RESUMEN
ETHNOPHARMACOLOGICAL RELEVANCE: Psidium guajava L. (Myrtaceae) leaves are used as an herbal antidiabetic remedy in several parts of the world. On Madagascar, both the bark and leaves are used for treatment of diabetes. MATERIALS AND METHODS: Dilution series of ethanolic extracts of P. guajava leaves and bark were used for determining inhibitory activities against yeast α-glucosidase and porcine α-amylase. Skeletal muscle glucose uptake was measured using 2-deoxy-D-(1-3H)-glucose in murine C2C12 skeletal muscle cells. Hepatic glucose-6-phosphatase activity in rat hepatoma H4IIE cells and triglyceride accumulation in murine 3T3-L1 adipocyte-like cells were assessed using Wako AutoKit Glucose assays and AdipoRed reagent, respectively. Cells were incubated for 18 h with the maximal non-toxic concentrations of the plant extracts determined by the lactate dehydrogenase cytotoxicity assay. RESULTS: Ethanolic extracts of P. guajava leaf and bark inhibited α-glucosidase with IC50 values of 1.0 ± 0.3 and 0.5 ± 0.01 µg/mL, respectively. In the α-amylase inhibition assay, the ethanolic extract of bark of P. guajava showed an IC50 value of 10.6 ± 0.4 µg/mL. None of the extracts were able to reduce glucose-6-phosphatase activity in rat hepatoma H4IIE cells. In contrast, P. guajava leaf extract significantly increased 2-deoxy-D-[1-3H]-glucose uptake in C2C12 muscle cells (161.4 ± 10.1%, p = 0.0015) in comparison to the dimethyl sulfoxide (DMSO) vehicle control, as did the reference compounds metformin (144.0 ± 7.7%, p = 0.0345) and insulin (141.5 ± 13.8%, p = 0.0495). Furthermore, P. guajava leaf and bark extracts, as well as the reference compound rosiglitazone, significantly enhanced triglyceride accumulation in 3T3-L1 cells (252.6 ± 14.2%, p < 0.0001, 211.1 ± 12.7%, p < 0.0001, and 201.1 ± 9.2%, p < 0.0001, respectively) to levels higher than the DMSO vehicle control. Moreover, P. guajava leaf extract significantly enhanced the triglyceride accumulation in 3T3-L1 cells compared to rosiglitazone. CONCLUSION: The results demonstrated that P. guajava leaf and bark extracts can be used as a natural source of α-glucosidase inhibitors. In addition, the bark extract of P. guajava was an effective α-amylase inhibitor. Moreover, P. guajava leaf extract improved glucose uptake in muscle cells, while both leaf and bark extracts enhanced the triglyceride content in adipocytes in culture. P. guajava leaf and bark extracts may thus hypothetically have future applications in the treatment of type 2 diabetes.
Asunto(s)
Adipocitos/efectos de los fármacos , Glucosa/metabolismo , Inhibidores de Glicósido Hidrolasas/farmacología , Hígado/efectos de los fármacos , Músculo Esquelético/efectos de los fármacos , Psidium , Triglicéridos/metabolismo , alfa-Amilasas/antagonistas & inhibidores , Células 3T3-L1 , Adipocitos/enzimología , Animales , Línea Celular Tumoral , Inhibidores de Glicósido Hidrolasas/aislamiento & purificación , Hígado/enzimología , Ratones , Músculo Esquelético/enzimología , Corteza de la Planta , Hojas de la Planta , Psidium/química , Ratas , alfa-Amilasas/metabolismoRESUMEN
ETHNOPHARMACOLOGICAL RELEVANCE: Berries of Sorbus species have been used to treat type 2 diabetes in many regions in Europe. AIMS OF THE STUDY: To investigate the inhibitory activity of berry extract of Sorbus on the digestive enzymes α-amylase and α-glucosidase, two important targets for management of blood glucose for type 2 diabetics. Furthermore, to test the anti-hyperglycaemic potential of S. norvegica berry extract in vivo. MATERIALS AND METHODS: 70% acetone berry extracts of 16 Sorbus species were tested in vitro for inhibition of α-amylase and α-glucosidase. Single berry extracts were analysed by 1H-NMR spectroscopy and principal component analysis to evaluate the chemical profiles of the extracts. The anti-hyperglycaemic effect was evaluated in an oral starch tolerance test in STZ-treated C57BL/6 mice. RESULTS: The lowest IC50 values against α-amylase and α-glucosidase were obtained with the Sorbus species belonging to the subspecies Aria, which have simple leaves compared to pinnately compound leaves of the other Sorbus species. Species belonging to subspecies Aria grouped together and away from the other Sorbus species in the score plot, indicating a difference in chemistry. Both the carbohydrate- and polyphenol-fraction contributed to the enzyme inhibition. Extract of the most active species, S. norvegica, had anti-hyperglycaemic activity, at a level 36 times lower than clinically used acarbose, corresponding to a needed daily dose of 900â¯mg extract. CONCLUSIONS: Sorbus species of subspecies Aria have the potential to be used for management of type 2 diabetes.
