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In recent decades, there has been an increasing focus on the alarming decline in global bee populations, given their critical ecological contributions to natural pollination and biodiversity. This decline, marked by a substantial reduction in bee colonies in forested areas, has serious implications for sustainable beekeeping practices and poses a broader risk to ecological well-being. Addressing these pressing issues requires innovative solutions, one of which involves the development and fabrication of beehives crafted from composite materials that are ecologically compatible with bee biology. Importantly, these materials should also exhibit a high resistance to environmental factors, such as ultraviolet (UV) radiation, in order to maintain their mechanical integrity and longevity. To investigate this, we conducted accelerated UV degradation tests on a variety of composite materials to rapidly assess their susceptibility to UV-induced changes. High-density polyethylene (HDPE) served as the matrix material and was reinforced with natural fibers, specifically fique fibers (Furcraea bedinghausii), banana fibers, and goose feathers. Our findings indicate that UV radiation exposure results in a noticeable reduction in the tensile strength of these materials. For example, wood composites experienced a 48% decline in tensile strength over a 60-day period, a rate of deterioration notably higher than that of other tested composite materials. Conversely, HDPE composites fortified with banana fibers initially demonstrated tensile strengths exceeding 9 MPa and 10 MPa. Although these values gradually decreased over the observation period, the composites still displayed favorable stress-strain characteristics. This research underscores the substantial influence of UV radiation on the longevity and efficacy of beehive materials, which in turn affects the durability of natural wood hives exposed to these environmental factors. The resultant increased maintenance and replacement costs for beekeepers further emphasize the need for judicious material selection in beehive construction and point to the viability of the composite materials examined in this study.
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Uncertainty persists regarding the specific chemical causal factors and their corresponding behavioral effects in anxiety disorders. Commonly employed first-line treatments for anxiety target G protein-coupled receptors (GPCRs), including inhibitors of monoaminergic systems. Alternatively, emerging natural bioactive strategies offer potential for mitigating adverse effects. Recent investigations have implicated adenosine in anxiety-triggering mechanisms, while eritadenine, an adenosine analog derived from Shiitake mushroom, has displayed promising attributes. This study explores eritadenine's potential as a bioactive substance for anxiety disorders in mice, employing behavioral tests, pentobarbital-sleep induction, and molecular docking. Behavioral test results reveal a pronounced anxiolytic and sedative-hypnotic pharmacological effect of eritadenine. Our findings suggest that eritadenine may modulate locomotor functions mediated by adenosine receptors, with a stronger affinity for binding to A2AAR over A1AR, thus eliciting these effects.
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Transtornos de Ansiedade , Hipnóticos e Sedativos , Camundongos , Animais , Simulação de Acoplamento Molecular , AdenosinaRESUMO
BACKGROUND: The burden of having neurologic symptoms (NS) in cancer patients has scantly been studied; therefore, we performed a study whose purpose was to measure the impact of having clinically active (NS) on the quality of life (QoL) of non-primary CNS cancer patients. METHODS: Patients with systemic cancer (non-primary CNS cancer) sent for neurological evaluation at a single cancer center (INCAN) were prospectively invited to respond the EORTC-QLQ-C30 and BN20 questionnaires. Associations of the questionnairés items were blindly measured for the following groups: NS+ or not (NS-) and having active cancer (AC+) or not (AC-). RESULTS: Of 205 patients aged 55.4 ± 15.4 years, 122 (60%) had NS+ and 107 (52%) AC +. The NS+ group (compared with the NS-) showed a significant worse perception in the following scales/items of the EORTC QLQ-C30: physical functioning (median 86 vs. 92, P = 0.012), role functioning (66 vs. 100, P < 0.001), emotional functioning (75 vs. 83, P = 0.005), cognitive functioning (66 vs. 83, P < 0.001), fatigue (33 vs. 22, P < 0.001), nausea and vomiting (P = 0.021), pain (33 vs. 16, P < 0.001), insomnia (33 vs. 0, P = 0.011), appetite loss (P = 0.021), and global health (66 vs. 75, P = 0.001). CONCLUSION: In patients with systemic (non-CNS) cancer, the QoL is significantly worse for patients with active neurologic symptoms.
