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AssignmentAssignment
Subject : Breeding Designer Crops (GPB822)Subject : Breeding Designer Crops (GPB822)
Presented by: Mr.Presented by: Mr. IndranilIndranil BhattacharjeeBhattacharjee
Student I.D. No.: 17PHGPB102Student I.D. No.: 17PHGPB102
Presented to : Prof. (Dr.)Presented to : Prof. (Dr.) B.G.SureshB.G.Suresh
SamSam HigginbottomHigginbottom University of Agriculture, Technology &University of Agriculture, Technology &
SciencesSciences
AllahabadAllahabad--211007211007
History
“The physical body is the product of diet and
sensory input (lifestyle). Similarly, all diseases are
the result of non correct diet and lifestyle. Diet
and lifestyle wholesome and unwholesome are
the foundations of health and illness”
Caraka Samhita Sutrasthana (1, 28:45)
An Apple a Day Keeps the Doctor Away.
-English Proverb
• Greek Physician Hippocrates,
Known as father of Medicine.
(said several centuries ago)
“Let Food be Your Medicine”
The Philosophy behind is:
“Focus on Prevention”
( World( World HealthHealth Organization, 1947 )Organization, 1947 )
“Health is a state of complete
well-being, physical, mental and
social, and not merely the
absence of disease”
The definition of health status.
Definition
( Dame( Dame CicelyCicely MaryMary SaundersSaunders))
“Do not be
worried on how to add days
to our life, but on how to give
more life to our days”
The main focus.
(Merriam-Webster, 2013)
- 1989 Stephen DeFelice, President of the
Foundation for Innovation in Medicine (Cranford), NJ, USA.
Nutraceutical: food or part of food that
provides medical or health benefits,
including the prevention and/or
treatment of a disease.
Nutraceuticals: TORs.
The term nutraceutical refers to products for oral
use containing high concentrations of active principles derived
from food, and provide health benefits from a preventive and/or
therapeutic point of view.
They are not considered drugs, there is lack of
controlled studies stating their real efficacy.
Nutraceuticals: TORs.
There is lack of a shared regulation
assessment.
• The term “Nutraceutical” was coined from
“Nutrition” & “Pharmaceutical” in 1989 by
Stephen DeFelice,
MD, Founder and Chairman of the Foundation for
Innovation in Medicine (FIM).
• Other words used in the context:
Dietary supplementation, Functional, Multi-
functional Foods, etc.
• Nutraceutical can be defined as
“ A food or part of food or nutrient, that
provides health benefits, including the
prevention and treatment of a disease.”
Class /
components
Source Potential benefit
1. Fatty acids
CLA
Milk & Meat Improve body
composition,
reduce cancers
n-3 FA(DHA,
EPA)
Fish oils, berseem &
maize
fodder,mustard,linseed,
rapeseed
Reduce CVD &
improve mental,
visual function
Examples of functional
components
Class /
components
Source Potential benefit
2. Polyphenols
Anthocyanidin
e
Fruits Nutralises free
radicals, reduce
risk of cancerCatechins Tea,babul pods,mustard
cake,rape seed,salseed
Flavonone Citrus
Flavones Fruits, vegetables,soya
bean
proanthocyani
dine
Cocoa,
chocolate,tea,rape seed
Reduce CVD
EXAMPLES OF FUNCTIONAL COMPONENTS
3. Saponins Soybeans,GNC,lucer
ne,chick pea
Lower cholesterol,
anti cancer
4.Probiotics / Prebiotics / Synbiotics
Lactobacillus Dahi,yogurt Improve GI health
Fructo -
oligosaccharides
Whole grains,
onions, combination
of Pro & Prebiotics
5.Phytoestrogen
Daidzein ,
Zenistein
Soybean, flax,
lentilseed,maize,
berseem,lucerne,sub
abul fodder
Reduce menopause
symptoms,  bone
health
Lignans Flax,rye, vegetables Reduce cancer and
heart diseases
6.Caroteinoids
- caroteine Berseem,lucerne ,oat &
maize fodder, Carrots,
vegetabels,fruits
Nutralises free
radicals
Luteine vegetabels Healthy vision
Zeoxanthine Eggs,citrus,corn
Lycopene Tomatoes Reduce prostate
cancer
7.dietary fiber
Insoluble fiber Wheat bran Reduce breast,
colon cancer
-glucan Oats Reduce CVD
Whole grain Cereal grains
Brand name Components Function
Betatene Carotenoids Immune function
Xangold Lutein esters Eye health
Lipoec -lipoic acid Potent
antioxidant
Generol Phytosterol CHD reduction
Premium
probiotics
probiotics Intestinal
disorder
Soylife Soyabean
phytoestrogen
Bone health
NUTRACEUTICALS AVAILABLE IN MARKET
Brand name Components Function
Z-trim Wheat Zero calorie fat
replacer
Linumlife Lignan extract flax Prostate health
Fenulife Fenugreek
galactomannon
Control blood
sugar
Teamax Green tea extract Potent antioxidant
Marinol  3 FA, DHA, EPA Heart health
protection
Clarinol CLA Weight loss
ingredient
Cholestaid Saponin Reduce cholesterol
NUTRACEUTICALS AVAILABLE IN MARKET
i. The olistic medical approach.
ii. The static approach: the patient, often unaware of a
potential health risk, waits till the clear signs of the onset
of a disease appear (watchful waiting or active
surveillance medicine) and then obtain a diagnosis and
starts using prescription drugs.
iii. The nutraceutical dynamic approach also known as
“initiative medicine or proactive medicine”: taking
preventive action before the onset of a disease instead
of waiting for the disease to become evident.
