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1.
Bol. latinoam. Caribe plantas med. aromát ; 20(3): 226-243, may. 2021. ilus, tab
Article in English | LILACS | ID: biblio-1342815

ABSTRACT

Several species of the Myrcia genus have been used in folk medicine to treat diabetes. Therefore, the aim of this work was to investigate the inhibitory activity of α-glucosidase and pancreatic lipase in the crude extract (EBF) and in the ethyl acetate fraction (FFA) of Myrcia hatschbachii, as well as to identify isolated phenolic compounds and to evaluate the antioxidant property and preliminary in vitro toxicity against Artemia salina. EBF (IC50: 3.21 µg/mL) and FFA (IC50: 1.14 µg/mL) showed inhibitory activity superior to acarbose (IC50: 193.65 µg/mL). In addition, they showed inhibitory effects of pancreatic lipase (IC50: 556.58 µg/mL for EBF and 532.68 µg/mL for FFA), antioxidant potential, absence of preliminary toxicity and presence of gallic andellagic acids in FFA. The relevant results in the inhibition of α-glucosidase and pancreatic lipase motivate new studies for the development of herbal medicines that assist in the treatment of diabetic patients.


Varias especies del género Myrcia se han utilizado en la medicina popular para tratar la diabetes. Por lo tanto, el objetivo de este trabajo fue investigar la actividad inhibitoria de la α-glucosidasa y la lipasa pancreática en el extracto crudo (EBF) y en la fracción de acetato de etilo (FFA) de Myrcia hatschbachii, así como identificar compuestos fenólicos aislados y evaluar la propiedad antioxidante y toxicidad in vitro preliminar contra Artemia salina. EBF (IC50: 3.21 µg/mL) y FFA (IC50: 1.14 µg/mL) mostraron una actividad inhibitoria superior a la acarbosa (IC50: 193.65 µg/mL). Además, mostraron efectos inhibitorios de la lipasa pancreática (IC50: 556.58 µg/mL para EBF y 532.68 µg/mL para FFA), potencial antioxidante, ausencia de toxicidad preliminar y presencia de ácidos gálico y elágico en FFA. Los resultados relevantes en la inhibición de la α-glucosidasa y la lipasa pancreática motivan nuevos estudios para el desarrollo de medicamentos a base de hierbas que ayudan en el tratamiento de pacientes diabéticos.


Subject(s)
Plant Extracts/pharmacology , Myrtaceae/chemistry , Glycoside Hydrolase Inhibitors/pharmacology , Lipase/drug effects , Antioxidants/pharmacology , Pancreas/enzymology , Phenols/analysis , X-Ray Diffraction , In Vitro Techniques , Plant Extracts/toxicity , Plant Extracts/chemistry , Free Radical Scavengers , Complex Mixtures , Ellagic Acid , Gallic Acid , Antioxidants/chemistry
2.
Rev. Hosp. Ital. B. Aires (2004) ; 40(3): 105-116, sept. 2020. ilus, tab
Article in Spanish | LILACS | ID: biblio-1129064

ABSTRACT

Este trabajo tiene como objetivo revisar las contribuciones de la biotecnología, en relación con el tratamiento, diagnóstico y la monitorización de la enfermedad renal crónica (ERC) y sus comorbilidades más frecuentes, especialmente la anemia. En relación con los tratamientos, enfocamos el desarrollo de productos biofarmacéuticos como los agentes estimulantes de la eritropoyesis (ESA), que fueron los primeros biofármacos utilizados para el tratamiento de la anemia asociada a la ERC; analizamos sus características y utilización actual después de varios años de experiencia clínica, así como también otras alternativas en desarrollo. Revisamos distintos tipos de bioterapias, la utilización de las células estromales mesenquimales de médula ósea (MSC) y tratamientos alternativos con modificaciones dietarias, que se basan en la asociación entre la microbiota intestinal de los pacientes renales crónicos y sus condiciones fisiopatológicas. Finalmente, en relación con el diagnóstico y monitorización, nos referimos al estudio y validación de biomarcadores diagnósticos, predictivos y terapéuticos que han permitido optimizar los resultados clínicos en este tipo de pacientes. (AU)


