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Vitae (Medellín) ; 31(1): 1-7, 2024-05-03. Ilustraciones
Article in English | LILACS, COLNAL | ID: biblio-1538070


Background: Moringa peregrina is widely used in the traditional medicine of the Arabian Peninsula to treat various ailments, because it has many pharmacologically active components with several therapeutic effects. Objective: This study aimed to investigate the inhibitory effect of Moringaperegrina seed ethanolic extract (MPSE) against key enzymes involved in human pathologies, such as angiogenesis (thymidine phosphorylase), diabetes (α-glucosidase), and idiopathic intracranial hypertension (carbonic anhydrase). In addition, the anticancer properties were tested against the SH-SY5Y (human neuroblastoma). Results: MPSE extract significantly inhibited α-glucosidase, thymidine phosphorylase, and carbonic anhydrase with half-maximal inhibitory concentrations (IC50) values of 303.1 ± 1.3, 471.30 ± 0.3, and 271.30 ± 5.1 µg/mL, respectively. Furthermore, the antiproliferative effect of the MPSE was observed on the SH-SY5Y cancer cell line with IC50 values of 55.1 µg/mL. Conclusions: MPSE has interesting inhibitory capacities against key enzymes and human neuroblastoma cancer cell line.

Antecedentes: La Moringa peregrina se utiliza ampliamente en la medicina tradicional de la Península Arábiga para tratar diversas dolencias, ya que posee numerosos componentes farmacológicamente activos con varios efectos terapéuticos. Objetivo: Este estudio tenía como objetivo investigar el efecto inhibidor del extracto etanólico de semillas de Moringaperegrina (MPSE) frente a enzimas clave implicadas en patologías humanas, como la angiogénesis (timidina fosforilasa), la diabetes (α-glucosidasa) y la hipertensión intracraneal idiopática (anhidrasa carbónica). Además, se comprobaron las propiedades anticancerígenas frente al SH-SY5Y (neuroblastoma humano). Resultados: El extracto de MPSE inhibió significativamente la α-glucosidasa, la timidina fosforilasa y la anhidrasa carbónica con concentraciones inhibitorias semimáximas (IC50) de 303,1 ± 1,3, 471,30 ± 0,3 y 271,30 ± 5,1 µg/mL, respectivamente. Además, se observó el efecto antiproliferativo del MPSE en la línea celular del cáncer SH-SY5Y con valores de IC50 de 55,1 µg/mL. Conclusiones: MPSE posee interesantes capacidades inhibitorias frente a enzimas clave y línea celular de neuroblastoma canceroso humano.

Humans , Anticarcinogenic Agents , Moringa , Enzyme Inhibitors , alpha-Glucosidases
Acta neurol. colomb ; 39(2)jun. 2023.
Article in Spanish | LILACS | ID: biblio-1533488


Introducción: La enfermedad de Pompe es un trastorno de origen genético causado por la deficiencia de la enzima alfa-glucosidasa ácida, que se caracteriza por el acumulo anormal de glucógeno en los músculos y otros tejidos, generando una debilidad muscular progresiva, la cual debe ser diagnosticada y tratada de forma oportuna, ya que de esto dependerá el pronóstico, la sobrevida y la funcionalidad de los pacientes con esta condición. Contenidos: El abordaje multidisciplinario incluye tanto una adecuada valoración y soporte nutricional como el inicio del tratamiento modificador de enfermedad a través de la terapia de reemplazo enzimático, que a su vez dependerá de la forma de presentación, la variante genética, el perfil inicial del paciente, las condiciones especiales que puedan existir y las metas propias para cada paciente. Para garantizar un manejo adecuado, se deben realizar estudios de seguimiento con parámetros objetivos, evaluar posibles eventos secundarios e instaurar su manejo en caso de presentarlos. Conclusiones: El pronóstico de esta enfermedad dependerá del inicio oportuno del tratamiento, la implementación de pautas nutricionales adecuadas y el establecimiento del seguimiento de los parámetros clínicos y paraclínicos para cada uno de los pacientes.

Introduction: Pompe disease is a disorder of genetic origin caused by the deficiency of the acid alpha-glucosidase enzyme, which is characterized by the abnormal accumulation of glycogen in the muscles and other tissues, generating progressive muscle weakness, which must be diagnosed and treated in a timely manner, since the prognosis, survival, and functionality of patients with this condition will depend on this. Contents: The multidisciplinary approach includes both an adequate evaluation and nutritional support as well as the initiation of disease-modifying treatment through enzyme replacement therapy, which in turn will depend on the form of presentation, the genetic variant, the initial profile of the patient, the special conditions that may exist and the specific goals for each patient. To guarantee adequate management, follow-up studies must be carried out with objective parameters, evaluate possible secondary events and establish their management in case of presenting them. Conclusions: The prognosis of this disease will depend on the timely initiation of treatment, the implementation of adequate nutritional guidelines and the establishment of monitoring of clinical and paraclinical parameters for each of the patients.

