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Photopharmacology is an approach that aims to be an alternative to classical chemotherapy. Herein, the different classes of photoswitches and photocleavage compounds and their biological applications are described. Proteolysis targeting chimeras (PROTACs) containing azobenzene moieties (PHOTACs) and photocleavable protecting groups (photocaged PROTACs) are also mentioned. Furthermore, porphyrins are referenced as successful photoactive compounds in a clinical context, such as in the photodynamic therapy of tumours as well as preventing antimicrobial resistance, namely in bacteria. Porphyrins combining photoswitches and photocleavage systems are highlighted, taking advantage of both photopharmacology and photodynamic action. Finally, porphyrins with antibacterial activity are described, taking advantage of the synergistic effect of photodynamic treatment and antibiotic therapy to overcome bacterial resistance. [ABSTRACT FROM AUTHOR]

Wastewater (WW) from urban and industrial activities is often contaminated with microorganisms and chemical pollutants. To reduce the concentration of microorganisms in WW to levels comparable to those found in natural waters, the sewage effluent is usually subjected to disinfection with chlorine, ozone, or ultraviolet light, which may lead to the formation of toxic products and contribute to the selection of resistant genes. Moreover, the changing patterns of infectious diseases and the emerging of multidrug resistant microbial strains entail the development of new technologies for WW decontamination. Microbial photodynamic inactivation (PDI) with photosensitizers, oxygen, and visible light has demonstrated to be effective in the inactivation of microorganisms via photogeneration of reactive oxygen species able to induce microbial damage at the external structures level. The promising results of PDI suggest that this principle can be applied to WW treatment to inactivate microorganisms but also to photodegrade chemical pollutants. The aim of this study was to assess the applicability of PDI for the microbial and chemical decontamination of secondarily treated WW. To evaluate the efficiency of bacterial inactivation in WW, experiments were done in both phosphate buffer saline (PBS) and filtered WWwith the bioluminescent Escherichia coli, using small and large volumes ofWW. The potential of PDI to inactivate the native bacteria (E. coli and Enterococcus) present in WW was tested and assays without the adding of bacteria to the WW were performed. It was also tested if the same PDI protocol was able to induce phototransformation of phenol. The cationic porphyrin 5,10,15,20-tetrakis(1-methylpyridinium-4-yl)porphyrin tetra-iodide (Tetra-Py+-Me) was shown to be effective against both bacterial groups representing both Gram-negative and Gram-positive bacteria used as microbiological parameters to instigate water quality and even showing the power to photooxidate organic compounds. As the photosensitizer when immobilized on solid matrixes can be easily removed, recovered, and reused, an effective, less-expensive, easy-applicable, and environmentally friendly technology can be applied to treatWW, inactivating microorganisms and degrading chemical contaminants at the same time. [ABSTRACT FROM AUTHOR]

The evidence that telomerase is overexpressed in almost 90% of human cancers justifies the proposal of this enzyme as a potential target for anticancer drug design. The inhibition of telomerase by quadruplex stabilizing ligands is being considered a useful approach in anticancer drug design proposals. Several aromatic ligands, including porphyrins, were exploited for telomerase inhibition by adduct formation with G-Quadruplex (GQ). 5,10,15,20-Tetrakis(N-methyl-4-pyridinium)porphyrin (H2TMPyP) is one of the most studied porphyrins in this field, and although reported as presenting high affinity to GQ, its poor selectivity for GQ over duplex structures is recognized. To increase the desired selectivity, porphyrin modifications either at the peripheral positions or at the inner core through the coordination with different metals have been handled. Herein, studies involving the interactions of TMPyP and analogs with different DNA sequences able to form GQ and duplex structures using different experimental conditions and approaches are reviewed. Some considerations concerning the structural diversity and recognition modes of G-quadruplexes will be presented first to facilitate the comprehension of the studies reviewed. Additionally, considering the diversity of experimental conditions reported, we decided to complement this review with a screening where the behavior of H2TMPyP and of some of the reviewed metal complexes were evaluated under the same experimental conditions and using the same DNA sequences. In this comparison under unified conditions, we also evaluated, for the first time, the behavior of the AgII complex of H2TMPyP. In general, all derivatives showed good affinity for GQ DNA structures with binding constants in the range of 106–107 M−1 and ligand-GQ stoichiometric ratios of 3:1 and 4:1. A promising pattern of selectivity was also identified for the new AgII derivative. [ABSTRACT FROM AUTHOR]