The aim of this work is to review the contributions of biotechnology, in relation to the treatment, diagnosis and monitoring of chronic kidney disease (CKD) and its most frequent comorbidities, especially anemia. Regarding the treatment, we focus on the development of biopharmaceutical products such as erythropoiesis stimulating agents (ESA), which were the first biopharmaceuticals used to treat anemia associated with chronic kidney disease (CKD). We analyzed their characteristics and their current use after several years of clinical experience, as well as other alternatives in development. We also review different types of biotherapies, the use of bone marrow mesenchymal stromal cells (MSC) and alternative treatments with dietary modifications, which are based on the association between the intestinal microbiota of chronic kidney patients and their pathophysiological conditions. Finally, in relation to diagnosis and monitoring, we refer to the study and validation of diagnostic, predictive and therapeutic biomarkers that have made clinical results possible to be optimized in this type of patient. (AU)


Subject(s)
Humans , Biological Therapy/trends , Renal Insufficiency, Chronic/therapy , Quality of Life , Biotechnology , Biomarkers , Erythropoietin/deficiency , Probiotics/therapeutic use , Mesenchymal Stem Cell Transplantation/trends , Erythropoiesis/drug effects , Renal Insufficiency, Chronic/diagnosis , Renal Insufficiency, Chronic/diet therapy , Renal Insufficiency, Chronic/rehabilitation , Prebiotics/classification , Glycoside Hydrolase Inhibitors/therapeutic use , Gastrointestinal Microbiome , Hematinics/administration & dosage , Hematinics/pharmacology , Hematinics/pharmacokinetics , Anemia/diagnosis , Anemia/etiology , Anemia/drug therapy
3.
Acta amaz ; 49(1): 48-53, jan. - mar. 2019.
Article in English | LILACS | ID: biblio-1119223

ABSTRACT

Virola venosa, popularly known in Brazil as ucuuba-da-mata, occurs naturally in the Amazon region and has potential to provide useful natural compounds, as already known for other Virola species. Therefore, the objective of this study was to determine the chemical composition of bark and leaf extracts of V. venosa, and to test the antioxidant capacity and α-glucosidase inhibition potential of their compounds. Polar extracts showed to be more active in both assays, therefore a bioactivity-guided fractionation was performed to identify the compounds that were responsible for the recorded activities. Using a combination of LC-MS/MS analysis and isolation with NMR identification, eight phenolic compounds were identified. Assays with pure compounds of the active fraction revealed that ferulic acid was the main contributor compound to the observed bioactivity in the crude extracts. (AU)


Subject(s)
Amazonian Ecosystem , Phenolic Compounds , Glycoside Hydrolase Inhibitors , Antioxidants
4.
Braz. J. Pharm. Sci. (Online) ; 55: e17032, 2019. tab, graf
Article in English | LILACS | ID: biblio-1019533

ABSTRACT

The aim of the present research work was to investigate the enzyme inhibitory potential of some new sulfonamides having benzodioxane and acetamide moieties. The synthesis was started by the reaction of N-2,3-dihydrobenzo[1,4]-dioxin-6-amine (1) with 4-methylbenzenesulfonyl chloride (2) in the presence of 10% aqueous Na2CO3 to yield N-(2,3-dihydrobenzo[1,4]-dioxin-6-yl)-4-methylbenzenesulfonamide (3), which was then reacted with 2-bromo-N-(un/substituted-phenyl)acetamides (6a-l) in DMF and lithium hydride as a base to afford various 2-{2,3-dihydro-1,4-benzodioxin-6-yl[(4-methylphenyl)sulfonyl]amino}-N-(un/substituted-phenyl)acetamides (7a-l). All the synthesized compounds were characterized by their IR and 1H-NMR spectral data along with CHN analysis data. The enzyme inhibitory activities of these compounds were tested against a-glucosidase and acetylcholinesterase (AChE). Most of the compounds exhibited substantial inhibitory activity against yeast a-glucosidase and weak against AChE. The in silico molecular docking results were also consistent with in vitro enzyme inhibition data.


