An α-carbonic anhydrase (CA, EC 4.2.1.1) was purified and characterized kinetically from erythrocytes of the sturgeon Acipenser gueldenstaedti, an endangered species. The sturgeon enzyme (AgCA) showed kinetic parameters for the CO₂ hydration reaction comparable with those of the human erythrocytes enzyme hCA II, being a highly active enzyme, whereas its esterase activity with 4-nitrophenyl acetate as substrate was lower. Sulphonamide inhibitors (acetazolamide, sulphanilamide) strongly inhibited AgCA, whereas metal ions (Ag⁺, Zn²⁺, Cu²⁺ and Co²⁺) were weak, millimolar inhibitors. Several widely used pesticides (2,4-dichlorophenol, dithiocarbamates, parathion and carbaryl) were also assayed as inhibitors of this enzyme. The dithiocarbamates were low micromolar AgCA inhibitors (IC₅₀ of 16–18 µM), whereas the other pesticides inhibited the enzyme with IC₅₀s in the range of 102–398 µM. The wide use of dithiocarbamate pesticides may be one of the factors enhancing the vulnerability of this sturgeon species to pollutants.

Monoamine oxidase (MAO) inhibitors are generally used in the treatment of depressive disorders and some neurodegenerative illnesses, such as Parkinson’s disease and Alzheimer’s disease. The aim of this preliminary study was to investigate the MAO [MAO (E.C.1.4.3.4)] inhibiting effect of various apitherapeutic products, such as chestnut honey, pollen and propolis. Extracts’ MAO inhibition was measured using peroxidase-linked spectrophotometric assay in enzyme isolated from rat liver microsomes, and the values are expressed as the inhibition concentration (IC₅₀) causing 50% inhibition of MAO. The antioxidant activity of the bee products was also determined in terms of total phenolic content (TPC) and ferric reducing/antioxidant power in aquatic extracts. All samples exhibited substantial inhibition of MAO, propolis having the highest. Inhibition was related to samples’ TPCs and antioxidant capacities. These results show that bee products possess a sedative effect and may be effective in protecting humans against depression and similar diseases.

Lack of Variation in Inflammatory Hematological Parameters between Benign Nodular Goiter and Papillary Thyroid Cancer N/L ratio;MPV;PDW;papillary thyroid cancer;benign nodular goiter; Background: Inflammatory hematological parameters like the neutrophil/lymphocyte (N/L) ratio have been investigated in many cancer types and significant relationships found with prognosis, for example. The aim of this present study was to investigate the impact of hematological parameters notably on N/L ratio and mean platelet volume (MPV) in papillary thyroid cancer cases. Materials and Methods: A total of 79 patients who underwent a thyroidectomy operation in Findikli, Goiter Research and Treatment Center during 2011-2015 period were enrolled in the study, 41 with papillary thyroid cancer and 38 with benign goiter confirmed by pathological examination. We collected clinical and laboratory data for the patients from hospital records retrospectively. Blood samples taken at admission were assessed for parameters compared between the groups. Results: No significant differences between papillary thyroid cancer and benign goiter groups were apparent in terms of age, the N/L ratio, MPV, white blood cell count (WBC), red blood cell count (RBC), hemoglobin, hematocrit, platelet, neutrophil, lymphocyte, red blood cell distribution width (RDW) and platelet crit (PCT) levels (p>0.05). Only the level of platelet distribution width (PDW) significantly differed, being lower in the papillary cancer group (p<0.05). Conclusions: No significant relationship between papillary thyroid cancer and inflammatory hematological parameters including in particular the N/L ratio and MPV. The relevance of the PDW values remains unclear.

New acrylamide compounds based on 4-aminoantipyrine were synthesized. 4-Acetaminoantipyrine was synthesized and its reactivity with salicylic aldehyde, vanillin, isovanillin and 5-methoxysalicylaldehyde with the formation of new N-(1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-yl)-3-(aryl)acrylamides was investigated. In addition, synthesized acrylamides were screened for ADME studies to elucidate their properties. The antimicrobial and antioxidant activitiy of the newly synthesized compounds were exceptionally high, surpassing the performance of the reference standard drug. Molecular docking simulations further confirmed these results, highlighting the heightened activity attributed to the substitute groups on the aromatic rings with different proteins and showed different interactions, confirming their biological evaluation. The optimization of target compounds using the DFT/B3LYP/6-311G(d) basis set demonstrated their stability and provided insights into their physical descriptors—Electrostatic Potential (ESP) and Molecular Electrostatic Potential (MEP). The analysis revealed both electrophilic and nucleophilic characters, showcasing their versatile binding capabilities in various pockets and confirming the biological results.

Polyphenols are important secondary products of plants with the potential to inhibit carbonic anhydrases. The aim of this study was to investigate the inhibition effects of various phenolic standards, honey, propolis, and pollen species on human carbonic anhydrase I and II. The inhibition values (IC₅₀) of the phenolics (gallic acid, protocatechuic acid, quercetin, catechin, tannic acid, and chrysin) ranged from 0.009 to 0.32 μg/mL, tannic acid emerging as the best inhibitor. The inhibition values of three different types of honey, heather, rhododendron, and chestnut ranged between 2.32 and 25.10 μg/mL, the chestnut honeys exhibiting the best inhibition. The ethanolic extracts of pollen and propolis exhibited good inhibitory properties, with IC₅₀ values between 0.486 and 3.320 μg/mL. In order to evaluate the phenolic composition of bee products, phenolic profiles and total phenolic contents (TFC) were also measured. The inhibition ranking among the natural products studied was phenolic standards > propolis > pollen > honeys, and inhibition was related to TFC.