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Diabetes Mellitus Experimental/tratamiento farmacológico , Diabetes Mellitus Tipo 2/tratamiento farmacológico , Hipoglucemiantes/uso terapéutico , Extractos Vegetales/uso terapéutico , Sorbus , Animales , Frutas , Hipoglucemiantes/química , Masculino , Metabolómica , Ratones Endogámicos C57BL , Extractos Vegetales/química , Espectroscopía de Protones por Resonancia Magnética , alfa-Amilasas/antagonistas & inhibidores , alfa-Amilasas/química , alfa-Glucosidasas/químicaRESUMEN
FMRFamide-related proteins have been described in both vertebrate and invertebrate nervous systems and have been suggested to play important roles in a variety of physiological processes. One proposed function is the modulation of signal transduction in mechanosensory neurons and their associated behavioral pathways in the Central American wandering spider Cupiennius salei; however, little is known about the distribution and abundance of FMRFamide-related proteins (FaRPs) within this invertebrate system. We employ immunohistochemistry, Hoechst nuclear stain and confocal microscopy of serial sections to detect, characterize and quantify FMRFamide-like immunoreactive neurons throughout all ganglia of the spider brain and along leg muscle. Within the different ganglia, between 3.4 and 12.6% of neurons showed immunolabeling. Among the immunoreactive cells, weakly and strongly labeled neurons could be distinguished. Between 71.4 and 81.7% of labeled neurons showed weak labeling, with 18.3 to 28.6% displaying strong labeling intensity. Among the weakly labeled neurons were characteristic motor neurons that have previously been shown to express ɣ-aminobutyric acid or glutamate. Ultrastructural investigations of neuromuscular junctions revealed mixed presynaptic vesicle populations including large electron-dense vesicles characteristic of neuropeptides. Double labeling for glutamate and FaRPs indicated that a subpopulation of neurons may co-express both neuroactive compounds. Our findings suggest that FaRPs are expressed throughout all ganglia and that different neurons have different expression levels. We conclude that FaRPs are likely utilized as neuromodulators in roughly 8% of neurons in the spider nervous system and that the main transmitter in a subpopulation of these neurons is likely glutamate.
Asunto(s)
Encéfalo/metabolismo , FMRFamida/metabolismo , Ganglios de Invertebrados/metabolismo , Neuronas/metabolismo , Arañas/metabolismo , Animales , Femenino , Neurotransmisores/metabolismoRESUMEN
Mold and yeast contamination constitutes a major problem in food commodities, including dairy products, hence new natural preventive measures are in high demand. The aim of the current study is to identify and characterize novel antifungal peptides produced by lactic acid bacteria (LAB) in sour cream. By the use of a newly developed image-based 96-well plate fungal growth inhibition assay targeting Debaryomyces hansenii, combined with a range of analytical tools comprising HPLC-high-resolution mass spectrometry, ultrahigh-performance liquid chromatography-Triple Quadrupole MS and nuclear magnetic resonance spectroscopy, we successfully identified a new antifungal peptide (DMPIQAFLLY; 1211 Da) in sour cream enriched with two bioprotective LAB strains. This peptide represents a fragment of casein, the most abundant protein in milk. Presumably, the proteolytic activity of these bioprotective strains results in the observed 4-fold higher concentration of the peptide during storage. Both bioprotective strains are able to generate this peptide in concentrations up to 0.4 µM, independently of the sour cream starter culture employed. The peptide attenuates the growth rate of D. hansenii at concentrations ≥35 µM, and results in smaller cells and more compact colonies. Hence, the peptide is likely contributing to the overall preserving effect of the investigated bioprotective LAB strains.
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Antifúngicos/farmacología , Productos Lácteos Cultivados/microbiología , Debaryomyces/efectos de los fármacos , Lactobacillus/crecimiento & desarrollo , Lactobacillus/metabolismo , Péptidos/farmacología , Antifúngicos/aislamiento & purificación , Cromatografía Líquida de Alta Presión , Espectroscopía de Resonancia Magnética , Espectrometría de Masas , Pruebas de Sensibilidad Microbiana , Péptidos/aislamiento & purificaciónRESUMEN
Acacia ligulata A.Cunn. ex Benth. (Fabaceae: Mimosoideae) is a native Australian plant used traditionally by Australian Aboriginal groups. This study was undertaken to investigate the bioactivity of A. ligulata extracts and to evaluate their chemical composition. Potential antibacterial, cytotoxic and enzyme inhibitory effects relevant to traditional medicinal and food uses of the species were examined and LC-MS/MS was performed to investigate the chemical composition. Antibacterial activity was observed for bark and leaf extracts with an MIC for the bark extract of 62.5 µg/mL against Streptococcus pyogenes. Pod extracts showed cytotoxic effects against cancer cells, with the highest activity against melanoma SK-MEL28 cells with IC50 values between 40.8 and 80.6 µg/mL. Further, the leaf and pod extracts also inhibited α-amylase EC-3.2.1.1 and α-glucosidase EC-3.2.1.20 with IC50 values between 9.7-34.8 and 12.6-64.3 µg/mL, respectively. The LC-MS/MS profiling indicated that several different saponins were present in the active extracts.
