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Background and Purpose: Fentanyl analogues have been implicated in many cases of intoxication and death with overdose worldwide. The aim of this study is to investigate the pharmaco‐toxicology of two fentanyl analogues: butyrylfentanyl (BUF) and 4‐fluorobutyrylfentanyl (4F‐BUF). Experimental Approach: In vitro, we measured agonist opioid receptor efficacy, potency, and selectivity and ability to promote interaction of the μ receptor with G protein and β‐arrestin 2. In vivo, we evaluated thermal antinociception, stimulated motor activity and cardiorespiratory changes in female and male CD‐1 mice injected with BUF or 4F‐BUF (0.1–6 mg·kg−1). Opioid receptor specificity was investigated using naloxone (6 mg·kg−1). We investigated the possible role of stress in increasing cardiorespiratory toxicity using the corticotropin‐releasing factor 1 (CRF1) antagonist antalarmin (10 mg·kg−1). Key Results: Agonists displayed the following rank of potency at μ receptors: fentanyl > 4F‐BUF > BUF. Fentanyl and BUF behaved as partial agonists for the β‐arrestin 2 pathway, whereas 4F‐BUF did not promote β‐arrestin 2 recruitment. In vivo, we revealed sex differences in motor and cardiorespiratory impairments but not antinociception induced by BUF and 4F‐BUF. Antalarmin alone was effective in blocking respiratory impairment induced by BUF in both sexes but not 4F‐BUF. The combination of naloxone and antalarmin significantly enhanced naloxone reversal of the cardiorespiratory impairments induced by BUF and 4F‐BUF in mice. Conclusion and Implications: In this study, we have uncovered a novel mechanism by which synthetic opioids induce respiratory depression, shedding new light on the role of CRF1 receptors in cardiorespiratory impairments by μ agonists. [ABSTRACT FROM AUTHOR]

Herein we present the biocatalysed preparation of a mono-N-carbamate-protected precursor of antitumoral Nutlin-3a through enantioselective alkoxycarbonylation of meso-1,2-disubstituted-1,2-diaminoethane using enzyme lipases and dialkyl carbonates as acylating agents. A series of supported or free lipase enzymes were screened in combination with commercially available diallyl, diethyl and dimethyl carbonates. The reactions were conducted at different temperatures, for different reaction times and with variable co-solvent systems to evaluate the effects on the enzyme catalytic activity. The best results in terms of conversion, enantiomeric excess and yield were obtained when lipase from Candida antarctica B (CAL-B) was used with diallyl carbonate (DAC) when conducting the reaction solventless at 75 °C. [ABSTRACT FROM AUTHOR]

Copyright of Revista Movimenta is the property of Universidade Estadual de Goias and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

The current study reports the results of non‐aqueous dyeing on polyamide fabrics based on a reverse micellar system composed of a stable emulsion of soybean oil, a co‐surfactant, a nonionic surfactant and acid dyes. The system does not make use of water or electrolytes and significantly reduces the dyebath volume. The influence of the hydrophilic lipophilic balance of the surfactants was evaluated, and it was found that the more hydrophilic the surfactant, the better the interaction of the reverse micellar emulsion with the substrate and, consequently, the greater the resulting colour strength. The co‐surfactant plays an important role in the system, as its proportion to the surfactant/oil mixture is directly related to better exhaustion of the dyebath. The results were compared with those from a conventional water‐based dyeing system. Colour matching was performed using the CIELab colour difference formula (ΔE) measured by a reflectance spectrophotometer. [ABSTRACT FROM AUTHOR]

Simple Summary: Obesity is a significant health concern among companion animals, particularly dogs and cats, with numerous detrimental health implications. Many pet owners struggle with managing their pets' weight, and they often underestimate their pets' body condition. This study, held in France from 2020 to 2022, revealed that about one quarter of pet owners underestimate their pets' body condition. Having children was linked to this underestimation for both dog and cat owners. This discovery highlights the importance of taking a comprehensive approach to the health and well-being of pets and emphasizes the need for a holistic "One Health" strategy. Managing pet obesity relies heavily on the active involvement of owners; however, a key challenge arises from misperceptions about their own pet's body condition. Given evolving societal dynamics like the body positivity movement, understanding owners' perceptions is increasingly pivotal. To evaluate the differences in owners' perception, this study compared the use of verbal and visual body condition score scales versus the established nine-point body condition score system. The factors linked to underestimation were further specifically investigated. Owners of healthy adult dogs and cats attending vaccination consultations in Veterinary Hospitals in France between 2020 and 2022 were recruited. They were required to assess their pets' body condition initially using an oral description and then with the nine-point BCS visual scale. Their assessments were then compared with the BCS determined by veterinary health care personnel, considered the primary investigator. A total of 304 dogs and 270 cats were included in the study. It was observed that 27% of dog owners and 24% of cat owners underestimated their pets' body condition. Among dog and cat owners, factors associated with the underestimation of body condition were the pets' overweight status and having children. This discovery emphasizes the need for a holistic One Health approach that prioritizes the health and well-being of both humans and their pets. When it comes to pet owners evaluating their pets' body condition, underestimation proved to be the predominant misperception. Addressing this issue requires comprehensive education to empower owners to recognize and comprehend their pets' overweight status, a critical step for the overall well-being of companion animals. [ABSTRACT FROM AUTHOR]