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Neoplasias , Qualidade de Vida , Humanos , Qualidade de Vida/psicologia , Neoplasias/complicações , Dor/complicações , Náusea , Vômito , Inquéritos e QuestionáriosRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Caesalpinia coriaria (Jacq.) Willd is widely used as a traditional medinal plant in Mexico for protective and healing purposes and the treatment of gastrointestinal diseases. AIM OF THE STUDY: To investigate the gastroprotective effect of extract of Caesalpinia coriaria pods against ethanol-induced and indomethacin-induced gastric lesion models, its anti-inflammatory and antioxidative activities, and its main compounds through LC-MS analysis. MATERIALS AND METHODS: Male Wistar rats were orally administered a methanol extract obtained from the pods of C. coriaria at doses of 10, 30, 100, and 300 mg/kg prior to inducing gastric lesions with ethanol or indomethacin. Gastric mucosal lesions were evaluated by macroscopic and histopathological alterations. Determination of prostaglandin E2 (PGE2), alpha tumor necrosis factor (TNF-α), leukotriene B4 (LTB4), nitrites/nitrates, superoxide dismutase (SOD), and H2S gastric levels were investigated. Its main compounds of the active extract through LC-MS analysis. RESULTS: Phenolic compounds were identified as major components of methanol extract. LC-MS analysis identified 15 constituents, and the significant compounds were gallic acid, 3-O-galloylquinic acid, digalloylglucose, tetragalloylglucose, valoneic acid dilactone, pentagalloylglucose, digalloylshikimic acid, and ellagic acid. Pretreatment with the extract at doses of 100 and 300 mg/kg significantly reduced gastric ulcer lesions in both models. Compared with the reference drugs (omeprazole or ranitidine, respectively), no significant difference was found (p < 0.05). The extract's gastroprotective effect was accompanied by significant decreases in leukocyte recruitment, and gastric levels of TNF-α and LTB4 by two to fourfold (p < 0.05). Also, gastric levels of PGE2 gastric levels were maintained and the antioxidant enzyme activities of SOD and nitrate/nitrite in the gastric tissue were improved (p < 0.05). The LC-MS analysis indicated the presence of hydrolyzable tannins (mainly gallic acid derivatives). CONCLUSION: The results suggest that the gastroprotective effect of the methanol extract of C. coriaria pods occurs through anti-inflammatory, antioxidant, and NO modulation properties, and gallic acid derivatives may be the main possible compounds responsible for its actions.
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Antiulcerosos , Caesalpinia , Magnoliopsida , Úlcera Gástrica , Ratos , Animais , Indometacina , Metanol/uso terapêutico , Ratos Wistar , Etanol/uso terapêutico , Antioxidantes/uso terapêutico , Extratos Vegetais/efeitos adversos , Fitoterapia , Fator de Necrose Tumoral alfa , Úlcera Gástrica/induzido quimicamente , Úlcera Gástrica/tratamento farmacológico , Úlcera Gástrica/prevenção & controle , Anti-Inflamatórios/uso terapêutico , Ácido Gálico/uso terapêutico , Superóxido Dismutase , Antiulcerosos/farmacologia , Antiulcerosos/uso terapêuticoRESUMO
Infusions and poultices prepared from the aerial parts of Baccharis heterophylla Kunth (Asteraceae) are widely used in Oaxaca (Mexico) for relieving painful and inflammatory complaints. Therefore, the antinociceptive potential of an aqueous extract (31.6-316 mg/kg, p.o.) and essential oil (30-177 µg/paw, i.pl.) of the plant was assessed using the formalin test. Both preparations inhibited the formalin-induced nociception response (100-316 mg/kg and 100-177 µg/paw, respectively) during the test's second phase. Chemical analysis of the aqueous extract revealed that the major active components were chlorogenic acid (1), 3,4-di-O-(E)-caffeoylquinic acid (2), 3,5-di-O-(E)-caffeoylquinic acid (3), 4,5-di-O-(E)-caffeoylquinic acid (4), 3,5-di-O-(E)-caffeoylquinic acid methyl ester (5), apigenin (6), genkwanin (7), acacetin (8). Compounds 1-5 and 8 are new for B. heterophylla. A high-pressure liquid chromatographic method for quantifying chlorogenic acid (1) and di-caffeoylquinic acids 2-4 in the plant was developed and validated. Analyses of the essential oil and the headspace solid-phase microextraction products, via gas-chromatography-mass spectrometry, revealed that the major volatiles were ß-pinene, myrcene, D-limonene, ß-caryophyllene, and α-caryophyllene, which have demonstrated antinociceptive properties.
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RESUMEN: La neoplasia quística mucinosa del páncreas (NQMP) es un tumor infrecuente, que afecta predominantemente a mujeres (90-95 %), afectando especialmente entre la quinta y séptima década de la vida; cuyo descubrimiento suele ser incidental. Por lo general, son lesiones solitarias, sin compromiso del conducto pancreático principal; poco sintomáticas y asociadas a malignidad (10 % a 40 %). El objetivo de este manuscrito fue reportar un caso de neoplasia quística mucinosa gigante del páncreas intervenida quirúrgicamente y revisar la evidencia existente respecto de sus características morfológicas, terapéuticas y pronósticas. Mujer de 29 años, con masa abdominal poco sintomática. El diagnóstico se verificó por medio de ultrasonografía, tomografía axial computarizada y resonancia nuclear magnética. Se intervino quirúrgicamente, realizándose pancreatectomía corporocaudal con preservación esplénica, sin incidentes. La paciente fue dada de alta al quinto día, sin complicaciones, y evolucionó de forma adecuada, sin complicaciones postoperatorias. La NMQP es una lesión compleja, que puede asociarse a malignidad, pero el diagnóstico preoperatorio de malignidad no puede establecerse con seguridad. El pronóstico depende de un diagnóstico precoz y un tratamiento oportuno.