Asunto(s)
Acacia/química , Antibacterianos/farmacología , Inhibidores de Glicósido Hidrolasas/farmacología , Plantas Medicinales/química , Espectrometría de Masas en Tándem/métodos , Antibacterianos/química , Australia , Línea Celular Tumoral , Cromatografía Liquida , Evaluación Preclínica de Medicamentos/métodos , Inhibidores de Glicósido Hidrolasas/química , Humanos , Concentración 50 Inhibidora , Pruebas de Sensibilidad Microbiana , Corteza de la Planta/química , Extractos Vegetales/análisis , Extractos Vegetales/química , Hojas de la Planta/efectos de los fármacos , Saponinas/análisis , Streptococcus pyogenes/efectos de los fármacos , alfa-Amilasas/antagonistas & inhibidores , alfa-Glucosidasas/metabolismoRESUMEN
Phyllanthus niruri is used in herbal medicine for treatment of diabetes. The objective of this study was to investigate the antidiabetic potential of P. niruri, using assays for α-glucosidase, muscle glucose transport, liver glucose production and adipogenesis. α-Glucosidase inhibitory activity was performed on aqueous and ethanolic extract of aerial parts of P. niruri. The aqueous and ethanolic extract of P. niruri showed α-glucosidase inhibitory activity with IC50 values of 3.7 ± 1.1 and 6.3 ± 4.8 µg/mL, respectively. HR-bioassay/HPLC-HRMS and NMR analysis was used for identification of compounds. Corilagin (1) and repandusinic acid A (2) were identified as α-glucosidase inhibitors in the water extract of P. niruri with IC50 values of 0.9 ± 0.1 and 1.9 ± 0.02 µM, respectively. In in vitro cell-based bioassays, cells were treated for 18 h with maximal non-toxic concentrations of the ethanolic extract of P. niruri, which were determined by the lactate dehydrogenase cytotoxicity assay. The ethanolic extract of P. niruri was not able to reduce glucose-6-phosphatase activity. However, the extract increased deoxyglucose uptake in C2C12 muscle cells and enhanced adipogenesis in 3T3-L1 fat cells which has been reported for the first time. The present study demonstrated that P. niruri may thus have potential application for treatment and/or management of type 2 diabetes.
Asunto(s)
Adipogénesis/efectos de los fármacos , Glucosa/metabolismo , Hipoglucemiantes/administración & dosificación , Hígado/metabolismo , Músculo Esquelético/metabolismo , Phyllanthus/química , alfa-Glucosidasas/metabolismo , Células 3T3 , Animales , Bioensayo , Relación Dosis-Respuesta a Droga , Estudios de Factibilidad , Hígado/efectos de los fármacos , Ratones , Músculo Esquelético/efectos de los fármacos , Extractos Vegetales/administración & dosificación , Resultado del TratamientoRESUMEN
Protein tyrosine phosphatase 1B (PTP1B) plays a key role as a negative regulator in insulin signal transduction by deactivating the insulin receptor. Thus, PTP1B inhibition has emerged as a potential therapeutic strategy for curing insulin resistance. In this study, 40 extracts from 18 different plant species were investigated for PTP1B inhibitory activity in vitro. The most promising one, the EtOAc extract of Ficus racemosa, was investigated by high-resolution PTP1B inhibition profiling combined with HPLC-HRMS-SPE-NMR analysis. This led to the identification of isoderrone (1), derrone (2), alpinumisoflavone (3) and mucusisoflavone B (4) as PTP1B inhibitors. IC50 of these compounds were 22.7 ± 1.7, 12.6 ± 1.6, 21.2 ± 3.8 and 2.5 ± 0.2 µM, respectively. Kinetics analysis revealed that these compounds inhibited PTP1B non-competitively with Ki values of 21.3 ± 2.8, 7.9 ± 1.9, 14.3 ± 2.0, and 3.0 ± 0.5 µM, respectively. These findings support the important role of F. racemosa as a novel source of new drugs and/or as a herbal remedy for treatment of type 2 diabetes.