The enormous influence in terms of bioactivity, affinity, and selectivity represented by the replacement of (L)-2,6-dimethyl tyrosine (Dmt) instead of Phenylalanine (Phe) into Nociceptin/orphanin (N/OFQ) neuropeptide analogues has been well documented in the literature. More recently, the non-natural amino acid (L)-2-methyl tyrosine (Mmt), with steric hindrance included between Tyr and Dmt, has been studied because of the modulation of steric effects in opioid peptide chains. Here, we report a new synthetic strategy to obtain Mmt based on the well-known Pd-catalyzed ortho-C(sp2)–H activation approach, because there is a paucity of other synthetic routes in the literature to achieve it. The aim of this work was to force only the mono-ortho-methylation process over the double ortho-methylation one. In this regard, we are pleased to report that the introduction of the dibenzylamine moiety on a Tyr aromatic nucleus is a convenient and traceless solution to achieve such a goal. Interestingly, our method provided the aimed Mmt either as N-Boc or N-Fmoc derivatives ready to be inserted into peptide chains through solid-phase peptide synthesis (SPPS). Importantly, the introduction of Mmt in place of Phe1 in the sequence of N/OFQ(1-13)-NH2 was very well tolerated in terms of pharmacological profile and bioactivity. [ABSTRACT FROM AUTHOR]

Premise: Cacti are characteristic elements of the Neotropical flora and of major interest for biogeographic, evolutionary, and ecological studies. We tested global biogeographic boundaries for Neotropical Cactaceae using specimen‐based occurrences, coupled with data from visual observations, as a means to tackle the known collection biases in the family. Methods: Species richness and record density were assessed for preserved specimens and human observations, and a bioregional scheme tailored to Cactaceae was produced using the interactive web application Infomap Bioregions, based on data from 261,272 point records cleaned through automated and manual steps. Results: We found that areas in Mexico and southwestern USA, in eastern Brazil, and along the Andean region have the greatest density of records and the highest species richness. Human observations complement information from preserved specimens substantially, especially along the Andes. We propose 24 cactus bioregions, among which the most species‐rich are northern Mexico/southwestern USA, central Mexico, southern central Mexico, Central America, Mexican Pacific coast, central and southern Andes, northwestern Mexico/extreme southwestern USA, southwestern Bolivia, northeastern Brazil, and Mexico/Baja California. Conclusions: The bioregionalization proposed shows biogeographic boundaries specific to cacti and can thereby aid further evolutionary, biogeographic, and ecological studies by providing a validated framework for further analyses. This classification builds upon, and is distinctive from, other expert‐derived regionalization schemes for other taxa. Our results showcase how observation data, including citizen‐science records, can complement traditional specimen‐based data for biogeographic research, particularly for taxa with specific specimen collection and preservation challenges and those that are threatened or internationally protected. [ABSTRACT FROM AUTHOR]

We evaluated the effects of a Bacillus -based direct-fed microbial (DFM) on total in vitro gas production, dry matter (DM), neutral detergent fiber (NDF), and starch disappearance of different feedstuffs and total mixed rations (TMR) in three different experiments. In experiment 1, six single fiber-based feedstuffs were evaluated: alfalfa hay, buffalo grass, beet pulp, eragrostis hay, oat hay, and smutsvinger grass. Experimental treatments were control (with no probiotic inoculation; CON) or incubation of a probiotic mixture containing Bacillus licheniformis and B. subtilis (3.2 × 109 CFU/g; DFM). The calculation of DFM dose under in vitro conditions was based on the assumption of a rumen capacity of 70 liter and the dose of 3 g of the DFM mixture/head/d (9.6 × 109 CFU). Total in vitro gas production, DM, and NDF disappearance were evaluated at 24- and 48 h posttreatment incubation. Mean treatment effects were observed at 24- and 48 h gas production (P < 0.0001), as DFM incubation increased in vitro gas production by 5.0% and 6.5%, respectively. For nutrient digestibility, mean DM digestibility was increased at 48 h (P = 0.05), whereas mean NDF digestibility increased at both timepoints by incubating DFM in vitro (P ≤ 0.02). In experiment 2, nine commercial dairy TMR were collected and evaluated for the same variables and treatments described in experiment 1, with the additional analysis of starch digestibility at 7 h post in vitro incubation. The only difference was the concentration of the DFM included, being representative for a dosage of 8.8 × 109 CFU/head/d. In vitro gas production was increased only at 48 h due to DFM incubation (P = 0.05), whereas DM and NDF digestibility were improved at 24 and 48 h (P ≤ 0.02). No treatment effects were observed on in vitro starch digestibility (P = 0.31). In experiment 3, a combined analysis of DM and NDF digestibility was performed by using quality values (NDF and crude protein or CP) of 16 substrates. Regardless of CP and NDF levels of the substrates, DFM improved in vitro 24 and 48 h DM and NDF digestibility (P ≤ 0.03). In summary, incubating a Bacillus -based DFM (B. licheniformis and B. subtilis; BOVACILLUS) improved mean in vitro gas production, DM, and NDF digestibility of single feedstuffs and commercial dairy TMR, highlighting the potential of this combination of Bacillus spp. to improve nutrient utilization, mainly fiber. [ABSTRACT FROM AUTHOR]

