Ruthenium(II) Polypyridyl Complexes as Photosensitizers for Antibacterial Photodynamic Therapy: A Structure-Activity Study on Clinical Bacterial Strains

ChemMedChem ◽  
2018 ◽  
Vol 13 (20) ◽  
pp. 2229-2239 ◽  
Author(s):  
Tony Le Gall ◽  
Gilles Lemercier ◽  
Sylviane Chevreux ◽  
Katrin-Stephanie Tücking ◽  
Julian Ravel ◽  
...  
2019 ◽  
Vol 2019 ◽  
pp. 1-13 ◽  
Author(s):  
M. Atif ◽  
Seemab Iqbal ◽  
M. Fakhar-E-Alam ◽  
M. Ismail ◽  
Qaisar Mansoor ◽  
...  

In this experimental approach, we explored the structures, morphologies, phototoxicities, and antibacterial activities of undoped and Mn-doped ceria nanocomposite materials, MnxCe1−xO2. The MnxCe1−xO2 nanocomposites were synthesized by employing a soft chemical route. Our prime focus was on the influence of different factors, both physical and chemical, i.e., the concentration of manganese in the product, size of the nanocomposite, drug dose, and incubation time, on the bacterial strains. Different bacterial strains were selected as experimental biological models of the antibacterial activity of the manganese-doped cerium oxide nanocomposite. In addition to the photodynamic response, the adenocarcinoma cell line (MCF-7) was also studied. Based on cell viability losses and bacterial inhibition analyses, the precise mechanisms of apoptosis or necrosis of 5-ALA/PpIX-exposed MCF-7 cells under 630 nm red lights and under dark conditions were elucidated. It was observed that the undoped nanocomposites had lower cytotoxicities and inhibitions compared with those of the doped nanocomposites towards pathogens. The antibacterial activity and effectiveness for photodynamic therapy were enhanced in the presence of the manganese-doped ceria nanocomposite, which could be attributed to the correlation of the maximum reactive oxygen species generation for targeted toxicity and maximum antioxidant property in bacteria growth inhibition. The optimized cell viability dose and doping concentration will be beneficial for treating cancer and bacterial infections in the future.


2019 ◽  
Vol 25 (45) ◽  
pp. 10606-10615 ◽  
Author(s):  
Luca Conti ◽  
Andrea Bencini ◽  
Camilla Ferrante ◽  
Cristina Gellini ◽  
Paolo Paoli ◽  
...  

2017 ◽  
Vol 46 (2) ◽  
pp. 445-454 ◽  
Author(s):  
Jing Yang ◽  
Qian Cao ◽  
Wei-Liang Hu ◽  
Rui-Rong Ye ◽  
Liang He ◽  
...  

New TEMPO-functionalized Ru(ii) polypyridyl complexes displayed greatly improved PDT efficacy, capable of simultaneously monitoring cellular oxidative stress during photodynamic therapy.


Molecules ◽  
2018 ◽  
Vol 23 (12) ◽  
pp. 3320 ◽  
Author(s):  
Kai-Yi Wang ◽  
Zhi-Wen Zhou ◽  
Heng-Yuan Zhang ◽  
Yu-Cheng Cao ◽  
Jin-Yi Xu ◽  
...  

Antibiotic resistance has become a serious global problem that threatens public health. In our previous work, we found that ocotillol-type triterpenoid saponin showed good antibacterial activity. Based on preliminary structure-activity relationship, novel serious C-3 substituted ocotillol-type derivatives 7–26 were designed and synthesized. The in vitro antibacterial activity was tested on five bacterial strains (B. subtilis 168, S. aureus RN4220, E. coli DH5α, A. baum ATCC19606 and MRSA USA300) and compared with the tests on contrast. Among these derivatives, C-3 position free hydroxyl substituted compounds 7–14, showed good antibacterial activity against Gram-positive bacteria. Furthermore, compound 22 exhibited excellent antibacterial activity with minimum inhibitory concentrations (MIC) values of 2 μg/mL against MRSA USA300 and 4 μg/mL against B. subtilis. The structure-activity relationships of all current ocotillol-type derivatives our team synthesised were summarized. In addition, the prediction of absorption, distribution, metabolism, and excretion (ADME) properties and the study of pharmacophores were also conducted. These results can provide a guide to further design and synthesis works.


Pharmaceutics ◽  
2020 ◽  
Vol 12 (10) ◽  
pp. 961
Author(s):  
Nancy Soliman ◽  
Vincent Sol ◽  
Tan-Sothea Ouk ◽  
Christophe M. Thomas ◽  
Gilles Gasser

Antimicrobial photodynamic therapy (aPDT) also known as photodynamic inactivation (PDI) is a promising strategy to eradicate pathogenic microorganisms such as Gram-positive and Gram-negative bacteria. This therapy relies on the use of a molecule called photosensitizer capable of generating, from molecular oxygen, reactive oxygen species including singlet oxygen under light irradiation to induce bacteria inactivation. Ru(II) polypyridyl complexes can be considered as potential photosensitizers for aPDT/PDI. However, to allow efficient treatment, they must be able to penetrate bacteria. This can be promoted by using nanoparticles. In this work, ruthenium-polylactide (RuPLA) nanoconjugates with different tacticities and molecular weights were prepared from a Ru(II) polypyridyl complex, RuOH. Narrowly-dispersed nanoparticles with high ruthenium loadings (up to 53%) and an intensity-average diameter < 300 nm were obtained by nanoprecipitation, as characterized by dynamic light scattering (DLS). Their phototoxicity effect was evaluated on four bacterial strains (Staphylococcus aureus, Staphylococcus epidermidis, Escherichia coli and Pseudomonas aeruginosa) and compared to the parent compound RuOH. RuOH and the nanoparticles were found to be non-active towards Gram-negative bacterial strains. However, depending on the tacticity and molecular weight of the RuPLA nanoconjugates, differences in photobactericidal activity on Gram-positive bacterial strains have been evidenced whereas RuOH remained non active.


Author(s):  
JONATHAN M. SUTTON ◽  
NELSON FERNANDEZ ◽  
ROSS W. BOYLE

A range of 5,15-diphenylporphyrins with symmetric and unsymmetric substitution patterns were subjected to osmium tetroxide-mediated dihydroxylations. The resulting chlorins and bacteriochlorins present an important group of compounds for studying structure-activity relationships of photodynamic sensitizers. The regioselectivity of the dihydroxylation of various 5,15-diphenylporphyrins with unsymmetrical substitution patterns was also examined. Both diphenylchlorin diol (DPC) and diphenylbacteriochlorin tetrol (DPBC) examples were converted into reactive isothiocyanates and conjugated with bovine serum albumin (BSA).


2022 ◽  
Author(s):  
Isadora Tisoco ◽  
Maria Carolina Donatoni ◽  
Henrique Victória ◽  
José Roberto de Toledo ◽  
Klaus Krambrock ◽  
...  

We report the synthesis and characterization of two novel tetra-cationic porphyrins, containing Pt(II) or Pd(II) polypyridyl complexes attached at the peripheral position of N4-macrocycle. Compounds were characterized through elemental analysis,...


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