Design,in Silico Studies and Biological Evaluation of New Chiral Thiourea and 1,3-Thiazolidine-4,5-dione Derivatives

In this study, new chiral thiourea and 1,3-thiazolidine-4,5-dione derivatives were synthesized, it was aimed to evaluate the various biological activities and molecular docking of these compounds. Firstly, the new thioureas ( 1 – 16 ) were obtained by reacting 1-naphthylisothiocyanate with different chiral amines. Then, the chiral thioureas were cyclized with oxalyl chloride to obtain 1,3-thiazolidine-4,5-dione derivatives ( 17 – 32 ). All compounds were evaluated with several in vitro antioxidant and enzyme inhibition activities. Compound 30 was the most active compound against AChE, with a value of IC₅₀=8.09±0.58 μM. On the other hand, all compounds were tested in silico absorption, distribution, metabolism, and excretion (ADME) assays to better understand their bioavailability. These physicochemical properties, pharmacokinetics, and drug-likeness of all compounds were calculated using SwissADME. Furthermore, according to molecular docking analyses compound 30 exhibited significant binding affinities for all enzymes. Based on our overall observations, compound 30 could be recommended as a potential lead for the therapuetic of Alzheimer's.     

Curcumin prevents liver fat accumulation and serum fetuin-A increase in rats fed a high-fat diet

Fetuin-A is synthesized in the liver and is secreted into the bloodstream. Clinical studies suggest involvement of fetuin-A in metabolic disorders such as visceral obesity, insulin resistance, diabetes, and fatty liver. Curcumin is extracted from the rhizome Curcuma longa and has been shown to possess potent antioxidant, anticarcinogenic, anti-inflammatory, and hypoglycemic properties. In this study, we investigated the effect of curcumin treatment on serum fetuin-A levels as well as hepatic lipids and prooxidant–antioxidant status in rats fed a high-fat diet (HFD). Male Sprague–Dawley rats were divided into six groups. Group 1 was fed control diet (10 % of total calories from fat). Groups 2 and 3 were given curcumin (100 and 400 mg/kg bw/day, respectively ) by gavage for 8 weeks and were fed control diet. Group 4 was fed with HFD (60 % of total calories from fat). Groups 5 and 6 received HFD together with the two doses of curcumin, respectively. Curcumin treatment appeared to be effective in reducing liver triglycerides and serum fetuin-A levels. These findings suggest that the reduction of fetuin-A may contribute to the beneficial effects of curcumin in the pathogenesis of obesity.     

Rapid and label-free bacteria detection by surface plasmon resonance (SPR) biosensors

Surface Plasmon Resonance (SPR) biosensor technology has been successfully used for the detection of various analytes such as proteins, drugs, DNA, and microorganisms. SPR-based immunosensors that coupled with a specific antigen-antibody reaction, have become a promising tool for the quantification of bacteria as it offers sensitive, specific, rapid, and label-free detection. In this paper, we review the important issues in the development of SPR-based immunoassays for bacteria detection, concentrating on instrumentation, surface functionalization, liquid handling, and surface regeneration. In addition, this review touches on the recent advances in SPR biosensing for sensitivity enhancement.     

Caligus solea n. sp. (Copepoda: Caligidae) parasitic on the common sole Solea solea (Linnaeus) from the north-eastern Mediterranean off the Turkish coast

A new species of caligid copepod, Caligus solea n. sp., is described from the common sole Solea solea (Linnaeus) caught off the north-eastern Mediterranean coast of Turkey. Both sexes of the parasite were collected from all over the upper body surface of its host. The new species belongs to the macarovi-group of species as established by Boxshall & Gurney (Bull Br Mus (Nat Hist) (Zool), 39:161–178, 1980), with which it shares the following four characters: (i) leg 4 with two-segmented exopod, distal segment carrying three apical spines but no lateral spine; (ii) distal exopodal segment of leg 1 with three plumose setae posteriorly plus four distal margin elements, spine 1 naked, spines 2 and 3 with accessory process and spine 4 about twice length of the others; (iii) females with one-segmented abdomen while males with two-segmented abdomen; (iv) male maxilliped with myxal process opposing the tip of the subchela. However, the new species differs from its congeners within the macarovi-group in the number of sensillae on each papilla on and around the postantennal process, and also in the absence of serrations along the distal margin of the maxilla. This is the twenty-eighth species of Caligus to be reported from the Mediterranean Sea.     

Population-response model for vibrotactile spatial summation

A computational model based on previous physiological and psychophysical data is presented for the human Pacinian (P) psychophysical channel. The model can predict the probability of detection in simple psychophysical tasks, and hence psychometric functions and thresholds. The model simulates stimulating variable and fixed glabrous skin sites with different-sized contactors and includes spatial variation of monkey P-fiber sensitivities. Therefore, it is especially suitable for studying spatial summation, i.e. the improvement of threshold with increasing contactor area. Selective contributions of neural integration (n.i.) and probability summation (p.s.) are also incorporated into the model. Model predictions are compared to psychophysical results of Gescheider et al. (). The performance of the model regarding the effects of contactor size is very good. In addition to predicting approximately 3?dB improvement of thresholds when the contactor area is doubled, the model also reveals nonlinear contributions of p.s. and n.i. Furthermore, the model asserts that thresholds are largely governed by neural integration when small contactors are used. These and other findings discussed in the article show that the presented model is a helpful tool for formulating testable hypotheses. Although the model can also simulate some temporal summation effects, simulation results do not conform well to previous data on temporal response properties. Thus, the model needs to be refined in that respect.     

