Structure–Activity Relationship (SAR) of Flavones on Their Anti-Inflammatory Activity in Murine Macrophages in Culture through the NF-κB Pathway and c-Src Kinase Receptor

Wang, Xiang; Cao, Yujia; Chen, Siyu; Lin, Jiachen; Yang, Xin; Huang, Dejian

doi:10.1021/acs.jafc.2c03050

Cited by 8 publications

(5 citation statements)

References 40 publications

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“…Numerous studies have attempted to explore the structure–activity relationship of flavonoids. − However, no clear conclusion has been reached so far, which may be due to insufficient investigation on the influence mechanism under specific systems. The results of our entire research indicated that for compounds with inherent lipid-lowering activity, the bioavailability, which manifests as stability and cellular uptake ratio, is the crucial condition that determines whether compounds can exert efficacy in cell experiments.…”

Section: Discussionmentioning

confidence: 99%

In Vitro Comparative Analysis of the Effect and Structure-Based Influencing Factors of Flavonols on Lipid Accumulation

Ang,

Yang,

Wang

et al. 2024

J. Agric. Food Chem.

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Flavonols represented by quercetin have been widely reported to have biological activities of regulating lipid metabolism. However, the differences in flavonols with different structures in lipid-lowering activity and the influencing factors remain unclear. In this study, the stability, transmembrane uptake ratio, and lipid metabolism regulation activities of 12 flavonol compounds in the 3T3-L1 cell model were systematically compared. The results showed that kaempferide had the highest cellular uptake ratio and the most potent inhibitory effect on adipogenesis at a dosing concentration of 20 μM, followed by isorhamnetin and kaempferol. They inhibited TG accumulation by more than 65% and downregulated the expression of PPARγ and SREBP1c by more than 60%. The other four aglycones, including quercetin, did not exhibit significant activity due to the structural instability in the cell culture medium. Meanwhile, five quercetin glucosides were quite stable but showed a low uptake ratio that no obvious activity was observed. Correlation analysis also showed that for 11 compounds except galangin, the activity was positively correlated with the cellular uptake ratio (p < 0.05, r = 0.6349). These findings may provide a valuable idea and insight for exploring the structure-based activity of flavonoids at the cellular level.

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Section: Discussionmentioning

confidence: 99%

In Vitro Comparative Analysis of the Effect and Structure-Based Influencing Factors of Flavonols on Lipid Accumulation

Ang,

Yang,

Wang

et al. 2024

J. Agric. Food Chem.

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“…The cellular inflammation induction model refers to previous research [ 32 ], RAW 264.7 mouse macrophages were cultured in DMEM containing fetal bovine serum, penicillin, and streptomycin (37 °C, 5% CO 2 ). Change the medium every 1–2 days and pass the passage every 2 days.…”

Section: Methodsmentioning

confidence: 99%

Study on the Cellular Anti-Inflammatory Effect of Torularhodin Produced by Sporidiobolus pararoseus ZQHL Isolated from Vinegar Fungus

Liu

Han

Lv³

et al. 2023

Molecules

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The red stretcher bacterium Sporidiobolus pararoseus is a high producer of carotenoids such as torularhodin, but its presence in vinegar has not been detected. Moreover, torularhodin has several biological activities, but its effect on the LPS-induced RAW 264.7 inflammatory cell model has also yet to be elucidated. In this study, S. pararoseus was identified in different vinegar samples from China by ITS sequencing. Meanwhile, one of the strains was deeply resolved by whole genome sequencing and functional annotation and named S. pararoseus ZQHL. Subsequently, the antioxidant effect of the fungal carotenoid torularhodin was investigated using in vitro DPPH, ABTS, and cellular models. Finally, LPS-induced RAW 264.7 cells were used as an inflammation model to assess torularhodin’s protective effect on inflammatory cells and to determine whether the TLR4 pathway is associated with this process. The results indicate that torularhodin has good free radical scavenging ability in vitro and can contribute to cell viability. More importantly, torularhodin alleviated LPS-induced cellular inflammatory damage and reduced the expression of inflammatory factors such as TLR4, MyD88, and TNF-a. The mechanism may attenuate the cellular inflammatory response by inhibiting the TLR4 inflammatory pathway. In conclusion, torularhodin produced by S. pararoseus fungi in vinegar samples significantly scavenged free radicals in vitro and alleviated RAW 264.7 cellular inflammation by modulating the TLR4 pathway.

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“…Human peripheral blood mononuclear cells (PBMCs) and TNBS-induced colitis rat IL-10, transforming growth factor (TGF)-β1, IL-2p70, forkhead box protein 3 (Foxp3) and Treg production [28,29] Caco-2 cells and TNBS-induced colitis mice IL-10 IL-12, interferon-γ (IFN-γ), IL-8 and NF-κB activation [19] DSS colitis C57BL/6 mice Claudin-1 and claudin-2 expressions Weight and colon length [30] Dinitrobenzene sulfonic acid (DNBS) -induced colitis mice…”

Section: Faecalibacterium Faecalibacterium Prausnitziimentioning

confidence: 99%

Understanding the mechanism underlying the anti-inflammatory effect of dietary flavonoids on IBD: a focus on gut microbiota and its metabolites involved in SCFA, bile acid, tryptophan and lipopolysaccharides

Xiong,

Chen,

Chen

et al. 2024

Food Science and Human Wellness

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Inflammatory bowel disease (IBD) is a chronic gastrointestinal disease with a high incidence. Treatment for IBD includes medications and diet, and common anti-inflammatory medications have limitations like drug resistance and serious adverse effects. Accumulating evidence has demonstrated that dietary flavonoids exhibit an alleviative effect on IBD by influencing gut microbiota. The microbiota-derived metabolites also regulate IBD and maintain intestinal homeostasis. In this review, we investigate the therapeutic effect of gut microbiota and metabolites on IBD by intestinal immune and intestinal barrier function. We demonstrate the underlying mechanism of dietary flavonoids as an anti-inflammatory molecule alleviating IBD by regulating gut microbiota, short chain fatty acid (SCFA), bile acid (BA), tryptophan (Trp) metabolism and lipopolysaccharides (LPS)-toll-like receptor 4 (TLR4) signaling pathway. Based on structural differences of flavonoids, we summarize the recent research progress on the role of different dietary flavonoids in alleviating IBD by gut microbiota and metabolites in animal and clinical trials. This review indicates that dietary flavonoids targeting gut microbiota and metabolites provide a promising strategy for the treatment of inflammation and novel insights into the management of IBD.

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Structure–Activity Relationship (SAR) of Flavones on Their Anti-Inflammatory Activity in Murine Macrophages in Culture through the NF-κB Pathway and c-Src Kinase Receptor

Cited by 8 publications

References 40 publications

In Vitro Comparative Analysis of the Effect and Structure-Based Influencing Factors of Flavonols on Lipid Accumulation

In Vitro Comparative Analysis of the Effect and Structure-Based Influencing Factors of Flavonols on Lipid Accumulation

Study on the Cellular Anti-Inflammatory Effect of Torularhodin Produced by Sporidiobolus pararoseus ZQHL Isolated from Vinegar Fungus

Understanding the mechanism underlying the anti-inflammatory effect of dietary flavonoids on IBD: a focus on gut microbiota and its metabolites involved in SCFA, bile acid, tryptophan and lipopolysaccharides

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