The NASA InSight Lander on Mars includes the Heat Flow and Physical Properties Package HP3 to measure the surface heat flow of the planet. The package uses temperature sensors that would have been brought to the target depth of 3–5 m by a small penetrator, nicknamed the mole. The mole requiring friction on its hull to balance remaining recoil from its hammer mechanism did not penetrate to the targeted depth. Instead, by precessing about a point midway along its hull, it carved a 7 cm deep and 5–6 cm wide pit and reached a depth of initially 31 cm. The root cause of the failure – as was determined through an extensive, almost two years long campaign – was a lack of friction in an unexpectedly thick cohesive duricrust. During the campaign – described in detail in this paper – the mole penetrated further aided by friction applied using the scoop at the end of the robotic Instrument Deployment Arm and by direct support by the latter. The mole tip finally reached a depth of about 37 cm, bringing the mole back-end 1–2 cm below the surface. It reversed its downward motion twice during attempts to provide friction through pressure on the regolith instead of directly with the scoop to the mole hull. The penetration record of the mole was used to infer mechanical soil parameters such as the penetration resistance of the duricrust of 0.3–0.7 MPa and a penetration resistance of a deeper layer (> 30 cm depth) of 4.9 ± 0.4 MPa . Using the mole’s thermal sensors, thermal conductivity and diffusivity were measured. Applying cone penetration theory, the resistance of the duricrust was used to estimate a cohesion of the latter of 2–15 kPa depending on the internal friction angle of the duricrust. Pushing the scoop with its blade into the surface and chopping off a piece of duricrust provided another estimate of the cohesion of 5.8 kPa. The hammerings of the mole were recorded by the seismometer SEIS and the signals were used to derive P-wave and S-wave velocities representative of the topmost tens of cm of the regolith. Together with the density provided by a thermal conductivity and diffusivity measurement using the mole’s thermal sensors, the elastic moduli were calculated from the seismic velocities. Using empirical correlations from terrestrial soil studies between the shear modulus and cohesion, the previous cohesion estimates were found to be consistent with the elastic moduli. The combined data were used to derive a model of the regolith that has an about 20 cm thick duricrust underneath a 1 cm thick unconsolidated layer of sand mixed with dust and above another 10 cm of unconsolidated sand. Underneath the latter, a layer more resistant to penetration and possibly containing debris from a small impact crater is inferred. The thermal conductivity increases from 14 mW/m K to 34 mW/m K through the 1 cm sand/dust layer, keeps the latter value in the duricrust and the sand layer underneath and then increases to 64 mW/m K in the sand/gravel layer below. [ABSTRACT FROM AUTHOR]

Plant-derived remedies rich in chalcone-based compounds have been known for centuries in the treatment of specific diseases, and nowadays, the fascinating chalcone framework is considered a useful and, above all, abundant natural chemotype. Velutone F, a new chalconoid from Millettia velutina, exhibits a potent effect as an NLRP3-inflammasome inhibitor; the search for new natural/non-natural lead compounds as NLRP3 inhibitors is a current topical subject in medicinal chemistry. The details of our work toward the synthesis of velutone F and the unknown non-natural regioisomers are herein reported. We used different synthetic strategies both for the construction of the distinctive benzofuran nucleus (BF) and for the key phenylpropenone system (PhP). Importantly, we have disclosed a facile entry to the velutone F via synthetic routes that can also be useful for preparing non-natural analogs, a prerequisite for extensive SAR studies on the new flavonoid class of NLRP3-inhibitors. [ABSTRACT FROM AUTHOR]

3-(1-Naphthalenylmethyl)-1-pentyl-1H-indole (JWH-175) is a synthetic cannabinoid illegally marketed for its psychoactive cannabis-like effects. This study aimed to investigate and compare in vitro and in vivo pharmacodynamic activity of JWH-175 with that of 1-naphthalenyl (1-pentyl-1H-indol-3-yl)-methanone (JWH-018), as well as evaluate the in vitro (human liver microsomes) and in vivo (urine and plasma of CD-1 male mice) metabolic profile of JWH-175. In vitro binding studies showed that JWH-175 is a cannabinoid receptor agonist less potent than JWH-018 on mouse and human CB1 and CB2 receptors. In agreement with in vitro data, JWH-175 reduced the fESPS in brain hippocampal slices of mice less effectively than JWH-018. Similarly, in vivo behavioral studies showed that JWH-175 impaired sensorimotor responses, reduced breath rate and motor activity, and increased pain threshold to mechanical stimuli less potently than JWH-018. Metabolic studies demonstrated that JWH-175 is rapidly bioactivated to JWH-018 in mice blood, suggesting that in vivo effects of JWH-175 are also due to JWH-018 formation. The pharmaco-toxicological profile of JWH-175 was characterized for the first time, proving its in vivo bio-activation to the more potent agonist JWH-018. Thus, it highlighted the great importance of investigating the in vivo metabolism of synthetic cannabinoids for both clinical toxicology and forensic purposes. [ABSTRACT FROM AUTHOR]

Background: Nowadays, more people are treating dogs as family members. This reflects their increased attention towards their nutrition, with renewed interest for non-conventional diets such as Biologically Appropriate Raw Food/ Bones and Raw Food in United States (BARF) or homemade. In previous studies, owners feeding their dog non-conventional diets reported lower levels of trust in veterinary advice. The aim of the study was to identify differences in lifestyle between owners feeding dogs non-conventional diets and those feeding conventional diets (i.e., dry/wet pet food) to give further insight for improving communication between veterinarians and owners. Results: A total of 426 surveys were usable. Fifteen percent of the participants lived in the metropole of Paris and had more than one dog (mean 1.72 dogs). Thirty-eight percent of the survey respondents stated that their dogs were fed exclusively with non-conventional diets, while 55% declared using conventional diets alone (not considering treats). The study canine population was for the most part neutered (63%) and purebred (68%). Amongst owners feeding conventional diets exclusively, 47% determined how much food to feed by consulting the feeding guidelines on the packaging, and only 28% said that the amount of food was prescribed by their veterinarian or veterinary nurse. Out of the participants feeding non-conventional diets, 65% declared that the information for formulating the recipes was gathered on the internet or in non-veterinary books. When compared with owners feeding exclusively conventional diets, those feeding non-conventional diets were living more frequently outside the metropole of Paris, had fewer children (0.23 ± 0.57 vs 0.37 ± 0.78; p = 0.03) and had more frequently other animals. They also dewormed less often their pets, walked their dog more each day (91 vs 78%; p < 0.001) and without leash for more than 6 h per week (46 vs 31%; p = 0.003). Conclusions: This survey described differences in the habits of owners feeding dogs non-conventional diets in comparison with those feeding conventional diets. Data suggest that owners using non-conventional diets may be more attentive to the ethological needs of their dog which could be a starting point for practitioners for achieving better client-veterinarian communication. [ABSTRACT FROM AUTHOR]

