Triterpene saponins from Barringtonia acutangula (L.) Gaertn as a potent inhibitor of 11β-HSD1 for type 2 diabetes mellitus, obesity, and metabolic syndrome

Patil, Vishal S.; Khatib, N. A.

doi:10.1186/s40816-020-00210-y

Cited by 11 publications

(5 citation statements)

References 17 publications

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“…Other herbal extracts indirectly act on the PPAR pathway through very different biological targets. An extract from Barringtonia acutangula inhibits the 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1); however, this enzyme has been shown to decrease the expression of PPARγ and increase that of PPARα [ 76 ].…”

Section: Resultsmentioning

confidence: 99%

Nutraceuticals and the Network of Obesity Modulators

Ammendola¹,

d’Abusco

2022

Nutrients

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Obesity is considered an increasingly widespread disease in the world population, regardless of age and gender. Genetic but also lifestyle-dependent causes have been identified. Nutrition and physical exercise play an important role, especially in non-genetic obesity. In a three-compartment model, the body is divided into fat mass, fat-free mass and water, and obesity can be considered a condition in which the percentage of total fat mass is in excess. People with a high BMI index or overweight use self-medications, such as food supplements or teas, with the aim to prevent or treat their problem. Unfortunately, there are several obesity modulators that act both on the pathways that promote adipogenesis and those that inhibit lipolysis. Moreover, these pathways involve different tissues and organs, so it is very difficult to identify anti-obesity substances. A network of factors and cells contributes to the accumulation of fat in completely different body districts. The identification of natural anti-obesity agents should consider this network, which we would like to call “obesosome”. The nutrigenomic, nutrigenetic and epigenetic contribute to making the identification of active compounds very difficult. This narrative review aims to highlight nutraceuticals that, in vitro or in vivo, showed an anti-obesity activity or were found to be useful in the control of dysfunctions which are secondary to obesity. The results suggest that it is not possible to use a single compound to treat obesity, but that the studies have to be addressed towards the identification of mixtures of nutraceuticals.

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Section: Resultsmentioning

confidence: 99%

Nutraceuticals and the Network of Obesity Modulators

Ammendola¹,

d’Abusco

2022

Nutrients

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“…Diabetes can result from chronically high levels of glucocorticoids through the enzymatic action of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). Some triterpene saponins isolated from Barringtonia acutangula have shown anti-diabetic activity by interacting with the active site amino acid residues of 11β-HSD1 and targeting other protein molecules involved in insulin insensitivity pathways [ 25 ]. Considerable attention has been given to triterpenes as potential sources for the development of active pharmacological agents.…”

Section: Discussionmentioning

confidence: 99%

Anti-Diabetic Potential of Plant-Based Pentacyclic Triterpene Derivatives: Progress Made to Improve Efficacy and Bioavailability

et al. 2021

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Diabetes mellitus (DM) results from the inability of the pancreas to produce sufficient insulin or weakened cellular response to the insulin produced, which leads to hyperglycemia. Current treatments of DM focus on the use of oral hypoglycemic drugs such as acarbose, alpha-glucose inhibitors, sulphonylureas, thiazolidinediones, and biguanides to control blood glucose levels. However, these medications are known to have various side effects in addition to their bioavailability, efficacy, and safety concerns. These drawbacks have increased interest in the anti-diabetic potential of plant-derived bioactive compounds such as oleanolic and maslinic acids. Although their efficacy in ameliorating blood glucose levels has been reported in several studies, their bioavailability and efficacy remain of concern. The current review examines the anti-diabetic effects of oleanolic, maslinic, asiatic, ursolic, and corosolic acids and their derivatives, as well as the progress made thus far to enhance their bioavailability and efficacy. The literature for the current review was gathered from leading academic databases—including Google Scholar and PubMed—the key words listed below were used. The literature was searched as widely and comprehensively as possible without a defined range of dates.

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“…The edge count was applied to “low values to small sizes” for node size and “low values to bright colors” for node color. The network was designed by utilizing the layout “degree sorted circular layout” [ 53 , 54 , 55 ].…”

Section: Methodsmentioning

confidence: 99%

Hepatitis C Virus NS3/4A Inhibition and Host Immunomodulation by Tannins from Terminalia chebula: A Structural Perspective

Patil¹,

Harish²,

Vetrivel

et al. 2022

Molecules

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Terminalia chebula Retz. forms a key component of traditional folk medicine and is also reported to possess antihepatitis C virus (HCV) and immunomodulatory activities. However, information on the intermolecular interactions of phytochemicals from this plant with HCV and human proteins are yet to be established. Thus, by this current study, we investigated the HCV NS3/4A inhibitory and host immune-modulatory activity of phytocompounds from T. chebula through in silico strategies involving network pharmacology and structural bioinformatics techniques. To start with, the phytochemical dataset of T. chebula was curated from biological databases and the published literature. Further, the target ability of the phytocompounds was predicted using BindingDB for both HCV NS3/4A and other probable host targets involved in the immune system. Further, the identified targets were docked to the phytochemical dataset using AutoDock Vina executed through the POAP pipeline. The resultant docked complexes with significant binding energy were subjected to 50 ns molecular dynamics (MD) simulation in order to infer the stability of complex formation. During network pharmacology analysis, the gene set pathway enrichment of host targets was performed using the STRING and Reactome pathway databases. Further, the biological network among compounds, proteins, and pathways was constructed using Cytoscape 3.6.1. Furthermore, the druglikeness, side effects, and toxicity of the phytocompounds were also predicted using the MolSoft, ADVERpred, and PreADMET methods, respectively. Out of 41 selected compounds, 10 were predicted to target HCV NS3/4A and also to possess druglike and nontoxic properties. Among these 10 molecules, Chebulagic acid and 1,2,3,4,6-Pentagalloyl glucose exhibited potent HCV NS3/4A inhibitory activity, as these scored a lowest binding energy (BE) of −8.6 kcal/mol and −7.7 kcal/mol with 11 and 20 intermolecular interactions with active site residues, respectively. These findings are highly comparable with Asunaprevir (known inhibitor of HCV NS3/4A), which scored a BE of −7.4 kcal/mol with 20 key intermolecular interactions. MD studies also strongly suggest that chebulagic acid and 1,2,3,4,6-Pentagalloyl glucose as promising leads, as these molecules showed stable binding during 50 ns of production run. Further, the gene set enrichment and network analysis of 18 protein targets prioritized 10 compounds and were predicted to potentially modulate the host immune system, hemostasis, cytokine levels, interleukins signaling pathways, and platelet aggregation. On overall analysis, this present study predicts that tannins from T. chebula have a potential HCV NS3/4A inhibitory and host immune-modulatory activity. However, further experimental studies are required to confirm the efficacies.

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Triterpene saponins from Barringtonia acutangula (L.) Gaertn as a potent inhibitor of 11β-HSD1 for type 2 diabetes mellitus, obesity, and metabolic syndrome

Cited by 11 publications

References 17 publications

Nutraceuticals and the Network of Obesity Modulators

Nutraceuticals and the Network of Obesity Modulators

Anti-Diabetic Potential of Plant-Based Pentacyclic Triterpene Derivatives: Progress Made to Improve Efficacy and Bioavailability

Hepatitis C Virus NS3/4A Inhibition and Host Immunomodulation by Tannins from Terminalia chebula: A Structural Perspective

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