Asunto(s)
Cromatografía Líquida de Alta Presión/métodos , Espectroscopía de Resonancia Magnética/métodos , Extractos Vegetales/farmacología , Plantas Medicinales/química , Proteína Tirosina Fosfatasa no Receptora Tipo 1/metabolismo , Diabetes Mellitus Tipo 2/tratamiento farmacológico , Ficus/química , Flavonoides/análisis , Flavonoides/farmacología , Humanos , Isoflavonas/análisis , Isoflavonas/farmacología , Extractos Vegetales/análisis , Proteína Tirosina Fosfatasa no Receptora Tipo 1/antagonistas & inhibidoresRESUMEN
An ethyl acetate extract the bark of Garcinia xanthochymus exhibited strong inhibition towards α-glucosidase and PTP1B with IC50 values of 0.3±0.1µg/mL and 2.3±0.4µg/mL, respectively. Chemical constituents of the extract were therefore examined, and two new compounds, xanthochymusxanthones A (1) and B (2), along with ten known xanthones (3-12), were isolated. Their structures were determined using spectroscopic methods, mainly 1D and 2D NMR. Inhibitory activity of the isolated compounds was then tested, and subelliptenone F (12) showed significant effect towards α-glucosidase with IC50 value of 4.1±0.3µM (compared with acarbose, IC50=900.0±3.0µM) whilst xanthochymusxanthone B (2) exhibited remarkable activity towards PTP1B with IC50 value of 8.0±0.6µM (compared with RK682, IC50=4.4±0.3µM).
Asunto(s)
Garcinia/química , Inhibidores de Glicósido Hidrolasas/química , Inhibidores de Glicósido Hidrolasas/farmacología , Proteína Tirosina Fosfatasa no Receptora Tipo 1/antagonistas & inhibidores , Xantonas/química , Xantonas/farmacología , Diabetes Mellitus/tratamiento farmacológico , Diabetes Mellitus/metabolismo , Inhibidores de Glicósido Hidrolasas/aislamiento & purificación , Humanos , Hipoglucemiantes/química , Hipoglucemiantes/aislamiento & purificación , Hipoglucemiantes/farmacología , Modelos Moleculares , Corteza de la Planta/química , Proteína Tirosina Fosfatasa no Receptora Tipo 1/metabolismo , Xantonas/aislamiento & purificación , alfa-Glucosidasas/metabolismoRESUMEN
Lavender essential oil is traditionally used and approved by the European Medicines Agency (EMA) as herbal medicine to relieve stress and anxiety. Some animal and clinical studies reveal positive results in models of anxiety and depression although very little research has been done on molecular mechanisms. Our work consisted of evaluating the effects of lavender (Lavandula angustifolia) essential oil on central nervous system well-established targets, such as MAO-A, SERT, GABAAand NMDA receptors as well as in vitro models of neurotoxicity. The results showed that lavender essential oil and its main components exert affinity for the glutamate NMDA-receptor in a dose-dependent manner with an IC50 value of 0.04 µl/mL for lavender oil. In addition, lavender and linalool were also able to bind the serotonin transporter (SERT) whereas they did not show affinity for GABAA-benzodiazepine receptor. In three different models of neurotoxicity, lavender did not enhance the neurotoxic insult and improved viability of SH-SY5Y cells treated with hydrogen peroxide. According to our data, the anxiolytic and antidepressant-like effects attributed to lavender may be due to an antagonism on the NMDA-receptor and inhibition of SERT. This study suggests that lavender essential oil may exert pharmacological properties via modulating the NMDA receptor, the SERT as well as neurotoxicity induced by hydrogen peroxide.
RESUMEN
Radix Astragali is a component of several traditional medicines used for the treatment of type 2 diabetes in China. Radix Astragali is known to contain isoflavones, which inhibit α-glucosidase in the small intestines, and thus lowers the blood glucose levels. In this study, 21 samples obtained from different regions of China were extracted with ethyl acetate, then the IC50-values were determined, and the crude extracts were analyzed by 1H-NMR spectroscopy. A principal component analysis of the 1H-NMR spectra labeled with their IC50-values, that is, bioactivity-labeled 1H-NMR spectra, showed a clear correlation between spectral profiles and the α-glucosidase inhibitory activity. The loading plot and LC-HRMS/NMR of microfractions indicated that previously unknown long chain ferulates could be partly responsible for the observed antidiabetic activity of Radix Astragali. Subsequent preparative scale isolation revealed a compound not previously reported, linoleyl ferulate (1), showing α-glucosidase inhibitory activity (IC50 0.5 mM) at a level comparable to the previously studied isoflavones. A closely related analogue, hexadecyl ferulate (2), did not show significant inhibitory activity, and the double bonds in the alcohol part of 1 seem to be important structural features for the α-glucosidase inhibitory activity. This proof of concept study demonstrates that bioactivity-labeling of the 1H-NMR spectral data of crude extracts allows global and nonselective identification of individual constituents contributing to the crude extract's bioactivity.
