Synthesis and photodynamic activities of integrin-targeting silicon(IV) phthalocyanine-cRGD conjugates - Details

author：

Indexed by：

Scopus

Abstract：

A　series　of　novel　symmetric　or　unsymmetric　silicon　(IV)　phthalocyanines　axially　substituted　with　cyclic　Arg-Gly-Asp　(cRGD)　ligands　through　different　ethylene　glycol　chains　have　been　synthesized　by　a　facile　and　mild　“click”　reaction.　All　the　compounds　show　efficient　photosensitizing　activities　in　N,N-dimethylformamide,　and　are　essentially　non-aggregated　in　RPMI　1640　medium　with　0.05%　Cremophor　EL.　Owing　to　the　presence　of　two　cRGD　ligands,　the　conjugate　6b　exhibits　highest　selectivity　toward　αvβ3　+　HT-29　cells　in　photocytotoxicities.　It　shows　higher　cellular　uptake　and　ROS　generation　efficiency　toward　the　αvβ3　+　HT-29　cells　compared　with　that　of　αvβ3　-　MCF-7　cells.　The　competitive　cellular　uptake　and　subcellular　localization　indicate　that　6b　is　internalized　mainly　through　integrin-mediated　endocytosis.　In　addition,　the　in　vivo　studies　showed　that　6b　can　mainly　accumulate　in　tumor　sites　and　show　a　significant　PDT　effect　resulting　in　75%　tumor　growth　inhibition.　The　results　indicate　that　6b　is　a　highly　promising　photosensitizer　for　targeted　photodynamic　therapy.　©　2018　Elsevier　Masson　SAS

Keyword：

Cancer; cRGD; Integrin; Photodynamic therapy; Silicon(IV) phthalocyanine

Community：

[ 1 ] [Zheng, B.-Y.]College of Chemistry, State Key Laboratory of Photocatalysis on Energy and Environment, Fujian Provincial Key Laboratory of Cancer Metastasis Chemoprevention and Chemotherapy, Fuzhou University, Fuzhou, 350116, China
[ 2 ] [Yang, X.-Q.]College of Chemistry, State Key Laboratory of Photocatalysis on Energy and Environment, Fujian Provincial Key Laboratory of Cancer Metastasis Chemoprevention and Chemotherapy, Fuzhou University, Fuzhou, 350116, China
[ 3 ] [Zhao, Y.]College of Chemistry, State Key Laboratory of Photocatalysis on Energy and Environment, Fujian Provincial Key Laboratory of Cancer Metastasis Chemoprevention and Chemotherapy, Fuzhou University, Fuzhou, 350116, China
[ 4 ] [Zheng, Q.-F.]College of Chemistry, State Key Laboratory of Photocatalysis on Energy and Environment, Fujian Provincial Key Laboratory of Cancer Metastasis Chemoprevention and Chemotherapy, Fuzhou University, Fuzhou, 350116, China
[ 5 ] [Ke, M.-R.]College of Chemistry, State Key Laboratory of Photocatalysis on Energy and Environment, Fujian Provincial Key Laboratory of Cancer Metastasis Chemoprevention and Chemotherapy, Fuzhou University, Fuzhou, 350116, China
[ 6 ] [Lin, T.]Department of Pharmacy, The Affiliated First Hospital of Fujian Medical University, Fuzhou, 350001, China
[ 7 ] [Chen, R.-X.]School of Chemistry, University of New South Wales, Sydney, NSW 2052, Australia
[ 8 ] [Ho, K.K.K.]School of Chemistry, University of New South Wales, Sydney, NSW 2052, Australia
[ 9 ] [Kumar, N.]School of Chemistry, University of New South Wales, Sydney, NSW 2052, Australia
[ 10 ] [Huang, J.-D.]College of Chemistry, State Key Laboratory of Photocatalysis on Energy and Environment, Fujian Provincial Key Laboratory of Cancer Metastasis Chemoprevention and Chemotherapy, Fuzhou University, Fuzhou, 350116, China

Reprint 's Address：

[Huang, J.-D.]College of Chemistry, State Key Laboratory of Photocatalysis on Energy and Environment, Fujian Provincial Key Laboratory of Cancer Metastasis Chemoprevention and Chemotherapy, Fuzhou UniversityChina

Email：

jdhuang@fzu.edu.cn

Show more details

Related Keywords：

Source ：

European Journal of Medicinal Chemistry

ISSN： 0223-5234

Year： 2018

Volume： 155

Page： 24-33

4 . 8 3 3

JCR@2018

6 . 0 0 0

JCR@2023

ESI HC Threshold：209

JCR Journal Grade：1

CAS Journal Grade：1

Cited Count：

WoS CC Cited Count：

SCOPUS Cited Count： 33

ESI Highly Cited Papers on the List： 0 Unfold All

WanFang Cited Count：

Chinese Cited Count：

30 Days PV： 1

Affiliated Colleges：

Get Fulltext

DOI Library Discovery Baidu Scholar Search SCOPUS

Type
Departments

All Years Choose Year From to