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Polyphenol-rich extract and fractions of Terminalia phaeocarpa Eichler possess hypoglycemic effect, reduce the release of cytokines, and inhibit lipase, α-glucosidase, and α-amilase enzymes.
J Ethnopharmacol. 2021 May 10; 271:113847.JE

Abstract

ETHNOPHARMACOLOGICAL RELEVANCE

species of Terminalia (Combretaceae) are used to treat diabetes and metabolic disorders in Asia, Africa, and America. Terminalia phaeocarpa Eichler is an endemic tree from Brazil, popularly known as capitão. This species is closely related to Terminalia argentea Mart., also vulgarly known as capitão, a native but not endemic tree. Due to their phenotype similarity, these species might eventually prove inseparable and they are indistinctly used by locals to treat diabetes, among other diseases. The potential antidiabetic effect of T. argentea has been previously reported, whereas the biological effects and chemical composition of T. phaeocarpa have never been addressed so far.

AIM OF THE STUDY

investigate the hypoglycaemic effect of an ethanol extract (EE) of T. phaeocarpa leaves and its ethyl acetate (FrEtOAc) and hydromethanolic (FrMEOH) fractions, in addition to their activity on the release of pro-inflammatory mediators and inhibition of lipase, α-amylase, and α-glucosidase enzymes. Additionally, it aimed to characterize the chemical composition of the extract and fractions, seeking to identify the compounds related to the biological activities.

MATERIALS AND METHODS

The effect on the release of TNF-α, IL-1β, and CCL-2 was evaluated in LPS-stimulated THP-1 cells (ATCC TIB-202). The inhibition of lipase, α-amylase, and α-glucosidase was tested in vitro, whereas the hypoglycemic effect was assayed in the oral starch tolerance test. The chemical composition was investigated by extensive UHPLC-DAD-ESI-MS/MS analyses.

RESULTS

The extract and derived fractions reduced TNF-α (EE pIC50 = 4.58 ± 0.01; FrEtOAc pIC50 = 4.69 ± 0.01; FrMeOH pIC50 = 4.54 ± 0.02) and IL-1β (EE pIC50 = 4.86 ± 0.02; FrEtOAc pIC50 = 4.86 ± 0.02; FrMeOH pIC50 = 4.75 ± 0.01) release by LPS-stimulated THP-1 cells in a concentration-dependent manner, whereas the inhibitory effect on CCL-2 release did not reach a clear linear relationship for the tested concentrations. The extract and fractions also inhibited in vitro the activity of lipase (EE pIC50 = 3.97 ± 0.12; FrEtOAc pIC50 = 3.87 ± 0.04; FrMeOH pIC50 = 3.67 ± 0.14), α-amylase (EE pIC50 = 4.46 ± 0.27; FrEtOAc pIC50 = 5.47 ± 0.27; FrMeOH pIC50 = 4.26 ± 0.22), and α-glucosidase (EE pIC50 = 5.46 ± 0.05; FrEtOAc pIC50 = 5.79 ± 0.11; FrMeOH pIC50 = 5.74 ± 0.05). The pIC50 values of the test samples were lower than those obtained with orlistat (7.59 ± 0.08) and acarbose (6.04 ± 0.37 and 7.63 ± 0.04) employed as the positive controls respectively in the lipase, α-amylase, and α-glucosidase assays. When assayed in the oral starch tolerance test, the extract and fractions also reduced animal glycaemia. UHPLC-DAD-ESI-MS/MS analyses of the extract and fractions led to the identification of 38 phenolic compounds, mainly phenolic acids, ellagitannins and flavonoids, among others, all of them first-time described for the species.

CONCLUSION

Based on our findings, T. phaeocarpa has hypoglycaemic activity and polyphenols are the probable bioactive compounds, which support the ethnomedical use of the species.