SUMMARY: Mucinous cystic neoplasm of the pancreas (MCNP) are variable types of tumors, which predominantly affect women (90-95 %), and usually appear incidentally in the 5th to 7th decade of life. They are generally solitary lesions, with no involvement of the main pancreatic duct, rarely symptomatic and are associated with malignancy (10 % to 40 %). The aim of this manuscript was to report a case of giant mucinous cystic neoplasm of the pancreas surgically treated and review the existing evidence regarding its morphological, therapeutic and prognosis characteristics. Patient: A 29-year-old woman with a slightly symptomatic abdominal mass. The diagnosis was verified with ultrasound, computed axial tomography and magnetic nuclear resonance. The patient underwent surgery; an uneventful corporocaudal pancreatectomy with splenic preservation was performed. She was discharged on the fifth day, and has evolved adequately, without postoperative complications. MCNP is a complex lesion, which can be associated with malignancy, but the preoperative diagnosis of malignancy cannot be established with certainty. Its prognosis depends on early diagnosis and timely treatment.
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Humanos , Feminino , Adulto , Pancreatectomia/métodos , Neoplasias Pancreáticas/cirurgia , Cistadenoma Mucinoso/cirurgia , Neoplasias Pancreáticas/diagnóstico por imagem , Baço/cirurgia , Imageamento por Ressonância Magnética , Tomografia Computadorizada por Raios X , Cistadenoma Mucinoso/diagnóstico por imagemRESUMO
The antiallodynic effect of PhAR-DBH-Me was evaluated on two models of neuropathic pain, and the potential roles of CB1, CB2, and TRPV1 receptors as molecular targets of PhAR-DBH-Me were studied. Female Wistar rats were submitted to L5/L6 spinal nerve ligation (SNL) or repeated doses of cisplatin (0.1 mg/kg, i.p.) to induce experimental neuropathy. Then, tactile allodynia was determined, and animals were treated with logarithmic doses of PhAR-DBH-Me (3.2-100 mg/kg, i.p.). To evaluate the mechanism of action of PhAR-DBH-Me, in silico studies using crystallized structures of CB1, CB2, and TRPV1 receptors were performed. To corroborate the computational insights, animals were intraperitoneally administrated with antagonists for CB1 (AM-251, 3 mg/kg), CB2 (AM-630, 1 mg/kg), and TRPV1 receptors (capsazepine, 3 mg/kg), 15 min before to PhAR-DBH-Me (100 mg/kg) administration. Vagal stimulation evoked on striated muscle contraction in esophagus, was used to elicited pharmacological response of PhAR-DBH-ME on nervous tissue. Systemic administration of PhAR-DBH-Me reduced the SNL- and cisplatin-induced allodynia. Docking studies suggested that PhAR-DBH-Me acts as an agonist for CB1, CB2, and TRPV1 receptors, with similar affinity to the endogenous ligand anandamide. Moreover antiallodynic effect of PhAR-DBH-Me was partially prevented by administration of AM-251 and AM-630, and completely prevented by capsazepine. Finally, PhAR-DBH-Me decreased the vagally evoked electrical response in esophagus rat. Taken together, results indicate that PhAR-DBH-Me induces an antiallodynic effect through partial activation of CB1 and CB2 receptors, as well as desensitization of TRPV1 receptors. Data also shed light on the novel vanilloid nature of the synthetic compound PhAR-DBH-Me.