Subject(s)
Sulfonamides/agonists , Cholinesterase Inhibitors , Glycoside Hydrolase Inhibitors , Spectrum Analysis/instrumentation , Acetamides/analysis
5.
Article in Chinese | WPRIM | ID: wpr-777474

ABSTRACT

Chemical constituents were isolated from the fruiting bodies of Ganoderma australe by various column chromatographic techniques and HPLC method, and their chemical structures were identified through the combined analysis of physicochemical properties and spectral data. Meanwhile, their α-glucosidase inhibitory activity and anti-oxidative ability were evaluated. Seven compounds were isolated from G. australe and were identified as 6-methoxyl-cyclo-(Phe-Ile)(1), applanoxidic acid A methyl ester(2), ergosta-7,22 E-dien-3β-ol(3), cinnamic acid(4), 5α,8α-epidioxy-(20S,22E,24R)-ergosta-6,22-diene-3β-ol(5), 1-(3, 4-dihydroxyphenyl) ethanone(6), salicylic acid(7) and benzoic acid(8). Among the compounds, compound 1 was a new cyclic dipeptide. Compound 2 was a new lanosta natural product, and compounds 4, 6, 7 and 8 were obtained from G. australe for the first time. Moreover, compounds 4 and 8 exhibited α-glucosidase inhibitory activity with inhibition rates of 36.8% and 34.7%, and compounds 4, 7 and 8 had a certain activity in DPPH free radical scavenging activity with IC_(50) values of 0.168, 0.458 and 0.170 g·L~(-1), respectively. The DPPH radical scavenging rate of compound 1 was 41.1%.


Subject(s)
Free Radical Scavengers , Fruiting Bodies, Fungal , Chemistry , Ganoderma , Chemistry , Glycoside Hydrolase Inhibitors , Molecular Structure
6.
Article in English | WPRIM | ID: wpr-776882

ABSTRACT

Four new octadecanoid derivatives (1-4) including a pair of enantiomers (1/2), along with 12 known analogues (5-16), were isolatedfrom the seeds of Ipomoea nil. Their structures were determined by detailed spectroscopic analyses and comparison with reported data of structurally related compounds, with the absolute configurations of 1 and 2 being assigned by an in situ dimolybdenum ECD method. Our bioassays revealed that these isolates did not show ABTS radical scavenging activity while 10 and 13 displayed better α-glucosidase inhibitory activity than the positive control acarbose (IC 167.7 ± 1.55 μmol·L), with IC of 92.73 ± 3.12 and 11.39 ± 2.18μmol·L, respectively.


Subject(s)
Fatty Acids , Chemistry , Metabolism , Glycoside Hydrolase Inhibitors , Chemistry , Metabolism , Inhibitory Concentration 50 , Ipomoea nil , Chemistry , Molecular Structure , Plant Extracts , Chemistry , Metabolism , Seeds , Chemistry
7.
Article in English | WPRIM | ID: wpr-776866

ABSTRACT

The aim of the study was to determine the feasibility of the Vitellaria paradoxa nutshell as a new medicinal resource for treating diabetes. A total of forty-one compounds were identified by HPLC-DAD-Q-TOF-MS and phytochemical methods in V. paradoxa nutshell methanol extract. Based on HPLC fingerprints, four characteristic constituents were quantified and the origin of twenty-eight V. paradoxa nutshells from seven sub-Saharan countries was compared, which were classified into three groups with chemometric method. Twenty-eight samples contained high total phenolic content, and exhibited moderate-higher antioxidant activity and strong α-glucosidase inhibitory activity. Furthermore, all fractions and isolated compounds were evaluated for their antioxidant and α-glucosidase inhibitory activities, and α-glucosidase inhibitory action mechanism of four characteristic constituents including protocatechuic acid, 3, 5, 7-trihydroxycoumarin, (2R, 3R)-(+)-taxifolin and quercetin was investigated via molecular docking method, which were all stabilized by hydrogen bonds with α-glucosidase. The study provided an effective approach to waste utilization of V. paradoxa nutshell, which would help to resolve waste environmental pollution and provide a basis for developing potential herbal resource for treating diabetes.


Subject(s)
Africa South of the Sahara , Chromatography, High Pressure Liquid , Diabetes Mellitus , Drug Therapy , Glycoside Hydrolase Inhibitors , Chemistry , Pharmacology , Humans , Hypoglycemic Agents , Chemistry , Pharmacology , Molecular Docking Simulation , Plant Extracts , Chemistry , Pharmacology , Plants, Medicinal , Chemistry , Sapotaceae , Chemistry , alpha-Glucosidases , Metabolism
8.
Article in Chinese | WPRIM | ID: wpr-771512

ABSTRACT

Six compounds were isolated from the aerial part of cultivated Clerodendranthus spicatus in Hainan with various chromatographic techniques,and their structures were determined as:1-dehydroxy-1-oxo-rupestrinol(1),N-trans-feruloyltyramine(2),methyl 3,4-dihydroxyphenyllactate(3),caffein acid(4),methyl caffeate(5) and ethyl caffeate(6),via analysis of physicochemical properties and spectroscopic evidence.Compound 1 was a new compound,while compounds 2 and 3 were isolated from C.spicatus for the first time.Biological activity results showed that compounds 2-4 exhibited α-glucosidase inhibitory activity with different inhibition ratio.


