Liposomal Quercetin Efficiently Suppresses Growth of Solid Tumors in Murine Models

Yuan, Zhiping; Chen, Lijuan; Fan, Lijun; Tang, Minghai; Yang, Guangli; Yang, Han-su; Du, Xiaobo; Wang, Guoqing; Yao, Wenxiu; Zhao, Qu-mei; Ye, Bin; Wang, Rui; Diao, Peng; Zhang, Wei; Wu, H. C.; Zhao, Xia; Wei, Yuquan

doi:10.1158/1078-0432.ccr-05-2365

Cited by 231 publications

(181 citation statements)

References 30 publications

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“…The concentrations of quercetin used in our experiments are not dramatically higher than the concentrations that could be achieved in the plasma after oral administration of dietary supplements or indeed dietary components (26,27).…”

Section: Discussionmentioning

confidence: 69%

Quercetin enhances TRAIL-mediated apoptosis in colon cancer cells by inducing the accumulation of death receptors in lipid rafts

Psahoulia

Drosopoulos²,

Doubravská³

et al. 2007

Molecular Cancer Therapeutics

161

103

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Cytokines such as tumor necrosis factor-related apoptosisinducing ligand (TRAIL) can induce apoptosis in colon cancer cells through engagement of death receptors. Nevertheless, evading apoptosis induced by anticancer drugs characterizes many types of cancers. This results in the need for combination therapy. In this study, we have investigated whether the flavonoid quercetin could sensitize human colon adenocarcinoma cell lines to TRAIL-induced apoptosis. We report that quercetin enhanced TRAILinduced apoptosis by causing the redistribution of DR4 and DR5 into lipid rafts. Nystatin, a cholesterol-sequestering agent, prevented quercetin-induced clustering of death receptors and sensitization to TRAIL-induced apoptosis in colon adenocarcinoma cells. In addition, our experiments show that quercetin, in combination with TRAIL, triggered the mitochondrial-dependent death pathway, as shown by Bid cleavage and the release of cytochrome c to the cytosol. Together, our findings propose that quercetin, through its ability to redistribute death receptors at the cell surface, facilitates death-inducing signaling complex formation and activation of caspases in response to death receptor stimulation. Based on these results, this study provides a challenging approach to enhance the efficiency of TRAILbased therapies. [Mol Cancer Ther 2007;6(9):2591-9]

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Section: Discussionmentioning

confidence: 69%

Quercetin enhances TRAIL-mediated apoptosis in colon cancer cells by inducing the accumulation of death receptors in lipid rafts

Psahoulia

Drosopoulos²,

Doubravská³

et al. 2007

Molecular Cancer Therapeutics

161

103

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“…On the other hand, quercetin can also elicit pro-oxidant effects [3]. A relationship has been demonstrated between the free radical scavenging activity and anti-carcinogenic and anti-inflammatory properties of quercetin [17,32]. Studies have been performed to evaluate the physiological functions and biological activities of quercetin in humans and animals [1,13].…”

Section: Introductionmentioning

confidence: 99%

Quercetin Improves In Vitro Development of Porcine Oocytes by Decreasing Reactive Oxygen Species Levels.

Kang

Kwon

Park

et al. 2011

Biology of Reproduction

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Quercetin is a plant-derived flavonoid found in fruits or vegetables that has antioxidant properties and acts as a free radical scavenger. We investigated the effects of quercetin on porcine oocyte nuclear maturation and embryonic development after parthenogenetic activation. We then evaluated the antioxidant activities of quercetin by measuring reactive oxygen species (ROS) levels in matured oocytes. Immature oocytes were untreated or treated with 1, 10, and 50 μg/mL quercetin during in vitro maturation (IVM). Quercetin treatment did not improve oocyte nuclear maturation, but significantly higher blastocyst rates (p ＜ 0.05) of parthenogenetically activated oocytes were achieved when the IVM medium was supplemented with an adequate concentration of quercetin (1 μg/mL). However, cleavage rates and blastocyst cell numbers were not affected. Oocytes treated with 1 or 10 μg/mL quercetin had significantly lower (p ＜ 0.05) levels of ROS than the control and group treated with the highest concentration of quercetin (50 μg/mL). Moreover, this highest concentration was detrimental to oocyte nuclear maturation and blastocyst formation. Based on our findings, we concluded that exogenous quercetin reduces ROS levels during oocyte maturation and is beneficial for subsequent embryo development.

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“…To address this challenge, the use of liposomes to encapsulate QU has been described. 32 Recently, MPEG-PCL micelles were used to load curcumin and honokiol, 28,33 successfully solving their water solubility. In this paper, MPEG-PCL micelles were used to encapsulate QU with the goal of improving the water solubility of QU and creating a novel formulation for QU.…”

Section: Discussionmentioning

confidence: 99%

Treating acute cystitis with biodegradable micelle-encapsulated quercetin

Gou¹,

Wang²

2012

IJN

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Intravesical application of an anti-inflammatory drug is an efficient strategy for acute cystitis therapy. Quercetin (QU) is a potent anti-inflammatory agent; however, its poor water solubility restricts its clinical application. In an attempt to improve water solubility of QU, biodegradable monomethoxy poly(ethylene glycol)-poly(ε-caprolactone) (MPEG-PCL) micelles were used to encapsulate QU by self-assembly methods, creating QU/MPEG-PCL micelles. These QU/MPEG-PCL micelles with DL of 7% had a mean particle size of ∼34 nm, and could release QU for an extended period in vitro. The in vivo study indicated that intravesical application of MPEG-PCL micelles did not induce any toxicity to the bladder, and could efficiently deliver cargo to the bladder. Moreover, the therapeutic efficiency of intravesical administration of QU/MPEG-PCL micelles on acute cystitis was evaluated in vivo. Results indicated that QU/ MPEG-PCL micelle treatment efficiently reduced the edema and inflammatory cell infiltration of the bladder in an Escherichia coli-induced acute cystitis model. These data suggested that MPEG-PCL micelle was a candidate intravesical drug carrier, and QU/MPEG-PCL micelles may have potential application in acute cystitis therapy.

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Liposomal Quercetin Efficiently Suppresses Growth of Solid Tumors in Murine Models

Cited by 231 publications

References 30 publications

Quercetin enhances TRAIL-mediated apoptosis in colon cancer cells by inducing the accumulation of death receptors in lipid rafts

Quercetin enhances TRAIL-mediated apoptosis in colon cancer cells by inducing the accumulation of death receptors in lipid rafts

Quercetin Improves In Vitro Development of Porcine Oocytes by Decreasing Reactive Oxygen Species Levels.

Treating acute cystitis with biodegradable micelle-encapsulated quercetin

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