Antiproliferative effects of quercetin through cell cycle arrest and apoptosis in human breast cancer MDA-MB-453 cells

Choi, Eun Jeong; Bae, Su Mi; Ahn, Woong Shick

doi:10.1007/s12272-001-2107-0

Cited by 147 publications

(93 citation statements)

References 34 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…The prooxidant activity of quercetin is now becoming accepted as contributing to cancer chemotherapy and inhibition of tumor growth, and increasing evidence suggests that quercetin shows specific inhibition of cancer cell growth (17)(18)(19). Consistent with that finding, our report indicated that quercetin significantly inhibited cellular proliferation and induced cell cycle arrest and apoptosis in human breast cancer in vivo (20) and in vitro (21).…”

Section: Introductionsupporting

confidence: 86%

Quercetin acts as an antioxidant and downregulates CYP1A1 and CYP1B1 against DMBA-induced oxidative stress in mice

Choi

Kim

2012

Oncol Rep

View full text Add to dashboard Cite

Abstract. We investigated the effects of quercetin on 7,12-dimethylbenz(a)anthracene (DMBA)-induced oxidative stress and the expression of CYP1A1 and CYP1B1 in mice. Quercetin was administered orally to mice at 100 or 250 mg/kg BW for 18 days, after which DMBA (34 mg/kg BW) was administered intragastrically twice. Quercetin showed side effects such as increased aspartate aminotransferase (AST) and alanine aminotransferase (ALT) in DMBA-untreated mice. Also, quercetin induced AST and ALT in DMBA-treated, although this was not significantly different from levels in DMBA-treated controls. The thiobarbituric acid reactive substances (TBARS) value showed a tendency to decrease following quercetin treatment; these decreases were significantly greater in the DMBA-treated compared to the untreated groups. Also, catalase and superoxide dismutase (SOD) activities as well as their mRNA expression were increased by quercetin; this increase was more pronounced in DMBA-treated compared to untreated mice. DMBA induced CYP1 activity as well as expression of CYP1A1 and CYP1B1. Each of these effects was significantly reduced by quercetin; however, this reduction was observed for CYP1A1 at only the higher dose and for CYP1B1 at both doses. These data suggest that quercetin shows antioxidant activity against DMBA-induced oxidative stress. Moreover, its regulation of CYP1A1 and CYP1B1 suggests the potential of quercetin as an anticancer supplement.

show abstract

Section: Introductionsupporting

confidence: 86%

Quercetin acts as an antioxidant and downregulates CYP1A1 and CYP1B1 against DMBA-induced oxidative stress in mice

Choi

Kim

2012

Oncol Rep

View full text Add to dashboard Cite

show abstract

“…In similar fashion, the effect of DF on cell cycle modulation was very mild. The effect of Quercetin was similar to that reported in the literature 16 .…”

Section: Resultssupporting

confidence: 89%

Cytotoxic effects of Fisturalin-3 and 11-Deoxyfisturalin-3 on Jurkat and U937 cell lines

Mijares¹,

Ochoa²,

Barroeta³

et al. 2013

Biomed Pap Med Fac Univ Palacky Olomouc Czech Repub

View full text Add to dashboard Cite

Background. Fisturalines are bromotyrosine compounds isolated from marine sponges. Previous studies have shown antineoplasic, antiviral and antibacterial effects in Vitro; however, the possible effects of these compounds in hematologic malignancies have not been assessed. Methods. In the present study, the antiproliferative and pro apoptotic effects of Fistularin-3 (F) and 11-Deoxyfistularin-3 (DF) were assessed using the MTT method and annexin V/propidium iodide by flow cytometry using the cell lines: Jurkat E6.1 and U937. In addition, the cell cycle was assessed by flow cytometry. Results. Inhibition of the proliferative response was concentration and time dependent. The IC50 of F was 7.39 and 8.10 M for Jurkat E6.1 and U937 respectively. At 24 and 48 h, in the U937 cell line, but not in the Jurkat cell line, both compounds induced up to 35% annexin V increase. Necrosis was not observed in any case. Compound F induced, in both cell lines, a decrease in the number of cells in the S phase and increase in the G0/G1 phase. In the Jurkat cell line only, there was an increase in the number of cells in the G2/M phase. Compound DF was not as effective as F. Conclusions. F is more active than DF in repressing the cell cycle and inducing apoptosis. Both compounds are potentially useful in the development of new drugs to treat hematologic malignancies.

