RESUMEN
Passiflora cincinnata Mast. is described as a native Caatinga species, used by nutritional and medicinal purposes, although there are still few studies and pharmacological data related to this species. This paper aims to evaluate the safety profile and hypolipidemic potential of the fruit peel of this species in mice. It was analyzed the chemical composition of ethanolic extract (EtOH-Pc) by HPLC-DAD-MS/MS, and the organic and inorganic composition of flour (MF-Pc). Also were evaluated the acute toxicity, the lipid-lowering potential of these samples, through of a pretreatment (oral: 100 and 200 mg/kg), and a single treatment with the same doses, after hyperlipidemic induction with triton WR-1339, using as animal model Swiss Mus musculus mice, besides histopathological analysis. The presence of flavonoids in the extract was confirmed, mainly C-glycosides, and antioxidant minerals and pectin, in flour. No clinical signs of toxicity or death were reported in the study. In the hyperlipidemia study model used, the analyzed substances, at all doses, notably decreased the lipid levels of TC, TG, LDL-c and VLDL-c and increase the HDL-c levels in the induced hyperlipidemic mice (p < 0.05). The results of the histopathological analysis showed that in the group only induced was identified the discrete presence of hepatic steatosis, in 2 animals at the analysis of 24 h, not being visualized in the groups treated with the substances evaluated. The results obtained in the present study suggest a hypolipidemic potential of the extract and flour, obtained from the fruit peel of Passiflora cincinnata Mast.
Asunto(s)
Passiflora , Passifloraceae , Ratones , Animales , Passiflora/química , Harina , Espectrometría de Masas en Tándem , Extractos Vegetales/farmacología , Etanol , Pectinas , LípidosRESUMEN
BACKGROUND: Passiflora L. is a genus belonging to the Passifloraceae family, with many species widely used in folk medicine and several pharmacological activities described in the scientific literature, being a major target for the development of new therapeutic products. Studies have identified several bioactive compounds in their composition as responsible for these activities, mainly C-glycoside flavonoids. OBJECTIVE: The aim of this study was to carry out a review of patents related to the genus and its application in several pharmacological activities, important for the development of new drugs and formulations. METHODS: The search was carried out in 5 specialized databases, INPI, EPO, WIPO, Latipat and Derwent, using the term 'Passiflora' combined with 'A61K and A61P', subclasses of section A of the International Patent Classification (IPC), which are destined to medical, dental or hygienic purposes, and therapeutic activity of chemical compounds or medicinal preparation, respectively. RESULTS: 1,198 patents citing the genus in the title or abstract have been found, 508 being duplicates. After exclusion and inclusion criteria, 23 patents written in English, Portuguese and Spanish were selected, which demonstrated biological assays in vivo with species of Passiflora as the only active constituent or incorporated in formulations with other compounds. CONCLUSION: The findings of this search showed growing interest in research and industrial areas in the pharmaceutical development with species of Passiflora, suggesting that the different bioactive compounds present in the genus can be considered as an important tool for the development of new effective and safe products with pharmacological potential.
RESUMEN
ETHNOPHARMACOLOGICAL RELEVANCE: There are many studies and therapeutic properties attributed to the flowers and leaves of the Cannabis species, but even with few pharmacological studies, Cannabis sativa L. (Cannabaceae) roots presents several therapeutic indications in folk medicine. AIM OF THE STUDY: This study aimed to evaluate the anti-inflammatory and spasmolytic effects as well as the toxicological profile of the aqueous extract of Cannabis sativa roots (CsAqEx) in mice. MATERIALS AND METHODS: We assessed the anti-inflammatory effect with carrageenan-induced leukocyte migration assay, and carrageenan and histamine-induced paw edema methods; The spasmolytic effect was assessed through in vitro assays with isolated mice trachea. To assess motor coordination and mobility, mice went through the rotarod and open field tests, respectively. For the single-dose toxicity study, we administered CsAqEx at the dose of 1000 mg/kg by gavage. In a repeated dose toxicity study, animals received CsAqEx at doses of 25 mg or 100 mg/kg for 28 days. RESULTS: The CsAqEx inhibited the migration of leukocytes at the doses of 25, 50, and 100 mg/kg. The CsAqEx showed anti-inflammatory activity after the intraplantar injection of carrageenan, presenting a reduction in edema formation at all tested doses (12.5, 25, 50 and 100 mg/kg). The dose of 12.5 mg/kg of CsAqEx prevented edema formation after intraplantar injection of histamine. In an organ bath, 729 µg/mL of CsAqEx did not promote spasmolytic effect on isolated mice tracheal rings contracted by carbachol (CCh) or potassium chloride (KCl). We did not observe clinical signs of toxicity in the animals after acute treatment with CsAqEx, which suggested that the median lethal dose (LD50) is greater than 1000 mg/kg. Repeated dose exposure to the CsAqEx did not produce significant changes in hematological, biochemical, or organ histology parameters. CONCLUSIONS: The results suggest that the anti-inflammatory effect of CsAqEx is related to the reduction of vascular extravasation and migration of inflammatory cells, without effects on the central nervous system. Moreover, there was no spasmolytic effect on airway smooth muscle and no toxicity was observed on mice.
