期刊
PLANTA MEDICA
卷 79, 期 6, 页码 471-479出版社
GEORG THIEME VERLAG KG
DOI: 10.1055/s-0032-1328332
关键词
arctigenin; Arctium lappa; Asteraceae; arctigenic acid; hydrolysis; paraoxonase 1
资金
- Chinese University of Hong Kong [2041449, 3800005]
- Health Authority of Hong Kong [7010213]
- National Science and Technology Major Project of China [2011ZX09307-002-01]
The phenylpropanoid dibenzylbutyrolactone lignan arctigenin, a key component found in Arctium lappa, or burdock, has been reported with a variety of therapeutic effects including anticancer, anti-inflammation, and antivirus effects. Using LC/MS/MS, three novel metabolites of arctigenin, namely, arctigenic acid, arctigenin-4-O'-glucuronide, and 4-O-demethylarctigenin were identified after oral administration of arctigenin in rats for the first time. Another potential metabolite of arctigenin, arctigenin-4'-O-sulfate, was identified in vitro but not in vivo. Structure of arctigenic acid, the major metabolite of arctigenin, was confirmed by C-13-NMR and H-1-NMR. Rapid hydrolysis in plasma was identified as the major metabolic pathway of arctigenin after its oral administration, with V-max, K-m, and Cl-int in rat plasma determined to be 2.21 +/- 0.12 nmol/min/mg, 89.12 +/- 9.44 mu M, and 24.74 mu L/min/mg, respectively. Paraoxonase 1 was further confirmed to be the enzyme responsible for arctigenin hydrolysis, with Vmax, Km, and Clint determined to be 55.39 +/- 1.49 nmol/min/mg, 300.3 +/- 10.86 mu M, and 184.45 mu L/min/mg, respectively.
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