Asunto(s)
Medicamentos Herbarios Chinos/química , Medicamentos Herbarios Chinos/farmacología , Inhibidores de Glicósido Hidrolasas/química , Metabolómica , Análisis de Componente Principal , Espectroscopía de Protones por Resonancia Magnética , Astragalus propinquus , Cromatografía Líquida de Alta Presión , Activación Enzimática/efectos de los fármacos , Inhibidores de Glicósido Hidrolasas/farmacología , Concentración 50 Inhibidora , Metabolómica/métodos , alfa-Glucosidasas/químicaRESUMEN
A hyphenated procedure involving high-performance liquid chromatography, photodiode array detection, high-resolution mass spectrometry, solid-phase extraction, and nuclear magnetic resonance spectroscopy, i.e., HPLC-PDA-HRMS-SPE-NMR, has proven an effective technique for the identification of compounds in complex matrices. Most HPLC-PDA-HRMS-SPE-NMR investigations reported so far have relied on analytical-scale reversed-phase C18 columns for separation. Herein is reported the use of an analytical-scale pentafluorophenyl column as an orthogonal separation method following fractionation of a crude ethyl acetate extract of leaves of Coleonema album on a preparative-scale C18 column. This setup allowed the HPLC-PDA-HRMS-SPE-NMR analysis of 23 coumarins, including six new compounds, 8-O-ß-d-glucopyranosyloxy-6-(2,3-dihydroxy-3-methylbut-1-yl)-7-methoxycoumarin (4), (Z)-6-(4-ß-d-glucopyranosyloxy-3-methylbut-2-en-1-yl)-7-hydroxycoumarin (6), 6-(4-ß-d-glucopyranosyloxy-3-methylbut-1-yl)-7-hydroxycoumarin (8), (Z)-7-(4-ß-d-glucopyranosyloxy-3-methylbut-2-en-1-yloxy)coumarin (13), (S)-8-(3-chloro-2-hydroxy-3-methylbut-1-yloxy)-7-methoxycoumarin (19), and 7-(3-chloro-2-hydroxy-3-methylbut-1-yloxy)coumarin (20). The use of the pentafluorophenyl column even allowed separation of several regioisomers that are usually difficult to separate using reversed-phase C18 columns. The phytochemical investigation described for C. album in this report demonstrates the potential and wide applicability of HPLC-PDA-HRMS-SPE-NMR for accelerated structural identification of natural products in complex mixtures.
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Cumarinas/análisis , Umbeliferonas/análisis , Cromatografía Líquida de Alta Presión/métodos , Cumarinas/química , Espectroscopía de Resonancia Magnética/métodos , Estructura Molecular , Resonancia Magnética Nuclear Biomolecular , Extractos Vegetales/química , Rutaceae/química , Extracción en Fase Sólida , Sudáfrica , Umbeliferonas/química , Umbeliferonas/aislamiento & purificaciónRESUMEN
The present study was carried out to investigate the wound healing potentials of 17 medicinal plants historically used in Ghana for wound healing. Warm and cold water extracts were prepared from the 17 dried plant species and tested in vitro in the scratch assay with NIH 3T3 fibroblasts from mice. The wound healing scratch assay was used to evaluate the effect of the plants on cell proliferation and/or migration in vitro, as a test for potential wound healing properties. After 21 hours of incubation increased proliferation and/or migration of fibroblasts in the scratch assay was obtained for 5 out of the 17 plant species. HPLC separation of the most active plant extract, which was a warm water extract of Philenoptera cyanescens, revealed the wound healing activity to be attributed to rutin and a triglycoside of quercetin. The present study suggests that Allophylus spicatus, Philenoptera cyanescens, Melanthera scandens, Ocimum gratissimum, and Jasminum dichotomum have wound healing activity in vitro.
RESUMEN
Three new xanthones, oblongixanthone F-H (1-3), along with eight known xanthones (4-11), were isolated from an EtOAc extract of the twigs of Garcinia oblongifolia. Their structures were elucidated by spectroscopic analysis including 1D- and 2D-NMR spectroscopy and mass spectrometry. The antidiabetic effects of all isolated compounds were evaluated by in vitro α-glucosidase and PTP1B inhibition assays. Compound 11 was the most active compound, and inhibited α-glucosidase and PTP1B with IC50 values of 1.7±0.5 and 14.1±3.5µM, respectively.
