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Hi All, The attached paper descried below is on grain antioxidants. Grains

may go against the grains for some of us for good reasons, but this paper

presents the good properties of grains quite well, I thought.

Maybe the point is variety in individual and classes of food categories can

be of benefit.

Cheers, Al.

Adom KK, Liu RH.

Antioxidant Activity of Grains.

J Agric Food Chem. 2002 Oct 9;50(21):6182-6187.

PMID: 12358499 [PubMed - as supplied by publisher]

Alan Pater, Ph.D.; Faculty of Medicine; Memorial University; St. 's, NF

A1B 3V6 Canada; Tel. No.: (709) 777-6488; Fax No.: (709) 777-7010; email:

apater@...

[ACS Publications Division]

[Journal Home Page] [search the Journals] [Table of Contents] [PDF version

of this article]

J. Agric. Food Chem., 50 (21), 6182 -6187, 2002. 10.1021/jf0205099

S0021-8561(02)00509-5

Web Release Date: August 31, 2002

Copyright © 2002 American Chemical Society

Antioxidant Activity of Grains

Kafui Kwami Adom[image] and Rui Hai Liu*[image][image]

Institute of Comparative and Environmental Toxicology and Department of

Food Science, Cornell University, Stocking Hall, Ithaca, New York

14853-7201

Received for review May 3, 2002. Revised manuscript received July 25, 2002.

Accepted July 25, 2002.

Abstract:

Epidemiological studies have shown that consumption of whole grains and

grain-based products is associated with reduced risk of chronic diseases.

The health benefits of whole grains are attributed in part to their unique

phytochemical composition. However, the phytochemical contents in grains

have been commonly underestimated in the literature, because bound

phytochemicals were not included. This study was designed to investigate

the complete phytochemical profiles in free, soluble conjugated, and

insoluble bound forms, as well as their antioxidant activities in uncooked

whole grains. Corn had the highest total phenolic content (15.55 ± 0.60

[image]mol of gallic acid equiv/g of grain) of the grains tested, followed

by wheat (7.99 ± 0.39 [image]mol of gallic acid equiv/g of grain), oats

(6.53 ± 0.19 [image]mol of gallic acid equiv/g of grain), and rice (5.56 ±

0.17 [image]mol of gallic acid equiv/g of grain). The major portion of

phenolics in grains existed in the bound form (85% in corn, 75% in oats and

wheat, and 62% in rice), although free phenolics were frequently reported

in the literature. Ferulic acid was the major phenolic compound in grains

tested, with free, soluble-conjugated, and bound ferulic acids present in

the ratio 0.1:1:100. Corn had the highest total antioxidant activity

(181.42 ± 0.86 [image]mol of vitamin C equiv/g of grain), followed by wheat

(76.70 ± 1.38 [image]mol of vitamin C equiv/g of grain), oats (74.67 ± 1.49

[image]mol of vitamin C equiv/g of grain), and rice (55.77 ± 1.62

[image]mol of vitamin C equiv/g of grain). Bound phytochemicals were the

major contributors to the total antioxidant activity: 90% in wheat, 87% in

corn, 71% in rice, and 58% in oats. Bound phytochemicals could survive

stomach and intestinal digestion to reach the colon. This may partly

explain the mechanism of grain consumption in the prevention of colon

cancer, other digestive cancers, breast cancer, and prostate cancer, which

is supported by epidemiological studies.

Keywords: Phytochemicals; phenolics; grains; ferulic acid; antioxidant

activity

------------------------------------------------------------------------

Introduction

Epidemiological studies have strongly suggested that diets play a crucial

role in the prevention of chronic diseases such as heart disease, cancer,

diabetes, and Alzheimers's disease (1, 2). Consumption of fruits and

vegetables, as well as grains, has been associated with reduced risk of

chronic diseases (1-3). This has been hypothesized to be because they

contain phytochemicals that combat oxidative stress in the body by helping

to maintain a balance between oxidants and antioxidants. An imbalance

caused by overproduction of oxidants leads to oxidative stress, resulting

in damage to large biomolecules such as lipids, DNA, and proteins.

