7 research outputs found
Quantification of Chaoborus and small fish by mobile upward-looking echosounding
Chaoborus larvae inhabit frequently the water column of lakes, when they can be mistaken for small fish. Because larvae ascend up to the blind zone of downward-looking echo sounding at night, quantitative acoustic estimation of them is possible only with upward-looking approach. For this reason, the mobile hydroacoustic upward-looking system (120 and 38 kHz split-beam echosounder) in combination with a direct catch method (trawling) was tested to investigate the night community of invertebrates and juvenile fish in the surface layer of the #Ămov reservoir (Czech Republic). In the target strength range of invertebrates (smaller than -59 dB), the 38 kHz echosounder recorded only a small proportion of targets while the 120 kHz echosounder recorded distinct peaks corresponding to high densities of Chaoborus (target strength, TS range -70 to -60 dB, average TS -66 to -64 dB). At 120 kHz frequency, the TS distribution of smaller cohort of juvenile fish ( 1.5 ind.m^
Filling the blank space: Branched 4-nonylphenols isomers are responsible for robust constitutive androstane receptor (CAR) activation by nonylphenol
4-Nonylphenol (4-NP), a para-substituted phenolic compound mixture comprising a straight or branched carbon chain, is a widespread ubiquitous environmental pollutant and food contaminant. 4-NP, particularly the branched form, has been identified as an endocrine disruptor with potent activities on estrogen nuclear receptors. Constitutive Androstane Receptor (CAR, NR1I3) is another crucial nuclear receptor that regulates hepatic lipid, glucose, and steroid metabolism and is involved in endocrine disruption mechanism. The nonylphenol mixture has been described as an extremely potent activator of both human and rodent CAR. However, detailed mechanistic aspects of CAR activation by NP are enigmatic and it is not known if 4-NP can directly interact with the CAR ligand binding domain (LBD).
Here we examined interactions of individual branched (22NP, 33NP, and 353NP) and linear 4-NPs with CAR and its variants using molecular dynamics (MD) simulations, cellular experiments with various CAR constructs or CAR ligand binding domain (LBD) mutants, or in differentiated HepaRG hepatocyte cellular model.
Our results demonstrate that branched 4-NPs display more stable poses to activate both wild-type (wt)CAR1 as well as CAR3 variant LBDs in MD simulations. Consistently, branched 4-NP activated CAR3 and wtCAR1 LBD more efficiently than linear 4-NP or tert-nonylphenol (22NP). Furthermore, in HepaRG cells, we observed that all NP significantly up-regulated CYP2B6, a relevant hallmark for CAR activation. This is the first study to provide detailed insights into the direct interaction between individual 4-NPs and the human CAR-LBD, as well as its dominant variant CAR3 The work could contribute to the safer use of individual NPs in many areas of industry
3β-Isoobeticholic acid efficiently activates the farnesoid X receptor (FXR) due to its epimerization to 3ι-epimer by hepatic metabolism
Bile acids (BAs) are important signaling molecules acting via the farnesoid X nuclear receptor (FXR) and the membrane G protein-coupled bile acid receptor 1 (GPBAR1). Besides deconjugation of BAs, the oxidoreductive enzymes of colonic bacteria and hepatocytes enable the conversion of BAs into their epimers or dehydrogenated forms. Obeticholic acid (OCA) is the first-in-class BA-derived FXR agonist approved for the treatment of primary biliary cholangitis. Herein, a library of OCA derivatives, including 7-keto, 6-ethylidene derivatives and 3β-epimers, was synthetized and investigated in terms of interactions with FXR and GPBAR1 in transaction assays and evaluated for FXR target genes expression in human hepatocytes and C57BL/6 mice. The derivatives were further subjected to cell-free analysis employing in silico molecular docking and a TR-FRET assay. The conversion of the 3βhydroxy epimer and its pharmacokinetics in mice were studied using LC-MS. We found that only the 3β-hydroxy epimer of OCA (3β-isoOCA) possesses significant activity to FXR in hepatic cells and mice. However, in a cell-free assay, 3β-isoOCA had about 9-times lower affinity to FXR than did OCA. We observed that 3β-isoOCA readily epimerizes to OCA in hepatocytes and murine liver. This conversion was significantly inhibited by the hydroxy-Î5-steroid dehydrogenase inhibitor trilostane. In addition, we found that 3,7-dehydroobeticholic acid is a potent GPBAR1 agonist. We conclude that 3β-isoOCA significantly activates FXR due to its epimerization to the more active OCA by hepatic metabolism. Other modifications as well as epimerization on the C3/C7 positions and the introduction of 6-ethylidene in the CDCA scaffold abrogate FXR agonism and alleviate GPBAR1 activation
