Fargesin exerts anti-inflammatory effects in THP-1 monocytes by suppressing PKC-dependent AP-1 and NF-ĸB signaling

Pham, Thu-Huyen; Kim, Man-Sub; Le, Minh-Quan; Song, Yong; Bak, Yesol; Ryu, Hyung Won; Oh, Sei‐Ryang; Yoon, Do‐Young

doi:10.1016/j.phymed.2016.11.014

Cited by 66 publications

(70 citation statements)

References 28 publications

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“…In this study, we observed a rise in the expression of iNOS and COX‐2 in THP‐1 cells treated with LPS alone, which was in accordance with the findings of previous study (Guo et al., ). Reportedly, iNOS and COX‐2 are vital regulators of NO and PGE2 products, respectively (Bi et al., ; Pham et al., ; Yang et al., ; Yashaswini, Kurrey, & Singh, ). Indeed, we also found the products of NO and PGE2 increased with the overexpression of iNOS and COX‐2.…”

Section: Discussionmentioning

confidence: 99%

“…However, choosing human cells as the cell model to explore the inhibitory effect of VA on human inflammation is more suitable and valuable. In view of monocytes (major components of the innate immune system of the human body) playing crucial roles in host defenses against infection through inflammation (Bi et al., ; Pham et al., ), THP‐1 human monocytic cell was chosen as the cell model to uncover the anti‐inflammatory effect of VA in the present study. Moreover, to explore the mechanism underlying the anti‐inflammatory effect, the effect of VA on the expression of upstream signaling pathway needs to be conducted.…”

Section: Introductionmentioning

confidence: 99%

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Elucidation of The Anti‐Inflammatory Effect of Vanillin In Lps‐Activated THP‐1 Cells

Zhao

Jiang

et al. 2019

Journal of Food Science

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Vanillin, a kind of phenolic compound, is naturally found in food and beverage and widely used as a flavoring agent. In view of the safety and universality of vanillin, exploring the functions of vanillin on human is of great value. Thus, lipopolysaccharide (LPS)‐activated THP‐1 cells were selected as the cell model to evaluate the anti‐inflammatory effect of vanillin in this study. On the basis of the results, vanillin markedly suppressed the expression of inflammatory cytokines (that is, TNF‐α, IL‐1β, IL‐6, and IL‐8), mediators (NO, iNOS, PGE2, and COX‐2), and NLRP3 inflammasome (that is, NLRP3, ASC, and caspase‐1), blocked the LPS‐induced activation of the NF‐κB/IκBα/AP‐1 signaling pathway, and activated the gene expression of the Nrf2/HO‐1 signaling pathway. In addition, it was confirmed that vanillin was unable to react with LPS due to the results of quantification by HS‐SPME‐GC‐MS. Hence, vanillin could effectively attenuate LPS‐induced inflammatory response by regulating the expression of intracellular signaling pathways in THP‐1 cells. It is a potent anti‐inflammatory component found in food and beverage. These findings might contribute to the overall understanding of the potential health benefits of vanillin for food application. Practical Application In this study, the anti‐inflammatory effect of vanillin (VA) was evaluated by ELISA, real‐time PCR, and western blot in LPS‐induced THP‐1 cells. The hypothesis that VA could react with LPS was excluded due to the results of quantification by HS‐SPME‐GC‐MS. On the basis of the result, vanillin could effectively attenuate LPS‐induced inflammatory response in THP‐1 cells and was a potent anti‐inflammatory component natural in food and beverage. These findings might contribute to the overall understanding of the potential health benefits of vanillin for food application.

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Elucidation of The Anti‐Inflammatory Effect of Vanillin In Lps‐Activated THP‐1 Cells

Zhao

Jiang

et al. 2019

Journal of Food Science

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“…MTS assay is a colorimetric assay quantifying the activity of mitochondrial reductase that reduces tetrazolium to formazan. The THP‐1 cells (1 × 10 5 cells/well) were seeded in 100 μL of the medium in 96‐well plates and were treated with epimagnolin A at noncytotoxic concentrations of 1 to 20 μM for 24 hours along with 10 nM PMA as previously reported . The effect of epimagnolin A on cell viability was estimated using the CellTiter 96 aqueous one solution assay (Promega, Madison, Wisconsin) containing MTS and phenazine methosulfate, an electron coupling reagent.…”

Section: Methodsmentioning

confidence: 99%

“…The compounds isolated from M. fargesii have shown anti‐angiogenic, anti‐allergic, anti‐rheumatoid arthritis, and anti‐inflammatory activities . In our previous study, fargesin, is a lignin obtained from flower buds of M. fargesii, was found to exert strong anti‐inflammatory properties in THP‐1 cell line . Epimagnolin A is a different lignan obtained from the same flower bud and was anticipated that could also modulate inflammatory responses in the THP‐1 cells.…”

Section: Introductionmentioning

confidence: 98%

Epimagnolin A inhibits IL‐6 production by inhibiting p38/NF‐κB and AP‐1 signaling pathways in PMA‐stimulated THP‐1 cells

