Orally Administered Delphinidin 3-Rutinoside and Cyanidin 3-Rutinoside Are Directly Absorbed in Rats and Humans and Appear in the Blood as the Intact Forms

• Published in: Journal of agricultural and food chemistry Vol. 49; no. 3; pp. 1546 - 1551
• Main Authors: Matsumoto, Hitoshi, Inaba, Hiromi, Kishi, Mitsuo, Tominaga, Shigeru, Hirayama, Masao, Tsuda, Takanori
• Format: Journal Article
• Language: English
• Published: Washington, DC American Chemical Society 01.03.2001
• Subjects: Administration, Oral; Adult; Animals; Anthocyanins - administration & dosage; Anthocyanins - blood; Anthocyanins - pharmacokinetics; Biological and medical sciences; General pharmacology; Humans; Intestinal Absorption; Male; Medical sciences; Metabolic Clearance Rate; Middle Aged; Pharmacokinetics. Pharmacogenetics. Drug-receptor interactions; Pharmacology. Drug treatments; Rats; Rats, Wistar; Anthocyanin; Human; Urine; Excretion; Rat; Small fruits; Rodentia; Black currant; Oral administration; Ribes nigrum; Bioavailability; Metabolism; Blood; Vertebrata; Mammalia; Absorption; Diet; Dicotyledones; Angiospermae; Pigments; Spermatophyta; Saxifragaceae; Pharmacokinetics
• ISSN: 0021-8561; 1520-5118
• DOI: 10.1021/jf001246q

Four components of black currant anthocyanins (BCA), delphinidin 3-O-β-rutinoside (D3R), cyanidin 3-O-β-rutinoside (C3R), delphinidin 3-O-β-glucoside (D3G), and cyanidin 3-O-β-glucoside (C3G), were found to be directly absorbed and distributed to the blood and excreted into urine as the glycosylated forms. In a rat study, following oral administration of purified D3R, C3R, and C3G (800 μmol/kg of body weight), the anthocyanins were detected in the plasma and the C max values were 580 ± 410, 850 ± 120, and 840 ± 190 nmol/L, respectively, 0.5−2.0 h after administration. In a human study, when a mixtue of BCA [6.24 μmol (3.58 mg) consisting of 2.75 μmol (1.68 mg) of D3R, 2.08 μmol (1.24 mg) of C3R, 1.04 μmol (0.488 mg) of D3G, and 0.37 μmol (0.165 mg) of C3G/kg of body weight)] was orally ingested by eight volunteers, D3R, C3R, D3G, and C3G were detected in the plasma and urine. The plasma C max values were 73.4 ± 35.0, 46.3 ± 22.5, 22.7 ± 12.4, and 5.0 ± 3.7 nmol/L, respectively, 1.25−1.75 h after intake, and the cumulative excretion of the four compounds in urine in the period 0−8 h after intake was 0.11 ± 0.05% of the dose ingested. These results indicate that 3-O-β-rutinosyl anthocyanins were directly absorbed and distributed to the blood. Keywords: Anthocyanins; absorption; excretion; black currant; delphinidin 3-rutinoside; cyanidin 3-rutinoside; delphinidin 3-glucoside; cyanidin 3-glucoside; human; rat