Glycogen Storage Disease Type II , Diet , alpha-Glucosidases , Nutritional Sciences , Enzyme Replacement Therapy
Braz. J. Pharm. Sci. (Online) ; 59: e19544, 2023. tab, graf
Article in English | LILACS | ID: biblio-1429970


Abstract A new series of N-Mannich bases of 2-Phenyl-5-benzimidazole sulfonic acid have been synthesized through amino methylation reaction with secondary amines. The two moieties were held together through a methylene bridge, which comes from formaldehyde (Formalin Solution 37%) used in the reaction. Chemical structures of the newly synthesized compounds have been confirmed using FT-IR, 1HNMR and 13CNMR. Different in vitro assays including Anti-oxidant, Enzyme inhibition, Anti-microbial and Cytotoxicity assay were performed to evaluate the biological potential with reference to the standard drug. Among the synthesized library, compound 3a shows maximum alpha-glucosidase inhibition with an IC50 value of 66.66 µg/ml, compound 3d was found most toxic with LC50 value of 10.17 µg/ml. ADME evaluation studies were performed with the help of Molinspiration online software. Docking calculations were also performed. Given the importance of the nucleus involved, the synthesized compound might find extensive medicinal applications as reported in the literature.

Benzimidazoles/agonists , Mannich Bases/analysis , Antioxidants/pharmacology , Sulfonic Acids/adverse effects , Pharmaceutical Preparations/administration & dosage , alpha-Glucosidases/adverse effects , Molecular Docking Simulation/instrumentation , Methylation
China Journal of Chinese Materia Medica ; (24): 6676-6681, 2023.
Article in Chinese | WPRIM | ID: wpr-1008865


Nine compounds were isolated from the 90% ethanol extract of Salacia polysperma by silica gel, Sephadex LH-20 column chromatography, together with preparative HPLC methods. Based on HR-ESI-MS, MS, 1D and 2D NMR spectral analyses, the structures of the nine compounds were identified as 28-hydroxy wilforlide B(1), wilforlide A(2), 1β,3β-dihydroxyurs-9(11),12-diene(3),(-)-epicatechin(4),(+)-catechin(5),(-)-4'-O-methyl-ent-galloepicatechin(6), 3-hydroxy-1-(4-hydroxy-3-methoxy-phenyl)propan-1-one(7),(-)-(7S,8R)-4-hydroxy-3,3',5'-trimethoxy-8',9'-dinor-8,4'-oxyneoligna-7,9-diol-7'-aldehyde(8), and vanillic acid(9). Compound 1 is a new oleanane-type triterpene lactone. Compounds 1, 3, 4, 7-9 were isolated from the Salacia genus for the first time. All compounds were assayed for their α-glucosidase inhibitory activity. The results suggested that compound 8 exhibited moderate α-glucosidase inhibitory activity, with an IC_(50) value of 37.2 μmol·L~(-1), and the other compounds showed no α-glucosidase inhibitory activity.

Salacia/chemistry , alpha-Glucosidases , Triterpenes/pharmacology , Magnetic Resonance Spectroscopy , Ethanol , Molecular Structure
Braz. j. biol ; 83: 00264, 2023. tab, graf
Article in English | LILACS, VETINDEX | ID: biblio-1339364


Abstract Allium cepa L. is a commonly consumed vegetable that belongs to the Amaryllidaceae family and contains nutrients and antioxidants in ample amounts. In spite of the valuable food applications of onion bulb, its peel and outer fleshy layers are generally regarded as waste and exploration of their nutritional and therapeutic potential is still in progress with a very slow progression rate. The present study was designed with the purpose of doing a comparative analysis of the antioxidant potential of two parts of Allium cepa, i.g., bulb (edible part) and outer fleshy layers and dry peels (inedible part). Moreover, the inhibitory effect of the onion bulb and peel extracts on rat intestinal α-glucosidase and pancreatic α-amylase of porcine was also evaluated. The antioxidant potential of onion peel and bulb extracts were evaluated using 2,2-diphenyl- 1-picryl hydrazyl (DPPH), ferric-reducing antioxidant power assay (FRAP), 2,2'-azino-bis- 3-ethylbenzothiazoline-6-sulfonic acid (ABTS) radical scavenging assay, H2O2 radical scavenging activity and Fe2+ chelating activity. Total flavonoids and phenolic content of ethanolic extract of onion peel were significantly greater as compared to that of onion bulb. Ethanolic extract of onion peel also presented better antioxidant and free-radical scavenging activity as compared to the ethanolic extract of bulb, while the aqueous extract of bulb presented weakest antioxidative potential. Onion peel extract's α-glucosidase inhibition potential was also correlated with their phenolic and flavonoid contents. The current findings presented onion peel as a possible source of antioxidative agents and phenolic compounds that might be beneficial against development of various common chronic diseases that might have an association with oxidative stress. Besides, outer dry layers and fleshy peels of onion exhibited higher phenolic content and antioxidant activities, compared to the inner bulb. The information obtained by the present study can be useful in promoting the use of vegetable parts other than the edible mesocarp for several future food applications, rather than these being wasted.

