Effects of 2-methoxyestradiol on proliferation, apoptosis and PET-tracer uptake in human prostate cancer cell aggregates

• The purpose of this study was to investigate the potential use of PET in vivo to record cytotoxic effects of 2-methoxyestradiol (2-ME), an endogenous metabolite of 17beta-estradiol. The anti-proliferative and pro-apoptotic effects of 2-ME on human prostate cancer cell (PC3) aggregates in vitro, were correlated with the uptake of fluoro-deoxy-D-glucose, FMAU and choline labelled with 18F, 11C, or 3H. 2-ME clearly reduced growth of PC3 aggregates and induced apoptosis in a dose-dependent manner. However, the uptake of the putative proliferation markers 11C-FMAU or 3H-choline failed to record the growth inhibitory effects of 2-ME on PC3 cell aggregates. The uptake of 18F-FDG was used as a marker for effects on cellular metabolism and also failed to show any dose-dependent effects in PC3 aggregates. The use of these PET-tracers in vivo is therefore not recommended in order to evaluate the cytotoxic effects of 2-ME on human prostate cancer cells.

Nyckelord

Antineoplastic Agents/administration & dosage

Apoptosis/*drug effects

Cell Aggregation/drug effects

Cell Line; Tumor

Cell Proliferation/*drug effects

Comparative Study

Dose-Response Relationship; Drug

Estradiol/*administration & dosage/*analogs & derivatives

Humans

Male

Neoplasm Staging/methods

Positron-Emission Tomography/*methods

Prostatic Neoplasms/drug therapy/*metabolism/pathology/*radionuclide imaging

Radioisotopes/*diagnostic use/*pharmacokinetics

Radiopharmaceuticals/diagnostic use/pharmacokinetics

Reproducibility of Results

Research Support; Non-U.S. Gov't

Sensitivity and Specificity

Publikations- och innehållstyp

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