Scope of use - Some preliminary considerations
on handling an health condition.
Primary prevention
Secondary prevention
• Lifestyle – behaviour – dietary habits
Possible approaches:
• Drugs (waitchful waiting medicine)
• Nutraceuticals (pro active medicine)
The availabile tools.
The possible approaches.
Nutraceuticals: TORs.
Classification
Broadly can be classified as:
• Nutrients: Substances which have established
Nutritional functions e.g. Vitamins, Minerals, Amino Acids,
Fatty acids, etc.
• Herbals/ Phytochemicals: Herbs or Botanical products
• Dietary Supplements: Probiotics, Prebiotics,
Antioxidents, Enzymes, etc.
Nutraceuticals: classification.
Nutraceuticals: classification.
Nutraceuticals: classification.
Legal View
Nutraceuticals: food or drugs?
QUESTION placed at the European Commission E-000065/2011 (dr.
Christian Muscardin) about the presence on the market of products, called
"nutraceuticals", which, unlike normal dietary supplements, have the effects
of preventing or reducing the risk of disease, especially degenerative of a
particular structure or function of the organism.
• ANSWER given by Commissioner John Dalli on behalf of the European
Commission, February 21, 2011:
• The term "nutraceutical" is not currently defined in Community
legislation.
• These products, under the current legislation, should be classified as
dietary supplements or following authorization for marketing as drugs.
Court of Justice of the European Union: medicine/drug food.
• if it is presented as having properties for treating or preventing disease in human beings
(definition of "presentation");
• if it is to be administered to human beings with a view to making a medical diagnosis or to
restoring, correcting or modifying physiological functions (definition "by function").
Plant-based products marketed in the form of dietary supplements (vegetable origin similar
to nutraceuticals) must comply with Directive 2002/46/EC on food supplements and
Regulation (EC) n. 1924/2006 on the claims about the effects of nutrition and health foods.
If a product, taking into account all its characteristics, may fall within the definition of a
medicinal product and the definition of a product covered by other Community legislation,
apply the Directive 2001/83/EC revised by Directive 2004/27/EC (food and drugs
nutraceuticals).
Nutraceuticals: food or drugs?
Source of Nutraceuticals: where can be
found.
An approximate number of about 30,000 phyto components have
been identified in plants.
• Approximately 5,000-10,000 are present in plant foods of
common use/consumption.
• Assuming 5 daily servings of fruits and vegetables, you ensure
the intake of about 1.5 g / day of nutraceuticals
phytocomponents.
Nutraceuticals: where can be found.
Nutraceuticals: where can be found.
Nutraceuticals: where can be found.
Nutraceuticals: where can be found.
Uses of Nutraceuticals: therapeutic uses.
Prevention/Therapy using nutraceuticals.
- Hypercholesterolemia
- Hypertension
- Type II diabetes
- Hypertryglyceridemia
- ………..
Metabolic syndrome
A nutraceutical pro active
approach is possible?
Nutraceuticals: possible uses.
An example.
The artichoke (Cynara scolymus) extract polyphenols: the main
components are chlorogenic acid, caffeic acid and cynarin.
In year 1900 scientific research has focused on the properties
hepatostimulants, hepatoprotective, choleretic and
hypocholesterolemic associated to extracts of Cynara leaves, as
advocated by medicine doctors already in year 1700.
Cynara extracts
Chlorogenic acids
Flavanoids
• 5-O-caffeilchinic acid
• 1,5-dicaffeilchinic acid
• caffeic acid
• Luteoline
• Cinaroside
• Scolimoside
Artichoke: bioactive substances.
Nutraceuticals: possible uses.
Artichoke variety mg chlorogenic
acid/100g
Romolo stem 27,826
Romolo head 6,276
Romolo leaves 0,5
Artichoke variety Total phenolic
content
mg AGE/100g
DPPH Îźmol
TE/100g
FRAP Îźmol
TE/100g
Romolo stem 21,35 78,61 104,46
Romolo head 4,53 38,95 24
Romolo leaves 26,44 124,47 64,54
Anti oxidant activity:
Nutraceuticals: possible uses.
Sustainable use of industrial wastes.
Bioactive molecules
rich sources
Nutraceuticals: recovery/uses.
Cholesterol-lowering action of artichoke
extracts.
1. increased choleresis and then increased excretion
of salts and bile acids rich in cholesterol;
2. inhibition of cholesterol biosynthesis.
• Cholesterol is synthesized in the liver from acetyl-CoA
and released in plasma.
• The extent of hepatic biosynthesis is controlled by the
intracellular concentration of cholesterol.
