In vitro and in silico Studies of Mangiferin from Aphloia theiformis on Key Enzymes Linked to Diabetes Type 2 and Associated Complications

Picot, Marie Carene Nancy; Zengin, Gökhan; Mollica, Adriano; Stefanucci, Azzurra; Carradori, Simone; Mahomoodally, Mohamad Fawzi

doi:10.2174/1573406413666170307163929

Cited by 45 publications

(15 citation statements)

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“…The results showed that mangiferin bonds to both allosteric and orthosteric sites by p-p interactions. In addition, the difference in the fitness value found for the docking at the allosteric site (68.11) with that in the orthosteric site (59.11) is in agreement with a noncompetitive type of inhibition [92].…”

Section: Compsupporting

confidence: 57%

A comprehensive review on xanthone derivatives as α-glucosidase inhibitors

Santos

Freitas

Fernandes

2018

European Journal of Medicinal Chemistry

162

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a-Glucosidase plays an important role in carbohydrate metabolism and is therefore an attractive therapeutic target for the treatment of diabetes, obesity and other related complications. In the last two decades, considerable interest has been given to natural and synthetic xanthone derivatives in this field of research. Herein, a comprehensive review of the literature on xanthones as inhibitors of a-glucosidase activity, their mechanism of action, experimental procedures and structure-activity relationships have been reviewed for more than 280 analogs. With this overview we intend to motivate and challenge researchers (e.g. chemistry, biology, pharmaceutical and medicinal areas) for the design of novel xanthones as multipotent drugs and exploit the properties of this class of compounds in the management of diabetic complications.

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Section: Compsupporting

confidence: 57%

A comprehensive review on xanthone derivatives as α-glucosidase inhibitors

Santos

Freitas

Fernandes

2018

European Journal of Medicinal Chemistry

162

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“…The observed enzyme inhibitory activity of B. speciosa stem bark methanol extract might be related to more than one phytochemical that is present in the extracts. Interestingly, molecular docking studies have previously shown that mangiferin effectively binds to acetylcholinesterase and butyrylcholinesterase [45]. Ferulic acid was reported to hybridise with quinoline in a competitive manner.…”

Section: Resultsmentioning

confidence: 99%

Bridelia speciosa Müll.Arg. Stem bark Extracts as a Potential Biomedicine: From Tropical Western Africa to the Pharmacy Shelf

et al. 2020

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Bridelia species have been used in traditional African medicine for the management of diverse human ailments. In the current work, the detailed phytochemical profiles of the extracts of the stem bark of B. speciosa were evaluated and the antioxidant and enzyme inhibitory properties of the extracts were assessed. The anti-bacterial and anti-mycotic effects of the extracts were evaluated against selected pathogen strains. Additionally, the anti-proliferative effects were studied on the liver cancer HepG2 cell line. Finally, the putative protective effects were assessed on isolated rat liver that was challenged with lipopolysaccharide (LPS). The results revealed the presence of 36 compounds in the ethyl acetate extract, 44 in the methanol extract, and 38 in the water extract. Overall, the methanol extract showed the highest antioxidant activity, particularly in LPS-stimulated rat liver. Additionally, this extract exerted the highest antimycotic effect on C. albicans, whereas the water extract showed a promising anti-proliferative effect on liver cancer HepG2 cells. The methanol extract was also the most active as enzyme inhibitor, against acetylcholinesterase and butyrylcholinesterase. The current study appraises the antioxidant and enzyme inhibition properties of B. speciosa methanol extract and showed that this specie could be a promising source of biologically active phytochemicals, with potential health uses. Supplementary Materials: The following are available online at http://www.mdpi.com/2076-3921/9/2/128/s1. Supplementary Materials and Methods; CFF-strains. Author Contributions: Conceptualization, C.F. and G.Z.; methodology, G.O.; L.M.; software, L.M.; validation,: C.F.; G.Z.; L.M.; G.O.; formal analysis, C.F.; G.Z.; investigation, K.I.S.; K.B.; S.L.; L.R.; A.C. (Annalisa Chiavaroli); S.V.; P.A.; V.H.; S.C.; R.V.; L.D.L.; A.C. (Alessandro Cama); M.C.N.P.-A.; Z.C.; J.J.; M.F.M.; resources, C.F.; G.O.; L.M.; data curation, C.F.; G.Z.; writing-original draft preparation, M.F.M.; writing-review and editing, C.F., G.Z.; G.O.; L.M.; visualization, L.B.; supervision, L.B.; project administration, C.F.; L.M.; G.O.; G.Z.; funding acquisition, C.F.; G.O.; L.M. All authors have read and agreed to the published version of the manuscript.