Subject(s)
China , Glycoside Hydrolase Inhibitors , Pharmacology , Lamiaceae , Chemistry , Molecular Structure , Phytochemicals , Pharmacology , Sesquiterpenes, Eudesmane , Pharmacology
9.
Rev. Soc. Odontol. La Plata ; 28(55): 41-45, mayo 2018.
Article in Spanish | LILACS | ID: biblio-912038

ABSTRACT

Los inhibidores selectivos de la α-amilasa salival y pancreática humana, son un medio eficaz para controlar los niveles de azúcar en la saliva y la sangre, durante el control de la caries y la diabetes. En la presente revisión, después de identificar las principales funciones de la enzima, se discutieron exponen algunas de las respuestas observadas después de la exposición de la α-amilasa a las plantas, en escala molecular y entera. Diferentes tipos de moléculas de plantas medicinales actúan como inhibidores de la α-amilasa, como una terapia alternativa o complementaria en el tratamiento de la diabetes en y en el control de uno de los factores de la formación la caries (dieta) (AU)


Selective inhibitors of human salivary and pancreatic α-amylase are an effective means of controlling saliva and blood sugar levels in the management of caries and diabetes. In the present review, after identifying the main functions of the enzyme, it was exposed some of the observed responses after exposure to α-amylase at the molecular and whole plants scale. Different types of medicinal plants molecules have been found to act as α-amylase inhibitors, as an alternative or complementary therapy in the management of diabetes and control to one of the predisposing factors to caries (diet) (AU)


Subject(s)
Humans , alpha-Amylases , Dental Caries , Diabetes Mellitus , Enzyme Inhibitors , Plants, Medicinal , Complementary Therapies , Glycoside Hydrolase Inhibitors
10.
Article in Chinese | WPRIM | ID: wpr-771675

ABSTRACT

The present study compared active ingredients of tea from different sources to select tea type and the fraction of tea extracts for the highest anti-hyperglycemic activity, and to verify anti-hyperglycemic activity of the selected tea extract. Tea extracts were separated and enriched by molecular weight using ultra-filtration technology. The extracts were first screened by -glucosidase inhibition assay, followed by using a rat inverted intestine sac system to measure the effect on glucose transport. Both alloxan-induced diabetic rat model and high-fat diet combined with streptozotocin-induced rat diabetes mellitus model were used to study the effects of active components on blood glucose, body weight, insulin resistance. The experimental results showed that the different kinds of tea extracts had different inhibitory effects on -glucosidase, and the inhibitory effect of tea extract E on -glucosidase was stronger. The effects of different components of tea extract E also varied greatly, of which Fraction AN protein had stronger inhibitory effect on -glucosidase than other fragments, and Fraction AN protein had a strong inhibitory effect on glucose transport, reduced blood sugar and normalized insulin secretion in diabetic rats. The results suggest that a glycol-protein fraction(AN) from the extracts might be responsible for the anti-hyperglycemic activity of tea polysaccharides. The AN glycol-protein fraction has strong inhibitory effects on both -glucosidase activity and glucose transport by the small intestine. It also reduced blood glucose level and normalized insulin secretion in diabetic rats, and has a protective effect on diabetic rats.


