PMID- 21920738
OWN - NLM
STAT- MEDLINE
DCOM- 20120131
LR  - 20131121
IS  - 1464-3405 (Electronic)
IS  - 0960-894X (Linking)
VI  - 21
IP  - 21
DP  - 2011 Nov 1
TI  - Radiolabeling of folic acid-modified chitosan with (99m)Tc as potential agents 
      for folate-receptor-mediated targeting.
PG  - 6446-50
LID - 10.1016/j.bmcl.2011.08.086 [doi]
AB  - The feasibility of chitosan (CS) as a backbone for the design of (99m)Tc-labeled 
      targeting agent was evaluated in this study. Chitosan-folate conjugate (CSFA) and 
      chitosan-folate dithiocarbamate (CSFADTC) were synthesized, characterized and 
      radiolabeled with (99m)Tc as model compounds for folate-receptor (FR) targeting. 
      (99m)Tc-complexes were prepared with high radiochemical purity and high 
      stability. The hydrophilicities of these (99m)Tc-complexes were determined by 
      partition coefficient experiments. The results of biodistribution in normal mice 
      showed that the folic-acid modified agents ((99m)Tc-CSFA and (99m)TcN-CSFADTC) 
      had obviously higher uptake in FR-positive kidney and much lower liver and spleen 
      uptakes than that of non-folic-acid modified (99m)Tc-agent, and the kidney 
      uptakes of FA-modified agents could be blocked significantly by the corresponding 
      cold ligand. Furthermore in vitro and in vivo specific studies will be done in 
      cell line and tumor bearing mice to confirm the usefulness of this chitosan 
      backbone for FR targeting agent design.
CI  - Copyright (c) 2011 Elsevier Ltd. All rights reserved.
FAU - Guo, Wenyan
AU  - Guo W
AD  - Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of 
      Chemistry, Beijing Normal University, 19 Xinjiekou Outer St., Beijing 100875, 
      China.
FAU - Jing, Huihui
AU  - Jing H
FAU - Yang, Wenjiang
AU  - Yang W
FAU - Guo, Zhide
AU  - Guo Z
FAU - Feng, Shi
AU  - Feng S
FAU - Zhang, Xianzhong
AU  - Zhang X
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
DEP - 20110824
PL  - England
TA  - Bioorg Med Chem Lett
JT  - Bioorganic & medicinal chemistry letters
JID - 9107377
RN  - 0 (Folic Acid Transporters)
RN  - 0 (Organotechnetium Compounds)
RN  - 9012-76-4 (Chitosan)
RN  - 935E97BOY8 (Folic Acid)
SB  - IM
MH  - Animals
MH  - Chitosan/*chemistry/pharmacokinetics
MH  - Chromatography, High Pressure Liquid
MH  - Folic Acid/*chemistry
MH  - Folic Acid Transporters/*drug effects
MH  - Mice
MH  - Mice, Nude
MH  - Organotechnetium Compounds/*chemistry
MH  - Radiometry
MH  - Spectrophotometry, Infrared
MH  - Spectrophotometry, Ultraviolet
MH  - Tissue Distribution
EDAT- 2011/09/17 06:00
MHDA- 2012/02/01 06:00
CRDT- 2011/09/17 06:00
PHST- 2011/04/30 00:00 [received]
PHST- 2011/08/01 00:00 [revised]
PHST- 2011/08/18 00:00 [accepted]
PHST- 2011/09/17 06:00 [entrez]
PHST- 2011/09/17 06:00 [pubmed]
PHST- 2012/02/01 06:00 [medline]
AID - S0960-894X(11)01185-1 [pii]
AID - 10.1016/j.bmcl.2011.08.086 [doi]
PST - ppublish
SO  - Bioorg Med Chem Lett. 2011 Nov 1;21(21):6446-50. doi: 10.1016/j.bmcl.2011.08.086. 
      Epub 2011 Aug 24.