Copyright of Revista Movimenta is the property of Universidade Estadual de Goias and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

This document is a summary of a special issue of the journal Pharmaceuticals, which focuses on methyl-containing pharmaceuticals. The issue includes various papers and reviews on this topic. The "magic-methyl effect" is a well-known phenomenon in medicinal chemistry and drug discovery, which has implications for biological activity, selectivity, solubility, and other properties. The issue covers different aspects related to the methyl effect, including the anticancer activity of a methyl-containing selenylated imidazo[1,2-a]-pyridine derivative, the synthesis of novel bis-terephthalthioamides, a computational method for predicting the binding mode of COX inhibitors, and the synthesis of mono-methyl tyrosine. The issue also includes a review that analyzes the relationship between chemical structures and biological activity. [Extracted from the article]

In the early years of school, pupils have a very positive approach towards any new topic. Very often, the first contact with mathematics in the Italian school risks giving a limited and somehow negative impression, generating long-lasting effects. In this paper, we report on a series of experiences carried out in a second-year class of a primary school that allowed us to introduce new concepts and approaches through games and puzzles. The aim was to stimulate the creativity and empower pupils. We have used simple materials and applied the Puzzle-Based Learning method. Despite the limited time devoted to this experience, the outcomes have been extremely positive. [ABSTRACT FROM AUTHOR]

A topical subject in human nutrition is the steadily growing number of people choosing to limit or completely avoid all animal‐derived food products either for moral dilemma, health concerns or both. To meet people's will of applying their dietary choices to their domestic animals, the pet food industry answered by launching on the market some plant‐based diets. This leads to concerns about whether these diets are adequately formulated to satisfy the target species nutritional requirements, especially for cats which are still considered strict carnivores. This case report follows a 2‐year‐old male neutered Main Coon and a 1‐year‐old female spayed Domestic Shorthair cat, presented to the nutrition service of the University of Toulouse, France. Reason for consultation was lethargy with in anamnesis a recent dietary transition to a plant‐based pet food. Dysorexia, lethargy and muscle waste were present at first consultation. Progressive weight loss developed during follow‐ups. A macrocytic, non‐regenerative anaemia with serum folates below reference were the main clinical features. Analysis of pet food showed multiple nutrients below minimum recommendation at the average daily intake of both cats. Folic acid supplementation improved dysorexia, and subsequent reintroduction of animal‐derived ingredients in the diet restored appetite, weight and a normal mentation in both cases. [ABSTRACT FROM AUTHOR]

More than one-third of the cases of infective endocarditis (IE) occur in older patients. The disease is often characterized by atypical symptoms. The incidence of neurological complications is high and represents a strong independent predictor of severe outcomes and mortality. IE is a rare but serious complication of transcatheter aortic valve implantation (TAVI). A persistent delirium as a unique manifestation of post-TAVI IE in an older patient is presented in this clinical case. [ABSTRACT FROM AUTHOR]

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Background: Bromide is a halide ion of the element bromine usually administered in the form of potassium salt as monotherapy or add-on treatment in epileptic dogs. It is excreted unchanged in the urine and undergoes tubular reabsorption in competition with chloride. Thus, dietary chloride content affects serum bromide concentrations. This is the first published clinical report of bromide toxicosis secondary to a dietary modification of chloride content in an epileptic dog treated with potassium bromide. Case presentation: A 3-year-old 55-kg neutered male Tibetan Mastiff was evaluated because of a 1-month history of progressive signs including ataxia, lethargy and behaviour changes. The dog was successfully treated for idiopathic epilepsy since the age of 1-year-old with phenobarbital and potassium bromide. Two months prior to presentation, the owners decided to change the dog's diet without veterinary advice. Physical examination was unremarkable. A 12-kg weight gain was recorded since last follow-up (8 months). Neurological examination revealed severe symmetric 4-limbs ataxia with altered vigilance and intermittent episodes of hyperactivity and aggressive behaviour without significant abnormality of cranial nerves. Serum bromide concentration was high and increased by 103 % since last follow-up. Nutritional evaluation revealed a 53 % decrease of chloride content in the diet before and after dietary transition. Bromide toxicosis was suspected, due to bromide reduced clearance secondary to the decreased dietary chloride content. Potassium bromide treatment was lowered by 15 % without further dietary changes. Neurologic signs progressively improved over the next month, without any seizure. After two months, the serum bromide concentration lowered to the same level measured before dietary modification. After four months, neurological examination was unremarkable. Conclusions: Dietary chloride content can directly influence serum bromide concentrations, therefore affecting seizure control or contributing to unexpected adverse effects. In the present case, a reduction in chloride intake markedly increased serum bromide concentrations causing bromism. Dietary changes should be avoided in dogs treated with potassium bromide to maintain stable serum bromide levels. [ABSTRACT FROM AUTHOR]