Chun

Kim

Pham

et al. 2019

Environmental Toxicology

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Epimagnolin A is a lignan obtained from the flower buds of Magnolia fargesii, which is traditionally used in Asian medicine for treating headache and nasal congestion. A herbal compound fargesin obtained from M. fargesii, has exerted anti‐inflammatory effects in human monocytic THP‐1 cells in the previous study. The anti‐inflammatory effects of epimagnolin A, however, have been not elucidated yet. In this study, it was demonstrated that epimagnolin A reduced phorbol‐12‐myristate‐13‐acetate (PMA)‐induced IL‐6 promoter activity and IL‐6 production in human monocytic THP‐1 cells. Furthermore, it was investigated the modulating effects of epimagnolin A on mitogen‐activated protein kinase, nuclear factor‐kappa B (NF‐κB), and activator protein 1 (AP‐1) activities. Phosphorylation of p38 and nuclear translocation of p50 and c‐Jun were down‐regulated by epimagnolin A in the PMA‐stimulated THP‐1 cell. The results revealed that epimagnolin A attenuated the binding affinity of NF‐κB and AP‐1 transcription factors to IL‐6 promoter and IL‐6 production through p38/NF‐kB and AP‐1 signaling pathways in the PMA‐stimulated THP‐1 cells. These results suggest that epimagnolin A can be a useful drug for the treatment of inflammatory diseases.

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“…[1,2,3,4,5]. Magnolin, epimagnolin A, dimethyllirioresinol, eudesmin, and fargesin exhibit various biological activities, including anti-inflammatory activity [6,7,8,9,10], 5-lipoxygenase inhibitory activity [6], antimycobacterial activity [11], and the inhibition of tumor growth and cancer-catalyzed bone destruction [12]. Fargesin exhibits additional biological activities, including β1-adrenergic receptor antagonistic and cardioprotective effects [13], stimulation of basal glucose uptake and glucose transporter-4 translocation in muscle cells [14], treatment of dyslipidemia and hyperglycemia in high-fat diet-induced obese mice via activation of Akt and 5′-adenosine monophosphate-activated protein kinase in white adipose tissue [15], and antihypertensive effects in 2K1C hypertensive rats [16].…”

Section: Introductionmentioning

confidence: 99%

Inhibitory Effects of Dimethyllirioresinol, Epimagnolin A, Eudesmin, Fargesin, and Magnolin on Cytochrome P450 Enzyme Activities in Human Liver Microsomes

Kim

Kwon

Jeong

et al. 2017

IJMS

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Magnolin, epimagnolin A, dimethyllirioresinol, eudesmin, and fargesin are pharmacologically active tetrahydrofurofuranoid lignans found in Flos Magnoliae. The inhibitory potentials of dimethyllirioresinol, epimagnolin A, eudesmin, fargesin, and magnolin on eight major human cytochrome P450 (CYP) enzyme activities in human liver microsomes were evaluated using liquid chromatography-tandem mass spectrometry to determine the inhibition mechanisms and inhibition potency. Fargesin inhibited CYP2C9-catalyzed diclofenac 4′-hydroxylation with a Ki value of 16.3 μM, and it exhibited mechanism-based inhibition of CYP2C19-catalyzed [S]-mephenytoin 4′-hydroxylation (Ki, 3.7 μM; kinact, 0.102 min−1), CYP2C8-catalyzed amodiaquine N-deethylation (Ki, 10.7 μM; kinact, 0.082 min−1), and CYP3A4-catalyzed midazolam 1′-hydroxylation (Ki, 23.0 μM; kinact, 0.050 min−1) in human liver microsomes. Fargesin negligibly inhibited CYP1A2-catalyzed phenacetin O-deethylation, CYP2A6-catalyzed coumarin 7-hydroxylation, CYP2B6-catalyzed bupropion hydroxylation, and CYP2D6-catalyzed bufuralol 1′-hydroxylation at 100 μM in human liver microsomes. Dimethyllirioresinol weakly inhibited CYP2C19 and CYP2C8 with IC50 values of 55.1 and 85.0 μM, respectively, without inhibition of CYP1A2, CYP2A6, CYP2B6, CYP2C9, CYP2D6, and CYP3A4 activities at 100 μM. Epimagnolin A, eudesmin, and magnolin showed no the reversible and time-dependent inhibition of eight major CYP activities at 100 μM in human liver microsomes. These in vitro results suggest that it is necessary to investigate the potentials of in vivo fargesin-drug interaction with CYP2C8, CYP2C9, CYP2C19, and CYP3A4 substrates.

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Fargesin exerts anti-inflammatory effects in THP-1 monocytes by suppressing PKC-dependent AP-1 and NF-ĸB signaling

Cited by 66 publications

References 28 publications

Elucidation of The Anti‐Inflammatory Effect of Vanillin In Lps‐Activated THP‐1 Cells

Elucidation of The Anti‐Inflammatory Effect of Vanillin In Lps‐Activated THP‐1 Cells

Epimagnolin A inhibits IL‐6 production by inhibiting p38/NF‐κB and AP‐1 signaling pathways in PMA‐stimulated THP‐1 cells

Inhibitory Effects of Dimethyllirioresinol, Epimagnolin A, Eudesmin, Fargesin, and Magnolin on Cytochrome P450 Enzyme Activities in Human Liver Microsomes

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