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The flowers of Yucca aloifolia ("flor de izote") are considered a millenary food in the Northeastern Highlands of Puebla, Mexico. The present investigation reports on the chemical and biological activities of the hydroalcoholic extract (YAHF) obtained from this edible source. HPLC-MS profiling revealed twenty bioactive phenolic compounds with chlorogenic acid (16.5â mg g-1 DW), quercetin (9.5â mg g-1 FW), and their glycosides (rutin and quercitrin), as well as caffeic acid (8.4â mg g-1 DW) and ferulic acid (7.9â mg g-1 DW) as major compounds dissolved in YAHF. Six metabolites had potent anti-lipase (IC50<100â µg mL-1) and anti-ornithine decarboxylase activity (IC50<100â µg mL-1), whereas thirteen exerted strong anti-alpha-glucosidase properties (IC50<100â µg mL-1). The evaluation of YAHF in mice subjected to standard oral glucose tolerance tests and prolonged administration of hypercaloric/atherogenic diet (30â days), unraveled their ability to improve glucose and lipid profiles. YAHF and six phenolic compounds significantly reduced DLD-1 cell viability (IC50, 117.9â µg mL-1) and avoided polyamine accumulation linked to anti-ornithine decarboxylase activity. YAHF and its twenty constituents exerted low toxicity in probiotics (>1000â µg mL-1) and 3T3 fibroblasts (>2.5â mg-mL-1), sustaining their safeness for human consumption.
Assuntos
Sobrevivência Celular , Flores , Fenóis , Extratos Vegetais , Fenóis/farmacologia , Fenóis/química , Fenóis/isolamento & purificação , Animais , Flores/química , Camundongos , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Humanos , Sobrevivência Celular/efeitos dos fármacos , Suplementos Nutricionais/análise , MasculinoRESUMO
We present the inhibitory properties of the R. pompana anthocyanin fraction (RPAF) and its major constituents on alpha-glucosidase (AG), pancreatic lipase (PL), HMG-CoA reductase, and ornithine decarboxylase (ODC). The effect of RPAF was also evaluated in ICR male mice subjected to oral glucose tolerance test (OGTT) and hypercaloric/atherogenic diet for 30â days. RP-HPLC/MS profiling revealed that RPAF contained five major anthocyanins and induced slight inhibition on PL and HMG-CoA reductase (IC50 , 245-338â µg mL-1 ) whereas strong activity on AG and ODC (IC50 , 130-133â µg mL-1 ) was observed. Kinetic studies and molecular docking with pelargonidin-3-O-rutinoside (P3R) on ODC, revealed changes in Km (0.9514-0.9746â mM) and Vmax (1.96-2.32â µmol mg-1 min-1 ) suggesting mixed inhibition and molecular interaction with two active sites of ODC. P3R showed antiproliferative activity (IC50, 46.5â µM) and decreased polyamine accumulation in DLD-1 cells. The results of OGTT confirmed that RPAF regulates postprandial glucose levels in diabetic animals which experienced a significant glucose depletion (30 %; p<0.001) from 30 to 120â min post-treatment. Prolonged supplementation of RPAF caused significant decrease (p<0.001) in plasma glucose, total cholesterol, LDL-c and triglycerides as well as significant increase (p<0.001) of HDL-c compared with normoglycemic untreated animals.
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There are approximately 250 species of Eryngium L. distributed throughout the world, with North America and South America being centers of diversity on this continent. In the central-western region of Mexico there may be around 28 species of this genus. Some Eryngium species are cultivated as leafy vegetables, ornamental, and medicinal plants. In traditional medicine they are used to treat respiratory and gastrointestinal conditions, diabetes, and dyslipidemia, among others. This review addresses the phytochemistry and biological activities, as well as traditional uses, distribution, and characteristics of the eight species of Eryngium reported as medicinal in the central-western region of Mexico: E. cymosum, E. longifolium, E. fluitans (or mexicanum), E. beecheyanum, E. carlinae, E. comosum, E. heterophyllum, and E. nasturtiifolium. The extracts of the different Eryngium spp. have shown biological activities such as hypoglycemic, hypocholesterolemic, renoprotective, anti-inflammatory, antibacterial, and antioxidant, among others. E. carlinae is the most studied species, and phytochemical analyses, performed mainly by high-performance liquid chromatography (HPLC) and gas chromatography coupled with mass spectrometry (GC-MS), have shown its content of terpenoids, fatty acids, organic acids, phenolic acids, flavonoids, sterols, saccharides, polyalcohols, and aromatic and aliphatic aldehydes. According to the results of this review on Eryngium spp., they constitute a relevant alternative as a source of bioactive compounds for pharmaceutical, food, and other industries. However, there is a lot of research to be conducted regarding phytochemistry, biological activities, cultivation, and propagation, in those species with few or no reports.
