Chemistry of Food Additives and Preservatives (Msagati/Chemistry of Food Additives and Preservatives) || Nutraceuticals and Functional Foods

P1: SFK/UKS P2: SFKBLBK430-c16 August 27, 2012 12:7 244mm×172mm

16 Nutraceuticals and Functional Foods

‘Let food be your medicine and medicine be your food.’Hippocrates, 460–370 BC

Abstract: There are components in foodstuffs which are useful for maintaining our bodyhealth and immune system. Scientifically, there is a strong relationship between food andhealth such that some food items contain medicinal constituents with the ability to keepthe body healthy and fit. There has been much research activity recently on the types offood items and other natural products (mainly of plant origin) and their possibility of beingsources of therapeutic and prophylactic agents. The types of foods in this regard are thosefunctional foods that, when consumed regularly and appropriately, can result in beneficialhealth effects beyond their natural properties. Alternatively, dietary supplements can beprescribed in concentrated form to deliver an intended bioactive agent from some foodstuffs.These nutraceuticals are administered in higher doses than in normal food, but in a non-foodcomposition to improve human health.

Keywords: dietary supplement; food and health; nutraceuticals; nutrition; pharmaceutical

16.1 WHAT ARE NUTRACEUTICALS?

The reasons for why we need food go beyond satisfying hunger and getting the energy weneed to work or be active because of the presence of essential fuel-nutrient ingredients in foodproducts. This introduces the concept of nutraceuticals, which is a term coined from the words‘nutrition’ and ‘pharmaceutical’ and refers to a foodstuff or product with ingredients whichcan render health benefits to consumers. Nutraceutical can also refer to a product isolated orpurified from foodstuffs, but which can be supplied to consumers in medicinal formulationsthat under normal circumstances may not be associated with foodstuffs. Another definitionthat is used for nutraceuticals is any non-toxic food component with health benefits that havebeen proven beyond reasonable doubt, including disease treatment and prevention. Anotherterm used specifically in relation to animal husbandry is ‘veterinary nutraceutical’, definedas a substance produced in a purified or extracted form that is administered with the purposeof improving health.

In general, nutraceuticals perform the important functions of promoting wellness, prevent-ing malignant processes and controling symptoms in humans. The exact difference betweennutraceuticals and functional foods may be difficult to identify; however, while functional

Chemistry of Food Additives and Preservatives, First Edition. Titus A. M. Msagati.C© 2013 John Wiley & Sons, Ltd. Published 2013 by John Wiley & Sons, Ltd.


Nutraceuticals and Functional Foods 245

Fig. 16.1 Chemical structure of �-carotene.

foods are consumed normally like any other food, nutraceuticals are always consumed in theform of either tablets, capsules or other forms of medicinal formats.

For longer than can be remembered, it has been known that some types of food items ordiet, such as varieties of fruits, vegetables or herbs, are generally composed of ingredientswith medicinal activity that can pretreat or vent different types of diseases and ailments (e.g.diabetes or high blood pressure). Examples of food items known to contain medicinal ingre-dients include carrots, garlic, apples and honey, to mention a few. Carrots contains a terpenoidred pigment known as �-carotene (1,1’-(3,7,12,16-Tetramethyl-1,3,5,7,9,11,13,15,17-octadecanonaene-1,18-diyl)bis(2,6,6-trimethylcyclohexene; Figure 16.1). This isoprenoidpigment molecule in carrots has been linked to a reduced probability of developing lungcancer, stroke or heart attack, as well as keeping skin cells and hair fresh.

Garlic contains ingredients which are antibacterial and antiviral in nature, and has beenassociated with increasing immunity systems. Fruits such as apples contain fibres whichhelp digestion functions and reduce the risks of cholesterol. Moreover, a flavonol chemicalcompound known as quercetin (2-(3,4-dihydroxyphenyl)-3,5,7-trihydroxy-4H-chromen-4-one; Figure 16.2) found in apple skin is known for its powerful antioxidant activities and isalso suspected to play an important role in combating heart diseases, tumours and cancer.

16.2 CLASSIFICATION OF NUTRACEUTICALS

Nutraceuticals currently found in the market include both traditional or natural and non-traditional.

