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Effects of Daily Oral Administration of Quercetin Chalcone and Modified Citrus Pectin on Implanted Colon-25 Tumor Growth in Balb-c Mice | Alternative Medicine Review | Find Articles at BNETOn
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Health Care IndustryIndustry: Email Alert RSS FeedEffects of Daily Oral
Administration of Quercetin Chalcone and Modified Citrus Pectin on Implanted
Colon-25 Tumor Growth in Balb-c Mice
Alternative Medicine Review, Dec, 2000 by Adam Hayashi, Aric C. Gillen,
James R. LottE-mail Print Link Abstract
The health benefits of fruits and vegetables have been the subject of numerous
investigations over many years. Two natural substances, quercetin (a flavonoid)
and citrus pectin (a polysaccharide found in the cell wall of plants) are of
particular interest to cancer researchers. Two modified versions of these
substances -- quercetin chalcone (QC) and a pH-modified citrus pectin (MCP) --
are the focus of this study. Previous research has confirmed that quercetin
exhibits antitumor properties, likely due to immune stimulation, free radical
scavenging, alteration of the mitotic cycle in tumor cells, gene expression
modification, anti-angiogenesis activity, or apoptosis induction, or a
combination of these effects. MCP has inhibited metastases in animal studies of
prostate cancer and melanoma. To date, no study has demonstrated a reduction in
solid tumor growth with MCP, and there is no research into the antitumor effect
of QC. This study examines the effects of MOP and QC on the size and weight of
colon-25 tumors implanted in balb-c mice.
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Plant Sterols and Sterolins Fifty mice were orally administered either 1 mL
distilled water (controls), low-dose QC (0.8 mg/mL), high-dose QC (1.6 mg/mL),
low-dose MCP (0.8 mg/mL) or high-dose MCP (1.6 mg/mL) on a daily basis,
beginning the first day of tumor palpation (usually eight days
post-implantation). A significant reduction in tumor size was noted at day 20 in
all groups compared to controls. The groups given low-dose QC and MCP had a
29-percent (NS) and 38-percent (p [is less than] 0.02) decrease in size,
respectively. The high-dose groups had an even more impressive reduction in
size; 65 percent in the QC group and 70 percent in the mice given MCP (both p
[is less than] 0.001).
This is the first evidence that MCP can reduce the growth of solid primary
tumors, and the first research showing QC has antitumor activity. Additional
research on these substances and their effect on human cancers is warranted.
Altern Med Rev 2000;5(6):546-552.
The benefits of fruits and vegetables have been studied fairly extensively.
Flavonoids, found in many plants, are of particular interest for their
anticancer properties. In his text, Boik divides the flavonoids into five
categories: anthocyanins, minor flavonoids, flavones or flavonoids,
isoflavonoids, and tannins.[1] Quercetin, a member of the flavones group, is
thought to be the most widely distributed in nature; approximately 25-50 mg of
quercetin is consumed in a normal daily diet.[2] Bioflavonoids have been
reported to be involved in several important biological processes including
antihistamine effects, immunological modulation, inhibition of platelet
aggregation, and antitumor activity.
Early research conducted on the effect of oral administration of quercetin on
colon-25 tumors in balb-c mice showed a significant reduction (50%) in size.[3]
This research was based on reported antitumor properties of quercetin including:
lymphocyte proliferation,[4] neutrophilia,[5] free radical scavenging,[6]
anti-angiogenesis,[7] down-regulation of the mitotic cycle in tumor cells,[8]
gene expression alteration,[9] and induction of apoptosis (cell suicide).[10] A
comprehensive review of quercetin's antitumor effects was conducted recently by
Lamson and Brignall and published in this journal.[11]
An important remaining question is how much quercetin is absorbed from an oral
dose. Varying estimates have been concluded from clinical studies, ranging from
less than one percent to 50 percent (this in ileostomy patients).[12-15]
Quercetin Chalcone
A modified version of quercetin -- quercetin chalcone (2',3,4,4',6'
pentahydroxy-flavone, U.S. Patent #5,977,184) -- may provide a solution to the
potential problem of poor absorption. To convert quercetin to quercetin chalcone
(QC), a hydrogen is added to the oxygen at the number 1 position of the center
ring, breaking the bond between that oxygen and the number 2 carbon and creating
a hydroxyl group (Figure 1). This reduction of quercetin potentially gives QC
the same anticancer effects of quercetin with the hydrophilic effect of a
chalcone. The hydrophilic effect of QC may allow for greater absorption in the
intestine as well as by tumor cells.
Modified Citrus Pectin
A water-soluble polysaccharide extracted from orange peel, citrus pectin is
further pH-modified in the laboratory to allow for smaller carbohydrate chains
rich in galactose residues.[16] Previous studies have shown a link between
administration of modified citrus pectin (MCP) and decreased metastasis of
prostate tumors in rats and melanoma in mice.[17,18] With the use of MCP, Pienta
et al were able to demonstrate a significant reduction in the number of
metastatic MAT-LyLu tumor colonies formed in the lungs of rats.[17] MCP is
believed to adhere to tumor cells through cell surface carbohydrate-binding
proteins called lectins, preventing aggregation of tumor cells and adhesion to
normal cells.[16]
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