Assuntos
Apiaceae , Eryngium , Etnobotânica , Eryngium/química , México , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/química , EtnofarmacologiaRESUMO
This study describes the synthesis, characterization, and biological activity of a new class of antidiabetic oxidovanadium(IV)-complexes with S2O2 coordination mode. The target complex 3,6-dithio-1,8-octanediolatooxidovanadium(IV), abbreviated as ([VIVO(octd)]), where octd = 3,6-dithio-1,8-octanediol, is formed from the reaction between the 3,6-dithio-1,8-octanediol and vanadyl sulfate (VIVOSO4). The effects of treatment with ([VIVO(octd)] on blood glucose, lipidic profile, body weight, food intake, water intake, urinary volume, glycogen levels, and biomarkers for liver toxicity were investigated using a streptozotocin (STZ)-induced diabetic Wistar rats model. The results have shown that the [VIVO(octd)] complex caused a significant decrease in blood glucose (247.6 ± 19.3 mg/dL vs 430.1 ± 37.6 mg/dL diabetic group, p < 0.05), triglycerides (TG, 50%) and very low-density cholesterol (VLDL-C, 50%) levels in STZ-diabetic rats after 3 weeks of treatment. The [VIVO(octd)] has shown antihyperglycemic activity in diabetic rats as well as a reduction in elevated lipid levels. Time-dependent studies using EPR and 51V NMR spectroscopy of [VIVO(octd)] were done in aqueous solutions to determine the complex stability and species present in the oral gavage solution used for complex administration. The spectroscopic studies have shown that the antidiabetic/hypolipidemic activity could be attributed to [VIVO(octd)], vanadium species resulting from redox processes, the hydrolysis of [VIVO(octd)] and its decomposition products, or some combination of these factors. In summary, the oxidovanadium(IV) complex containing the S2O2 donor ligand has desirable antidiabetic properties eliminating the symptoms of Diabetes mellitus and its comorbidities.
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Diabetes Mellitus Experimental , Hipoglicemiantes , Ratos , Animais , Hipoglicemiantes/farmacologia , Glicemia , Ratos Wistar , Vanádio/químicaRESUMO
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.
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Passiflora , Passifloraceae , Camundongos , Animais , Passiflora/química , Farinha , Espectrometria de Massas em Tandem , Extratos Vegetais/farmacologia , Etanol , Pectinas , LipídeosRESUMO
RESUMEN INTRODUCCIÓN: El ACV es uno de los eventos cardiovasculares más prevalentes en el mundo, en Colombia es la segunda causa de muerte y la primera de discapacidad. Uno de los factores de riesgo más importantes para tener en cuenta es el control del colesterol, la reducción de los niveles de C-LDL, principalmente por medio del tratamiento con estatinas y otros fármacos hipolipemiantes. MATERIALES Y MÉTODOS: En esta revisión narrativa de la literatura se ha recogido la información más relevante sobre el uso y los beneficios de este tratamiento y algunas consideraciones adicionales. CONCLUSIÓN: Los hallazgos de esta revisión demuestran el efecto protector de esta terapia cuando se consiguen reducir los niveles de C-LDL y colesterol, además, las otras terapias como ezetimiba o inhibidores de PSCK9. Por otro lado, los estudios mencionan posibles efectos beneficiosos en el contexto de ACV pero se requieren más ensayos clínicos.
ABSTRACT INTRODUCTION: Stroke is one of the most prevalent cardiovascular events in the world, in Colombia it is the second cause of death and first in disability. One of the most important risk factors to consider is cholesterol control, the reduction of LDL-C and cholesterol levels, mainly through treatment with statins and other lipid-lowering drugs. MATERIALS AND METHODS: The most relevant information on the use and benefits of this treatment and some additional considerations have been collected in this narrative review of the literature. CONCLUSION: The results of this narrative review show the protective effect of this therapy when it is possible to reduce LDL-C and cholesterol levels, in addition to other therapies such as ezetimibe or PSCK9 inhibitors. On the other hand, studies mention possible beneficial effects in the context of stroke but more clinical trials are required.
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Inibidores de Hidroximetilglutaril-CoA Redutases , Acidente Vascular Cerebral , LDL-Colesterol , HipolipemiantesRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Although Mexican oregano inhibits digestive enzymes in vitro its effect on the absorption of carbohydrates and lipids in vivo has not been addressed. AIM OF THE STUDY: Assess the effect of Mexican oregano (Lippia graveolens Kunth) on carbohydrates and lipids absorption in vivo. The antioxidant activity also was investigated. MATERIALS AND METHODS: Enzymatic inhibitory action of lipase, α-amylase, and α-glucosidase was evaluated in vitro. Oral lipid (OLTT) and starch tolerance tests (OSTT) were conducted with L. graveolens acetone (O-A) and ethanol (O-E) extracts (at 102 mg/kg body weight equivalent to a 1 g human doses) in male Wistar rats. The antioxidant activity was evaluated through inhibition of lipid peroxidation and scavenging radical. RESULTS: Both extracts exhibited higher inhibitory median concentration (IC50) of lipase activity (1.9 µg/µL for O-E and 1.8 µg/µL for O-A) than the positive control (Orlistat) (0.07 µg/µL). The IC50 of α-amylase was higher (41.8 µg/µL for O-E and 25.2 µg/µL for O-A) than the Acarbose (2.5 µg/µL); while α-glucosidase results showed not statistically differences between groups (â¼1.7 µg/µL). The OLTT results showed that both extracts significantly reduced serum triglycerides (â¼147 mg/dL for O-E and â¼155 mg/dL for O-A) as compared with negative control group (only lipid load). In the OSTT, glucose levels showed a significant decrease (â¼31 mg/dL for O-E and â¼17 mg/dL for O-A) than the negative control group (only starch load). About in vitro antioxidant evaluation, not statistically differences between extracts and positive control (Trolox) were observed for scavenged free radicals (â¼2.0 µg/µL); whereas O-A inhibited lipid peroxidation similar to the Trolox (â¼0.8 µg/µL IC50). The main chemical composition of both extracts was coumaric acid, luteolin, rutinoside, naringenin, and carvacrol. CONCLUSIONS: Both extracts reduce lipid absorption; whereas O-E decreases carbohydrate absorption in vivo. Both extracts inhibit lipid peroxidation and scavenging free radicals in vitro.