Authors+Show Affiliations

Department of Pharmaceutical Products, Faculty of Pharmacy, Universidade Federal de Minas Gerais, Av. Antônio Carlos, 6627, Belo Horizonte, Brazil.Department of Pharmacology, Institute of Biological Sciences, Universidade Federal de Minas Gerais, Av. Antônio Carlos, 6627, Belo Horizonte, Brazil.Department of Pharmaceutical Products, Faculty of Pharmacy, Universidade Federal de Minas Gerais, Av. Antônio Carlos, 6627, Belo Horizonte, Brazil.Department of Botany, Institute of Biological Sciences, Universidade Federal de Minas Gerais, Av. Antônio Carlos, 6627, Belo Horizonte, Brazil.Department of Pharmaceutical Products, Faculty of Pharmacy, Universidade Federal de Minas Gerais, Av. Antônio Carlos, 6627, Belo Horizonte, Brazil.Department of Pharmacology, Institute of Biological Sciences, Universidade Federal de Minas Gerais, Av. Antônio Carlos, 6627, Belo Horizonte, Brazil.Department of Pharmaceutical Products, Faculty of Pharmacy, Universidade Federal de Minas Gerais, Av. Antônio Carlos, 6627, Belo Horizonte, Brazil. Electronic address: fernaobraga@farmacia.ufmg.br.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

