Fig. 5 | Nature Communications

Fig. 5

From: Synergistic enzymatic and bioorthogonal reactions for selective prodrug activation in living systems

Fig. 5

Biodistribution of self-assemblies and in vivo prodrug activation to inhibit tumour growth. a, b SPECT/CT imaging demonstrated the distribution of 2 at different time points after i.v. administration of a a mixture of 50 mg kg−1 2 and 0.875 mg kg−1 125I-labelled 2 (700 μCi) and b 0.875 mg kg−1 125I-labelled 2 (700 μCi) alone. Tumour sites are highlighted by white circles. Scale bars, 5 mm. c UPLC-MS/MS analysis of the pharmacokinetics of 2 and 3 in the tumour, liver and plasma after i.v. injection of 50 mg kg−1 2 (n = 5). The results demonstrated the selective accumulation of 3 in tumours over liver or plasma. d UPLC-MS/MS analysis of activated Dox in tumour, liver and plasma after treatment [i.v. injection of 50 mg kg−1 2 followed by i.v. injection of 30 mg kg−1 TCO-Dox after a 2-h interval] (n = 5). The results demonstrated the effective enrichment of activated Dox in tumours over liver or plasma. e Tumour growth curves for mice after i.v. injection with saline, 50 mg kg−1 2, 30 mg kg−1 TCO-Dox, 5 mg kg−1 Dox and 50 mg kg−1 2–2 h-30 mg kg−1 TCO-Dox (n = 8). The arrows on the x-axis indicate treatment duration in days. f Quantification of mouse weights in each group of (e). Error bars indicate standard deviation. g Photograph of dissected tumour samples after treatment for 14 days. Scale bar, 10 mm. h Representative histological examination results of the dissected tumours using HE staining. Scale bar, 50 μm

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