Asunto(s)
Antiinflamatorios/farmacología , Antiinflamatorios/toxicidad , Cannabis/química , Parasimpatolíticos/farmacología , Parasimpatolíticos/toxicidad , Extractos Vegetales/farmacología , Extractos Vegetales/toxicidad , Administración Oral , Animales , Antiinflamatorios/administración & dosificación , Conducta Animal/efectos de los fármacos , Carragenina/toxicidad , Edema/inducido químicamente , Edema/prevención & control , Histamina/toxicidad , Inflamación/inducido químicamente , Inflamación/prevención & control , Riñón/efectos de los fármacos , Riñón/patología , Hígado/efectos de los fármacos , Hígado/patología , Ratones , Músculo Liso/efectos de los fármacos , Prueba de Campo Abierto/efectos de los fármacos , Parasimpatolíticos/administración & dosificación , Extractos Vegetales/administración & dosificación , Raíces de Plantas/química , Desempeño Psicomotor/efectos de los fármacos , Prueba de Desempeño de Rotación con Aceleración Constante , Estómago/efectos de los fármacos , Estómago/patología , Tráquea/efectos de los fármacosRESUMEN
Ethanol extracts of different parts of Passiflora cincinnata were obtained by maceration. The total phenolic and flavonoid contents were evaluated. The antioxidant activities were determined by ß-carotene-linoleic acid bleaching test, 2,2-diphenyl-1-picrylhydrazil (DPPH), and 2,2'-azinobis-3-ethylbenzothiazoline-6-sulfonic acid (ABTS) radical scavenging. The crude ethanol stem extract showed the highest amount of total polyphenols (45.53 mg gallic acid equivalent/g) while the highest total flavonoid contents (1.42 mg of quercetin equivalent/g) were observed in the leaf extract. The lowest IC50 (25.65 µg/ml) by the DPPH method was observed for the stem extract. The ABTS method showed a significant antioxidant activity for all investigated extracts. The secondary metabolite composition of ethanol extracts was assessed by HPLC-DAD-MS/MS analysis, leading to the identification of fourteen secondary metabolites in P. cincinnata extracts. These results showed the potentiality of this species as a source of phenolic compounds and antioxidants.
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Antioxidantes/química , Flavonoides/análisis , Passiflora/química , Fenoles/análisis , Extractos Vegetales/química , Metabolismo Secundario , Antioxidantes/farmacología , Cromatografía Líquida de Alta Presión/métodos , Flavonoides/química , Polifenoles/análisis , Quercetina/análisis , Espectrometría de Masas en Tándem/métodosRESUMEN
BACKGROUND: Passiflora cincinnata Mast. is described as a native species from the Caatinga biome, and used by traditional medicine for several pharmacological purposes, such as inflammatory disorders. However, studies that prove its biological activities are scarce. HYPOTHESIS/PURPOSE: This paper aims to evaluate the antinociceptive and anti-inflammatory activities of the aerial parts of Passiflora cincinnata (Pc-EtOH) in mice. METHODS: The chemical composition of Pc-EtOH was assessed by high-performance liquid chromatography coupled to diode array detector (HPLC-DAD). The antinociceptive profile of the extract (given orally: 100, 200 and 400â¯mg/kg) was established using the in vivo chemical models (acetic acid-induced abdominal constriction and formalin-induced paw licking test) and thermal (hot plate test) of nociception. The role of opioid, potassium channels, TRPV-1, muscarinic, serotoninergic (5-HT3) receptors and the participation of the nitric oxide pathway also was determined. The rota-rod test was used to verify the possible interference of the extract treatment in motor performance. Paw edema induced by carrageenan or histamine, and leukocyte migration, determination of total protein and nitric oxide to the peritoneal cavity were used for anti-inflammatory profile. RESULTS: The presence of flavonoids in the extract was confirmed using HPLC-DAD. At all doses tested the Pc-EtOH significantly reduced the number of writhing and decreased the paw licking time in both phases of the formalin test (pâ¯<â¯0.05). In the hot plate test, the extract increased the reaction time, reducing painful behavior. The antinociceptive mechanism probably involves central and peripheral pathways, involving the pathway of opioid and muscarinic receptors with influence of potassium channels and the nitric oxide pathway. However, the motor coordination test indicated that in the time of 120â¯min the extract decreases the stay time of the animal in the rota-rod. Pc-EtOH inhibited significantly (pâ¯<â¯0.05) the increase of the edema volume after administration of carrageenan and histamine. In the peritonitis test, acute pre-treatment with Pc-EtOH inhibited leukocyte migration, with a reduction in the number of neutrophils and concentration of total proteins and nitric oxide. CONCLUSION: The present study suggests that Pc-EtOH possesses peripheral and central antinociceptive action, and showed potential in inhibition of release of mediators of the inflammatory process.
