Inhibitory Effects of Benzaldehyde Derivatives from the Marine Fungus Eurotium sp. SF-5989 on Inflammatory Mediators via the Induction of Heme Oxygenase-1 in Lipopolysaccharide-Stimulated RAW264.7 Macrophages

International Journal of Molecular Sciences

Kyoung-Su Kim⁴  Xiang Cui⁴  Dong-Sung Lee¹  Wonmin Ko⁴  Jae Hak Sohn³  Joung Han Yim²  Ren-Bo An⁵  Youn-Chul Kim⁴  Hyuncheol Oh⁴ 

[1] Inha Research Institute for Medical Sciences, Inha University School of Medicine, Incheon 400-712, Korea; E-Mail:;Korea Polar Research Institute, KORDI, 7-50 Songdo-dong, Yeonsu-gu, Incheon 406-840, Korea; E-Mail:;College of Medical and Life Sciences, Silla University, Busan 617-736, Korea; E-Mail:;College of Pharmacy, Wonkwang University, Iksan 570-749, Korea; E-Mails:;Key Laboratory of Natural Resources and Functional Molecules of the Changbai Mountain, Affiliated Ministry of Education, Yanbian University College of Pharmacy, 977 Gongyuan Road, Yanji 133002, China; E-Mail:

关键词: benzaldehyde derivatives;    marine fungus;    Eurotium rubrum;    RAW264.7 macrophages;    heme oxygenase-1;    anti-inflammatory effect;    nuclear factor-κB;   

DOI  :  10.3390/ijms151223749

来源: mdpi

【 摘 要 】

Two benzaldehyde derivatives, flavoglaucin (1) and isotetrahydro-auroglaucin (2), were isolated from the marine fungus Eurotium sp. SF-5989 through bioassay- and ¹H NMR-guided investigation. In this study, we evaluated the anti-inflammatory effects of these compounds in lipopolysaccharide (LPS)-stimulated RAW264.7 macrophages. We demonstrated that compounds 1 and 2 markedly inhibited LPS-induced nitric oxide (NO) and prostaglandin E2 (PGE₂) production by suppressing inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) protein expression without affecting cell viability. We also demonstrated that the compounds reduced the secretion of pro-inflammatory cytokines such as tumor necrosis factor-α (TNF-α), interleukin-1β (IL-1β) and interleukin-6 (IL-6). Furthermore, compounds 1 and 2 inhibited LPS-induced nuclear factor-κB (NF-κB) activation by suppressing phosphorylation of IkappaB (IκB). These results indicated that the anti-inflammatory effects of these benzaldehyde derivatives in LPS-stimulated RAW264.7 macrophages were due to the inactivation of the NF-κB pathway. In addition, compounds 1 and 2 induced heme oxygenase-1 (HO-1) expression through the nuclear transcription factor-E2–related factor 2 (Nrf2) translocation. The inhibitory effects of compounds 1 and 2 on the production of pro-inflammatory mediators and on NF-κB binding activity were reversed by HO-1 inhibitor tin protoporphyrin (SnPP). Thus, the anti-inflammatory effects of compounds 1 and 2 also correlated with their ability of inducing HO-1 expression.

【 授权许可】

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