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1.
Nutrients ; 13(12)2021 Dec 01.
Artigo em Inglês | MEDLINE | ID: mdl-34959892

RESUMO

Bariatric surger (BS) is characterized by lipid metabolic changes as a response to the massive release of non-esterified fatty acids (NEFA) from adipose depots. The study aimed at evaluating changes in polyunsaturated fatty acids (PUFA) metabolism and biosynthesis of the lipid mediators N-acylethanolamines (NAE), as indices of nuclear peroxisome proliferator-activated receptor (PPAR)-α activation. The observational study was performed on 35 subjects (27 female, 8 male) with obesity, undergoing bariatric surgery. We assessed plasma FA and NAE profiles by LC-MS/MS, clinical parameters and anthropometric measures before and 1 and 6 months after bariatric surgery. One month after bariatric surgery, as body weight and clinical parameters improved significantly, we found higher plasma levels of N-oleoylethanolamine, arachidonic and a 22:6-n3/20:5-n3 ratio as evidence of PPAR-α activation. These changes corresponded to higher circulating levels of NEFA and a steep reduction of the fat mass. After 6 months 22:6-n3/20:5-n3 remained elevated and fat mass was further reduced. Our data suggest that the massive release of NEFA from adipose tissue at 1-Post, possibly by inducing PPAR-α, may enhance FA metabolism contributing to fat depot reduction and improved metabolic parameters in the early stage. However, PUFA metabolic changes favor n6 PUFA biosynthesis, requiring a nutritional strategy aimed at reducing the n6/n3 PUFA ratio.


Assuntos
Cirurgia Bariátrica , Ácidos Graxos Insaturados/metabolismo , Obesidade/metabolismo , PPAR alfa/metabolismo , Tecido Adiposo/metabolismo , Adulto , Ácido Araquidônico/metabolismo , Composição Corporal , Endocanabinoides/metabolismo , Etanolaminas/metabolismo , Feminino , Humanos , Masculino , Ácidos Oleicos/metabolismo , Período Pós-Operatório
2.
Int J Mol Sci ; 22(21)2021 Oct 21.
Artigo em Inglês | MEDLINE | ID: mdl-34768820

RESUMO

Disseminated intravascular coagulation (DIC) is a severe condition characterized by the systemic formation of microthrombi complicated with bleeding tendency and organ dysfunction. In the last years, it represents one of the most frequent consequences of coronavirus disease 2019 (COVID-19). The pathogenesis of DIC is complex, with cross-talk between the coagulant and inflammatory pathways. The objective of this study is to investigate the anti-inflammatory action of ultramicronized palmitoylethanolamide (um-PEA) in a lipopolysaccharide (LPS)-induced DIC model in rats. Experimental DIC was induced by continual infusion of LPS (30 mg/kg) for 4 h through the tail vein. Um-PEA (30 mg/kg) was given orally 30 min before and 1 h after the start of intravenous infusion of LPS. Results showed that um-PEA reduced alteration of coagulation markers, as well as proinflammatory cytokine release in plasma and lung samples, induced by LPS infusion. Furthermore, um-PEA also has the effect of preventing the formation of fibrin deposition and lung damage. Moreover, um-PEA was able to reduce the number of mast cells (MCs) and the release of its serine proteases, which are also necessary for SARS-CoV-2 infection. These results suggest that um-PEA could be considered as a potential therapeutic approach in the management of DIC and in clinical implications associated to coagulopathy and lung dysfunction, such as COVID-19.


Assuntos
Amidas/uso terapêutico , Transtornos da Coagulação Sanguínea/tratamento farmacológico , Coagulação Intravascular Disseminada/tratamento farmacológico , Etanolaminas/uso terapêutico , Ácidos Palmíticos/uso terapêutico , Sepse/complicações , Amidas/química , Amidas/farmacologia , Animais , Transtornos da Coagulação Sanguínea/etiologia , COVID-19/patologia , COVID-19/virologia , Citocinas/sangue , Citocinas/metabolismo , Modelos Animais de Doenças , Coagulação Intravascular Disseminada/etiologia , Etanolaminas/química , Etanolaminas/farmacologia , Produtos de Degradação da Fibrina e do Fibrinogênio/metabolismo , Lipopolissacarídeos/toxicidade , Pulmão/metabolismo , Pulmão/patologia , Masculino , Mastócitos/citologia , Mastócitos/efeitos dos fármacos , Mastócitos/metabolismo , Ácidos Palmíticos/química , Ácidos Palmíticos/farmacologia , Tempo de Tromboplastina Parcial , Tempo de Protrombina , Ratos , Ratos Sprague-Dawley , SARS-CoV-2/isolamento & purificação , Sepse/patologia , Serina Proteases/metabolismo
3.
Molecules ; 26(21)2021 Nov 03.
Artigo em Inglês | MEDLINE | ID: mdl-34771072