Resumo Allium cepa pertence à família Liliaceae e é rica em nutrientes e antioxidantes. Apesar das expressivas aplicações alimentares do bulbo da cebola, sua casca e outras camadas externas são geralmente consideradas resíduos, e seu potencial nutricional e terapêutico ainda é pouco explorado. O presente estudo foi delineado com o objetivo de investigar comparativamente o potencial antioxidante de duas partes de Allium cepa, por exemplo o bulbo (parte comestível) e camadas externas e cascas secas (parte não comestível). Além disso, o efeito inibitório dos extratos do bulbo de cebola e casca sobre a α-glucosidase intestinal de ratos e α-amilase pancreática suína também foi avaliado. O potencial antioxidante dos extratos da casca de cebola e bulbo foi avaliado utilizando-se 2,2-difenil-1-picrilhidrazil (DPPH), método de poder antioxidante de redução do ferro (FRAP), método 2,2'-azino-bis-3-etilbenzotiazolina-6-ácido sulfônico (ABTS) de eliminação de radicais, atividade de eliminação de radicais H2O2 e atividade quelante do Fe2+. Os flavonoides totais e os teores fenólicos do extrato de etanol da casca de cebola foram significativamente maiores quando comparados ao do bulbo. O extrato de etanol da casca de cebola também apresentou melhor atividade antioxidante e eliminação de radicais livres quando comparado ao extrato de etanol do bulbo, enquanto o extrato aquoso de bulbo apresentou menor potencial antioxidante. O potencial de inibição da α-glicosidase dos extratos de casca de cebola correlacionou-se com seus teores fenólicos e de flavonoides. Os resultados encontrados identificaram que a casca de cebola é uma possível fonte de agentes antioxidantes e compostos fenólicos que podem ser benéficos contra o desenvolvimento de várias doenças crônicas que estão associadas ao estresse oxidativo. Além disso, as camadas externas secas e as cascas da cebola exibiram maior conteúdo fenólico e atividades antioxidantes, em comparação com o bulbo interno. As informações obtidas pelo presente estudo podem promover o uso de outras partes vegetais além do mesocarpo comestível para futuras aplicações em alimentos, ao invés de serem desperdiçadas.

Animals , Rats , Onions , Antioxidants , Swine , Plant Extracts/pharmacology , alpha-Glucosidases , Hydrogen Peroxide
China Journal of Chinese Materia Medica ; (24): 4686-4692, 2023.
Article in Chinese | WPRIM | ID: wpr-1008635


The chemical constituents of the seeds of Moringa oleifera were isolated and purified by using Sephadex LH-20, Toyo-pearl HW-40F, silica gel, ODS, and MCI column chromatography. The structures of compounds were identified by high-resolution mass spectrometry, ~1H-NMR, ~(13)C-NMR, HMQC, HMBC, and ~1H-~1H COSY, as well as physicochemical properties of compounds and literature data. Twelve compounds were isolated from 30% ethanol fraction of the seeds of M. oleifera and identified as ethyl-4-O-α-L-rhamnosyl-α-L-rhamnoside(1), ethyl-3-O-α-L-rhamnosyl-α-L-rhamnoside(2),(4-hydroxybenzyl)ethyl carbamate(3),(4-aminophenyl)acetic acid(4), ethyl-α-L-rhamnoside(5), methyl-α-L-rhamnoside(6), moringapyranosyl(7), 2-[4-(α-L-rhamnosyl)phenyl]methyl acetate(8), niaziridin(9), 5-hydroxymethyl furfural(10), 4-hydroxybenzeneacetamide(11), and 4-hydroxybenzoic acid(12). Among them, compounds 1 and 2 are two new compounds, compound 3 is a new natural product, and compounds 4-5 were yielded from Moringa plant for the first time. All compounds were evaluated for α-glucosidase inhibitory activity in vitro. Compound 10 showed excellent inhibitory activity with IC_(50) of 210 μg·mL~(-1).

Moringa oleifera/chemistry , alpha-Glucosidases , Moringa , Seeds , Plant Extracts/pharmacology
Chinese Journal of Contemporary Pediatrics ; (12): 420-424, 2023.
Article in Chinese | WPRIM | ID: wpr-981973


Pompe disease, also known as glycogen storage disease type Ⅱ, is a rare autosomal recessive disease. With the application of enzyme replacement therapy, more and more patients with Pompe disease can survive to adulthood, and nervous system-related clinical manifestations gradually emerge. Nervous system involvement seriously affects the quality of life of patients with Pompe disease, and a systematic understanding of the clinical manifestations, imaging features and pathological changes of nervous system injury in Pompe disease is of great significance for the early identification and intervention of Pompe disease. This article reviews the research progress of neurological damage in Pompe disease.

Humans , Glycogen Storage Disease Type II/drug therapy , alpha-Glucosidases , Quality of Life , Enzyme Replacement Therapy
Chinese Journal of Medical Genetics ; (6): 711-717, 2023.
Article in Chinese | WPRIM | ID: wpr-981813


