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

• Published in: European journal of nutrition Vol. 44; no. 1; pp. 1 - 9
• Main Authors: Baba, S, Osakabe, N, Natsume, M, Yasuda, A, Muto, Y, Hiyoshi, T, Takano, H, Yoshikawa, T, Terao, J
• Format: Journal Article
• Language: English
• Published: Heidelberg Steinkopff-Verlag 2005; Springer; Springer Nature B.V
• Subjects: absorption; Adult; anti-inflammatory activity; Anti-Inflammatory Agents, Non-Steroidal - metabolism; Antioxidants - metabolism; Biological and medical sciences; Biomarkers - metabolism; blood; body mass index; caffeic acid; Caffeic Acids - metabolism; Catechol O-Methyltransferase - drug effects; Catechol O-Methyltransferase - metabolism; Cinnamates - metabolism; Cinnamates - urine; Coumaric Acids - metabolism; Cross-Over Studies; Depsides; excretion; Feeding. Feeding behavior; ferulic acid; Fundamental and applied biological sciences. Psychology; Gas Chromatography-Mass Spectrometry; herbs; Humans; Male; men; metabolism; metabolites; Methylation - drug effects; Middle Aged; Perilla frutescens; Perilla frutescens - metabolism; placebos; Plant Extracts; Plant Structures; Reference Values; Rosmarinic Acid; Serine Proteinase Inhibitors - metabolism; Serine Proteinase Inhibitors - urine; urine; Vertebrates: anatomy and physiology, studies on body, several organs or systems; Degradation; Human; Urine; Biological fluid; Excretion; Absorption; Nutrition; Extract; Perilla frutescens; rosmarinic acid; Metabolism
• ISSN: 1436-6207; 1436-6215
• DOI: 10.1007/s00394-004-0482-2

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 6h 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.