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Favorable Biokinetic and Tumor-Targeting Properties of ^99mTc-Labeled Glucosamino RGD and Effect of Paclitaxel Therapy

¹ Department of Nuclear Medicine, Samsung Medical Center, Sungkyunkwan University School of Medicine, Seoul, Korea; and ² Department of Chemistry, Inha University, Inchun, Korea

View larger version (11K): [in this window] [in a new window]   FIGURE 1.  (A) Schematic structure of glucosamino 99mTc-D-c(RGDfK). (B) Competitive binding of glucosamino 99mTc-D-c(RGDfK) to human umbilical endothelial cells. Cell-binding levels are expressed as percentage relative to that in absence of nonradiolabeled cRGDyV. Results are mean ± SD of triplicate samples obtained from single experiment representative of 2 separate experiments. **P < 0.05 compared with controls. ***P < 0.001 compared with controls.

View larger version (12K): [in this window] [in a new window]   FIGURE 2.  Inhibition study of tumor glucosamino 99mTc-D-c(RGDfK) accumulation. LLC- and RR1022 fibrosarcoma–bearing mice that received intravenous injection of glucosamino 99mTc-D-c(RGDfK) in absence or presence of excess nonradiolabeled cRGDyV were sacrificed 4 h later and measured for blood, muscle, and tumor uptake. Data are shown as mean ± SD of 5 and 2 animals per each carcinoma and sarcoma group, respectively. *P < 0.05 compared with corresponding uninhibited group. **P < 0.005 compared with corresponding uninhibited group.

View larger version (14K): [in this window] [in a new window]   FIGURE 3.  Comparison of biokinetic characteristics. Uptake levels of 125I-c(RGD(I)yV) (A and C) and glucosamino 99mTc-D-c(RGDfK) (B and D) in major organs at 1 and 4 h after coinjection into same RR1022 sarcoma–bearing nude mice. Data are shown as mean ± SD of 3 animals. *P < 0.05 compared with 125I-c(RGD(I)yV). **P < 0.01 compared with 125I-c(RGD(I)yV). ***P < 0.001 compared with 125I-c(RGD(I)yV).

View larger version (72K): [in this window] [in a new window]   FIGURE 4.  Scintigraphic pinhole images of tumor-bearing mice. (A) RR1022 fibrosarcoma and LLC tumors on right flank of BALB/C nude mice and C57Bl6 mice are clearly visualized after intravenous injection with glucosamino 99mTc-D-c(RGDfK). (B) RR1022 fibrosarcoma–bearing mice demonstrate appreciably reduced tumor visualization at 4 h when radiotracer is coinjected with nonradiolabeled cRGDyV.

View larger version (9K): [in this window] [in a new window]   FIGURE 5.  Effect of paclitaxel therapy. (A) Relative tumor volume of LLC during repeated administration of 0, 20, or 40 mg of paclitaxel per kilogram. Data are mean ± SD of measurements obtained from 7 animals per group. Tumor volume was calculated from caliper measurements of length and width of masses: volume (mm3) = length x width2 x . Relative tumor volume was calculated as volume at a given time divided by volume on second day after initiation of treatment. *P < 0.05 compared with control group. **P < 0.01 compared with control group. (B) Tumor uptake of glucosamino 99mTc-D-c(RGDfK) at 4 h on day 14 of paclitaxel therapy. Data are expressed as mean ± SD of %ID/g obtained from 7 animals per group. *P < 0.05 compared with control group. (C) Correlation between tumor glucosamino 99mTc-D-c(RGDfK) uptake expressed as %ID/g and v integrin levels on day 14 of paclitaxel therapy. v integrin levels were measured by Western blot of protein from homogenized tumor tissue using anti-v antibody and chemiluminescence system. Protein band intensities were measured by a calibrated densitometer and quantification software and are expressed in arbitrary units.