New In Vitro Studies on the Bioprofile of Genista tenera Antihyperglycemic Extract

doi:10.1007/s13659-015-0077-z

Natural Products and Bioprospecting ›› 2015, Vol. 5 ›› Issue (6): 277-285.DOI: 10.1007/s13659-015-0077-z

• Original article • Previous Articles Next Articles

New In Vitro Studies on the Bioprofile of Genista tenera Antihyperglycemic Extract

Daniela Batista¹, Pedro L.Falé^1,2, Maria L.Serralheiro¹, Maria E.Araújo¹, Paulo J.A.Madeira¹, Carlos Borges¹, Isabel Torgal³, Margarida Goulart³, Jorge Justino³, Alice Martins¹, Amélia P.Rauter¹

1. Centro de Quĺmica e Bioquĺmica, Faculdade de Ciências, Universidade de Lisboa, Campo Grande, 1749-016 Lisbon, Portugal;
2. Institute of Pharmaceutical Science, King's College London, 150 Stamford Street, London SE19 NH, UK;
3. Escola Superior Agrária de Santarém, Quinta do Galinheiro, 2001-904 Santarém, Portugal

Received:2015-09-01 Revised:2015-10-14 Online:2018-02-11 Published:2015-12-24
Supported by:
The authors gratefully acknowledge Funda??o para a Ciência e a Tecnologia for financial support of the projects PTDC/QUI/67165/2006 and PEst-OE/QUI/UI0612/2013. The authors also thank the European Commission for approval of the INOVAFUNAGEING commitment and the support of the project "PER-sonalised ICT supported Service for Independent Living and Active Ageing", FP7-ICT-2013-10, Project Nr. 610359, 2013-2016. The collaboration of the staff from the Herbarium of Jardim Botanico da Madeira, for providing plant material, is also acknowledged.

New In Vitro Studies on the Bioprofile of Genista tenera Antihyperglycemic Extract

Daniela Batista¹, Pedro L. Falé^1,2, Maria L. Serralheiro¹, Maria E. Araújo¹, Paulo J. A. Madeira¹, Carlos Borges¹, Isabel Torgal³, Margarida Goulart³, Jorge Justino³, Alice Martins¹, Amélia P. Rauter¹

1. Centro de Quĺmica e Bioquĺmica, Faculdade de Ciências, Universidade de Lisboa, Campo Grande, 1749-016 Lisbon, Portugal;
2. Institute of Pharmaceutical Science, King's College London, 150 Stamford Street, London SE19 NH, UK;
3. Escola Superior Agrária de Santarém, Quinta do Galinheiro, 2001-904 Santarém, Portugal

通讯作者: Alice Martins,e-mail:aimartins@fc.ul.pt;aprauter@fc.ul.pt
基金资助:
The authors gratefully acknowledge Funda??o para a Ciência e a Tecnologia for financial support of the projects PTDC/QUI/67165/2006 and PEst-OE/QUI/UI0612/2013. The authors also thank the European Commission for approval of the INOVAFUNAGEING commitment and the support of the project "PER-sonalised ICT supported Service for Independent Living and Active Ageing", FP7-ICT-2013-10, Project Nr. 610359, 2013-2016. The collaboration of the staff from the Herbarium of Jardim Botanico da Madeira, for providing plant material, is also acknowledged.

Abstract

Abstract: The inhibition of α-glucosidase and glucose-6-phosphatase, two enzymes involved in the carbohydrate metabolism, is an important target to control glycaemia on individuals with type 2 diabetes. In this work we report for the first time the inhibition of both enzymes by the antihyperglycemic n-butanol extract from Genista tenera(Fabaceae). This extract decreased a-glucosidase and glucose-6-phosphatase activities to 0.97 and 80.25%, respectively, being more effective than acarbose, and phlorizin, the positive controls, which reduced enzymes activities only to 17.39 and 96.06%. Once inflammation and oxidative stress are related to diabetic impairments, the anti-inflammatory activity of the extract was also evaluated, through its inhibitory activity over COX-1 enzyme(47.5% inhibition). Moreover, after induction of oxidative stress by UV radiation, the viability of irradiated rat liver hepatoma cells exposed to the extract was significantly higher(67.82%) than that promoted by ascorbic acid, the positive control(45.05%). In addition, the stability of the extract under gastrointestinal conditions was evaluated by HPLC-DAD-ESI-MS/MS. Flavonoid diglycosides were identified as the main constituents of the extract, and no alterations in the chemical composition nor in the antioxidant activity were observed after in vitro digestion with artificial gastric and pancreatic juices.

Key words: α-Glucosidase inhibition, In vitro digestion, HPLC-DAD-ESI-MS/MS, Antioxidant activity, Flavonoid glycosides

摘要： The inhibition of α-glucosidase and glucose-6-phosphatase, two enzymes involved in the carbohydrate metabolism, is an important target to control glycaemia on individuals with type 2 diabetes. In this work we report for the first time the inhibition of both enzymes by the antihyperglycemic n-butanol extract from Genista tenera(Fabaceae). This extract decreased a-glucosidase and glucose-6-phosphatase activities to 0.97 and 80.25%, respectively, being more effective than acarbose, and phlorizin, the positive controls, which reduced enzymes activities only to 17.39 and 96.06%. Once inflammation and oxidative stress are related to diabetic impairments, the anti-inflammatory activity of the extract was also evaluated, through its inhibitory activity over COX-1 enzyme(47.5% inhibition). Moreover, after induction of oxidative stress by UV radiation, the viability of irradiated rat liver hepatoma cells exposed to the extract was significantly higher(67.82%) than that promoted by ascorbic acid, the positive control(45.05%). In addition, the stability of the extract under gastrointestinal conditions was evaluated by HPLC-DAD-ESI-MS/MS. Flavonoid diglycosides were identified as the main constituents of the extract, and no alterations in the chemical composition nor in the antioxidant activity were observed after in vitro digestion with artificial gastric and pancreatic juices.

关键词: α-Glucosidase inhibition, In vitro digestion, HPLC-DAD-ESI-MS/MS, Antioxidant activity, Flavonoid glycosides

Daniela Batista,Pedro L.Falé,Maria L.Serralheiro,Maria E.Araújo,Paulo J.A.Madeira,Carlos Borges,Isabel Torgal,Margarida Goulart,Jorge Justino,Alice Martins,Amélia P.Rauter. New In Vitro Studies on the Bioprofile of Genista tenera Antihyperglycemic Extract[J]. Natural Products and Bioprospecting, 2015, 5(6): 277-285.

Daniela Batista, Pedro L. Falé, Maria L. Serralheiro, Maria E. Araújo, Paulo J. A. Madeira, Carlos Borges, Isabel Torgal, Margarida Goulart, Jorge Justino, Alice Martins, Amélia P. Rauter. New In Vitro Studies on the Bioprofile of Genista tenera Antihyperglycemic Extract[J]. 应用天然产物, 2015, 5(6): 277-285.

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New In Vitro Studies on the Bioprofile of Genista tenera Antihyperglycemic Extract

New In Vitro Studies on the Bioprofile of Genista tenera Antihyperglycemic Extract

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