Abstract
Thalidomide is a sedative drug discovered at the end of the 50s, it showed high anticancer activity so attempts were made to synthesize thalidomide analogs that had fewer side effects than the parent compound. DPDQA showed higher anticancer activities than thalidomide. Labeling of a DPDQA with 99mTc using Na2S2O4 as reducing agent was performed. The dependence of the radiolabeling yield on the concentrations of DPDQA and reducing agent, pH of the reaction mixture, reaction time, and reaction temperature was studied. Bio-distribution studies in mice with tumor induced in the right thigh were carried out. The tumor infected thigh/contralateral thigh uptake ratio (T/NT) was evaluated. The time for the maximum accumulation of the 99mTc–DPDQA in the tumor site was evaluated after administration of the compound.
Highlights
Molecular imaging is a well-defined technique which can visualize, characterize, and measure the biological processes at the molecular and cellular levels in humans and other living systems
The labeling yield and the in vitro stability of 99mTc– DPDQA complex were assessed by ascending paper chromatography (PC) to evaluate the percent of 99mTc– DPDQA, free 99mTcO4- and reduced hydrolyzed 99mTc colloid species as follows(Motaleb 2007; Hall et al 1998; Kashani, Cooper, and Das 2004)
A mixture of ethanol: water: ammonium hydroxide (2:5:1, v/v/v) as developing solvent to develop another paper strip where reduced hydrolyzed technetium colloid remained at the origin (Rf = 0) while free 99mTcO4- and 99mTc– DPDQA species migrated with the solvent front (Rf = 1)
Summary
Molecular imaging is a well-defined technique which can visualize, characterize, and measure the biological processes at the molecular and cellular levels in humans and other living systems. The development of tumor-sensitive radiotracer markers for noninvasive nuclear medicine imaging will allow hypoxic tumors to be revealed in early stages. Among such markers are 99mTc-citrofolate (Altiparmak et al 2010), 99mTc-N2S2-Tat(49–57)-bombesin (Santos-Cuevas et al 2009) 18F fluoromisonidazole (FMISO) (Rasey et al 1996; Rischin et al 2006), 123Iiodoazomycin arabinoside (IAZA) (Parliament et al 1992), 99mTc-bombesin (de Barros et al 2013), and 99mTc-meropenem (Sakr, Motaleb, and Ibrahim 2012). Due to the excellent physical properties of 99mTc (ideal half-life of 6.02 h and ideal γ-ray energy of 140 keV and to its low cost and good availability, researchers interest in 99mTc-labeled compounds as hypoxic tumor radiotracer markers increases (Dilworth and Parrott 1998; Jurisson and Lydon 1999). Followed by its preclinical biological evaluation in male mice models
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