Bioactivity-guided isolation of anti-inflammatory triterpenoids from the sclerotia of Poria cocos using LPS-stimulated Raw264.7 cells
- Authors
- Lee, SR[Lee, Seoung Rak]; Lee, S[Lee, Seulah]; Moon, E[Moon, Eunjung]; Park, HJ[Park, Hye-Jin]; Park, HB[Park, Hyun Bong]; Kim, KH[Kim, Ki Hyun]
- Issue Date
- Feb-2017
- Publisher
- ACADEMIC PRESS INC ELSEVIER SCIENCE
- Keywords
- Poria cocos; Polyporaceae; seco-Lanostane triterpenoid; Bioactivity-guided isolation; Anti-inflammation
- Citation
- BIOORGANIC CHEMISTRY, v.70, pp.94 - 99
- Indexed
- SCIE
SCOPUS
- Journal Title
- BIOORGANIC CHEMISTRY
- Volume
- 70
- Start Page
- 94
- End Page
- 99
- URI
- https://scholarworks.bwise.kr/skku/handle/2021.sw.skku/30306
- DOI
- 10.1016/j.bioorg.2016.11.012
- ISSN
- 0045-2068
- Abstract
- Poria cocos Wolf (Polyporaceae) has been used as a medicinal fungus to treat various diseases since ancient times. This study aimed to investigate the anti-inflammatory chemical constituents of the sclerotia of P. cocos. Based on bioassay-guided fractionation using lipopolysaccharide (LPS)-stimulated Raw264.7 cells, chemical investigation of the EtOH extract of the sclerotia of P. cocos resulted in the isolation and identification of eight compounds including six triterpenoids, namely poricoic acid A (1), 3-O-acetyl-16 alpha-hydroxydehydrotrametenolic acid (2), polyporenic acid C (3), 3 beta-hydroxylanosta-7,9( 11), 24-trien-21-oic acid (4), trametenolic acid (5), and dehydroeburicoic acid (6), as well as (-)-pinoresinol (7) and protocatechualdehyde (8). The structures of the isolated compounds were determined by spectroscopic analysis, including H-1 and C-13 NMR spectra, and LC/MS analysis. The anti-inflammatory activities of the isolates were evaluated by estimating their effect on the production of nitric oxide (NO) and prostaglandin E-2 (PGE(2)) in LPS-stimulated Raw264.7 as well as on the expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2). Compounds 1-5 inhibited NO production and iNOS expression in LPS-stimulated Raw264.7 cells. Among them, compound 1 exerted the highest anti-inhibitory activity and reduced PGE2 levels via downregulation of COX-2 protein expression. The findings of this study provide experimental evidence that the sclerotia of P. cocos are a potential source of natural anti-inflammatory agents for use in pharmaceuticals and functional foods. Furthermore, the most active compound 1, seco-lanostane triterpenoid, could be a promising lead compound for the development of novel anti-inflammatory agents. (C) 2016 Elsevier Inc. All rights reserved.
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