OBJECTIVE@#To explore the clinical features, lysosomal enzymatic [acid α-glucosidase (GAA)] activities and genetic variants in a child with late-onset Pompe disease (LOPD).@*METHODS@#Clinical data of a child who had presented at the Genetic Counseling Clinic of West China Second University Hospital in August 2020 was retrospectively analyzed. Blood samples were collected from the patient and her parents for the isolation of leukocytes and lymphocytes as well as DNA extraction. The activity of lysosomal enzyme GAA in leukocytes and lymphocytes was analyzed with or without addition of inhibitor of GAA isozyme. Potential variants in genes associated with neuromuscular disorders were analyzed, in addition with conservation of the variant sites and protein structure. The remaining samples from 20 individuals undergoing peripheral blood lymphocyte chromosomal karyotyping were mixed and used as the normal reference for the enzymatic activities.@*RESULTS@#The child, a 9-year-old female, had featured delayed language and motor development from 2 years and 11 months. Physical examination revealed unstable walking, difficulty in going upstairs and obvious scoliosis. Her serum creatine kinase was significantly increased, along with abnormal electromyography, whilst no abnormality was found by cardiac ultrasound. Genetic testing revealed that she has harbored compound heterozygous variants of the GAA gene, namely c.1996dupG (p.A666Gfs*71) (maternal) and c.701C>T (p.T234M) (paternal). Based on the guidelines from the American College of Medical Genetics and Genomics, the c.1996dupG (p.A666Gfs*71) was rated as pathogenic (PVS1+PM2_Supporting+PM3), whilst the c.701C>T (p.T234M) was rated as likely pathogenic (PM1+PM2_Supporting+PM3+PM5+PP3). The GAA in the leukocytes from the patient, her father and mother were respectively 76.1%, 91.3% and 95.6% of the normal value without the inhibitor, and 70.8%, 112.9% and 128.2% of the normal value with the inhibitor, whilst the activity of GAA in their leukocytes had decreased by 6 ~ 9 times after adding the inhibitor. GAA in lymphocytes of the patient, her father and mother were 68.3%, 59.0% and 59.5% of the normal value without the inhibitor, and 41.0%, 89.5% and 57.7% of the normal value with the inhibitor, the activity of GAA in lymphocytes has decreased by 2 ~ 5 times after adding the inhibitor.@*CONCLUSION@#The child was diagnosed with LOPD due to the c.1996dupG and c.701C>T compound heterozygous variants of the GAA gene. The residual activity of GAA among LOPD patients can range widely and the changes may be atypical. The diagnosis of LOPD should not be based solely on the results of enzymatic activity but combined clinical manifestation, genetic testing and measurement of enzymatic activity.

Humans , Child , Male , Female , Glycogen Storage Disease Type II/pathology , Retrospective Studies , alpha-Glucosidases/genetics , Mothers , Lysosomes/pathology , Mutation
Chinese Journal of Natural Medicines (English Ed.) ; (6): 443-453, 2023.
Article in English | WPRIM | ID: wpr-982715


This study employed the α-glucosidase inhibitory activity model as an anti-diabetic assay and implemented a bioactivity-guided isolation strategy to identify novel natural compounds with potential therapeutic properties. Hypericum sampsoniiwas investigated, leading to the isolation of two highly modified seco-polycyclic polyprenylated acylphloroglucinols (PPAPs) (1 and 2), eight phenolic derivatives (3-10), and four terpene derivatives (11-14). The structures of compounds 1 and 2, featuring an unprecedented octahydro-2H-chromen-2-one ring system, were fully characterized using extensive spectroscopic data and quantum chemistry calculations. Six compounds (1, 5-7, 9, and 14) exhibited potential inhibitory effects against α-glucosidase, with IC50 values ranging from 0.050 ± 0.0016 to 366.70 ± 11.08 μg·mL-1. Notably, compound 5 (0.050 ± 0.0016 μg·mL-1) was identified as the most potential α-glucosidase inhibitor, with an inhibitory effect about 6900 times stronger than the positive control, acarbose (IC50 = 346.63 ± 15.65 μg·mL-1). A docking study was conducted to predict molecular interactions between two compounds (1 and 5) and α-glucosidase, and the hypothetical biosynthetic pathways of the two unprecedented seco-PPAPs were proposed.

Molecular Structure , Hypericum/chemistry , alpha-Glucosidases , Magnetic Resonance Spectroscopy , Glycoside Hydrolase Inhibitors/pharmacology
Med. lab ; 26(3): 287-296, 2022. Tabs
Article in Spanish | LILACS | ID: biblio-1412413


La enfermedad de Pompe es un desorden neuromuscular autosómico recesivo de baja prevalencia, causado por la deficiencia total o parcial de la enzima alfa glucosidasa ácida (GAA), cuya única terapia de reemplazo enzimático disponible es la alglucosidasa alfa recombinante. Las reacciones adversas asociadas a la infusión se presentan con frecuencia. Se reportan dos casos de desensibilización exitosa con alglucosidasa alfa utilizando protocolos con dosis meta de 20 mg/kg, administrados quincenalmente; el primero de ellos, en una niña con historia de reacción adversa grave a los 15 meses de edad, en quien se utilizó un esquema con una dilución inicial de 1/10.000.000 de 28 pasos y una duración total de 13,1 horas. En el segundo caso, la paciente tuvo una reacción adversa grave a los 4 años de edad, se utilizó el protocolo de 22 pasos, concentración inicial de 1/1.000.000 y duración total de 7,2 horas. Se concluye que en pacientes con enfermedad de Pompe que presentan reacciones adversas durante la terapia de reemplazo enzimático, es posible realizar la desensibilización cada dos semanas con la dosis estándar de 20 mg/kg de forma exitosa, y progresivamente lograr la administración usual de la infusión

Pompe disease is a low prevalence autosomal recessive neuromuscular disorder, caused by total or partial deficiency of the acid alpha-glucosidase (GAA) enzyme, and its only available enzyme replacement therapy is the recombinant alglucosidase alfa. Infusion-associated adverse reactions occur frequently. Two cases of successful desensitization with alglucosidase alfa using protocols with a target dose of 20 mg/kg administered biweekly are reported; the first was a girl who had a history of serious adverse reaction at the age of 15 months, and undergone to a scheme with an initial dilution of 1/10,000,000 with 28 steps and a total duration of 13.1 hours. In the second case, the patient had a severe adverse reaction at the age of 4 years, a 22-step protocol was used with an initial concentration of 1/1,000,000 and a total duration of 7.2 hours. In conclusion, in patients with Pompe disease who presented adverse reactions during enzyme replacement therapy with alglucosidase alfa, it is possible to perform desensitization every two weeks with the standard dose of 20 mg/kg, and progressively achieve the usual administration of the infusion