Recently, new agricultural policies and European Directives brought to important changes in farming practice, some of which could affect food availability for the wild bird population endangering biodiversity. This study aims to evaluate the consequences of such agricultural changes in France on the woodpigeon's dietary regimen. A total of 1,093 woodpigeons were collected over a four‐year period (2014–2017). Voluntary sampling was performed in six regions in the south‐west of France by local hunters during this species' autumnal migration and wintering. Ingluvies contents were recovered, macroscopically and microscopically identified, and then weighed before and after drying. Five food groups were identified: acorns, corn, green plant material, cultivated seeds and others. ANOVA testing followed by Tukey's test for multiple comparison were performed (R version 3.5.2). Significance was set at p <.05. A total of 762 woodpigeons met the study's inclusion criteria. Mean weight of total crop contents was less of 9 grams of dry matter. Most frequent food groups were "green plant material" (70.3%), acorns (42.3%) and corn (27.2%). In terms of grams of dry matter, the most important food in the crop content were acorns (62%): these were eaten more during the first two hunting seasons (p <.001), and in region A, lower amount was consumed compared to all other regions. On the contrary, corn intake peaked during the third year (p <.001), and in region A, birds had an increasing intake of this cereal. Cultivated seeds contributed to the diet more during migration (p =.007), while "green plant material" and others more during wintering (p =.011; p =.004). In conclusion, results confirm the opportunistic nature of the woodpigeon, balancing its diet according to food availability. Corn was eaten more in areas where the winter burying of chopped maize stover (mulching), provided by the Nitrate's directive, was in derogation. [ABSTRACT FROM AUTHOR]

Species occurrence records provide the basis for many biodiversity studies. They derive from georeferenced specimens deposited in natural history collections and visual observations, such as those obtained through various mobile applications. Given the rapid increase in availability of such data, the control of quality and accuracy constitutes a particular concern. Automatic filtering is a scalable and reproducible means to identify potentially problematic records and tailor datasets from public databases such as the Global Biodiversity Information Facility (GBIF; http://www.gbif.org), for biodiversity analyses. However, it is unclear how much data may be lost by filtering, whether the same filters should be applied across all taxonomic groups, and what the effect of filtering is on common downstream analyses. Here, we evaluate the effect of 13 recently proposed filters on the inference of species richness patterns and automated conservation assessments for 18 Neotropical taxa, including terrestrial and marine animals, fungi, and plants downloaded from GBIF. We find that a total of 44.3% of the records are potentially problematic, with large variation across taxonomic groups (25-90%). A small fraction of records was identified as erroneous in the strict sense (4.2%), and a much larger proportion as unfit for most downstream analyses (41.7%). Filters of duplicated information, collection year, and basis of record, as well as coordinates in urban areas, or for terrestrial taxa in the sea or marine taxa on land, have the greatest effect. Automated filtering can help in identifying problematic records, but requires customization of which tests and thresholds should be applied to the taxonomic group and geographic area under focus. Our results stress the importance of thorough recording and exploration of the meta-data associated with species records for biodiversity research. [ABSTRACT FROM AUTHOR]

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Copyright of Revista Movimenta is the property of Universidade Estadual de Goias and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Mucus form H. aspersa muller has been reported to have several therapeutic proprieties, such as antimicrobial activity, skin protection and wound repair. In this study, we have analyzed H. aspersa mucus (Helixcomplex) bio-adhesive efficacy and its defensive properties against the ozone (O3) (0.5 ppm for 2 hours) exposure in human keratinocytes and reconstructed human epidermis models. Cytotoxicity, tissue morphology and cytokine levels were determined. We confirmed HelixComplex regenerative and bio-adhesive properties, the latter possibly via the characteristic mucopolysaccharide composition. In addition, HelixComplex was able to protect from O3 exposure by preventing oxidative damage and the consequent pro-inflammatory response in both 2D and 3D models. Based on this study, it is possible to suggest HelixComplex as a potentially new protective technology against pollution induced skin damage. [ABSTRACT FROM AUTHOR]

The aim of this review is to highlight the rich chemistry of α‐haloamides originally mainly used to discover new C−N, C−O and C−S bond forming reactions, and later widely employed in C−C cross‐coupling reactions with C(sp3), C(sp2) and C(sp) coupling partners. Radical‐mediated transformations of α‐haloamides bearing a suitable located unsaturated bond has proven to be a straightforward alternative to access diverse cyclic compounds by means of either radical initiators, transition metal redox catalysis or visible light photoredox catalysis. On the other hand, cycloadditions with α‐halohydroxamate‐based azaoxyallyl cations have garnered significant attention. Moreover, in view of the important role in life and materials science of difluoroalkylated compounds, a wide range of catalysts has been developed for the efficient incorporation of difluoroacetamido moieties into activated as well as unactivated substrates. [ABSTRACT FROM AUTHOR]

AKB48 is a designer drug belonging to the indazole synthetic cannabinoids class, illegally sold as herbal blend, incense, or research chemicals for their psychoactive cannabis-like effects. In the present study, we investigated the in vivo pharmacological and behavioral effects of AKB48 in male rats and measured the pharmacodynamic effects of AKB48 and simultaneously determined its plasma pharmacokinetic. AKB48 at low doses preferentially stimulated dopamine release in the nucleus accumbens shell (0.25 mg/kg) and impaired visual sensorimotor responses (0.3 mg/kg) without affecting acoustic and tactile reflexes, which are reduced only to the highest dose tested (3 mg/kg). Increasing doses (0.5 mg/kg) of AKB48 impaired place preference and induced hypolocomotion in rats. At the highest dose (3 mg/kg), AKB48 induced hypothermia, analgesia, and catalepsy; inhibited the startle/pre-pulse inhibition test; and caused cardiorespiratory changes characterized by bradycardia and mild bradipnea and SpO2 reduction. All behavioral and neurochemical effects were fully prevented by the selective CB1 receptor antagonist/inverse agonist AM251. AKB48 plasma concentrations rose linearly with increasing dose and were correlated with changes in the somatosensory, hypothermic, analgesic, and cataleptic responses in rats. For the first time, this study shows the pharmacological and behavioral effects of AKB48 in rats, correlating them to the plasma levels of the synthetic cannabinoid. Chemical Compound Studied in This Article: AKB48 (PubChem CID: 57404063); AM251 (PubChem CID: 2125). [ABSTRACT FROM AUTHOR]