Oxidative damage increases the risk of degenerative diseases such as cancer

and cardiovascular diseases (1, 4, 5). Antioxidants reduce oxidative damage

to biomolecules by modulating the effects of reactive oxidants (6, 7).

Therefore, increased consumption of fruits and vegetables containing high

levels of antioxidants has been recommended. The importance and health

benefits of grain consumption in the prevention of chronic diseases such as

cancers and heart disease have also been documented (8-16). However, the

attention paid to grain consumption has been little compared to that for

fruits and vegetables, although nutritional guidelines put grains and grain

products at the base of the food guide pyramid to emphasize their

importance for optimal health (17).

Recent research has shown that the complex mixture of phytochemicals in

foods provides better protective health benefits than single phytochemicals

through a combination of additive and/or synergistic effects (18). This has

been supported by results from previous studies on health benefits of

single antioxidants that gave inconsistent results in human clinical trials

(19, 20). About 5000 of phytochemicals present in plants have been

identified, and still a large percentage remains unknown (21). Different

plants have different compositions of phytochemicals with different

structures and thus offer different protective functions with different

extents. Hence, for the maximum health benefits, sufficient amounts of

phytochemicals from a variety of sources such as fruits, vegetables, and

whole grain-based foods are recommended.

Grains contain unique phytochemicals that complement those in fruits and

vegetables when consumed together. For instance, various classes of

phenolic compounds in grains include derivatives of benzoic and cinnamic

acids, anthocyanidins, quinones, flavonols, chalcones, flavones,

flavanones, and amino phenolic compounds (9, 21, 22, 23). Grains contain

tocotrienols and tocopherol (9), and rice contains oryzanols (23). Some of

these phytochemicals such as ferulic acid and diferulates are predominantly

found in grains but are not present in significant quantities in some

fruits and vegetables (21, 24). Phenolic compounds present in grains have

antioxidant properties associated with the health benefits of grains and

grain products. Flavonoids have potent antioxidant and anticancer

activities. Fruits and vegetables have most of their phytochemicals in free

or soluble conjugate forms as glycosides (25, 26). On the other hand, grain

phytochemicals may exist in free, soluble conjugate, and insoluble bound

forms. Most are in the insoluble bound forms, bound to cell wall materials

(23, 24, 27). About 74% and 69% of the total phenolics present in rice and

corn, respectively, are in the insoluble bound forms, with ferulic acid

being the major phenolic compound present. Cell wall materials are

difficult to digest and may survive gastrointestinal digestion to reach the

colon. Colonic digestion of such materials would release the bulk of bound

phytochemicals. sen et al. (28) showed that human and rat colonic

microflora can release diferulic acids from dietary cereal brans. Thus,

nondigested or bound phytochemicals may have their unique health benefits

in the colon and beyond after absorption.

Most previous studies in the literature reported the phenolic levels of

grains using various aqueous solutions of methanol, ethanol, and acetone to

extract soluble phenolics (29-33). These studies assumed long extraction

times and/or use of finely powdered samples would ensure maximum extraction

of phenolic compounds from grains. Therefore, the total phenolic contents

of grains were underestimated in the literature without determining the

content of bound phenolics. Maillard and Berset (22) reported total

antioxidant activity of free and bound extracts of barley and malt, as well

as bound ferulic acid and p-coumaric acid. However, they did not report

free and soluble conjugate ferulic acids or free and bound total phenols

and total flavonoids. Sosulski et al. (27) reported free, soluble

conjugate, and bound phenolic acid contents of rice, oats, wheat, and corn

flours, but antioxidant activity, total phenols, and total flavonoids were

not investigated.

To our knowledge, there is still limited literature on the complete profile

(free, soluble conjugate, insoluble bound) of phenolic compounds and total

antioxidant activity of grains. Additionally, the total phenolic contents

of grains have been underestimated in the literature. The objective of this

study was to investigate the complete phytochemical profiles that exist in

the free, soluble conjugate, and insoluble bound forms, as well as their

antioxidant activity in corn, wheat, oats, and rice.

