Abstract:Candida albicans is an opportunistic pathogen that often causes skin infections such as oral thrush, nail fungus, athlete’s foot, and diaper rash. Under particular conditions, C. albicans alters the natural balance of the host microbiota, and as a result, the skin or its accessory structures lose their function and appearance. Conventional antimycotic drugs are highly toxic to host tissues, and long-lasting drug administration induces the arising of resistant strains that make the antimycotic therapy ineffecti… Show more
“…Moreover, the eukaryotic microorganism Candida albicans showed to be sensitive in the dark to most cationic and dicationic diaryl-porphyrins tested in this study, irrespective of Soret band height [32]. Cormick reported that tri-and tetracationic porphyrins were more tightly bound to C. albicans cells than anionic porphyrins, supporting the requirement of positive charge on porphyrins to promote the electrostatic interaction with the yeast cell wall [41].…”
Section: Discussionsupporting
confidence: 63%
“…A panel of novel diaryl-porphyrins, synthetized by our group and previously tested as antimicrobials [33] antifungals [32] and antitumorals [31,34], was investigated for anti-Pseudomonas activity (Table 1). The neutral and asymmetrical P1 and P2 bear in mesopositions (positions 5 and 15) a pentafluorophenyl group, associated with a C4 or C8 para-bromoalkyloxy-phenyl group, respectively.…”
Section: Panel Of Diaryl-porphyrinsmentioning
confidence: 99%
“…Among synthetic porphyrins, diaryl-porphyrins, bearing two substituents in two meso-positions, were shown to be efficient PSs both in antitumoral and in antifungal applications [31,32]. In the present study a panel of 5,15 meso-substituted diaryl-porphyrins was assayed for anti-biofilm activity.…”
In recent years, antimicrobial photodynamic therapy (aPDT) has received increasing attention as a promising tool aimed at both treating microbial infections and sanitizing environments. Since biofilm formation on biological and inert surfaces makes difficult the eradication of bacterial communities, further studies are needed to investigate such tricky issue. In this work, a panel of 13 diaryl-porphyrins (neutral, mono- and di-cationic) was taken in consideration to photoinactivate Pseudomonas aeruginosa. Among cationic photosensitizers (PSs) able to efficiently bind cells, in this study two dicationic showed to be intrinsically toxic and were ruled out by further investigations. In particular, the dicationic porphyrin (P11) that was not toxic, showed a better photoinactivation rate than monocationic in suspended cells. Furthermore, it was very efficient in inhibiting the biofilms produced by the model microorganism Pseudomonas aeruginosa PAO1 and by clinical strains derived from urinary tract infection and cystic fibrosis patients. Since P. aeruginosa represents a target very difficult to inactivate, this study confirms the potential of dicationic diaryl-porphyrins as photo-activated antimicrobials in different applicative fields, from clinical to environmental ones.
“…Moreover, the eukaryotic microorganism Candida albicans showed to be sensitive in the dark to most cationic and dicationic diaryl-porphyrins tested in this study, irrespective of Soret band height [32]. Cormick reported that tri-and tetracationic porphyrins were more tightly bound to C. albicans cells than anionic porphyrins, supporting the requirement of positive charge on porphyrins to promote the electrostatic interaction with the yeast cell wall [41].…”
Section: Discussionsupporting
confidence: 63%
“…A panel of novel diaryl-porphyrins, synthetized by our group and previously tested as antimicrobials [33] antifungals [32] and antitumorals [31,34], was investigated for anti-Pseudomonas activity (Table 1). The neutral and asymmetrical P1 and P2 bear in mesopositions (positions 5 and 15) a pentafluorophenyl group, associated with a C4 or C8 para-bromoalkyloxy-phenyl group, respectively.…”
Section: Panel Of Diaryl-porphyrinsmentioning
confidence: 99%
“…Among synthetic porphyrins, diaryl-porphyrins, bearing two substituents in two meso-positions, were shown to be efficient PSs both in antitumoral and in antifungal applications [31,32]. In the present study a panel of 5,15 meso-substituted diaryl-porphyrins was assayed for anti-biofilm activity.…”
In recent years, antimicrobial photodynamic therapy (aPDT) has received increasing attention as a promising tool aimed at both treating microbial infections and sanitizing environments. Since biofilm formation on biological and inert surfaces makes difficult the eradication of bacterial communities, further studies are needed to investigate such tricky issue. In this work, a panel of 13 diaryl-porphyrins (neutral, mono- and di-cationic) was taken in consideration to photoinactivate Pseudomonas aeruginosa. Among cationic photosensitizers (PSs) able to efficiently bind cells, in this study two dicationic showed to be intrinsically toxic and were ruled out by further investigations. In particular, the dicationic porphyrin (P11) that was not toxic, showed a better photoinactivation rate than monocationic in suspended cells. Furthermore, it was very efficient in inhibiting the biofilms produced by the model microorganism Pseudomonas aeruginosa PAO1 and by clinical strains derived from urinary tract infection and cystic fibrosis patients. Since P. aeruginosa represents a target very difficult to inactivate, this study confirms the potential of dicationic diaryl-porphyrins as photo-activated antimicrobials in different applicative fields, from clinical to environmental ones.