RESUMO

The synthesis of nanoparticles is most important in the context of cancer therapy, particularly copper nanoparticles, which are widely used. In this work, copper(II)-tyrosinase was isolated from potato peel powder. Copper nanoparticles (Tyr-Cu(II)-AEEA NPs) were synthesized via the reaction of tyrosinase with N-aminoethylethanolamine to produce Cu(II)-NPs and these were characterized by means of FT-IR, UV-Spectroscopy, XRD, SEM, TEM and a particle size analyzer. These Tyr-Cu(II)-AEEA NPs were tested as anticancer agents against MCF-7 breast cancer cells. Fluorescence microscopy and DNA fragmentation were also performed, which revealed the inhibiting potentials of Cu(II)-AEEA NPs and consequent cell death; Tyr-Cu(II)-AEEA NPs show potential cytotoxicity activity and this nano material could be contemplated as an anticancer medicament in future investigations.


Assuntos
Antineoplásicos/farmacologia , Complexos de Coordenação/farmacologia , Cobre/farmacologia , Etanolaminas/farmacologia , Nanopartículas Metálicas/química , Monofenol Mono-Oxigenase/metabolismo , Solanum tuberosum/metabolismo , Antineoplásicos/química , Antineoplásicos/metabolismo , Proliferação de Células/efeitos dos fármacos , Complexos de Coordenação/química , Complexos de Coordenação/metabolismo , Cobre/química , Cobre/metabolismo , Ensaios de Seleção de Medicamentos Antitumorais , Etanolaminas/química , Etanolaminas/metabolismo , Feminino , Humanos , Células MCF-7 , Microscopia de Fluorescência , Solanum tuberosum/química
4.
Int J Mol Sci ; 22(19)2021 Oct 03.
Artigo em Inglês | MEDLINE | ID: mdl-34639071

RESUMO

The search for methods of cognitive impairment treatment and prevention in neurological and neurodegenerative diseases is an urgent task of modern neurobiology. It is now known that various diseases, accompanied by dementia, exhibit a pronounced neuroinflammation. Considering the significant docosahexaenoic and eicosapentaenoic polyunsaturated fatty acids' therapeutic potential, we decided to investigate and compare anti-inflammatory activity of their N-acylethanolamine derivatives. As a result, we found that both N-docosahexaenoylethanolamine (synaptamide) and N-eicosapentaenoylethanolamine (EPEA) prevents an LPS-mediated increase in the proinflammatory cytokines TNF-α and IL-6 production in the SIM-A9 microglia culture. In an in vivo experiment, synaptamide reversed an increase in LPS-mediated hippocampal TNF-α and IL-1ß, but EPEA did not. However, both compounds contributed to the microglia polarization towards the M2-phenotype. Synaptamide, rather than EPEA, inhibited the Iba-1-positive microglia staining area increase. However, both synaptamide and EPEA prevented the LPS-mediated astrogliosis. A study of BDNF immunoreactivity showed that synaptamide, but not EPEA, reversed an LPS-mediated decrease in BDNF production. Despite the more pronounced anti-inflammatory activity of synaptamide, both compounds were effective in maintaining a normal level of hippocampal long-term potentiation in neuroinflammation. The results indicate a high therapeutic potential for both compounds. However, some tests have shown higher activity of synaptamide compared to EPEA.


Assuntos
Anti-Inflamatórios/farmacologia , Etanolaminas/farmacologia , Inflamação/etiologia , Inflamação/metabolismo , Lipopolissacarídeos/efeitos adversos , Animais , Biomarcadores , Fator Neurotrófico Derivado do Encéfalo/metabolismo , Citocinas/metabolismo , Modelos Animais de Doenças , Imuno-Histoquímica , Inflamação/diagnóstico , Inflamação/tratamento farmacológico , Mediadores da Inflamação/metabolismo , Camundongos , Microglia/metabolismo , Resultado do Tratamento
5.
Anal Methods ; 13(39): 4557-4584, 2021 10 14.
Artigo em Inglês | MEDLINE | ID: mdl-34611673

RESUMO

Malaria is a life-threatening disease being treated by oral medication. This is the best treatment to reduce morbidity and mortality, prevent disease progression to the most severe form, lower the transmission of the disease and hinder the appearance of strains resistant to antimalarials. According to the World Health Organization, the most common antimalarial drugs are chloroquine, primaquine, mefloquine, lumefantrine, artemether, and artesunate in single dosage forms or fixed-dose combination. Within this context, the present review aims to show the evolution of different analytical methods that have been applied to the determination of these antimalarial drugs in pharmaceutical formulations and human blood by liquid chromatography in the last 10 years, along with statistical analyses of the methods.


