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1,7‑Bis(4‑hydroxy‑3‑methoxyphenyl)‑1,4,6‑heptatrien‑3‑one alleviates lipopolysaccharide‑induced inflammation by targeting NF‑κB translocation in murine macrophages and it interacts with MD2 in silico.

Abstract：

:Trienones are curcuminoid analogues and are minor constituents in the rhizomes of numerous Curcuma plant species. Studies investigating the biological activities of trienones, particularly their anti‑inflammatory activities, are limited. In the present study, the trienone 1,7‑bis(4‑hydroxy‑3‑methoxyphenyl)‑1,4,6‑heptatrien‑3‑one (HMPH) was structurally modified from curcumin using a novel and concise method. HMPH was shown to exhibit potential anti‑inflammatory effects on lipopolysaccharide (LPS)‑activated RAW264.7 macrophages. Furthermore, LPS‑induced nitric oxide secretion in RAW264.7 cells was markedly and dose‑dependently inhibited by HMPH; in addition, HMPH had a greater efficacy compared with curcumin. This inhibition was accompanied by the suppression of inducible nitric oxide synthase and cyclooxygenase‑2 expression, as well as pro‑inflammatory cytokine secretion. To elucidate the molecular mechanism underlying the anti‑inflammatory effects of HMPH, the effects of this compound on nuclear factor‑κB (NF‑κB) translocation were assessed. HMPH significantly inhibited the translocation of p65 NF‑κB into the nucleus to a greater extent than curcumin, thus indicating that HMPH has more potent anti‑inflammatory activity than curcumin. In addition, an in silico modelling study revealed that HMPH possessed stronger binding energy to myeloid differentiation factor 2 (MD2) compared with that of curcumin, and indicated that the anti‑inflammatory effects of HMPH may be through upstream inhibition of the inflammatory pathway. In conclusion, HMPH may be considered a promising compound for reducing inflammation via targeting p65 NF‑κB translocation and interfering with MD2 binding.

journal_name

Mol Med Rep

journal_title

Molecular medicine reports

authors

Jansakun C,Chulrik W,Chaichompoo W,Yotmanee P,Lehboon K,Chunglok W,Sattayakhom A,Hiransai P,Kamdee K,Utaipan T,Suksamrarn A,Chunglok W

doi

10.3892/mmr.2021.11848

subject

Has Abstract

pub_date

2021-03-01 00:00:00

issue

eissn

1791-2997

issn

1791-3004

pii

209

journal_volume

pub_type

杂志文章

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1,7‑Bis(4‑hydroxy‑3‑methoxyphenyl)‑1,4,6‑heptatrien‑3‑one alleviates lipopolysaccharide‑induced inflammation by targeting NF‑κB translocation in murine macrophages and it interacts with MD2 in silico.