Materials and Methods

Chemicals and Reagents. Folin-Ciocalteu reagent, sodium nitrite, catechin,

and gallic acid were purchased from Sigma (St. Louis, MO). Sodium

hydroxide, hexane, aluminum chloride, and acetonitrile were obtained from

Fisher Scientific (Pittsburgh, PA), while ethyl acetate, triflouroacetic

acid, and ethanol were purchased from Mallinckrodt (Paris, KN).

Grain Samples and Sample Preparation. Samples of oats, corn, wheat, and

rice were obtained from General Mills (Golden Valley, MN). Whole oats and

whole brown rice were received as flours. Whole grain wheat and Sunlite

whole yellow corn were received as dehulled kernels. The wheat and corn

samples were milled in a coffee grinder to a fine powder. All samples were

individually mixed thoroughly and divided using the quartering system. Each

sample was divided into two portions and stored at -20 and -80 [image]C.

The -20 [image]C samples were used for routine analysis within 2 weeks.

Extraction of Free Phenolic Compounds. Free phenolic compounds in grains

were extracted by blending 25 g of whole grain flour with 50 mL of 80%

chilled ethanol for 10 min. After centrifugation at 2500 g for 10 min, the

supernatant was removed and extraction was repeated one more time.

Supernatants were pooled, evaporated at 45 [image]C to 10 mL, and

reconstituted with water to a final volume of 25 mL. The extracts were

stored at -40 oC until use (18).

Extraction of Bound Phenolic Compounds. One gram of whole grain flour was

extracted twice with 80% chilled ethanol with centrifugation at 2500g for

10 min, and the supernatant was discarded after each extraction. The

residues were then digested with 2 M sodium hydroxide at room temperature

for 1 h with shaking under nitrogen gas. The mixture was neutralized with

an appropriate amount of hydrochloric acid and extracted with hexane to

remove lipids. The final solution was extracted five times with ethyl

acetate. The ethyl acetate fraction was evaporated to dryness. Phenolic

compounds were reconstituted in 10 mL of water and stored at -40 [image]C

until use (27).

Extraction of Soluble Conjugated Ferulic Acid. Extracts from the free

phenolic extractions above were used for soluble conjugate extractions. The

extract (0.5 mL) was digested with 2 M NaOH for 1 h under nitrogen gas, and

the solution was neutralized with an appropriate amount of HCl. The mixture

was extracted five times with ethyl acetate, and the ethyl acetate fraction

was evaporated to dryness at 35 [image]C under nitrogen gas. Phenolics were

recovered for analysis in 2 mL of water (22, 27).

Determination of Ferulic Acid Content. Ferulic acid in sample extracts was

quantified using a RP-HPLC procedure employing a Supelcosil LC-18-DB, 150

mm × 4.6 mm, 3 mm column. Isocratic elution was conducted with 20%

acetonitrile in water adjusted to pH 2 with triflouroacetic acid, at a flow

rate of 0.6 mL/min. This was delivered using a Waters 515 HPLC pump (Waters

Corp., Milford, MA). A Waters 2487 dual wavelength absorbance detector

(Waters Corp.) was used for UV detection of analytes at 280 nm. Data

signals were acquired and processed on a PC running the Waters Millennium

software, version 3.2 (1999) (Waters Corp.). The ferulic acid concentration

of sample extracts was extrapolated from the pure trans-ferulic acid

standard curve. Ten microliter injections were made in each run, and peak

heights were used for all calculations. The recoveries for free ferulic

acid and bound ferulic acid analyses were 105.13 ± 5.23% (n = 3) and 89.30

± 1.01% (n = 3), respectively.

Determination of Total Phenolic Content. The total phenolic content of each

extract was determined using methods previously described by Singleton et

al. (34). Briefly, the appropriate dilutions of extracts were oxidized with

Folin-Ciocalteu reagent, and the reaction was neutralized with sodium

carbonate. The absorbance of the resulting blue color was measured at 760

nm after 90 min. Using gallic acid as standard, total phenolic content was

expressed as micromoles of gallic acid equivalent per gram of grain. Data

are reported as mean ± SD for at least three replications.

