Potent inhibition of human neutrophil activations by bractelactone, a novel chalcone from Fissistigma bracteolatum

Wu, Yang; Sureshbabu, Munisamy; Fang, Yao Ching; Wu, Yuan-Hua; Lan, Yu; Chang, Fang Rong; Chang, Ya Wen; Hwang, Tsong‐Long

doi:10.1016/j.taap.2012.11.021

Cited by 21 publications

(9 citation statements)

References 49 publications

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“…We concluded that this compound may interfere with intracellular signaling pathways common to both FPR1 and CXCR1/2 [196]. Viscolin and bractelactone, which are chalcones from Viscum coloratum and Fissistigma bracteolatum , respectively, also inhibited f MLF-induced O 2 −· production and HNE release by neutrophils; however, these compounds did not inhibit f MLF-induced Ca 2+ flux [198, 199], suggesting targets other than FPR1. Likewise, inhibition of f MLF-stimulated rat neutrophil respiratory burst activity by broussochalcone A, a prenylated chalcone isolated from Broussonetia papyrifera , was found to be due to the suppression of PKC [200].…”

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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“…This compound also was shown to significantly reduce CD11b, an integrin expressed in human neutrophils stimulated with fMLP and cytochalasin B, thus ameliorating the inflammatory condition by preventing the neutrophils migration into tissues. 50 …”

Section: Chalcones As Immunomodulatory Agentsmentioning

confidence: 99%

Effects of chalcone derivatives on players of the immune system

Lee¹,

Bukhari²,

Fauzi³

2015

DDDT

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The immune system is the defense mechanism in living organisms that protects against the invasion of foreign materials, microorganisms, and pathogens. It involves multiple organs and tissues in human body, such as lymph nodes, spleen, and mucosa-associated lymphoid tissues. However, the execution of immune activities depends on a number of specific cell types, such as B cells, T cells, macrophages, and granulocytes, which provide various immune responses against pathogens. In addition to normal physiological functions, abnormal proliferation, migration, and differentiation of these cells (in response to various chemical stimuli produced by invading pathogens) have been associated with several pathological disorders. The unwanted conditions related to these cells have made them prominent targets in the development of new therapeutic interventions against various pathological implications, such as atherosclerosis and autoimmune diseases. Chalcone derivatives exhibit a broad spectrum of pharmacological activities, such as immunomodulation, as well as anti-inflammatory, anticancer, antiviral, and antimicrobial properties. Many studies have been conducted to determine their inhibitory or stimulatory activities in immune cells, and the findings are of significance to provide a new direction for subsequent research. This review highlights the effects of chalcone derivatives in different types of immune cells.

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“…The binding of fMLF to GPCR triggers a rapid and transient increase in [Ca 2+ ] i , resulting in neutrophil activation. Some specific inhibitors of Ca 2+ signaling have been investigated as anti-inflammatory drugs because of their suppressive effects on neutrophil functions 44 . Our experiments using a Ca 2+ chelator (BAPTA-AM) proved that increased [Ca 2+ ] i was required for the fMLF-induced respiratory burst and elastase release.…”

Section: Discussionmentioning

confidence: 99%

Anti-inflammatory effects of Perilla frutescens in activated human neutrophils through two independent pathways: Src family kinases and Calcium

Chen

Leu

Fang

et al. 2015

Sci Rep

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The leaves of Perilla frutescens (L.) Britt. have been traditionally used as an herbal medicine in East Asian countries to treat a variety diseases. In this present study, we investigated the inhibitory effects of P. frutescens extract (PFE) on N-formyl-Met-Leu-Phe (fMLF)-stimulated human neutrophils and the underlying mechanisms. PFE (1, 3, and 10 μg/ml) inhibited superoxide anion production, elastase release, reactive oxygen species formation, CD11b expression, and cell migration in fMLF-activated human neutrophils in dose-dependent manners. PFE inhibited fMLF-induced phosphorylation of the Src family kinases (SFKs), Src (Tyr416) and Lyn (Tyr396), and reduced their enzymatic activities. Both PFE and PP2 (a selective inhibitor of SFKs) reduced the phosphorylation of Burton’s tyrosine kinases (Tyr223) and Vav (Tyr174) in fMLF-activated human neutrophils. Additionally, PFE decreased intracellular Ca2+ levels ([Ca2+]i), whereas PP2 prolonged the time required for [Ca2+]i to return to its basal level. Our findings indicated that PFE effectively regulated the inflammatory activities of fMLF-activated human neutrophils. The anti-inflammatory effects of PFE on activated human neutrophils were mediated through two independent signaling pathways involving SFKs (Src and Lyn) and mobilization of intracellular Ca2+.

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Potent inhibition of human neutrophil activations by bractelactone, a novel chalcone from Fissistigma bracteolatum

Cited by 21 publications

References 49 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

Effects of chalcone derivatives on players of the immune system

Anti-inflammatory effects of Perilla frutescens in activated human neutrophils through two independent pathways: Src family kinases and Calcium

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