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Compostos Azabicíclicos/farmacologia , Antagonistas de Receptores de Canabinoides/farmacologia , Hiperalgesia/induzido quimicamente , Ácidos Oleicos/farmacologia , Canais de Cátion TRPV/efeitos dos fármacos , Animais , Antineoplásicos/administração & dosagem , Antineoplásicos/efeitos adversos , Ácidos Araquidônicos/metabolismo , Compostos Azabicíclicos/administração & dosagem , Antagonistas de Receptores de Canabinoides/metabolismo , Capsaicina/administração & dosagem , Capsaicina/análogos & derivados , Capsaicina/farmacologia , Cisplatino/administração & dosagem , Cisplatino/efeitos adversos , Endocanabinoides/metabolismo , Feminino , Hiperalgesia/tratamento farmacológico , Injeções Intraperitoneais , Ligadura/métodos , Modelos Animais , Neuralgia/induzido quimicamente , Neuralgia/tratamento farmacológico , Ácidos Oleicos/administração & dosagem , Alcamidas Poli-Insaturadas/metabolismo , Ratos , Ratos Wistar , Nervos Espinhais/efeitos dos fármacos , Nervos Espinhais/cirurgia , Canais de Cátion TRPV/antagonistas & inibidores , Estimulação do Nervo Vago/métodosRESUMO
The co-administration of 3α-hydroxymasticadienoic acid (3α-OH MDA) and diligustilide (DLG) generates a synergist gastroprotective effect on indomethacin-induced gastric damage. However, the related protective activities of the compounds alone (or in combination) remain unclear. In the present study, we evaluated the anti-inflammatory and antioxidative activities, as well as the potential modulation of important gasotransmitters of each compound individually and in combination using the indomethacin-induced gastric damage model. Male Wistar rats were treated orally with the 3α-OH MDA, DLG, or their combination (at a fixed ratio of 1:1, 1:3, and 3:1) 30 min before the generation of gastric mucosal lesions with indomethacin (30 mg/kg, p.o.). Three hours later, the gastric injury (mm2) was determined. Results from these experiments indicate, in addition to maintaining basal levels of PGE2, the gastroprotective effect of the pre-treatment with 3α-OH MDA (70%), DLG (81%), and their combination (72%) which was accompanied by significant decreases in leukocyte recruitment, as well as decreases in TNF-α and LTB4 gastric levels (p < 0.05). We also found that the pre-treatment maintains the basal antioxidant enzyme activities (SOD) and gastric NO and H2S production even in the presence of indomethacin (p < 0.05). In conclusion, when 3α-OH MDA-DLG is given at a 1:1 combination ratio, the gastroprotective effect and the inflammatory, antioxidant, and gaso-modulation properties are not different from those of treatments using the maximum doses of each compound, revealing that this combination produces promising results for the treatment of gastric ulcers.
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Anti-Inflamatórios/farmacologia , Antiulcerosos/farmacologia , Antioxidantes/farmacologia , Mucosa Gástrica/efeitos dos fármacos , Úlcera Gástrica/prevenção & controle , Triterpenos/farmacologia , Animais , Dinoprostona/metabolismo , Modelos Animais de Doenças , Quimioterapia Combinada , Mucosa Gástrica/metabolismo , Mucosa Gástrica/patologia , Sulfeto de Hidrogênio/metabolismo , Indometacina , Leucotrieno B4/metabolismo , Masculino , Óxido Nítrico/metabolismo , Ratos Wistar , Úlcera Gástrica/metabolismo , Úlcera Gástrica/patologia , Superóxido Dismutase/metabolismo , Fator de Necrose Tumoral alfa/metabolismoRESUMO
Endopleura uchi, is used for the treatment of inflammatory disease and related to the female reproductive tract. The aim of this study was to evaluate the acute toxicity of the Endopleura uchi stem bark hydroethanolic extract (EEu) in zebrafish, emphasizing the histopathological and biochemical parameters, as well as evaluating the in silico pharmacokinetic and toxicological parameters of the phytochemical/pharmacological marker, bergenin, as their metabolites. The animals were orally treated with EEu at a single dose of 75 mg/kg, 500 mg/kg, 1000 mg/kg and 3000 mg/kg. the oral LD50 of the EEu higher to the dose of 3000 mg/kg. Behavioral, biochemical and histopathological changes were dose dependent. In silico pharmacokinetic predictions for bergenin and its metabolites showed moderate absorption in high human intestinal absorption (HIA) and Caco-2 models, reduced plasma protein binding, by low brain tissue binding and no P-glycoprotein (P-Gp) inhibition. Their metabolism is defined by the CYP450 enzyme, in addition to bergenin inhibition of CYP2C9, CYP3A4 and CYP2C19. In the bergenin and its metabolites in silico toxicity test it have been shown to cause carcinogenicity and a greater involvement of the bergenin with the CYP enzymes in the I and II hepatic and renal metabolism's phases was observed. It is possible to suggest that the histopathological damages are involved with the interaction of this major compound and its metabolites at the level of the cellular-biochemical mechanisms which involve the absorption, metabolization and excretion of these possible prodrug and drug.