Subject(s)
Animals , Blood Glucose , Diabetes Mellitus, Experimental , Drug Therapy , Glycols , Pharmacology , Glycoside Hydrolase Inhibitors , Hypoglycemic Agents , Pharmacology , Plant Extracts , Chemistry , Rats , Tea , Chemistry , alpha-Glucosidases
11.
Journal of Integrative Medicine ; (12): 192-198, 2018.
Article in English | WPRIM | ID: wpr-691071

ABSTRACT

<p><b>OBJECTIVE</b>The current study was designed to evaluate the various antioxidant potentials and inhibitory effects of phenolic-rich leaf extracts of Bridelia ferruginea (BF) on the in vitro activities of some key enzymes involved in the metabolism of carbohydrates.</p><p><b>METHODS</b>In this study, BF leaf free and bound phenolic-rich extracts were used. We quantified total phenolic and flavonoid contents, and evaluated several antioxidant activities using assays for ferric reducing antioxidant power, total antioxidant activity (phosphomolybdenum reducing ability), 1,1-diphenyl-2-picrylhydrazyl and thiobarbituric acid reactive species. Also, extracts were tested for their ability to inhibit α-amylase and α-glucosidase activity.</p><p><b>RESULTS</b>The total phenolic and total flavonoid contents in the free phenolic extract of BF were significantly greater than in the bound phenolic extract. Also, all the antioxidant activities considered were significantly greater in the free phenolic extract than in the bound phenolic extract. In the same vein, the free phenolic-rich extract had a significantly higher percentage inhibition against α-glucosidase activity (IC = 28.5 µg/mL) than the bound phenolic extract (IC = 340.0 µg/mL). On the contrary, the free phenolic extract (IC = 210.0 µg/mL) had significantly lower inhibition against α-amylase than the bound phenolic-rich extract (IC = 190.0 µg/mL).</p><p><b>CONCLUSION</b>The phenolic-rich extracts of BF leaves showed antioxidant potentials and inhibited two key carbohydrate-metabolizing enzymes in vitro.</p>


Subject(s)
Animals , Antioxidants , Chemistry , Pharmacology , Diabetes Mellitus, Type 2 , Metabolism , Enzyme Inhibitors , Chemistry , Pharmacology , Glycoside Hydrolase Inhibitors , Chemistry , Pharmacology , Humans , Iron , Magnoliopsida , Chemistry , Oxidative Stress , Pancreas , Metabolism , Phenols , Chemistry , Pharmacology , Plant Extracts , Chemistry , Pharmacology , Rats , Swine , alpha-Amylases , Chemistry , alpha-Glucosidases , Chemistry
12.
Article in English | WPRIM | ID: wpr-812053

ABSTRACT

The present study was designed to characterize the polyphenols isolated from Acacia mearnsii bark crude extract (B) and fractions (B1-B7) obtained by high-speed counter-current chromatography (HSCCC) and evaluate their anti-inflammatory and carbolytic enzymes (α-glucosidase and α-amylase) inhibitory activities. Fractions B4, B5, B6, B7 (total phenolics 850.3, 983.0, 843.9, and 572.5 mg·g, respectively; proanthocyanidins 75.7, 90.5, 95.0, and 44.8 mg·g, respectively) showed significant activities against reactive oxygen species (ROS), nitric oxide (NO) production, and expression of pro-inflammatory genes interleukin-1β (IL-1β) and inducible nitric oxide synthase (iNOS) in a lipopolysaccharide (LPS)-stimulated mouse macrophage cell line RAW 264.7. All the extracts suppressed α-glucosidase and α-amylase activities, two primary enzymes responsible for carbohydrate digestion. A. mearnsii bark samples possessed significantly stronger inhibitory effects against α-glucosidase enzyme (IC of 0.4-1.4 μg·mL) than the pharmaceutical acarbose (IC 141.8 μg·mL). B6 and B7 (IC 17.6 and 11.7 μg·mL, respectively) exhibited α-amylase inhibitory activity as efficacious as acarbose (IC 15.4 μg·mL). Moreover, B extract, at 25 µg·mL, significantly decreased the non-mitochondrial oxidative burst that is often associated with inflammatory response in human monocytic macrophages.


Subject(s)
Acacia , Chemistry , Animals , Anti-Inflammatory Agents , Pharmacology , Carbohydrate Metabolism , Glycoside Hydrolase Inhibitors , Pharmacology , Inflammation , Metabolism , Interleukin-1beta , Metabolism , Lipopolysaccharides , Macrophages , Mice , Nitric Oxide , Metabolism , Nitric Oxide Synthase Type II , Metabolism , Plant Bark , Chemistry , Plant Extracts , Chemistry , Pharmacology , Polyphenols , Pharmacology , Proanthocyanidins , Pharmacology , alpha-Amylases , alpha-Glucosidases , Metabolism
13.
Article in English | WPRIM | ID: wpr-812048

ABSTRACT

Three new labdane diterpenoids, leojaponicone A (1), isoleojaponicone A (2) and methylisoleojaponicone A (3), were isolated from the herb of Leonurus japonicus. The chemical structures of these secondary metabolites were elucidated on the basis of 1D and 2D NMR, including HMQC, and HMBC spectroscopic techniques. All the new compounds were tested in vitro for their acetylcholinesterase and α-glucosidase inhibitory activity. Compounds 1-3 exhibited low inhibitory effects on α-glucosidase with respect to acarbose and exhibited high inhibitory effects on acetylcholinesterase with respect to huperzine A.