O

OOH

HO

OH

HOOH

Fig. 16.2 Chemical structure of quercetin.


246 Chemistry of Food Additives and Preservatives

16.2.1 Natural nutraceuticals

The class of natural nutraceuticals includes whole foods with potential health qualitiessuch as fish (contains active compounds known as �-3 fatty acids which promotes health);vegetables; fruits, especially tomatoes which are known to contain lycopene; and soy beanswhich is rich in saponins. Other natural nutraceuticals which have been demonstrated tocontain ingredients with health benefits include tea and chocolate.

16.2.2 Non-natural nutraceuticals

Non-natural nutraceuticals are scientifically produced in processes which tend to add somenutritional ingredients with health benefits to agricultural foods. For example, cereals canbe enriched with some vitamins or �-carotene, qualifying these foods as nutraceuticals.In general practice, many food products are enriched with antioxidant and/or fat-solublevitamins which are known to have many potential health benefits such as the prevention ofcancer and cerebrovascular disease by the action of antioxidants.

Food items enriched with vitamins such as tocopherols (vitamin E) have been associatedwith the prevention of diseases such as Parkinson’s disease, if taken constantly and consis-tently. The oxidised form of vitamin C (ascorbic acid) known as dehydroascorbic acid readilycrosses the blood brain barrier, thus giving the potential to combat Alzheimer’s disease. Somestudies have shown that a synergy of vitamin E, C and �-carotene can play an important rolein reducing low-density lipoprotein oxidation, thus reducing the risk of atherosclerosis.

16.3 MECHANISMS OF ACTION

The mechanism of certain food items in functioning as prophylactic and curative agentscan be explained by the presence of chemicals known as secondary metabolites which havea wide range of biological activities. Although the activity of these secondary metabolites(present mainly in plant-derived foods) is lower than that of normal drugs prescribed forsome diseases and ailments, a regular and consistent intake through diet can have a greateffect on lasting physiological effects.

There are many different types of foods (both whole foods and processed foods) witha variety of ingredients and chemistries imparting health benefits (in treating or preventingdifferent types of disease conditions), so a number of different biological mechanisms bywhich nutraceuticals work can therefore be expected. The following sections discussing themechanisms of action of nutraceuticals is therefore based on the types of diseases in whichthey have been reported to have health benefits.

16.3.1 Obsessive compulsive disorder

The medical/clinical treatment for a mental condition known as obsessive–compulsive dis-order (OCD) involves the prescription of tricyclic antidepressant clomipramine and other se-lective serotonin re-uptake inhibitors (SSRIs). Among the SSRIs usually prescribed includefluvoxamine, fluoxetine, sertraline, paroxetine, citalopram and escitalopram. Dual reuptakeinhibitors, including either venlafaxine or duloxetine (Jenike 2004; Fineberg and Gale 2005;Dell’Osso et al. 2006; Denys et al. 2007; Camfield et al. 2011), are also prescribed.



H3C ON+

O H3C

CH3

CH3

Fig. 16.3 Chemical structure of acetylcholine.

However, drugs used for OCD treatment have been reported to be associated with manyside effects such as anxiety, nausea, dizziness, sedation, diarrhoea, headache and insomnia(Jenike 2004; Camfield et al. 2011). Apart from the side effects, the treatment itself is saidto be temporal in the sense that once patients stop using the medication, they immediatelybecome sick again. This situation forces them to continue with the dose for a period afterOCD symptoms have stopped (Pato et al. 1988; Steiner 1995; Jenike 2004). In addition toall these drawbacks, the OCD treatment takes a considerable period of time before curativeeffects are realised by patients. Finally, OCD treatment is not universally effective in thesense that only 40–60% of patients treated with these medications experience improvementsin their condition (Pallanti et al. 2002; Jenike 2004; Camfield et al. 2011). Because ofthese disadvantages in the treatment of OCD, research on the use of nutraceuticals for OCDtreatment is underway.

