Table 1. Cytotoxicity of Ru-RGD Conjugatesa,b,c,d.
Λ-[1]Cl2 |
Δ-[1]Cl2 |
cisplatin |
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---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
cell lines | % O2 | EC50,dark (μM) | CI95 (μM) | EC50,light (μM) | CI95 (μM) | PI | EC50,dark (μM) | CI95 (μM) | EC50,light (μM) | CI95 (μM) | PI | EC50,dark (μM) | CI95 (μM) | EC50,light (μM) | CI95 (μM) |
A549 | 21 | 66.8 | –7.9 | 5.0 | –0.4 | 13 | 72.5 | - | 4.3 | –0.2 | 17 | 2.3 | –0.2 | 2.4 | –0.3 |
+5.5 | +0.4 | +48.2 | +0.2 | +0.3 | +0.3 | ||||||||||
1 | 51.0 | –2.4 | 19.0 | –2.4 | 2.7 | 50.1 | - | 17.3 | –3.9 | 2.9 | 6.5 | –1.5 | 6.3 | –1.3 | |
+3.0 | +2.1 | + | +3.1 | +2.0 | +1.7 | ||||||||||
U87MG | 21 | 41.6 | –8.9 | 3.8 | –0.8 | 12 | 39.5 | –8.6 | 3.6 | –0.4 | 11 | 2.8 | –0.4 | 4.0 | –0.5 |
+16 | +0.8 | +6.6 | +0.3 | +0.4 | +0.6 | ||||||||||
1 | 41.4 | –1.7 | 19.0 | –1.5 | 2.2 | 42.7 | –5.0 | 18.8 | –0.9 | 2.3 | 13.0 | –1.2 | 12.5 | –1.1 | |
+6.6 | +1.7 | +7.0 | +1.0 | +1.3 | +1.2 | ||||||||||
PC-3 | 21 | 66.6 | - | 5.3 | –1.1 | 12 | 52.0 | - | 6.0 | –1.3 | 9 | 4.5 | –0.8 | 4.1 | –0.9 |
+>50 | +1.5 | + | +1.9 | +1.0 | +1.1 | ||||||||||
1 | 74.3 | - | 46.5 | –6.8 | 1.5 | 61.4 | - | 50.7 | –7.1 | 1.2 | 23.1 | –3.8 | 25.8 | –3.2 | |
+>50 | +11 | +>50 | +13 | +4.9 | +3.8 | ||||||||||
U87MG spheroids | 21 | 37.0 | –4.4 | 7.6 | –1.3 | 4.9 | 46.0 | –3.1 | 10.9 | –2.2 | 4.2 | 8.6 | –2.9 | 7.9 | –2.2 |
+4.5 | +1.4 | +3.3 | +2.6 | +3.9 | +2.7 |
Half-maximal effective concentrations (EC50 in μM, n = 3) and 95% confidence intervals (CI95 in μM) for Λ-[1]Cl2, Δ-[1]Cl2, and cisplatin in the dark or upon green light irradiation in 2D monolayers of A549, U87MG, and PC-3 cell lines under normoxic (21% O2) and hypoxic (1% O2) conditions and three-dimensional (3D) spheroids of U87MG under normoxia (21%).
PI = photoindexes, defined as (EC50,dark/EC50,light).
Irradiation condition: normoxia 520 nm, 10.9 mW/cm2, 13.1 J/cm2, 20 min; hypoxia 520 nm, 7.22 mW/cm2, 13.1 J/cm2, 30 min.
Cancer cells were treated for 24 h in the dark and were not washed before or after irradiation.