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Erythrocyte Partitioning Profile of Isosteviol in Human and Rat Blood
BACKGROUND: Isosteviol is a synthetic derivative of steviol glycosides with promising pharmacological properties and might find future use as a cardioprotective agent. OBJECTIVE: A simple LC-MS/MS technique was developed and validated for the bioanalysis of isosteviol in plasma and erythrocytes. Thi...
Autores principales: | , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Elsevier
2019
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6658822/ https://www.ncbi.nlm.nih.gov/pubmed/31372188 http://dx.doi.org/10.1016/j.curtheres.2019.06.003 |
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author | Adehin, Ayorinde Tan, Keai Sinn Tan, Wen |
author_facet | Adehin, Ayorinde Tan, Keai Sinn Tan, Wen |
author_sort | Adehin, Ayorinde |
collection | PubMed |
description | BACKGROUND: Isosteviol is a synthetic derivative of steviol glycosides with promising pharmacological properties and might find future use as a cardioprotective agent. OBJECTIVE: A simple LC-MS/MS technique was developed and validated for the bioanalysis of isosteviol in plasma and erythrocytes. This method was subsequently utilized for the in vitro assessment of isosteviol's partitioning into blood compartments of humans and rats. METHODS: Fresh blood samples from healthy humans and Wistar rats were equilibrated with 1, 10, and 30 µM isosteviol at 37 °C in a shaking dry-bath. The levels of isosteviol in plasma and erythrocytes partitions were determined in these samples, after separation, at intervals over a 60-minute period. The data derived was used to estimate erythrocyte-to-plasma and blood-to-plasma coefficients. RESULTS: Mean erythrocyte-to-plasma partition coefficients (SD) after 60 minutes of equilibration were observed to be 0.039 (0.002) and 0.040 (0.003) in humans and rats, respectively. Derived values for the blood-to-plasma ratio (SD) were 0.576 (0.001) in humans and 0.543 (0.007) in rats, whereas plasma component binding was estimated to be more than 96%. CONCLUSIONS: The findings suggest that isosteviol preferentially partitions into plasma compartments in humans and rats. The significance of this profile for the efficacy, tissue uptake, and retention of isosteviol will have to be further studied. |
format | Online Article Text |
id | pubmed-6658822 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2019 |
publisher | Elsevier |
record_format | MEDLINE/PubMed |
spelling | pubmed-66588222019-08-01 Erythrocyte Partitioning Profile of Isosteviol in Human and Rat Blood Adehin, Ayorinde Tan, Keai Sinn Tan, Wen Curr Ther Res Clin Exp Original Research BACKGROUND: Isosteviol is a synthetic derivative of steviol glycosides with promising pharmacological properties and might find future use as a cardioprotective agent. OBJECTIVE: A simple LC-MS/MS technique was developed and validated for the bioanalysis of isosteviol in plasma and erythrocytes. This method was subsequently utilized for the in vitro assessment of isosteviol's partitioning into blood compartments of humans and rats. METHODS: Fresh blood samples from healthy humans and Wistar rats were equilibrated with 1, 10, and 30 µM isosteviol at 37 °C in a shaking dry-bath. The levels of isosteviol in plasma and erythrocytes partitions were determined in these samples, after separation, at intervals over a 60-minute period. The data derived was used to estimate erythrocyte-to-plasma and blood-to-plasma coefficients. RESULTS: Mean erythrocyte-to-plasma partition coefficients (SD) after 60 minutes of equilibration were observed to be 0.039 (0.002) and 0.040 (0.003) in humans and rats, respectively. Derived values for the blood-to-plasma ratio (SD) were 0.576 (0.001) in humans and 0.543 (0.007) in rats, whereas plasma component binding was estimated to be more than 96%. CONCLUSIONS: The findings suggest that isosteviol preferentially partitions into plasma compartments in humans and rats. The significance of this profile for the efficacy, tissue uptake, and retention of isosteviol will have to be further studied. Elsevier 2019-06-22 /pmc/articles/PMC6658822/ /pubmed/31372188 http://dx.doi.org/10.1016/j.curtheres.2019.06.003 Text en © 2019 The Author(s) http://creativecommons.org/licenses/by-nc-nd/4.0/ This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/). |
spellingShingle | Original Research Adehin, Ayorinde Tan, Keai Sinn Tan, Wen Erythrocyte Partitioning Profile of Isosteviol in Human and Rat Blood |
title | Erythrocyte Partitioning Profile of Isosteviol in Human and Rat Blood |
title_full | Erythrocyte Partitioning Profile of Isosteviol in Human and Rat Blood |
title_fullStr | Erythrocyte Partitioning Profile of Isosteviol in Human and Rat Blood |
title_full_unstemmed | Erythrocyte Partitioning Profile of Isosteviol in Human and Rat Blood |
title_short | Erythrocyte Partitioning Profile of Isosteviol in Human and Rat Blood |
title_sort | erythrocyte partitioning profile of isosteviol in human and rat blood |
topic | Original Research |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6658822/ https://www.ncbi.nlm.nih.gov/pubmed/31372188 http://dx.doi.org/10.1016/j.curtheres.2019.06.003 |
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