Synthesis of Tumor-Avid Photosensitizer-Gd(III)DTPA Conjugates: Impact of the Number of Gadolinium Units in T1/T2 Relaxivity, Intracellular localization, and Photosensitizing Efficacy

被引：31

作者：

Goswami, Lalit N. ^{[1
]}

White, William H., III ^{[1
]}

Spernyak, Joseph A. ^{[2
]}

Ethirajan, Manivannan ^{[1
]}

Chen, Yihui ^{[1
]}

Missert, Joseph R. ^{[1
]}

Morgan, Janet ^{[3
]}

Mazurchuk, Richard ^{[2
]}

Pandey, Ravindra K. ^{[1
]}

机构：

[1] Roswell Pk Canc Inst, PDT Ctr, Buffalo, NY 14263 USA

[2] Roswell Pk Canc Inst, Preclin Imaging Facil, Buffalo, NY 14263 USA

[3] Roswell Pk Canc Inst, Dept Dermatol, Buffalo, NY 14263 USA

来源：

BIOCONJUGATE CHEMISTRY | 2010年 / 21卷 / 05期

关键词：

PHOTODYNAMIC THERAPY; AGENTS; FLUORESCENCE; PHARMACOKINETICS; SERIES; HPPH;

D O I：

10.1021/bc9005305

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

To develop novel bifunctional agents for tumor imaging (MR) and photodynamic therapy (PDT), certain tumor-avid photosensitizers derived from chlorophyll-a were conjugated with variable number of Gd(III)aminobenzyl DTPA moieties. All the conjugates containing three or six gadolinium units showed significant T-1 and T-2 relaxivities. However, as a bifunctional agent, the 3-(1'-hexyloxyethyl)pyropheophorbide-a (HPPH) containing 3Gd(III) aminophenyl DTPA was most promising with possible applications in tumor-imaging and PDT. Compared to HPPH, the corresponding 3- and 6Gd(III)aminobenzyl DTPA conjugates exhibited similar electronic absorption characteristics with a slightly decreased intensity of the absorption band at 660 nm. However, compared to HPPH, the excitation of the broad "Soret" band (near 400 nm) of the corresponding 3Gd(III)aminobenzyl-DTPA analogues showed a significant decrease in the fluorescence intensity at 667 nm.

引用

页码：816 / 827

页数：12