Table 4.
Chemical properties and biological activity of photosensitizers used in vivo/ex vivo pre-clinical studies for treatment of infections by Gram-positive bacteria
| # | Structure | Model | Results |
|---|---|---|---|
| 1 |
ZnPc-(Lys)5 (PS26) Charge: 0 to + 5 (pH dependent) MW = 1272 Da |
In vivo: Sprague–Dawley rats with wound infected by S. aureus Xen29 [159] |
Outcome: 0.7 log CFU reduction [PS]: 1 µM Light dose: 15 J/cm2 (LED λ = 680 nm) |
| 2 |
Arg–Arg–ArgPc (PS27) Charge: 0 to + 6 MW = 1924 Da |
In vivo: adult KM mice infected by S. aureus [160] |
Outcome: 1.6 log CFU reduction [PS]: 50 µM Light dose: 30 J/cm2 (500 W halogen lamp with filter λ > 610 nm) |
| 3 |
RLP068 (PS28) Charge: + 4 MW = 1257 Da |
In vivo: BALB⁄c mice with wound infected by MRSA ATCC 43300 [161] |
Outcome: ~ 3 log CFU reduction in 2nd day after treatment [PS]: 2 mM Light dose: 60 J/cm2 (Laser λ = 698 nm) |
| 4 |
Sinoporphyrin sodium (PS29) Charge: − 4 MW = 1231 Da |
In vivo: female BALB/c mice (5–6 weeks) with burn wound infection by MDR S. aureus ATCC 29213 [162] |
Outcome: 1 log CFU reduction in 1st and 2nd days; 3 log in in 3rd day after treatment [PS]: 20 µM Light dose: 50 J/cm2 (Laser λ = 635 nm) |
| 5 |
5-ALA: protoporphyrin IX precursor (PS9a) Charge: 0 MW = 131 Da |
In vivo: male C57BL/ksj db/db mice with ulcers infected with S. aureus MRSA ATCC 33591 [163] |
Outcome: 2 log CFU reduction, 7 days after treatment [PS]: 200 mg/kg (1.5 mmol/kg) Light dose: 50 J/cm2 (LED λ = 410 nm) |
| 6 | In vivo: Sprague–Dawley rats CD osteomyelitis model with S. aureus Xen29 [164] |
Outcome: qualitative inhibition of biofilm formation in bone [PS]: 300 mg/kg (2.3 mmol/kg) Light dose: 75 J/cm2 (LEDs λ = 640 ± 40 nm) |
|
| 7 |
Chlorin e6 (PS7) Charge: − 3 MW = 597 Da |
In vivo: male BALB/c mice (6 weeks) with subcutaneous infection by S. aureus NCTC8532 [165] |
Outcome: complete reduction of infection after 5 days [PS]: 10 mg/kg (16 µmol/kg) Light dose: 100 J/cm2 (Laser λ = 664 nm) |
| 8 |
Chlorin e6- polyethylenimine conjugate (PS30) Charge: positive MW = 10,000–25,000 Da |
In vivo: female BALB/c mice wound infected with MRSA Xen31 [166] |
Outcome: 2.7 log CFU reduction [PS]: 400 µM Light dose: 360 J/cm2 (Light λ = 660 ± 15 nm) |
| 9 |
Photogem (PS31) Charge: − 2 to − 12 MW = n.d. |
In vivo: Mongolian Gerbils with otitis caused by S. pneumonia ATCC 27336 [167] |
Outcome: complete reduction of S. pneumonia in 87.5% of infections [PS]: 1 mg/ml (20 μl) Light dose: n.d. total energy: 90 J (Laser λ = 632 nm) |
| 10 |
PTMPP (PS32) Charge: + 3 MW = 663 Da |
In vivo: male BALB/c with third degree burns infected with S. aureus 8325–4 [168] |
Outcome: 1.7 log CFU reduction (7th day) [PS]: 500 µM Light dose: 210 J/cm2 (Light λ = 635 ± 15 nm) |
| 11 |
Indocyanine green (PS33) Charge: − 2 MW = 775 Da |
In vivo: rat abrasion wound model infected with MDR S. aureus (clinical isolate) [169] |
Outcome: 1 log CFU reduction [PS]: 1.2 mM Light dose: 450 J/cm2 (Laser λ = 808 nm) |
| 12 |
Hypericin (in nanoparticle formulation) (PS12) Charge: 0 MW = 504 Da |
In vivo: female Wistar rats with wounds infected by MRSA ATCC 6538 [170] |
Outcome: disappearance of infection 10 days after treatment [PS]: 0.124 μM Light dose: 23.5 J/cm2 (Halogen lamps 20 W) |
| 13 |
Y1 (PS34) Charge: − 1 MW = 432 Da |
In vivo: adult male ICR mice with skin infection by MRSA [171] |
Outcome: 3 log CFU reduction (7th day) [PS]: 2.5 µM Light dose: 30 J/cm2 (laser λ = 532 nm) |
| 14 |
Curcumin (PS14) Charge: 0 MW = 368 Da |
In vivo: female Balb/C mice infected in the right ear with S. aureus ATCC 43300 [172] |
Outcome: 2 log CFU reduction on the draining lymph node 72 h after treatment [PS]: 40 mM Light dose: 54 J/cm2 (Light λ = 450 ± 20 nm) |
| 15 | In vivo: male Wistar rats with infection by S. aureus ATCC 25923 [173] |
Outcome: 2 log CFU reduction after treatment [PS]: 1.5% gel (60 µl) Light dose: 60 J/cm2 (light λ = 450 ± 30 nm) |
|
| 16 |
Methylene blue (PS18) Charge: + 1 MW = 284 Da |
Ex vivo: human skin infected with MRSA ATCC 33592 [174] |
Outcome: 5.1 log CFU reduction (immediately); 5.9 log reduction (after 24 h) [PS]: 31 µM Light dose: 96 J/cm2 (laser λ = 670 nm) |
| 17 |
SAPYR (PS16) Charge: + 1 MW = 272 Da |
Ex vivo: human skin colonized by S. aureus MRSA ATCC BAA-44 [175] |
Outcome: 4 log CFU reduction [PS]: 100 µM Light dose: 60 J/cm2 (light λ = 380–480 nm) |
| 18 |
SACUR-3 (PS35) Charge: + 4 MW = 517 Da |
Ex vivo: porcine skin infected with S. aureus ATCC 25923 [176] |
Outcome: 2 log CFU reduction [PS]: 100 μM Light dose: 34 J/cm2 (LED λ = 435 ± 10 nm) |