Nutraceuticals: possible uses.
Nutraceuticals: possible uses.
Green tea: functional food/nutraceutical
Obtained from a plant: Camellia sinensis (L.).
The freshly harvested leaves are immediately processed to inactivate the
enzymatic oxidation process.
• Green tea has the highest concentration of polyphenols than other types of
tea.
• Green tea has hypoglycemic properties.
Nutraceuticals: possible uses.
Nutraceuticals: possible uses.
Catechins neuro protective role.
0
20
40
60
80
100
120
C EC ECG EGC EGCG GC CG
mg/gdw
C = (-)-Catechina
EC = (-)-Epicatechina
ECG = (-)-Epicatechingallato
EGC = (-)-Epigallocatechina
EGCG = (-)-Epigallocatechingallato
GC = (-)-Gallocatechina
CG = (-)-Catechingallato
Nutraceuticals: possible uses.
0
1
2
3
4
5
6
7
8
Cholesterol(mg/dL/Âľgprotein)
ECG = (-)-Epicatechingallato EGCG = (-)-Epigallocatechingallato CG = (-)-Catechingallato
Nutraceuticals: possible uses.
0
1
2
3
4
5
6
Triglycerides(mg/dL/Âľgprotein)
C = (-)-Catechina ECG = (-)-Epicatechingallato EGCG = (-)-Epigallocatechingallato
Nutraceuticals: possible uses.
Nutraceuticals: possible uses.
Catechins: antioxidant action.
Nutraceuticals: possible uses.
Catechins: cardio protective role.
Nutraceuticals: possible uses.
Apple: an in se functional food ?
I. Significant source of phytocompounds (flavonoids) among which quercetin (5 -
15 mg / 100 g) is the main one.
II. Contains antioxidant polyphenols with proven efficacy.
III. Apple extracts inhibit the cholesterol uptake.
IV. The effect on the organism is similar to statins.
Apple: extract nutraceutic
FleshFlesh
Nutraceuticals: possible uses.
Cholesterol uptake
inhibition.
OligomericOligomeric procyanidinsprocyanidins
Red Delicious Pink Lady Fuji Golden DeliciousAnnurca
BucceBucce
PolpaPolpa
Hypocholesterolemic metabolites
Nutraceuticals: possible uses.
Justification of why we use?
Metabolic syndrome (SM): some data.
50% of people from Europe are
overweight
30% suffer from obesity
23-24% of USA suffer from SM
WHO estimated an about 2.5
millions of people dead
worldwide due to overweight
and to cardiovascular diseases
SM: ICD-9-CM code = 277.7
Van Gaal LF, et al. Lancet 2005;365:1389-97
Abdominal obesityAbdominal obesity
Glucose intolerant/Glucose intolerant/InsulineInsuline
resistencyresistency
HypertensionHypertension
AterogenAterogen dislipidemydislipidemy
ProinflammatoryProinflammatory state/state/
ProtromboticProtrombotic
National Cholesterol Educational Program (NCEP), Adult Treatment Panel (ATP) III; 2001
DiabetisDiabetis CVDCVD
Metabolic syndrome “cluster” of risk factors.
Metabolic syndrome.
Central obesity (european and north american population).
i. Waist circumference ≥ 94 cm (male) and ≥ 80 (female)
Together with at least TWO of the following:
ii. TG > 150 mg/dL or specific treatment
iii. CHDL < 40 mg/dL (male) e < 50 mg/dL (female) or specific
treatment
iv. SBP ≥ 130 mmHg e/o DBP ≥ 85 mmHg or anti hypertension
treatment
v. Glycemic index ≥ 100 mg/dL or a DM2 diagnosis
Nutraceuticals and metabolic syndrome.
Apple variety “annurca”
Lipidic profile in patients treated with
atorvastatin v/s nutraceutical (NUT)
Apple variety “annurca”
Therapeutic approach.
Therapeutic approach.
METABOLIC SYNDROME
ORGAN DAMAGE
PRESENCE
YESNO
LYFESTYLE CHANGE
NUTRACEUTICALS
PHARMACOLOGIC
THERAPY
Active Bio-chemical Components
NUTRIENTS
• Most common Nutrients used/ supplemented as
Nutraceutical are:
Minerals and Vitamins.
or in combination
or in combination with other antioxidants
Health Benefits of different common nutrients
Vitamins
Fat Soluble Vitamins
• Vitamin A: Acts as antioxidant, essential for growth and
development, maintains healthy vision, skin and mucous
membranes, may aid in the prevention and treatment of
certain cancers and in the treatment of certain skin
disorders.
• Vitamin D: Essential for formation of bones and
teeth, helps the body to absorb and use
calcium
• Vitamin E: Antioxidant, helps to form blood cells,
boosts immune system
• Vitamin K: Essential for blood clotting
Water Soluble Vitamins
• Vitamin C: Antioxidant, necessary for healthy bones,
gums, teeth and skin. Helps in wound healing,
prevent from common cold
• Vitamin B 1: Helps in carbohydrate metabolism,
essential for neurological function.
• Vitamin B 2: Energy metabolism, maintain healthy
eye, skin and nerve function.
