ROS production, cellular targets, and dark- and photo-toxicity data for selected Ru, Ir and Pt photosensitizersa.
Complex | Metal center | λ ir [nm] | Dose [J cm−2] | ROS/ΦΔ | IC50 [μM] | PI | Cell line | Cellular target | Cell death | Ref. | |
---|---|---|---|---|---|---|---|---|---|---|---|
Dark | Light | ||||||||||
Photofrin | — | 630 | 25 | — | — | ∼1.15 | — | ISOS-1 | — | Apo | 83 |
— | 635 | 80 | — | >574 | 57.4 | >10 | HepG2 | Mito | Apo | 84 | |
5 | Ru | 625 | 100 | 1O2 | 123 | 9.96 | 12 | SKME28 | Nuc | — | 21 |
143 | 126 | 1.1 | HL60 | ||||||||
6 | Ru | 635 | 1.8 | 1O2, 0.033, ˙OH | — | — | — | HeLa | — | — | 22 |
7 | Ru | 635 | 1.8 | 1O2, 0.058, ˙OH | — | — | — | HeLa | — | — | 22 |
9 | Ru | 595 | 11.2 | 1O2, 0.92 | >100 | 2.4 | >41.7 | CT-26 | Cyto | Apo | 24 |
12 | Ru | 450 | 18 | 1O2, 0.92 | 75.46 | 5.21 | 14.48 | HeLa (MCTs) | Mito | Apo | 25 |
810 | 800 | 108.56 | 5.71 | 19 | |||||||
13 | Ru | 450 | 18 | 1O2, 0.4 | 76.71 | 5.01 | 15.31 | HeLa (MCTs) | Mito | Apo | 25 |
110.36 | 5.45 | 20 | |||||||||
14 | Ru | 400–800 | 18 | 1O2, 0.14 | — | — | — | HeLa | — | Apo | 29 |
15 | Ru | 400–800 | 18 | 1O2, 0.16 | — | — | — | HeLa | — | Apo | 29 |
16 | Ru | 820 | 0.032 | 1O2, 0.87 | 72.9 | 3.3 | 22.1 | A549R | — | Apo | 34 |
17 | Ru | 450 | 12 | 1O2, 0.52 | 230 | 28 | 8.2 | U87MG (MCTs) | Mito | Apo | 35 |
820 | 3 | 216 | 34 | 6.4 | |||||||
216 | 9 | 24 | |||||||||
25 | Ru | 800 | 10 | 1O2, 0.99 | 470 | 1.1 | 313 | HeLa (MCTs) | Lyso | Nec | 45 |
>500 | 1.9 | 250 | |||||||||
28 | Ru | 660 | 60 | 1O2, ˙OH, O2−˙ | 43 | 3.1 | 13.9 | MCF7 | Lyso | Apo | 46 |
35 | Ir | 625 | 100 | 1O2, 0.56 | 3.27 | 0.2 | 16 | SKMEL28 | — | — | 59 |
36 | Ir | 405 | 12 | 1O2, 0.7 | 30.3 | 0.4 | 75 | HeLa (MCTs) | Mito | — | 60 |
730 | 38.6 | 0.35 | 110 | ||||||||
39 | Ir | 808 | 480 | 1O2, 0.15, ˙OH, O2−˙ | >100 | 14.4 | — | A549 | — | — | 61 |
41 | Ir | 420 | 28 | 1O2 < 0.01, O2−˙ | N:213 | N: 1.32 | 161 | HeLa | — | — | 62 |
H: 1.43 | 153 | ||||||||||
550 | 21 | H: 219 | N:2.51 | 85 | |||||||
H: 2.77 | 79 | ||||||||||
42 | Ir | N: 465 | N: 8.9 | 1O2, 0.71 | N: 16.6 | N: 1.0 | N: 16.6 | NCI–H460 | Mito | Apo | 63 |
H: 450 | H: 10.0 | H: 31.6 | H: 8.7 | H: 3.6 | |||||||
N: 35.4 | N: 1.9 | N: 18.6 | HeLa | ||||||||
H: 43.6 | H: 5.2 | H: 8.3 | |||||||||
N: 19.9 | N: 1.1 | N: 18.1 | SGC791 | ||||||||
