Abstract
BackgroundOvarian cancer is a serious threat for women health and the early diagnosis of this cancer might improves the survival rate of patients. The use of the targeted radiopharmaceuticals could be a non-invasive and logical method for tumor imaging. The aim of this study was to radiolabel GE11 peptide as a new specific probe for imaging of ovarian tumor.MethodsHYNIC-SSS-GE11 peptide was labeled with 99mTc using tricine as a coligand. The 99mTc-tricine-HYNIC-SSS-GE11 peptide was evaluated for specific cellular binding in three cell lines with different levels of EGFR expression. Tumor targeting was assessed in SKOV3 tumor bearing mice.ResultsBy using tricine as a coligand, labeling yield was more than 98% and the stability of the radiolabelled peptide in human serum up to 4 h was 96%. The in vitro cell uptake test showed that this radiolabeled peptide had a good affinity to SKOV3 cells with dissociation constant of 73 nM. The in vivo results showed a tumor/muscle ratio of 3.2 at 4 h following injection of 99mTc-tricine-HYNIC-SSS-GE11 peptide.ConclusionsResults of this study showed that 99mTc-tricine-HYNIC-SSS-GE11 peptide could be a promising tool for diagnosis and staging of ovarian cancer.Graphical 99mTc-tricine-HYNIC-SSS-GE11, a novl targeted agent for ovarian tumor imaging
Highlights
Ovarian cancer is a serious threat for women health and the early diagnosis of this cancer might improves the survival rate of patients
Radiochemical purity (RCP) assessed by radio HPLC was found to be 97 and 95% at 1 and 4 h respectively, considering 1–2% reduced hydrolyzed technetium (Fig. 2a)
Experimental results showed acceptable radiochemical purity on the basis of the presence of a single radioactivity peak corresponding to 99 m-Technetium (99mTc)-HYNIC-SSS-GE11 with a retention time of 18–20 min
Summary
Ovarian cancer is a serious threat for women health and the early diagnosis of this cancer might improves the survival rate of patients. The use of the targeted radiopharmaceuticals could be a non-invasive and logical method for tumor imaging. The aim of this study was to radiolabel GE11 peptide as a new specific probe for imaging of ovarian tumor. Methods: HYNIC-SSS-GE11 peptide was labeled with 99mTc using tricine as a coligand. The 99mTc-tricine-HYNIC-SSS-GE11 peptide was evaluated for specific cellular binding in three cell lines with different levels of EGFR expression. Since the symptoms of the ovarian cancer in early stages are not clear, nearly 50% of patients are diagnosed in advanced stages (stage III/ IV) whereas patient are over 65 years old [1, 2]. Considering that ovarian cancer is frequently diagnosed at stage III or IV, a convenient screening method for early detection is highly desirable [3]. It has been shown that in approximately 70% of ovarian cancers there is an overexpression
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