Phytochemical Profiles,Antioxidant, Cytotoxic,and Anti-Inflammatory Activities of Traditional Medicinal Plants: Centaurea pichleri subsp. pichleri,Conyza canadensis,and Jasminum fruticans

Centaurea pichleri subsp. pichleri, Conyza canadensis, and Jasminum fruticans are traditionally used plants grown in Turkey. Methanol extracts were obtained from these plants and pharmacological activity studies and phytochemical analyses were carried out. To evaluate the phytochemical composition, spectrophotometric and chromatographic techniques were used. The extracts were evaluated for antioxidant activity by DPPH^●, ABTS^●+ radical scavenging, and FRAP assays. The cytotoxic effects of the extracts were investigated on DU145 prostate cancer and A549 lung cancer cell lines. The anti-inflammatory effects of extracts were investigated on the NO amount, TNF-α, IFN-γ, and PGE 2 levels in lipopolysaccharide-stimulated Raw 264.7 cells. The richest extract in terms of phenolic compounds (98.19 ± 1.64 mg_GAE/g_extract) and total flavonoids (21.85 ± 0.64 mg_CA/g_extract) was identified as C. pichleri subsp. pichleri methanol extract. According to antioxidant activity determinations, the C. pichleri subsp. pichleri extract was found to be the most active extract. Finally, the C. pichleri subsp. pichleri methanol extract was revealed to be the most effective inhibitor of viability in the cytotoxic activity investigation, and the extract with the best anti-inflammatory action. The findings point to C. pichleri subsp. pichleri as a promising source of bioactive compounds in the transition from natural sources to industrial uses, such as new medications, cosmeceuticals, and nutraceuticals.     

Electrochemical Characteristics of a Novel Pyridinium Salt as a Candidate Drug Molecule and Its Interaction with DNA

In this article, for the first time, the electrochemical properties of a novel pyridine derivative, 4‐(2‐(2‐hydroxybenzylidene) hydrazinyl)‐1‐(3‐phenylpropyl) pyridinium bromide (abbreviated as 4‐Pyri), and its interaction with double stranded DNA (dsDNA) was investigated. The interaction between candidate drug molecule (4‐Pyri) and dsDNA was analyzed by examining 4‐Pyri (+0.6 V and +0.8 V) and guanine (+1.0 V) oxidation signal changes with Differential Pulse Voltammetry (DPV) and Cyclic Voltammetry (CV). Electrochemical Impedance Spectroscopy (EIS) was used to show the resistance changes before and after the interaction between 4‐Pyri and dsDNA. We showed that after the interaction with 4‐Pyri, the oxidation currents of guanine decreased dramatically, whereas the intrinsic oxidation currents of 4‐Pyri dramatically increased. 4‐Pyri oxidation current differences before and after the interaction with dsDNA enabled us to determine such interaction separately from guanine oxidation signals. In addition, resistance differences were observed at before and after the interaction with each other that confirmed the possible interaction. In addition, toxicity effect (S%) value, which is an important parameter for electrochemical studies indicated 4‐Pyri's toxicity to dsDNA. Our results demonstrated that 4‐Pyri interacts with dsDNA, and could be used as a potential candidate drug molecule due to its remarkable impact on dsDNA.     

