Nanoparticle-Delivered Quercetin for Cancer Therapy

Men, Ke; Duan, Xingmei; Wei, Xing; Gou, Ma Ling; Huang, Mei; Chen, Li Juan; Qian, Zhi; Wei, Yu Quan

doi:10.2174/1871520614666140521122932

Cited by 50 publications

(28 citation statements)

References 63 publications

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“…When considering dietary sources, onions seem a good source as regards quantity and bioavailability [Lee and Mitchell, ]. In view of the low bioavailability arising from low aqueous solubility and intestinal absorption, one of the approaches that is being explored to improve flavonol bioavailabilty is delivery in a nanoparticle form [Men et al, ; Tran et al, ].…”

Section: Absorption and Bioavailabilitymentioning

confidence: 99%

Flavonol Regulation in Tumor Cells

Lea¹

2015

J of Cellular Biochemistry

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Flavonols comprise a group of flavonoid molecules that are widely distributes in fruits and vegetables. There is epidemiological data to suggest that consumption of flavonols can be accompanied by decreased cancer incidence. The anti-oxidant activity of flavonols may have an important role in preventing carcinogenesis. Therapeutic potential of flavonols is indicated by their growth inhibitory action accompanied by a decrease in several hallmarks of cancer such as resistance to apoptosis. Multiple mechanisms of action have been reported for the action of flavonols on cancer cells. Particular emphasis has been directed to inhibitory effects on several protein kinases and on the potential for prooxidant effects. The diversity of actions presents a problem in trying to elucidate primary and secondary effects but it may be a strength of the therapeutic potential of flavonols that it renders development of resistance more difficult for cancer cells. Cancer chemotherapy is usually characterized by the use of drug combinations. Some additive or synergistic combinations have been identified for flavonols and this is an area of ongoing investigation. As with other polyphenolic molecules there have been questions of cellular uptake and bioavailability. Several investigations have been and are being conducted to modify the structures of flavonols with the goal of increasing bioavailability. At present many investigators are sufficiently encouraged by past observations that they are responding to the challenge to optimize the dietary and therapeutic use of flavonols in cancer prevention and treatment.

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Section: Absorption and Bioavailabilitymentioning

confidence: 99%

Flavonol Regulation in Tumor Cells

Lea¹

2015

J of Cellular Biochemistry

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“…NPs have also been used as drug delivery systems that enable unique approaches for tuberculosis treatment (Gelperina et al , ). In medical applications, the vast majority of studies have focused on fighting cancer using NPs (Alexis et al , ; Hallaj‐Nezhadi et al , ; Chatterjee et al , ; Miele et al , ; Men et al , ).…”

Section: Introductionmentioning

confidence: 99%

The effect of Fe₂O₃ and ZnO nanoparticles on cytotoxicity and glucose metabolism in lung epithelial cells

Lai

Wei

Zhao

et al. 2015

J of Applied Toxicology

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Metallic nanoparticles (NPs) have potential applications in industry and medicine, but they also have the potential to cause many chronic pulmonary diseases. Mechanisms for their cytotoxicity, glucose and energy metabolism responses need to be fully explained in lung epithelial cells after treatment with metallic nanoparticles. In our study, two different metallic nanoparticles (Fe2O3 and ZnO) and two cell‐based assays (BEAS‐2B and A549 cell lines) were used. Our findings demonstrate that ZnO nanoparticles, but not Fe2O3 nanoparticles, induce cell cycle arrest, cell apoptosis, reactive oxygen species (ROS) production, mitochondrial dysfunction and glucose metabolism perturbation, which are responsible for cytotoxicity. These results also suggest that the glucose metabolism and bioenergetics had a great potential in evaluating the cytotoxicity and thus were very helpful in understanding their underlying molecular mechanisms. Copyright © 2015 John Wiley & Sons, Ltd.