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Lippia , Origanum , Animais , Antioxidantes/química , Antioxidantes/farmacologia , Carboidratos , Humanos , Lipase , Lipídeos , Lippia/química , Masculino , Origanum/química , Extratos Vegetais/química , Ratos , Ratos Wistar , Amido , alfa-Amilases , alfa-GlucosidasesRESUMO
Abstract The extract of Belamcanda chinensis leaves (BCLE) is a traditional Chinese herbal medicine for the treatment of diabetes-related hyperlipidemia in Hainan province, South China. In this study, the lipid-decreasing effects of BCLE on obese diabetes were investigated on KK-Ay mice. The component F2 ameliorated lipid disorder, as indicated by decreased levels of body weight, liver index, levels of TC, TG and LDL-c in the serum and liver. The enhancement effect of F2 on liver SOD and the inhibitory effect of F2 on MDA demonstrated that F2 exhibited significant antioxidant activity on liver injury. F2 also prevented vacuolar degeneration and reduced pathological tissue injury in liver. In addition, the component F1 decreased the levels of TG, LDL-c and MDA in the liver. These findings suggest that F2 may have therapeutic potential in the prevention and therapy of hyperlipemia and liver disease associated with obesity-related diabetes.
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Campomanesia xanthocarpa, a plant belonging to the Myrtaceae family, is popularly known as gabiroba. Leaves of gabiroba has been popularly used to treat various diseases, including inflammatory, renal, and digestive, among others. Additionally, studies have shown an effect to reduce blood cholesterol levels. The aim of this study was to evaluate the antihyperglycemic and hypolipidemic effects of Campomanesia xanthocarpa seed extract in hyperglycemic rats. The results showed that 400 mg/kg of seed extract was able to decrease blood glucose levels and to increase the muscular and hepatic glycogen content as well as to inhibit the sucrase and maltase activity. At doses of 200 mg/kg and 800 mg/kg, the activity of these enzymes was also reduced. In the lipid profile 400 mg/kg produced a decrease in total and LDL cholesterol serum levels; and with 200 mg/kg there was an increase in HDL cholesterol levels. The extract did not present hepatic and renal toxic effects at the different doses tested. The results suggest that the treatment with Campomanesia xanthocarpa seeds extract is useful in reducing glycemia, total cholesterol and LDL levels with potential adjuvant therapeutic in the treatment of diabetes and hypercholesterolemia, however, additional pharmacological and toxicological studies are still required.(AU)
Campomanesia xanthocarpa, planta pertencente à família Mirtaceae, é popularmente conhecida como gabiroba. Folhas da gabiroba são popularmente usadas para tratar de doenças inflamatórias, renais, digestivas entre outras. Além disso, estudos têm mostrado um efeito redutor dos níveis de colesterol. O objetivo deste estudo foi avaliar os efeitos anti-hiperglicêmico e hipolipidêmico do extrato de sementes de Campomanesia xanthocarpa em ratos hiperglicêmicos. Os resultados mostraram que 400 mg/kg do extrato da semente foi capaz de reduzir os níveis de glicose sanguínea e aumentar o conteúdo de glicogênio hepático e muscular, bem como inibir a atividade da maltase e sacarase. Na dose de 200 mg/kg e 800 mg/kg, a atividade das enzimas também foi reduzida. No perfil lipídico, 400 mg/kg produziu uma redução nos níveis séricos de colesterol total e LDL e com 200 mg/kg houve um aumento nos níveis de colesterol HDL. O extrato não apresentou efeitos tóxicos hepáticos e renais nas doses testadas. Os resultados sugerem que o tratamento com o extrato de Campomanesia xanthocarpa é eficaz na redução da glicemia, de colesterol total e LDL com potencial para tratamento adjuvante do diabetes e hipercolesterolemia, no entanto estudos farmacológicos e toxicológicos adicionais são necessários.(AU)
Assuntos
Animais , Ratos , Hipoglicemiantes , Hipolipemiantes , Extratos Vegetais/uso terapêutico , Hiperglicemia/veterináriaRESUMO
Abstract Campomanesia xanthocarpa, a plant belonging to the Myrtaceae family, is popularly known as gabiroba. Leaves of gabiroba has been popularly used to treat various diseases, including inflammatory, renal, and digestive, among others. Additionally, studies have shown an effect to reduce blood cholesterol levels. The aim of this study was to evaluate the antihyperglycemic and hypolipidemic effects of Campomanesia xanthocarpa seed extract in hyperglycemic rats. The results showed that 400 mg/kg of seed extract was able to decrease blood glucose levels and to increase the muscular and hepatic glycogen content as well as to inhibit the sucrase and maltase activity. At doses of 200 mg/kg and 800 mg/kg, the activity of these enzymes was also reduced. In the lipid profile 400 mg/kg produced a decrease in total and LDL cholesterol serum levels; and with 200 mg/kg there was an increase in HDL cholesterol levels. The extract did not present hepatic and renal toxic effects at the different doses tested. The results suggest that the treatment with Campomanesia xanthocarpa seeds extract is useful in reducing glycemia, total cholesterol and LDL levels with potential adjuvant therapeutic in the treatment of diabetes and hypercholesterolemia, however, additional pharmacological and toxicological studies are still required.