Subject(s)
Acetylcholinesterase , Metabolism , Cholinesterase Inhibitors , Chemistry , Pharmacology , Diterpenes , Chemistry , Pharmacology , Glycoside Hydrolase Inhibitors , Chemistry , Pharmacology , Leonurus , Chemistry , Magnetic Resonance Spectroscopy , Molecular Structure , Plant Extracts , Chemistry , Pharmacology
14.
Article in English | WPRIM | ID: wpr-812632

ABSTRACT

In the present study, two new compounds from Ipomoea cairica were identified and demonstrated to have α-glucosidase inhibitory activity. They were isolated by column chromatography on silica gel and sephadex LH-20 and finally purified by prep-HPLC, with their structures being elucidated by spectroscopic methods, such as 1D- and 2D-NMR and HR-TOF-MS, and chemical methods. Compounds 1 and 2, named cairicoside A and cairicoside B, were evaluated for α-glucosidase inhibitory activity by the MTT method, with the IC50 values being 25.3 ± 1.6 and 28.5 ± 3.3 μmol·L(-1), respectively.


Subject(s)
Glycoside Hydrolase Inhibitors , Pharmacology , Ipomoea , Chemistry , Molecular Structure , Plant Extracts , Pharmacology , Resins, Plant , Pharmacology , Spectrum Analysis , alpha-Glucosidases
15.
Acta Pharmaceutica Sinica ; (12): 93-99, 2016.
Article in Chinese | WPRIM | ID: wpr-320011

ABSTRACT

In order to develop potent antidiabetic agents that have inhibitory effect to a-glucosidase, twelve β-acetamido ketone derivatives such as N-{[(substituted-4-oxo-thiochroman-3-yl)phenyl]-methyl}acetamide are designed and synthesized through one-pot Dakin-West reaction. Their chemical structures are confirmed by 1H NMR, 13C NMR, IR and HR-MS. In vitro α-glucosidase inhibition assays of compounds 4a-41 were carried out using glucose oxidase method. The result indicated that most of them possess inhibitory activity in vitro. Compound 4k showed the most potent inhibitory activity with 87.3% inhibition of α-glucosidase at the concentration of 5.39 mmol x L(-1). The structure-activity relationship of these β-acetamido ketone derivatives was discussed preliminarily. Moreover, the molecular docking method was used to study the interaction mode of compound 4k and α-glucosidase. Our results will be helpful for designing of α-glucosidase inhibitors in the future.


Subject(s)
Acetamides , Glycoside Hydrolase Inhibitors , Pharmacology , Hypoglycemic Agents , Pharmacology , Molecular Docking Simulation , Structure-Activity Relationship , alpha-Glucosidases , Metabolism
16.
Bol. latinoam. Caribe plantas med. aromát ; 14(6): 483-490, Nov. 2015. tab, ilus
Article in English | LILACS | ID: biblio-907510

ABSTRACT

Euphorbia dioeca Kunth belongs to the Wanderer’s herb complex that is traditionally used for skin diseases and recently as antidiabetic. The methanol and aqueous extracts were evaluated for their in vitro alpha-glucosidase inhibitory activity and an oral starch tolerance test. These extracts showed an IC50 of 0.55 and 0.85 mg/mL, respectively. In diabetic Long Evans rats, the methanol and aqueous extracts reduced significantly the postprandial hyperglycemia peak in 15.2 percent and 12.8 percent, respectively. The alpha-glucosidase inhibitory activity is related with the presence of glycosides, phenolic compounds and flavonoids. Additionally, the safety parameters of both extracts were assessed by means of an acute toxicity test, being classified as innocuous. The traditional use of E. dioeca to control type 2 diabetes was confirmed, being an important source of alfa-glucosidase inhibitors.


