The amidation of fatty acid is an important reaction for synthesis of fatty alkolamines with a variety of pharmacological activities. The objective of this paper was to demonstrate the aminolysis ...direct and solvent of the triglycerides from the patawa oil by heterogeneous catalysis. The results of the amidation direct free solvents were favorable using 5% Al
2
O
3
as catalyst, with a conversion of 94% at 24 h of reaction. After spectroscopic characterization, we decided explore the antimicrobial tests of the fatty amides (FAA) against the
Staphylococcus aureus
strain (ATCC 33591), showing a MIC activity of 1.9612 mg/mL and the fatty ethyl esters (FAEE) a 3.4125 mg/mL MIC. Therefore, the synthesis direct free solvents of FAA by Al
2
O
3
from patawa oil was viable and innovative.
Graphical Abstract
The hypothalamus plays especially important roles in various endocrine, autonomic, and behavioral responses that guarantee the survival of both the individual and the species. In the rat, a distinct ...hypothalamic defensive circuit has been defined as critical for integrating predatory threats, raising an important question as to whether this concept could be applied to other prey species. To start addressing this matter, in the present study, we investigated, in another prey species (the mouse), the pattern of hypothalamic Fos immunoreactivity in response to exposure to a predator (a rat, using the Rat Exposure Test). During rat exposure, mice remained concealed in the home chamber for a longer period of time and increased freezing and risk assessment activity. We were able to show that the mouse and the rat present a similar pattern of hypothalamic activation in response to a predator. Of particular note, similar to what has been described for the rat, we observed in the mouse that predator exposure induces a striking activation in the elements of the medial hypothalamic defensive system, namely, the anterior hypothalamic nucleus, the dorsomedial part of the ventromedial hypothalamic nucleus and the dorsal premammillary nucleus. Moreover, as described for the rat, predator-exposed mice also presented increased Fos levels in the autonomic and parvicellular parts of the paraventricular hypothalamic nucleus, lateral preoptic area and subfornical region of the lateral hypothalamic area. In conclusion, the present data give further support to the concept that a specific hypothalamic defensive circuit should be preserved across different prey species.
Methicillin-resistant Staphylococcus aureus (MRSA) has emerged as a therapeutic problem. In the present study, the molecular characterization by pulsed-field gel electrophoresis of MRSA isolates ...collected from a university hospital revealed that the predominant variant of the Brazilian epidemic clonal complex (BECC) was responsible for the increase in the incidence of MRSA strains, which reached 28% in 1998. It was verified that this predominant variant of the BECC displayed an enhanced ability to produce biofilm on inert polystyrene surfaces and to adhere to and invade epithelial airway cells. These results indicate that MRSA strains belonging to the BECC have evolved advantageous properties that might play a role in their predominance as international nosocomial pathogens
Azadirachta indica (Meliaceae) extracts have been reported to exhibit anti-inflammatory and antinociceptive properties. However, the activities of azadirachtin, a limonoid and the major bioactive ...compound found in the extracts, have been poorly investigated in animal models. In the present study, we investigated the effects induced by azadirachtin in experimental models of pain and inflammation in mice. Carrageenan-induced paw edema and fibrovascular tissue growth induced by subcutaneous cotton pellet implantation were used to investigate the anti-inflammatory activity of azadirachtin in mice. Zymosan-induced writhing and hot plate tests were employed to evaluate the antinociceptive activity. To explore putative mechanisms of action, the level of tumor necrosis factor-α in inflammatory tissue was measured and the effect induced by opioidergic and serotonergic antagonists was evaluated. Previous per os (p. o.) administration of azadirachtin (120 mg/kg) significantly reduced the acute paw edema induced by carrageenan. However, the concomitant increase of the paw concentration of tumor necrosis factor-α induced by this inflammatory stimulus was not reduced by azadirachtin. In addition to inhibiting the acute paw edema induced by carrageenan, azadirachtin (6, 60, and 120 mg/kg) inhibited the proliferative phase of the inflammatory response, as demonstrated by the reduced formation of fibrovascular tissue growth. Azadirachtin (120 mg/kg) also inhibited the nociceptive response in models of nociceptive (hot plate) and inflammatory (writhing induced by zymosan) pain. The activity of azadirachtin (120 mg/kg) in the model of nociceptive pain was attenuated by a nonselective opioid antagonist, naltrexone (10 mg/kg, i. p.), but not by a nonselective serotonergic antagonist, cyproheptadine. In conclusion, this study demonstrates the activity of azadirachtin in experimental models of nociceptive and inflammatory pain, and also in models of acute and chronic inflammation. Finally, multiple mechanisms, including the inhibition of the production of inflammatory mediators and activation of endogenous opioid pathways, may mediate azadirachtin activities in experimental models of inflammation and pain.
Phthalimide analogs have been shown to exhibit anti-inflammatory, analgesic and immunomodulatory activities in different preclinical assays. This study aimed to investigate the potential role of ...2-phthalimidethanol (PTD-OH) and 2-phthalimidethyl nitrate (PTD-NO) in a murine model of antigen-induced articular inflammation.
Articular inflammation was induced by intra-articular injection of methylated bovine serum albumin (mBSA) in the knee joint of immunized male C57BL/6J mice. The animals were pre-treated with PTD-OH or PTD-NO (500mg/kg, per os, - 1h). Nociceptive threshold was measured using an electronic von Frey apparatus. The total number of leukocytes in the synovial cavity was determined. Concentrations of tumor necrosis factor (TNF)-α and CXCL-1 and myeloperoxidase (MPO) activity were determined in periarticular tissue.