Asunto(s)
Garcinia/química , Hipoglucemiantes/química , Xantonas/química , Inhibidores de Glicósido Hidrolasas/química , Inhibidores de Glicósido Hidrolasas/aislamiento & purificación , Humanos , Hipoglucemiantes/aislamiento & purificación , Estructura Molecular , Proteína Tirosina Fosfatasa no Receptora Tipo 1/antagonistas & inhibidores , Xantonas/aislamiento & purificación , alfa-Glucosidasas/metabolismoRESUMEN
ETHNOPHARMACOLOGICAL RELEVANCE: Type 2 diabetes is the most common type of diabetes and its prevalence is rapidly increasing throughout the world. Modifications of lifestyle such as suitable diet and exercise programs along with pharmacotherapy and education of patients are beneficial therapies for patients with type 2 diabetes. The ethnopharmacological use of herbal medicines, many of them part of our diet as spices, vegetables and fruits, has been developed for the treatment of diabetes due to inexpensiveness, easy availability and few side effects. AIM OF THE STUDY: Our aim is to present a review for researchers who are interested in the biologically active dietary plants traditionally utilized in the treatment of diabetes. MATERIALS AND METHODS: Information was obtained from a literature search of electronic databases such as Google Scholar, Pubmed, Sci Finder and Cochrane. Common and scientific name of the fruits, vegetables, beverages, oils and spices and the words 'antidiabetic', 'hypoglycemic', 'anti-hyperglycemic', 'type 2 diabetes' were used as keywords for search. RESULTS: Certain fruits and vegetables are functional foods and their consumption reduces the incidence of type 2 diabetes. Hypoglycemic effects of fruits and vegetables may be due to their inducing nature on pancreatic ß-cells for insulin secretion, or bioactive compounds such as flavonoids, alkaloids and anthocyanins, which act as insulin-like molecules or insulin secretagogues. CONCLUSION: This write-up covers hypoglycemic, anti-hyperglycemic and anti-diabetic activities of some dietary fruits, vegetables, beverages, oils and spices and their active hypoglycemic constituents. Including such plant species in the diet might improve management of type 2 diabetes.
Asunto(s)
Diabetes Mellitus Tipo 2/dietoterapia , Alimentos Funcionales , Hipoglucemiantes , Animales , Bebidas , Dieta , Frutas , Humanos , Aceites de Plantas , Especias , VerdurasRESUMEN
ETHNOPHARMACOLOGICAL RELEVANCE: Plants used in the traditional medicine of Europe to treat memory dysfunction and/or to enhance memory were investigated for activity against the underlying mechanisms of Alzheimer's disease. AIM OF THE STUDY: To investigate 35 ethanolic extracts of plants, selected using an ethnopharmacological approach, for anti-amyloidogenic activity as well as an ability to inhibit the enzymatic activity of acetylcholinesterase. MATERIALS AND METHODS: The anti-amyloidogenic activity of the extracts against amyloid beta was investigated by Thioflavin T fibrillation assays and the ability to inhibit the enzymatic activity of acetylcholinesterase was evaluated monitoring the hydrolysis of acetylthiocholine RESULTS: Under the experimental conditions investigated, extracts of two plants, Carum carvi and Olea sylvestris, inhibited amyloid beta fibrillation considerably, eight plant extracts inhibited amyloid beta fibrillation to some extent, 16 plant extracts had no effect on amyloid beta fibrillation and nine extracts accelerated fibrillation of amyloid beta. Furthermore, five plant extracts from Corydalis species inhibited the enzymatic activity of acetylcholinesterase considerably, one plant extract inhibited the enzymatic activity of acetylcholinesterase to some extent and 29 plant extract had no effect on the enzymatic activity of acetylcholinesterase. CONCLUSIONS: An optimal extract in this study would possess acetylcholinesterase inhibitory activity as well as anti-amyloidogenic activity in order to address multiple facets of Alzheimer's disease, until the molecular origin of the disease is unraveled. Unfortunately no such extract was found.
Asunto(s)
Acetilcolinesterasa/metabolismo , Péptidos beta-Amiloides/antagonistas & inhibidores , Inhibidores de la Colinesterasa/farmacología , Medicina Tradicional , Trastornos de la Memoria , Extractos Vegetales/farmacología , Péptidos beta-Amiloides/metabolismo , Inhibidores de la Colinesterasa/aislamiento & purificación , Inhibidores de la Colinesterasa/uso terapéutico , Europa (Continente) , Humanos , Medicina Tradicional/métodos , Trastornos de la Memoria/tratamiento farmacológico , Trastornos de la Memoria/enzimología , Extractos Vegetales/aislamiento & purificación , Extractos Vegetales/uso terapéutico , Plantas MedicinalesRESUMEN
ETHNOPHARMACOLOGICAL RELEVANCE: Studies show that ethnic minorities continue to use their cultural traditional medicines also after migration to the West. Research in this field is necessary, given that little is known about traditional medicines' impact on health-related problems. This study sheds light on the issue through a qualitative study among ethnic Pakistanis residing in Denmark. AIM OF THE STUDY: The study addresses perception, knowledge and attitudes regarding the use of medicinal plants among Pakistanis living in Copenhagen. We furthermore document and identify the medicinal plants used in households. MATERIALS AND METHODS: Data were collected through in-depth, semi-structured interviews with sixteen ethnic Pakistanis aged 30-80 years. Interviews were transcribed verbatim and analysed through Emerson's two-phased analysis method. Medicinal plant products in the interviewees' households were collected, photographed, identified and deposited at Museum of Natural Medicine at University of Copenhagen. RESULTS: A total number of 121 Pakistani traditional medicines were identified, and found to represent both medicinal plants and foods. The average number of quoted Pakistani Traditional Medicines was 18 (N=16). Interviewees independently reported the same traditions for preparation and consumption of Pakistani traditional medicines. Factors that play a role in choosing to use Pakistani traditional medicines are frequent visits to Pakistan, belief in the healing power of totkas (homemade medicinal preparation), religious knowledge and the occurrence of recent illness within the family. Further, the upkeep of traditional use depends on the availability of Pakistani traditional medicines. CONCLUSION: The study enhanced understanding of ethnic Pakistanis' perception and continued use of traditional medicines within the household after migration to the West. In the context of Western biomedicine, little is known of the potential toxicity and side-effects of many of the Pakistani traditional medicines found to be used in households in Copenhagen.