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Analgésicos/farmacología , Antiinflamatorios/farmacología , Passiflora/química , Extractos Vegetales/farmacología , Animales , Carragenina/efectos adversos , Edema/tratamiento farmacológico , Etanol/efectos adversos , Flavonoides/uso terapéutico , Masculino , Ratones , Nocicepción/efectos de los fármacos , Dolor/tratamiento farmacológico , Dimensión del Dolor , Componentes Aéreos de las Plantas/químicaRESUMEN
Pain and inflammation are complex clinical conditions that are present in a wide variety of disorders. Most drugs used to treat pain and inflammation have potential side effects, which makes it necessary to search for new sources of bioactive molecules. In this paper, we describe the ability of LASSBio-1586, an N-acylhydrazone derivative, to attenuate nociceptive behavior and the inflammatory response in mice. Antinociceptive activity was evaluated through acetic acid-induced writhing and formalin-induced nociception tests. In these experimental models, LASSBio-1586 significantly (p<0.05) reduced nociceptive behavior. Several methods of acute and chronic inflammation induced by different chemical (carrageenan, histamine, croton oil, arachidonic acid) and physical (cotton pellet) agents were used to evaluate the anti-inflammatory effect of LASSBio-1586. LASSBio-1586 exhibited potent anti-inflammatory activity in all tests (p<0.05). Study of the mechanism of action demonstrated the possible involvement of the nitrergic, serotonergic and histamine signaling pathways. In addition, a molecular docking study was performed, indicating that LASSBio-1586 is able to block the COX-2 enzyme, reducing arachidonic acid metabolism and consequently decreasing the production of prostaglandins, which are important inflammatory mediators. In summary, LASSBio-1586 exhibited relevant antinociceptive and anti-inflammatory potential and acted on several targets, making it a candidate for a new multi-target oral anti-inflammatory drug.
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Analgésicos/farmacología , Antiinflamatorios no Esteroideos/farmacología , Inhibidores de la Ciclooxigenasa 2/farmacología , Edema/tratamiento farmacológico , Hidrazonas/farmacología , Nocicepción/efectos de los fármacos , Dolor Nociceptivo/tratamiento farmacológico , Ácido Acético , Analgésicos/síntesis química , Animales , Antiinflamatorios no Esteroideos/síntesis química , Ácido Araquidónico/administración & dosificación , Carragenina/administración & dosificación , Aceite de Crotón/administración & dosificación , Ciclooxigenasa 2/química , Ciclooxigenasa 2/metabolismo , Inhibidores de la Ciclooxigenasa 2/síntesis química , Dexametasona/farmacología , Modelos Animales de Enfermedad , Edema/inducido químicamente , Edema/metabolismo , Edema/patología , Formaldehído , Miembro Posterior , Histamina/administración & dosificación , Hidrazonas/síntesis química , Indometacina/farmacología , Inflamación , Masculino , Ratones , Simulación del Acoplamiento Molecular , NG-Nitroarginina Metil Éster/farmacología , Dolor Nociceptivo/inducido químicamente , Dolor Nociceptivo/metabolismo , Dolor Nociceptivo/fisiopatología , Ondansetrón/farmacología , Prostaglandinas/biosíntesisRESUMEN
Alzheimer's and Parkinson's diseases are considered the most common neurodegenerative disorders, representing a major focus of neuroscience research to understanding the cellular alterations and pathophysiological mechanisms involved. Several natural products, including flavonoids, are considered able to cross the blood-brain barrier and are known for their central nervous system-related activity. Therefore, studies are being conducted with these chemical constituents to analyze their activities in slowing down the progression of neurodegenerative diseases. The present systematic review summarizes the pharmacological effects of flavonoids in animal models for Alzheimer's and Parkinson's diseases. A PRISMA model for systematic review was utilized for this search. The research was conducted in the following databases: PubMed, Web of Science, BIREME, and Science Direct. Based on the inclusion criteria, 31 articles were selected and discussed in this review. The studies listed revealed that the main targets of action for Alzheimer's disease therapy were reduction of reactive oxygen species and amyloid beta-protein production, while for Parkinson's disease reduction of the cellular oxidative potential and the activation of mechanisms of neuronal death. Results showed that a variety of flavonoids is being studied and can be promising for the development of new drugs to treat neurodegenerative diseases. Moreover, it was possible to verify that there is a lack of translational research and clinical evidence of these promising compounds.