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Pseudomonas aeruginosa is a Gram-negative bacterium that commonly infects subjects with weakened immune system causing deadly infections above all at pulmonary level. During infection, P. aeruginosa produces a well-organized bacterial structure, called biofilm, activating the quorum-sensing (QS) signaling, a mechanism of gene regulation. In this work, we synthesized already known QS inhibitors (QSi) designed on the scaffold of the N-(3-oxododecanoyl) homoserine lactone (3O-C12-HSL) QS molecule and conjugated them with ciprofloxacin to inhibit P. aeruginosa biofilm formation and increase the antibiotic susceptibility of clinical strains. We identified, for the first time, a QSi conjugated with ciprofloxacin (ET37), that is able to reduce the formation of biofilm and the onset of tolerant clones in P. aeruginosa clinical strains. This compound could have a wide application in clinical setting. The possibility to affect biofilm formation in chronically infected patients, such as patients affected by cystic fibrosis, and to reduce the onset of ciprofloxacin resistance would improve patient healing and allow to decrease antibiotic drug dosage. [ABSTRACT FROM AUTHOR]

Background: New approaches based on the receptor-targeted molecular interaction have been recently developed with the aim to investigate specific probes for sentinel lymph nodes. In particular, the mannose receptors expressed by lymph node macrophages became an attractive target and different multifunctional mannose derivate ligands for the labeling with 99mTc have been developed. In this study, we report the synthesis of a specific class of dextran-based, macromolecular, multifunctional ligands specially designed for labeling with the highly stable [99mTc=N]2+ core. Methods: The ligands have been obtained by appending to a macromolecular dextran scaffold pendant arms bearing a chelating moiety for the metallic group and a mannosyl residue for allowing the interaction of the resulting macromolecular 99mTc conjugate with specific receptors on the external membrane of macrophages. Two different chelating systems have been selected, S-methyl dithiocarbazate [H2N-NH-C(=S)SCH3=HDTCZ] and a sequence of two cysteine residues, that in combination with a monophosphine coligand, are able to bind the [99mTc=N]2+ core. Conclusions: High-specific-activity labeling has been obtained by simple mixing and heating of the [99mTc=N]2+ group with the new mannose-dextran derivatives. [ABSTRACT FROM AUTHOR]

Abstract: PEDOT (Poly(3,4‐ethylenedioxythiophene)) is one of the most promising electrode materials for biomedical applications like neural recording and stimulation, thanks to its enhanced biocompatibility and electronic properties. Drug delivery by PEDOT is typically achieved by incorporating drugs as dopants during the electrodeposition procedure and a subsequent release can be promoted by applying a cathodic trigger that reduces PEDOT while enabling the drug to diffuse. This approach has several disadvantages including, for instance, the release of contaminants mainly due to PEDOT decomposition during electrochemical release. Herein we describe a new strategy based on the formation of a chemical linkage between the drug and the conductive polymer. In particular, dexamethasone was successfully integrated into a new electropolymerized PEDOT–Dex composite, leading to a self‐adjusting drug release system based on a biochemically hydrolysable bond between dexamethasone and PEDOT. [ABSTRACT FROM AUTHOR]

This microreview highlights the utility of 1,4‐dithiane‐2,5‐diol (1) as a source for the in situ generation of 2‐mercaptoacetaldehyde (2), a versatile two‐carbon synthon featuring both electrophilic and nucleophilic reaction centres and widely utilized as an attractive platform for the preparation of sulfur‐containing molecules. We discuss the chemistry involved, mainly focusing on its applications to the construction of sulfur‐containing heterocyclic compounds including the thiophene and 1,3‐thiazole families and other different sulfur–nitrogen and sulfur–oxygen heterocycles that continue to be a pillar of organic synthesis as a result of their broad application in organic and medicinal chemistry. [ABSTRACT FROM AUTHOR]

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Direct-fed microbials (DFM) support the health and performance of the herd through different modes of action, including improvements on nutrient digestibility. In fact, Bacillus spp. has been identified as an important enzyme-producing bacteria that could benefit overall nutrient utilization by the beef and dairy cattle herd. Based on this rationale, we hypothesized that incubation of a Bacillus-based DFM would improve nutrient digestibility of feedstuffs often fed to ruminants. Therefore, our objective was to evaluate the effects of a Bacillus-based DFM on in vitro nutrient digestibility of different single feedstuffs. Six individual feedstuffs were sampled from China and South Africa and used herein. Feedstuffs were incubated or not (CON) with a Bacillus-based DFM (DFM; BOVACILLUS; B. licheniformis and B. subtilis; 3.2 × 109 CFU/gram; Chr. Hansen A/S., Hørsholm, Denmark) over a 48-h in vitro period. The dose of DFM was adjusted to the volume of the flasks being used and to represent the commercial dose of 3 grams/head per day (9.6 × 109 CFU/head). In vitro gas production, dry matter (DM), and neutral detergent fiber (NDF) digestibility were evaluated at 24 and 48 h. Data were analyzed using PROC MIXED of SAS (version 9.4). Mean total in vitro gas production increased by 5.1 and 6.5% when DFM was incubated at 24 and 48 h, respectively (P < 0.01). At 24 h, NDF digestibility was 12.6% greater for DFMtreated feedstuffs vs. CON (P = 0.02; 27.7 vs. 24.6% for DFM and CON, respectively), but no effects were observed on DM digestibility (P = 0.26). Conversely, 48-h DM and NDF digestibility were greater for DFM vs. CON (P = 0.05), with improvements that were in the order of 3.7 and 15.1%, respectively. In conclusion, we observed greater in vitro fiber degradability and gas production of feedstuffs collected from China and South Africa over a 48-h period when the DFM BOVACILLUS was added at a dose representative of 9.6 × 109 CFU per head. Greater improvements in fiber degradability are likely due to the enzymes produced by the DFM BOVACILLUS. [ABSTRACT FROM AUTHOR]