Resumo Campomanesia xanthocarpa, planta pertencente à família Mirtaceae, é popularmente conhecida como gabiroba. Folhas da gabiroba são popularmente usadas para tratar de doenças inflamatórias, renais, digestivas entre outras. Além disso, estudos têm mostrado um efeito redutor dos níveis de colesterol. O objetivo deste estudo foi avaliar os efeitos anti-hiperglicêmico e hipolipidêmico do extrato de sementes de Campomanesia xanthocarpa em ratos hiperglicêmicos. Os resultados mostraram que 400 mg/kg do extrato da semente foi capaz de reduzir os níveis de glicose sanguínea e aumentar o conteúdo de glicogênio hepático e muscular, bem como inibir a atividade da maltase e sacarase. Na dose de 200 mg/kg e 800 mg/kg, a atividade das enzimas também foi reduzida. No perfil lipídico, 400 mg/kg produziu uma redução nos níveis séricos de colesterol total e LDL e com 200 mg/kg houve um aumento nos níveis de colesterol HDL. O extrato não apresentou efeitos tóxicos hepáticos e renais nas doses testadas. Os resultados sugerem que o tratamento com o extrato de Campomanesia xanthocarpa é eficaz na redução da glicemia, de colesterol total e LDL com potencial para tratamento adjuvante do diabetes e hipercolesterolemia, no entanto estudos farmacológicos e toxicológicos adicionais são necessários.
Assuntos
Animais , Ratos , Dióxido de Carbono , Myrtaceae , Sementes , Extratos Vegetais/farmacologia , Hipoglicemiantes/farmacologiaRESUMO
BACKGROUND: Type 2 diabetes mellitus (T2DM) greatly increases cardiovascular risk. Primary and secondary cardiovascular prevention lead to lower cardiovascular events, improved quality of life and lower costs related to complications. OBJECTIVE: To estimate the proportion of patients with T2DM undergoing drug therapy for cardiovascular prevention (aspirin and statins) in Colombia and to describe the change in patterns of use between 2008 and 2018. METHODS: This was a cross-sectional study comparing prescriptions for aspirin and statins in 2008 and in 2018 in outpatients diagnosed with T2DM. Records were obtained from a national drug claim database. The proportion of use of cardiovascular prevention drugs and antidiabetic drugs, medications for comorbidities and sociodemographic variables were analyzed for both periods. RESULTS: In total, 26 742 patients in 2008 and 188 321 in 2018 with a diagnosis of T2DM treated with antidiabetic drugs were identified, among whom 57.5% and 44.2% received aspirin and 44.9% and 60.2% received statins, respectively. The use of high-intensity statins increased from 1.1% in 2008 to 95.2% in 2018. The probabilities of receiving drugs in 2008 and in 2018 were higher for men (OR: 1.12, 95% CI: 1.06-1.17 and OR: 1.26, 95% CI: 1.23-1.28, respectively), for those persons over 75 years of age (OR: 6.5, 95% CI: 5.3-7.9 and OR: 5.8, 95% CI: 5.4-6.2) and for those who also received clopidogrel (OR: 5.8, 95% CI: 4.4-7.6 and OR: 2.2, 95% CI: 2.1-2.4). CONCLUSIONS: The use of high-intensity statins in patients with T2DM has increased significantly in the last decade, which should reduce cardiovascular events, morbidity and mortality.
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Doenças Cardiovasculares , Diabetes Mellitus Tipo 2 , Inibidores de Hidroximetilglutaril-CoA Redutases , Preparações Farmacêuticas , Aspirina/uso terapêutico , Doenças Cardiovasculares/epidemiologia , Doenças Cardiovasculares/prevenção & controle , Colômbia/epidemiologia , Estudos Transversais , Diabetes Mellitus Tipo 2/tratamento farmacológico , Diabetes Mellitus Tipo 2/epidemiologia , Humanos , Inibidores de Hidroximetilglutaril-CoA Redutases/uso terapêutico , Masculino , Prevalência , Qualidade de VidaRESUMO
Background: Statins have extensive hepatic metabolism and can have multiple pharmacological interactions. The aim was to identify the main pharmacokinetic interactions between statins and their comedications in a group of patients from Colombia.Research design and methods: A cross-sectional study of pharmacokinetic interactions in patients treated with statins who were identified from a population database. The interactions were documented using the Lexicomp® database.Results: A total of 123,026 patients with statin prescriptions were identified, with a mean age of 68.4 ± 11.5 years; 57.1% were women, and 81.6% received atorvastatin. A total of 19.4% (n = 23.831) of patients presented pharmacological interactions. Some 15,474 (12.6%) had interactions classified as category C, 7.4% (n = 9077) as category D, and 0.5% (n = 660) as category X. 36.8% of the patients with lovastatin prescriptions had some interaction. Age older than 65 years, male sex, residence in capital cities, comorbidities, endocrine pathologies and HIV were associated with an increase in the probability of having contraindicated or risky interactions.Conclusions: Important interactions between statins and other medications were more common in adults over 65 years of age and those with endocrine comorbidities or HIV infection. This knowledge should help when proposing solutions that reduce the risk of adverse reactions.
