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Identification of Potential Plant-Derived Pancreatic Beta-Cell-Directed Agents Using New Custom-Designed Screening Method: Gymnema sylvestre as an Example

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Title: Identification of Potential Plant-Derived Pancreatic Beta-Cell-Directed Agents Using New Custom-Designed Screening Method: Gymnema sylvestre as an Example
Authors: Altaf Al-Romaiyan, Shanta J. Persaud, Peter M. Jones
Source: Molecules, Vol 29, Iss 1, p 194 (2023)
Publisher Information: MDPI AG, 2023.
Publication Year: 2023
Collection: LCC:Organic chemistry
Subject Terms: diabetes, screening, plant-derived therapies, beta-cell function, insulin, apoptosis, Organic chemistry, QD241-441
More Details: Background: Folk medicines are attractive therapeutic agents for treating type 2 diabetes mellitus (T2DM). Most plant extracts that have been suggested to restore β-cells function were tested in vivo. Some only have been tested in vitro to determine whether they have a direct effect on β-cells islets of Langerhans. Currently, there are no defined criteria for screening of β-cell-directed plant-based remedies as potential antidiabetic agents. Summary: In this review, we have identified certain criteria/characteristics that can be used to generate a “screening portfolio” to identify plant extracts as potential β-cell-directed agents for the treatment of T2DM. To validate our screening method, we studied the potential therapeutic efficacy of a Gymnema sylvestre (GS) extract using the screening criteria detailed in the review. Six criteria have been identified and validated using OSA®, a GS extract. By using this screening method, we show that OSA® fulfilled most of the criteria identified for an effective β-cell-directed antidiabetic therapy, being an effective insulin-releasing agent at nontoxic concentrations; maintaining β-cell insulin content by stimulating a concomitant increase in insulin gene transcription; maintaining β-cell mass by protecting against apoptosis; and being effective at maintaining normoglycemia in vivo in a mouse model and a human cohort with T2DM. Key messages: The present review has highlighted the importance of having a screening portfolio for plant extracts that have potential antidiabetic effects in the treatment of T2DM. We propose that this screening method should be adopted for future studies to identify new β-cell-directed antidiabetic plant derived agents.
Document Type: article
File Description: electronic resource
Language: English
ISSN: 1420-3049
Relation: https://www.mdpi.com/1420-3049/29/1/194; https://doaj.org/toc/1420-3049
DOI: 10.3390/molecules29010194
Access URL: https://doaj.org/article/018778f4e32d426fa38b3b3641573b7a
Accession Number: edsdoj.018778f4e32d426fa38b3b3641573b7a
Database: Directory of Open Access Journals
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  Data: Identification of Potential Plant-Derived Pancreatic Beta-Cell-Directed Agents Using New Custom-Designed Screening Method: Gymnema sylvestre as an Example
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  Data: Molecules, Vol 29, Iss 1, p 194 (2023)
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  Data: MDPI AG, 2023.
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  Data: <searchLink fieldCode="DE" term="%22diabetes%22">diabetes</searchLink><br /><searchLink fieldCode="DE" term="%22screening%22">screening</searchLink><br /><searchLink fieldCode="DE" term="%22plant-derived+therapies%22">plant-derived therapies</searchLink><br /><searchLink fieldCode="DE" term="%22beta-cell+function%22">beta-cell function</searchLink><br /><searchLink fieldCode="DE" term="%22insulin%22">insulin</searchLink><br /><searchLink fieldCode="DE" term="%22apoptosis%22">apoptosis</searchLink><br /><searchLink fieldCode="DE" term="%22Organic+chemistry%22">Organic chemistry</searchLink><br /><searchLink fieldCode="DE" term="%22QD241-441%22">QD241-441</searchLink>
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  Data: Background: Folk medicines are attractive therapeutic agents for treating type 2 diabetes mellitus (T2DM). Most plant extracts that have been suggested to restore β-cells function were tested in vivo. Some only have been tested in vitro to determine whether they have a direct effect on β-cells islets of Langerhans. Currently, there are no defined criteria for screening of β-cell-directed plant-based remedies as potential antidiabetic agents. Summary: In this review, we have identified certain criteria/characteristics that can be used to generate a “screening portfolio” to identify plant extracts as potential β-cell-directed agents for the treatment of T2DM. To validate our screening method, we studied the potential therapeutic efficacy of a Gymnema sylvestre (GS) extract using the screening criteria detailed in the review. Six criteria have been identified and validated using OSA®, a GS extract. By using this screening method, we show that OSA® fulfilled most of the criteria identified for an effective β-cell-directed antidiabetic therapy, being an effective insulin-releasing agent at nontoxic concentrations; maintaining β-cell insulin content by stimulating a concomitant increase in insulin gene transcription; maintaining β-cell mass by protecting against apoptosis; and being effective at maintaining normoglycemia in vivo in a mouse model and a human cohort with T2DM. Key messages: The present review has highlighted the importance of having a screening portfolio for plant extracts that have potential antidiabetic effects in the treatment of T2DM. We propose that this screening method should be adopted for future studies to identify new β-cell-directed antidiabetic plant derived agents.
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