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Avens Root (Geum Urbanum L.) Extract Discovered by Target-Based Screening Exhibits Antidiabetic Activity in the Hen’s Egg Test Model and Drosophila melanogaster

Medicinal plant extracts are becoming increasingly important as an alternative for traditional drugs against diabetes mellitus (DM). For this reason, we initialized a target-based screening of 111 root extracts from an open access plant extract library (PECKISH) by ascertaining their in-vitro inhibi...

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Autores principales: Günther, Ilka, Rimbach, Gerald, Nevermann, Sandra, Neuhauser, Cathrina, Stadlbauer, Verena, Schwarzinger, Bettina, Schwarzinger, Clemens, Ipharraguerre, Ignacio R., Weghuber, Julian, Lüersen, Kai
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Frontiers Media S.A. 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8715001/
https://www.ncbi.nlm.nih.gov/pubmed/34975489
http://dx.doi.org/10.3389/fphar.2021.794404
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author Günther, Ilka
Rimbach, Gerald
Nevermann, Sandra
Neuhauser, Cathrina
Stadlbauer, Verena
Schwarzinger, Bettina
Schwarzinger, Clemens
Ipharraguerre, Ignacio R.
Weghuber, Julian
Lüersen, Kai
author_facet Günther, Ilka
Rimbach, Gerald
Nevermann, Sandra
Neuhauser, Cathrina
Stadlbauer, Verena
Schwarzinger, Bettina
Schwarzinger, Clemens
Ipharraguerre, Ignacio R.
Weghuber, Julian
Lüersen, Kai
author_sort Günther, Ilka
collection PubMed
description Medicinal plant extracts are becoming increasingly important as an alternative for traditional drugs against diabetes mellitus (DM). For this reason, we initialized a target-based screening of 111 root extracts from an open access plant extract library (PECKISH) by ascertaining their in-vitro inhibitory efficacy on α-glucosidase. The two most active extracts Geum urbanum L. (roseroot) and Rhodiola rosea L. (avens root) were further tested for their antidiabetic activities in terms of their impact on different regulatory key points of glucose homeostasis. To this end, various enzyme- and cell culture-based in-vitro assays were employed including the determination of sodium-dependent glucose transporter 1 (SGLT1) activity in Caco-2 monolayers by Ussing chambers and of glucose transporter 4 (GLUT4) translocation in a GFP-reporter cell line. Subsequently, the antidiabetic potential of the root extracts were further evaluated in in-vivo models, namely hen’s eggs test and the fruit fly Drosophila melanogaster. Avens root extract was found to be a more potent inhibitor of the enzymes α-glucosidase and dipeptidyl peptidase-4 (DPP4) than roseroot extract. Most importantly, only avens root extract exhibited antidiabetic activity in the two in-vivo models eliciting a reduced blood glucose level in the in-ovo model and a decline of the triglyceride level in a dietary starch-induced D. melanogaster obesity model. Analyses of the polyphenolic composition of the avens root extract by HPLC revealed a high content of ellagic acid and its derivatives as well as ellagitannins such as pedunculagin, stenophyllanin, stachyurin, casuarinin and gemin A. In conclusion, avens root extract represents a promising medicinal plant that should be considered in further in-vivo studies on hyperglycemia in laboratory rodents and humans.
