4.8 Article

The cis-Diammineplatinum(II) Complex of Curcumin: A Dual Action DNA Crosslinking and Photochemotherapeutic Agent

期刊

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
卷 54, 期 47, 页码 13989-13993

出版社

WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.201507281

关键词

antitumor agents; cell imaging; curcumin; DNA; platinum

资金

  1. Department of Science and Technology (DST), Government of India [SR/S5/MBD-02/2015]
  2. DST

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[Pt(cur)(NH3)(2)](NO3) (1), a curcumin-bound cis-diammineplatinum(II) complex, nicknamed Platicur, as a novel photoactivated chemotherapeutic agent releases photoactive curcumin and an active platinum(II) species upon irradiation with visible light. The hydrolytic instability of free curcumin reduces upon binding to platinum(II). Interactions of 1 with 5'-GMP and ct-DNA indicated formation of platinum-bound DNA adducts upon exposure to visible light (lambda = 400-700 nm). It showed apoptotic photocytotoxicity in cancer cells (IC50 approximate to 15 mu M), thus forming (OH)-O-center dot, while remaining passive in the darkness (IC50 > 200 mu M). A comet assay and platinum estimation suggest Pt-DNA crosslink formation. The fluorescence microscopic images showed cytosolic localization of curcumin, thus implying possibility of dual action as a chemo-and phototherapeutic agent.

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