RÉSUMÉ
A library of novel bis-Schiff base derivatives based on thiobarbituric acid has been effectively synthesized by multi-step reactions as part of our ongoing pursuit of novel anti-diabetic agents. All these derivatives were subjected to in vitro α-glucosidase inhibitory potential testing after structural confirmation by modern spectroscopic techniques. Among them, compound 8 (IC50 = 0.10 ± 0.05 µM), and 9 (IC50 = 0.13 ± 0.03 µM) exhibited promising inhibitory activity better than the standard drug acarbose (IC50 = 0.27 ± 0.04 µM). Similarly, derivatives (5, 6, 7, 10 and 4) showed significant to good inhibitory activity in the range of IC50 values from 0.32 ± 0.03 to 0.52 ± 0.02 µM. These derivatives were docked with the target protein to elucidate their binding affinities and key interactions, providing additional insights into their inhibitory mechanisms. The chemical nature of these compounds were reveal by performing the density functional theory (DFT) calculation using hybrid B3LYP functional with 6-311++G(d,p) basis set. The presence of intramolecular H-bonding was explored by DFT-d3 and reduced density gradient (RGD) analysis. Furthermore, various reactivity parameters were explored by performing TD-DFT at CAM-B3LYP/6-311++G(d,p) method.
Sujet(s)
Inhibiteurs des glycoside hydrolases , Thiobarbituriques , alpha-Glucosidase , alpha-Glucosidase/métabolisme , Simulation de docking moléculaire , Inhibiteurs des glycoside hydrolases/composition chimique , Bases de Schiff/composition chimique , Relation structure-activité , Structure moléculaireRÉSUMÉ
Fluorinated and formaldehyde-based compounds impart excellent hydrophobicity and flame-retardant properties to cotton fabrics. However, they come with various health and environmental risks. A novel hydrophobic, flame retardant, and antimicrobial finishing agent free from fluorine and formaldehyde was synthesized. The diammonium phosphate octadecyl citrate (DAPOC) was synthesized by using stearic acid (octadecanoic acid), citric acid (propane-1,2,3-tricarboxylic acid), and diammonium hydrogen phosphate. It was grafted onto the cotton fabrics by employing the conventional pad-dry-cure method. The results indicated that this newly developed finish could be chemically bonded to cotton fabrics through C-O-C covalent bonds. The contact angle of the cotton fabric finished with a 12% concentration of the finishing agent reached 151.9°. Additionally, the finished cotton fabrics displayed evident flame-retardant properties. After undergoing 20 laundering cycles, DAPOC maintained strong hydrophobic and flame-retardant characteristics, demonstrating its durability. The chemical structure of DAPOC was verified by nuclear magnetic resonance spectroscopy (1H-NMR). The thermogravimetric analysis confirmed the flame-retardant nature of the treated cotton fabric samples. Scanning electron microscopy (SEM), Energy dispersive X-ray analysis (EDX), and Fourier-transform infrared spectroscopy (FTIR) results demonstrated the successful grafting of the newly created finish onto the cotton fiber. X-ray diffraction (XRD) spectra depicted that the crystalline structure of finished cotton fabric remained mostly unaltered. Furthermore, the finished cotton fabric exhibited commendable antimicrobial properties due to the inclusion of citric acid.
RÉSUMÉ
BACKGROUND Cerebral malaria is a lethal complication of Plasmodium falciparum infections in need of better therapies. Previous work in murine experimental cerebral malaria (ECM) indicated that the combination of artemether plus intraperitoneal whole blood improved vascular integrity and increased survival compared to artemether alone. However, the effects of blood or plasma transfusion administered via the intravenous route have not previously been evaluated in ECM. OBJECTIVES To evaluate the effects of intravenous whole blood compared to intravenous plasma on hematological parameters, vascular integrity, and survival in artemether-treated ECM. METHODS Mice with late-stage ECM received artemether alone or in combination with whole blood or plasma administered via the jugular vein. The outcome measures were hematocrit and platelets; plasma angiopoietin 1, angiopoietin 2, and haptoglobin; blood-brain barrier permeability; and survival. FINDINGS Survival increased from 54% with artemether alone to 90% with the combination of artemether and intravenous whole blood. Intravenous plasma lowered survival to 18%. Intravenous transfusion provided fast and pronounced recoveries of hematocrit, platelets, angiopoietins levels and blood brain barrier integrity. MAIN CONCLUSIONS The outcome of artemether-treated ECM was improved by intravenous whole blood but worsened by intravenous plasma. Compared to prior studies of transfusion via the intraperitoneal route, intravenous administration was more efficacious.