Determination of Total Flavonoid Content. Total flavonoid content was

determined by a colorimetric method described previously (35). Appropriate

dilutions of sample extracts were reacted with sodium nitrite, followed by

a flavonoid-aluminum complex formation using aluminum chloride. Solution

absorbance at 510 nm was immediately measured and compared to that of

catechin standards. Flavonoid content was expressed as micromoles of

catechin equivalent per gram of grain. Data are reported as mean ± SD for

at least three replications.

Determination of Total Antioxidant Activity. A modified total oxyradical

scavenging capacity (TOSC) assay (18, 36) was used for determining the

total antioxidant capacity of extracts. In this assay, peroxy radicals

formed from 2,2'-azobis-amidinopropane (ABAP) oxidize

[image]-keto-[image]-methiolbutyric acid (KMBA) to form ethylene gas, which

was measured by gas chromatographic headspace analysis. The degree of

inhibition of ethylene gas formation by sample extracts was used as the

basis for calculating the total antioxidant capacity.[image] The dose

required to cause a 50% inhibition (EC50) for each sample was used to

calculate the total antioxidant activity, which was expressed as micromoles

of vitamin C equivalent per gram of grain.

Statistical Analysis. Data were reported as mean ± SD for at least three

analyses for each type of extraction and parameter. Results were subjected

to ANOVA, and differences between means were located using Tukey's multiple

comparison test run on Minitab Release 12 software (State College, PA).

Correlations between various parameters were also investigated.

Results

Phenolic Contents of Grains. The phenolic contents of the four grains were

expressed as micromoles of gallic acid equivalent per gram of grain (Figure

1). Corn had the highest free phenolic content (2.12 ± 0.09 [image]mol/g of

grain), followed by rice (2.10 ± 0.12 [image]mol/g of grain) and then wheat

(1.90 ± 0.06 [image]mol/g of grain). Oats had the lowest free phenolic

content (1.77 ± 0.12 [image]mol/g of grain). In statistical testing, p <

0.05 for corn versus oats, and p > 0.05 for all other comparisons. The

bound phenolic content was highest for corn (13.43 ± 0.59 [image]mol/g of

grain), followed by wheat (6.10 ± 0.39 [image]mol/g of grain) and then oats

(4.76 ± 0.14 [image]mol/g of grain). Rice had the lowest bound phenolic

content (3.46 ± 0.13 [image]mol/g of grain). There were significant

differences ( p < 0.05) in the bound phenolic contents of all grains. Also

bound phenolics were significantly higher than free phenolics. The total

phenolic content was highest in corn (15.55 ± 0.60 [image]mol/g of grain),

followed by wheat (7.99 ± 0.39 [image]mol/g of grain) and then oats (6.53 ±

0.19 [image]mol/g of grain). Rice (5.56 ± 0.17 [image]mol/g of grain) had

the lowest total phenolic content. There were significant differences ( p <

0.05) in total phenolic contents among the grains.

------------------------------------------------------------------------

[image] Figure 1 Phenolic content of grains.

------------------------------------------------------------------------

Ferulic Acid Contents of Grains. Ferulic acid contents of grains were

expressed as micromoles of ferulic acid per 100 g of grain (Table 1). Free

ferulic acid was highest in corn (0.92 ± 0.02 [image]mol/100 g of grain),

followed by rice (0.7 ± 0.05 [image]mol/100 g of grain) and oats (0.65 ±

0.04 [image]mol/100 g of grain), and was lowest in wheat (0.57 ± 0.02

[image]mol/100 g of grain). Statistical analyses show p < 0.05 for corn

versus other grains and for rice versus wheat, and they show p > 0.05 for

all other comparisons. Soluble conjugated ferulic acid contents were

similar (p > 0.05) in corn (8.95 ± 0.11 [image]mol/100 g of grain) and rice

(9.9 ± 0.34 [image]mol/100 g of grain), and both grains had higher (p <

0.01) conjugated ferulic acid contents than wheat (3.27 ± 0.27

[image]mol/100 g of grain) and oats (3.4 ± 0.56 [image]mol/100 g of grain).