Asunto(s)
Conocimientos, Actitudes y Práctica en Salud/etnología , Medicina Tradicional , Fitoterapia , Adulto , Anciano , Anciano de 80 o más Años , Pueblo Asiatico/etnología , Ciudades , Dinamarca , Femenino , Conductas Relacionadas con la Salud , Humanos , Masculino , Medicina Tradicional/estadística & datos numéricos , Persona de Mediana Edad , Pakistán/etnología , Fitoterapia/estadística & datos numéricosRESUMEN
Ascariasis affects more than 1 billion people worldwide, mainly in developing countries, causing substantial morbidity. Current treatments for Ascaris infection are based on mass drug administration (MDA) with synthetic anthelmintic drugs such as albendazole, however continual re-infection and the threat of drug resistance mean that complementary treatment options would be highly valuable. Here, we screened ethanolic extracts from 29 medicinal plants used in Africa (Ghana) and the Caribbean (US Virgin Islands) for in vitro anthelmintic properties against Ascaris suum, a swine parasite that is very closely related to the human A. lumbricoides. A wide variety of activities were seen in the extracts, from negligible to potent. Extracts from Clausena anisata, Zanthoxylum zanthoxyloides and Punica granatum were identified as the most potent with EC50 values of 74, 97 and 164 µg/mL, respectively. Our results encourage further investigation of their use as complementary treatment options for ascariasis, alongside MDA.
Asunto(s)
Antihelmínticos/farmacología , Ascaris suum/efectos de los fármacos , Medicinas Tradicionales Africanas/métodos , Extractos Vegetales/farmacología , Plantas Medicinales/química , Animales , Antihelmínticos/uso terapéutico , Ascariasis/tratamiento farmacológico , Ghana , Intestinos/parasitología , Extractos Vegetales/uso terapéutico , Porcinos , Islas Virgenes de los Estados UnidosRESUMEN
The presence of Lewy bodies and Lewy neurites is a major pathological hallmark of Parkinson's disease and is hypothesized to be linked to disease development, although this is not yet conclusive. Lewy bodies and Lewy neurites primarily consist of fibrillated α-Synuclein; yet, there is no treatment available targeting stabilization of α-Synuclein in its native state. The aim of the present study was to investigate the inhibitory activity of an ethanolic extract of Geum urbanum against α-Synuclein fibrillation and examine the structural changes of α-Synuclein in the presence of the extract. The anti-fibrillation and anti-aggregation activities of the plant extract were monitored by thioflavin T fibrillation assays and size exclusion chromatography, while structural changes were followed by circular dichroism, Fourier transform infrared spectroscopy, intrinsic fluorescence, small angle X-ray scattering and electron microscopy. Since the extract is a complex mixture, structure-function relationships could not be determined. Under the experimental conditions investigated, Geum urbanum was found to inhibit α-Synuclein fibrillation in a concentration dependent way, and to partly disintegrate preformed α-Synuclein fibrils. Based on the structural changes of α-Synuclein in the presence of extract, we propose that Geum urbanum delays α-Synuclein fibrillation either by reducing the fibrillation ability of one or more of the aggregation prone intermediates or by directing α-Synuclein aggregation towards a non-fibrillar state. However, whether these alterations of the fibrillation pathway lead to less pathogenic species is yet to be determined.