• Vitamin B 3: Energy metabolism, brain function
• Vitamin B 6: Helps to produce essential proteins,
convert proteins to energy
• Vitamin B 12: Help in producing genetic material,
formation of RBC, maintenance of CNS, synthesis of
amino acids, involved in metabolism of protein, fat
and carbohydrate.
• Folic acid: Helps in RBC formation, formation of
genetic material of cell, very much essential during
pregnancy
• Pantothenic acid: Aids in synthesis of cholesterol,
steroids, and fatty acids, crucial for intraneuronal
synthesis of acetylcholine
Vitamins like Compounds
• L- Carnitine: Helps in oxidation of fatty acids, role in
oxidative phosphorylation,
• Choline: Lipotropic agent, used to treat fatty liver and
disturbed fat metabolism,
• Inositol: For amino acid transport and movement of
Potassium and sodium,
• Taurine: Helps in retinal photoreceptor activity, bile acid
conjugation, WBC antioxidant activity, CNS
neuromodulation, platelet aggregation, cardiac
contractibility, sperm motility, insuline activity,
• Minerals:
• Calcium: essential for bone and teeth, maintaining bone
strength, nerve, muscle and glandular function, blood
clotting,
• Iron: energy production, Hb, oxygen transport,
• Magnesium: for healthy nerve and muscle function, bone
formation,
• Phosphorous: energy production, phosphorylation process,
bone and teeth, for genetic material,
• Cobalt: component of Vit. B 12 and B 12
coenzymes,
• Copper: Hb and collagen production, function of
heart, energy production, absorption of Iron,
• Iodine: proper function of Thyroid gland,
• Chromium: with insulin it helps in conversion of
carbohydrate and fat into energy, treatment of
diabetes,
• Selenium: Antioxidant, functioning of heart
muscle, part of GPX enzyme,
• Zinc: Essential for cell reproduction, for
development in Neonates, wound healing,
production of sperm and testosterone
hormone,
• Herbals:
• Aloe vera: Anti-inflammatory, emollient, wound
healing,
• Evening Primrose oil: Dietary supplement of linoleic
acid, treatment of atopic eczema,
• Garlic: Antibacterial, antifungal, antithrombotic,
antiinflammatory,
• Ginger: carminative, antiemetic, treatment of
dizziness
• Ginseng: Adaptogen,
• Green tea: Antioxidant, reduces risk of CVD,
enhances humoral and cell mediated Immunity,
• Vegetables, fruits, whole grain, herbs, nuts and
various seeds contain an abundance of phenolic
compounds, terpenoids, sulphur compounds,
pigments etc. that has been associated with
protection / treatment of certain disease
conditions,
•Phytochemicals:
• Phytochemicals could provide health benefits as:
1. Substrate for biochemical reactions
2. Cofactors of enzymatic reactions
3. Inhibitors of enzymatic reactions
4. Absorbents that bind to & eliminate undesirable
constituent in the intestine
5. Scavengers of reactive or toxic chemicals
6. Enhance the absorption and / or stability of essential
nutrients
7. Selective growth factor for beneficial bacteria
8. Fermentation substrate for beneficial bacteria
9. Selective inhibitors of deleterious intestinal bacteria
Various Phytochemicals
Phytochemicals Source Role
Tocotrienols &
tocopherols
Grains Suppressed the growth of
diverse tumors cell lines via
initiation of apoptosis and
concomitant arrest of cells in
the G1 phase of the cell cycle
Carotenoids Fruits &
vegetables
Antioxidants, protects against
uterine, prostate, colorectal,
lung and digestive tract
cancers, and protection to
other antioxidants.
Limonoids Citrus fruits Inhibiting phase I
enzymes & inducing
phase II detoxification
enzymes in liver, provide
protection to lung tissue.
Phytosterols Various
plants
Exhibit anti-inflammatory,
anti-neoplastic, anti-
pyretic & immune-
modulating activity,
decrease cholesterol
Phenolic
constituents
Various
plants,
wholegrain
Antioxidants, lowers the
risk of CHD, diabetes,
hypertension etc.
Flavonoids Grapes, wines Action against free
radicals, free radicals
mediated cellular
signaling, inflammation,
allergies, platelet
aggregation, &
hepatotoxins
Catechin &
gallic acids
Grapes,
berries, cocoa,
green tea,
acacia spp.
Antioxidants, free
radical scavenging
ability, inhibition of
eicosanoid synthesis,
reduces CHD
Isoflavonoids Soybeans Treating cancers &
osteoporosis
Anthocyanidins Fruits & flowers Antioxidants & anti-
mutagenic properties
Glucosinolates Cruciferous Activators of liver
detoxification
enzymes, inhibit the
neoplastic effect of
various carcinogens
Indoles Reduces estrogen-
dependent cancer
risk,
Fiber Various
vegetables,
fruits,
Protects against
colorectal diseases,
Method to enhance active components in
food
• Manipulating the diet to get maximum
level of active components
• Combination of food ingredients rich in
nutraceuticals
• Fortifying food with active ingredients
• By fermentation of food products
• Changing food habits to natural type of
diet
Monomeric and oligomeric phenols.