16.3.1.1 Nutraceuticals for OCDs

Among the foodstuffs that are recommended as nutraceuticals for OCD treatment are those inwhich N-acetylcysteine (NAC; Figure 16.3), which is also a neurotransmitter, has been addedas a supplement. NAC is a derivative of cysteine which, unlike cysteine, is not usually obtainednaturally from dietary sources and therefore must be added as a supplement (Bonanomi andGazzaniga 1980). When a diet rich in NAC is consumed, the NAC is metabolised in the liversystem to form cysteine which has the ability to cross and enter the brain system (Smith2000). There, it plays the very important role of inhibiting the synaptic release of glutamate,bringing positive effects as far as the treatment of OCD and many other psychiatric disordersare concerned.

16.3.1.2 Mechanisms of action in OCD

To understand the mechanism of action of NAC in the treatment of OCD, it is necessary tointroduce metabotropic glutamate receptors (mGluRs) which bind glutamate, an amino acidcompound which performs the function of an excitatory neurotransmitter (Bonsi et al. 2005).The mGluRs are a class of receptors divided into three main groups (group I, II and III).Group I is mainly located in postsynaptic sites while groups II and III are mainly located inpresynaptic site on all neurons (Wright et al. 2001). The mGluRII and mGluRIII receptorsplay a crucial role in regulation of the synaptic release of glutamate; when stimulated by theextracellular glutamate, they inhibit the synaptic release of glutamate (Moran et al. 2001).The extracellular glutamate levels are known to be controlled by cysteine (a disulphidederivative of cysteine)-glutamate antiporter, found on the neuroglia cells in the neurons(Baker et al. 2002). When there is an increase of extracellular glutamate in the neurons,the cysteine-glutamate antiporter located in the neuroglia cells facilitates the exchange of



extracellular cysteine for the intracellular glutamate, which in turn stimulates the activityof mGluRII receptors and, in the process, inhibits the release of synaptic glutamate (Moranet al. 2003).

An investigation involving a randomised controlled trial of NAC 3000 mg/day has beenproposed (Camfield et al. 2011) to test the potential efficacy of NAC in the treatment strategyof OCD.

16.3.1.3 Glycine, myo-inositol, tryptophan and 5-hydroxytryptophan

A number of other amino acids and glucose-based nutrients, which are also used for thetreatment of psychiatric disorders, are being investigated as potential nutraceuticals for OCDtreatment (Camfield et al. 2011). They operate via many different types of mechanismsinvolving various receptors located in the brain cells. However, the N acetylcholine hasreceived more attention than glycine. This is due to the fact that the administration of theamino acid glycine is problematic, as large doses are associated with the side effect of nausea(Greenberg 2009).

16.3.2 Mental health problems

Myo-inositol is an isomer of glucose which has been used for the treatment of mental-relatedproblems for a long time, and is the most abundant chemically active compound (Frey et al.1998; Sarris et al. 2010). Myo-inositol is an ingredient found abundantly in many foodstuffsincluding fruits, beans, grains and nuts (Clements and Darnell 1980). It has been observedthat the exogenous administration of myo-inositol is directly related to the increase in thelevels of myo-inositol in the cerebrospinal fluid as well as in the brain (Einat and Belmaker2001). The mechanisms by which myo-inositol exerts its therapeutic effects are yet to bedetermined; there are many theories which are yet to be proven (Marazziti et al. 2000, 2002;Harvey et al. 2001, 2002).

Myo-inositol administration is known to have some drawbacks in the form of gastro-intestinal side effects. Normally categorised as mild side effects, these include diarrhoea,flatulence, bloating and nausea (Levine 1997; Carey et al. 2004). There are a number offood products which are known to be rich in the amino acid nutrients of tryptophan and 5-hydroxytryptophan, including egg white, cheese, Atlantic cod, spirulina, soybeans and pump-kin seed (Camfield et al. 2011). Unlike tryptophan, which can be obtained directly from diet,5-hydroxytryptophan has to be synthesised from tryptophan in the body system. Prescribing adiet high in tryptophan with the intention of raising the levels of 5-hydroxytryptophan is an op-tion which does not work however, due to the minute fraction of tryptophan which is convertedto 5-hydroxytryptophan (Brown 1994). Moreover, the amount of tryptophan that crosses theblood–brain barrier is still dependent on the partitioning ratio due to the presence of otherlarge neutral amino acids (LNAA) which compete for the same transporter (Birdsall 1998).

