Development of organogel-based emulsions to enhance the loading and bioaccessibility of 5-demethylnobiletin

Zhang, Man; Pan, Yijun; Dong, Qiaoru; Tang, Xudong; Xin, Yanping; Yin, Baoer; Zhu, Jieyu; Kou, Xingran; Ho, Chi Tang

doi:10.1016/j.foodres.2021.110592

Cited by 17 publications

(10 citation statements)

References 36 publications

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“…5-Demethyl NOB is a PMF, like other flavonoids, and possesses a poor solubility and bioavailability in vivo. To improve the bioactivity of 5-demethyl NOB in vivo, novel systems for delivery or chemical modification may enhance its solubility and achieve the concentration used in this study [48][49][50][51].…”

Section: Discussionmentioning

confidence: 99%

5-Demethylnobiletin Inhibits Cell Proliferation, Downregulates ID1 Expression, Modulates the NF-κB/TNF-α Pathway and Exerts Antileukemic Effects in AML Cells

Chen

Wang

Tsao

et al. 2022

IJMS

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Acute myeloid leukemia (AML) is characterized by the dysregulation of hematopoietic cell proliferation, resulting in the accumulation of immature myeloid cells in bone marrow. 5-Demethylnobiletin (5-demethyl NOB), a citrus 5-hydroxylated polymethoxyflavone, has been reported to exhibit various bioactivities, such as antioxidant, anti-inflammatory and anticancer properties. In this study, we investigated the antileukemic effects of 5-demethyl NOB and its underlying molecular mechanisms in human AML cells. We found that 5-demethyl NOB (20–80μM) significantly reduced human leukemia cell viability, and the following trend of effectiveness was observed: THP-1 ≈ U-937 > HEL > HL-60 > K562 cells. 5-Demethyl NOB (20 and 40μM) modulated the cell cycle through the regulation of p21, cyclin E1 and cyclin A1 expression and induced S phase arrest. 5-Demethyl NOB also promoted leukemia cell apoptosis and differentiation. Microarray-based transcriptome, Gene Ontology (GO) and Gene Set Enrichment Analysis (GSEA) of differentially expressed genes (DEGs) analysis showed that the expression of inhibitor of differentiation/DNA binding 1 (ID1), a gene associated with the GO biological process (BP) cell population proliferation (GO: 0008283), was most strongly suppressed by 5-demethyl NOB (40μM) in THP-1 cells. We further demonstrated that 5-demethyl NOB-induced ID1 reduction was associated with the inhibition of leukemia cell growth. Moreover, DEGs involved in the hallmark gene set NF-κB/TNF-α signaling pathway were markedly enriched and downregulated by 5-demethyl NOB. Finally, we demonstrated that 5-demethyl NOB (20 and 40μM), combined with cytarabine, synergistically reduced THP-1 and U-937 cell viability. Our current findings support that 5-demethyl NOB dramatically suppresses leukemia cell proliferation and may serve as a potential phytochemical for human AML chemotherapy.

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Section: Discussionmentioning

confidence: 99%

5-Demethylnobiletin Inhibits Cell Proliferation, Downregulates ID1 Expression, Modulates the NF-κB/TNF-α Pathway and Exerts Antileukemic Effects in AML Cells

Chen

Wang

Tsao

et al. 2022

IJMS

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“…For example, improved concentrations of malvidin-3-O-glucoside and its metabolites, such as syringic acid, in human urine delivered by zein nanoparticles were successfully determined by high-performance liquid chromatography with tandem mass spectrometry (HPLC− MS/MS). 46 By introduction of the stable isotopic tracers, such as 2 H, 13 C, 15 N, 18 O, and 34 S, analysis of the metabolic pathway was achieved by investigating microbial biotransformation of [2′,3′,5′,6′-D 4 ]-naringin (D 4 -naringin) in the human gut. 47 Despite the benefits of the diverse analytical techniques, there are still some problems limiting their application to the metabolism evaluation of encapsulated phytochemicals: (1) phytochemical degradation during sample preparation, (2) lacking commercial metabolite standards for identification, (3) requiring higher sensitivity and resolution of MS for detection of analytes in the trace level, (4) lacking synthesis technologies for better application of stable isotope labeling.…”