Catecolic derivatives.
curcumin
hydroxytyrosol
alkylresorcinols
carnosol
oleuropein
Resorcinic derivatives.
Amorpha
fruticosa
Resveratrol
Liquorice
Tomatoes, grapes, cauliflower
Oligomeric polyphenols –Tannins.
Apple
Dates
Pomegranate
Raspberry
80
Nutraceutic potential of grape polyphenols.
Flavonols
Antocianins
Pro-antocyanidins Shao et al. (2006). Grape seed proanthocyanidin extract
attenuates oxidant injury in cardiomyocytes.
Pharmacological Research
PoliphenolsPoliphenols contentcontent:: juicejuice >> winewine >> grape/fruitsgrape/fruits
“Antioxidant protection of
the cardiovascular system”
Malvidin-3-O-glucoside
114 mg/100 mL
35% anthocyanins
Main active molecules.
Myricetin-3-O-glucoside
93 mg/100 mL
27% flavonols
Quercetin-3-O-glucuronide
76 mg/100 mL
22% flavonols
Quercetin-3-O-glucoside
80 mg/100 mL
23% flavonols
AntocianinsAntocianins FlavonolsFlavonols
0.00
100.00
200.00
300.00
400.00
500.00
600.00
700.00
800.00
900.00
1000.00
Phenols Flavonols Anthocyanins
992.00 Âą 2.1
404.77 Âą 1.5 402.41 Âą 0.8
989.80 Âą 1.8
402.05 Âą 1.6 400.12 Âą 0.9
mg/100mL
RGJ lioRGJ
Red grape juice poliphenolic content before (RGJ) and after
lyophilization (lioRGJ).
83
84
Antioxidant activity of red grape juice before (RGJ) and
after lyophilization (lioRGJ)
FRAP = Antiradical indirect power
DPPH = Antiradical direct power
“Antioxidant profile and“Antioxidant profile and in vitroin vitro cardiac radicalcardiac radical--scavengingscavenging vsvs propro--oxidant effects ofoxidant effects of
commercial red grape juices (commercial red grape juices (VitisVitis viniferavinifera L. cv.L. cv. AglianicoAglianico N.)”N.)”
Gian Carlo Tenore, Michele Manfra, Paola Stiuso, Luigi Coppola, Mariateresa
Russo, Isabel Maria Gomez Monterrey, Pietro Campiglia
Journal of Agricultural and Food Chemistry, 2012
Nutraceutical potential of grape polyphenols.
Grape juice:
“Functional food → Nutraceutic potential”
Possible use as nutraceutical:
Support for the treatment of neoplastic diseases.
Nutraceutical potential of grape polyphenols.
(Jones et al., Int. J. Cancer Res., 10(1), 46-53, 2014)
Hyperglicemy: a new therapeutic
approach.
PPARg (proliferator-activated receptor gamma) a nuclear receptor has a primary role in
lipid and carbohydrates metabolism.
Problem: PPARg-targeting drugs are characterized by unwanted side effects.
Natural products from edible biomaterials are a structurally different resource to easy
the complex side effects of common use drugs.
It can be adopted a nutritional tailored approach to easy side unwanted effetcts.
Amorfrutins, extracted from the edible part of two legumes, namely Glycyrrhiza
foetida and Amorpha fruticosa, are new and potent anti diabetes agents.
They selectively bond to the PPARg receptor and activate it.
Hyperglicemy.
“Beyond diet, before drugs” (E.
Novellino, 2012)
A. Santini, Journal of Food Research,
2014, (4), 1-5.
Pro active nutraceutical approach:
when and where?
“Beyond diet, before drugs” (E.
Novellino, 2012)
Antonello Santini and Ettore Novellino
Current Bioactive Compounds, 2014, 10(1), 1-12.
Increasing Nutraceuticular Value of food
through Genetic Bio fortification
Increasing Nutracuticular Value in Field
Crops
Increasing Nutracuticular
Value in Horticultural
Crops
Increasing Nutracuticular
Value in Medicinal Crops
CONCLUSION
• Nutraceuticals are present in most of the food
ingredients with varying concentration
• Concentration, time and duration of supply of
nutraceuticals influence human health
• Manipulating the foods, the concentration of active
ingredients can be increased
• Diet rich in nutraceuticals along with regular
exercise, stress reduction and maintenance of
healthy body weight will maximise health and
reduce disease risk
13 nutraceuticles
13 nutraceuticles

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13 nutraceuticles

  • 1. AssignmentAssignment Subject : Breeding Designer Crops (GPB822)Subject : Breeding Designer Crops (GPB822) Presented by: Mr.Presented by: Mr. IndranilIndranil BhattacharjeeBhattacharjee Student I.D. No.: 17PHGPB102Student I.D. No.: 17PHGPB102 Presented to : Prof. (Dr.)Presented to : Prof. (Dr.) B.G.SureshB.G.Suresh SamSam HigginbottomHigginbottom University of Agriculture, Technology &University of Agriculture, Technology & SciencesSciences AllahabadAllahabad--211007211007
  • 2. History “The physical body is the product of diet and sensory input (lifestyle). Similarly, all diseases are the result of non correct diet and lifestyle. Diet and lifestyle wholesome and unwholesome are the foundations of health and illness” Caraka Samhita Sutrasthana (1, 28:45) An Apple a Day Keeps the Doctor Away. -English Proverb
  • 3. • Greek Physician Hippocrates, Known as father of Medicine. (said several centuries ago) “Let Food be Your Medicine” The Philosophy behind is: “Focus on Prevention”
  • 4. ( World( World HealthHealth Organization, 1947 )Organization, 1947 ) “Health is a state of complete well-being, physical, mental and social, and not merely the absence of disease” The definition of health status. Definition
  • 5. ( Dame( Dame CicelyCicely MaryMary SaundersSaunders)) “Do not be worried on how to add days to our life, but on how to give more life to our days” The main focus.