Glycogen Storage Disease Type II , Therapeutics , Desensitization, Immunologic , Enzymes , alpha-Glucosidases , Hypersensitivity
Malaysian Journal of Microbiology ; : 192-203, 2022.
Article in English | WPRIM | ID: wpr-977616


Aims@#This study aimed to evaluate antidiabetic potential of indigenous Lactobacillus isolates by measuring the ability of α-glucosidase inhibitory (AGI) and antioxidant activity. The mechanism of probiotics as antidiabetic can occur through the AGI and antioxidant activity of LAB, which is able to suppress oxidative stress that causes chronic inflammation and pancreatic β cell apoptosis, and then through the ability to produce exopolysaccharide (EPS) and short chain fatty acids (SCFA).@*Methodology and results@#MRS broth enriched with 10% glucose was selected as the growth medium for Lactobacillus. The growth medium was then centrifuged to obtain CFS and CFE was produced by extracting the medium with 96% ethanol as a solvent. The results showed that Lactobacillus pentosus MK42 had the highest AGI activity of 80.32 ± 2.20%. Antioxidant activity was not significantly different (P>0.05) among the tested Lactobacillus isolates. Lactobacillus paracasei RK41 produced the highest EPS (360.13 ± 50.01 mg/L), which was not significantly different (P>0.05) from Lactobacillus plantarum1 RB210. All Lactobacillus isolates were able to produce acetic acid, but not all were able to produce propionic and butyric acid. The highest propionic acid was produced by L. plantarum1 RB210 at 0.40 ± 0.31 mmol/L and the highest butyric acid was produced by L. plantarum1 MK2 at 0.22 ± 0.08 mmol/L.@*Conclusion, significance and impact of study@#The results show definitively that indigenous Lactobacillus isolates have considerable α-glucosidase inhibitor, antioxidant activity and the ability to produce of EPS and SCFA. This preliminary study suggests the use of indigenous Lactobacillus isolates which have the potential as antidiabetic agent, although the responsible compounds are unknown.

alpha-Glucosidases , Antioxidants , Hypoglycemic Agents
Rev. peru. med. integr ; 5(1): 5-11, 2020. tab, ilus
Article in Spanish | MTYCI, LILACS | ID: biblio-1146111


La etnomedicina es una disciplina idónea para elegir especies vegetales con el fin de ser estudiadas farmacológicamente; las cuatro especies seleccionadas para el presente estudio se usan como hipoglucemiantes en la medicina tradicional de la Amazonía peruana. Objetivos. Estudiar la capacidad inhibitoria in vitro de los extractos de cuatro plantas de uso tradicional, sobre la actividad de la α-glucosidasa, una enzima importante involucrada en la regulación de la glicemia. Materiales y métodos. Mediante el ensayo de inhibición de la enzima α-glucosidasa se evaluaron diferentes concentraciones de cada extracto para determinar la concentración inhibitoria media (IC50) y compararlos con la droga control acarbosa. Resultados. El extracto acuoso liofilizado de Guazuma ulmifolia mostró significante efecto inhibitorio (IC50 :13,49±3,65 µg/mL), al compararlo con la droga control, acarbosa (IC50: 858,67±29,73 µg/mL) y los otros extractos. Conclusiones. Los resultados sugieren que la actividad antidiabética de la Guazuma ulmifolia estaría mediada por la inhibición de la α-glucosidasa, lo que implicaría su potencial en la reducción de la glucosa posprandial.

Ethnomedicine is an ideal discipline for choosing plant species to be studied pharmacologically; the four species selected for this study are used as hypoglycemics in the traditional medicine of the Peruvian Amazon. Objectives. To study the inhibitory capacity in vitro of the extracts of four plants of traditional use, on the activity of α-glucosidase, an important enzyme involved in the regulation of glycemia. Materials and methods. Using the inhibition test of the enzyme α-glucosidase, different concentrations of each extract were evaluated to determine the average inhibitory concentration (IC50) and to compare them with the control drug acarbose. Results. The freeze-dried aqueous extract of Guazuma ulmifolia showed a significant inhibitory effect (IC50:13,49±3,65 µg/mL) when compared with the control drug, acarbose (IC50: 858,67±29,73 µg/mL), and the other extracts. Conclusions. The results suggest that the antidiabetic activity of Guazuma ulmifolia would be mediated by the inhibition of α-glucosidase, which would imply its potential in the reduction of postprandial glucose.

