New vanadium-based magnetic resonance imaging probes: clinical potential for early detection of cancer

摘要: We have developed a magnetic resonance imaging (MRI) method for improved detection of cancer with new class cancer-specific contrast agents, containing vanadyl (VO2+)-chelated organic ligands, specifically bis(acetylacetonato)oxovanadium(IV) [VO(acac)2]. Vanadyl compounds been found to accumulate within cells, where they interact intracellular glycolytic enzymes. Aggressive cancers are metabolically active and highly glycolytic; an MRI agent that enters cells high activity could provide high-resolution functional images tumor boundaries internal structure, which cannot be achieved by conventional agents. The present work demonstrates properties VO(acac)2 may give it excellent specificity detection. A dose did not cause any acute or short-term adverse reactions in murine subjects. Calorimetry spectrofluorometric methods demonstrate is blood pool binds serum albumin dissociation constant Kd ~ 2.5 ± 0.7 × 10−7 M binding stoichiometry n = 1.03 0.04. Owing its prolonged half-life selective leakage from hyperpermeable vasculature, low (0.15 mmol/kg) selectively enhanced vivo tumors, providing their interior structure. kinetics uptake washout consistent the hypothesis preferentially accumulates cells. Although has lower relaxivity than gadolinium-based lead innovative approach since potential produce agents nontoxic sensitive metabolism.