  • 6. (Merriam-Webster, 2013) - 1989 Stephen DeFelice, President of the Foundation for Innovation in Medicine (Cranford), NJ, USA. Nutraceutical: food or part of food that provides medical or health benefits, including the prevention and/or treatment of a disease. Nutraceuticals: TORs.
  • 7. The term nutraceutical refers to products for oral use containing high concentrations of active principles derived from food, and provide health benefits from a preventive and/or therapeutic point of view. They are not considered drugs, there is lack of controlled studies stating their real efficacy. Nutraceuticals: TORs. There is lack of a shared regulation assessment.
  • 8. • The term “Nutraceutical” was coined from “Nutrition” & “Pharmaceutical” in 1989 by Stephen DeFelice, MD, Founder and Chairman of the Foundation for Innovation in Medicine (FIM). • Other words used in the context: Dietary supplementation, Functional, Multi- functional Foods, etc.
  • 9. • Nutraceutical can be defined as “ A food or part of food or nutrient, that provides health benefits, including the prevention and treatment of a disease.”
  • 10. Class / components Source Potential benefit 1. Fatty acids CLA Milk & Meat Improve body composition, reduce cancers n-3 FA(DHA, EPA) Fish oils, berseem & maize fodder,mustard,linseed, rapeseed Reduce CVD & improve mental, visual function Examples of functional components
  • 11. Class / components Source Potential benefit 2. Polyphenols Anthocyanidin e Fruits Nutralises free radicals, reduce risk of cancerCatechins Tea,babul pods,mustard cake,rape seed,salseed Flavonone Citrus Flavones Fruits, vegetables,soya bean proanthocyani dine Cocoa, chocolate,tea,rape seed Reduce CVD EXAMPLES OF FUNCTIONAL COMPONENTS
  • 12. 3. Saponins Soybeans,GNC,lucer ne,chick pea Lower cholesterol, anti cancer 4.Probiotics / Prebiotics / Synbiotics Lactobacillus Dahi,yogurt Improve GI health Fructo - oligosaccharides Whole grains, onions, combination of Pro & Prebiotics 5.Phytoestrogen Daidzein , Zenistein Soybean, flax, lentilseed,maize, berseem,lucerne,sub abul fodder Reduce menopause symptoms,  bone health Lignans Flax,rye, vegetables Reduce cancer and heart diseases
  • 13. 6.Caroteinoids - caroteine Berseem,lucerne ,oat & maize fodder, Carrots, vegetabels,fruits Nutralises free radicals Luteine vegetabels Healthy vision Zeoxanthine Eggs,citrus,corn Lycopene Tomatoes Reduce prostate cancer 7.dietary fiber Insoluble fiber Wheat bran Reduce breast, colon cancer -glucan Oats Reduce CVD Whole grain Cereal grains
  • 14. Brand name Components Function Betatene Carotenoids Immune function Xangold Lutein esters Eye health Lipoec -lipoic acid Potent antioxidant Generol Phytosterol CHD reduction Premium probiotics probiotics Intestinal disorder Soylife Soyabean phytoestrogen Bone health NUTRACEUTICALS AVAILABLE IN MARKET
  • 15. Brand name Components Function Z-trim Wheat Zero calorie fat replacer Linumlife Lignan extract flax Prostate health Fenulife Fenugreek galactomannon Control blood sugar Teamax Green tea extract Potent antioxidant Marinol  3 FA, DHA, EPA Heart health protection Clarinol CLA Weight loss ingredient Cholestaid Saponin Reduce cholesterol NUTRACEUTICALS AVAILABLE IN MARKET
  • 16. i. The olistic medical approach. ii. The static approach: the patient, often unaware of a potential health risk, waits till the clear signs of the onset of a disease appear (watchful waiting or active surveillance medicine) and then obtain a diagnosis and starts using prescription drugs. iii. The nutraceutical dynamic approach also known as “initiative medicine or proactive medicine”: taking preventive action before the onset of a disease instead of waiting for the disease to become evident. Scope of use - Some preliminary considerations on handling an health condition.
  • 17. Primary prevention Secondary prevention • Lifestyle – behaviour – dietary habits Possible approaches: • Drugs (waitchful waiting medicine) • Nutraceuticals (pro active medicine) The availabile tools.
