Fig 1.
Overview of the synthesized unlabeled compounds, radiolabeling procedures and the nomenclature of the 99mTc-radiolabeled pyrene derivatives (M = 99mTc/99Tc).
Fig 2.
Representative radio-HPLC chromatogram of [99mTc]Ib after radiolabeling and purification by HPLC; radioactive peak is shown at tR = 11.3 min with RCP = 97% (HPLC-gradient: 5/95% A/B to 95/5% A/B within 11 min; A: H2O (0.05% TFA) B: acetonitrile (0.05% TFA).
Table 1.
Summary of HPLC retention times (tR) of chelators 4, 8a, 8b, 9 and the radiolabeled pyrene derivatives [99mTc]Ia, [99mTc]Ib, [99mTc]II, [99mTc]III in comparison with [99mTc(CO)3(H2O)3]+ and 99mTcO4– as references.
Fig 3.
Representative agarose gel of supercoiled (SC) pUC 19 plasmid DNA incubated with various activities of [99mTc]Ib and [99mTc]III in presence of DMSO (0.2 M).
Lane C is the control pUC 19 plasmid DNA (SC) and lane L is the linear control pUC 19 plasmid DNA (L). OC represent open circular conformation of pUC 19 plasmid DNA. Lanes 1–5 show pUC 19 plasmid DNA incubated with [99mTc]Ib (3–15 MBq). Lanes 6–10 show pUC 19 plasmid DNA incubated with [99mTc]III (3–15 MBq).
Table 2.
Summary of quantitative analysis of the fractions of OC (SSB) and L (DSB) caused by incubation of 15 MBq [99mTc]Ia, [99mTc]Ib, [99mTc]II, [99mTc]III, and 99mTcO4– in absence (–) and presence (+) of 0.2 M DMSO.
Table 3.
Calculation of the average yields of SSB and DSB per plasmid molecule and per decay (YSSB and YDSB) of 99mTc by incubation of 15 MBq [99mTc]Ia, [99mTc]Ib, [99mTc]II, [99mTc]III, and 99mTcO4– in absence (–) and presence (+) of 0.2 M DMSO.
Fig 4.
Quantitative analysis of agarose gel electrophoresis for determination of decreasing SC plasmid fraction in absence (–) and presence (+) of 0.2 M DMSO.
Incubation of pUC 19 plasmid DNA with 3–15 MBq of [99mTc]Ib and [99mTc]II, and 99mTcO4– for 24 h at room temperature.
Table 4.
Overview of the detected OC (SSB) and L (DSB) plasmid fractions regarding to the radical scavenging qualities of the 99Tc-labeled pyrene derivatives [99Tc]Ia, [99Tc]Ib, [99Tc]II, and [99Tc]III in comparison to 0.2 M DMSO.
Incubation of pUC 19 plasmid DNA with 3 MBq 99mTcO4– and 3 MBq equivalent amount of the respective 99Tc-labeled pyrene derivative as well as 15 MBq 99mTcO4– and 15 MBq equivalent amount of the respective 99Tc-labeled pyrene derivative.
Fig 5.
Quantitative analysis of agarose gel electrophoresis for determination of single-strand breaks and double-strand breaks by plotting open circular (OC) and linear (L) plasmid fractions in absence of 0.2 M DMSO.
Incubation of pUC 19 plasmid DNA with 3–15 MBq of [99mTc]Ia, [99mTc]Ib, [99mTc]II, [99mTc]III, and 99mTcO4– reference for 24 h at room temperature.
Fig 6.
Quantitative analysis of agarose gel electrophoresis for quantification of single-strand breaks and double-strand brekas by plotting open circular (OC) and linear (L) plasmid fractions in presence of 0.2 M DMSO.
PUC 19 plasmid DNA was incubated with [99mTc]Ia, [99mTc]Ib, [99mTc]II, [99mTc]III, and 3–15 MBq 99mTcO4– as reference.
Fig 7.
Examples of conformations of Tc-complexes Ia, Ib, II, and III in presence of DNA.
(A) Ia, hook-like conformation, (B) Ia, extended conformation, (C) Ib, (D) II, twisted conformation, (E) II, extended conformation, (F) III, twisted conformation, (G) III, extended conformation.