Asunto(s)
Amiloide/química , Geum/química , Extractos Vegetales/química , Agregado de Proteínas , alfa-Sinucleína/química , Amiloide/antagonistas & inhibidores , Benzotiazoles , Humanos , Soluciones , Espectrometría de Fluorescencia , Espectroscopía Infrarroja por Transformada de Fourier , Tiazoles , alfa-Sinucleína/antagonistas & inhibidoresRESUMEN
ETHNOPHARMACOLOGICAL RELEVANCE: The 18 plant species investigated in this study have been used as herbal antidiabetic remedies in Vietnamese traditional medicines. This study aimed to evaluate their ability to inhibit α-glucosidase and α-amylase, two key enzymes involved in serum glucose regulation. MATERIALS AND METHODS: Chloroform, ethanol and water extracts of 18 plants were screened for α-glucosidase and α-amylase inhibitory activity. Analytical-scale HPLC was subsequently used to investigate the most active extracts, where samples with low level of tannins were identified and fractionated into 96-well microplates, followed by α-glucosidase and α-amylase assessment of each well. High-resolution α-glucosidase and α-amylase inhibition profiles constructed from these assays allowed identification of HPLC peaks correlated with α-glucosidase and α-amylase inhibitory activity. The active constituents were subsequently isolated using preparative-scale HPLC and their structure was elucidated by HR-ESIMS and NMR. RESULTS: Ethanol extracts of Nepenthes mirabilis, Phyllanthus urinaria, and Kandelia candel significantly inhibited α-glucosidase with IC50 values of 32.7±6.3, 39.7±9.7, and 35.4±13.9µg/mL, respectively. Water extracts of N. mirabilis, Phyllanthus amarus, P. urinaria, Lagerstroemia speciosa, Syzygium cumini, Rhizophora mucronata, and K. candel showed IC50 values of 3.3±0.8, 34.9±1.5, 14.6±4.6, 5.4±0.5, 20.9±1.8, 3.3±0.6, and 4.0±0.8µg/mL, respectively. In the α-amylase inhibition assay, ethanol extracts of K. candel and Ficus racemosa showed IC50 of 7.6±0.9 and 46.7±23.6µg/mL, respectively. Showing low tannin constituents as seen from HPLC profiles, P. amarus and P. urinaria water extracts and F. racemosa ethanol extract were subjected to microfractionation. Only high-resolution α-glucosidase inhibition profiles of P. amarus and P. urinaria water extracts showed several active compounds, which were isolated and identified as corilagin (1), repandusinic acid A (2), and mallotinin (3). IC50 of these compounds were 1.70±0.03, 6.10±0.10, and 3.76±0.15µM, respectively. Kinetics analysis revealed that 1 displayed a mixed type mode of inhibition with Ki and Ki' values of 2.37±0.90 and 2.61±0.61µM, respectively, whereas 2 and 3 competitively inhibited α-glucosidase with Ki values of 4.01±0.47 and 0.65±0.11µM, respectively. CONCLUSION: Corilagin (1), repandusinic acid A (2), and mallotinin (3) were potent α-glucosidase inhibitors contributing significantly to the inhibitory effect observed for the water extracts of P. amarus and P. urinaria.
Asunto(s)
Diabetes Mellitus Tipo 2/tratamiento farmacológico , Inhibidores de Glicósido Hidrolasas/farmacología , Extractos Vegetales/uso terapéutico , Plantas Medicinales/química , alfa-Amilasas/antagonistas & inhibidores , alfa-Glucosidasas/metabolismo , Benzopiranos/química , Benzopiranos/farmacología , Glucosa/análogos & derivados , Glucosa/química , Glucosa/farmacología , Glucósidos/química , Glucósidos/farmacología , Humanos , Taninos Hidrolizables/química , Taninos Hidrolizables/farmacología , Hipoglucemiantes/química , Hipoglucemiantes/farmacología , Medicina Tradicional , Estructura Molecular , Extractos Vegetales/administración & dosificación , VietnamRESUMEN
Crude chloroform, ethanol and acetone extracts of nineteen seaweed species were screened for their antioxidant and α-glucosidase inhibitory activity. Samples showing more than 60% α-glucosidase inhibitory activity, at a concentration of 1 mg/ml, were furthermore investigated using high-resolution α-glucosidase inhibition profiling combined with high-performance liquid chromatography-high-resolution mass spectrometry-solid-phase extraction-nuclear magnetic resonance spectroscopy (HR-bioassay/HPLC-HRMS-SPE-NMR). The results showed Ascophyllum nodosum and Fucus vesicolosus to be rich in antioxidants, equaling a Trolox equivalent antioxidant capacity of 135 and 108 mM Troloxmg(-1) extract, respectively. HR-bioassay/HPLC-HRMS-SPE-NMR showed the α-glucosidase inhibitory activity of A. nodosum, F. vesoculosus, Laminaria digitata, Laminaria japonica and Undaria pinnatifida to be caused by phlorotannins as well as fatty acids - with oleic acid, linoleic acid and eicosapentaenoic acid being the most potent with IC50 values of 0.069, 0.075 and 0.10 mM, respectively, and showing a mixed-type inhibition mode.