  • 21. Broadly can be classified as: • Nutrients: Substances which have established Nutritional functions e.g. Vitamins, Minerals, Amino Acids, Fatty acids, etc. • Herbals/ Phytochemicals: Herbs or Botanical products • Dietary Supplements: Probiotics, Prebiotics, Antioxidents, Enzymes, etc.
  • 25. Legal View Nutraceuticals: food or drugs? QUESTION placed at the European Commission E-000065/2011 (dr. Christian Muscardin) about the presence on the market of products, called "nutraceuticals", which, unlike normal dietary supplements, have the effects of preventing or reducing the risk of disease, especially degenerative of a particular structure or function of the organism. • ANSWER given by Commissioner John Dalli on behalf of the European Commission, February 21, 2011: • The term "nutraceutical" is not currently defined in Community legislation. • These products, under the current legislation, should be classified as dietary supplements or following authorization for marketing as drugs.
  • 26. Court of Justice of the European Union: medicine/drug food. • if it is presented as having properties for treating or preventing disease in human beings (definition of "presentation"); • if it is to be administered to human beings with a view to making a medical diagnosis or to restoring, correcting or modifying physiological functions (definition "by function"). Plant-based products marketed in the form of dietary supplements (vegetable origin similar to nutraceuticals) must comply with Directive 2002/46/EC on food supplements and Regulation (EC) n. 1924/2006 on the claims about the effects of nutrition and health foods. If a product, taking into account all its characteristics, may fall within the definition of a medicinal product and the definition of a product covered by other Community legislation, apply the Directive 2001/83/EC revised by Directive 2004/27/EC (food and drugs nutraceuticals). Nutraceuticals: food or drugs?
  • 27. Source of Nutraceuticals: where can be found. An approximate number of about 30,000 phyto components have been identified in plants. • Approximately 5,000-10,000 are present in plant foods of common use/consumption. • Assuming 5 daily servings of fruits and vegetables, you ensure the intake of about 1.5 g / day of nutraceuticals phytocomponents.
  • 32. Uses of Nutraceuticals: therapeutic uses. Prevention/Therapy using nutraceuticals. - Hypercholesterolemia - Hypertension - Type II diabetes - Hypertryglyceridemia - ……….. Metabolic syndrome A nutraceutical pro active approach is possible?
  • 33. Nutraceuticals: possible uses. An example. The artichoke (Cynara scolymus) extract polyphenols: the main components are chlorogenic acid, caffeic acid and cynarin. In year 1900 scientific research has focused on the properties hepatostimulants, hepatoprotective, choleretic and hypocholesterolemic associated to extracts of Cynara leaves, as advocated by medicine doctors already in year 1700.
  • 34. Cynara extracts Chlorogenic acids Flavanoids • 5-O-caffeilchinic acid • 1,5-dicaffeilchinic acid • caffeic acid • Luteoline • Cinaroside • Scolimoside Artichoke: bioactive substances. Nutraceuticals: possible uses.
  • 35. Artichoke variety mg chlorogenic acid/100g Romolo stem 27,826 Romolo head 6,276 Romolo leaves 0,5 Artichoke variety Total phenolic content mg AGE/100g DPPH Îźmol TE/100g FRAP Îźmol TE/100g Romolo stem 21,35 78,61 104,46 Romolo head 4,53 38,95 24 Romolo leaves 26,44 124,47 64,54 Anti oxidant activity: Nutraceuticals: possible uses.
  • 36. Sustainable use of industrial wastes. Bioactive molecules rich sources Nutraceuticals: recovery/uses.
  • 37. Cholesterol-lowering action of artichoke extracts. 1. increased choleresis and then increased excretion of salts and bile acids rich in cholesterol; 2. inhibition of cholesterol biosynthesis. • Cholesterol is synthesized in the liver from acetyl-CoA and released in plasma. • The extent of hepatic biosynthesis is controlled by the intracellular concentration of cholesterol. Nutraceuticals: possible uses.
  • 38. Nutraceuticals: possible uses. Green tea: functional food/nutraceutical Obtained from a plant: Camellia sinensis (L.). The freshly harvested leaves are immediately processed to inactivate the enzymatic oxidation process. • Green tea has the highest concentration of polyphenols than other types of tea. • Green tea has hypoglycemic properties.
  • 41. 0 20 40 60 80 100 120 C EC ECG EGC EGCG GC CG mg/gdw C = (-)-Catechina EC = (-)-Epicatechina ECG = (-)-Epicatechingallato EGC = (-)-Epigallocatechina EGCG = (-)-Epigallocatechingallato GC = (-)-Gallocatechina CG = (-)-Catechingallato Nutraceuticals: possible uses.
  • 42. 0 1 2 3 4 5 6 7 8 Cholesterol(mg/dL/Âľgprotein) ECG = (-)-Epicatechingallato EGCG = (-)-Epigallocatechingallato CG = (-)-Catechingallato Nutraceuticals: possible uses.
  • 43. 0 1 2 3 4 5 6 Triglycerides(mg/dL/Âľgprotein) C = (-)-Catechina ECG = (-)-Epicatechingallato EGCG = (-)-Epigallocatechingallato Nutraceuticals: possible uses.
