In vitro: The Modulating Effect of Myricetin on the Atherosclerosis Related Processes in THP1 Macrophages

Almassabi, Rehab; Huwait, Etimad; Almowallad, Sanaa; Saddeek, Salma; Gauthaman, Kalamegam

doi:10.9734/jpri/2020/v32i4731116

Cited by 4 publications

(2 citation statements)

References 30 publications

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“…In our docking results, fucoidan was found to be attached to ABCA1 ECD2 at Ser1540, Thr1542, and Thr1586, which suggests that it can form O-linked glycosylation, increasing ABCA1 stability and leading to regulated cholesterol efflux. Previous studies assessed cholesterol efflux in the presence or absence of extracellular acceptors following treatment with bioactive substances in the THP-1 macrophage model [26,51,52] without taking into account the kinetics of cholesterol efflux. Therefore, further studies are required to evaluate the kinetics of cholesterol efflux in a time-dependent manner.…”

Section: Discussionmentioning

confidence: 99%

Atheroprotective Effect of Fucoidan in THP-1 Macrophages by Potential Upregulation of ABCA1

Mirza,

Al-Saedi,

Saddeek

et al. 2023

Biomedicines

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Targeting foam cells reduces the risk and pathophysiology of atherosclerosis, of which they are one of its early hallmarks. The precise mechanism of action of fucoidan, a potential anti-atherogenic drug, is still unknown. Our objective was to assess the ability of fucoidan to regulate expression of ATP-binding cassette transporter A1 (ABCA1) in ox-LDL-induced THP-1 macrophages. Molecular docking was used to predict how fucoidan interacts with anti-foam cell markers, and further in vitro experiments were performed to evaluate the protective effect of fucoidan on modulating uptake and efflux of lipids. THP-1 macrophages were protected by 50 µg/mL of fucoidan and were then induced to form foam cells with 25 µg/mL of ox-LDL. Expression levels were assessed using RT-qPCR, and an Oil Red O stain was used to observe lipid accumulation in THP-1 macrophages. In addition, ABCA1 protein was examined by Western blot, and cellular cholesterol efflux was determined using fluorescently labeled cholesterol. Under a light microscope, decreased lipid accumulation in ox-LDL-induced-THP-1 macrophages pre-treated with fucoidan showed a significant effect, although it did not affect the expression of scavenger receptors (SR-AI and CD36). It is interesting to note that fucoidan dramatically increased the gene and protein expression of ABCA1, perhaps via the liver X receptor-α (LXR-α). Moreover, fucoidan’s ability to increase and control the efflux of cholesterol from ox-LDL-induced THP-1 macrophages revealed how it may alter ABCA1’s conformation and have a major effect on how it interacts with apolipoprotein A (ApoA1). In vitro results support a rationale for predicting fucoidan and its interaction with its receptor targets’ predicted data, hence validating its anti-atherogenic properties and suggesting that fucoidan could be promising as an atheroprotective.

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Section: Discussionmentioning

confidence: 99%

Atheroprotective Effect of Fucoidan in THP-1 Macrophages by Potential Upregulation of ABCA1

Mirza,

Al-Saedi,

Saddeek

et al. 2023

Biomedicines

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“…Cholesterol efflux assay was performed using the commercial Cholesterol Efflux Assay kit as previously described (Almowallad et al, 2020;Almassabi et al, 2021) to analyze the impact of quercetin on AS progression in our cellular model. THP-1 monocytes were seeded at a density of 1 × 10 5 cells/well in the culture medium (100 μl media/well) in a 96well black plate with a clear bottom (kit content) and incubated for 1 h to settle down.…”

Section: Cholesterol Efflux Assaymentioning

confidence: 99%

Antiatherogenic Effects of Quercetin in the THP-1 Macrophage Model In Vitro, With Insights Into Its Signaling Mechanisms Using In Silico Analysis

et al. 2021

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Background: Atherosclerosis (AS), a major risk factor for stroke and brain tissue destruction, is an inflammatory disease of the blood vessels, and the underlying pathology is inflammation mediated by various chemokines and cytokines. Quercetin, a natural flavonol, is reported to have both anti-inflammatory and antioxidant properties. As such, in the present study, we evaluated the antiatherogenic effects of quercetin in a human THP-1 cell line in vitro and also the signaling mechanisms using in silico analysis.Materials and Methods: THP-1 macrophages exposed to different concentrations of quercetin (5–100 μM for 24 h) were tested for cytotoxicity. Real-time gene expression assay for intercellular adhesion molecule-1 (ICAM-1) and monocyte chemoattractant protein-1 (MCP-1) was carried out following treatment with quercetin at 15 and 30 μM for 24 h either in the absence or presence of interferon (IFN-γ) for 3 h to induce inflammation. Monocyte migration and cholesterol efflux were also assessed.Results: Quercetin did not exert any cytotoxic effects on THP-1 cells at the various concentrations tested. The gene expression assay showed a significant decrease in ICAM-1 (by 3.05 and 2.70) and MCP-1 (by 22.71 and 27.03), respectively. Quercetin at 15 µM decreased THP-1 monocyte migration by 33% compared to the MCP-1-treated cells. It also increased cholesterol efflux significantly by1.64-fold and 1.60-fold either alone or in combination with IFN-γ, respectively. Ingenuity Pathway Analysis of the molecular interactions of quercetin identified canonical pathways directly related to lipid uptake and cholesterol efflux. Furthermore, CD36, SR-A, and LXR-α also demonstrated significant increases by 72.16-, 149.10-, and 29.68-fold, respectively.Conclusion: Our results from both in vitro and in silico studies identified that quercetin inhibited the THP-1 monocyte migration, MCP-1, and ICAM-1 and increased cholesterol efflux probably mediated via the LXR/RXR signaling pathway. Therefore, quercetin will help prevent cell infiltration in atherosclerotic plaques and reduce the risk of stroke or brain destruction.

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Anti-inflammatory potential of myricetin in leukemia cells: in silico and in vitro exploration

Nishad,

Usha,

Kumar

et al. 2024

ADV TRADIT MED (ADTM)

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In vitro: The Modulating Effect of Myricetin on the Atherosclerosis Related Processes in THP1 Macrophages

Cited by 4 publications

References 30 publications

Atheroprotective Effect of Fucoidan in THP-1 Macrophages by Potential Upregulation of ABCA1

Atheroprotective Effect of Fucoidan in THP-1 Macrophages by Potential Upregulation of ABCA1

Antiatherogenic Effects of Quercetin in the THP-1 Macrophage Model In Vitro, With Insights Into Its Signaling Mechanisms Using In Silico Analysis

Anti-inflammatory potential of myricetin in leukemia cells: in silico and in vitro exploration

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