Assuntos
Antimaláricos , Artemisininas , Malária Falciparum , Antimaláricos/uso terapêutico , Artemisininas/uso terapêutico , Cromatografia Líquida , Composição de Medicamentos , Etanolaminas/uso terapêutico , Fluorenos/uso terapêutico , Humanos , Malária Falciparum/tratamento farmacológico
6.
Parasite ; 28: 67, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34569928

RESUMO

BACKGROUND: Artemisinin-based treatment in malaria patients with abnormal hemoglobin may be ineffective because of their genetic particularity, which could lead to resistance. The main purpose of this study was to assess the effect of artemisinin derivatives on in vivo parasite clearance according to erythrocyte variants. In vivo response was investigated through retrospective data obtained over a 42-day artemether-lumefantrine/artesunate amodiaquine efficacy protocol conducted from 2012 to 2016. RESULTS: A total of 770 patients in Côte d'Ivoire attending the hospitals of Anonkoua-koute (Abidjan), Petit Paris (Korhogo), Libreville (Man), Dar es salam (Bouaké), Ayamé and Yamoussoukro with acute uncomplicated falciparum malaria were selected for successful hemoglobin typing. HbAS, HbSS, HbAC, and HbSC genotypes were found. Parasite clearance time was obtained for 414 patients. In the population with abnormal hemoglobin, parasite densities on admission and parasite clearance rates were significantly lower in the HbSC group compared to HbAA (p = 0.02 and p = 0.007, respectively). After PCR correction on day 42, the acute treatment rate was 100% for each group. Parasite half-life and time for initial parasitaemia to decline by 50 and 99% were longer for the HbSC group (p < 0.05). The study also investigated the prevalence of K13-propeller polymorphisms across different hemoglobin genotype groups. A total of 185 and 63 samples were sequenced in the HbAA group and patients with abnormal Hb, respectively. Only two nonsynonymous mutations D559N and V510M were found in the HbAA group. CONCLUSION: Although this study proved good efficacy of artemether-lumefantrine and artesunate amodiaquine in the treatment of uncomplicated Plasmodium falciparum malaria in patients with abnormal hemoglobin, the increased delay of parasite clearance may represent a threat to health in these patients in relation with sickle cell crisis, which could support selection of parasites resistant to artemisinin.


Assuntos
Antimaláricos , Artemisininas , Hemoglobinas Anormais , Malária Falciparum , Antimaláricos/uso terapêutico , Artemeter/uso terapêutico , Combinação Arteméter e Lumefantrina , Artemisininas/uso terapêutico , Costa do Marfim/epidemiologia , Combinação de Medicamentos , Etanolaminas/uso terapêutico , Hemoglobinas Anormais/uso terapêutico , Humanos , Malária Falciparum/tratamento farmacológico , Malária Falciparum/epidemiologia , Plasmodium falciparum/genética , Estudos Retrospectivos , Resultado do Tratamento
7.
Molecules ; 26(17)2021 Aug 27.
Artigo em Inglês | MEDLINE | ID: mdl-34500646

RESUMO

Arachidonylethanolamide (anandamide) acts as an endogenous ligand of cannabinoid receptors, while other N-acylethanolamines (NAEs), such as palmitylethanolamide and oleylethanolamide, show analgesic, anti-inflammatory, and appetite-suppressing effects through other receptors. In mammalian tissues, NAEs, including anandamide, are produced from glycerophospholipid via N-acyl-phosphatidylethanolamine (NAPE). The ɛ isoform of cytosolic phospholipase A2 (cPLA2) functions as an N-acyltransferase to form NAPE. Since the cPLA2 family consists of six isoforms (α, ß, γ, δ, ɛ, and ζ), the present study investigated a possible involvement of isoforms other than ɛ in the NAE biosynthesis. Firstly, when the cells overexpressing one of the cPLA2 isoforms were labeled with [14C]ethanolamine, the increase in the production of [14C]NAPE was observed only with the ɛ-expressing cells. Secondly, when the cells co-expressing ɛ and one of the other isoforms were analyzed, the increase in [14C]N-acyl-lysophosphatidylethanolamine (lysoNAPE) and [14C]NAE was seen with the combination of ɛ and γ isoforms. Furthermore, the purified cPLA2γ hydrolyzed not only NAPE to lysoNAPE, but also lysoNAPE to glycerophospho-N-acylethanolamine (GP-NAE). Thus, the produced GP-NAE was further hydrolyzed to NAE by glycerophosphodiesterase 1. These results suggested that cPLA2γ is involved in the biosynthesis of NAE by its phospholipase A1/A2 and lysophospholipase activities.