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ETHNOPHARMACOLOGICAL RELEVANCE: Endopleura uchi (Huber) Cuatrec is a plant species from the Brazilian Amazon. The barks of this tree are used in folk medicine - mainly as a decoction - for dyslipidemia, uterine infection, fibroids, polycystic ovary, menstrual disorders, as a contraceptive and abortive agent, among others. However, the data available about its developmental toxicity are still insufficient. AIM OF THE STUDY: This study aimed to evaluate the reproductive toxicity and teratogenic effects in embryos from zebrafish treated with the hydroethanolic extract from the barks of Endopleura uchi (EEu). MATERIALS AND METHODS: Both sexes of zebrafish (Danio rerio) were treated with EEu either through immersion (1.2, 2.5, and 5â¯mg/L) or orally (75, 200, and 500â¯mg/kg) over 21 consecutive days. Next, we assessed their fertility and gonads' histopathology; in their embryos were assessed teratogenesis, lethalities, and heart rate during daily observations (24, 48, 72, and 96 hpf). RESULTS: The phytochemical analysis of EEu through HPLC/MS shows bergenin as the major compounds. After 21 days of treatment were detected minor histopathological changes in parental fishes, such as atretic oocytes, interstitial fibrosis, and decreased the percentage of early vitellogenic oocytes, but without impairing the reproduction of treated animals. However, in the embryos was observed significantly increased frequency of malformation in all the groups treated through immersion, and in the group treated orally with the highest concentration (500â¯mg/kg). CONCLUSION: Based on the results, EEu caused no adverse effects in the progenitors on both treatments (immersion and oral). However, it was observed that the concentrations 1.2, 2.5, and 5â¯mg/L (immersion), and the dose 500â¯mg/kg (oral) caused malformations in the offspring (F1 generation). These results emphasize the need for attention when using preparations from E. uchi, mainly for pregnant women. Further studies are needed to compare its effects with the extract's primary compound (bergenin).
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Embrião não Mamífero/efeitos dos fármacos , Malpighiales , Extratos Vegetais/toxicidade , Reprodução/efeitos dos fármacos , Teratogênicos/toxicidade , Animais , Embrião não Mamífero/anormalidades , Desenvolvimento Embrionário/efeitos dos fármacos , Feminino , Doenças dos Genitais Femininos/tratamento farmacológico , Masculino , Compostos Fitoquímicos/análise , Compostos Fitoquímicos/toxicidade , Casca de Planta , Extratos Vegetais/química , Plantas Medicinais , Teratogênicos/química , Peixe-Zebra/anormalidadesRESUMO
Abstract The present work investigates the chemical composition of seeds of Cascabela thevetioides (Kunth) Lippold, an ornamental shrub of México. Six thevetia cardiac glycosides or thevetosides (thevetin A, B, and C, acetylthevetin A, B and C) were identified from the methanol extract of seeds of C. thevetioides by High-Performance Liquid Chromatography-Mass Spectrometry and by comparison of mass spectral fragmentation patterns. Enzymatic hydrolysis of a sample of thevetosides from methanol extract of seeds and subsequent High-Performance Liquid Chromatography-Mass Spectrometry analysis yielded the monoglycosides neriifolin, acetylneriifolin and acetylperuvoside, previously reported for this plant. For the fisrt time thevetin A, B and C, and acetylthevetin A, B and C are reported as components of seeds of C. thevetioides.
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ETHNOBOTANICAL RELEVANCE: Spondias mombin L. is a plant dispersed throughout the tropical regions of South America, Africa, and Asia, being found mainly in the North and Northeast of Brazil, where the leaves are used in preparations for neuropsychiatric disorders. Therefore, it is of great importance to carry out studies in different pharmacological models that can prove the traditional use of this plant species. MATERIALS AND METHODS: the hydroethanolic extract from S. mombin leaves (HELSm) was evaluated by oral administration (25â¯mg/kg) and by immersion (25â¯mg/l) in scototaxis test in zebrafish (Danio rerio). For this study, caffeine (100â¯mg/kg) and buspirone (25â¯mg/kg) were used as standard drugs. The antidepressant action of the HELSm was evaluated assessed in the novel tank diving test (NTDT). In this study, a group with 1% ethanol, one with unpredictable chronic mild stress (UCMS), and another with developmental, social isolation (DSI) were used as induction groups for depression-like behavior and fluoxetine (20â¯mg/kg) as a drug pattern. RESULTS: by the HPLC-UV fingerprint analysis, the HELSm presented several derivatives of polyphenolic compounds and flavonoids and identified ellagic acid and isoquercitrin, and by the gas-chromatographic, the majority of the identified compounds were fatty acids, esters, and alcohols. By immersion, the LC50 was 49.86â¯mg/l and by oral via the LD50 in 48â¯h, was 4.515â¯g/kg in zebrafish. For all spatiotemporal and behavioral variables (time spent, white compartment, latency, toggle, erratic swimming, freezing duration, thigmotaxis, and risk assessment), the treatment with HELSm produced a similar effect to buspirone and was significant when compared to the caffeine and control group (pâ¯<â¯0.01, Tukey-Kramer test). For all spatiotemporal and behavioral variables evaluated (time spent at the top of the apparatus, crossed quadrants, erratic swimming, and duration of freezing), treatment with HELSm produced a change in the depression-like behavior in the groups tested, with a similar effect to fluoxetine, both with a significant difference when compared to the control groups (pâ¯<â¯0.01). CONCLUSIONS: Our results suggest that the acute administration of the HELSm in the scototaxis and NTDT tests in a zebrafish model (Danio rerio) produced anxiolytic and antidepressant effects, devoid of hypnotic and sedative actions by immersion, and this action was improved when administered by oral via. Possibly, the presence of isoquercitrin in the leaves of Spondias mombin participates in the anxiolytic and antidepressant effects.
