A Zinc(II) Phthalocyanine Conjugated with an Oxaliplatin Derivative for Dual Chemo- and Photodynamic Therapy
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摘要A novel zinc(II) phthalocyanine substituted with an oxaliplatin derivative via a triethylene glycol linker has been synthesized. The two components work in a cooperative manner in the antitumor action. The conjugate shows a cytotoxic effect in the dark due to the cytostatic oxaliplatin moiety and an enhanced cytotoxicity upon illumination due to the photosensitizing phthalocyanine unit against the HT29 human colon adenocarcinoma cells, The IC50 value of the conjugate is as low as 0.11 mu M, which is S-fold lower than that of the reference compound without the platinum complex. The high photodynamic activity of the conjugate can be attributed to its high cellular uptake and efficiency in generating intracellular reactive oxygen species. The conjugate also shows preferential localization in the lysosomes of the cells and induces cell death mainly through apoptosis.
著者Lau JTF, Lo PC, Fong WP, Ng DKP
期刊名稱Journal of Medicinal Chemistry
出版年份2012
月份6
日期14
卷號55
期次11
出版社American Chemical Society
頁次5446 - 5454
國際標準期刊號0022-2623
電子國際標準期刊號1520-4804
語言英式英語
Web of Science 學科類別Chemistry, Medicinal; CHEMISTRY, MEDICINAL; Pharmacology & Pharmacy

上次更新時間 2020-18-10 於 00:32