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Bioactivity-guided isolation of anti-inflammatory triterpenoids from the sclerotia of Poria cocos using LPS-stimulated Raw264.7 cells.
Lee, Seoung Rak; Lee, Seulah; Moon, Eunjung; Park, Hye-Jin; Park, Hyun Bong; Kim, Ki Hyun.
Afiliação
  • Lee SR; School of Pharmacy, Sungkyunkwan University, Suwon 440-746, Republic of Korea.
  • Lee S; School of Pharmacy, Sungkyunkwan University, Suwon 440-746, Republic of Korea.
  • Moon E; Charmzone R&D Center, Charmzone Co. Ltd., Seoul 135-851, Republic of Korea.
  • Park HJ; Department of Food Science and Biotechnology, College of BioNano Technology, Gachon University, Seongnam 461-701, Republic of Korea.
  • Park HB; Department of Chemistry, Yale University, New Haven, CT 06520, United States.
  • Kim KH; School of Pharmacy, Sungkyunkwan University, Suwon 440-746, Republic of Korea. Electronic address: khkim83@skku.edu.
Bioorg Chem ; 70: 94-99, 2017 02.
Article em En | MEDLINE | ID: mdl-27912907
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-16α-hydroxydehydrotrametenolic acid (2), polyporenic acid C (3), 3ß-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 1H and 13C 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 E2 (PGE2) 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.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Triterpenos / Wolfiporia / Macrófagos / Anti-Inflamatórios Tipo de estudo: Prognostic_studies Limite: Animals Idioma: En Revista: Bioorg Chem Ano de publicação: 2017 Tipo de documento: Article

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Triterpenos / Wolfiporia / Macrófagos / Anti-Inflamatórios Tipo de estudo: Prognostic_studies Limite: Animals Idioma: En Revista: Bioorg Chem Ano de publicação: 2017 Tipo de documento: Article