Blockade of cytosolic phospholipase A2 and 5-lipoxygenase activation in neutrophils by a natural isoflavanquinone abruquinone A

Hsu, Mei‐Feng; Chang, Ling‐Chu; Chen, Sheng‐Chih; Kuo, Sheng‐Chu; Lee, Hsiao-Yun; Lu, Min-Chi; Wang, Jih-Pyang

doi:10.1016/j.ejphar.2008.09.007

Cited by 5 publications

(2 citation statements)

References 37 publications

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“…Likewise, a related methyl naphthalene carboxylate, lawsonaphthoate A (Table 1), and had potent inhibitory activity [73]. Although embelin, abruquinone A, and acetylshikonin inhibited f MLF-induced functional responses in neutrophils, these natural quinones also suppressed ionophore A23187-induced biosynthesis of eicosanoids in neutrophils [117–119], and embelin directly inhibited enzymatic activity of purified 5-lipoxygenase [119]. Finally, ehretiquinone isolated from the root of Ehretia longiflora potently inhibited f MLF-induced O 2 −· production, although effects on f MLF-induced HNE release and other functional activities were not evaluated [120].…”

Section: Small-molecule Non-peptide Fpr1 Antagonists and Their Synmentioning

confidence: 99%

Antagonism of human formyl peptide receptor 1 with natural compounds and their synthetic derivatives

Schepetkin

Khlebnikov

Kirpotina

et al. 2016

International Immunopharmacology

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Formyl peptide receptor 1 (FPR1) regulates a wide variety of neutrophil functional responses and plays an important role in inflammation and the pathogenesis of various diseases. To date, a variety of natural and synthetic molecules have been identified as FPR1 ligands. Here, we review current knowledge on natural products and natural product-inspired small-molecules reported to antagonize and/or inhibit the FPR1-mediated responses. Based on this literature, additional screening of selected commercially available natural compounds for their ability to inhibit fMLF-induced Ca2+ mobilization in human neutrophils and FPR1 transfected HL-60 cells, and pharmacophore modeling, natural products with potential as FPR1 antagonists are considered and discussed in this review. The identification and characterization of natural products that antagonize FPR1 activity may have potential for the development of novel therapeutics to limit or alter the outcome of inflammatory processes.

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Section: Small-molecule Non-peptide Fpr1 Antagonists and Their Synmentioning

confidence: 99%

Antagonism of human formyl peptide receptor 1 with natural compounds and their synthetic derivatives

Schepetkin

Khlebnikov

Kirpotina

et al. 2016

International Immunopharmacology

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“…The Chinese herbs, which contain the hit compounds, mostly have the efficacy of 'heat-clearing and detoxifying', and are suggested in many studies to have the anti-inflammatory activity. Abruquinone A [ 5 ] , Embelin [ 6 ] and Nobiletin [ 7 ] are experimental proved to have anti-inflammatory activity and has been confirmed for the COX-2 inhibitor screening. In summary, ten structure-based COX-2 inhibitor pharmacophore models were constructed by LigandScout.…”

Section: Resultsmentioning

confidence: 84%

Combinatorial Screening of COX-2 Inhibitors from Chinese Herbs Based on Multiple Structure-Based Pharmacophores

Zhang

Wang

Qiao

2013

AMR

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Ten structure-based pharmacophore models of Cyclooxygenase 2 (COX-2) inhibitors were generated by LigandScout based on COX-2 inhibitor complexes from the Protein Data Bank (PDB). The potential COX-2 inhibitors were identified from traditional Chinese medicine with the method of combinatorial screening with ten models. Based on the screening results of MDDR and the metrics of E, A% and comprehensive appraisal index (CAI), the threshold of hit frequency of molecules was defined and used to identify the active molecules from Chinese herbs. The molecules hit by not less than six pharmacophore models were taken as the screening objects of COX-2 inhibitor, and 1103 molecules were obtained.

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A novel C(28)-hydroxylated lupeolic acid suppresses the biosynthesis of eicosanoids through inhibition of cytosolic phospholipase A2

Verhoff

Seitz

Northoff³

et al. 2012

Biochemical Pharmacology

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Blockade of cytosolic phospholipase A2 and 5-lipoxygenase activation in neutrophils by a natural isoflavanquinone abruquinone A

Cited by 5 publications

References 37 publications

Antagonism of human formyl peptide receptor 1 with natural compounds and their synthetic derivatives

Antagonism of human formyl peptide receptor 1 with natural compounds and their synthetic derivatives

Combinatorial Screening of COX-2 Inhibitors from Chinese Herbs Based on Multiple Structure-Based Pharmacophores

A novel C(28)-hydroxylated lupeolic acid suppresses the biosynthesis of eicosanoids through inhibition of cytosolic phospholipase A2

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