These limitations mean that tryptophan and 5-hydroxytryptophan are suitable as nutraceu-ticals for OCD because, under normal circumstances, OCD patients have been reported tohave lower tryptophan as well as tryptophan/LNAA ratios in their blood plasma. On the otherhand, a tryptophan-rich diet may not add much value to consumers free of OCD disorders,since research has shown that the depletion of tryptophan does not result in OCD symptomsin a healthy set of testants. It can therefore be interpreted that tryptophan may not be the onlyparameter that has an influence in the expression of OCD symptoms (Smeraldi et al. 1996).



16.3.3 Obesity and diabetes mellitus

There are two main basic types of diabetes mellitus, referred to as types 1 and 2. Excessiveelevation of blood glucose in the body is the major cause of diabetic complications, affectingmany organs and body systems in both type 1 and 2 diabetes mellitus. Type 1 diabetesmellitus is a condition of absolute insulin deficiency, and type 2 diabetes mellitus is a relativeinsulin deficiency condition caused by a beta cell failure as well as varying degrees of insulinresistance (Kaiser et al. 2003).

Diabetes diseases normally occur in people who tend to consume foodstuffs with a highcontent of trans-fats and saturated fatty acids. Controlling the consumption of saturated andtrans-fats is therefore essential for the improvement of blood lipid levels, diabetic parametersand reversing of the progression of diabetes. For this reason, diabetes treatment involves themodification of behaviour, lifestyle and eating habits (Dubnov et al. 2003).

Among the nutraceuticals that have been reported to treat diabetes is R-lipoic acid (R-LA),which is both a natural coenzyme and an antioxidant known to lower levels of serum lactateand pyruvate in sufferers of diabetes mellitus. The decrease of serum lactate and pyruvatehas the effect of enhancing the process of glucose uptake by activating insulin-signallingpathways (Korotchkina et al. 2004). Polar extract from some plants, for example a plantspecies from Gramin family known as Triticum repens, has demonstrated success in treatingdiabetes as it has shown potential in lowering the blood glucose levels (Maghrani et al. 2004).

Quercetin flavonoids are among those compounds which are known to have antidiabeticactivity. A study by Vessal et al. (2003) has indicated that quercetin flavonoid was able toexert regeneration of pancreatic islets, and this compound was suspected of having an effecton increasing the release of insulin. Hif and Howell (1984, 1985) published findings whichshowed that quercetin flavonoid was able to induce insulin release together with an increasein the uptake of calcium ions from isolated islets.

16.3.4 Cardiovascular diseases

Diet rich in flavonoids, especially plant-derived phenolic compounds such as those fromfruits, vegetables and grains, have been reported to have anticancer and anti-inflammatoryactivity with beneficial health effects on cardiovascular and neurodegenerative diseases (seeChapter 1). Pomegranate juice (POM) is known to be the richest source of polyphenolicantioxidants with health benefits related to heart conditions. Pomegranate is rich in a numberof flavonoid compounds, including tannins and anthocyanins. The health benefits of diets richin polyphenolic compounds is due to the ability of polyphenols to transfer electrons, chelateferrous ions and scavenge reactive oxygen species (Kandaswami and Middleton 1994).

It has been reported that a significant and constant intake of diet containing the long-chainpolyunsaturated fatty acids of eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA),also known as �-3 fatty acid (mainly found in fish such as salmon, rainbow trout, mackereland sardines), has benefits to health (Mandel et al. 2005). These ingredients are especiallybeneficial to individuals who are overweight, suffering from hypertension and on weightloss diets. The compounds decrease triglycerides, thus lowering the heart rhythms whichwill tend to lower the blood pressure and improve the blood-clotting regulation mechanisms(Leaf et al. 1999).

It has been reported that a diet rich in flavonoid compounds has a positive effect onthe prevention of endothelial dysfunction. This is possible as these compounds tend toenhance the vasorelaxant process, which cause the reduction of arterial pressure (Iijima and



Aviram 2001; Bernatova et al. 2002). The reduction of arterial pressure which is importantin the reduction of endothelial dysfunction is important because otherwise the process willencourage the initiation of cardiovascular diseases (Jayakody et al. 1985).