Humans , Tabebuia , Physalis , alpha-Glucosidases , In Vitro Techniques , Plant Extracts , Amazonian Ecosystem , Freeze Drying , Hypoglycemic Agents , Medicine, Traditional
China Journal of Chinese Materia Medica ; (24): 1180-1187, 2020.
Article in Chinese | WPRIM | ID: wpr-1008489


Based on the idea of plant metabolomics, ultra performance liquid chromatography-quadrupole time-of-flight mass spectrometry(UPLC-Q-TOF-MS/MS) was used to compare the chemical composition between 6 batches of fruit vinegar brewed from Choerospondias axillaris fruit peel and 6 batches of apple vinegar purchased from 3 companies. Antioxidant and α-glucosidase inhibition activities were also tested in vitro. A total of 43 compounds were identified by reference substance, liquid chromatography-mass spectrometry(LC-MS/MS) fragmentation information or literature data. A total of 40 compounds were identified in the C. axillaris fruit peel vinegar. A total of 16 compounds were identified in apple vinegar. There were 13 common ingredients including organic acids and esters such as citric acid, 2-isopropyl malic acid, and triethyl citrate. The results of partial leastsquares-discriminant analysis(PLS-DA) indicated that they had 33 significantly different compounds such as proanthocyanidin oligomer, quercetin-3-O-rhamnoside and heptadecanoic acid. The proanthocyanidins and flavonoid glycosides in C. axillaris peel vinegar were more abundant than apple vinegar, so it had better health function than ordinary fruit vinegar. The results showed that C. axillaris fruit peel vinegar had stronger antioxidant and α-glucosidase inhibition activities in vitro. The vinegar brewed from waste C. axillaris fruit peel had more chemical ingredients than the apple vinegar. C. axillaris fruit peel vinegar had better biological activity and health function, so it had good development prospect. This study provided the scientific evidence for exploiting the C. axillaris fruit peel into high value-added products. It also provided ideas for the comprehensive development and utilization of similar Chinese medicine waste.

Acetic Acid/pharmacology , Anacardiaceae/chemistry , Antioxidants , Chromatography, High Pressure Liquid , Fruit/chemistry , Glycoside Hydrolase Inhibitors/pharmacology , Malus/chemistry , Plant Extracts , Tandem Mass Spectrometry , alpha-Glucosidases
Adv Rheumatol ; 59: 10, 2019. tab
Article in English | LILACS | ID: biblio-1088593


Abstract Introduction: Anti-nucleosome and anti-C1q antibodies demonstrated an association with the development of glomerulonephritis in systemic lupus erythematosus (SLE). Some investigators have proposed that monitoring anti- C1q and anti-nucleosome antibodies might be valuable for making predictions about lupus nephritis (LN) and assessment of disease activity as a non-invasive biological marker of renal disease. Objectives: The current study was proposed to investigate the presence of anti-C1q and anti-nucleosome antibodies in the sera of Egyptian patients with SLE and their association with LN. Methods: Eighty patients with SLE were included. Patients were classified into, a LN group including 40 cases with active LN (based on the results of renal biopsy and renal SLEDAI≥4) and a non renal SLE group including 40 patients (with no clinical or laboratory evidence of renal involvement that were attributed in the past or present to SLE). They were subjected to full medical history taking, clinical examination, routine laboratory investigations, measurement of antinuclear antibody (ANA), anti-ds DNA, anti-C1q & anti-nucleosome antibodies. Results: Anti-C1q antibody showed a statistically significant association with the presence of vasculitis and nephritis while anti-nucleosome antibody didn't show a significant association with the presence of any clinical features. Double positivity of anti-nucleosome and anti-C1q antibodies showed a statistically significant association with the presence of vasculitis and photosensitivity, high ECLAM score, elevated ESR, low serum albumin and low C3 levels. Conclusion: Serum anti-C1q antibody has a significant association with LN while double positive antibodies have a significant association with vasculitis and low C3 levels in Egyptian patients with SLE.

Adult , Aged , Female , Humans , Male , Middle Aged , Pulmonary Medicine/methods , Glycogen Storage Disease Type II/complications , Glycogen Storage Disease Type II/diagnosis , Dried Blood Spot Testing/standards , Late Onset Disorders/diagnosis , Lung Diseases/complications , Biopsy , Glycogen Storage Disease Type II/blood , Glycogen Storage Disease Type II/enzymology , Early Diagnosis , alpha-Glucosidases/metabolism , Late Onset Disorders/blood , Late Onset Disorders/enzymology , Italy , Lung Diseases/blood , Muscles/surgery , Muscles/enzymology
Korean Journal of Pediatrics ; : 224-234, 2019.
Article in English | WPRIM | ID: wpr-760211


PURPOSE: Pompe disease (PD) is an autosomal recessive disorder caused by a deficiency of acid alpha-glucosidase resulting from pathogenic GAA variants. This study describes the clinical features, genotypes, changes before and after enzyme replacement therapy (ERT), and long-term outcomes in patients with infantile-onset PD (IOPD) and late-onset PD (LOPD) at a tertiary medical center. METHODS: The medical records of 5 Korean patients (2 male, 3 female patients) diagnosed with PD between 2002 and 2013 at Samsung Medical Center in Seoul, Republic of Korea were retrospectively reviewed for data, including clinical and genetic characteristics at diagnosis and clinical course after ERT. RESULTS: Common initial symptoms included hypotonia, cyanosis, and tachycardia in patients with IOPD and limb girdle weakness in patients with LOPD. Electrocardiography at diagnosis revealed hypertrophic cardiomyopathy in all patients with IOPD who showed a stable disease course during a median follow-up period of 10 years. Patients with LOPD showed improved hepatomegaly and liver transaminase level after ERT. CONCLUSION: As ERT is effective for treatment of PD, early identification of this disease is very important. Thus, patients with IOPD should be considered candidates for clinical trials of new drugs in the future.

