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KMID : 0043320120350050823
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Archives of Pharmacal Research
2012 Volume.35 No. 5 p.823 ~ p.837
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Anti-inflammatory and antioxidant activities of constituents isolated from Pueraria lobata roots
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Jin Seong-Eun
Son You-Kyung
Min Byung-Sun
Jung Hyun-Ah
Choi Jae-Sue
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Abstract
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In order to evaluate the anti-inflammatory and antioxidant activities of Pueraria lobata roots and its active components, in vitro inhibitory activities against lipopolysaccharide (LPS)-induced nitric oxide (NO) production, inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2) protein expression, and tert-butylhydroperoxide (t-BHP)-induced reactive oxygen species (ROS) generation in RAW 264.7 cells, as well as in vitro scavenging activities against 1,1-diphenyl-2-picrylhydrazyl (DPPH), peroxynitrite (ONOO?), nitric oxide (NO·), superoxide anion (·O2?) and total ROS, and inhibitory activities against ONOO?-mediated tyrosine nitration, were determined. Repeated column chromatography was performed to isolate four known compounds from the anti-inflammatory and antioxidant EtOAc fraction: daidzein; genistein; puerarin; (+)-puerarol B-2-O-glucopyranoside; four known compounds from the anti-inflammatory n-hexane fraction: lupenone; lupeol; puerarol; coumestrol; seven known compounds from the antioxidant n-BuOH fraction: allantoin; 3′-hydroxypuerarin; daidzein 8-C-apiosyl-(1→6)-glucoside; puerarin; genistin; 3′-methoxypuerarin; daidzin. Among these compounds, lupenone and lupeol reduced NO production, as well as iNOS and COX-2 protein levels in LPS-stimulated RAW 264.7 cells. Furthermore, lupeol showed significant inhibitory activity against intracellular ROS generation by t-BHP. Meanwhile, 3′-hydroxypuerarin showed marked ONOO?, NO·, total ROS scavenging activities, and weak ·O2? scavenging activity, while 3′-methoxypuerarin showed ONOO? scavenging activity and weak NO· and O2? scavenging activities, suggesting that existence of the 3′-hydroxyl group in puerarin plays an important role in the scavenging of ONOO?, NO·, and total ROS, as well as inhibiting the ONOO?-mediated tyrosine nitration mechanism. These results indicate that P. lobata roots and its constituents may be a useful therapeutic and preventive approach to various inflammatory diseases and oxidative stress-related disease.
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KEYWORD
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Pueraria lobata, Lupenone, Lupeol, 3′-Hydroxypuerarin, Anti-inflammation, Antioxidant
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