Euphorbia dioeca Kunth, pertenece al complejo de plantas medicinales denominado Hierba de la Golondrina; el cual se utiliza para diversos padecimientos, destacando su uso como antidiabético. En dicho marco, se evaluó tanto la actividad inhibitoria de alfa-glucosidasa in vitro, como su desempeño en una prueba de tolerancia a una carga de almidón postprandial. Los extractos inhibieron la actividad de la alfa-glucosidasa con una CI50 de 0.55 y 0.85 mg/mL, respectivamente. Los extractos metanólico y acuoso disminuyeron significativamente el pico hiperglucémico postprandial en un 15.2 por ciento y un 12.8 por ciento, respectivamente, cuando se evaluó en ratas diabéticas. La actividad inhibitoria de alfa-glucosidasa, reflejada en ambas pruebas, está relacionada con la presencia de glicósidos, compuestos fenólicos y flavonoides. De manera adicional, ambos extractos fueron evaluados en una prueba de toxicidad aguda, siendo clasificados como inocuos. Se corroboró el uso tradicional de E. dioeca para el control de la diabetes tipo 2, siendo una importante fuente de compuestos inhibidores de alfa-glucosidasa.


Subject(s)
Animals , Mice , /drug therapy , Euphorbia/chemistry , Glycoside Hydrolase Inhibitors/pharmacology , Plant Extracts/pharmacology , Hyperglycemia/drug therapy , Mice, Inbred BALB C
17.
Mem. Inst. Oswaldo Cruz ; 110(1): 75-85, 03/02/2015. graf
Article in English | LILACS | ID: lil-741624

ABSTRACT

In our previous study, we have found that 5-cyclopropyl-2-[1-(2-fluoro-benzyl)-1H-pyrazolo[3,4-b]pyridine-3-yl]-pyrimidin-4-ylamine (BAY 41-2272), a guanylate cyclase agonist, activates human monocytes and the THP-1 cell line to produce the superoxide anion, increasing in vitro microbicidal activity, suggesting that this drug can be used to modulate immune functioning in primary immunodeficiency patients. In the present work, we investigated the potential of the in vivo administration of BAY 41-2272 for the treatment of Candida albicans and Staphylococcus aureus infections introduced via intraperitoneal and subcutaneous inoculation. We found that intraperitoneal treatment with BAY 41-2272 markedly increased macrophage-dependent cell influx to the peritoneum in addition to macrophage functions, such as spreading, zymosan particle phagocytosis and nitric oxide and phorbol myristate acetate-stimulated hydrogen peroxide production. Treatment with BAY 41-2272 was highly effective in reducing the death rate due to intraperitoneal inoculation of C. albicans, but not S. aureus. However, we found that in vitro stimulation of peritoneal macrophages with BAY 41-2272 markedly increased microbicidal activities against both pathogens. Our results show that the prevention of death by the treatment of C. albicans-infected mice with BAY 41-2272 might occur primarily by the modulation of the host immune response through macrophage activation. .


Subject(s)
Animals , Mice , Adipocytes, White/metabolism , Ananas/chemistry , Dietary Supplements , Fruit/chemistry , Hypoglycemic Agents/isolation & purification , Industrial Waste/analysis , Plant Extracts/isolation & purification , Adipogenesis , Adipocytes, White/cytology , Antioxidants/chemistry , Antioxidants/economics , Antioxidants/isolation & purification , Enzyme Inhibitors/chemistry , Enzyme Inhibitors/economics , Enzyme Inhibitors/isolation & purification , Food-Processing Industry/economics , Glycosylation , Glycerolphosphate Dehydrogenase/antagonists & inhibitors , Glycerolphosphate Dehydrogenase/metabolism , Glycoside Hydrolase Inhibitors/chemistry , Glycoside Hydrolase Inhibitors/economics , Glycoside Hydrolase Inhibitors/isolation & purification , Hypoglycemic Agents/chemistry , Hypoglycemic Agents/economics , India , Industrial Waste/economics , Lipotropic Agents/chemistry , Lipotropic Agents/economics , Lipotropic Agents/isolation & purification , Plant Extracts/chemistry , Plant Extracts/economics , Solvents/chemistry , alpha-Amylases/antagonists & inhibitors , alpha-Amylases/metabolism
18.
Article in English | WPRIM | ID: wpr-812155