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“…25,29,30 Our results indicated that raw eupafolin may blend together with Eudragit E100 in the alcohol as hydrophobic phase, and then the hydrophilic end of PVA as an emulsion stabilizer can interpenetrate them during the nanoprecipitation process to finally form nanoparticles with reproducible size and uniform distribution; 2) The conversion of crystalline structure Figure 8 Eupafolin nanoparticle delivery system (ENDS) inhibited the activation of MAPKs in PM-stimulated HaCaT keratinocytes. Notes: (A-C) Effects of specific NADPH oxidase inhibitor apocynin (APO, 100 µM), antioxidant N-acetylcysteine (NAC, 100 µM), specific MAPK inhibitors (10 µM U0126, SB202190, and SP600125), ENDS (10 µM), and raw eupafolin (10 µM) on the phosphorylation status of (A) ERK, (B) p38, and (C) JNK in HaCaT keratinocytes stimulated with PM (50 µg cm −2 ) for 4 hours, as determined by Western blotting.…”

Section: Discussionmentioning

confidence: 82%

“…24 However, the chemical structure of flavonoids, such as quercetin and naringenin, has also limited their administration and application in clinical medicine, due to their extremely low water solubility and poor bioavailability. 25,26 Eupafolin has a similar flavone backbone structure and displays poor water solubility, resulting in poor cutaneous penetration following topical administration on skin. Therefore, many studies have attempted to develop nanoparticle delivery systems using nanoprecipitation and high pressure homogenization techniques to overcome the physicochemical drawbacks of the active compounds 27,28 and thereby improve their solubility and skin absorption.…”

Section: Introductionmentioning

confidence: 99%

Eupafolin nanoparticles protect HaCaT keratinocytes from particulate matter-induced inflammation and oxidative stress

Lin

Lee²,

Tsai

et al. 2016

IJN

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Exposure to particulate matter (PM), a major form of air pollution, can induce oxidative stress and inflammation and may lead to many diseases in various organ systems including the skin. Eupafolin, a flavonoid compound derived from Phyla nodiflora , has been previously shown to exhibit various pharmacological activities, including antioxidant and anti-inflammatory effects. Unfortunately, eupafolin is characterized by poor water solubility and skin penetration, which limits its clinical applications. To address these issues, we successfully synthesized a eupafolin nanoparticle delivery system (ENDS). Our findings showed that ENDS could overcome the physicochemical drawbacks of raw eupafolin with respect to water solubility and skin penetration, through reduction of particle size and formation of an amorphous state with hydrogen bonding. Moreover, ENDS was superior to raw eupafolin in attenuating PM-induced oxidative stress and inflammation in HaCaT keratinocytes, by mediating the antioxidant pathway (decreased reactive oxygen species production and nicotinamide adenine dinucleotide phosphate oxidase activity) and anti-inflammation pathway (decreased cyclooxygenase-2 expression and prostaglandin E2 production through downregulation of mitogen-activated protein kinase and nuclear factor-κB signaling). In summary, ENDS shows better antioxidant and anti-inflammatory activities than raw eupafolin through improvement of water solubility and skin penetration. Therefore, ENDS may potentially be used as a medicinal drug and/or cosmeceutical product to prevent PM-induced skin inflammation.

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Nanoparticle-Delivered Quercetin for Cancer Therapy

Cited by 50 publications

References 63 publications

Flavonol Regulation in Tumor Cells

Flavonol Regulation in Tumor Cells

The effect of Fe₂O₃ and ZnO nanoparticles on cytotoxicity and glucose metabolism in lung epithelial cells

Eupafolin nanoparticles protect HaCaT keratinocytes from particulate matter-induced inflammation and oxidative stress

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Nanoparticle-Delivered Quercetin for Cancer Therapy

Cited by 50 publications

References 63 publications

Flavonol Regulation in Tumor Cells

Flavonol Regulation in Tumor Cells

The effect of Fe2O3 and ZnO nanoparticles on cytotoxicity and glucose metabolism in lung epithelial cells

Eupafolin nanoparticles protect HaCaT keratinocytes from particulate matter-induced inflammation and oxidative stress

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Product

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The effect of Fe₂O₃ and ZnO nanoparticles on cytotoxicity and glucose metabolism in lung epithelial cells