Assuntos
Etanolaminas/metabolismo , Fosfolipases A2/metabolismo , Isoformas de Proteínas/metabolismo , Aciltransferases/metabolismo , Amidas/metabolismo , Animais , Ácidos Araquidônicos/metabolismo , Linhagem Celular , Endocanabinoides/metabolismo , Etanolamina/metabolismo , Células HEK293 , Humanos , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Ácidos Oleicos/metabolismo , Ácidos Palmíticos/metabolismo , Fosfatidiletanolaminas/metabolismo , Diester Fosfórico Hidrolases/metabolismo , Alcamidas Poli-Insaturadas/metabolismo
8.
J Assoc Physicians India ; 69(4): 11-12, 2021 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-34470194

RESUMO

For decades, short acting beta agonists (SABAs) have been prescribed for giving symptomatic relief to asthmatics. However, this symptomatic benefit perceived by the patient leads to the overuse and dependency of the patient to the SABA inhaler and underusage of the inhaled corticosteroid (ICS) containing controller inhalers resulting in destabilizing disease control and increased risk of exacerbations. In order to address this issue, the 2019 update of the Global Initiative for Asthma (GINA) strategy document no longer recommends the use of SABA inhalers as the preferred reliever for asthma due to concerns around poor outcomes and safety. Instead, it strongly supports the use of a combined ICS-fast acting beta agonist as a reliever also termed as an Anti-inflammatory Reliever Therapy (AIR). In this review we discuss the extent of SABA overusage and its impact on asthma outcomes, the resultant change in the recommendations in the GINA document and finally the evidence supporting the use of formoterol- budesonide as AIR therapy.


Assuntos
Antiasmáticos , Asma , Administração por Inalação , Corticosteroides , Antiasmáticos/uso terapêutico , Asma/tratamento farmacológico , Budesonida/uso terapêutico , Combinação de Medicamentos , Etanolaminas/uso terapêutico , Fumarato de Formoterol/uso terapêutico , Humanos , Nebulizadores e Vaporizadores
9.
Biochem Biophys Res Commun ; 577: 32-37, 2021 11 05.
Artigo em Inglês | MEDLINE | ID: mdl-34500233

RESUMO

4,8-Sphingadienines (SD), metabolites of glucosylceramides (GlcCer), are sometimes determined as key mediators of the biological activity of dietary GlcCer, and cis/trans geometries of 4,8-SD have been reported to affect its activity. Since regulating excessive activation of mast cells seems an important way to ameliorate allergic diseases, this study was focused on cis/trans stereoisomeric-dependent inhibitory effects of 4,8-SD on mast cell activation. Degranulation of RBL-2H3 was inhibited by treatment of 4-cis-8-trans- and 4-cis-8-cis-SD, and their intradermal administrations ameliorated ear edema in passive cutaneous anaphylaxis reaction, but 4-trans-8-trans- and 4-trans-8-cis-SD did not. Although the activation of mast cells depends on the bound IgE contents, those stereoisomers did not affect IgE contents on RBL-2H3 cells after the sensitization of anti-TNP IgE. These results indicated that 4-cis-8-trans- and 4-cis-8-cis-SD directly inhibit the activation of mast cells. In conclusion, it was assumed that 4,8-SD stereoisomers with cis double bond at C4-position shows anti-allergic activity by inhibiting downstream pathway after activation by the binding of IgE to mast cells.