ABSTRACT

The present study aimed at identifying potential lead compounds for diabetes mellitus drug discovery. We developed a novel method involving centrifugal ultrafiltration separation subsequent liquid chromatography with quadrupole time of flight tandem mass spectrometry (LC-Q/TOF-MS/MS) determination to screen α-glucosidase inhibitors in complex Scutellaria baicalensis Georgi (SBG) extract. By adding a second filter to the screening process, the level of non-specific binding of Compounds 1, 3, 10 and 11 was significantly decreased, and the level of non-specific binding of Compounds 5 and 15 also was reduced. As a result, five flavonoids identified as baicalein, baicalein, wogonin, chrysin, and oroxylin A, were rapidly found to interact with α-glucosidase and possess potent anti-α-glucosidase activity in vitro. Specific binding of ligands to α-glucosidase was demonstrated though the proposed method and the ligands could be ranked in order of affinity for α-glucosidase, which were corresponded to the order of inhibitory activity in vitro. In conclusion, our results indicated that the developed method is a rapid and effective screening method for rat intestinal α-glucosidase inhibitors from complex herbal medicines such as SBG.


Subject(s)
Animals , Chromatography, Liquid , Methods , Flavonoids , Allergy and Immunology , Glycoside Hydrolase Inhibitors , Allergy and Immunology , Hypoglycemic Agents , Allergy and Immunology , Plant Extracts , Chemistry , Rats , Tandem Mass Spectrometry , Methods , Ultrafiltration , Methods
19.
Journal of Taibah University Medical Sciences. 2015; 10 (3): 278-287
in English | IMEMR | ID: emr-171858

ABSTRACT

This study investigated the phenolic constituents, antioxidant properties and effect of aqueous extracts from some Corchorus species [C. aestuans, C. bougoudo, C. capsularis, C. olitorius and C. urtifolicus] on alpha-amylase and alpha-glucosidase activities in vitro. Gas Chromatography with Flame Ionization Detector [GC-FID] was used to characterize the phenolic constituents. Aqueous extracts were prepared weight/volume [w/v] and their effects on alpha-amylase and alpha-glucosidase activities, Fe[2+] induced lipid peroxidation, and 1,1-diphenyl[-2] picrylhydrazyl [DPPH] radical scavenging properties were determined. Fe[2+] chelating abilities and Ferric Reducing Antioxidant Power [FRAP] properties were also studied. The predominant phenolics detected by GCFID were kaempferol, rutin, apigenin, luteolin, caffeic acid and quercetin. The results showed that all the Corchorus species significantly [P < 0.05] inhibited alpha-amylase and alpha-glucosidase activities dose-dependently [0-8 micro g/ml]. C. olitorius had the highest alpha-amylase inhibitory ability while C. bougoudo demonstrated the maximum alpha-glucosidase inhibition. However, all the Corchorus species inhibited alpha-glucosidase better than alpha-amylase and also exhibited antioxidant properties. The enzyme inhibitory and antioxidant properties exhibited by the Corchorus species could be attributed to their phenolic constituents and vitamin C content; a possible mechanism by which Corchorus species could elicit therapeutic effects on type 2 diabetes mellitus as obtained in folklore medicine


Subject(s)
Animals, Laboratory , Antioxidants , alpha-Amylases/drug effects , alpha-Glucosidases/drug effects , Glycoside Hydrolase Inhibitors , alpha-Amylases/antagonists & inhibitors , Phenols , Rats, Wistar
20.
Pakistan Journal of Pharmaceutical Sciences. 2015; 28 (2): 521-523
in English | IMEMR | ID: emr-178149

ABSTRACT

Anti-glycation and alpha-glucosidase inhibition activities of microbial transformed compounds of dydrogesterone [1]; 20R-hydroxy-9 beta,10 alpha-pregna-4,6-diene-3-one [2], 17 beta-hydroxy-9 beta,10 alpha-androsta-4,6-diene-3-one [3] and 9 beta,10 alpha- androsta-4,6-diene-3,17-dione [4] were evaluated. Compounds 1 and 4 showed potent alpha-glucosidase inhibitory activities, while 2 and 3 were found to be weak inhibitors, whereas anti-glycation activities of 1-4 were not observed


Subject(s)
Glycosylation , alpha-Glucosidases , Glycoside Hydrolase Inhibitors
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