33515684

Citation

Gomes, José Hugo de Sousa, et al. "Polyphenol-rich Extract and Fractions of Terminalia Phaeocarpa Eichler Possess Hypoglycemic Effect, Reduce the Release of Cytokines, and Inhibit Lipase, Α-glucosidase, and Α-amilase Enzymes." Journal of Ethnopharmacology, vol. 271, 2021, p. 113847.
Gomes JHS, Mbiakop UC, Oliveira RL, et al. Polyphenol-rich extract and fractions of Terminalia phaeocarpa Eichler possess hypoglycemic effect, reduce the release of cytokines, and inhibit lipase, α-glucosidase, and α-amilase enzymes. J Ethnopharmacol. 2021;271:113847.
Gomes, J. H. S., Mbiakop, U. C., Oliveira, R. L., Stehmann, J. R., Pádua, R. M., Cortes, S. F., & Braga, F. C. (2021). Polyphenol-rich extract and fractions of Terminalia phaeocarpa Eichler possess hypoglycemic effect, reduce the release of cytokines, and inhibit lipase, α-glucosidase, and α-amilase enzymes. Journal of Ethnopharmacology, 271, 113847. https://doi.org/10.1016/j.jep.2021.113847
Gomes JHS, et al. Polyphenol-rich Extract and Fractions of Terminalia Phaeocarpa Eichler Possess Hypoglycemic Effect, Reduce the Release of Cytokines, and Inhibit Lipase, Α-glucosidase, and Α-amilase Enzymes. J Ethnopharmacol. 2021 May 10;271:113847. PubMed PMID: 33515684.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Polyphenol-rich extract and fractions of Terminalia phaeocarpa Eichler possess hypoglycemic effect, reduce the release of cytokines, and inhibit lipase, α-glucosidase, and α-amilase enzymes. AU - Gomes,José Hugo de Sousa, AU - Mbiakop,Ulrich Carlos, AU - Oliveira,Renata Leite, AU - Stehmann,João Renato, AU - Pádua,Rodrigo Maia de, AU - Cortes,Steyner F, AU - Braga,Fernão Castro, Y1 - 2021/01/27/ PY - 2020/10/28/received PY - 2021/01/08/revised PY - 2021/01/15/accepted PY - 2021/1/31/pubmed PY - 2021/8/17/medline PY - 2021/1/30/entrez KW - Hypoglycaemic activity KW - In vitro assays KW - Oral starch tolerance test KW - Phenolics KW - Terminalia phaeocarpa KW - UHPLC-DAD-ESI-MS/MS analyses SP - 113847 EP - 113847 JF - Journal of ethnopharmacology JO - J Ethnopharmacol VL - 271 N2 - ETHNOPHARMACOLOGICAL RELEVANCE: species of Terminalia (Combretaceae) are used to treat diabetes and metabolic disorders in Asia, Africa, and America. Terminalia phaeocarpa Eichler is an endemic tree from Brazil, popularly known as capitão. This species is closely related to Terminalia argentea Mart., also vulgarly known as capitão, a native but not endemic tree. Due to their phenotype similarity, these species might eventually prove inseparable and they are indistinctly used by locals to treat diabetes, among other diseases. The potential antidiabetic effect of T. argentea has been previously reported, whereas the biological effects and chemical composition of T. phaeocarpa have never been addressed so far. AIM OF THE STUDY: investigate the hypoglycaemic effect of an ethanol extract (EE) of T. phaeocarpa leaves and its ethyl acetate (FrEtOAc) and hydromethanolic (FrMEOH) fractions, in addition to their activity on the release of pro-inflammatory mediators and inhibition of lipase, α-amylase, and α-glucosidase enzymes. Additionally, it aimed to characterize the chemical composition of the extract and fractions, seeking to identify the compounds related to the biological activities. MATERIALS AND METHODS: The effect on the release of TNF-α, IL-1β, and CCL-2 was evaluated in LPS-stimulated THP-1 cells (ATCC TIB-202). The inhibition of lipase, α-amylase, and α-glucosidase was tested in vitro, whereas the hypoglycemic effect was assayed in the oral starch tolerance test. The chemical composition was investigated by extensive UHPLC-DAD-ESI-MS/MS analyses. RESULTS: The extract and derived fractions reduced TNF-α (EE pIC50 = 4.58 ± 0.01; FrEtOAc pIC50 = 4.69 ± 0.01; FrMeOH pIC50 = 4.54 ± 0.02) and IL-1β (EE pIC50 = 4.86 ± 0.02; FrEtOAc pIC50 = 4.86 ± 0.02; FrMeOH pIC50 = 4.75 ± 0.01) release by LPS-stimulated THP-1 cells in a concentration-dependent manner, whereas the inhibitory effect on CCL-2 release did not reach a clear linear relationship for the tested concentrations. The extract and fractions also inhibited in vitro the activity of lipase (EE pIC50 = 3.97 ± 0.12; FrEtOAc pIC50 = 3.87 ± 0.04; FrMeOH pIC50 = 3.67 ± 0.14), α-amylase (EE pIC50 = 4.46 ± 0.27; FrEtOAc pIC50 = 5.47 ± 0.27; FrMeOH pIC50 = 4.26 ± 0.22), and α-glucosidase (EE pIC50 = 5.46 ± 0.05; FrEtOAc pIC50 = 5.79 ± 0.11; FrMeOH pIC50 = 5.74 ± 0.05). The pIC50 values of the test samples were lower than those obtained with orlistat (7.59 ± 0.08) and acarbose (6.04 ± 0.37 and 7.63 ± 0.04) employed as the positive controls respectively in the lipase, α-amylase, and α-glucosidase assays. When assayed in the oral starch tolerance test, the extract and fractions also reduced animal glycaemia. UHPLC-DAD-ESI-MS/MS analyses of the extract and fractions led to the identification of 38 phenolic compounds, mainly phenolic acids, ellagitannins and flavonoids, among others, all of them first-time described for the species. CONCLUSION: Based on our findings, T. phaeocarpa has hypoglycaemic activity and polyphenols are the probable bioactive compounds, which support the ethnomedical use of the species. SN - 1872-7573 UR - https://www.unboundmedicine.com/medline/citation/33515684/Polyphenol_rich_extract_and_fractions_of_Terminalia_phaeocarpa_Eichler_possess_hypoglycemic_effect_reduce_the_release_of_cytokines_and_inhibit_lipase_α_glucosidase_and_α_amilase_enzymes_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0378-8741(21)00073-8 DB - PRIME DP - Unbound Medicine ER -