小：771K
• 年卷期：v.23,no.8(August 15, 2012)
• ISSN：1520-4812

文摘

Six water-soluble free-base porphyrin-Ru(II) conjugates, 1鈥?b>3, and Zn(II) porphyrin-Ru(II) conjugates, 4鈥?b>6, with different linkers between the hydrophobic porphyrin moiety and the hydrophilic Ru(II)-polypyridyl complex, have been synthesized. The linear and two-photon-induced photophysical properties of these conjugates were measured and evaluated for their potential application as dual in vitro imaging and photodynamic therapeutic (PDT) agents. Conjugates 1鈥?b>3, with their high luminescence and singlet oxygen quantum yields, were selected for further study of their cellular uptake, subcellular localization, and cytotoxic and photocytotoxic (under linear and two-photon excitation) properties using HeLa cells. Conjugate 2, with its hydrophobic phenylethynyl linker, was shown to be highly promising for further development as a bifunctional probe for two-photon (NIR) induced PDT and in vitro imaging. Cellular uptake and subcellular localization properties were shown to be crucial to its PDT efficacy.