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spelling pubmed-87150012021-12-30 Avens Root (Geum Urbanum L.) Extract Discovered by Target-Based Screening Exhibits Antidiabetic Activity in the Hen’s Egg Test Model and Drosophila melanogaster Günther, Ilka Rimbach, Gerald Nevermann, Sandra Neuhauser, Cathrina Stadlbauer, Verena Schwarzinger, Bettina Schwarzinger, Clemens Ipharraguerre, Ignacio R. Weghuber, Julian Lüersen, Kai Front Pharmacol Pharmacology Medicinal plant extracts are becoming increasingly important as an alternative for traditional drugs against diabetes mellitus (DM). For this reason, we initialized a target-based screening of 111 root extracts from an open access plant extract library (PECKISH) by ascertaining their in-vitro inhibitory efficacy on α-glucosidase. The two most active extracts Geum urbanum L. (roseroot) and Rhodiola rosea L. (avens root) were further tested for their antidiabetic activities in terms of their impact on different regulatory key points of glucose homeostasis. To this end, various enzyme- and cell culture-based in-vitro assays were employed including the determination of sodium-dependent glucose transporter 1 (SGLT1) activity in Caco-2 monolayers by Ussing chambers and of glucose transporter 4 (GLUT4) translocation in a GFP-reporter cell line. Subsequently, the antidiabetic potential of the root extracts were further evaluated in in-vivo models, namely hen’s eggs test and the fruit fly Drosophila melanogaster. Avens root extract was found to be a more potent inhibitor of the enzymes α-glucosidase and dipeptidyl peptidase-4 (DPP4) than roseroot extract. Most importantly, only avens root extract exhibited antidiabetic activity in the two in-vivo models eliciting a reduced blood glucose level in the in-ovo model and a decline of the triglyceride level in a dietary starch-induced D. melanogaster obesity model. Analyses of the polyphenolic composition of the avens root extract by HPLC revealed a high content of ellagic acid and its derivatives as well as ellagitannins such as pedunculagin, stenophyllanin, stachyurin, casuarinin and gemin A. In conclusion, avens root extract represents a promising medicinal plant that should be considered in further in-vivo studies on hyperglycemia in laboratory rodents and humans. Frontiers Media S.A. 2021-12-15 /pmc/articles/PMC8715001/ /pubmed/34975489 http://dx.doi.org/10.3389/fphar.2021.794404 Text en Copyright © 2021 Günther, Rimbach, Nevermann, Neuhauser, Stadlbauer, Schwarzinger, Schwarzinger, Ipharraguerre, Weghuber and Lüersen. https://creativecommons.org/licenses/by/4.0/This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) and the copyright owner(s) are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.
spellingShingle Pharmacology
Günther, Ilka
Rimbach, Gerald
Nevermann, Sandra
Neuhauser, Cathrina
Stadlbauer, Verena
Schwarzinger, Bettina
Schwarzinger, Clemens
Ipharraguerre, Ignacio R.
Weghuber, Julian
Lüersen, Kai
Avens Root (Geum Urbanum L.) Extract Discovered by Target-Based Screening Exhibits Antidiabetic Activity in the Hen’s Egg Test Model and Drosophila melanogaster
title Avens Root (Geum Urbanum L.) Extract Discovered by Target-Based Screening Exhibits Antidiabetic Activity in the Hen’s Egg Test Model and Drosophila melanogaster
title_full Avens Root (Geum Urbanum L.) Extract Discovered by Target-Based Screening Exhibits Antidiabetic Activity in the Hen’s Egg Test Model and Drosophila melanogaster
title_fullStr Avens Root (Geum Urbanum L.) Extract Discovered by Target-Based Screening Exhibits Antidiabetic Activity in the Hen’s Egg Test Model and Drosophila melanogaster
title_full_unstemmed Avens Root (Geum Urbanum L.) Extract Discovered by Target-Based Screening Exhibits Antidiabetic Activity in the Hen’s Egg Test Model and Drosophila melanogaster
title_short Avens Root (Geum Urbanum L.) Extract Discovered by Target-Based Screening Exhibits Antidiabetic Activity in the Hen’s Egg Test Model and Drosophila melanogaster
title_sort avens root (geum urbanum l.) extract discovered by target-based screening exhibits antidiabetic activity in the hen’s egg test model and drosophila melanogaster
topic Pharmacology
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8715001/
https://www.ncbi.nlm.nih.gov/pubmed/34975489
http://dx.doi.org/10.3389/fphar.2021.794404
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