H: 23.6 | H: 5.8 | H: 4.0 | |||||||||
N: > 50 | N:1.9 | N: >25 | Hep G2 | ||||||||
H: > 50 | H: 3.5 | H: > 14 | |||||||||
N: 43.6 | N: 1.6 | N: 27.2 | A549 | ||||||||
H: 42.5 | H: 2.3 | H: 18.5 | |||||||||
43 | Ir | 405 | 2.83 | 1O2, 0.68 | N: 69.4 | N: 3.8 | N: 18.4 | FaDu | Mito | Apo | 64 |
H: 79.6 | H: 18.1 | H: 4.4 | |||||||||
N: >100 | N: 8.7 | N: >11.5 | HT-29 | ||||||||
H: 96.2 | H: 28.6 | H: 3.4 | |||||||||
44 | Ir | 405 | 2.83 | 1O2, 0.08 | N: >100 | N: 5.4 | N: >18.5 | FaDu | Mito | Apo | 64 |
H: >100 | H: 12.8 | H: >7.8 | |||||||||
N: >100 | N: 12.0 | N: >8.3 | HT-29 | ||||||||
H: >100 | H: 24.2 | H: >4.3 | |||||||||
45 | Ir | 405 | 12 | 1O2, 0.79 | N:49.42 | N < 0.052 | N: >959 | A549 | Mito | Apo | 65 |
H: 41.42 | H: 0.06 | H: >690 | |||||||||
46 | Ir | 450 | 30 | 1O2, 0.81, ˙OH, O2−˙ | N: 20.48 | N: 0.51 | N: 40.39 | MCF-7 | — | Fer | 66 |
H: 17.41 | H: 1.74 | H: 10.01 | |||||||||
47 | Ir | 450 | 30 | 1O2, 0.76, ˙OH, O2−˙ | N: 15.26 | N: 0.20 | N: 74.81 | MCF-7 | Mito | Apo | 66 |
H: 14.76 | H: 0.41 | H: 36.27 | Fer | ||||||||
48 | Ir | 465 | 11.7 | 1O2, 0.76, O2−˙ | 63.8 | 0.37 | 172 | HepG2-SR | Mito–Lyso | Apo | 67 |
Nec | |||||||||||
49 | Ir | 405 | 6 | 1O2, 0.39 | >100 | 24.3 | >4.1 | A594 | ER | — | 54 |
50 | Ir | 405 | 6 | 1O2, 0.45 | 56.6 | 0.6 | 94.3 | A594 | ER | Apo | 54 |
51 | Ir | 405 | 6 | 1O2, 0.49 | 22.3 | 0.5 | 44.6 | A594 | ER | — | 54 |
52 | Ir | 465 | 5.76 | 1O2, 0.06 | 89.6 | 53.3 | 1.7 | A594 | Nuc | — | 68 |
53 | Ir | 465 | 5.76 | 1O2, 0.83 | 62.3 | 1.1 | 56.6 | A594 | Nuc | — | 68 |
54 | Pt | 720–740 | 9.45 | 1O2, 0.15 | 8.4 | 0.14 | 60 | C-33 A | Mito–Lyso | Apo | 75 |
18.2 | 0.65 | 28 | MCF-7 | ||||||||
55 | Pt | 425 | 36 | 1O2, 0.31 | 96.8 | 0.18 | 538 | A594 | Nuc | Apo | 76 |
56 | Pt | 425 | 36 | 1O2, 0.28 | 49.2 | 4.6 | 11 | A594 | Lyso | — | 76 |
57 | Pt | 520 | 6 | 1O2, 0.92 | — | — | — | HeLa | — | Apo | 77 |
58 | Pt | 600–720 | 30 | 1O2, 0.58 | 91.4 | 2.6 | 35.2 | HeLa | Mito | — | 79 |
>100 | 6.0 | >16.7 | A594 | ||||||||
>100 | 2.3 | >43.5 | MCF-7 | ||||||||
59 | Pt | 532 | 1 | 1O2, 0.13 | >50 | 4.1 | >12 | MCF-7 | Lyso–Nuc | — | 82 |
>50 | 5.8 | >8 | SGC791 | ||||||||
>50 | 3.8 | >13 | A594 |
Mito: mitochondria, Lyso: lysosome, Cyto: cytoplasm, Nuc: nucleus, ER: endoplasmic reticulum; Apo: apoptosis, Fer: ferroptosis, and Nec: necrosis.