Assuntos
Atorvastatina/farmacocinética , Inibidores de Hidroximetilglutaril-CoA Redutases/farmacocinética , Lovastatina/farmacocinética , Adolescente , Adulto , Fatores Etários , Idoso , Idoso de 80 Anos ou mais , Atorvastatina/administração & dosagem , Colômbia , Estudos Transversais , Bases de Dados Factuais , Interações Medicamentosas , Doenças do Sistema Endócrino/epidemiologia , Feminino , Infecções por HIV/epidemiologia , Humanos , Inibidores de Hidroximetilglutaril-CoA Redutases/administração & dosagem , Lovastatina/administração & dosagem , Masculino , Pessoa de Meia-Idade , Fatores de Risco , Fatores Sexuais , Adulto JovemRESUMO
The plant, Malva neglecta wallr., is widely consumed for medicinal and nutritional purposes. The current study was carried out to assess the hypoglycemic and antihyperlipidemic potential of aqueous methanolic extract of M. neglecta. Chemical evaluation of the extract was performed by high pressure liquid chromatography. Oral glucose tolerance test (OGTT) was done in diabetic rats pre-exposed to 250, 500 and 750 mg/kg plant extract via the oral route. For hypoglycemic and biochemical study, the same therapy was administered to alloxan induced diabetic rats for 14 days. The standard control group received Glibenclamide (5 mg/kg). Ferulic acid, p-coumaric acid and other phenolic acids were detected and estimated in the extract. Administration of the plant extract significantly reduced blood glucose level in diabetic rats subjected to OGTT. The plant extract lowered the fasting blood glucose and alpha amylase, and prevented the damage to pancreas. It also corrected dyslipidemia in diabetic animals following 14 days therapy. Hence, this experimental study establishes the fact that M. neglecta exhibited significant antidiabetic and antihyperlipidemic activities in alloxan induced diabetic rats.
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Animais , Masculino , Feminino , Ratos , Extratos Vegetais/análise , Malvaceae/classificação , Malva/efeitos adversos , Hiperglicemia/tratamento farmacológico , Hiperlipidemias/tratamento farmacológico , Hipolipemiantes/administração & dosagem , Cromatografia Líquida de Alta Pressão/métodosRESUMO
Metabolic syndrome comprises a cluster of metabolic disorders related to the development of cardiovascular disease and type 2 diabetes mellitus. In latter years, plant secondary metabolites have become of special interest because of their potential role in preventing and managing metabolic syndrome. Sesquiterpene lactones constitute a large and diverse group of biologically active compounds widely distributed in several medicinal plants used for the treatment of metabolic disorders. The structural diversity and the broad spectrum of biological activities of these compounds drew significant interests in the pharmacological applications. This review describes selected sesquiterpene lactones that have been experimentally validated for their biological activities related to risk factors of metabolic syndrome, together with their mechanisms of action. The potential beneficial effects of sesquiterpene lactones discussed in this review demonstrate that these substances represent remarkable compounds with a diversity of molecular structure and high biological activity, providing new insights into the possible role in metabolic syndrome management.
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Abstract Campomanesia xanthocarpa, a plant belonging to the Myrtaceae family, is popularly known as gabiroba. Leaves of gabiroba has been popularly used to treat various diseases, including inflammatory, renal, and digestive, among others. Additionally, studies have shown an effect to reduce blood cholesterol levels. The aim of this study was to evaluate the antihyperglycemic and hypolipidemic effects of Campomanesia xanthocarpa seed extract in hyperglycemic rats. The results showed that 400 mg/kg of seed extract was able to decrease blood glucose levels and to increase the muscular and hepatic glycogen content as well as to inhibit the sucrase and maltase activity. At doses of 200 mg/kg and 800 mg/kg, the activity of these enzymes was also reduced. In the lipid profile 400 mg/kg produced a decrease in total and LDL cholesterol serum levels; and with 200 mg/kg there was an increase in HDL cholesterol levels. The extract did not present hepatic and renal toxic effects at the different doses tested. The results suggest that the treatment with Campomanesia xanthocarpa seeds extract is useful in reducing glycemia, total cholesterol and LDL levels with potential adjuvant therapeutic in the treatment of diabetes and hypercholesterolemia, however, additional pharmacological and toxicological studies are still required.