Introduction Among novel psychoactive substances notified to EMCDDA and Europol were 1-cyclohexyl-x-methoxybenzene stereoisomers ( ortho, meta , and para). These substances share some structural characteristics with phencyclidine and tramadol. Nowadays, no information on the pharmacological and toxicological effects evoked by 1-cyclohexyl-x-methoxybenzene are reported. The aim of this study was to investigate the effect evoked by each one stereoisomer on visual stimulation, body temperature, acute thermal pain, and motor activity in mice. Methods Mice were evaluated in behavioral tests carried out in a consecutive manner according to the following time scheme: observation of visual placing response, measures of core body temperature, determination of acute thermal pain, and stimulated motor activity. Results All three stereoisomers dose-dependent inhibit visual placing response (rank order: meta > ortho > para), induce hyperthermia at lower and hypothermia at higher doses ( meta > ortho > para) and cause analgesia to thermal stimuli ( para > meta = ortho), while they do not alter motor activity. Conclusions For the first time, this study demonstrates that systemic administration of 1-cyclohexyl-x-methoxybenzene compounds markedly inhibit visual response, promote analgesia, and induce core temperature alterations in mice. This data, although obtained in animal model, suggest their possible hazard for human health (i.e., hyperthermia and sensorimotor alterations). In particular, these novel psychoactive substances may have a negative impact in many daily activities, greatly increasing the risk factors for workplace accidents and traffic injuries. [ABSTRACT FROM AUTHOR]

The ubiquitin-proteasome system has been largely investigated for its key role in protein degradation mechanisms that regulate both apoptosis and cell division. Because of their antitumour activity, different classes of proteasome inhibitors have been identified to date. Some of these compounds are currently employed in the clinical treatment of several types of cancer among which multiple myeloma. Here, we describe the design, chemistry, biological activity and modelling studies of a large series of amino acid derivatives linked to a naphthoquinone pharmacophoric group through variable spacers. Some analogues showed interesting inhibitory potency for the β1 and β5 subunits of the proteasome with IC50values in the sub-µm range. [ABSTRACT FROM PUBLISHER]

Rationale: AKB48 and its fluorinate derivate 5F-AKB48 are two novel synthetic cannabinoids belonging to a structural class with an indazole core structure. They are marketed as incense, herbal preparations or chemical supply for their psychoactive Cannabis-like effects. Objectives: The present study was aimed at investigating the in vitro and in vivo pharmacological activity of AKB48 and 5F-AKB48 in male CD-1 mice and comparing their in vivo effects with those caused by the administration of Δ-THC and JWH-018. Results: In vitro competition binding experiments performed on mouse and human CB and CB receptors revealed a nanomolar affinity and potency of the AKB48 and 5F-AKB48. In vivo studies showed that AKB48 and 5F-AKB48, induced hypothermia, increased pain threshold to both noxious mechanical and thermal stimuli, caused catalepsy, reduced motor activity, impaired sensorimotor responses (visual, acoustic and tactile), caused seizures, myoclonia, hyperreflexia and promoted aggressiveness in mice. Moreover, microdialysis study in freely moving mice showed that systemic administration of AKB48 and 5F-AKB48 stimulated dopamine release in the nucleus accumbens. Behavioural, neurological and neurochemical effects were fully prevented by the selective CB receptor antagonist/inverse agonist AM 251. Conclusions: For the first time, the present study demonstrates the overall pharmacological effects induced by the administration of AKB48 and 5F-AKB48 in mice and suggests that the fluorination can increase the power and/or effectiveness of SCBs. Furthermore, this study outlines the potential detrimental effects of SCBs on human health. [ABSTRACT FROM AUTHOR]

