The urine of rats administered rosmarinic acid (7) orally contained se
ven metabolites, which were identified as trans-caffeic acid 4-O-sulfa
te (1), trans-m-coumaric acid 3-O-sulfate (2), transferulic acid 4-O-s
ulfate (3), trans-caffeic acid (4), m-hydroxyphenylpropionic acid (5),
trans-m-coumaric acid (6), and unchanged rosmarinic acid (7) by spect
roscopic and chemical data. The total cumulative amount of 1-7 excrete
d in the urine 48 h after the oral administration of rosmarinic acid w
as approximately 31.8% of the dose administered. On the other hand, th
e metabolites attributed to rosmarinic acid could not be found in the
bile. Orally administered rosmarinic acid may thus be concluded to be
excreted in the urine rather than in the bile, with cleavage of eater
bonds, selective para-dehydroxylation, methylation, and sulfate-conjug
ation. Metabolites 2, 3, 5, and 6 were also detected in the plasma.