16.3.5 Cancer

Fresh fruits and vegetables are among the functional nutrition that has been reported to havehealth benefits including that of decreasing cancer risk (Donaldson 2004). The presence ofantioxidant flavonoids in these foodstuffs contributes greatly to their anticancer properties.As well as acting as radical scavengers these flavonoid antioxidants play a very importantrole as inducers of enzymes, decreasing the cancer risk. These enzymes include catalasesand glutathione peroxidase (Frei and Higdon 2003).

The mechanisms of action of these anticancer compounds are believed to be acting on mul-tiple target-signalling pathways, for example activator protein-1 (AP-1) and/or nuclear factor� B (NF-nB). All of these signalling pathways play crucial roles in tumour promoter-inducedcell transformation and tumour promotion (Sarkar and Li 2004). In some other reports fromanimal studies, it has been demonstrated that flavonoid antioxidants from plants such asgreen tea catechins, curcumin, anthocyanins, quercetin and silibinin have high chemopre-ventive activity (Kresty et al. 2001). In many other studies, the anti-inflammatory activityof flavonoids and other related class of compounds and derivatives have been numerouslyreported. For instance, flavone glycosides, flavonol glycosides, flavonoid aglycons, apigenin,luteolin and quercetin have been shown to have health benefits as far as anti-inflammatoryactivity is concerned (Lee et al. 1993; Farmica and Regelson 1995; Hang et al. 2002). Otherflavonoid compounds such as hesperidin, an extract from citrus plants, has been reported toexert anti-inflammatory as well as analgesic effects (Shahid et al. 1998).

16.3.5.1 Mechanism of flavonoid antioxidants in reducing cancer risk

Nutraceuticals of interest in treating cancer diseases include the isoflavones (Mason 2001).The major source of dietary isoflavones which occur naturally in the form of glycosides issoybeans (Messina 1999). Apart from being nutraceuticals for cancer diseases, isoflavones arealso suspected to perform the protective function against osteoporosis, menopausal symptomsand high levels of cholesterol in the blood (Mason 2001; Awaisheh et al. 2005).

Huang et al. (2002) have reported that extracts of raspberries inhibited benzo(a)pyrenediol-epoxide-induced transactivation of activated protein 1 and nuclear factor kappa B. Themechanism of the inhibition has been suggested to be via both the down-regulation of protein(enzyme) cyclooxygenase-2 (COX-2) as well as the down-regulation of the transcription ac-tivators, AP-1 and NF-nB in JB-6 epidermal cells (Huang et al. 2002). A similar mechanisticpathway has been suggested for the phenolic antioxidants from green tea and soybeans, i.e. apolyphenol epigallocatechin-3-gallate and isoflavone genistein, respectively. These polyphe-nols play important roles in the inhibition of the activation of NF-nB and AP-1 transcriptionactivators, thus preventing the COX-2 induction in the epidermal/epithelial cells (Park andSurh 2004).

Extracts from some plants such as Curcuma longa L. from the family Zingiberaceae,which also yields the yellow colouring agent curcumin, have been reported to inhibit theexpression of COX-2 in epidermal cells. They also suppress carcinogenesis in the oral cavity,skin, liver, lung, colon, stomach and breast. The mechanism for the inhibition of the extracts



from Curcuma longa has been suggested to be via the inactivation of transcription factorNF-nB, the regulation of the transcription factors NF-nB, signal transducer and activator oftranscription 3 (STAT-3) and suppression of InB kinase (Surh 2002).

Apart from phytoantioxidants, phenolic extracts from dietary supplement milk-thistle,known as silibinin and silymarin, have been reported to have antihepatotoxic activity aswell as activity against skin and prostate cancer (Bhatia and Agarwal 2001). The reportedmechanism of action of silibinin has been linked to its ability to induce transcription factorswhich then inhibits the kinase activity of CDKs and cyclins, resulting in the arrest of G1 aswell as the control of cell growth (Bhatia and Agarwal 2001).