Child , Female , Humans , Male , alpha-Glucosidases , Cardiomyopathy, Hypertrophic , Cyanosis , Diagnosis , Electrocardiography , Enzyme Replacement Therapy , Extremities , Follow-Up Studies , Genotype , Glycogen Storage Disease Type II , Hepatomegaly , Liver , Medical Records , Muscle Hypotonia , Republic of Korea , Retrospective Studies , Seoul , Tachycardia
Chinese Journal of Natural Medicines (English Ed.) ; (6): 446-460, 2019.
Article in English | WPRIM | ID: wpr-776866


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.

Humans , Africa South of the Sahara , Chromatography, High Pressure Liquid , Diabetes Mellitus , Drug Therapy , Glycoside Hydrolase Inhibitors , Chemistry , Pharmacology , Hypoglycemic Agents , Chemistry , Pharmacology , Molecular Docking Simulation , Plant Extracts , Chemistry , Pharmacology , Plants, Medicinal , Chemistry , Sapotaceae , Chemistry , alpha-Glucosidases , Metabolism
Braz. J. Pharm. Sci. (Online) ; 55: e17695, 2019. tab, graf
Article in English | LILACS | ID: biblio-1039080


The influence of common tea preparation procedures (temperature, infusion time, consumption time interval and tea bag/loose-leaf) and the type of water used, on the total phenolic content (TPC), the radical scavenging activity and the α-glucosidase inhibitory activity were assessed. Higher TPC and antioxidant activity were obtained when using lower mineralized waters. Tea bags also evidenced higher antioxidant activity than loose-leaf samples. Under the same conditions (90 ºC and five minutes of infusion time) green tea contains almost twice the quantity of polyphenols and the free radical scavenging ability of black tea. In the α-glucosidase assay all infusions were active (97-100 %). Furthermore, HPLC allowed to identify some of the polyphenols present in both teas and to monitor their composition change with time. After twenty-four hours, the antioxidant activity was maintained without significant changes, but a small decrease in enzyme inhibition was observed, although this activity was still very high

Tea/classification , alpha-Glucosidases/analysis , Antioxidants/analysis , Water/analysis , Chromatography, High Pressure Liquid/methods , Polyphenols
Arch. latinoam. nutr ; 68(2): 164-174, jun. 2018. tab, graf
Article in Spanish | LIVECS, LILACS | ID: biblio-1016695


El objetivo de la presente investigación fue evaluar el valor nutrimental, actividad antioxidante e inhibición de la enzima α-glucosidasa de brownies libres de gluten enriquecidos principalmente con leguminosas. Los brownies fueron elaborados principalmente con leguminosas cocidas de frijol pinto (Phaseolus vulgaris L.), alubia chica (Phaseolus vulgaris L.), garbanzo (Cicer arietinum L.) o lenteja (Lens culinaris L.) (300 g de producto). Cada producto fue dividido en porciones de 100 g cada uno. Posteriormente, se determinó su composición nutrimental, y de los extractos etanólicos libres y ligados obtenidos, se evaluó el contenido de fenólicos totales, flavonoides, actividad antioxidante y el potencial inhibitorio de la enzima α-glucosidasa. Los brownies a base de leguminosas cocidas fueron significativamente mejores que los comerciales, y presentaron un contenido de proteínas entre 6.2 y 6.9%, 1.6-4.2% de lípidos, 1.2-5.8% de fibra dietaria soluble y 11.7-21.5% de fibra dietaria insoluble. Los productos presentaron en mayor proporción a los ácidos grasos linolénico y linoleico, además fueron ricos en minerales. El contenido de fenólicos totales, y flavonoides varió dependiendo de la leguminosa con la cual se desarrolló el producto, así como de la fracción que se evaluó. La actividad antioxidante total fue mayor en los brownies de alubia. La mayor inhibición de α-glucosidasa la presentaron los extractos de brownies elaborados a base de lenteja (fracción libre) y garbanzo (fracción ligada). Los brownies elaborados con lenteja fueron sensorialmente los más aceptados. La introducción de este tipo de productos promoverá un consumo nutritivo de alimentos por personas de diferentes edades y con efectos benéficos en la salud(AU)

The aim of the present study was to evaluate the nutritional value, antioxidant activity and inhibition of α-glucosidase enzyme of gluten-free brownies enriched mainly with legumes. The brownies were elaborated mainly with cooked legumes of pinto (Phaseolus vulgaris L.), haricot bean (Phaseolus vulgaris L.), chickpea (Cicer arietinum L.) or lentils (Lens culinaris L.) (300 g of product). Each product was divided into portions of 100 g and the chemical and nutritive composition were determined. From the free and bound ethanolic extracts obtained, the content of total phenolics, flavonoids, antioxidant activity and the potential inhibitor of the α-glucosidase enzyme were evaluated. Brownies based on cooked legumes were significantly better than commercial brownies, with a protein content between 6.2 and 6.8%, 1.6-4.2% lipids, 1.2-5.8% soluble dietary fiber and 11.7-21.5% insoluble dietary fiber. The products had a higher proportion of linolenic and linoleic fatty acids, and they were rich in minerals. The content of total phenolics and flavonoids varied depending on the legume as well as the fraction that was evaluated. Total antioxidant activity was higher in haricot bean-brownies. The highest inhibition of α-glucosidase was detected in extracts obtained from lentil (free fraction) and chickpea (bound fraction) brownies. Brownies based on lentil were the most accepted in the sensory test. The introduction of this type of products promotes a nutritious consumption of foods by people of different ages with beneficial effects on health(AU)

