Therapeutic Potential of Sol-Gel ZnO Nanocrystals: Anticancer, Antioxidant, and Antimicrobial Tri-Action.

Zinc oxide nanocrystals (ZnO NCs) hold great promise in nanomedicine with fascinating multifunctional properties. We investigated the therapeutic potential of sol-gel synthesized ZnO NCs with crystal sizes of 52.65 and 25.11 nm, focusing on their anticancer effects on HepG2 and HT29 cells, antioxidant properties, and antimicrobial activity. Both samples displayed a hexagonal wurtzite ZnO structure, wherein the crystal sizes diminished with lower calcination temperatures according to X-ray diffraction. The scanning electron microscopy analysis revealed that lowering the calcination temperature resulted in a decrease in the grain size of the ZnO NCs, as expected. This reduction in grain size combined with a decrease in crystal size resulted in a significant 40% reduction in the reflectance of the ZnO NCs in UV-vis-NIR spectroscopy. It was also observed that the ZnO NCs calcined at higher temperatures exhibited larger particle sizes with a reduced surface area mean of 69.30 µm and a stable negative zeta potential of -11.2 mV. In contrast, the ZnO NCs calcined at lower temperatures exhibited a larger surface area mean of 34.56 µm and a positive zeta potential of +10 mV. In both cell lines, the cytotoxic potential was found to be higher in HepG2 cells. Specifically, when ZnO nanocrystals (NCs) with a crystal size of 52.65 nm were used, the lowest cell viability was observed at a concentration of 5.74 µg/mL. Based on oxidative stress index values, a lower crystal size of ZnO NCs displayed greater effectiveness in HT29 cells, while a higher crystal size of ZnO NCs had pronounced effects in HepG2 cells. Moreover, both ZnO NCs exhibited significant antimicrobial activity against Gram-positive bacteria (Enterococcus faecalis and Staphylococcus aureus) and Candida parapsilopsis fungus. These findings emphasize sol-gel ZnO NCs' potential as versatile agents in nanomedicine, spurring research on targeted cancer therapies and antimicrobial innovations.

Exenatide increases CTRP3 gene expression in adipose cells by inhibiting adipogenesis and induces apoptosis.

Considering the rapidly increasing prevalence of obesity worldwide, the number of weight control drugs is very few. Incretin-based therapies are currently being developed to achieve weight control, and Glucagon-Like Peptide-1 Receptor Agonists (GLP-1RA) are used in incretin-based therapies. This study aimed to investigate the cytotoxicity of exenatide, a GLP-1A, on 3T3-L1 adipocytes and the effect of exenatide on the expression of adipogenesis-related genes, insulin and glucose levels, and apoptosis. Cytotoxic activity of exenatide on 3T3-L1 adipocytes was determined by MTT method. Gene expression levels were determined by qPCR. Apoptosis studies were performed on the Muse Cell Analyzer. C1q/TNF-related protein-3 (CTRP3) expression levels were found to be higher in exenatide treated adipocyte cells than in control cells (p < 0.001). Adipocyte cells treated with exenatide were found to have lower PPAR-γ gene expression levels when compared to control adipocyte cells (p < 0.001). Intracellular insulin (p < 0.001) and glucose levels were higher in 3T3-L1 adipocytes treated with exenatide compared to control adipocyte cells. Total apoptosis increased approximately 1.5 times as a result of exenatide administration. The increase in CTRP3 gene expression, which is thought to be a new biomarker for obesity, and the decrease in PPAR-γ gene expression indicate that exenatide is a promising new pharmacotherapeutic agent in the treatment of obesity by regulating the expression of genes related to adipogenesis and lipogenesis and inducing apoptosis.

Therapeutic Effects of Newly Synthesized Boron Compounds (BGM and BGD) on Hepatocellular Carcinoma.

Boron has an important potential for facilitating biological activity and for use in pharmaceutical drug design. Boron glycine monoester (BGM) and boron glycine diester (BGD) compounds containing boron atoms were synthesized and investigated their cytotoxic, oxidative stress, and antimicrobial activities on the HepG2 cancer cell line. The cytotoxic activity of newly synthesized boron compounds on hepatocellular carcinoma was determined by the MTT method for 48 h. Antioxidant (CAT, GSH), lipid peroxidation (MDA), and enzyme activity (ACP, ALP) analyses were determined by spectrophotometric methods in HepG2 cells. Antimicrobial activity was determined by the disk diffusion method. After 48 h of BGM and BGD application to HepG2 cells, we found the IC50 values as 9.9 mM and 24 mM, respectively. While CAT and ACP enzyme activities decreased in all groups compared to the control, ALP enzyme activity did not change in the BGM group but increased in the BGD group. It was determined that the GSH level did not change in all groups, while the MDA level increased. It has been stated that these IC50 doses of BGM and BGD have antibacterial effects on Staphylococcus aureus ATCC 29213 and Escherichia coli ATCC 25922. Newly synthesized boron compounds, particularly BGM, with their cytotoxic, oxidative stress, and antimicrobial effects, could provide a new therapeutic approach for the treatment of hepatocellular carcinoma.

Synthesis of New Boron Derived Compounds; Anticancer, Antioxidant and Antimicrobial Effect in Vitro Glioblastoma Tumor Model.

OBJECTIVE: The aim of our study is to investigate the cytotoxic, antioxidant, and antimicrobial effects of newly synthesized boron compounds in U87MG glioblastoma cell treatment. METHODS: We synthesized boron glycine monoester (BGM) and boron glycine diester (BGD) structures containing boron atoms and determined their cytotoxic activities on glioblastoma by the MTT method. The inhibitory concentration 50 (IC50) value was calculated with GraphPad Prism 5.0 program. The IC50 values were administered 48 hours on U87MG glioblastoma cell. Catalase (CAT), acid phosphatase (ACP) and alkaline phosphatase (ALP) enzyme activity, malondialdehyde (MDA), total glutathione (GSH), and total protein levels were detected using spectrophotometric methods. We determined the antimicrobial activities of BGM and BGD with the disc diffusion method. RESULTS: After 48 hours of BGM and BGD application to U87MG glioblastoma cells, we found the IC50 value as 6.6 mM and 26 mM, respectively. CAT and ACP enzyme activities were decreased in BGM and BGD groups. MDA which is a metabolite of lipid peroxidation was increased in both boron compounds groups. GSH level was reduced especially in BGD group. BGM and BGD have been found to be antimicrobial effects. CONCLUSION: Boron compounds, especially the BGM, can provide a new therapeutic approach for the treatment of glioblastoma with their anticancer, antioxidant, and antimicrobial effects.