The objective of this study was to compare the efficiency of transfer of selenium (Se) to plasma and milk from inorganic sodium selenite, either free or microencapsulated, and from selenized yeast in dairy cows. The study consisted of an in situ-nylon bags incubation, and in an in vivo experiment to compare the Se status of cows supplemented with either sodium selenite, microencapsulated sodium selenite, or Se yeast. Thirty dairy cows, divided in five groups, were fed the following diets: the control group (CTR) received a total mixed ration supplemented with sodium selenite in order to have 0.3 mg/kg DM of total Se; 0.3M and 0.5M groups received the same control diet supplemented with lipid microencapsulated sodium selenite to provide 0.3 and 0.5 mg/kg DM of total Se, respectively; 0.3Y and 0.5Y groups received selenized yeast to provide 0.3 and 0.5 mg/kg of total Se, respectively. Cows were fed the supplements for 56 days during which milk, blood, and fecal samples were collected weekly to conduct analysis of Se and glutathione peroxidase (GSH-px) activity. Se concentration in the nylon bags was assessed to 72%, 64%, and 40% of the initial value (time 0) after 4, 8, and 24 h of incubation, respectively. In vivo, cows supplemented with 0.3 mg/kg of microencapsulated Se had higher milk Se concentration compared to CTR. The increment was more pronounced at the highest inclusion rate (0.5 mg/kg, 0.5M group). GSH-px activity was not significantly affected by treatments. The results indicate that lipid microencapsulation has the potential to protect nutrients from complete rumen reduction and that Se from microencapsulated selenite is incorporated in milk more efficiently than the free form. Microencapsulated sodium selenite was shown to be comparable to Se-yeast in terms of availability and incorporation in milk when fed at 0.3 mg/kg DM, whereas the inclusion in the diet at 0.5 mg/kg DM resulted in higher plasma and milk concentrations than selenized yeast. [ABSTRACT FROM PUBLISHER]

Aim In vitro and in vivo challenge studies were undertaken to develop an in-feed additive of microencapsulated propionic, sorbic acids and pure botanicals to control Campylobacter jejuni in broilers at slaughter age. Methods and Results Organic acids ( OA) and pure botanicals were tested in vitro against Camp. jejuni, whereas in vivo, chickens were fed either a control diet, or increasing doses of the additive for 42 days (experiment 1); in the second experiment, chickens received the additive at 0·1 or 0·3% from day 0 to 21 or from day 22 to 42. The additive consistently reduced Camp. jejuni caecal counts at any given dose (exp. 1) or inclusion plan (exp. 2). Moreover, it was able to reduce the number of goblet cells and modify mucin glycoconjugates biosynthesis pattern. Conclusions We developed an additive that was effective in reducing Camp. jejuni in slaughter-age chickens even at low doses (0·1%). That efficacy was the result of the synergistic action between OA and botanicals. Significance and Impact of the Study This study provides a strategy to reduce Camp. jejuni in broilers and, as a consequence, to improve the safety of the food chain. Moreover, data suggest that a treatment limited to the last weeks before slaughter would allow to save on inclusion of the additive throughout the whole production cycle. [ABSTRACT FROM AUTHOR]

The occurrence and seasonal distribution of 14 pharmaceutical substances of different classes were investigated in two drinking water treatment plants (DWTPs) supplied by the two main Italian rivers, the Po and the Adige (Northern Italy). The therapeutic categories of the selected pharmaceuticals included anti-inflammatory drugs, β-blockers, lipid regulators, diuretics, anti-epileptics, antibiotics and a steroidal hormone. The named compounds were assessed in samples collected from the river water inlet and after each purification stage (sand filtration, ozone treatment, granular active carbon (GAC)). Six of the 14 selected pharmaceuticals were found in all analysed samples, with concentration levels ranging from 1 ng l-1 for atorvastatin to 69 ng l-1 for atenolol in the drinking water produced. The granular active carbon stage resulted the most efficient in eliminating the examined chemicals from the water (removal range: 12-95%, average: 68%), while the sand filtration stage resulted the least effective treatment (removal range: 4-37%, average: 13%). The observed differences between winter and summer conditions, in terms of residual concentrations and number of detected analytes, seemed to depend mainly on the quality of the river water supplies. To the best of our knowledge, these are the first reported data on the presence of pharmaceuticals in drinking water obtained from the water treatment of these two rivers. [ABSTRACT FROM AUTHOR]

Studies the stimulatory effects of fasting on vascular endothelial growth factor production by growing pig ovarian follicles. Measurement of the concentration of VEGF and albumin; Alteration in steroidogenic enzymatic cascade.

2,3-dihydroxy-2-methylbutyric acid, also known as 2,3-dimethylglyceric acid, constitutes the acyl and/or the alcoholic moiety of many bioactive natural esters. Herein, we describe a chemoenzymatic methodology which gives access to all the four possible stereoisomers of the 2,3-dimethylglyceric acid ethyl ester. The racemic ethyl α-acetolactate, produced by the N-heterocycle carbene (NHC)-catalyzed coupling of ethyl pyruvate and methylacetoin was employed as the starting material. The racemic mixture was resolved through (S)-selective reductions, promoted by the acetylacetoin reductase (AAR) affording the resulting ethyl (2R,3S)-2,3-dimethylglycerate; the isolated remaining (S)-ethyl α-acetolactate was successively treated with baker's yeast to obtain the corresponding (2S,3S) stereoisomer. syn-2,3-Dimethylgliceric acid ethyl ester afforded by reducing the rac-α-acetolactate with NaBH4 in the presence of ZnCl2 was kinetically resolved through selective acetylation with lipase B from Candida antarctica (CAL-B) and vinyl acetate to access to (2S,3R) stereoisomer. Finally, the (2R,3R) stereoisomer, was prepared by C3 epimerization of the (2R,3S) stereoisomer recovered from the above kinetic resolution, achieved through the TEMPO-mediated oxidation, followed by the reduction of the produced ketone with NaBH4. The resulting 2,3-dimethylglycertate enriched in the (2R,3R) stereoisomer was submitted to stereospecicific acetylation with vinyl acetate and CAL-B in order to separate the major stereoisomer. The entire procedure enabled conversion of the racemic α-acetolactate into the four enantiopure stereoisomers of the ethyl 2,3-dihydroxy-2-methylbutyrate with the following overall yields: 42% for the (2R,3S), 40% for the (2S,3S), 42% for the (2S,3R) and 20% for the (2R,3R). [ABSTRACT FROM AUTHOR]