Assuntos
Antialérgicos/farmacologia , Degranulação Celular/efeitos dos fármacos , Etanolaminas/farmacologia , Mastócitos/efeitos dos fármacos , Anafilaxia Cutânea Passiva/efeitos dos fármacos , Animais , Antialérgicos/química , Células CACO-2 , Linhagem Celular Tumoral , Orelha/patologia , Edema/prevenção & controle , Etanolaminas/química , Etanolaminas/metabolismo , Feminino , Glucosilceramidas/química , Glucosilceramidas/metabolismo , Glucosilceramidas/farmacologia , Humanos , Mastócitos/fisiologia , Camundongos Endogâmicos BALB C , Estrutura Molecular , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Ratos , Estereoisomerismo
10.
J Neuropsychiatry Clin Neurosci ; 33(4): 328-336, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34340527

RESUMO

OBJECTIVE: There are few effective pharmacological treatments for Tourette's syndrome. Many patients with Tourette's syndrome experience impairing tic symptoms despite use of available evidence-based treatments. The investigators conducted a small, uncontrolled trial to examine the safety, tolerability, and dosing of THX-110, a combination of Δ9-tetrahydracannabinol (Δ9-THC) and palmitoylethanolamide (PEA), in Tourette's syndrome. METHODS: A 12-week uncontrolled trial of THX-110 (maximum daily Δ9-THC dose, 10 mg, and a constant 800-mg dose of PEA) in 16 adults with Tourette's syndrome was conducted. The primary outcome was improvement on the Yale Global Tic Severity Scale (YGTSS) total tic score. Secondary outcomes included measures of comorbid conditions and the number of participants who elected to continue treatment in the 24-week extension phase. RESULTS: Tic symptoms significantly improved over time with THX-110 treatment. Improvement in tic symptoms was statistically significant within 1 week of starting treatment compared with baseline. THX-110 treatment led to an average improvement in tic symptoms of more than 20%, or a 7-point decrease in the YGTSS score. Twelve of the 16 participants elected to continue to the extension phase, and only two participants dropped out early. Side effects were common but were generally managed by decreasing Δ9-THC dosing, slowing the dosing titration, and shifting dosing to nighttime. CONCLUSIONS: Although the initial data from this trial in adults with refractory Tourette's syndrome are promising, future randomized double-blind placebo-controlled trials are necessary to demonstrate efficacy of THX-110 treatment. The challenges raised by the difficulty in blinding trials due to the psychoactive properties of many cannabis-derived compounds need to be further appreciated in these trial designs.


Assuntos
Amidas/uso terapêutico , Agonistas de Receptores de Canabinoides/uso terapêutico , Dronabinol/uso terapêutico , Etanolaminas/uso terapêutico , Ácidos Palmíticos/uso terapêutico , Índice de Gravidade de Doença , Síndrome de Tourette/tratamento farmacológico , Adulto , Método Duplo-Cego , Feminino , Humanos , Masculino , Projetos Piloto , Escalas de Graduação Psiquiátrica , Resultado do Tratamento
11.
Water Res ; 203: 117508, 2021 Sep 15.
Artigo em Inglês | MEDLINE | ID: mdl-34375933

RESUMO

Enteric viruses are commonly present in water bodies in regions with poor sanitation. Although the occurrence of these viruses poses a health risk they are difficult to quantify due to their low concentration and they may remain undetected in the absence of adequate preconcentration. The present study reports the synthesis and utilization of DEAE silica gel (DSiG) as an adsorbent for virus concentration. Two coliphages, MS2 and SUSP2, and an enteric virus, rotavirus A (RVA) were chosen for examining the preconcentration efficiency of DSiG columns. Studies conducted at a low flow rate of 5 mL/min yielded good removal of viruses through adsorption. Studies at a higher flow rate of 50 mL/min followed by elution with optimized eluents yielded a high recovery of MS2 and RVA even when they were present at low concentration (0.01 copy/mL). The eluent Na(1.5 M)-Tw(2%)-G3X (glycine 3X broth, 1.5 M NaCl, 2% Tween, pH 10.2) showed maximum elution of RVA and MS2. Optimal SUSP2 recovery was observed on employing an eluent composed of 1.5 M NaCl, 3% Tween, 0.05 M KH2PO4 at pH 9.2. Subsequently, both the eluents were successively applied for elution of the adsorbed viruses. This method was applied for virus preconcentration from lake water in the monsoon and winter seasons. The DSiG column could achieve adequate preconcentration for all the three viruses, i.e., SUSP2, MS2, and RVA, even when they were present at very low concentration and the recovery achieved was comparable to that achieved with ultracentrifugation while the processing time required for handling large volumes of water was considerably lower.