RÉSUMÉ
Abstract In Brazil, species of the genus Ramphocelus with the presence of various endoparasites have already been reported. Coccidia have been the parasites most frequently found. All species of this genus have similar habitats and ecological niches, which makes parasite transmission easy. The aim of this study was to diagnose the presence of endoparasites in fecal samples from specimens of Ramphocelus carbo that were caught in the Cazumbá-Iracema Extractive Reserve (Cazumbá Resex), in the State of Acre. The specimens (n = 30) were caught in mist nets arranged in different ecosystems of the Reserve. After identification, the bird specimens were placed in cloth bags for a maximum of 30 minutes to collect feces. Among the 22 samples collected, 63.63% (n = 14) were positive for endoparasites. The coccidia were the parasites most frequently. Helminths belonging to Ascaridiidae (Nematoda), Strongylida (Nematoda) and Davaneidae (Cestoda) were recorded for the first time in R. carbo in the State of Acre. Parasites belonging to Strongylida and Davaneidae were recorded for the first time in a species of Ramphocelus. These findings add information on the parasitic fauna of wild birds, since in the Amazon region there are few studies on this subject.
Resumo No Brasil, espécies do gênero Ramphocelus ja foram relatadas com a presença de vários endoparasitos, sendo os coccídios os parasitos mais frequentes. Todas as espécies do gênero possuem habitats e nichos ecológicos semelhantes, facilitando a transmissão desses parasitos. O presente estudo teve como objetivo diagnosticar a presença de endoparasitos em amostras fecais de Ramphocelus carbo capturadas na Reserva Extrativista Cazumbá-Iracema (Resex do Cazumbá), localizada no estado do Acre. Os espécimes (n=30) foram capturados em redes de neblina dispostas em diferentes ecossistemas da Reserva. Após a identificação das aves, os espécimes foram colocadas em sacos de pano por no máximo 30 minutos para coleta das fezes. Das 22 amostras coletadas, 63,63% (n = 14) foram positivas para endoparasitas. Os coccídíos foram os parasitos mais frequentes. Os helmintos Ascaridiidae (Nematoda), Strongylida(Nematoda) e Davaneidae (Cestoda) foram registrados pela primeira vez em R. carbo, no estado do Acre. Strongylida e Davaneidae são registrados pela primeira vez em uma espécie pertencente a Ramphocelus. Esses achados acrescentam informações sobre a fauna parasitária de aves silvestres, pois na Amazônia existem poucos estudos nessa área.
Sujet(s)
Animaux , Maladies des oiseaux/parasitologie , Passeriformes/parasitologie , Helminthoses animales/parasitologie , Helminthes/isolement et purification , Helminthes/classification , BrésilRÉSUMÉ
BACKGROUND: The outbreak of dengue during 2017 in Sri Lanka is the worst incidence of this mosquito-borne virus infection in the South Asian country since records began. METHODS: In this retrospective study, up to the end of December 2017 over 185,000 clinical cases were reported from all regions of the island nation. RESULTS: This crisis placed an overwhelming burden on Sri Lanka's public health system and also had a significant negative impact on its economy. CONCLUSIONS: The unsurpassed level of morbidity and mortality has highlighted the pressing need for an effective operational plan to both manage the existing outbreak and to reduce the threat of a future episode of disease. This should involve an integrated nationwide program of vector surveillance and control, tertiary care of severely affected individuals and the implementation of measures to prevent future infectio ns, including widespread vaccination.