16.3.6 Brain development

Scientific studies have shown that there is an association between the build up of iron/irongradient together with reactive oxygen species/reactive nitrogen species (ROS/RNS) (su-peroxide, hydroxyl radical and nitric oxide) with the death of brain cells (neurons) (Mandelet al. 2005). Moreover, other studies have linked the sulphoxide oxidation of some methionineamino acid residues with the occurrence of certain brain diseases. This is because the buildup of cellular toxicity leads to the accumulation of some peptides including amyloid-betapeptides, a-synuclein and cytochrome C (Moskovitz 2002). To reverse this oxidation process,the presence of methionine sulphoxide reductase enzymes is required (Moskovitz 2002). To-gether with this enzyme, studies have shown that the presence of effective brain-permeableiron-chelating and antioxidant-containing bioactive compounds play a very important rolein the prevention of neurons death (Mandel et al. 2005).

There exist a number of natural dietary antioxidant polyphenolic flavonoids, present infruits and vegetables such as green tea, pomegranate juice, raspberries, blueberries and redwine (all of which are rich in polyphenol (-) -epigallocatechin-3-gallate), which show activitytowards neurodegeneration disorders (Mandel et al. 2003). The activity by the polyphenolicflavonoids in fruits and vegetables is believed to be due to their radical scavenging property,transition metal chelating ability and their anti-inflammatory activities (Mandel and Youdim2004; Weinreb et al. 2004; Joseph et al. 2005). Polyphenol epigallocatechin-3-gallate arebeneficial not only as antioxidant and iron chelaters, but also as molecules which playan important role in the processes which govern cell survival or death genes and signaltransduction pathways (Schroeter et al. 2002). Other antioxidant flavonoid compounds, forexample EGb 761 which is extracted from Ginkgo biloba leaves, have been reported to haveactivity towards cognitive function, in memory impairment cases and in extending life span(Luo 2001).

Other nutraceuticals known to be beneficial in brain development are polyunsaturatedfatty acids (PUFAs) which include �-3-fatty acids such as linolenic, ecosapentaenoic anddocosahexaenoic acids as well as �-6 fatty acids (linoleic and arachidonic acids). Thesecompounds are precursors of long-chain fatty acids such as eicosapentaenoic acid (EPA) anddocosahexaenoic acid (DHA), which human bodies are unable to synthesise. These samefatty acids have been reported to be important in reducing plaque formation in the arteries(Milner and Alison 1999). The best dietary sources of �-3-fatty acids include vegetable oilsor fatty fish such as herrings or sardines (Childs and King 1993).

The mode of action of PUFAs which enable them to provide health benefits in-volves the formation of compounds such as prostacyclins and thromboxanes, as wellas pro-inflammatory cytokine production which include: tumour necrosis factor alpha



and interleukin-1; modulation of the hypothalamic–pituitary–adrenal anti-inflammatory re-sponses; and induction of the release of acetylcholine (Das 2000).

As well as playing an important role in brain development, diets rich in natural PUFAshave been reported to have health benefits in controlling immune function, blood pressure,bloodstream cholesterol and triglycerides levels (Russo et al. 1995; Kawasaki et al. 2000;Straniero et al. 2008; Chen et al. 2009).

16.3.7 Age-related diseases

When the functioning of body tissues and organs slows down due to miscellaneous mutations,especially the mutations associated with neurons as well as the general damage to proteinscaused by oxidative stress, the body become prone to age-related diseases and disorders.As discussed in Chapter 1, the generation of oxidative stress due to the reactive species(ROS/RNS) is considered responsible for accelerating the aging process which is charac-terised by, among other symptoms, brain-related diseases. These diseases/disorders includeage-associated cognitive decline and neuronal loss in neurodegenerative diseases such asAlzheimer’s, Parkinson’s and Huntington’s diseases (Markesbery 1997; Jenner 1998).

There exist compounds which are important constituents of nutritional dietary supple-ments, for example choline, folic acid and their metabolites (e.g. betaine, a choline metabo-lite), which are crucial for the normal and smooth functioning of body cells. These compoundsare known to play important roles in the structural integrity and signalling functions of cellmembranes (Zhu et al. 2004).

16.3.8 Viral diseases

There are a number of naturally occurring flavonoids which have been reported to have apromising activity against certain virus particles, include quercetin, morin, rutin, dihydro-quercetin (taxifolin), apigenin, catechin and hesperidine (Selway 1986). The antiviral activityof the flavonoids seems to be dependent on their structural chemistries, which demonstratefeatures such as the absence of sugar/glycoside moiety and the presence of hydroxyl groupat the 3-position in the flavonoid structure.