Production of neutral and alkaline extracellular proteases by the thermophilic fungus, Scytalidium thermophilum, grown on microcrystalline cellulose

Extracellular proteases produced by Scytalidium thermophilum, grown on microcrystalline cellulose, were most active at pH 6.5–8 and 37–45 °C when incubated for 60 min. Highest protease activity was at day 3 where endoglucanase activity was low. Protease activity measurements with and without the protease inhibitors, p-chloromercuribenzoate, PMSF, antipain, E-64, EDTA and pepstatin A, suggest production of thiol-containing serine protease and serine proteases. Endoglucanase and Avicel-adsorbable endoglucanase activity in culture medium was not significantly affected by protease inhibitors.     

The effect of caffeic acid phenethyl ester (CAPE) on metabolic enzymes including acetylcholinesterase,butyrylcholinesterase, glutathione S-transferase,lactoperoxidase, and carbonic anhydrase isoenzymes I,II, IX,and XII

Caffeic acid phenethyl ester (CAPE) is an active component of honeybee propolis extracts. Carbonic anhydrases (CAs, EC 4.2.1.1) are widespread and intensively studied metalloenzymes present in higher vertebrates including humans as many diverse isoforms. Acetylcholinesterase (AChE) is responsible for acetyl choline (ACh) hydrolysis and plays a fundamental role in nerve impulse transmission by terminating the action of the ACh neurotransmitter at cholinergic synapses and neuromuscular junctions. Butyrylcholinesterase (BChE) is another enzyme abundantly present in the liver and released into blood in a soluble form. Lactoperoxidase (LPO) is an enzyme involved in fighting pathogenic microorganisms whereas glutathione S-transferases (GSTs) are dimeric proteins present both in prokaryotic and eukaryotic organisms and involved in cellular detoxification mechanisms. In the present study, the inhibition effect of CAPE on human carbonic anhydrase (hCA) isoforms I, II, IX, and XII, AChE, BChE, LPO, and GST was evaluated. CAPE inhibited these enzymes with K_is in the range between micromolar to picomolar. The best inhibitory effect was observed against AChE and BChE.     

Description of two new species of the genus Gobio (Teleostei: Cyprinidae) from the Black Sea coast of Turkey

Thesystematics of the genus Gobio, especially of the populations on the southern Black Sea coast, seems to be still far from being resolved. Seven species were rec-orded from the northern Black Sea coast while three species were recognized from the southern Black Sea coast. We examined in total 43 specimens from K?z?l?rmak River (southern Black Sea basin), 80 specimens from Çoruh River (the Western Cau-casus of the Black Sea basin), 14 specimens from Rioni River (the Western Caucasus of the Black Sea basin), and 6 specimens from Kherota and Shakhe Rivers (the Western Caucasus of the Black Sea basin). Based on an analysis of 32 metric and 5 meristic data as well as the number of vertebrae, we concluded that the K?z?l?rmak and Coruh populations are two distinct, unnamed species, and we describe them here as Gobio kizilirmakensis from the K?z?l?rmak River and G. artvinicus from the Çoruh River.

http://www.zoobank.org/urn:urn:lsid:zoobank.org:pub:1ED54FB1-588F-4412-B376-4BE4E4516EB1     

A new species of Pomatoschistus (Teleostei: Gobiidae) from Southern Anatolia

Pomatoschistus anatoliae sp. n. is described from estuary of Göksu River on the Mediterranean coast of the Anatolia. It is distinguished from its congeners by the suborbital papilla pattern, meristic, and ecological features. DNA barcoding based on COI sequences revealed that there is a high nucleotide sequence divergence to the nearest neighbour. Kimura’s two parameter distances between P. anatoliae sp. n. and other species of Pomatoschistus and Knipowitchia have found to be at least 5.1%.

http://www.zoobank.org/urn:lsid:zoobank.org:pub:4592CF50-07B5-4C25-892F-5D009057675B     

Comparison of novel and familiar commercial kits for detection of C-reactive protein levels

In this study, randomized patient sera were used to simultaneously evaluate an automated C-reactive protein (CRP) assay and a commercial semi-automated microCRP assay with respect to correlation, linearity, and accuracy. Patient specimens were analyzed; two independent assay runs were performed on i-CHROMA (Boditech Med Inc., Korea) and IMMAGE 800 (Beckman Coulter Inc., USA) analyzers to estimate the between- and within-run precision. All systems were calibrated, and quality-control materials were analyzed according to the manufacturer’s instructions. The results using the control materials were within the respective manufacturers’ specified limits. The comparison studies were designed using the CLSI EP9-2A guidelines. The mean serum CRP concentrations were 123.2 ± 123.5 mg/L (95 % confidence of interval (CI) 97.9–148.3) using the CRP assay and 130.1 ± 109.3 mg/L (95 % CI 107.9–152.4) using the microCRP assay. The variance values were σ = 15,252.6 and 11,935.8 for the CRP and microCRP assays, respectively. The concordance correlation coefficient value was calculated as 0.8314 (95 % CI 0.7594–0.8833). There was a significant correlation between the CRP and microCRP assays: r = 0.8392 and 95 % CI 0.7675–0.8902 (p < 0.0001). The CRP and microCRP detection methods were well correlated. The i-CHROMA has many advantages over the IMMAGE 800 with respect to space required, analysis time, and system setup/application costs in a laboratory. It may be an attractive instrument for small and intermediate medical centers.