Chemo-biological evaluation of antidiabetic activity of Mentha arvensis L. and its role in inhibition of advanced glycation end products

Background: There has been enormous curiosity in the development of alternative plant based medicinesto control diabetes, oxidative stress and related disorders. One of the therapeutic approaches is to reducepostprandial release of glucose in the blood. Two key enzymes that are involved in reducing postprandialglucose are a-amylase and a-glucosidase. Mentha arvensis L. has been traditionally used by several tribesas a medicinal plant to treat various disorders.Objective: The present study was undertaken to test M. arvenisis L. for inhibition of postprandialhyperglycemia.Material and method: We performed various in vitro and in vivo tests to evaluate efficacy of M. arvenisis L.for antidiabetic activity (postprandial hyperglycemia).Results: Methanolic extract of M. arvensis L. leaves showed DPPH free radical scavenging activity (morethan 78% mg/ml) and high antiglycation potential (more than 90% inhibition of AGE formation). Methanolic extract also showed remarkable inhibitory effects on a-amylase (more than 50% mg/ml) and aglucosidase (68% mg/ml) and significant inhibition of postprandial hyperglycemia in starch induced diabetic Wistar rats.Conclusion: The non-insulin dependent antidiabetic or inhibition of postprandial hyperglycemic activityof methanolic extract of M. arvensis L. leaves was shown by using in vitro and in vivo approaches in thepresent study.© 2018 Transdisciplinary University, Bangalore and World Ayurveda Foundation. Publishing Services byElsevier B.V. This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).

Phenolic compounds from Virola venosa (Myristicaceae) and evaluation of their antioxidant and enzyme inhibition potential / Compostos fenólicos de Virola venosa (Myristicaceae) e avaliação de seu potencial antioxidante e de inibição enzimática

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)

Virola venosa, popularmente conhecida como ucuuba-da-mata, ocorre naturalmente na região amazônica e tem potencial para fornecer compostos naturais úteis, como já foi mostrado para outras espécies de Virola. Por isso, o objetivo deste estudo foi determinar a composição química dos extratos do tronco e das folhas de V. venosa e os possíveis potenciais antioxidantes e de inibição contra α-glucosidase de seus compostos. Os extratos polares mostraram-se mais ativos em ambos os testes, portanto, um fracionamento guiado por bioatividade foi realizado para designar os compostos responsáveis pelas atividades registradas. Através da combinação de análise CL-EM/EM e isolamento com identificação por RMN, foram identificados oito compostos fenólicos. Testes com os compostos puros principais das frações mais ativas indicaram o ácido ferúlico como o principal contribuinte das atividades biológicas observadas para os extratos brutos, e, consequentemente, o princípio ativo principal de V. venosa.(AU)

Synthesis of new 2-{2,3-dihydro-1, 4-benzodioxin-6-yl[(4-methylphenyl) sulfonyl]amino}-N-(un/substituted-phenyl)acetamides as α-glucosidase and acetylcholinesterase inhibitors and their in silico study

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.

A New Alkaloid from Bombycis Feculae and Its a-Glucosidase Inhibitory Activity / 中草药·英文版

Objective To study the chemical constituents of Bombycis Feculae. Methods Chemical constituents were isolated BPLC-ELSD. The structures of the isolated compounds were determined by spectral means. Results Two compounds were isolated and identified as 1-deoxynojirimycin (1) and (2R,3R,5R)-2-(hydroxymethyl)piperidine-3,5-diol, named as 1,3-dideoxygalatonojirimycin (2). Conclusion Compound 2 is a new alkaloid. The extract of Bombycis Feculae, compound 1 and compound 2 show inhibitory activities against a-glucosidase.