Synthesis of 99mTc-cationic steroid antimicrobial-107 and in vitro evaluation |
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| Authors: | Rizwana Zahoor Samina Roohi Mushtaq Ahmad Zafar Iqbal Nagina Amir Saima Tariq Paul B Savage |
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| Institution: | 1. Isotope Production Division, Pakistan Institute of Nuclear Science and Technology, P.O. Nilore, Islamabad, 45650, Pakistan
2. Department of Chemistry and Biochemistry, Brigham Young University, C100BNSN, Provo, UT, 84602, USA
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| Abstract: | Ceragenins/cationic steroid antimicrobials (CSAs) are a group of cholic acid derivatives with many properties that make them favourable for application as anti-infective agents. CSA-107 is also a member of this group that was labelled with 99mTc by using SnCl2·2H2O as reducing agent and Na–K tartrate as transchelating agent. Labelling efficiency was optimized by varying the amount of reducing agent, pH, and time of incubation. Labelling efficiency and the stability of 99mTc-CSA-107 in human serum was determined by paper and thin layer chromatography, which were >95 and >90 % respectively. In vitro binding of 99mTc-CSA-107 was >95 % determined by using Staphylococcus aureus bacteria. |
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