Assuntos
Rotavirus , Colífagos , Etanolaminas , Concentração de Íons de Hidrogênio , Sílica Gel , Água
12.
Eur J Neurosci ; 54(6): 5932-5950, 2021 09.
Artigo em Inglês | MEDLINE | ID: mdl-34396611

RESUMO

The peroxisome proliferator-activated receptor alpha (PPARα) is a nuclear receptor that has been linked to the modulation of several physiological functions, including the sleep-wake cycle. The PPARα recognizes as endogenous ligands the lipids oleoylethanolamide (OEA) and palmitoylethanolamide (PEA), which in turn, if systemically injected, they exert wake-promoting effects. Moreover, the activation of PPARα by the administration of OEA or PEA increases the extracellular contents of neurotransmitters linked to the control of wakefulness; however, the role of PPARα activated by OEA or PEA on additional biochemicals related to waking regulation, such as acetylcholine (ACh) and 5-hydroxytryptamine (5-HT), has not been fully studied. Here, we have investigated the effects of treatments of OEA or PEA on the contents of ACh and 5-HT by using in vivo microdialysis techniques coupled to HPLC means. For this purpose, OEA or PEA were systemically injected (5, 10 or 30 mg/kg; i.p.), and the levels of ACh and 5-HT were collected from the basal forebrain, a wake-related brain area. These pharmacological treatments significantly increased the contents of ACh and 5-HT as determined by HPLC procedures. Interestingly, PPARα antagonist MK-886 (30 mg/kg; i.p.) injected before the treatments of OEA or PEA blocked these outcomes. Our data suggest that the activation of PPARα by OEA or PEA produces significant changes on ACh and 5-HT levels measured from the basal forebrain and support the conclusion that PPARα is a suitable molecular element involved in the regulation of wake-related neurotransmitters.


Assuntos
PPAR alfa , Serotonina , Acetilcolina , Amidas , Encéfalo/metabolismo , Endocanabinoides , Etanolaminas , Ácidos Oleicos , PPAR alfa/metabolismo , Ácidos Palmíticos
13.
Biomolecules ; 11(8)2021 08 13.
Artigo em Inglês | MEDLINE | ID: mdl-34439873

RESUMO

The diversification of land plants largely relies on their ability to cope with constant environmental fluctuations, which negatively impact their reproductive fitness and trigger adaptive responses to biotic and abiotic stresses. In this limiting landscape, cumulative research attention has centred on deepening the roles of major phytohormones, mostly auxins, together with brassinosteroids, jasmonates, and abscisic acid, despite the signaling networks orchestrating the crosstalk among them are so far only poorly understood. Accordingly, this review focuses on the Arabidopsis Amidase Signature (AS) superfamily members, with the aim of highlighting the hitherto relatively underappreciated functions of AMIDASE1 (AMI1) and FATTY ACID AMIDE HYDROLASE (FAAH), as comparable coordinators of the growth-defense trade-off, by balancing auxin and ABA homeostasis through the conversion of their likely bioactive substrates, indole-3-acetamide and N-acylethanolamine.


Assuntos
Proteínas de Arabidopsis/metabolismo , Arabidopsis/metabolismo , Etanolaminas/metabolismo , Ácidos Indolacéticos/metabolismo , Amidoidrolases/metabolismo , Regulação da Expressão Gênica de Plantas
14.
Nutrients ; 13(8)2021 Jul 28.
Artigo em Inglês | MEDLINE | ID: mdl-34444748

RESUMO

Obesity is currently a major epidemic in the developed world. However, we lack a wide range of effective pharmacological treatments and therapies against obesity, and those approved are not devoid of adverse effects. Dietary components such as palmitoleic acid have been proposed to improve metabolic disbalance in obesity, although the mechanisms involved are not well understood. Both palmitoleic acid (POA) and oleic acid (OA) can be transformed in N-acylethanolamines (NAEs), mediating the effects of dietary POA and OA. To test this hypothesis, here, we study the effects on food intake and body weight gain of palmitoleylethanolamide (POEA) and the OA-derived NAE analogue, oleoylethanolamide (OEA), in Sprague-Dawley rats with a hypercaloric cafeteria diet (HFD). Plasma biochemical metabolites, inflammatory mediators, and lipogenesis-associated liver protein expression were also measured. The results indicate that POEA is able to improve health status in diet-induced obesity, decreasing weight, liver steatosis, inflammation, and dyslipemia. The action of POEA was found to be almost identical to that of OEA, which is an activator of the nuclear peroxisome proliferator receptor alpha (PPARα), and it is structurally related to POEA. These results suggest that the dietary administration of either POA or POEA might be considered as nutritional intervention as complementary treatment for complicated obesity in humans.