Turn-on fluorescent probe for Zn2+ ions based on thiazolidine derivative

In this study, simple on–off fluorescent/UV–visible (UV–Vis) probes were easily prepared using 2-(2-hydroxyphenyl)thiazolidine-4-carboxylic acid ( Sen-1 ) and/or 2-(2-hydroxy-5-nitrophenyl)thiazolidine-4-carboxylic acid ( Sen-2 ) for fast detection of Zn²⁺ ions. Their sensing properties towards common metal ions were investigated using UV–Vis and fluorescence spectroscopies. Sen-1 and Sen-2 displayed a significant change with the addition of Zn²⁺ ions in the UV–Vis spectra. The addition of Zn²⁺ ions induced a 104 nm bathochromic shift for Sen-1 . The binding ratio towards Zn²⁺ metal ions was determined to be 1:1 by using Job plot analysis and fluorescence spectroscopy. The association constant and free energy (ΔG) of Sen-1 and Sen-2 towards Zn²⁺ ions were calculated by the Benesi–Hildebrand equation. The limit of detection of Sen-1 towards Zn²⁺ ions is 3.73 × 10⁻⁸ M, which is about 1/100 of the value recommended by the World Health Organization for drinking water. Sen-1 was successfully applied to detect Zn²⁺ ions in water samples and the fluorescence test strip was prepared for visual detection of Zn²⁺ ions. Finally, the quantum chemical parameters of Sen-1 and Sen-2 , such as highest occupied molecular orbital, lowest unoccupied molecular orbital, and chemical hardness, were investigated by the Becke, three-parameter, Lee–Yang–Parr, Hartree–Fock, and M062x methods.     

Design,Synthesis, and Evaluation of Novel 2H-Benzo[b][1,4]thiazin-3(4H)-one Derivatives as New Acetylcholinesterase Inhibitors

Alzheimer’s disease (AD) is a slowly progressive neurodegenerative disease that causes dementia in people aged 65 and over. In the present study, a series of thiadiazole hybrid compounds with benzothiazine derivatives as acetylcholinesterase inhibitors were developed and evaluated for their biological activity. The AChE and BChE inhibition potentials of all compounds were evaluated by using the in vitro Ellman method. The biological evaluation showed that compounds 3i and 3j displayed significant inhibitory activity against AChE. Compounds 3i and 3j showed IC₅₀ values of 0.027 µM and 0.025 µM against AChE, respectively. The reference drug donepezil (IC₅₀ = 0.021 µM) also showed significant inhibition against AChE. Further docking simulation also revealed that these compounds (3i and 3j) interacted with the active site of the enzyme similarly to donepezil. The antioxidant study revealed that compounds 3i and 3j exhibited greater antioxidant effects. An in vitro blood–brain barrier permeability study showed that compounds 3i and 3j are promising compounds against AD. The cytotoxicity study of compounds 3i and 3j showed non-cytotoxic with an IC₅₀ value of 98.29 ± 3.98 µM and 159.68 ± 5.53 µM against NIH/3T3 cells, respectively.     

Fibroin nanofibers production by electrospinning method

Silk fibroin, which has many characteristic properties such as low inflammation reaction, biodegradation, suppleness, good antithrombogenic details, biocompatibility and high tensile strength is a very good candidate for biomedical applications. Electrospinning procures high surface area, porous, nanofiber dimension fiber generation, which is a plain method. An experimental study was carried out to produce nanofiber structure from silk fibroin by electrospinning and the electrospinning parameters for the spinning of uniform, continuous and silk fibroin fibers were optimized. As a result, the effect of variables of concentration, distance and applied voltage on the strength, thickness, surface structure, fiber diameter of nanomaterial was investigated. Then, in vitro cell viability of the silk fibroin mat was analyzed. It was seen that the strength, mat thickness, and fiber diameter increased with solution concentration rise. It was found that the values of the fiber diameter and tensile strength decreased with increasing distance. It was determined that the effect of distance varies depending on the concentration in the mat thicknesses. The tensile strength was affected inversely proportional the applied voltage rises and distance. It was found that the fiber diameter values decreased together with increasing applied voltage. At cell viability of silk fibroin mat was occurred high cell viability after 24 h, but it was obtained low cell viability at the 48th h.     

A heat transfer problem with exponential memory and the associated thermal stresses

In this study, a heat transfer problem defined by the Caputo–Fabrizio derivative, which is known to behave by the exponential decaying law, is addressed in an axially symmetric cylindrical region. Thus, the fundamental solutions of the heat diffusion process and the associated thermal stresses are aimed to find. For this purpose, Laplace and finite Hankel integral transforms are applied according to the geometry of the region. To obtain the thermal stresses, constitutive relations of the classical thermoelasticity theory are used. The effects of fractional orders on the diffusion process are illustrated graphically using MATLAB.