Other functional groups related to flavonoids such as flavonols and flavons have also shownto have antiviral activity; flavonols have been observed to be more active than flavones againstHerpes simplex virus type 1 (Tapas et al. 2008). In terms of comparison of antiviral activity,compounds can be ranked (in order of effectiveness): galangin, kaempferol and quercetin(Thomas et al. 1988). Activity towards HIV types I and II or other similar immunodeficiencyviruses have found flavans to be more active than flavones and flavonones (Gerdin andSrensso 1983).

16.3.9 Anti-gastrointestinal ulcers and anti-acids

Alarcon et al. (1994) and Izzo et al. (1994) reported the activity of flavonoids extracted fromOcimum basilicum plant species, which belong to a family Labiatae, against ulcers. Theflavonoid extracts (quercetin, rutin and kaempferol) were not only active in decreasing theulcer index, but also inhibited the effect of gastric acid and pepsin secretions.



16.3.10 Liver cell protection

A number of flavonoid compounds such as silymarin, apigenin, quercetin and naringenin haveshown health benefits when they protect liver cells against cyanobacterial toxins (microcrystinLR) (Carlo et al. 1993). Other flavonoid compounds, including rutin and venoruton, havealso been reported to play a protective role in cases of cirrhosis (Lorenz et al. 1994).

16.3.11 Blood coagulation and thrombotic diseases

Diseases associated with the formation of a blood clot within blood vessels (thrombosis),causing the obstruction of the flow of blood in the body, are known to affect many peopleworldwide (Furie and Furie 2008). The formation of a blood clot is known to have advantages,for instance when there is an injury on the blood vessels which may cause bleeding, thethrombocytes (also known as platelets) and fibrin aggregate to form a blood clot to stopbleeding. However, there are instances where blood clots may form in the vessels even whena blood vessel is not injured, for instance if there is a disturbed blood flow or a geneticaldisorder known as hypercoagulability. In cases where clotting is very severe, the situationmay lead to thrombotic diseases.

Some older publications have reported that extracts from tea have health benefits incombating thrombotic diseases by reducing blood coagulability, increasing fibrinolysis andprevention of thrombocytes adhesion and aggregation (Lou et al. 1989). Some flavonoidderivatives such quercetin, kempferol and myricetin have also been reported as being ableto prevent the formation of blood clots in animals (Osman et al. 1998). Flavonoids in theprevention of blood clot formation have been linked to their ability to inhibit the activity ofcyclooxegenase (COX) and lipoxigenase pathways (Alcaraz and Ferrandiz 1987). Flavonolderivatives also have been reported to be antithrombotic due to their ability to scavengefree radicals. This is advantageous because it tends to maintain the proper concentration ofendothelial prostacyclin and nitric oxide (Gryglewski et al. 1987). Thrombocytes themselvesare known to have the self-mechanism of releasing lipid peroxides and oxygen free radicals.Like flavonols, these have the ability to inhibit the endothelial formation of prostacyclin andnitrous oxide (Gryglewski et al. 1987).

16.3.12 Blood cholesterol cases

Diets containing natural phytosterols have been reported to have benefits in maintaining thelevel of cholesterol in the bloodstream. Phytosterols work by interfering with the uptake ofcholesterol from the intestinal tract (Heinemann et al. 1991; Jones et al. 1999), keeping it atacceptable lower levels.

16.4 CONCLUSION

This chapter provides evidence of the promising trend for nutraceuticals in combating orlessening the risks of some chronic diseases as well as other physiological health benefits.Since the active ingredients of these nutraceuticals are found in many foodstuffs, futureresearch activities may further strengthen their reliability as remedies of the health problemsfaced by many people.



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FURTHER READING

Moran, M. M., McFarland, K., Melendez, R. I., Kalivas, P. W. & Seamans, J. K. (2005) Cystine/glutamateexchange regulates metabotropic glutamate receptor presynaptic inhibition of excitatory transmission andvulnerability to cocaine seeking. Journal of Neurosciences 25, 6389–6393.

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Chemistry of Food Additives and Preservatives (Msagati/Chemistry of Food Additives and Preservatives) || Nutraceuticals and Functional Foods