Humans , Male , Female , Diabetes Mellitus/etiology , alpha-Glucosidases , Diet, Gluten-Free , Insulin/biosynthesis , Hyperglycemia , Fabaceae
Arq. neuropsiquiatr ; 76(4): 247-251, Apr. 2018. tab, graf
Article in English | LILACS | ID: biblio-888382


ABSTRACT Pompe disease is an inherited disease caused by acid alpha-glucosidase (GAA) deficiency. A single center observational study aimed at assessing the prevalence of late-onset Pompe disease in a high-risk Brazilian population, using the dried blood spot test to detect GAA deficiency as a main screening tool. Dried blood spots were collected for GAA activity assay from 24 patients with "unexplained" limb-girdle muscular weakness without vacuolar myopathy in their muscle biopsy. Samples with reduced enzyme activity were also investigated for GAA gene mutations. Of the 24 patients with dried blood spots, one patient (4.2%) showed low GAA enzyme activity (NaG/AaGIA: 40.42; %INH: 87.22%). In this patient, genetic analysis confirmed two heterozygous mutations in the GAA gene (c.-32-13T>G/p.Arg854Ter). Our data confirm that clinicians should look for late-onset Pompe disease in patients whose clinical manifestation is an "unexplained" limb-girdle weakness even without vacuolar myopathy in muscle biopsy.

RESUMO A doença de Pompe é uma doença hereditária causada pela deficiência da enzima alfa-glicosidase ácida (GAA). Estudo observacional foi realizado, em um único centro, para determinar a prevalência da doença de Pompe de início tardio (LOPD) em uma população brasileira de alto risco, usando teste em gota seca (DBS) como ferramenta principal de triagem para detectar a deficiência da GAA. DBS foi coletado para avaliar a atividade da GAA em 24 pacientes com fraqueza muscular de cinturas "não explicada" sem miopatia vacuolar na biópsia muscular. As amostras com atividade enzimática reduzida foram também submetidas a análise de mutações no gene GAA. Dos 24 pacientes com DBS, baixa atividade da enzima GAA (NaG/AaGIA: 40.42; %INH: 87.22%) foi encontrada em um paciente (4.2%). Nessa paciente, a análise genética confirmou duas mutações em heterozigose composta no gene GAA (c.-32-13T > G/p.Arg854Ter). Nossos resultados confirmam que LOPD deve ser investigada quando a manifestação clínica é uma fraqueza muscular de cinturas "não explicada", mesmo na ausência de miopatia vacuolar na biópsia muscular.

Humans , Male , Female , Adult , Glycogen Storage Disease Type II/diagnosis , Muscular Dystrophies, Limb-Girdle/diagnosis , Muscular Dystrophies, Limb-Girdle/blood , alpha-Glucosidases/blood , Biopsy , Glycogen Storage Disease Type II/pathology , Glycogen Storage Disease Type II/blood , Prevalence , Muscular Dystrophies, Limb-Girdle/pathology
Vitae (Medellín) ; 25(3): 148-153, 2018. Ilustraciones
Article in English | LILACS, COLNAL | ID: biblio-995065


Background: Momordica charantia is a vine, native to tropics and subtropics that has found use in herbal medicine. In Nigeria, the plant is locally used in the treatment of diabetes. Objective: To investigate the inhibitory effect of terpenoid-rich extract from Momordica charantia on α-glucosidase activity. Method: The inhibitory effect of the terpenoid-rich extract from Momordica charantia on the activity of alpha-glucosidase from Saccharomyces cerevisiae as well as the determination of the mode of inhibition were investigated using in vitro assay methods. Results: The results revealed that the terpenoid-rich extract had a high IC50 of 1.60 mg/mL. The Lineweaver-Burk plot revealed that the extract exhibited partially mixed­type inhibition of α-glucosidase. Conclusions: It can be inferred from this study that although terpenoid-rich extract inhibited α-glucosidase, further purification will be necessary on the extract so as to increase its potency as an inhibitor of α-glucosidase. The action of the extract on α-glucosidase provided an insight into the probable mechanism of action of Momordica charantia in reducing hyperglycemia.

Antecedentes: Momordica charantia es una vid, nativa de las regiones tropicales y subtropicales que ha sido usada en la medicina herbal. En Nigeria, esta planta se ha usado localmente en el tratamiento de la diabetes. Objetivo: Investigar el efecto inhibitorio del extracto rico en terpenoides de Momordica charantia sobre la actividad de la α-glucosidasa. Método: El efecto inhibitorio del extracto rico en terpenoides de Momordica charantia sobre sobre la actividad de la α-glucosidasa y el modo de inhibición se evaluó con un ensayo in vitro. Resultados: Los resultados mostraron que el extracto rico en terpenoides tiene un alto IC50 de 1,60 mg/mL. El gráfico Lineweaver-Burk reveló que el extracto presenta una inhibición combinada de la α-glucosidasa. Conclusión: De este estudio se infiere que aunque el extracto rico en terpenoides inhibió la α-glucosidasa, es necesario realizar una purificación con el fin de incrementar su potencia como inhibidor de la α-glucosidasa. La acción del extracto sobre la α-glucosidasa proporciona un entendimiento del mecanismo de acción probable de Momordica charantia en la reducción de la hiperglicemia.

Humans , Terpenes , Momordica charantia , alpha-Glucosidases , Reactive Inhibition , Hyperglycemia