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author:

Zhou, X.-Q. (Zhou, X.-Q..) [1] | Meng, L.-B. (Meng, L.-B..) [2] | Huang, Q. (Huang, Q..) [3] | Li, J. (Li, J..) [4] | Zheng, K. (Zheng, K..) [5] | Zhang, F.-L. (Zhang, F.-L..) [6] | Liu, J.-Y. (Liu, J.-Y..) [7] | Xue, J.-P. (Xue, J.-P..) [8]

Indexed by:

Scopus

Abstract:

The combination of photodynamic therapy and chemotherapy is a promising strategy to overcome growing problems in contemporary medicine, such as low therapeutic efficacy and drug resistance. Four zinc(II) phthalocyanine-coumarin conjugates were synthesized and characterized. In these complexes, zinc(II) phthalocyanine was used as the photosensitizing unit, and a coumarin derivative was selected as the cytostatic moiety; the two components were linked via a tri(ethylene glycol) chain. These conjugates exhibit high photocytotoxicity against HepG2 human hepatocarcinoma cells, with low IC50 values in the range of 0.014-0.044 μm. The high photodynamic activities of these conjugates are in accordance with their low aggregation tendency and high cellular uptake. One of these conjugates exhibits high photocytotoxicity and significantly higher chemocytotoxicity. The results clearly show that the two antitumor components in these conjugates work in a cooperative fashion. As shown by confocal microscopy, the conjugates can localize in the mitochondria and lysosomes, and one of the conjugates can also localize in the cell nuclei. © 2015 Wiley-VCH Verlag GmbH & Co. KGaA.

Keyword:

Chemotherapy; Conjugation; Coumarin; Photodynamic therapy; Phthalocyanine

Community:

  • [ 1 ] [Zhou, X.-Q.]Fujian Engineering Research Center for Drugs and Diagnoses - Photodynamic Therapy, College of Chemistry, Fuzhou University, Fuzhou, Fujian 350108, China
  • [ 2 ] [Meng, L.-B.]Fujian Engineering Research Center for Drugs and Diagnoses - Photodynamic Therapy, College of Chemistry, Fuzhou University, Fuzhou, Fujian 350108, China
  • [ 3 ] [Huang, Q.]Fujian Engineering Research Center for Drugs and Diagnoses - Photodynamic Therapy, College of Chemistry, Fuzhou University, Fuzhou, Fujian 350108, China
  • [ 4 ] [Li, J.]Fujian Engineering Research Center for Drugs and Diagnoses - Photodynamic Therapy, College of Chemistry, Fuzhou University, Fuzhou, Fujian 350108, China
  • [ 5 ] [Zheng, K.]Fujian Engineering Research Center for Drugs and Diagnoses - Photodynamic Therapy, College of Chemistry, Fuzhou University, Fuzhou, Fujian 350108, China
  • [ 6 ] [Zhang, F.-L.]Fujian Engineering Research Center for Drugs and Diagnoses - Photodynamic Therapy, College of Chemistry, Fuzhou University, Fuzhou, Fujian 350108, China
  • [ 7 ] [Liu, J.-Y.]Fujian Engineering Research Center for Drugs and Diagnoses - Photodynamic Therapy, College of Chemistry, Fuzhou University, Fuzhou, Fujian 350108, China
  • [ 8 ] [Xue, J.-P.]Fujian Engineering Research Center for Drugs and Diagnoses - Photodynamic Therapy, College of Chemistry, Fuzhou University, Fuzhou, Fujian 350108, China

Reprint 's Address:

  • [Xue, J.-P.]Fujian Engineering Research Center for Drugs and Diagnoses - Photodynamic Therapy, College of Chemistry, Fuzhou UniversityChina

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Source :

ChemMedChem

ISSN: 1860-7179

Year: 2015

Issue: 2

Volume: 10

Page: 304-311

2 . 9 8

JCR@2015

3 . 6 0 0

JCR@2023

ESI HC Threshold:193

JCR Journal Grade:2

CAS Journal Grade:2

Cited Count:

WoS CC Cited Count:

SCOPUS Cited Count: 35

ESI Highly Cited Papers on the List: 0 Unfold All

WanFang Cited Count:

Chinese Cited Count:

30 Days PV: 0

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