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Anacardiaceae , Ansiolíticos/farmacologia , Antidepressivos/farmacologia , Extratos Vegetais/farmacologia , Animais , Comportamento Animal/efeitos dos fármacos , Feminino , Masculino , Folhas de Planta , Isolamento Social , Estresse Psicológico/tratamento farmacológico , Peixe-Zebra/fisiologiaRESUMO
ETHNOBOTANICAL RELEVANCE: The oil obtained from the fruits of Pterodon emarginatus Vog. (OPe) is used orally and topically, in traditional medicine for some purposes, such as acute and chronic inflammatory states as rheumatoid arthritis. MATERIALS AND METHODS: In this work, the anti-inflammatory activity of the OPe was demonstrated based on several animal models and presented an in silico study based on the 6α,7ß-dihydroxy-vouacapan-17ß-oic acid (DHVA) majority compound of the OPe to evaluate the interaction this compound, with cyclooxygenase-2 (COX-2) in 4COX (Mus musculus) and 5KIR (Homo sapiens) and molecular dynamics simulation. RESULTS: The OPe (498â¯mg/kg, p.o) significantly inhibited (pâ¯<â¯0.05, Student t-test) the primary and secondary reactions of arthritis by Freund's Complete Adjuvant (FCA) and in dermatitis induced by croton oil in mice, OPe inhibited peak of edema. In vascular permeability test in rats, the treatment with OPe was able to block the response to PGE2, serotonin, and bradykinin (pâ¯<â¯0.05, Student t-test). In the writhing test in mice, the OPe at doses of 498 and 980â¯mg/kg (p.o) produced inhibition of 73% and 92%, respectively, and was not significantly effective in the hot plate test. In the evaluation of the potency in relation to gastric injury (gastric ulcer induced by stress) and combined assay in the assessment of anti-inflammatory potency and gastric damage, it was observed that indomethacin (10â¯mg/kg, p.o.) inhibited carrageenan edema by 51% and produced a higher number of gastric lesions when compared to the group treated with OPe, where only areas of hyperemia were observed, without the occurrence of ulcerative lesion, and which inhibited the edema by 47%. In the in silico study, it was found that the DHVA is capable of binding to two organisms (4COX - Mus musculus and 5KIR - Homo sapiens), however, with higher binding affinity to the organism Homo sapiens. CONCLUSIONS: As expected, all tested ligands were capable of forming hydrogen interactions with residues at their respective binding sites, but the DHVA ligand was capable of creating slightly more hydrogen bonds when docked to either 4COX or 5KIR than the other tested ligands, thus demonstrating the participation of this compound in the anti-inflammatory and antialgic responses observed in the in vivo assays as a COX-2 inhibitor. Therefore, the results obtained support the traditional use of OPe for inflammatory and gastric problems.
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Anti-Inflamatórios , Diterpenos , Fabaceae , Óleos de Plantas , Ácido Acético , Animais , Anti-Inflamatórios/análise , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/uso terapêutico , Artrite Experimental/tratamento farmacológico , Óleo de Cróton , Ciclo-Oxigenase 2/metabolismo , Dermatite de Contato/tratamento farmacológico , Diterpenos/análise , Diterpenos/farmacologia , Diterpenos/uso terapêutico , Frutas , Humanos , Indometacina , Masculino , Camundongos , Simulação de Acoplamento Molecular , Dor/induzido quimicamente , Dor/tratamento farmacológico , Fitoterapia , Óleos de Plantas/análise , Óleos de Plantas/farmacologia , Óleos de Plantas/uso terapêutico , Ratos Wistar , Úlcera Gástrica/induzido quimicamente , Úlcera Gástrica/tratamento farmacológicoRESUMO
INTRODUCTION: The development of electrochemical sensors for the detection of small molecules has already had a significant effect on the study of biology because of their selectivity and ability to measure low concentrations of small molecules that regulate various functions in living organisms. Hydrogen sulfide (H2S) is a gasotransmitter produced at low levels in several tissues including the stomach. Here, we propose a new method for detecting low concentrations of this transmitter in the rat stomach, in-vivo and in real time, with applications in pharmacology and physiology. METHODS: Wistar rats fasted for 12h. Then, the control group was given an intragastrical dose of saline. l-Cysteine (50mg/kg) or dl-propargylglycine (50mg/kg) were administered to the test groups to modify the H2S levels. Ranitidine (50mg/kg), omeprazole (40mg/kg) or carbenoxolone (30mg/kg) were used as reference anti-ulcer drugs. Thirty minutes later, the electrode was inserted in the middle of the stomach cavity of the anesthetized animals. The basal levels of H2S were recorded every 5min for 30min. Next, gastric lesions were induced with pure ethanol, and the recording continued for 30 additional minutes. RESULTS: The exogenous administration of an H2S precursor (l-cysteine) increased the level of this gasotransmitter whereas dl-propargylglycine, a selective inhibitor of the enzyme cystathionine γ lyase, reduced the total concentration of H2S. The administration of carbenoxolone, a gastroprotective, increased the total amount of H2S. However, the administration of the anti-secretors omeprazole and ranitidine did not modify the total concentration of H2S. DISCUSSION: This work provides the basis for a real-time analysis of the changes in-vivo of the gasotransmitter H2S in the normal and injured stomach and the exploration of the effect of drugs on the regulation of H2S.