There were no differences in soluble conjugated ferulic acid levels between

wheat and oats ( p > 0.05). The bound ferulic acid content was highest in

corn (896.27 ± 9.09 [image]mol/100 g of grain), followed by wheat (329.60 ±

16.20 [image]mol/100 g of grain) and then oats (180.61 ± 4.57

[image]mol/100 g of grain). Rice had the lowest bound ferulic acid content

(142.80 ± 8.68 [image]mol/100 g of grain). The bound ferulic acid contents

in grains were all significantly different (p < 0.05) from each other

(Table 1). The bound ferulic acid contents were significantly higher (p <

0.01) than both free and soluble conjugate ferulic acid contents in all

grains tested. The total ferulic acid content was highest in corn (906.13 ±

9.09 [image]mol/100 g of grain) followed by wheat (333.44 ± 16.20

[image]mol/100 g of grain) and then oats (184.66 ± 4.61 [image]mol/100 g of

grain), with rice having the lowest total ferulic acid content (153.39 ±

8.68 [image]mol/100 g of grain).

Flavonoid Contents of Grains. Flavonoid contents of grains were expressed

as micromoles of catechin equivalent per gram of grain (Figure 2). The free

flavonoid content was highest in oats (0.45 ± 0.02 [image]mol/g of grain),

followed by rice (0.33 ± 0.01 [image]mol/g of grain) and then corn (0.16 ±

0.004 [image]mol/g of grain). Wheat (0.09 ± 0.01 [image]mol/g of grain) had

the lowest flavonoid content. There were significant differences (p < 0.05)

in free flavonoid contents among the grains. For bound flavonoid content,

the level in corn (1.52 ± 0.17 [image]mol/g of grain) was higher (p < 0.01)

than that in wheat (1.15 ± 0.03 [image]mol/g of grain). Both corn and wheat

had higher flavonoid contents (p < 0.01) than rice (0.60 ± 0.04

[image]mol/g of grain) and oats (0.71 ± 0.05 [image]mol/g of grain). There

was no difference in bound flavonoid contents between rice and oats (p >

0.05). The total flavonoid content of corn (1.68 ± 0.17 [image]mol/g) was

higher (p < 0.01) than those of other grains. The total flavonoid contents

of wheat (1.24 ± 0.03 [image]mol/g of grain) and oats (1.16 ± 0.06

[image]mol/g of grain) were similar (p > 0.05), and both had levels higher

(p < 0.05) than that of rice (0.92 ± 0.04 [image]mol/g of grain).

------------------------------------------------------------------------

[image] Figure 2 Flavonoid content of grains.

------------------------------------------------------------------------

Total Antioxidant Activities of Grains. The total antioxidant activities of

grains were expressed as micromoles of vitamin C equivalent per gram of

grain (Figure 3). Free phytochemical extracts of oats had the highest

antioxidant activity (31.07 ± 1.37 [image]mol/g of grain), followed by corn

(24.00 ± 0.43 [image]mol/g of grain) and then rice (16.02 ± 0.37

[image]mol/g of grain). Free phytochemical extracts in wheat had the lowest

antioxidant activity (8.00 ± 0.30 [image]mol/g of grain). The antioxidant

activities of free phytochemical extracts were different (p < 0.05) among

the grains. The antioxidant activity of bound phytochemicals in corn

(157.68 ± 0.75 [image]mol/g of grain) was higher (p < 0.01) than those in

other grains. There was a significant difference (p < 0.05) among the

antioxidant activities of bound phytochemicals in wheat (68.74 ± 1.35

[image]mol/g of grain), oats (43.60 ± 0.59 [image]mol/g of grain), and rice

(39.76 ± 1.58 [image]mol/g of grain). The total antioxidant activity of

corn (free + bound) was 181.42 ± 0.86 [image]mol/g of grain and was the

highest (p < 0.01) of those of the grains tested. The total antioxidant

activities of wheat (76.70 ± 1.38 [image]mol/g of grain) and oats (74.67 ±

1.49 [image]mol/g of grain) were similar (p > 0.05) but higher (p < 0.05)

than the total antioxidant activity in rice (55.77 ± 1.62 [image]mol/g of

grain).