Assuntos
Ácidos Graxos Monoinsaturados/farmacologia , Ácidos Graxos Monoinsaturados/uso terapêutico , Obesidade/tratamento farmacológico , Ácidos Oleicos/farmacologia , Ácidos Oleicos/uso terapêutico , Animais , Peso Corporal , Citocinas , Dieta , Endocanabinoides , Etanolaminas , Ácidos Graxos , Fígado Gorduroso/metabolismo , Humanos , Resistência à Insulina , Lipogênese , Fígado/metabolismo , Masculino , Ácido Oleico/uso terapêutico , Ratos , Ratos Sprague-Dawley
15.
Int J Mol Sci ; 22(16)2021 Aug 13.
Artigo em Inglês | MEDLINE | ID: mdl-34445417

RESUMO

This study aimed to assess the neuro-regenerative properties of co-ultramicronized PEALut (Glialia®), composed of palmitoylethanolamide (PEA) and the flavonoid luteolin (Lut), in an in vivo model of traumatic brain injury (TBI) and patients affected by moderate TBI. An increase in neurogenesis was seen in the mice at 72 h and 7 d after TBI. The co-ultra PEALut treatment helped the neuronal reconstitution process to restore the basal level of both novel and mature neurons; moreover, it induced a significant upregulation of the neurotrophic factors, which ultimately led to progress in terms of memory recall during behavioral testing. Moreover, our preliminary findings in a clinical trial suggested that Glialia® treatment facilitated neural recovery on working memory. Thus, co-ultra PEALut (Glialia®) could represent a valuable therapeutic agent for intensifying the endogenous repair response in order to better treat TBI.


Assuntos
Amidas/administração & dosagem , Lesões Encefálicas Traumáticas/tratamento farmacológico , Etanolaminas/administração & dosagem , Luteolina/administração & dosagem , Neurogênese/efeitos dos fármacos , Ácidos Palmíticos/administração & dosagem , Administração Oral , Adulto , Idoso , Amidas/farmacologia , Animais , Lesões Encefálicas Traumáticas/etiologia , Lesões Encefálicas Traumáticas/psicologia , Modelos Animais de Doenças , Quimioterapia Combinada , Etanolaminas/farmacologia , Feminino , Humanos , Luteolina/farmacologia , Masculino , Memória de Curto Prazo/efeitos dos fármacos , Camundongos , Pessoa de Meia-Idade , Teste do Labirinto Aquático de Morris/efeitos dos fármacos , Ácidos Palmíticos/farmacologia , Distribuição Aleatória , Aprendizagem Espacial/efeitos dos fármacos , Resultado do Tratamento
16.
J Neuroimmunol ; 358: 577654, 2021 09 15.
Artigo em Inglês | MEDLINE | ID: mdl-34265624

RESUMO

Increasing evidence suggests that SARS-CoV-2, the virus responsible for the COVID-19 pandemic, is associated with increased risk of developing neurological or psychiatric conditions such as depression, anxiety or dementia. While the precise mechanism underlying this association is unknown, aberrant activation of toll-like receptor (TLR)3, a viral recognizing pattern recognition receptor, may play a key role. Synthetic cannabinoids and enhancing cannabinoid tone via inhibition of fatty acid amide hydrolase (FAAH) has been demonstrated to modulate TLR3-induced neuroimmune responses and associated sickness behaviour. However, the role of individual FAAH substrates, and the receptor mechanisms mediating these effects, are unknown. The present study examined the effects of intracerebral or systemic administration of the FAAH substrates N-oleoylethanolamide (OEA), N-palmitoylethanolamide (PEA) or the anandamide (AEA) analogue meth-AEA on hyperthermia and hypothalamic inflammatory gene expression following administration of the TLR3 agonist, and viral mimetic, poly I:C. The data demonstrate that meth-AEA does not alter TLR3-induced hyperthermia or hypothalamic inflammatory gene expression. In comparison, OEA and PEA attenuated the TLR3-induced hyperthermia, although only OEA attenuated the expression of hyperthermia-related genes (IL-1ß, iNOS, COX2 and m-PGES) in the hypothalamus. OEA, but not PEA, attenuated TLR3-induced increases in the expression of all IRF- and NFκB-related genes examined in the hypothalamus, but not in the spleen. Antagonism of PPARα prevented the OEA-induced attenuation of IRF- and NFκB-related genes in the hypothalamus following TLR3 activation but did not significantly alter temperature. PPARα agonism did not alter TLR3-induced hyperthermia or hypothalamic inflammatory gene expression. These data indicate that OEA may be the primary FAAH substrate that modulates TLR3-induced neuroinflammation and hyperthermia, effects partially mediated by PPARα.


