Tumor cell uptake of 99mTc-labeled 1-thio-β-D-glucose and 5-thio-D-glucose in comparison with 2-deoxy-2-[18F]fluoro-D-glucose in vitro: kinetics, dependencies, blockage and cell compartment of accumulation.
OBJECTIVE
This study was conducted to investigate the capacity of (99m)Tc-labeled 1-thio-β-D-glucose ((99m)Tc-1-TG) and 5-thio-D-glucose ((99m)Tc-5-TG) to act as a marker for glucose metabolism in tumor cells in vitro.


METHODS
We investigated the cellular uptake of (99m)Tc-1-TG, (99m)Tc-5-TG, and 2-deoxy-2-[(18)F]fluoro-D-glucose((18)F-FDG) in a human colorectal carcinoma and human lung adenocarcinoma cell line (HCT-116, A549) at different time points and varying glucose/insulin concentrations and under transporter blockage by cytochalasin-B and phloretin. Cell compartment analysis was performed.


RESULTS
A significant uptake and time dependency thereof, a significant uptake dependency on glucose and insulin and a significant uptake inhibition by cytochalasin-B for (99m)Tc-1-TG and (99m)Tc-5-TG, was shown. Albeit substantial, the uptake was less pronounced in (99m)Tc-1-TG and (99m)Tc-5-TG compared with (18)F-FDG. (99m)Tc-1-TG and (99m)Tc-5-TG showed a higher accumulation in the cell membranes compared with (18)F-FDG.


CONCLUSIONS
Tc-1-TG and (99m)Tc-5-TG showed an uptake in vitro with glucose analog characteristics but with membranous accumulation. Tumor imaging should be investigated in an animal model.
Klinik für Radiologie und Nuklearmedizin, Universitätsklinik Magdeburg, Leipziger Strasse 44, 39120, Magdeburg, Germany, max.seidensticker@med.ovgu.de.
M
M
Seidensticker
G
G
Ulrich
F L
FL
Muehlberg
A
A
Pethe
O S
OS
Grosser
I G
IG
Steffen
M
M
Stiebler
J
J
Goldschmidt
K H
KH
Smalla
R
R
Seidensticker
J
J
Ricke
H
H
Amthauer
K
K
Mohnike
D002451:Cell Compartmentation / Q000187:drug effects; D045744:Cell Line, Tumor; D003571:Cytochalasin B / Q000494:pharmacology; D019788:Fluorodeoxyglucose F18 / Q000493:pharmacokinetics*; D005947:Glucose / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D006801:Humans; D007328:Insulin / Q000378:metabolism; D010693:Phloretin / Q000494:pharmacology; D019275:Radiopharmaceuticals / Q000493:pharmacokinetics*; D013667:Technetium / Q000493:pharmacokinetics*; D013997:Time Factors
D007328:Insulin; D019275:Radiopharmaceuticals; D019788:Fluorodeoxyglucose F18; D003571:Cytochalasin B; C003002:5-thio-D-glucose; D013667:Technetium; C018399:1-thioglucose; D005947:Glucose; D010693:Phloretin