[Bioassay-guided fractionation of constituents targeting mediators of inflammation from lycii cortex as inhibitors of NF-kappaB].
Zhongguo Zhong Yao Za Zhi
; 39(4): 689-94, 2014 Feb.
Article
em Zh
| MEDLINE
| ID: mdl-25204148
ABSTRACT
Lycii Cortex, a popular herb medicine in traditional Chinese medicine, is used to treat different inflammation-related diseases. The aim of our work is to find the key constituents inhibiting NF-kappaB, a key regulator of inflammation. In the investigations of cell-based in vitro assays of extracts, we found that both ethyl acetate extract and methanol extract of Lycii Cortex inhibited the TNF-alpha-induced activation of NF-kappaB. Through bioassay-guided fractionation, we identified 4 phenolic amides including trans-N-(p-coumaroyl) tyramine (1), trans-N-feruloyltyramine (2), trans-N-caffeoyltyramine (3), and dihydro-N-caffeoyltyramine (4). Four phenolic amides showed differently inhibitory activities on TNF-alpha-induced NF-kappaB activation. Trans-N-caffeoyltyramine (3) was identified as the key component with an IC50 of 18.41 micromol x L(-1). It was suggested that the hydroxyl group at C-3 in trans-N-caffeoyltyramine might be a key binding site and its C-7,8-double bond might play an important role on NF-kappaB inhibitory activities as the link of the conjugation of pi electrons leading to a partial planar conformation. It might be inferred that the biological activity of compound 3 is attributed to the structure of Michael reaction acceptor containing alpha, beta-unsaturated ketones and benzene along with hydroxyl group in o-diphenol.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Medicamentos de Ervas Chinesas
/
NF-kappa B
/
Mediadores da Inflamação
/
Lycium
Tipo de estudo:
Prognostic_studies
Limite:
Humans
Idioma:
Zh
Revista:
Zhongguo Zhong Yao Za Zhi
Assunto da revista:
FARMACOLOGIA
/
TERAPIAS COMPLEMENTARES
Ano de publicação:
2014
Tipo de documento:
Article