Figures
Release of the SN38 drug
from FA-GFLG-SN38 promoted by CTSB. (A)
Images of different solutions (a, SN38; b, FA-GFLG-SN38; c, FA-GFLG-SN38
with CTSB; d, FA-GFLG-SN38 with CTSB and CA-074 Me) under (left) visible-light
and (right) UV irradiation. (B) Release of SN38 from FA-GFLG-SN38
monitored using a fluorometer (λex = 365 nm, λem = 540 nm). (C) Release of SN38 from FA-GFLG-SN38 in the
presence of CTSB monitored using RP-HPLC (detection at 254 nm) and
mass spectrometry (a, FA-GFLG-SN38; b, FA-linker-Gly-Phe-OH ([M +
Na]+m/z = 1114.7); c,
SN38).
Fluorescence imaging of cells treated
with FA-Rho. (a–c)
SK-Hep-1 cancer cells were incubated with (a) 5 μM FA-Rho for
24 h, (b) 3 mM FA for 1 h and then 5 μM FA-Rho for 24 h, and
(c) 20 μM CA-074 Me for 24 h and then 5 μM FA-Rho for
24 h. (d) A549 cancer cells were incubated with 5 μM FA-Rho
for 24 h. (e) 16-HBE normal cells were incubated with 5 μM FA-Rho
for 24 h. Hoechst 33342 (1 μg/mL) was used to stain the nuclei.
The incubated cells were imaged with confocal microscopy.
Fluorescence imaging of cells treated with FA-GFLG-SN38.
(a–c)
SK-Hep-1 cancer cells were incubated with (a) 5 μM FA-GFLG-SN38
for 24 h, (b) 3 mM FA for 1 h and then 5 μM FA-GFLG-SN38 for
24 h, and (c) 20 μM CA-074 Me for 24 h and then 5 μM FA-GFLG-SN38
for 24 h. (d) A549 cancer cells were incubated with 5 μM FA-GFLG-SN38
for 24 h. (e) 16-HBE normal cells were incubated with 5 μM FA-GFLG-SN38
for 24 h. Hoechst 33342 (1 μg/mL) was used to stain the nuclei.
The incubated cells were imaged with confocal microscopy.
Cancer and 16-HBE cells were incubated
with various concentrations
of (A) FA-GFLG-SN38 or (B) free SN38 for 72 h. Cell viability was
measured with the MTT assay.
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