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“…Natural bioactive compounds from plants extracts, either as pure compounds or as standardized extracts, are of increasing interest for their versatile applications in pharmaceutical, nutraceutical and cosmetic industry. For this purpose, specific extraction techniques are essentially required to ensure isolation of specific bioactive constituents, to optimize the concentration of known constituents and also to maintain their biological activities …”

Section: Introductionmentioning

confidence: 99%

“…For this purpose, specific extraction techniques are essentially required to ensure isolation of specific bioactive constituents, to optimize the concentration of known constituents and also to maintain their biological activities. [2][3][4] Extraction is one of the most important steps in the flowchart of phytochemical studies to obtain bioactive components. The choice of a suitable extraction method (with solvents and standardized process) are required for extraction of desirable constituents.…”

Section: Introductionmentioning

confidence: 99%

Innovative perspectives on Pulicaria dysenterica extracts: phyto‐pharmaceutical properties, chemical characterization and multivariate analysis

et al. 2019

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BACKGROUND In this study, we aimed to evaluate the influence of different extraction procedures [decoction, homogenizer‐assisted extraction (HAE), infusion, maceration, Soxhlet and ultrasound‐assisted extraction (UAE)] on the chemical profiling and biological properties of methanol and water extracts of Pulicaria dysenterica (L.) Bernh. The chemical profiles of the extracts were evaluated by high‐performance liquid chromatography coupled to electrospray ionization and time‐of‐flight mass spectrometry (HPLC‐ESI‐TOF‐MS). The antioxidant properties and enzymes (lipase, α‐amylase, α‐glucosidase, tyrosinase and cholinesterases) inhibitory potential of the extracts were evaluated. RESULTS The chemical profiles were dependent on the type of extraction methods as well as on the type of solvent. The methanolic extracts showed higher levels of total phenolic, flavonoid, and phenolic acid content, while the highest total flavonol content was observed in the HAE–water extract. Forty different compounds were identified from P. dysenterica. In relation to the potential in vitro anti‐diabetic effects, the highest activity against the studied key enzymes was observed for the macerated extract (α‐amylase: 0.58 ± 0.03 and α‐ glucosidase: 1.65 ± 0.03 mmol ACAE g−1). The HAE–methanol extract was the most potent inhibitor of cholisterases, whereas the highest activities against tyrosinase were observed for UAE–methanol extract, followed by macerated and Soxhlet. The inhibitory activity of the studied extracts against lipase were in the order: soxhlet > macerated> HAE–methanol > UAE–methanol. CONCLUSION This study has established scientific baseline data on the therapeutic properties of P. dysentrica, thereby advocating the need for further investigations in an endeavour to develop novel pharmaceuticals from this plant. © 2019 Society of Chemical Industry

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In vitro and in silico Studies of Mangiferin from Aphloia theiformis on Key Enzymes Linked to Diabetes Type 2 and Associated Complications

Abstract: This study provided an insight of the molecular interaction of mangiferin with the studied enzymes and can be considered as a valuable tool for designing new drugs for better management of these diseases.

Cited by 45 publications

References 0 publications

A comprehensive review on xanthone derivatives as α-glucosidase inhibitors

A comprehensive review on xanthone derivatives as α-glucosidase inhibitors

Bridelia speciosa Müll.Arg. Stem bark Extracts as a Potential Biomedicine: From Tropical Western Africa to the Pharmacy Shelf

Innovative perspectives on Pulicaria dysenterica extracts: phyto‐pharmaceutical properties, chemical characterization and multivariate analysis

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