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The worldwide rise in the antibiotic resistance of bacteria forces the development of alternative antimicrobial treatments. A potential approach is photodynamic inactivation (PDI). The aim of the present study was to determine the phototoxicity of protoporphyrin diarginate (PPArg2) against methicillin-resistant Staphylococcus aureus and human dermal fibroblasts. Different concentrations (0 to 20 µM) of PPArg2 and light dose of 6 J cm -2 were tested. Cell viability was evaluated using the methylthiazoletetrazolium (MTT) assay. Incubation with 10 µM followed by illumination yielded a 3.6 log10-unit reduction in the viable count for Staphylococcus aureus. At the same experimental conditions, only 22.5% of the fibroblasts were photoinactivated. Protoporphyrin diarginate at concentrations up to 20 µM demonstrated no toxicity towards S. aureus or fibroblasts when not irradiated. These results suggest that the protoporphyrin diarginate exerts a high bactericidal effect against methicillin-resistant S. aureus strain without harming eukaryotic cells.
A series of N-substituted N'-(2-alkylthio-4-chloro-5-methylbenzenesulfonyl)guanidine derivatives bearing sulfonamide moiety have been screened in vitro for antibacterial activity against isolates from patients with infections of oral cavity, respiratory tract and intestinal tract. The majority of compounds exhibited good antibacterial potency. 1-[4-Chloro-5-methyl-2-(4-trifluoromethylbenzylthio)benzenesulfonyl]-3-(3-sulfamoylphenyl)guanidine (13) showed very strong activity, with MIC ≤6.2 µg/ml against eleven bacteria strains belonged to Gram-positive anaerobes and aerobes. Furthermore, compound 13 exhibited promising activity toward highly resistant microorganisms such as methicillin-resistant Staphylococcus aureus and Enterococcus faecalis. It was found that Parvimonas micra, Finegoldia magna, Peptostreptococcus anaerobius, Propionibacterium acnes showed the highest susceptibility toward the investigated guanidines.
Steroidal saponins isolated from many plant species belonging to Monocotyledones display potent cytotoxic activity towards many human tumor cells. We examined the cytotoxic effects of crude Paris quadrifolia extract for the first time, testing isolated saponin-rich fractions against four different human cell lines using the [(3-(4,5- dimethylthiazol-2-yl)]-2,5-diphenyltetrazolium bromide (MTT) assay. Cytotoxic activity was tested against human promyelocytic leukemia (HL-60) cells, human cervical adenocarcinoma (HeLa) cells and human breast cancer (MDA-MB-468) cells. Human skin fibroblasts were used as non-neoplastic control cells. Our results show significant activity of the weakly water-soluble solid residue and butanolic fraction against HL-60 and HeLa cells. The solid residue exerted cytotoxicity against all tested cell lines.
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