“…The 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay was performed on all the cell lines tested as previously described 52 with minor modifications. Briefly, according to the growth profiles previously defined for each cell line, adequate numbers of cells were plated in each well of a 96-well plate in 0.1 mL of complete culture medium.…”
The potential anticancer
effect of fluoroquinolone antibiotics
has been recently unveiled and related to their ability to interfere
with DNA topoisomerase II. We herein envisioned the design and synthesis
of novel Ciprofloxacin and Norfloxacin nitric oxide (NO) photo-donor
hybrids to explore the potential synergistic antitumor effect exerted
by the fluoroquinolone scaffold and NO eventually produced upon light
irradiation. Anticancer activity, evaluated on a panel of tumor cell
lines, showed encouraging results with IC
50
values in the
low micromolar range. Some compounds displayed intense antiproliferative
activity on triple-negative and doxorubicin-resistant breast cancer
cell lines, paving the way for their potential use to treat aggressive,
refractory and multidrug-resistant breast cancer. No significant additive
effect was observed on PC3 and DU145 cells following NO release. Conversely,
antimicrobial photodynamic experiments on both Gram-negative and Gram-positive
microorganisms displayed a significant killing rate in
Staphylococcus aureus
, accounting for their potential
effectiveness as selective antimicrobial photosensitizers.
“…After overnight incubation at 37 °C, coverslip glasses were irradiated under light at 520 nm for 2 h in a humid chamber. Upon irradiation, adherent cells were stained for 30 min with 2 μM fluorochrome 4,4-difluoro-1,3,5,7-tetramethyl-8-(2-methoxyphenyl)-4-bora-3a,4a-diaza-s-indacene [26]. Then, the coverslips were transferred on microscope glass slides for confocal microscopy analysis.…”
Section: Photoinactivation Induced By Micelle-coated Glassmentioning
Decontaminating coating systems (DCSs) represent a challenge against pathogenic bacteria that may colonize hospital surfaces, causing several important infections. In this respect, surface coatings comprising photosensitizers (PSs) are promising but still controversial for several limitations. PSs act through a mechanism of antimicrobial photodynamic inactivation (aPDI) due to formation of reactive oxygen species (ROS) after light irradiation. However, ROS are partially deactivated during their diffusion through a coating matrix; moreover, coatings should allow oxygen penetration that in contact with the activated PS would generate 1O2, an active specie against bacteria. In the attempt to circumvent such constraints, we report a spray DCS made of micelles loaded with a PS belonging to the BODIPY family (2,6-diiodo-1,3,5,7-tetramethyl-8-(2,6-dichlorophenyl)-4,4′-difluoroboradiazaindacene) that is released in a controlled manner and then activated outside the coating. For this aim, we synthesized several amphiphilic copolymers (mPEG–(PLA)n), which form micelles, and established the most stable supramolecular system in terms of critical micelle concentration (CMC) and ∆Gf values. We found that micelles obtained from mPEG–(PLLA)2 were the most thermodynamically stable and able to release BODIPY in a relatively short period of time (about 80% in 6 h). Interestingly, the BODIPY released showed excellent activity against Staphylococcus aureus even at micromolar concentrations.
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