Phloroglucinol and dieckol isolated from Ecklonia cava suppress impaired diabetic angiogenesis; A study of in-vitro and in-vivo

Hwang, Jin; Yang, Hye-Won; Lu, Yu; Je, Jun-Geon; Lee, Hyo-Geun; Fernando, K.H.N.; Jeon, You‐Jin; Ryu, BoMi

doi:10.1016/j.biopha.2021.111431

Cited by 6 publications

(5 citation statements)

References 24 publications

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“…The interaction sites and energy values of VEGFRs, as modeled through in silico molecular docking simulations, have been explored in investigations into inhibitors to prevent or downregulate the signaling involved in angiogenesis-related eye diseases. As VEGFR inhibitors, several phenolic compounds or inhibitors with a metal-chelating ability have been widely studied in experimental and computational fields [ 57 ]. Our in silico results showed that IPA had the greatest binding energy with VEGFR2 among the VEGFRs, even benzimidazole urea, as a VEGFR2 antagonist ( Figure 3 A–C and Figure S2 ).…”

Section: Discussionmentioning

confidence: 99%

Ishophloroglucin A Ameliorates VEGF-Induced Epithelial-Mesenchymal Transition via VEGFR2 Pathway Inhibition in Microgravity-Stimulated Human Retinal Pigment Epithelial Cells

Son

Ryu

et al. 2022

Antioxidants

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Microgravity stimulation is associated with retinal pigment epithelial (RPE) cells that transition to mesenchymal cells (EMT), and these pathological changes cause visual impairment. Vascular endothelial growth factor (VEGF) is produced from the RPE and contributes to photoreceptor survival. However, changes in VEGF production and function under microgravity stimulation are unknown. In this study, we verified that microgravity stimulation changed the morphological characteristics of human RPE cells (ARPE19 cells) and the expression of actin cytoskeleton regulators, which are related to excessive VEGF expression. Interestingly, microgravity stimulation increased not only the production of VEGF but also the expression of EMT markers. Previously, we studied the potential of ishophloroglucin A (IPA), a phlorotannin, as an antioxidant. In silico results confirmed that IPA could structurally bind to VEGF receptor 2 (VEGFR2) among VEGFRs and inhibit the VEGF pathway. IPA significantly decreased VEGF production and EMT marker expression in microgravity-stimulated cells. It also significantly reduced excessive cell migration in VEGF-induced EMT. Overall, our findings suggested that IPA treatment decreased VEGF production and EMT marker expression in microgravity-stimulated or VEGF-treated ARPE19 cells, and this decrease in EMT could restore excessive cell migration by inhibiting the VEGF/VEGFR2 pathway. Therefore, it is a potential therapeutic candidate for angiogenesis-related eye diseases.

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Section: Discussionmentioning

confidence: 99%

Ishophloroglucin A Ameliorates VEGF-Induced Epithelial-Mesenchymal Transition via VEGFR2 Pathway Inhibition in Microgravity-Stimulated Human Retinal Pigment Epithelial Cells

Son

Ryu

et al. 2022

Antioxidants

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“…Cho et al [25] found that dieckol isolated from E. cava inhibited advanced glycation end products associated with the pathogenesis of diabetic nephropathy in mouse glomerular mesangial cells, suggesting dieckol might have the potential to treat diabetic nephropathy in humans. A related study by Hwang et al [26] reported that phloroglucinol and dieckol suppressed angiogenesis in diabetic vascular complications. Almutairi et al [27] reported that administering 600 mg of polyphenolic-rich E. cava extract to 20 Saudi Arabian prediabetic patients for up to 120 min reduced the postprandial blood glucose level with no associated side effects.…”

Section: Colored Corn Floursmentioning

confidence: 94%

Composition of Flatbreads Prepared from Blue, Red, Yellow, and White Corn Flours Supplemented with Edible Ecklonia cava Algae: Relationship to Health Benefits

2024

Food Nutr J

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The objective of the present study was to determine the composition of flatbreads prepared from corn and wheat flours supplemented with edible Ecklonia cava, which is a health-promoting medicinal food used as a dietary supplement. The Corn flours used were Whole Blue, Purcell Whole Blue, Purcell Whole Red, Purcell Whole Yellow, Purcell Whole White and Giant White and King Arthur Whole Wheat. Because the colored corn flours are reported to contain health-promoting anthocyanins and the Ecklonia alga contains multiple biologically active polyphenolic and other health-promoting compounds reported to show anti-asthma, anti-cancer, anti-diabetes, antimicrobial, anti-neurotoxicity, anti-obesity, and cardioprotective effects, the resulting flatbreads have the potential for multiple health benefits in humans after consumption. To facilitate the development of the newly created flatbreads for consumption, we determined, using standard methods, the effect of added E. cava on the proximate composition of protein, fat, carbohydrate, dry matter, ash (mineral), and water content of the flatbreads. The unexpected results, for which we have no explanation, show that the measured protein, mineral, and water content of the E. cava-supplemented flatbreads increased, whereas the fat, carbohydrate, and dry matter contents of the E. cava-supplemented flatbreads decreased compared to un-supplemented ones, suggesting that consumers will be able to select flatbreads with a high-protein and low-fat content.

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“…Hwang et al ( 2021 ) studied the effect of phloroglucinol and dieckol on inhibiting angiogenesis under high glucose conditions. In silico docking study revealed that both the compounds had strong binding affinity towards the antiangiogenic receptor,vascular endothelial growth factor VEFGR and thereby helped in inhibiting the endothelial cell proliferation, migration and vascular formation.…”

Section: Broader Applications Of Phlorotanninsmentioning

confidence: 99%

Phlorotannins–bioactivity and extraction perspectives

et al. 2022

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Phlorotannins, a seaweed based class of polyphenolic compounds, have proven to possess potential bioactivities such as antioxidant, antimicrobial, anti-allergic, anti-diabetic, anti-inflammatory, anti-cancerous, neuroprotection etc. These bioactivities have further increased demand globally and sustainable techniques such as supercritical fluid extraction, microwave assisted extraction, enzyme assisted extraction, extraction using deep eutectic solvents etc. are being explored currently for production of phlorotannin-rich extracts. In spite of such well documented bioactivities, very few phlorotannin-based nutraceuticals are available commercially which highlights the significance of generating consumer awareness about their physiological benefits. However, for industry level commercialization accurate quantification of phlorotannins with respect to the different classes is vital requiring sophisticated analytical techniques such as mass spectrometry, 1 H-NMR spectroscopy etc. owing to the wide structural diversity. This review summarizes the extraction and bioactivities of phlorotannins based on the findings of in vivo and in vitro studies.

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Phloroglucinol and dieckol isolated from Ecklonia cava suppress impaired diabetic angiogenesis; A study of in-vitro and in-vivo

Cited by 6 publications

References 24 publications

Ishophloroglucin A Ameliorates VEGF-Induced Epithelial-Mesenchymal Transition via VEGFR2 Pathway Inhibition in Microgravity-Stimulated Human Retinal Pigment Epithelial Cells

Ishophloroglucin A Ameliorates VEGF-Induced Epithelial-Mesenchymal Transition via VEGFR2 Pathway Inhibition in Microgravity-Stimulated Human Retinal Pigment Epithelial Cells

Composition of Flatbreads Prepared from Blue, Red, Yellow, and White Corn Flours Supplemented with Edible Ecklonia cava Algae: Relationship to Health Benefits

Phlorotannins–bioactivity and extraction perspectives

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