A new Cu(II) complex with the antihypertensive drug telmisartan, Cu8Tlm16·24H2O (CuTlm), was synthesized and characterized by elemental analysis and electronic, FTIR, Raman and electron paramagnetic ...resonance spectroscopy. The crystal structure (at 120 K) was solved by X-ray diffraction methods. The octanuclear complex is a hydrate of but otherwise isostructural to the previously reported Cu8Tlm16 complex. Cu8Tlm16·24H2O crystallizes in the tetragonal P4/ncc space group with a = b = 47.335(1), c = 30.894(3) Å, Z = 4 molecules per unit cell giving a macrocyclic ring with a double helical structure. The Cu(II) ions are in a distorted bipyramidal environment with a somewhat twisted square basis, cis-coordinated at their core N2O2 basis to two carboxylate oxygen and two terminal benzimidazole nitrogen atoms. Cu8Tlm16 has a toroidal-like shape with a hydrophobic nanometer hole, and their crystal packing defines nanochannels that extend along the crystal c-axis. Several biological activities of the complex and the parent ligand were examined in vitro. The antioxidant measurements indicate that the complex behaves as a superoxide dismutase mimic with improved superoxide scavenger power as compared with native sartan. The capacity of telmisartan and its copper complex to expand human mesangial cells (previously contracted by angiotensin II treatment) is similar to each other. The antihypertensive effect of the compounds is attributed to the strongest binding affinity to angiotensin II type 1 receptor and not to the antioxidant effects. The cytotoxic activity of the complex and that of its components was determined against lung cancer cell line A549 and three prostate cancer cell lines (LNCaP, PC-3, and DU 145). The complex displays some inhibitory effect on the A549 line and a high viability decrease on the LNCaP (androgen-sensitive) line. From flow cytometric analysis, an apoptotic mechanism was established for the latter cell line. Telmisartan and CuTlm show antibacterial and antifungal activities in various strains, and CuTlm displays improved activity against the Staphylococcus aureus strain as compared with unbounded copper(II).
The Large and Small Magellanic Clouds (LMC and SMC) are unique local laboratories for studying the formation and evolution of small galaxies in exquisite detail. The Survey of the MAgellanic Stellar ...History (SMASH) is an NOAO community DECam survey of the Clouds mapping 480 square degrees (distributed over ~2400 square degrees at ~20% filling factor) to ~24th mag in ugriz with the goal of identifying broadly distributed, low surface brightness stellar populations associated with the stellar halos and tidal debris of the Clouds. SMASH will also derive spatially-resolved star formation histories covering all ages out to large radii from the MCs that will further complement our understanding of their formation. Here, we present a summary of the survey, its data reduction, and a description of the first public Data Release (DR1). The SMASH DECam data have been reduced with a combination of the NOAO Community Pipeline, PHOTRED, an automated PSF photometry pipeline based mainly on the DAOPHOT suite, and custom calibration software. The attained astrometric precision is ~15 mas and the accuracy is ~2 mas with respect to the Gaia DR1 astrometric reference frame. The photometric precision is ~0.5-0.7% in griz and ~1% in u with a calibration accuracy of ~1.3% in all bands. The median 5 sigma point source depths in ugriz bands are 23.9, 24.8, 24.5, 24.2, 23.5 mag. The SMASH data already have been used to discover the Hydra II Milky Way satellite, the SMASH 1 old globular cluster likely associated with the LMC, and very extended stellar populations around the LMC out to R~18.4 kpc. SMASH DR1 contains measurements of ~100 million objects distributed in 61 fields. A prototype version of the NOAO Data Lab provides data access, including a data discovery tool, SMASH database access, an image cutout service, and a Jupyter notebook server with example notebooks for exploratory analysis.
Abstract
Mucormycosis is a fungal infection caused by Mucorales, with a high mortality rate. However, only a few virulence factors have been described in these organisms. This study showed that ...deletion of
rfs
, which encodes the enzyme for the biosynthesis of rhizoferrin, a siderophore, in
Mucor lusitanicus
, led to a lower virulence in diabetic mice and nematodes. Upregulation of
rfs
correlated with the increased toxicity of the cell-free supernatants of the culture broth (SS) obtained under growing conditions that favor oxidative metabolism, such as low glucose levels or the presence of H
2
O
2
in the culture, suggesting that oxidative metabolism enhances virulence through rhizoferrin production. Meanwhile, growing
M. lusitanicus
in the presence of potassium cyanide, N-acetylcysteine, a higher concentration of glucose, or exogenous cAMP, or the deletion of the gene encoding the regulatory subunit of PKA (
pkaR1
), correlated with a decrease in the toxicity of SS, downregulation of
rfs
, and reduction in rhizoferrin production. These observations indicate the involvement of the cAMP-PKA pathway in the regulation of rhizoferrin production and virulence in
M. lusitanicus
. Moreover,
rfs
upregulation was observed upon macrophage interaction or during infection with spores in mice, suggesting a pivotal role of
rfs
in
M. lusitanicus
infection.