Both PTD-OH and PTD-NO inhibited at similar extent the mechanical allodynia, neutrophil recruitment to the synovial cavity and periarticular tissue and TNF-α and CXCL-1 production induced by intra-articular challenge with mBSA in immunized mice.
PTD-OH and PTD-NO exhibit a marked activity in a murine model of antigen-induced articular inflammation in immunized animals. These results reinforce the interest in the investigation of phthalimide analogs devoid of the glutarimide ring as candidates to analgesic and anti-inflammatory drugs.
The reintroduction of thalidomide in the pharmacotherapy greatly stimulated the interest in the synthesis and pharmacological evaluation of phthalimide analogs with new and improved activities and ...also greater safety. In the present study, we evaluated the activities of two phthalimide analogs devoid of the glutarimide ring, namely 2-phthalimidethanol (PTD-OH) and 2-phthalimidethyl nitrate (PTD-NO), in experimental models of inflammatory pain and edema in male C57BL/6J mice. Intraplantar (i.pl.) injection of carrageenan (300μg) induced mechanical allodynia and this response was inhibited by previous per os (p.o.) administration of PTD-OH and PTD-NO (750mg/kg) and also by thalidomide (500 or 750mg/kg). The edema induced by carrageenan was also inhibited by previous p.o. administration of PTD-OH (500 and 750mg/kg) and PTD-NO (125, 250, 500 or 750mg/kg), but not by thalidomide. Carrageenan increased tumor necrosis factor (TNF)-α and CXCL1 concentrations and also the number of neutrophils in the paw tissue. Previous p.o. administration of PTD-NO (500mg/kg) reduced all the parameters, while PTD-OH (500mg/kg) reduced only the accumulation of neutrophils. Thalidomide, on the other hand, was devoid of effect on these biochemical parameters. Plasma concentrations of nitrite were increased after p.o. administration of the phthalimide analog coupled to a NO donor, PTD-NO (500mg/kg), but not after administration of PTD-OH or thalidomide. In conclusion, our results show that small molecules, structurally much simpler than thalidomide or many of its analogs under investigation, exhibit similar activities in experimental models of pain and inflammation. Finally, as there is evidence that the glutarimide moiety contributes to the teratogenic effect of many thalidomide analogs, our results indicate that phthalimide analogs devoid of this functional group could represent a new class of analgesic and anti-inflammatory candidates with potential greater safety.
•2-Phthalimidethanol and 2-phthalimidethyl nitrate reduce inflammatory pain and edema.•2-Phthalimidethyl nitrate reduces TNF-α and CXCL1 concentrations and MPO activity.•2-Phthalimidethyl nitrate increases nitrite concentrations.
Neomitranthes obscura (DC.) N. Silveira is an endemic plant of Brazilian Atlantic Forest and widely spread in the sandbanks of “Restinga de Jurubatiba” National Park. It is popularly known by local ...population as “camboim-de-cachorro” or “cambuí-preto” and recognized by its black ripe fruits. However, specimens with yellow ripe fruits were localized in the “Restinga de Jurubatiba” National Park. The aim of the present study was to evaluate chemical composition of essential oils obtained from leaves and fruits of N. obscura specimens with different fruit color (black and yellow) by GC and GC-MS. Essential oils from leaves of specimens with black and yellow fruits indicated a predominance of sesquiterpenes (81.1% and 84.8%, resp.). Meanwhile, essential oil from black fruits presented a predominance of monoterpenes (50.5%), while essential oil from yellow fruits had sesquiterpenes (39.9%) as major substances. Despite previous studies about this species, including essential oil extraction, to our knowledge this is the first report on N. obscura fruits with different colors. Our results suggest the occurrence of unless two different varieties for this species.
The amidation of fatty acid is an important reaction for synthesis of fatty alkolamines with a variety of pharmacological activities. The objective of this paper was to demonstrate the aminolysis ...direct and solvent of the triglycerides from the patawa oil by heterogeneous catalysis. The results of the amidation direct free solvents were favorable using 5% Al.sub.2O.sub.3 as catalyst, with a conversion of 94% at 24 h of reaction. After spectroscopic characterization, we decided explore the antimicrobial tests of the fatty amides (FAA) against the Staphylococcus aureus strain (ATCC 33591), showing a MIC activity of 1.9612 mg/mL and the fatty ethyl esters (FAEE) a 3.4125 mg/mL MIC. Therefore, the synthesis direct free solvents of FAA by Al.sub.2O.sub.3 from patawa oil was viable and innovative.
The amidation of fatty acid is an important reaction for synthesis of fatty alkolamines with a variety of pharmacological activities. The objective of this paper was to demonstrate the aminolysis ...direct and solvent of the triglycerides from the patawa oil by heterogeneous catalysis. The results of the amidation direct free solvents were favorable using 5% Al.sub.2O.sub.3 as catalyst, with a conversion of 94% at 24 h of reaction. After spectroscopic characterization, we decided explore the antimicrobial tests of the fatty amides (FAA) against the Staphylococcus aureus strain (ATCC 33591), showing a MIC activity of 1.9612 mg/mL and the fatty ethyl esters (FAEE) a 3.4125 mg/mL MIC. Therefore, the synthesis direct free solvents of FAA by Al.sub.2O.sub.3 from patawa oil was viable and innovative. Graphical
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