show abstract

“…Human beings regularly consume quercetin in various fruits, vegetables or herbal medicines; such as apple, onion, and sophora flower. Quercetin has been found to have various biological activities including antiproliferative effects on several cancer cells, [1][2][3] anti-inflammatory and anti-allergic effects, 4) anti-oxidative activity, 5) and atherosclerosis-preventing effect. 6) In clinical study, supplementation of quercetin in hypertensive patients for 28 d significantly reduced blood pressure.…”

mentioning

confidence: 99%

Enzymatically Modified Isoquercitrin, .ALPHA.-Oligoglucosyl Quercetin 3-O-Glucoside, Is Absorbed More Easily than Other Quercetin Glycosides or Aglycone after Oral Administration in Rats

Makino

Shimizu

Kanemaru

et al. 2009

Biological & Pharmaceutical Bulletin

148

View full text Add to dashboard Cite

Quercetin (3,3Ј,4Ј,5,7-pentahydroxyflavone) is a widely distributed secondary metabolite in plants. Human beings regularly consume quercetin in various fruits, vegetables or herbal medicines; such as apple, onion, and sophora flower. Quercetin has been found to have various biological activities including antiproliferative effects on several cancer cells, [1][2][3] anti-inflammatory and anti-allergic effects, 4) anti-oxidative activity, 5) and atherosclerosis-preventing effect. 6) In clinical study, supplementation of quercetin in hypertensive patients for 28 d significantly reduced blood pressure. 7) However, orally administered quercetin is poorly absorbed, and the bioavailability of quercetin administered in capsule form to human beings was reported to be less than 1%. 8) Therefore, several trials have been conducted to increase the bioavailability of quercetin by optimizing its formulation. For example, a pharmacokinetic study in rats revealed that bioavailability of quercetin was increased 5.7-fold by administration using a solid lipid nanoparticle as an oral delivery carrier compared with that administered as a quercetin suspension. 9)Quercetin is generally accumulated in plants as glycosides such as glucosides, rutinosides and xylosides. These quercetin glycosides show higher solubility in water than quercetin due to the hydrophilicity of the sugar moieties. Indeed, quercetin-4Ј-O-b-D-glucopyranoside has higher bioavailability than its aglycone in human beings, suggesting that conjugation with glucose would enhance quercetin absorption in the small intestine. 10,11) Glucosyl conjugation of lipophilic small molecules leads to an increase in their water solubility.12) Several glucosides of quercetin have been prepared by enzymatic synthesis to enhance the water solubility, as exemplified by a-monoglucosyl rutin (aMR), 13) a-oligoglucosyl rutin (aOR), 14) and "enzymatically modified isoquercitrin" (EMIQ).15) In Japan, EMIQ has been approved as a food additive, 16) and in U.S.A., FDA declared EMIQ generally regarded as safe (GRAS) for use in multiple food categories. However, how glucosyl conjugation affects the pharmacokinetic behavior of quercetin remains unknown except that aMR exhibited 4.5-fold higher area under the plasma concentration-time curve (AUC ) value than quercetin after oral administration as a suspension in carboxymethylcellulose (CMC) solution in rats. 13) In the present investigation, we examined the intestinal absorption and bioavailability of quercetin after oral administration of various quercetin glucosides, and revealed that glucosyl conjugation of isoquercitrin (IQC) with a-glucosidic linkages is quite effective for improving the bioavailability. We also showed that hydrolysis of the glycosidic linkage prior to the absorption through small intestinal epithelium is essential. We further suggest that the collaborative action of two glucosidases, mucosal maltose-glucoamylase (MGAM) and lactase-phlorozin hydrolase (LPH), both anchoring in the mucosal membrane of the epithelial tissue, pla...

show abstract

Antiproliferative effects of quercetin through cell cycle arrest and apoptosis in human breast cancer MDA-MB-453 cells

Cited by 147 publications

References 34 publications

Quercetin acts as an antioxidant and downregulates CYP1A1 and CYP1B1 against DMBA-induced oxidative stress in mice

Quercetin acts as an antioxidant and downregulates CYP1A1 and CYP1B1 against DMBA-induced oxidative stress in mice

Cytotoxic effects of Fisturalin-3 and 11-Deoxyfisturalin-3 on Jurkat and U937 cell lines

Enzymatically Modified Isoquercitrin, .ALPHA.-Oligoglucosyl Quercetin 3-O-Glucoside, Is Absorbed More Easily than Other Quercetin Glycosides or Aglycone after Oral Administration in Rats

Contact Info

Product

Resources

About