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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...

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Autores principales: Adehin, Ayorinde, Tan, Keai Sinn, Tan, Wen
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier 2019
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.
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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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