Resumo Campomanesia xanthocarpa, planta pertencente à família Mirtaceae, é popularmente conhecida como gabiroba. Folhas da gabiroba são popularmente usadas para tratar de doenças inflamatórias, renais, digestivas entre outras. Além disso, estudos têm mostrado um efeito redutor dos níveis de colesterol. O objetivo deste estudo foi avaliar os efeitos anti-hiperglicêmico e hipolipidêmico do extrato de sementes de Campomanesia xanthocarpa em ratos hiperglicêmicos. Os resultados mostraram que 400 mg/kg do extrato da semente foi capaz de reduzir os níveis de glicose sanguínea e aumentar o conteúdo de glicogênio hepático e muscular, bem como inibir a atividade da maltase e sacarase. Na dose de 200 mg/kg e 800 mg/kg, a atividade das enzimas também foi reduzida. No perfil lipídico, 400 mg/kg produziu uma redução nos níveis séricos de colesterol total e LDL e com 200 mg/kg houve um aumento nos níveis de colesterol HDL. O extrato não apresentou efeitos tóxicos hepáticos e renais nas doses testadas. Os resultados sugerem que o tratamento com o extrato de Campomanesia xanthocarpa é eficaz na redução da glicemia, de colesterol total e LDL com potencial para tratamento adjuvante do diabetes e hipercolesterolemia, no entanto estudos farmacológicos e toxicológicos adicionais são necessários.
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BACKGROUND: A considerable amount of randomized controlled trials (RCTs) have been published on statins and/or fibrates for diabetic retinopathy, a clinical condition associated with high social and economic burden. Adherence to the CONSORT statement items is imperative to ensure transparency and reproducibility in clinical research. The aim of this study is to assess the reporting quality and the adherence to CONSORT of RCTs assessing statins and/or fibrates for diabetic retinopathy. METHODS: We conducted a critical appraisal study at Discipline of Evidence-based Medicine, Escola Paulista de Medicina, Universidade Federal de São Paulo (Unifesp). A sensitive literature search was performed to identify all relevant RCTs, with no time or language limits. Two authors independently evaluated the reporting quality of the selected RCTs using the CONSORT statement as a standard. RESULTS: Thirteen reports of RCTs were included in this study. The adherence of the reports to CONSORT items ranged from 24% to 68%. The median score was 11 (interquartile range (IQR) 8 to 13). When analyzed separately, the methods sections of the reports had a median of three items (IQR 2 to 4) judged adherent to the methods items of CONSORT (items 3 to 12). The most underreported items were those related to trial design, title and abstract, allocation concealment, implementation of the randomization sequence, and blinding. Other important items, such as the one related to the description of the inclusion criteria, also had low adherence. CONCLUSIONS: The overall adherence to the CONSORT checklist items was poor, especially in the items related to the methods section. RCT reports on statins and/or fibrates for diabetic retinopathy must be optimized to avoid reporting biases and to improve transparency and reproducibility.
Assuntos
Lista de Checagem/normas , Confiabilidade dos Dados , Retinopatia Diabética/tratamento farmacológico , Ácidos Fíbricos/uso terapêutico , Fidelidade a Diretrizes/normas , Inibidores de Hidroximetilglutaril-CoA Redutases/uso terapêutico , Ensaios Clínicos Controlados Aleatórios como Assunto/normas , Projetos de Pesquisa/normas , Retinopatia Diabética/diagnóstico , Ácidos Fíbricos/efeitos adversos , Humanos , Inibidores de Hidroximetilglutaril-CoA Redutases/efeitos adversos , Resultado do TratamentoRESUMO
INTRODUCTION: Lipid-lowering drugs, especially statins, have shown great relevance in preventing and treating cardiovascular diseases. OBJECTIVE: To determine the prescription patterns of lipid-lowering drugs and the variables associated with their use in a Colombian population. MATERIALS AND METHODS: This is a cross-sectional descriptive study. From a drug dispensing database of approximately 4.5 million Colombian health system affiliates, patients of all ages and both sexes treated with lipid-lowering agents (statins, fibrates, ezetimibe) were identified between January and March, 2017. Demographic, pharmacological and co-medication variables were included. RESULTS: In total, 103,624 patients were identified as being treated with lipid-lowering agents. The average age was 67.5 years, and 49.8% were 65 years or older. Women comprised 58.0% of the patients. Statins were the most used (n=96,910; 93.5%), and atorvastatin (n=80,812; 78.0%) and lovastatin (n=12,621; 12.2%) were the most frequent. The mean atorvastatin dose was 30.3 mg/day, and 49.9% of its users received presentations of 40 mg or more. A total of 9,258 (8.9%) patients received fibrates, and only 780 (0.8%) were taking ezetimibe. Of this population, 94.9% were treated with lipid-lowering monotherapy, and 97.3% (n=100,813) had co-medication for their comorbidities, with the most frequent being antihypertensive (89.1%), antiplatelet (57.8%), antidiabetic (31.5%) and antiulcerative agents (34.2%). CONCLUSIONS: Atorvastatin is currently the most frequently used lipid-lowering drug in this group of Colombian patients, especially in monotherapy and at doses close to the defined daily dose. Only half received high-intensity doses. New studies are required to verify the efficacy of these therapies.
