Anti-inflammatory effects of 5-hydroxy-3,6,7,8,3',4'-hexamethoxyflavone via NF-κB inactivation in lipopolysaccharide-stimulated RAW 264.7 macrophage.
The anti-inflammatory mechanism of 5-hydroxy-3,6,7,8,3',4'-hexamethoxyflavone (5HHMF), a polyhydroxyflavone isolated from the marine algae Hizikia fusiforme, was investigated in RAW 264.7 murine macrophage cells. Western blot and reverse transcriptase PCR analyses indicated that adding 5HHMF to cultured cells significantly reduced the production of nitric oxide and prostaglandin E2 and downregulated inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) expression in lipopolysaccharide (LPS)-stimulated RAW 264.7 cells. In addition, 5HHMF inhibited the release of pro-inflammatory cytokines, such as tumor necrosis factor-α and interleukin-1β, and decreased the transcriptional levels. In particular, 5HHMF significantly inhibited the LPS-induced nuclear factor-κB (NF-κB) translocation from the cytosol to the nucleus, which was associated with the abrogation of inhibitory IκBα degradation and subsequent decreases in nuclear p65 levels. In conclusion, these results suggested that the anti-inflammatory activities of 5HHMF may be attributed to the inhibition of iNOS, COX-2 and cytokine expression by attenuating NF-κB activation via IκBα degradation in macrophages.
Department of Biotechnology, Dong-A University, Saha‑gu, Busan 604-714, Republic of Korea.
Min Jeong
MJ
Kim
Department of Biotechnology, Dong-A University, Saha‑gu, Busan 604-714, Republic of Korea.
Hye Hyeon
HH
Lee
Center for Core Research Facilities, Daegu Gyeongbuk Institute of Science and Technology, Dalseong‑gun, Daegu 711-873, Republic of Korea.
Jin Woo
JW
Jeong
Department of Biotechnology, Dong-A University, Saha‑gu, Busan 604-714, Republic of Korea.
Min Jeong
MJ
Seo
Medi-Farm Industrialization Research Center, Dong-A University, Saha‑gu, Busan 604-714, Republic of Korea.
Byoung Won
BW
Kang
Medi-Farm Industrialization Research Center, Dong-A University, Saha‑gu, Busan 604-714, Republic of Korea.
Jeong Uck
JU
Park
Department of Biotechnology, Dong-A University, Saha‑gu, Busan 604-714, Republic of Korea.
Kyoung-Sook
KS
Kim
Department of Biotechnology, Dong-A University, Saha‑gu, Busan 604-714, Republic of Korea.
Young-Su
YS
Cho
Department of Food and Nutrition, Sunchon National University, Sunchon, Jeollanam‑do 540-950, Republic of Korea.
Kwon-Il
KI
Seo
Laboratory of Immunobiology, Department of Marine Life Sciences, Jeju National University, Jeju-si, Jeju 690-756, Republic of Korea.
Gi-Young
GY
Kim
School of Food and Life Sciences, Inje University, Gimhae, Gyeongsang 621-749, Republic of Korea.
Jung-In
JI
Kim
Department of Biochemistry, Dongeui University College of Oriental Medicine, Busanjin-gu, Busan 614-052, Republic of Korea.
Yung Hyun
YH
Choi
Department of Biotechnology, Dong-A University, Saha‑gu, Busan 604-714, Republic of Korea.
Yong Kee
YK
Jeong
D000818:Animals; D000893:Anti-Inflammatory Agents / Q000494:pharmacology*; D016923:Cell Death / Q000187:drug effects; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D051546:Cyclooxygenase 2 / Q000378:metabolism; D015232:Dinoprostone / Q000096:biosynthesis; D047309:Flavones / Q000737:chemistry / Q000494:pharmacology*; D053583:Interleukin-1beta / Q000096:biosynthesis; D008070:Lipopolysaccharides / Q000494:pharmacology*; D008264:Macrophages / Q000166:cytology / Q000187:drug effects / Q000201:enzymology / Q000378:metabolism*; D051379:Mice; D016328:NF-kappa B / Q000378:metabolism*; D009569:Nitric Oxide / Q000096:biosynthesis; D052247:Nitric Oxide Synthase Type II / Q000378:metabolism; D020011:Protective Agents / Q000494:pharmacology; D015398:Signal Transduction / Q000187:drug effects; D014409:Tumor Necrosis Factor-alpha / Q000096:biosynthesis
D000893:Anti-Inflammatory Agents; D047309:Flavones; D053583:Interleukin-1beta; D008070:Lipopolysaccharides; D016328:NF-kappa B; D020011:Protective Agents; D014409:Tumor Necrosis Factor-alpha; C521815:5-hydroxy-3,6,7,8,3',4'-hexamethoxyflavone; D009569:Nitric Oxide; D052247:Nitric Oxide Synthase Type II; C077623:Ptgs2 protein, mouse; D051546:Cyclooxygenase 2; D015232:Dinoprostone