Document Detail


A Zinc(II) Phthalocyanine Conjugated with an Oxaliplatin Derivative for Dual Chemo- and Photodynamic Therapy.
MedLine Citation:
PMID:  22646131     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
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 IC(50) value of the conjugate is as low as 0.11 μM, which is 5-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.
Authors:
Janet T F Lau; Pui-Chi Lo; Wing-Ping Fong; Dennis K P Ng
Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2012-5-31
Journal Detail:
Title:  Journal of medicinal chemistry     Volume:  -     ISSN:  1520-4804     ISO Abbreviation:  -     Publication Date:  2012 May 
Date Detail:
Created Date:  2012-5-31     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9716531     Medline TA:  J Med Chem     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Affiliation:
Department of Chemistry and ‡School of Life Sciences, The Chinese University of Hong Kong , Shatin, N.T., Hong Kong, China.
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