Absorption, metabolism, degradation and urinary excretion of rosmarinic acid after intake of Perilla frutescens extract in humans

Seigo Baba, Naomi Osakabe, Midori Natsume, Akiko Yasuda, Yuko Muto, Kyoko Hiyoshi, Hirohisa Takano, Toshikazu Yoshikawa, Junji Terao

Research output: Contribution to journalArticle

79 Citations (Scopus)

Abstract

Background: Rosmarinic acid (RA) is a natural polyphenolic substance contained in many Lamiaceae herbs such as Perilla frutescens. Previous studies have shown RA has antioxidative and anti-inflammatory activity. However, little is known on the absorption, metabolism, degradation and excretion of RA. Aim of the study: The aim of this study in healthy humans was to determine the absorption, metabolism, and urinary excretion of RA after a single intake of perilla extract (PE). Method: Six healthy men (mean age 37.2 ± 6.2 y and mean body mass index 22.0 ± 1.9 kg/m2) were enrolled in the study that was a crossover design involving single intakes of PE containing 200 mg RA and placebo with a 10 day interval between treatments. Blood samples were collected before intake and at designated time intervals, while urine samples were collected over the periods 0-6 h, 6-24 h and 24-48 h after intake. RA and its related metabolites in plasma and urine were measured by LC-MS. Results: RA, methylated RA (methyl-RA), caffeic acid (CAA), ferulic acid (FA) and a trace of m-coumaric acid (COA) were detected in the urine after intake of PE. In plasma, RA, methyl-RA and FA were detected, with maximum levels obtained 0.5, 2 and 0.5 h after intake of PE, respectively. The majority of these components in both plasma and urine were present as conjugated forms (glucuronide and/or sulfated). The proportion of RA and its related metabolites excreted in the urine was 6.3 ± 2.2% of the total dose, with approximately 75% of these components being excreted within 6 h after intake of PE. Conclusions: RA contained in PE was absorbed, conjugated and methylated following intake, with a small proportion of RA being degraded into various components, such as conjugated forms of CAA, FA and COA. These metabolites were then rapidly excreted in the urine.

Original languageEnglish
Pages (from-to)1-9
Number of pages9
JournalEuropean Journal of Nutrition
Volume44
Issue number1
DOIs
Publication statusPublished - 2005 Jan
Externally publishedYes

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Perilla frutescens
rosmarinic acid
excretion
Perilla
metabolism
degradation
extracts
urine
ferulic acid
coumaric acids
caffeic acid
metabolites
Lamiaceae
anti-inflammatory activity

Keywords

  • Absorption
  • Human
  • Metabolism
  • Perilla frutescens
  • Rosmarinic acid

ASJC Scopus subject areas

  • Medicine (miscellaneous)
  • Food Science

Cite this

Absorption, metabolism, degradation and urinary excretion of rosmarinic acid after intake of Perilla frutescens extract in humans. / Baba, Seigo; Osakabe, Naomi; Natsume, Midori; Yasuda, Akiko; Muto, Yuko; Hiyoshi, Kyoko; Takano, Hirohisa; Yoshikawa, Toshikazu; Terao, Junji.

In: European Journal of Nutrition, Vol. 44, No. 1, 01.2005, p. 1-9.

Research output: Contribution to journalArticle

Baba, Seigo ; Osakabe, Naomi ; Natsume, Midori ; Yasuda, Akiko ; Muto, Yuko ; Hiyoshi, Kyoko ; Takano, Hirohisa ; Yoshikawa, Toshikazu ; Terao, Junji. / Absorption, metabolism, degradation and urinary excretion of rosmarinic acid after intake of Perilla frutescens extract in humans. In: European Journal of Nutrition. 2005 ; Vol. 44, No. 1. pp. 1-9.
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abstract = "Background: Rosmarinic acid (RA) is a natural polyphenolic substance contained in many Lamiaceae herbs such as Perilla frutescens. Previous studies have shown RA has antioxidative and anti-inflammatory activity. However, little is known on the absorption, metabolism, degradation and excretion of RA. Aim of the study: The aim of this study in healthy humans was to determine the absorption, metabolism, and urinary excretion of RA after a single intake of perilla extract (PE). Method: Six healthy men (mean age 37.2 ± 6.2 y and mean body mass index 22.0 ± 1.9 kg/m2) were enrolled in the study that was a crossover design involving single intakes of PE containing 200 mg RA and placebo with a 10 day interval between treatments. Blood samples were collected before intake and at designated time intervals, while urine samples were collected over the periods 0-6 h, 6-24 h and 24-48 h after intake. RA and its related metabolites in plasma and urine were measured by LC-MS. Results: RA, methylated RA (methyl-RA), caffeic acid (CAA), ferulic acid (FA) and a trace of m-coumaric acid (COA) were detected in the urine after intake of PE. In plasma, RA, methyl-RA and FA were detected, with maximum levels obtained 0.5, 2 and 0.5 h after intake of PE, respectively. The majority of these components in both plasma and urine were present as conjugated forms (glucuronide and/or sulfated). The proportion of RA and its related metabolites excreted in the urine was 6.3 ± 2.2{\%} of the total dose, with approximately 75{\%} of these components being excreted within 6 h after intake of PE. Conclusions: RA contained in PE was absorbed, conjugated and methylated following intake, with a small proportion of RA being degraded into various components, such as conjugated forms of CAA, FA and COA. These metabolites were then rapidly excreted in the urine.",
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T1 - Absorption, metabolism, degradation and urinary excretion of rosmarinic acid after intake of Perilla frutescens extract in humans