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Gasotransmissores/análise , Mucosa Gástrica/metabolismo , Sulfeto de Hidrogênio/análise , Eletrodos Seletivos de Íons , Úlcera Gástrica/metabolismo , Animais , Antiulcerosos/farmacologia , Modelos Animais de Doenças , Etanol/toxicidade , Gasotransmissores/metabolismo , Humanos , Sulfeto de Hidrogênio/metabolismo , Ratos , Ratos Wistar , Estômago/efeitos dos fármacos , Úlcera Gástrica/induzido quimicamente , Fatores de TempoRESUMO
Dyslipidemia is caused by disturbances in lipid metabolism that lead to chronic elevations of serum lipids, especially low-density lipoprotein (LDL)-cholesterol and triglycerides, increasing the risk of metabolic syndrome, obesity, diabetes, atherogenic processes, and cardiovascular diseases. The oil from the fruits of Euterpe oleracea (OFEO) is rich in unsaturated fatty acids with potential for treating alterations in lipid metabolism. In this study, we aimed to investigate the effect of OFEO on hyperlipidemia induced by Cocos nucifera L. saturated fat (GSC) in Wistar rats. Chromatographic profile showed that unsaturated fatty acids account for 66.08% in OFEO, predominately oleic acid (54.30%), and saturated fatty acids (palmitic acid 31.6%) account for 33.92%. GSC-induced dyslipidemia resulted in an increase in total cholesterol, LDL-cholesterol, triglycerides, glucose, and liver and abdominal fat, as well as atherogenic processes in the thoracic aorta. OFEO treatment did not reduce hypertriglyceridemia, but did reduce total cholesterol and LDL-cholesterol, thus contributing to the antiatherogenic action of OFEO. OFEO treatment inhibited the formation of atheromatous plaques in the vascular endothelium of the treated rats, as well as those who were treated with simvastatin. The results obtained suggest that OFEO has an antiatherogenic effect in a rat model of dyslipidemia.
Assuntos
Cocos/efeitos adversos , Dislipidemias/dietoterapia , Euterpe/química , Ácidos Graxos/efeitos adversos , Óleos de Plantas/metabolismo , Animais , Aorta Torácica/metabolismo , Colesterol/sangue , LDL-Colesterol/sangue , Cocos/química , Dislipidemias/etiologia , Dislipidemias/metabolismo , Ácidos Graxos/metabolismo , Frutas/química , Frutas/metabolismo , Humanos , Masculino , Ratos , Ratos Wistar , Triglicerídeos/sangueRESUMO
BACKGROUND: Advanced age is considered to be a relative contraindication to bariatric surgery because of increased perioperative risk and suboptimal excess weight loss. OBJECTIVES: The aim of this study was to analyze the safety and effectiveness of the sleeve gastrectomy (SG) procedure in a cohort of elderly patients (aged≥60 yr) compared with younger patients (aged<60 yr). SETTING: Hospital clinic, Barcelona, Spain. METHODS: A retrospective analysis of all cases of SG in patients≥60 years old between January 2006 and December 2012 was performed. RESULTS: The study included 206 patients, 103 in each group. The mean age was 63.3±2.8 years, and the body mass index was 45.8±22.8 kg/m2. The overall complication rate within the elderly group was 9.7% versus 15.5% in the younger group (P = .2). After SG, there was no statistical difference in body mass index between the groups until 24 (33.4 versus 31.5 kg/m2, P = .01) and 36 (34.6 versus 32.8 kg/m2, P = .01) months of follow-up, favoring the younger cohort. Mean percent excess weight loss was similar between the groups during all periods of follow-up. The mean percent total weight loss change was statistically higher in the younger group at 3 (15.1% versus 17.1%, P = .03); 6 (25.2% versus 27.5%, P = .04); 12 (32.4% versus 35.2%, P = .03); 24 (26.7% versus 32.4%, P<.01); and 36 months (24.9% versus 29.1%, P<.01). Neither groups revealed a statistical difference in resolution of all co-morbidities, except for obstructive sleep apnea (P = .02) in the younger group. CONCLUSIONS: SG is a safe and feasible procedure in the elderly with results comparable to those in the standard bariatric population.