------------------------------------------------------------------------

[image] Figure 3 Total antioxidant activity of grains.

------------------------------------------------------------------------

There was a low correlation between parameters measured for free extracts

(Table 3[image] [image]). For bound extractions, however, the total

antioxidant activity highly correlated with phenolic content (R2 = 0.991, p

< 0.01) and ferulic acid content (R2 = 0.999, p < 0.01) (Table 3). There

was a high correlation between phenolics and ferulic acid content for bound

extracts (R2 = 0.994, p < 0.01). Total values for phenolics, ferulic acid,

and flavonoids were highly correlated to the total antioxidant activity.

Also total ferulic acid and flavonoids correlated with total phenolic

content.

Discussion

Oxidative damage to biomolecules in the body has been associated with

certain disease conditions. Grains contain a wide array of phytochemicals

that exert health benefits in humans through various mechanisms including

antioxidant properties and mediation of hormones. Several studies involving

whole grain intakes have shown a consistent protective role of whole grain

consumption in reduced risk of colorectal cancer, breast cancer, coronary

heart disease, and diabetes, and reduced total mortality (8, 9, 12-14, 16,

37, 38). (9) suggests that lignans and phytoestrogens in grains

may reduce the risk of hormone-related diseases such as prostate and breast

cancers. Since most grain phenolics such as phenolic acids occur in the

outer layers of grains, whole grains (compared to refined grains) are

recommended for optimal health. Phytochemical contents of grains have been

underestimated in the literature without determining the content of bound

phytochemicals (29-32). This study was designed to determine the complete

profile of phenolic phytochemicals in grains, and their relationship and

contribution to the total antioxidant activities.

The total phenolic contents were analyzed using the method by Singleton et

al. (34), without distinguishing specific structures. The free phenolic

content represents contributions from free and soluble conjugated

phenolics. Conjugated phenolics may still be oxidized and contribute toward

total phenolic content and antioxidant activity. Our results clearly showed

that most grain phenolics were in the bound fraction (Figure 1 and Table

2). The percentage contributions of free and bound phenolics to the total

are shown in Table 2. The free phenolic contribution ranged from 15% in

corn to 38% in rice. The bound phenolic contribution ranged from 62% in

rice to 85% in corn. Therefore, the total phenolic contents of grains were

clearly underestimated in the literature without including the bound

phenolics. The total phenolic content among grains followed the same

concentration trend as the bound phenolics because of the larger

contribution from bound phenolics (Figure 1). Corn had the highest total

phenolic content while rice had the lowest content. Bound phenolics in

grains are associated with cell wall materials that may survive upper

gastrointestinal digestion conditions and may finally reach the colon.

Colonic digestion of such materials by intestinal microflora may release

the bulk of bound phytochemicals. On the basis of our results, most of the

grain phenolic compounds may be released in the colon to exert their health

benefits locally and beyond after absorption. sen et al. (28)

reported that both human and rat gastrointestinal esterase (from intestinal

mucosa and microflora) can release ferulic acid and diferulic acids from

cereal bran. These compounds have potent antioxidant properties, and their

absorption into the blood plasma has been reported (28). Therefore, our

results suggest that bound phytochemicals in whole grains may have a more

profound effect on health benefits. We believe this could partly explain

the inverse association between increased whole grain and whole grain-based

products consumption and reduced incidence of colon cancer, breast cancer,

prostate cancer, heart disease, and diabetes, and reduced total mortality

(8, 9, 11-16, 37-40).