AU - Baba, Seigo

AU - Osakabe, Naomi

AU - Natsume, Midori

AU - Yasuda, Akiko

AU - Muto, Yuko

AU - Hiyoshi, Kyoko

AU - Takano, Hirohisa

AU - Yoshikawa, Toshikazu

AU - Terao, Junji

PY - 2005/1

Y1 - 2005/1

N2 - Background: Rosmarinic acid (RA) is a natural polyphenolic substance contained in many Lamiaceae herbs such as Perilla frutescens. Previous studies have shown RA has antioxidative and anti-inflammatory activity. However, little is known on the absorption, metabolism, degradation and excretion of RA. Aim of the study: The aim of this study in healthy humans was to determine the absorption, metabolism, and urinary excretion of RA after a single intake of perilla extract (PE). Method: Six healthy men (mean age 37.2 ± 6.2 y and mean body mass index 22.0 ± 1.9 kg/m2) were enrolled in the study that was a crossover design involving single intakes of PE containing 200 mg RA and placebo with a 10 day interval between treatments. Blood samples were collected before intake and at designated time intervals, while urine samples were collected over the periods 0-6 h, 6-24 h and 24-48 h after intake. RA and its related metabolites in plasma and urine were measured by LC-MS. Results: RA, methylated RA (methyl-RA), caffeic acid (CAA), ferulic acid (FA) and a trace of m-coumaric acid (COA) were detected in the urine after intake of PE. In plasma, RA, methyl-RA and FA were detected, with maximum levels obtained 0.5, 2 and 0.5 h after intake of PE, respectively. The majority of these components in both plasma and urine were present as conjugated forms (glucuronide and/or sulfated). The proportion of RA and its related metabolites excreted in the urine was 6.3 ± 2.2% of the total dose, with approximately 75% of these components being excreted within 6 h after intake of PE. Conclusions: RA contained in PE was absorbed, conjugated and methylated following intake, with a small proportion of RA being degraded into various components, such as conjugated forms of CAA, FA and COA. These metabolites were then rapidly excreted in the urine.

AB - Background: Rosmarinic acid (RA) is a natural polyphenolic substance contained in many Lamiaceae herbs such as Perilla frutescens. Previous studies have shown RA has antioxidative and anti-inflammatory activity. However, little is known on the absorption, metabolism, degradation and excretion of RA. Aim of the study: The aim of this study in healthy humans was to determine the absorption, metabolism, and urinary excretion of RA after a single intake of perilla extract (PE). Method: Six healthy men (mean age 37.2 ± 6.2 y and mean body mass index 22.0 ± 1.9 kg/m2) were enrolled in the study that was a crossover design involving single intakes of PE containing 200 mg RA and placebo with a 10 day interval between treatments. Blood samples were collected before intake and at designated time intervals, while urine samples were collected over the periods 0-6 h, 6-24 h and 24-48 h after intake. RA and its related metabolites in plasma and urine were measured by LC-MS. Results: RA, methylated RA (methyl-RA), caffeic acid (CAA), ferulic acid (FA) and a trace of m-coumaric acid (COA) were detected in the urine after intake of PE. In plasma, RA, methyl-RA and FA were detected, with maximum levels obtained 0.5, 2 and 0.5 h after intake of PE, respectively. The majority of these components in both plasma and urine were present as conjugated forms (glucuronide and/or sulfated). The proportion of RA and its related metabolites excreted in the urine was 6.3 ± 2.2% of the total dose, with approximately 75% of these components being excreted within 6 h after intake of PE. Conclusions: RA contained in PE was absorbed, conjugated and methylated following intake, with a small proportion of RA being degraded into various components, such as conjugated forms of CAA, FA and COA. These metabolites were then rapidly excreted in the urine.

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KW - Metabolism

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KW - Rosmarinic acid

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