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Model Amphipathic Peptides 85
relative caspase-8 activity
FIGURE 4.10 Relative caspase-8 activity induced in ECV-304 cells after incubation with
0.5 µM I, I tagged N or C terminally with SLV, XV tagged C terminally with SLV or with
SLV-NH 2 for 120 min at 37°C. Each bar represents the mean of three experiments ± S.E.M.
relative MTT-activity
180,0
160,0
140,0
120,0
100,0
80,0
60,0
40,0
20,0
0,0
-20,0
120
100
80
60
40
20
0
I SLV-NH2 SLV-NH-I I-SLV-NH2 XV-SLV-NH2
control amanitin I amanitin-S-S-I amanitin-SS-XV
FIGURE 4.11 Relative viability of LKB Ez 7 cells determined by the MTT-method 55 after
incubation with 1 µM α-amanitin, I and disulfide-bridged constructs of amanitin and I or XV
for 48 h at 37°C. The peptides were administered twice, at 0 and 24 h. Each bar represents
the mean of three experiments ± S.E.M.
Extensive and comparable translocation into the cell interior was also found for
the oligonucleotide conjugates with MAPs and the Antennapedia peptide when
phosphorothioate oligonucleotides were used as the cargo molecule. 45 Surprisingly,
no improvement with respect to the cellular uptake of naked oligonucleotides was
observed (Figure 4.12); however, the opposite, an inhibiting effect of the peptide
moiety on the membrane permeation of the oligonucleotide dependent on cell type