The objective of the study was to examine the characteristics of randomized controlled trials (RCTs) evaluating physiotherapy interventions for low back pain (LBP) that specified a language-grounded ...eligibility criterion and the proportion of people being excluded consequently.
This is a meta-epidemiological study of RCTs evaluating at least one type of physiotherapy intervention for treatment or prevention of LBP. Records were retrieved from Physiotherapy Evidence Database (PEDro), LILACS, and SciELO from inception to May 2021. We retrieved metadata of each record from PEDro and extracted from included studies: country of recruitment, language-grounded eligibility criterion, and the number of consequent exclusions (if specified).
This study included 2,555 trials. A language-grounded eligibility criterion was specified in 463 trials (18.1%); the proportion was higher in trials conducted in North America and Europe, published after 2000, investigating cognitive and behavioral interventions, and including large sample size. Of these 463 trials, 75 trials (16.2%) reported a total number of 2,152 people being excluded due to lack of language proficiency, equivalent to 12.5% of randomized participants.
Nearly one in five physiotherapy clinical trials on LBP excludes people based on language proficiency, compromising the evidence to manage LBP in minority populations.
Coumarins (2H-chromen-2-one) are oxygen-containing heterocyclic compounds that belong to the benzopyranones family. In this work we have synthesized different coordination complexes with ...coumarin-3-carboxylic acid (HCCA), o-phenanthroline (phen) and zinc(II). In the reported Zn(CCA)2(H2O)2 complex, coumarin-3-carboxylate (CCA) is acting as a bidentate ligand while in the two prepared complexes, Zn(phen)3CCA(NO3) (obtained as a single crystal) and Zn(CCA)2phen.4H2O, CCA is acting as a counterion of the complex cation Zn(phen)3+2 or coordinated to the metal center along with phen, respectively. These compounds were characterized on the basis of elemental analysis and thermogravimetry. NMR, FTIR and Raman spectroscopies of the compounds and the CCA potassium salt (KCCA) allow to determine several similarities and differences among them. Finally, their behavior against alkaline phosphatase enzyme and their antimicrobial activities were also measured.
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•Zn coumarin-3-carboxylate o-phenanthroline compounds•Vibrational determinations based in bond length•NMR characterization•Antimicrobial activities and behavior against alkaline phosphatase
Aedes aegypti control programs require more sensitive tools in order to survey domestic and peridomestic larval habitats for dengue and other arbovirus prevention areas. As a consequence of the ...COVID-19 pandemic, field technicians have faced a new occupational hazard during their work activities in dengue surveillance and control. Safer strategies to monitor larval populations, in addition to minimum householder contact, are undoubtedly urgently needed. Drones can be part of the solution in urban and rural areas that are dengue-endemic. Throughout this study, the proportion of larvae breeding sites found in the roofs and backyards of houses were assessed using drone images. Concurrently, the traditional ground field technician’s surveillance was utilized to sample the same house groups. The results were analyzed in order to compare the effectiveness of both field surveillance approaches. Aerial images of 216 houses from El Vergel village in Tapachula, Chiapas, Mexico, at a height of 30 m, were obtained using a drone. Each household was sampled indoors and outdoors by vector control personnel targeting all the containers that potentially served as Aedes aegypti breeding sites. The main results were that the drone could find 1 container per 2.8 found by ground surveillance; however, containers that were inaccessible by technicians in roofs and backyards, such as plastic buckets and tubs, disposable plastic containers and flowerpots were more often detected by drones than traditional ground surveillance. This new technological approach would undoubtedly improve the surveillance of Aedes aegypti in household environments, and better vector control activities would therefore be achieved in dengue-endemic countries.
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•Temperature and vegetation effects are keys to control marching locust bands.•A band of south American locust in Argentina displayed thermoregulation behaviours.•Gut contents at ...different times of the day showed continuous feeding activity.•Walking speed and travelled distances of the band decreased with vegetation density.•Marching and thermoregulation are similar for south American and desert locust.
