Bisabolangelone isolated from Ostericum koreanum inhibits the production of inflammatory mediators by down-regulation of NF-κB and ERK MAP kinase activity in LPS-stimulated RAW264.7 cells

Jung, Hyo Won; Mahesh, R.; Park, Junhong; Boo, Yong Chool; Park, Kwon Moo; Park, Yong‐Ki

doi:10.1016/j.intimp.2009.10.010

Cited by 52 publications

(44 citation statements)

References 40 publications

(45 reference statements)

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“…BISA exerts several pharmacological activities, including antiinflammatory action by inhibition of NF-kB or AP1 activation in macrophages, antiulcer effects in animal models induced by ethanol or Pylorus ligation, and acaricidal effects against Dermatophagoides farinae or D. pteronyssinus (Kang et al, 2006;Wang et al, 2009;Jung et al, 2010). The molecular bases for these bioactivities might be attributable in part to the primary target of BISA, that is, cAMP-dependent PKA activation, as determined in this study, as PKA is often activated by extracellular stressors or various specific receptors, and its downstream substrate CREB can affect the expression of many genes containing conserved CRE elements adjacent to the TATA boxes (Zhang et al, 2005;Sands and Palmer, 2008;Taylor et al, 2008).…”

Section: Discussionmentioning

confidence: 99%

cAMP-Binding Site of PKA as a Molecular Target of Bisabolangelone against Melanocyte-Specific Hyperpigmented Disorder

Roh

Yun

et al. 2013

Journal of Investigative Dermatology

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Microphthalmia-associated transcription factor (MITF) is inducible in response to cAMP and has a pivotal role in the melanocyte-specific expression of tyrosinase for skin pigmentation. Here we suggest that the cAMP-binding site of protein kinase A (PKA) is a target in the inhibition of the melanogenic process in melanocytes, as evidenced from the molecular mechanism of small molecules such as bisabolangelone (BISA) and Rp-adenosine 3',5'-cyclic monophosphorothioate (Rp-cAMPS). BISA is a sesquiterpene constituent of Angelica koreana, a plant of the Umbelliferae family, whose roots are used as an alternative medicine. BISA competitively inhibited cAMP binding to the regulatory subunit of PKA and fitted into the cAMP-binding site on the crystal structure of PKA under the most energetically favorable simulation. In α-melanocyte-stimulating hormone (α-MSH)-activated melanocytes, BISA and Rp-cAMPS nullified cAMP-dependent PKA activation, dissociating catalytic subunits from an inactive holoenzyme complex. They resultantly inhibited cellular phosphorylation of the cAMP-responsive element-binding protein (CREB) or another transcription factor SOX9, thus downregulating the expression of MITF or the tyrosinase gene with decreased melanin production. Taken together, this study defined the antimelanogenic mechanism of BISA or Rp-cAMPS with a notable implication of the cAMP-binding site of PKA as a putative target ameliorating melanocyte-specific hyperpigmented disorder.

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Section: Discussionmentioning

confidence: 99%

cAMP-Binding Site of PKA as a Molecular Target of Bisabolangelone against Melanocyte-Specific Hyperpigmented Disorder

Roh

Yun

et al. 2013

Journal of Investigative Dermatology

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“…Recent studies have reported that plant extracts inhibit the generation of inflammation mediators (NO, PGE 2 , iNOS and IL-6) from macrophages such as Astragalus membranaceus, Ostericum koreanum and others (Clement-Kruzel et al, 2008;Jung et al, 2010). Anti-inflammatory effect of leaves and stem from Paeonia lactiflora was reported, but the anti-inflammatory effect of root is yet to be reported (Kim et al, 2007).…”

Section: Discussionmentioning

confidence: 99%

Suppression Effect of the Inflammatory Response in Macrophages by Paeoniae Radix Rubra Extracts

Bak¹,

Son²,

Kim³

et al. 2011

Korean Journal of Medicinal Crop Science

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: Paeoniae Radix Rubra is a preparation consisting of desiccated roots of Paeonia lactiflora PALL (belonging to Ranunculaceae). Paeoniae Radix Rubra is used as a medicinal herb in Asian countries to treat many diseases. Ethanol-or water-based extracts of Paeoniae Radix Rubra were prepared and tested on RAW 264.7 cells, a murine macrophage cell line. The expression of some pro-inflammatory proteins, including inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2), extracellular signal-regulated kinase 1/2 (ERK1/2) and phosphorylated ERK1/2 was detected by Western blot analyses, while PGE2 expression was quantified by ELISA. Both the water and ethanol extracts of Paeoniae Radix Rubra suppressed LPS-induced nitric oxide (NO) production and exhibited cell toxicity in accordance with increased NO production. Also, both extracts reduced the expression of COX-2 and iNOS, and inhibited phosphorylation of ERK1/2 in LPS-stimulated RAW 264.7 cells. Extracts prepared from Paeoniae Radix Rubra contain anti-inflammatory agents that inhibit the iNOS and MAPK pathways.

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“…When p65 was phosphorylated at specific residues, it could translate into the nucleus to bind the promoter regions of many cytokines genes (Hanada and Yoshimura, 2002;Jung et al, 2010). As showed in Fig.…”

Section: Effect Of Rdn On Phosphorylation Of P65 In Lps-induced Raw 2mentioning

confidence: 99%

Insight into the molecular mechanism of a herbal injection by integrating network pharmacology and in vitro

Zhang

et al. 2015

Journal of Ethnopharmacology

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Bisabolangelone isolated from Ostericum koreanum inhibits the production of inflammatory mediators by down-regulation of NF-κB and ERK MAP kinase activity in LPS-stimulated RAW264.7 cells

Cited by 52 publications

References 40 publications

cAMP-Binding Site of PKA as a Molecular Target of Bisabolangelone against Melanocyte-Specific Hyperpigmented Disorder

cAMP-Binding Site of PKA as a Molecular Target of Bisabolangelone against Melanocyte-Specific Hyperpigmented Disorder

Suppression Effect of the Inflammatory Response in Macrophages by Paeoniae Radix Rubra Extracts

Insight into the molecular mechanism of a herbal injection by integrating network pharmacology and in vitro

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