The reverse phase HPLC method used for ferulic acid analysis achieved

complete resolution of the ferulic acid peak (data not shown), especially

for bound extracts, allowing for accurate quantification. High recoveries

for both free (105.13 ± 5.23%) and bound (89.28 ± 1.01%) ferulic acid

analysis were obtained. The results showed that bound ferulic acid was

significantly higher than free and soluble conjugate ferulic acid in corn,

wheat, oats, and rice (Table 1). The ratio of free, soluble conjugated, and

bound ferulic acid in corn and wheat was 0.1:1:100. Free and soluble

conjugated ferulic acids made very small contributions (<0.6% and <7.0%,

respectively), while bound ferulic acid was the prevalent form of ferulic

acid present in the grains (>93%). Thus, total ferulic acid followed the

same concentration trend as bound ferulic acid (Table 1). The occurrence of

bound ferulic acid in such relatively high concentrations also strongly

supports our hypothesis that phytochemicals in grains have been

underestimated in the literature by excluding the bound fractions. Maillard

and Berset (22) estimated that free phenolic acids in methanol extracts of

barley were 100-fold lower than bound phenolic acids, which was consistent

with our findings. Although our extraction and analysis procedures were

similar to those used by Maillard and Berset, our percentage recoveries for

ferulic acid were much higher. Preliminary work in our laboratory showed

that 2 N NaOH digestion for 1-4 h produced similar percentage recoveries

with or without rice samples. On the basis of these findings, we used a 1 h

alkaline digestion combined with subsequent five times ethyl acetate

extractions for extracting bound phenolics. Maillard and Berset used a 4 h

alkaline digestion followed by three times ethyl acetate extraction, giving

a 63% ferulic acid recovery. It is possible that phenolic acids might be

partially destroyed during prolonged alkaline hydrolysis. Our preliminary

work showed that about 10% loss of bound ferulic acid occurred during

alkaline hydrolysis for 1-4 h (unpublished results). This may account for

differences in the results obtained, as well as possible varietal

differences between wheat samples used. The ferulic acid value reported in

this work for wheat (648 [image]g ferulic acid/g of grain) was slightly

higher than that obtained (590 [image]g ferulic acid/g of grain) by Yang et

al. (41), who used the method of Maillard and Berset. Ferulic acid and its

conjugates have antioxidant properties (15), and they are present in high

concentrations in grains.

The free flavonoid contents in grains were low compared to the bound

flavonoid content, and they were all significantly different (p < 0.05)

from each other (Figure 2). Total flavonoid contents followed a similar

pattern as bound flavonoid contents in all grains, because of the large

contribution from bound flavonoids. The percentage contributions of free

and bound flavonoids to the total are shown in Table 2. The free flavonoid

contribution to the total ranged from 7% in wheat to 39% in oats. The bound

flavonoid contribution ranged from 61% in oats to 93% in wheat (Table 2).

The total flavonoid contents of wheat and oats were similar, although their

free and bound flavonoid contents were different. This could be attributed

to the relatively higher free flavonoids in oats. Thus, whole wheat may

deliver more flavonoids to the colon compared to whole oats. Flavonoids

have potent antioxidant and anticancer activity.

The total antioxidant activities of grains were different between grains

and among different fractions (free and bound) of the same grain. Free

extracts of corn, wheat, oats, and rice had significantly lower antioxidant

activity (p < 0.01; Figure 3) compared to those of the bound extracts, as

was also observed by Maillard and Berset (22). This is attributable to

higher phenolic content in bound extracts compared to free extracts (Table

2). Although the free and bound antioxidant activities of wheat and oats

(Figure 3) were significantly different (p < 0.05), their total antioxidant

activities were similar (p > 0.05). This could be attributed to the

relatively higher antioxidant activity of free oat extracts or bound wheat

extracts. The major contribution to total antioxidant activity of whole

grains was from bound extracts and ranged from 58% to 90%. The TOSC assay

measures the overall antioxidant activity of extracts including both

additive and/or synergistic effects of phytochemicals. This gives a more

accurate representation of antioxidant capacity of extracts. Free

antioxidant activities represent contributions from both free and soluble

conjugate fractions of grains. Some derivatives of phenolic compounds

(conjugates) are known to have antioxidant properties. Avenanthramides are

cinnamoyl conjugates that occur in oats with higher antioxidant activity

(33, 42). Long chain mono- and di-alcohol esters of ferulic and caffeic

acids had potent antioxidant activity (43). -Conesa et al. (15)

measured the antioxidant activity of 8,8'-diferulic acid and compared that

to the antioxidant activities of ferulic acid and other diferulates. The

Trolox equivalent antioxidant capacity (TEAC) for ferulic acid was 1.96.