Introducción. Los fármacos hipolipemiantes, especialmente las estatinas, han demostrado gran relevancia para la prevención y el tratamiento de las enfermedades cardiovasculares. Objetivo. Determinar los patrones de prescripción de los fármacos hipolipemiantes y las variables asociadas con su uso en una población de Colombia. Materiales y métodos. Se trata de un estudio descriptivo y transversal. A partir de una base de datos de dispensación de medicamentos de 4,5 millones de afiliados al sistema de salud de Colombia, se identificaron los pacientes de cualquier edad y sexo en tratamiento con hipolipemiantes (estatinas, fibratos, ezetimibe), entre enero y marzo de 2017. Se incluyeron variables demográficas, farmacológicas y de comedicaciones. Resultados. Se identificaron 103.624 pacientes en tratamiento con hipolipemiantes. La edad promedio fue de 67,5 años y el 49,8 % tenía 65 o más años. El 58,0 % eran mujeres. Las estatinas fueron los más utilizados (n=96.910; 93,5 %), siendo la atorvastatina (n=80.812; 78,0 %) y la lovastatina (n=12.621; 12,2 %) las más frecuentes. La dosis promedio de atorvastatina fue de 30,3 mg/día y el 49,9 % de sus usuarios recibía presentaciones de 40 mg o más. Un total de 9.258 (8,9 %) pacientes recibían fibratos y solo 780 (0,8 %) tomaban ezetimibe. El 94,9 % de casos recibió tratamiento en monoterapia hipolipemiante y el 97,3 % (n=100.813) tenía comedicaciones para comorbilidades, siendo las más frecuentes antihipertensivos (89,1 %), antiagregantes plaquetarios (57,8 %), antidiabéticos (31,5 %) y antiulcerosos (34,2 %). Conclusiones. La atorvastatina es actualmente el medicamento hipolipemiante más utilizado en este grupo de pacientes de Colombia, especialmente en monoterapia y a dosis cercanas a las definidas, aunque solo la mitad recibían dosis recibían dosis de alta intensidad. Se requieren nuevos estudios que verifiquen la efectividad de estos tratamientos.
Assuntos
Hipolipemiantes/uso terapêutico , Adolescente , Adulto , Distribuição por Idade , Idoso , Idoso de 80 Anos ou mais , Atorvastatina/administração & dosagem , Atorvastatina/uso terapêutico , Cidades/estatística & dados numéricos , Colômbia , Estudos Transversais , Quimioterapia Combinada , Ezetimiba/administração & dosagem , Ezetimiba/uso terapêutico , Feminino , Humanos , Inibidores de Hidroximetilglutaril-CoA Redutases/administração & dosagem , Inibidores de Hidroximetilglutaril-CoA Redutases/uso terapêutico , Hipolipemiantes/administração & dosagem , Lovastatina/administração & dosagem , Lovastatina/uso terapêutico , Masculino , Pessoa de Meia-Idade , Distribuição por Sexo , Adulto JovemRESUMO
Introduction. Lipid-lowering drugs, especially statins, have shown great relevance in preventing and treating cardiovascular diseases. Objective. To determine the prescription patterns of lipid-lowering drugs and the variables associated with their use in a Colombian population. Materials and methods. This is a cross-sectional descriptive study. From a drugdispensing database of approximately 4.5 million Colombian health system affiliates, patients of all ages and both sexes treated with lipid-lowering agents (statins, fibrates, ezetimibe) were identified between January and March, 2017. Demographic, pharmacological and co-medication variables were included. Results. In total, 103,624 patients were identified as being treated with lipid-lowering agents. The average age was 67.5 years, and 49.8% were 65 years or older. Women comprised 58.0% of the patients. Statins were the most used (n=96,910; 93.5%), and atorvastatin (n=80,812; 78.0%) and lovastatin (n=12,621; 12.2%) were the most frequent. The mean atorvastatin dose was 30.3 mg/day, and 49.9% of its users received presentations of 40 mg or more. A total of 9,258 (8.9%) patients received fibrates, and only 780 (0.8%) were taking ezetimibe. Of this population, 94.9% were treated with lipid-lowering monotherapy, and 97.3% (n=100,813) had co-medication for their comorbidities, with the most frequent being antihypertensive (89.1%), antiplatelet (57.8%), antidiabetic (31.5%) and antiulcerative agents (34.2%). Conclusions. Atorvastatin is currently the most frequently used lipid-lowering drug in this group of Colombian patients, especially in monotherapy and at doses close to the defined daily dose. Only half received high-intensity doses. New studies are required to verify the efficacy of these therapies.
