Radiosynthesis and in vitro evaluation of 99mTc(CO)3-labeled folic acid derivative |
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Authors: | Drishty Satpati Archana Mukherjee Meera Venkatesh and Sharmila Banerjee |
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Institution: | (1) Radiopharmaceuticals Division, Bhabha Atomic Research Centre, Mumbai, 400085, India; |
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Abstract: | The over-expression of folate receptors in variety of neoplastic tissues makes radiolabeled folate conjugates potential agents
for imaging and therapy of such cancers. With the aim of preparing an imaging agent for targeting folate receptors, folic
acid has been conjugated with homocysteine for complexation with 99mTc(CO)3(H2O)3]+ core. The radiolabeled complex of the homocysteine-folate could be obtained in >95% radiochemical yield as observed by HPLC.
Stability of complex in saline was studied and challenge studies with histidine and cysteine revealed kinetic stability of
the complex. Lipophilicity of the radiolabeled complex (log P) was found to be 0.45. In vitro uptake of 99mTc(CO)3-labeled folic acid derivative was studied in KB cells and inhibition studies were carried out using 3H-folic acid and cold homocysteine–folate conjugate. The in vitro studies indicated loss of binding affinity of the derivative
towards folate receptors. |
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