The TEAC values for various diferulic acid conjugates ranged from 1.49 to

4.00. Generally, diferulic conjugates were reported to be more potent

antioxidants than ferulic acid in both aqueous and lipid phases. Among the

diferulates tested, 8,8'-diferulic acid was the most potent antioxidant in

the aqueous phase.

The total phenolic content has been directly related to the total

antioxidant activity and may explain the high correlation observed between

these parameters (Table 3). Flavonoids and ferulic acid contribute to total

phenolics in corn, wheat, oats, and rice. The high correlation between

phenolics and ferulic acid content for bound extracts reflects the major

contribution of ferulic acid to total phenolic content. The free ferulic

acid contribution to free phenolics was <0.5% in all grains, implying the

contributions of other compounds to total phenolics in the free extracts

were more important. On the other hand, the contribution of bound ferulic

acid content to bound phenolics was 76% in corn, 61% in wheat, 43% in oats,

and 47% in rice. Velioglu et al. (29) reported a significant relation (R2 =

0.905) between total phenolics and antioxidant activity of grain products.

Our results have shown that phytochemical contents of grains have been

underestimated in the literature without including the bound

phytochemicals. Among the grains we tested, corn had the highest content of

phenolic compounds followed by wheat and oats, while rice had the lowest

phenolic content. Ferulic acid was the major phenolic compound in grains

and was mainly present in the bound form. Free, soluble conjugated, and

bound ferulic acids were present in the ratio 0.1:1:100. Corn had the

highest total antioxidant activity followed by wheat and oats, and then

rice. Our results also show the major portions of phytochemicals in the

grains are present in the bound form and may survive stomach and intestinal

digestion to reach the colon. This may partially explain the mechanism of

grain consumption in the prevention of colon cancer, other digestive

cancers, breast cancer, and prostate cancer. Further studies of the unique

grain phytochemicals and their mechanism of action are warranted.

* To whom correspondence should be addressed. Telephone: (607) 255-6235.

Fax: (607) 254-4868. E-mail: RL23@....

[image] Department of Food Science.

[image] Institute of Comparative and Environmental Toxicology.

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------------------------------------------------------------------------

Table 1. Ferulic Acid Contents of Grains and the Percentage Contribution

of Each Fraction to the Total ([image]mol of ferulic acid/100 g of grain)

free soluble conjugate bound total

0.92 ± 0.02 896.27 ± 9.09 906.13 ±

corn (0.1%)a 8.95 ± 0.11 (1%)

(98.9%) 9.09

wheat 0.57 ± 0.02 3.27 ± 0.27 (1%) 329.60 ± 16.20 333.44 ±

(0.2%) (98.8%) 16.20

oats 0.65 ± 0.04 3.4 ± 0.56 (1.84%)180.61 ± 4.57 184.66 ±

(0.4%) (97.8%) 4.61

rice 0.7 ± 0.05 9.9 ± 0.34 (6.5%) 142.80 ± 8.68 153.39 ±

(0.5%) (93%) 8.68

a Mean ± SD (% contribution to total).

------------------------------------------------------------------------

------------------------------------------------------------------------

Table 2. Percentage Contributions of Free and Bound Fractions of Grains to

Total Phenolics, Flavonoids, and Total Antioxidant Activity

phenolic content flavonoid content total antioxidant activity

(%) (%) (%)

free bound free bound free bound

corn 15 85 9 91 13 87

wheat 25 75 7 93 10 90

oats 25 75 39 61 42 58

rice 38 62 35 65 29 71

------------------------------------------------------------------------

Table 3. Correlation Analysis of Phenolics and Total Antioxidant Activity

free extracts bound extracts total

total total total

antioxidant phenolics antioxidant phenolicsantioxidant phenolics

activity activity activity

phenolics 0.076a 0.991**b 0.983**

ferulic 0.0003c 0.695c

acid 0.999** 0.994** 0.974* 0.998**

flavonoids0.517 0.324 0.872 0.865 0.925* 0.933*

a Correlation coefficient R2.b Significantly different: *, p < 0.05; **, p

< 0.01; all others, p > 0.05.c Total of free and soluble conjugate ferulic

acid.

------------------------------------------------------------------------

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