Section: Profiles Using Static and Dynamic Modelsmentioning

confidence: 99%

“…Although dynamic models resemble digestion more approximately to the human body, their application is not common in nanoencapsulated phytochemicals. Available studies show that TIM-1 is most often used to evaluate lipid-based delivery systems, such as Pickering emulsions, organogel-based emulsions, nanoemulsions, and oil suspensions. , One possible reason for the lack of application is the low loading capacity in some nanoencapsulation systems, like nanoparticles . Considering the diluting effect from using a large amount of buffer and enzyme secretion fluid in TIM-1, high loading of phytochemicals is required to achieve detectable levels after digestion.…”

Section: Investigating Release and Digestion Profiles Using Static An...mentioning

confidence: 99%

Assessment of Digestion, Absorption, and Metabolism of Nanoencapsulated Phytochemicals Using In Vitro and In Vivo Models: A Perspective Paper

Zheng

Yin

2022

J. Agric. Food Chem.

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Nanoencapsulation delivery systems have been used to enhance the absorption and bioefficacy of phytochemicals. With modified physical and chemical properties, nanoencapsulated phytochemicals differ from their free forms in digestion, absorption, and metabolism. These pharmacokinetic processes can be assessed using a combination of various in vitro/in vivo models and analytical strategies, but each approach has its limitations. The correlation between current models and physiological conditions and their feasibility for nanoencapsulation systems require further validation. More detailed studies are still needed to clarify how nanoencapsulation affects the phytochemical and host interaction. Future investigations must take extra caution in model selection and result interpretation.

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“…For example, Sawalha et al [8] developed an emulsion based in organogels fusing several sterols. Zhang et al [9] developed a gelled emulsion with medium chain triacylglycerols, water, and several surfactants (Span 20 [sorbitan monolaurate], Span 40 [sorbitan monopalmitate], Span 60 [sorbitan monostearate], Span 80 [sorbitan monooleate], and Tween 80 [polyoxyethylene sorbitan monooleate], Sugar ester [sucrose stearic acid ester, S370]) in order to enhance the loading and bioaccessibility of 5-demethylnobiletin. Candelilla wax and monoglyceride have been used to produce safflower oil high in oleic acid and water (20%) emulsions.…”

Section: Introductionmentioning

confidence: 99%

A Water in Oil Gelled Emulsion as a Topical Release Vehicle for Curcumin

et al. 2022

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The objective of this work is to assess the influence of the concentration of polyglycerol polyricinoleate (PGPR) (at 1%, 1.5%, and 2%) on the physical properties of water in oil gelled emulsions (W/O) and evaluates their efficiency as a delivery vehicle for curcumin. Emulsions are characterized by drop size, centrifugal test, texture, and rheology during 28 days of storage. When the surfactant concentration increases, smaller droplet sizes are obtained (<5 µm), the phase separation (tested by centrifugal force) decreases from 6% to 4% with little variation of the time. The mechanical properties of emulsions show a tendency to decrease as time passed and concentration of PGPR increased. The emulsions increased viscosity as the concentration increased, but the addition of curcumin reduce the viscosity of the emulsions. About controlled release profiles, a low concentration of PGPR shows an increase in the affinity between curcumin and the emulsions, following a pseudo‐Fickian release behavior. At higher concentration of PGPR shows a decrease in the affinity between curcumin and the emulsion, displaying a Fickian release behavior. The authors were able to prepare tailor made curcumin water in oil emulsion systems for the topical release of this compound.

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Development of organogel-based emulsions to enhance the loading and bioaccessibility of 5-demethylnobiletin

Cited by 17 publications

References 36 publications

5-Demethylnobiletin Inhibits Cell Proliferation, Downregulates ID1 Expression, Modulates the NF-κB/TNF-α Pathway and Exerts Antileukemic Effects in AML Cells

5-Demethylnobiletin Inhibits Cell Proliferation, Downregulates ID1 Expression, Modulates the NF-κB/TNF-α Pathway and Exerts Antileukemic Effects in AML Cells

Assessment of Digestion, Absorption, and Metabolism of Nanoencapsulated Phytochemicals Using In Vitro and In Vivo Models: A Perspective Paper

A Water in Oil Gelled Emulsion as a Topical Release Vehicle for Curcumin

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