Assuntos
Etanolaminas/farmacologia , Hipertermia Induzida/métodos , Mediadores da Inflamação/metabolismo , PPAR alfa/metabolismo , Receptor 3 Toll-Like/administração & dosagem , Amidoidrolases/farmacologia , Animais , Feminino , Expressão Gênica , PPAR alfa/agonistas , PPAR alfa/antagonistas & inibidores , Poli I-C/toxicidade , Ratos , Ratos Sprague-Dawley
17.
Biochim Biophys Acta Mol Cell Biol Lipids ; 1866(11): 159017, 2021 11.
Artigo em Inglês | MEDLINE | ID: mdl-34332077

RESUMO

Sphingomyelin synthase related protein (SMSr) has no SM synthase activity but has ceramide phosphorylethanolamine (CPE) synthase activity in vitro. Although SMSr is ubiquitously expressed in all tested tissues, the CPE levels in most mammalian tissues or cells are extremely low or undetectable. Therefore, SMSr seems not to be a functional CPE synthase in vivo and its real biological function needs to be elucidated. In this study, we utilized purified recombinant SMSr and adenovirus-mediated SMSr in vivo expression to show that SMSr has phosphatidylethanolamine phospholipases C (PE-PLC) activity, i.e., it can generate DAG through PE hydrolysis in the absence of ceramide. Further, we found that SMSr has no phosphatidylcholine (PC)-PLC, phosphatidylserine (PS)-PLC, phosphatidylglycerol (PG)-PLC, and phosphatidic phosphatase (PAP) activities, indicating that SMSr-mediated PE-PLC activity has specificity. We conclude that SMSr is a mammalian PE-PLC. Importantly, SMSr can regulate steady state levels of PE in vivo, and it should be a new tool for PE-related biological study.


Assuntos
Transferases (Outros Grupos de Fosfato Substituídos)/metabolismo , Animais , Células Cultivadas , Chlorocebus aethiops , Etanolaminas/metabolismo , Hidrólise , Camundongos , Camundongos Endogâmicos C57BL , Camundongos Knockout , Transferases (Outros Grupos de Fosfato Substituídos)/deficiência
18.
Org Lett ; 23(15): 5922-5926, 2021 08 06.
Artigo em Inglês | MEDLINE | ID: mdl-34314177

RESUMO

Zwitterionic carbohydrate modifications, such as phosphoethanolamine (PEtN), govern host-pathogen interactions. Whereas it is recognized that these modifications stimulate the host immune system, the purpose of PEtN modification remains largely descriptive. As an enabling step toward studying this carbohydrate modification, we report a synthesis of the P. temperata zwitterionic trisaccharide repeating unit. The 32-step synthesis was enabled by H-phosphonate chemistry to install the PEtN arm on a poorly reactive and sterically hindered C4-alcohol.


Assuntos
Etanolaminas/síntese química , Photorhabdus/química , Trissacarídeos/síntese química , Etanolaminas/química , Estrutura Molecular , Trissacarídeos/química
19.
Environ Sci Pollut Res Int ; 28(39): 55754-55770, 2021 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-34143388

RESUMO

In this study, modification of the nanoclay montmorillonite adsorbent with diethanolamine and optimization of CO2 adsorption operating conditions to improve the adsorption capacity were carried out experimentally. The temperature, pressure, and weight percent of diethanolamine were considered in the range of 30-70 °C, 1-9 bar, and 10-30%wt, respectively, as input variables and adsorption capacity (mg/g) and adsorption percentage were considered as the responses in the response surface methodology. The maximum adsorption capacity was obtained 219.9 mg/g for montmorillonite adsorbent without modification at temperature and pressure of 30 °C and 9 bar, respectively. In addition, the optimum temperature, pressure, and weight percent of diethanolamine were obtained 30 °C and 9 bar and 22%wt, respectively, and the adsorption capacity was calculated 281.8 mg/g for modified montmorillonite with diethanolamine. Additionally, the adsorbent behavior was investigated using isotherm, kinetic, and thermodynamic modeling of the adsorption process. The results showed that, based on the obtained values of R2, Langmuir-Freundlich and Hill models have a better precision between isotherm models for the montmorillonite adsorbent without and with modification, respectively. Finally, the kinetic modeling result showed that the Elovich model is the best-proposed model for CO2 capture data.


Assuntos
Bentonita , Dióxido de Carbono , Etanolaminas
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