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Gustavia gracillima Miers. flowers effects on enzymatic targets underlying metabolic disorders and characterization of its polyphenolic content by HPLC-DAD-ESI/MSn

Title
Gustavia gracillima Miers. flowers effects on enzymatic targets underlying metabolic disorders and characterization of its polyphenolic content by HPLC-DAD-ESI/MSn
Type
Article in International Scientific Journal
Year
2020
Authors
Ferreres, F
(Author)
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Gomes, NGM
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Gil Izquierdo, A
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Bapia, S
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Duangsrisai, S
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David M Pereira
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Andrade, PB
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Journal
Vol. 137
ISSN: 0963-9969
Publisher: Elsevier
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Authenticus ID: P-00S-TGS
Abstract (EN): Notwithstanding Gustavia gracillima Miers widespread distribution in neotropical regions, its chemical profile and biological properties remain uninvestigated. A methanol extract obtained from the flowers was characterized through HPLC-DAD-ESI/MSn, nine ellagic acid derivatives and twelve kaempferol 3-O-glycosides being identified and quantitated for the first time at the species and genus. Preliminary cytotoxicity screening did not reveal noticeable effects upon gastrointestinal representative cell lines (AGS, Caco-2 and Hep G2), which further prompted us to evaluate the impact in a series of targets involved in metabolic disorders and associated complications. Despite of the moderate inhibition towards 5-lipoxygense activity, G. gracillima methanol extract displayed significant effects on carbohydrates-hydrolysing enzymes. In contrast with the antidiabetic reference drug acarbose, the extract was able to selectively inhibit yeast alpha-glucosidase activity (IC50 = 4.72 mu g/mL), with negligible inhibitory effects upon alpha-amylase. Kinetic studies pointed to a model of mixed inhibition with a great binding activity, characterized by an inhibitory constant of 2.91 mu g/mL. The notable inhibitory activity was also confirmed in alpha-glucosidase homogenates isolated from human intestinal cells (IC50 = 34.03 mu g/mL). Moreover, the extract obtained from the flowers of G. gracillima displayed significant aldose reductase inhibition (IC50 = 61.88 mu g/mL), as well as O-2(center dot-) and (NO)-N-center dot scavenging properties. A moderate inhibitory effect was also recorded against pancreatic lipase (IC50 = 362.17 mu g/mL) through a mixed inhibition mode. Recorded data supports the potential incorporation of G. gracillima flowers on antidiabetic herbal formulations and/or supplements, with not only straight action on carbohydrates digestion, but also direct interference with targets involved on subsequent diabetes events, such as triglycerides metabolism, inflammation and radical mediated stress.
Language: English
Type (Professor's evaluation): Scientific
No. of pages: 10
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