Assuntos
Índice de Massa Corporal , Gastrectomia/métodos , Laparoscopia/métodos , Obesidade Mórbida/cirurgia , Complicações Pós-Operatórias/epidemiologia , Redução de Peso/fisiologia , Idoso , Feminino , Seguimentos , Humanos , Masculino , Pessoa de Meia-Idade , Obesidade Mórbida/fisiopatologia , Estudos Retrospectivos , Espanha/epidemiologia , Resultado do TratamentoRESUMO
CONTEXT: Agastache mexicana ssp. mexicana (Kunth) Lint & Epling (Lamiaceae), popularly known as 'toronjil morado', is used in Mexican traditional medicine for the treatment of several diseases such as hypertension, anxiety and respiratory disorders. OBJECTIVE: This study investigates the relaxant action mechanism of A. mexicana ssp. mexicana essential oil (AMEO) in guinea-pig isolated trachea model. MATERIALS AND METHOD: AMEO was analyzed by GC/MS. The relaxant effect of AMEO (5-50 µg/mL) was tested in guinea-pig trachea pre-contracted with carbachol (3 × 10 - 6 M) or histamine (3 × 10 - 5 M) in the presence or absence of glibenclamide (10 - 5 M), propranolol (3 × 10 - 6 M) or 2',5'-dideoxyadenosine (10 - 5 M). The antagonist effect of AMEO (10-300 µg/mL) against contractions elicited by carbachol (10 - 15-10 - 3 M), histamine (10 - 15-10 - 3 M) or calcium (10-300 µg/mL) was evaluated. RESULTS: Essential oil composition was estragole, d-limonene and linalyl anthranilate. AMEO relaxed the carbachol (EC50 = 18.25 ± 1.03 µg/mL) and histamine (EC50 = 13.3 ± 1.02 µg/mL)-induced contractions. The relaxant effect of AMEO was not modified by the presence of propranolol, glibenclamide or 2',5'-dideoxyadenosine, suggesting that effect of AMEO is not related to ß2-adrenergic receptors, ATP-sensitive potassium channels or adenylate cyclase activation. AMEO was more potent to antagonize histamine (pA2' = -1.507 ± 0.122) than carbachol (pA2' = -2.180 ± 0.357). Also, AMEO antagonized the calcium chloride-induced contractions. CONCLUSION: The results suggest that relaxant effect of AMEO might be due to blockade of calcium influx in guinea-pig trachea smooth muscle. It is possible that estragole and d-limonene could contribute majority in the relaxant effect of AMEO.
Assuntos
Agastache/química , Broncoconstrição/efeitos dos fármacos , Broncodilatadores/farmacologia , Relaxamento Muscular/efeitos dos fármacos , Músculo Liso/efeitos dos fármacos , Óleos Voláteis/farmacologia , Extratos Vegetais/farmacologia , Traqueia/efeitos dos fármacos , Animais , Broncodilatadores/isolamento & purificação , Sinalização do Cálcio/efeitos dos fármacos , Relação Dose-Resposta a Droga , Cromatografia Gasosa-Espectrometria de Massas , Cobaias , Técnicas In Vitro , Masculino , Músculo Liso/metabolismo , Óleos Voláteis/isolamento & purificação , Fitoterapia , Componentes Aéreos da Planta , Extratos Vegetais/isolamento & purificação , Plantas Medicinais , Traqueia/metabolismoAssuntos
Neoplasias das Glândulas Endócrinas/cirurgia , Laparoscopia , Glomos Para-Aórticos , Paraganglioma/cirurgia , 3-Iodobenzilguanidina , Adulto , Neoplasias das Glândulas Endócrinas/diagnóstico por imagem , Feminino , Humanos , Paraganglioma/diagnóstico por imagem , Compostos Radiofarmacêuticos , Cirurgia Assistida por ComputadorRESUMO
Gastrointestinal stromal tumors (GIST) represent 0.1-3 % of gastrointestinal malignancy. Surgery is the mainstay of treatment, but in high-risk tumors, imatinib can help to achieve better oncological outcomes. We present a rare case of a patient with gastric GIST with very aggressive evolution in a short period of time despite the use of neoadjuvant therapy with imatinib.