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In this work, dendritic, water‐soluble, and nonaggregated axially substituted silicon phthalocyanines (EA‐TD‐Si and EA‐TD‐SiQ) were synthesized and characterized. Then, the supercoiled pBR322 plasmid DNA damage properties of EA‐TD‐Si and EA‐TD‐SiQ were examined using agarose gel electrophoresis without light irradiation. In addition, the cytotoxicity and phototoxicity of EA‐TD‐Si and EA‐TD‐SiQ on human endometrium adenocarcinoma (HEC‐1B) cells were investigated using an MTT assay. The results indicated that EA‐TD‐SiQ had high photodamage properties via singlet oxygen depending on the light dose, while EA‐TD‐Si did not show any DNA damage without light. In addition, EA‐TD‐SiQ had higher phototoxic effects than EA‐TD‐Si on HEC‐1B cells according to the MTT assay. These results revealed the potential of EA‐TD‐SiQ to be used as a PDT agent in endometrial cancer. [ABSTRACT FROM AUTHOR]

Alzheimer's disease, is one of the irreversible neurodegenerative disorders among older people, causes behavior, memory, and thinking problems. This study aim is to synthesize of 4‐({8‐[3‐(dimethylamino)phenoxy]octyl}oxy)phthalonitrile, zinc(II) phthalocyanine and its water soluble derivative containing ({8‐[3‐(dimethylamino)phenoxy]octyl}oxy) substituents at the peripheral positions first time. To determine the potential of water soluble silicon(IV) and zinc(II) phthalocyanines for use in AD, spectrophotometric assays were performed to determine their acetylcholinesterase/butyrylcholinesterase inhibitory effects. In addition, their DNA nuclease properties were evaluated by agarose gel electrophoresis. The results showed that the compounds inhibited acetylcholinesterase/butyrylcholinesterase. They did not damage pBR322 plasmid DNA depending on time and concentration. As a result of the experiments, it is revealed that the compounds may be the potential for use as cholinesterase inhibitors, which is a promising approach for the treatment of Alzheimer's disease. [ABSTRACT FROM AUTHOR]

In this study, magnesium (II) phthalocyanines (2a, 3a) and their water‐soluble derivatives (2b, 3b) were synthesized via multistep reactions. The structures of these phthalocyanines were identified by FT‐IR, NMR, MALDI‐TOF, and UV–Vis spectroscopy. The ct‐DNA binding (UV–Vis absorption, competitive EB binding, and agarose electrophoresis studies) and supercoiled plasmid DNA nuclease properties (hydrolytic, photonuclease, oxidative nuclease, and photooxidative nuclease) of the water‐soluble compounds were investigated using different methods. The DNA binding constant (Kb) values of 2b and 3b were calculated as 8.45 ± (0.25) × 104 and 7.71 ± (0.13) × 104 M−1 at 25°C, respectively. The results showed that 2b had a stronger ct‐DNA binding effect than 3b according to Kb and r values. The DNA nuclease studies claimed that both compounds indicated photonuclease activity on plasmid DNA depending on the light dose. Additionally, 2b had a higher photonuclease capacity than 3b. All of these results showed that 2b had promising potential as a photosensitizer agent for photodynamic therapy. [ABSTRACT FROM AUTHOR]

Alzheimer's disease (AD), one of the main causes of dementia, is a neurodegenerative disorder. Cholinesterase inhibitors are used in the treatment of AD, but prolonged use of these drugs can lead to serious side effects. Drug repurposing is an approach that aims to reveal the effectiveness of drugs in different diseases beyond their clinical uses. In this work, we investigated in vitro and in silico inhibitory effects of 11 different drugs on cholinesterases. The results showed that trimebutine, theophylline, and levamisole had the highest acetylcholinesterase inhibitory actions among the tested drugs, and these drugs inhibited by 68.70 ± 0.46, 53.25 ± 3.40, and 44.03 ± 1.20%, respectively at 1000 µM. In addition, these drugs are bound to acetylcholinesterase via competitive manner. Molecular modeling predicted good fitness in acetylcholinesterase active site for these drugs and possible central nervous system action for trimebutine. All of these results demonstrated that trimebutine was determined to be the drug with the highest potential for use in AD. [ABSTRACT FROM AUTHOR]