Determination of tetrodotoxin (TTX) levels in various tissues of the silver cheeked puffer fish (Lagocephalus sceleratus (Gmelin, 1789)) in Northern Cyprus Sea (Eastern Mediterranean)

Lagocephalus sceleratus from the family Tetraodontidae, which is originated from the Red Sea, started to migrate to Mediterranean waters after the opening of the Suez Channel in 1869. Since they do not have any predators in the Mediterranean Sea, their population increased in number very fast. Different tissues of L. sceleratus have tetrodotoxin (TTX). TTX is a non-protein, heat resistant molecule which binds to voltage-gated sodium channels of musculatory and nervous system. Ingestion of the fish can cause a wide variety of effects from mild toxications to death. This study is the first toxicity report of L. sceleratus for Cyprus. Due to the lack of data on toxicity levels of L. sceleratus, and some cases of poising after the ingestion of the fish were the reasons for the start of this work. 24 L. sceleratus were sampled from 3 different areas to represent Northern Cyprus, during one year period. 16 fish samples selected and grouped into 4 fishes per season for toxicity assay. TTX levels from liver, gonad, intestine, muscle and skin tissue homogenate were analyzed with TTX ELISA. Totally 80 tissues were analyzed, 40% of them were above the toxic limit (2.2 μg/g). Most toxic tissue, according to the seasonal average, was found in the summer season and was determined as; Liver = 13.48 μg/g. Most toxic three fishes were found to be female with a length of 45-60 cm. TTX distribution among tissues have similarities with previously published studies from different regions.status: publishe

Synthesis, characterization, molecular docking, dynamics simulations, and in silico absorption, distribution, metabolism, and excretion (ADME) studies of new thiazolylhydrazone derivatives as butyrylcholinesterase inhibitors

In this study, two novel series of thiazolylhydrazone derivatives containing 4-ethylpiperazine (3a-3f) and 4-methoxyphenylpiperazine (3g-3l) side chains were synthesized and their structures were characterized by spectral (H-1 NMR, C-13 NMR, and MS spectra) analyses. In vitro inhibitory activities of synthesized compounds against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) were determined by Ellman method. According to the results, all compounds showed a weak inhibitory effect on AChE, while promising results were obtained on BChE. Among the synthesized compounds, the activities of the derivatives carrying 4-ethylpiperazine (3a-3f) structure were found to be more effective than the compounds carrying 4-methoxyphenyl piperazine (3g-3l) derivatives. Especially, compound 3f bearing the nitro substituent was found to be the most promising compound on BChE in the series. The absorption, distribution, metabolism, and excretion (ADME) parameters of the synthesized compounds were predicted by using the SwissADME server. The potential binding mode and stability of compound 3f with BChE were investigated by the molecular docking and dynamics simulations. The results showed that 3f was strongly bound up with BChE with the optimal conformation; in addition, their binding free energy reached -167.936 +/- 13.109 kJ/mol

Assessment Of Anticholinesterase And Antioxidant Properties Of Selected Sage (Salvia) Species With Their Total Phenol And Flavonoid Contents

In this study, cholinesterase inhibitory potential relevant to Alzheimer's disease and antioxidant activities of the dichloromethane, ethyl acetate, and ethanol extracts from the aerial parts and/or roots of fourteen Salvia (sage) species (S. argentea, S. bracteata, S. caespitosa, S. cryptantha, S. glutinosa, S. indica, S. microstegia, S. multicaulis, S. pinnata, S. quezelii, S. syriaca, S. tobeyi, S. verticillata subsp. amasiaca, and S. viscosa) were investigated. Cholinesterase inhibition was determined by Ellman method at 25, 50, and 100?gml -1. Their antioxidant activity was assessed by 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity, metal-chelation capacity, and ferric-reducing antioxidant power (FRAP) assays. Total phenol and flavonoid contents of the extracts were also determined. The dichloromethane and ethanol extracts of the aerial parts of S. cryptantha were the most active ones against AChE (56.22±1.07%) and BChE (33.80±4.18%), respectively. The ethanol extracts exhibited better scavenging activity and FRAP. Anticholinesterase activity of 9 Salvia species (S. argentea, S. bracteata, S. caespitosa, S. indica, S. pinnata, S. quezelii, S. syriaca, S. tobeyi, and S. viscosa) is reported for the first time in the current study. © 2012 Elsevier B.V.TUBITAK-TBAG-104T450F.S. Senol expresses her genuine gratitude to the Scientific and Technological Research Council of Turkey (TUBITAK) for the scholarship provided for her Ph.D. program. Financial support for the field trips provided by Scientific and Technical Research Council of Turkey ( TUBITAK-TBAG-104T450 ) is also greatly acknowledged

Synthesis of Novel Benzothiazole-Piperazine Derivatives and Their Biological Evaluation as Acetylcholinesterase Inhibitors and Cytotoxic Agents

Objective and Method: A new series of benzothiazole-piperazine derivatives was synthesized and a complete chemical characterization of the novel compounds was provided. In vitro cytotoxic activities were screened against colorectal (HCT-116), breast (MCF-7) and hepatocellular (Huh7) cancer cell lines by Sulforhodamine B assay