At high density, juvenile locusts create marching hopper bands. Understanding the roles of temperature and vegetation on the movement of these bands shall allow to better forecast and control them. Following a hopper band in North Argentina in November 2019, we explored the thermoregulation behaviours of the South American locust, Schistocerca cancellata. Gut-content samples informed about the feeding status at different time of the day. Hoppers’ body temperature was above cold air temperature in the mornings during basking and group-basking activities and before the onset of marching behaviour. Marching by walking or hopping was dominant at body temperatures close to 40 °C. Jumping, stilting, shading and perching on plants were seen as thermoregulatory behaviours to avoid ground temperatures above 50 °C. Feeding was observed throughout the day with continuous high gut contents despite an intermittent pattern of feeding-resting-marching. Speed and daily travelled distance of the front of the hopper band was depending on the type of encountered vegetation. Daily behavioural patterns, thermoregulatory behaviours, walking speed and daily travelled distances of S. cancellata were similar to the ones observed for the Desert locust, S. gregaria, in Africa. High air temperatures recorded during the observation times could explain the continuous feeding patterns. These species may have evolved behaviours of alternating consuming a bit and marching as a migration strategy to avoid staying where no food is available after the havoc left behind large hopper bands. Recommendations made for the control of Desert locust hopper bands can be extended to South American locust ones.
To improve the antidepressant action of sertraline a new salt with coumarin-3-carboxylate anion (SerH-CCA) has been synthesized by two different methods and characterized by FTIR spectroscopy and ...structural determinations by X-ray diffraction methods. The new salt is stabilized by strong intermolecular H-bonds involving the protonated amine group of SerH and the deprotonated carboxylate group of CCA. These findings can be correlated with the interpretation of the infrared spectrum. The salt, sertraline (SerHCl) and the sodium salt of coumarin-3-carboxylate (NaCCA) were orally administered male Wistar rats (10 mg/kg, based on sertraline). Rats were evaluated in separate groups by means of the forced swimming (FST). SerH-CCA produced antidepressant effects in a magnitude that exceeded SerHCl individual effects. None of these treatments affected activity levels by the open field OFT tests. We have also determined that the ion pair also improve the binding to bovine serum albumin (BSA) of the drug but retain its antimicrobial activity. It is reasonable to conclude that the replacement of chloride anion by a large organic anion in sertraline strengthens the pharmacological action of the native drug, binding to BSA with higher activity and retaining the antimicrobial activity of the antidepressant compound.
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•New ion pair between sertraline cation and coumarin 3- carboxylate.•Crystal structure and FTIR determinations showed strong intermolecular H-bonds.•Higher binding constant to BSA indicated changes in transport and disposition.•The ion pair displays nearly the same antimicrobial effect than the commercial drug.•The antidepressant action of the native drug has been improved.
•Three new ternary complexes of sulfaquinoxaline were synthesized and characterized.•Intra and intermolecular contacts stabilize the crystal structure of the complexes.•Zn complex is more cytotoxic ...against tumoral cells than the Ni and Cu compounds.
Three monomeric ternary complexes of Ni(II) (1), Cu(II) (2), and Zn(II) (3) with sulfaquinoxaline (SQO), and 2,2’-bipyrimidine (bpm) as ligands have been prepared and their crystal structures have been determined. The complexes are formulated as M(SQO)2bpm·2H2O, completing MN6 coordination spheres. Hirshfeld surface analysis was employed to study the intermolecular interactions in the crystal lattices of the compounds. From these studies, it was found that hydrogen bonding and π-stacking interactions play an important role. Besides, the complexes have been characterized by FTIR and UV-Visible spectroscopies, and thermogravimetric techniques. The cytotoxicity of the complexes was screened against the tumoral A549 (human lung adenocarcinoma) and MG-63 (human osteosarcoma) cell lines. The complexes showed enhanced antibacterial activity against S. aureus and S. epidermidis as compared with the free SQO ligand.
In the first half of the twentieth century, the South American Locust (SAL), Schistocerca cancellata (Serville, 1838), was a major pest of agriculture in Argentina, Bolivia, Paraguay, Uruguay, and ...Brazil. From 1954–2014, a preventive management program appeared to limit SAL populations, with only small- to moderate-scale treatments required, limited to outbreak areas in northwest Argentina. However, the lack of major locust outbreaks led to a gradual reduction in resources, and in 2015, the sudden appearance of swarms marked the beginning of a substantial upsurge, with many swarms reported initially in Argentina in 2015, followed by expansion into neighboring countries over the next few years. The upsurge required a rapid allocation of resources for management of SAL and a detailed examination of the improvements needed for the successful management of this species. This paper provides a review of SAL biology, management history, and perspectives on navigating a plague period after a 60-year recession.
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