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Enfermedad de Alzheimer/tratamiento farmacológico , Flavonoides/uso terapéutico , Enfermedad de Parkinson/tratamiento farmacológico , Proteínas Quinasas Activadas por AMP/metabolismo , Enfermedad de Alzheimer/patología , Péptidos beta-Amiloides/metabolismo , Animales , Flavonoides/metabolismo , Flavonoides/farmacología , Humanos , Óxido Nítrico Sintasa/metabolismo , Estrés Oxidativo/efectos de los fármacos , Enfermedad de Parkinson/patología , Especies Reactivas de Oxígeno/metabolismoRESUMEN
Inflammatory diseases result from the body's response to tissue damage, and if the resolution is not adequate or the stimulus persists, there will be progression from acute inflammation to chronic inflammation, leading to the development of cancer and neurodegenerative and autoimmune diseases. Due to the complexity of events that occur in inflammation associated with the adverse effects of drugs used in clinical practice, it is necessary to search for new biologically active compounds with anti-inflammatory activity. Among natural products, essential oils (EOs) present promising results in preclinical studies, with action in the main mechanisms involved in the pathology of inflammation. The present systematic review summarizes the pharmacological effects of EOs and their compounds in in vitro and in vivo models for inflammation. The research was conducted in the following databases: PubMed, Scopus, BIREME, Scielo, Open Grey, and Science Direct. Based on the inclusion criteria, 30 articles were selected and discussed in this review. The studies listed revealed a potential activity of EOs and their compounds for the treatment of inflammatory diseases, especially in chronic inflammatory conditions, with the main mechanism involving reduction of reactive oxygen and nitrogen species associated with an elevation of antioxidant enzymes as well as the reduction of the nuclear factor kappa B (NF-κB), reducing the expression of proinflammatory cytokines. Thus, this review suggests that EOs and their major compounds are promising tools for the treatment of chronic inflammation.
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Antioxidantes/uso terapéutico , Inflamación/tratamiento farmacológico , Aceites Volátiles/uso terapéutico , Animales , Enfermedad Crónica , Citocinas/metabolismo , Humanos , Inflamación/metabolismo , Inflamación/patología , FN-kappa B/metabolismoRESUMEN
O estudo objetiva traçar o perfil das Equipes de Saúde da Família (ESF) do município de Petrolina-PE, Brasil, quanto àscondições físico-estruturais nas quais se encontram e quanto à qualidade dos serviços de saúde prestados à população,analisando os principais problemas a serem enfrentados pelos profissionais de saúde em seu processo de trabalho. Foirealizado um estudo de caráter observacional descritivo, baseado na aplicação de um questionário semiestruturado, destinadoaos profissionais de saúde das mais diversas categorias que trabalham nas ESF do município de Petrolina. Entre osserviços disponibilizados pelo município nas ESF citados pelos profissionais, os considerados mais eficientes foram: vacinação,serviço de enfermagem e pré-natal, enquanto que a farmácia e odontologia foram consideradas os mais precários.A estrutura das unidades foi relatada como o principal problema que dificulta a execução dos serviços nas unidades (43%)e 27% dos profissionais entrevistados afirmaram que as unidades em que trabalham não conseguem atender à demanda.A escassez de profissionais, aliada à falta de equipamentos, materiais e medicamentos, acaba inviabilizando as práticasde trabalho, tornando o sistema de saúde vigente no país defasado, sobrecarregando os macrocomponentes dos níveis demédia e alta complexidade em saúde.
The study aims to evaluate the profile of ESF (Family Health Teams) in the city of Petrolina (Pernambuco, Brazil), concerningphysical and structural conditions of the ESF and concerning the quality of health services rendered to the population, byanalyzing the main problems to be faced by health professionals at work. An observational descriptive study was conductedbased on a semi-structured questionnaire intended to health professionals from several categories working at Petrolinas ESF.Among the services provided by the municipality in the ESF, mentioned by the professionals, the ones considered as moreeffective were vaccination, nursing services and prenatal care, while pharmacy and dentistry were considered the most precarious.The units structure was reported by 43% of the professional as the main problem that hinders the implementation ofservices in the units and 27% said that the units in which they work cannot meet the demand. The shortage of professionalscoupled with lack of equipment, supplies and medicines preclude the working practices, lagging the current health system inthe country, overloading macrocomponents of medium and high levels of complexity in health.