A novel upward-looking hydroacoustic method for improving pelagic fish surveys
For ethical reasons and animal welfare, it is becoming increasingly more important to carry out ecological surveys with a non-invasive approach. Information about fish distribution and abundance in the upper water column is often fundamental. However, this information is extremely hard to obtain using classical hydroacoustic methods. We developed a rigid frame system for pushing upward looking transducers of the scientific echo sounder (38 and 120âkHz) in front of the research vessel. The efficiency of the new approach for monitoring juvenile fish at night was investigated by comparing the results with a quantitative fry trawl in the ĹĂmov Reservoir in the Czech Republic. The experimental setup enabled comparisons for the 0â3âm and 3â6âm depth layers, which are utilized by almost all juvenile fish in summer. No statistically significant differences in the estimated abundance of juveniles were found between the two sampling methods. The comparison of abundance estimates gathered by the two frequencies were also not significantly different. The predicted mean lengths from acoustic sampling and the trawl catches differed by less than 10 mm in all comparisons. Results suggest that mobile hydroacoustic upward-looking systems can fill the methodological gap in non-invasive surveying of surface fishes
Terbinafine-loaded branched PLGA-based cationic nanoparticles with modifiable properties
Calibration of fish biomass estimates from gillnets : Step towards broader application of gillnet data
Fish are an important component of aquatic ecosystems, thus representative and reliable assessments of their population variables are essential for a variety of ecological applications, management and conservation. Determining Fish Density per actual Spatial Unit (volume or area, FDSU) as a measure of absolute fish quantity is of particular interest. Gillnets are undoubtedly one of the most common and important methods for assessing fish populations in large lentic waters. However, direct calculating of FDSU from gillnet catches is impossible because of the passive nature of this method, and to date there is no reliable model for calculating FDSU from gillnet catches.This weakness largely limits the use of gillnet data for applications requiring FDSU estimates. The aim of this study was to calibrate gillnet catches using FDSU obtained by active methods (beach seine nets and hydroacoustics) to develop a tool for assessing FDSU from gillnet catches. To achieve this goal, we compared gillnet biomass to fish biomass estimated from the active methods, both of which cover similar spatiotemporal niches. This comparison was performed using a statistical approach based on the recognition of non-negligible random measurement error in both the explanatory (active methods) and response (gillnets) variables.We found a strong positive linear relationship between fish biomasses sampled with gillnets and with active methods. The slope of the fitted linear model was similar when comparing gillnets with the two active methods. The statistical method used allowed for the inclusion of error in the biomass estimates with gillnets and active methods, refining the credible intervals of the estimated relationship. The effect of gillnet effort on model accuracy was simulated to show how increased effort narrows the credible interval. Finally, comparison with previously published relationships revealed a large but explainable discrepancy between our model and previous models.Our study showed that conversion of gillnet biomass to biomass per actual spatial unit is possible. The effective sampling area of one square meter of gillnet was determined to be 8 m2 of waterbody surface area when European standard 12 mesh-sizes gillnets are used, and 5 m2 when four larger meshes are added to the European standard gillnets. Our model further stressed the impact of increased sampling effort on reducing estimation variability and shows that the model may be dependent on the fish community.Peer reviewe