Introducción. Los fármacos hipolipemiantes, especialmente las estatinas, han demostrado gran relevancia para la prevención y el tratamiento de las enfermedades cardiovasculares. Objetivo. Determinar los patrones de prescripción de los fármacos hipolipemiantes y las variables asociadas con su uso en una población de Colombia. Materiales y métodos. Se trata de un estudio descriptivo y transversal. A partir de una base de datos de dispensación de medicamentos de 4,5 millones de afiliados al sistema de salud de Colombia, se identificaron los pacientes de cualquier edad y sexo en tratamiento con hipolipemiantes (estatinas, fibratos, ezetimibe), entre enero y marzo de 2017. Se incluyeron variables demográficas, farmacológicas y de comedicaciones. Resultados. Se identificaron 103.624 pacientes en tratamiento con hipolipemiantes. La edad promedio fue de 67,5 años y el 49,8 % tenía 65 o más años. El 58,0 % eran mujeres. Las estatinas fueron los más utilizados (n=96.910; 93,5 %), siendo la atorvastatina (n=80.812; 78,0 %) y la lovastatina (n=12.621; 12,2 %) las más frecuentes. La dosis promedio de atorvastatina fue de 30,3 mg/día y el 49,9 % de sus usuarios recibía presentaciones de 40 mg o más. Un total de 9.258 (8,9 %) pacientes recibían fibratos y solo 780 (0,8 %) tomaban ezetimibe. El 94,9 % de casos recibió tratamiento en monoterapia hipolipemiante y el 97,3 % (n=100.813) tenía comedicaciones para comorbilidades, siendo las más frecuentes antihipertensivos (89,1 %), antiagregantes plaquetarios (57,8 %), antidiabéticos (31,5 %) y antiulcerosos (34,2 %). Conclusiones. La atorvastatina es actualmente el medicamento hipolipemiante más utilizado en este grupo de pacientes de Colombia, especialmente en monoterapia y a dosis cercanas a las definidas, aunque solo la mitad recibían dosis recibían dosis de alta intensidad. Se requieren nuevos estudios que verifiquen la efectividad de estos tratamientos.
Assuntos
Dislipidemias , Hipolipemiantes , Prescrições de Medicamentos , Farmacoepidemiologia , Inibidores de Hidroximetilglutaril-CoA Redutases , EzetimibaRESUMO
Resumen Introducción: Los estudios de utilización de medicamentos sirven para evaluar la efectividad y seguridad de los fármacos en la práctica real, diferente al contexto del estudio clínico controlado. Los hipolipemiantes actúan sobre el perfil lipídico disminuyendo el riesgo de enfermedades cardiovasculares. Objetivo: Describir el desempeño clínico y seguridad de la utilización de medicamentos hipolipemiantes en la práctica médica real en una cohorte de pacientes con diagnóstico de dislipidemia. Metodología: Estudio observacional de cohorte. Se siguió una cohorte de pacientes con indicación de hipolipemiantes durante 6 meses, en 12 ciudades de Colombia pertenecientes a un registro biomédico de seguimiento de pacientes tratados con medicamentos del portafolio de Abbott. Se midieron variables demográficas y clínicas basales, de seguridad y de desempeño clínico de los medicamentos sobre el perfil lipídico a los 3 y 6 meses. Resultados: Se siguieron 501 pacientes en tratamiento con hipolipemiantes. Las estatinas solas disminuyeron el colesterol de baja densidad de 249 mg/ dL (RIQ=226-268) en la medición basal a 190 (177.6-210) y 170 (108-170) en la segunda y tercera medición, respectivamente. Para estatina + ezetimibe, de 167 mg/dL (RIQ=139-184) a 132 (110-150) y 128.5 (101.5-128.5). El fenofibrato disminuyó los triglicéridos de 275 mg/dL (RIQ=21çj-346) a 201 (172-239) y 150.5 (140-150.5). Conclusiones: la administración de estatinas sola o en combinación disminuyó los niveles de LDL y colesterol total, mientras que el fenofibrato demostró su efectividad al disminuir los triglicéridos. No se reportaron efectos adversos. Hubo una adherencia parcial del médico tratante a la guía de práctica clínica para dislipidemias. MÉD.UIS.2019;32(1):13-20.
Abstract Introduction: Drug use studies are important to evaluate the effectiveness and safety of drugs in daily practice, outside the controlled clinical study. Lipid-lowering drugs act on the lipid profile, decreasing the risk of cardiovascular diseases. Objective: To describe the clinical performance and safety of the use of lipid-lowering drugs in real practice in a group of patients diagnosed with dyslipidemia. Methods: An observational, descriptive cohort study. A cohort of patients with hypolipidemic indication for 6 months was followed in 12 cities of Colombia that belong to the biomedical registry of follow-up of patients treated with medicines from the Abbott portfolio. Baseline demographic and clinical variables, safety and efectivity of the drugs were measured on the lipid profile at 3 and 6 months. Results: 501 patients received lipid-lowering agents. Statins alone decreased the low density (LDL) cholesterol of 249 mg / dL (RIQ = 226-268) at baseline to 190 (177.6-210) and 170 (108-170) at the second and third measurements, respectively. For statin + ezetimibe, from 167 mg / dL (RIQ = 139-184) to 132 (110-150) and 128.5 (101.5-128.5). Fenofibrate decreased triglycerides from 275 mg / dL (RIQ = 219-346) to 201 (172-239) and 150.5 (140-150.5). Conclusions: The administration of statins alone or in combination decreased LDL and total cholesterol levels, while fenofibrate demonstrated its effectiveness in lowering triglycerides. No adverse effects were reported. There was partial adherence of the treating physician to GPC for dyslipidemias. There were no adverse events. MÉD.UIS.2019;32(1):13-20.