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In Vitro and in Vivo Metabolism of Verproside in Rats

Verproside, a catalpol derivative iridoid glycoside isolated from Pseudolysimachion rotundum var. subintegrum, is a biologically active compound with anti-inflammatory, antinociceptic, antioxidant, and anti-asthmatic properties. Twenty-one metabolites were identified in bile and urine samples obtain...

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Autores principales: Kim, Min Gi, Hwang, Deok-Kyu, Jeong, Hyeon-Uk, Ji, Hye Young, Oh, Sei-Ryang, Lee, Yongnam, Yoo, Ji Seok, Shin, Dae Hee, Lee, Hye Suk
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2012
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6268120/
https://www.ncbi.nlm.nih.gov/pubmed/23085650
http://dx.doi.org/10.3390/molecules171011990
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author Kim, Min Gi
Hwang, Deok-Kyu
Jeong, Hyeon-Uk
Ji, Hye Young
Oh, Sei-Ryang
Lee, Yongnam
Yoo, Ji Seok
Shin, Dae Hee
Lee, Hye Suk
author_facet Kim, Min Gi
Hwang, Deok-Kyu
Jeong, Hyeon-Uk
Ji, Hye Young
Oh, Sei-Ryang
Lee, Yongnam
Yoo, Ji Seok
Shin, Dae Hee
Lee, Hye Suk
author_sort Kim, Min Gi
collection PubMed
description Verproside, a catalpol derivative iridoid glycoside isolated from Pseudolysimachion rotundum var. subintegrum, is a biologically active compound with anti-inflammatory, antinociceptic, antioxidant, and anti-asthmatic properties. Twenty-one metabolites were identified in bile and urine samples obtained after intravenous administration of verproside in rats using liquid chromatography-quadrupole Orbitrap mass spectrometry. Verproside was metabolized by O-methylation, glucuronidation, sulfation, and hydrolysis to verproside glucuronides (M1 and M2), verproside sulfates (M3 and M4), picroside II (M5), M5 glucuronide (M7), M5 sulfate (M9), isovanilloylcatalpol (M6), M6 glucuronide (M8), M6 sulfate (M10), 3,4-dihydroxybenzoic acid (M11), M11 glucuronide (M12), M11 sulfates (M13 and M14), 3-methyoxy-4-hydroxybenzoic acid (M15), M15 glucuronides (M17 and M18), M15 sulfate (M20), 3-hydroxy-4-methoxybenzoic acid (M16), M16 glucuronide (M19), and M16 sulfate (M21). Incubation of verproside with rat hepatocytes resulted in thirteen metabolites (M1–M11, M13, and M14). Verproside sulfate, M4 was a major metabolite in rat hepatocytes. After intravenous administration of verproside, the drug was recovered in bile (0.77% of dose) and urine (4.48% of dose), and O-methylation of verproside to picroside II (M5) and isovanilloylcatalpol (M6) followed by glucuronidation and sulfation was identified as major metabolic pathways compared to glucuronidation and sulfation of verproside in rats.
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spelling pubmed-62681202018-12-12 In Vitro and in Vivo Metabolism of Verproside in Rats Kim, Min Gi Hwang, Deok-Kyu Jeong, Hyeon-Uk Ji, Hye Young Oh, Sei-Ryang Lee, Yongnam Yoo, Ji Seok Shin, Dae Hee Lee, Hye Suk Molecules Article Verproside, a catalpol derivative iridoid glycoside isolated from Pseudolysimachion rotundum var. subintegrum, is a biologically active compound with anti-inflammatory, antinociceptic, antioxidant, and anti-asthmatic properties. Twenty-one metabolites were identified in bile and urine samples obtained after intravenous administration of verproside in rats using liquid chromatography-quadrupole Orbitrap mass spectrometry. Verproside was metabolized by O-methylation, glucuronidation, sulfation, and hydrolysis to verproside glucuronides (M1 and M2), verproside sulfates (M3 and M4), picroside II (M5), M5 glucuronide (M7), M5 sulfate (M9), isovanilloylcatalpol (M6), M6 glucuronide (M8), M6 sulfate (M10), 3,4-dihydroxybenzoic acid (M11), M11 glucuronide (M12), M11 sulfates (M13 and M14), 3-methyoxy-4-hydroxybenzoic acid (M15), M15 glucuronides (M17 and M18), M15 sulfate (M20), 3-hydroxy-4-methoxybenzoic acid (M16), M16 glucuronide (M19), and M16 sulfate (M21). Incubation of verproside with rat hepatocytes resulted in thirteen metabolites (M1–M11, M13, and M14). Verproside sulfate, M4 was a major metabolite in rat hepatocytes. After intravenous administration of verproside, the drug was recovered in bile (0.77% of dose) and urine (4.48% of dose), and O-methylation of verproside to picroside II (M5) and isovanilloylcatalpol (M6) followed by glucuronidation and sulfation was identified as major metabolic pathways compared to glucuronidation and sulfation of verproside in rats. MDPI 2012-10-12 /pmc/articles/PMC6268120/ /pubmed/23085650 http://dx.doi.org/10.3390/molecules171011990 Text en © 2012 by the authors; licensee MDPI, Basel, Switzerland. http://creativecommons.org/licenses/by/3.0/ This article is an open-access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/).
spellingShingle Article
Kim, Min Gi
Hwang, Deok-Kyu
Jeong, Hyeon-Uk
Ji, Hye Young
Oh, Sei-Ryang
Lee, Yongnam
Yoo, Ji Seok
Shin, Dae Hee
Lee, Hye Suk
In Vitro and in Vivo Metabolism of Verproside in Rats
title In Vitro and in Vivo Metabolism of Verproside in Rats
title_full In Vitro and in Vivo Metabolism of Verproside in Rats
title_fullStr In Vitro and in Vivo Metabolism of Verproside in Rats
title_full_unstemmed In Vitro and in Vivo Metabolism of Verproside in Rats
title_short In Vitro and in Vivo Metabolism of Verproside in Rats
title_sort in vitro and in vivo metabolism of verproside in rats
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6268120/
https://www.ncbi.nlm.nih.gov/pubmed/23085650
http://dx.doi.org/10.3390/molecules171011990
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