Temel, Hamdi; Atlan, Metin; Türkmenoğlu, Burçin; Ertaş, Abdulselam; Erdönmez, Demet; Çalışkan, Ufuk Koca

Boronic acid compounds and the natural flavonoid compound quercetin were handled to synthesize two novel ligands encoded as B1(2,2′-(1,4-phenylenebis (benzo [1,3,2] dioxaborole-2,5-diyl)) bis (3,5,7-trihydroxy-4H- chromen-4-one) and B2(3.3.6. 3,5,7-trihydroxy-2-(2-(6-methoxypyridin-3-yl)benzo[d][1,3,2]dioxaborol-5-yl)− 4 H-chromene-4). Antioxidant activities of ligands were investigated by DPPH, ABTS and CUPRAC methods. Cholinesterase inhibition effects of ligands were determined by acetylcholinesterase and butyrylcholinesterase enzyme inhibition methods, cytotoxic effects of ligands were applied to healthy breast and colon cancer cell lines by MTT method, and urease and tyrosinase enzyme activities were determined. Antimicrobial properties of the compounds were analyzed by detecting their anti-QS potentials on Chromobacterium violaceum biosensor strain. Both compounds were found to have significant antioxidant effects compared to controls. It was determined that the compound B1 at 1–10 µg/mL was more active than the reference compounds (α-TOC and BHT). Moreover, the enzyme activity studies on ligands demonstrated that acetylchoinesterase and butyrylcholinesterase enzyme inhibitions were higher than the reference compounds. As expected, boron derivatives exhibited respectable activity against the biofilms of Escherichia coli (E. coli) and P. aeruginosa (P. aeruginosa). These results demonstrate the potential applicability of boron derivatives in the treatment of biofilm-associated infections and provide a practical strategy for the design of new boron-based antimicrobial materials. In silico molecular docking studies were performed on ligands to identify newly synthesized compounds. The binding parameter values and binding sites of the compounds were also determined. In conclusion, our studies showed that newly synthesized hybrid compounds could be solutions for antimicrobial resistance and enzyme-related disorders.

Özmeriç, Ahmet; Tanoğlu, Oğuzhan; Ocak, Mert; Çelik, Hakan Hamdi; Fırat, Ayşegül; Kaymaz, Fevziye Figen; Koca, Gökhan; Şenes, Mehmet; Alemdaroğlu, Kadir Bahadır; İltar, Serkan

Background: Boron nitride is a biocompatible and an osteo-inductive material for orthopedic applications. The aim of this study was to evaluate the effects of two different allotrope boron nitride coated implants, cubic boron nitride and hexagonal boron nitride, on fracture healing. Methods: In this experimental study, a total of 24 rats were divided into three groups. Group A was the control group with Kirschner wire without coating, while the wires were coated dominantly by cubic boron nitride in Group B and hexagonal boron nitride in Group C. Then a mid-third femoral fracture was created. The fracture healing was examined in terms of new bone formation with micro-CT analysis and histopathological examination, quantitative measurement of bone turnover metabolites and scintigraphic examination of osteoblastic activity on 28th day post fracture. Results: Micro-CT measurement results revealed a statistically significant increase in bone volume/tissue volume ratio and bone surface values in group B compared to group A. Cortex diameter and osteoblast counts were statistically higher in group B compared to group A. Inflammatory response was increased in group C compared to groups A and B. Biochemical test results showed significantly increased alkaline phosphatase levels and decreased osteocalcin levels in group B compared to group A. The increase in serum phosphorus and decrease in serum calcium levels was statistically significant in group C compared to Group A. Conclusion: Both types of boron nitride coating had superior fracture healing features compared to control group. Therefore, c-BN coating can accelerate the fracture healing and could lead to shorten of union time.

Beytut, Ebru; Yilmaz, Seval; Aksakal, Mesut; Polat, Seher

Acute exposure to high doses of glucocorticoids (GCs) may potentially increase the basal levels of reactive oxygen species (ROS) by altering the defence capacity against oxidative damage. Also, antioxidants may affect the oxidative breakdown of tissues. Therefore, the aim of this work was to determine the effects of dietary intake vitamin E and selenium (Se) on lipid peroxidation (LPO) as thiobarbituric acid reactive substances (TBARS) and on the antioxidative defence mechanisms in the brain of rats treated with high doses of prednisolone. Two hundred and fifty adult male Wistar rats were randomly divided into five groups. The rats were fed a normal diet, but groups 3, 4, and 5 received a daily supplement in their drinking water of 20 mg vitamin E, 0.3 mg Se, and a combination of vitamin E and Se, respectively, for 30 days. For 3 days subsequently, the control (group 1) was treated with a placebo, and the remaining 4 groups were injected intramuscularly with 100 mg/kg body weight (bw) prednisolone. After the last administration of prednisolone, 10 rats from each group were killed at 4, 8, 12, 24, and 48 h and the activities of enzymes selenium-glutathione peroxidase (Se-GSH-Px) and catalase (CAT), and the levels of reduced glutathione (reduced GSH) and TBARS in their brains were measured. Se-GSH-Px and CAT enzyme activities, and reduced GSH levels in the prednisolone treatment group (group 2) began to decrease gradually at 4 h (p < 0.01, p < 0.05, respectively), falling respectively to 60, 50, and 40% of the control levels by 24 h (p < 0.001, p < 0.01), and recovering to the control levels at 48 h. In contrast, prednisolone administration caused an increase in the brain TBARS, reaching up to six times the level of the control at 24 h (p < 0.001). However, supplementation with vitamin E and Se had a preventive effect on the elevation of the brain TBARS and improved the diminished activities of antioxidative enzymes and the levels of reduced GSH. Therefore, the present study attempts to determine the sequence of cellular membrane damage in the brain of the rats after high doses GC administration and the possible roles in vivo of vitamin E and Se, and their combination.