  • 45. Nutraceuticals: possible uses. Catechins: cardio protective role.
  • 46. Nutraceuticals: possible uses. Apple: an in se functional food ? I. Significant source of phytocompounds (flavonoids) among which quercetin (5 - 15 mg / 100 g) is the main one. II. Contains antioxidant polyphenols with proven efficacy. III. Apple extracts inhibit the cholesterol uptake. IV. The effect on the organism is similar to statins. Apple: extract nutraceutic
  • 48. OligomericOligomeric procyanidinsprocyanidins Red Delicious Pink Lady Fuji Golden DeliciousAnnurca BucceBucce PolpaPolpa Hypocholesterolemic metabolites Nutraceuticals: possible uses.
  • 49. Justification of why we use? Metabolic syndrome (SM): some data. 50% of people from Europe are overweight 30% suffer from obesity 23-24% of USA suffer from SM WHO estimated an about 2.5 millions of people dead worldwide due to overweight and to cardiovascular diseases SM: ICD-9-CM code = 277.7 Van Gaal LF, et al. Lancet 2005;365:1389-97
  • 50. Abdominal obesityAbdominal obesity Glucose intolerant/Glucose intolerant/InsulineInsuline resistencyresistency HypertensionHypertension AterogenAterogen dislipidemydislipidemy ProinflammatoryProinflammatory state/state/ ProtromboticProtrombotic National Cholesterol Educational Program (NCEP), Adult Treatment Panel (ATP) III; 2001 DiabetisDiabetis CVDCVD Metabolic syndrome “cluster” of risk factors.
  • 51. Metabolic syndrome. Central obesity (european and north american population). i. Waist circumference ≥ 94 cm (male) and ≥ 80 (female) Together with at least TWO of the following: ii. TG > 150 mg/dL or specific treatment iii. CHDL < 40 mg/dL (male) e < 50 mg/dL (female) or specific treatment iv. SBP ≥ 130 mmHg e/o DBP ≥ 85 mmHg or anti hypertension treatment v. Glycemic index ≥ 100 mg/dL or a DM2 diagnosis
  • 52. Nutraceuticals and metabolic syndrome. Apple variety “annurca”
  • 53. Lipidic profile in patients treated with atorvastatin v/s nutraceutical (NUT) Apple variety “annurca”
  • 55. Therapeutic approach. METABOLIC SYNDROME ORGAN DAMAGE PRESENCE YESNO LYFESTYLE CHANGE NUTRACEUTICALS PHARMACOLOGIC THERAPY
  • 56. Active Bio-chemical Components NUTRIENTS • Most common Nutrients used/ supplemented as Nutraceutical are: Minerals and Vitamins. or in combination or in combination with other antioxidants
  • 57. Health Benefits of different common nutrients Vitamins Fat Soluble Vitamins • Vitamin A: Acts as antioxidant, essential for growth and development, maintains healthy vision, skin and mucous membranes, may aid in the prevention and treatment of certain cancers and in the treatment of certain skin disorders.
  • 58. • Vitamin D: Essential for formation of bones and teeth, helps the body to absorb and use calcium • Vitamin E: Antioxidant, helps to form blood cells, boosts immune system • Vitamin K: Essential for blood clotting
  • 59. Water Soluble Vitamins • Vitamin C: Antioxidant, necessary for healthy bones, gums, teeth and skin. Helps in wound healing, prevent from common cold • Vitamin B 1: Helps in carbohydrate metabolism, essential for neurological function. • Vitamin B 2: Energy metabolism, maintain healthy eye, skin and nerve function.
  • 60. • Vitamin B 3: Energy metabolism, brain function • Vitamin B 6: Helps to produce essential proteins, convert proteins to energy • Vitamin B 12: Help in producing genetic material, formation of RBC, maintenance of CNS, synthesis of amino acids, involved in metabolism of protein, fat and carbohydrate.
  • 61. • Folic acid: Helps in RBC formation, formation of genetic material of cell, very much essential during pregnancy • Pantothenic acid: Aids in synthesis of cholesterol, steroids, and fatty acids, crucial for intraneuronal synthesis of acetylcholine
  • 62. Vitamins like Compounds • L- Carnitine: Helps in oxidation of fatty acids, role in oxidative phosphorylation, • Choline: Lipotropic agent, used to treat fatty liver and disturbed fat metabolism, • Inositol: For amino acid transport and movement of Potassium and sodium, • Taurine: Helps in retinal photoreceptor activity, bile acid conjugation, WBC antioxidant activity, CNS neuromodulation, platelet aggregation, cardiac contractibility, sperm motility, insuline activity,
  • 63. • Minerals: • Calcium: essential for bone and teeth, maintaining bone strength, nerve, muscle and glandular function, blood clotting, • Iron: energy production, Hb, oxygen transport, • Magnesium: for healthy nerve and muscle function, bone formation, • Phosphorous: energy production, phosphorylation process, bone and teeth, for genetic material,
  • 64. • Cobalt: component of Vit. B 12 and B 12 coenzymes, • Copper: Hb and collagen production, function of heart, energy production, absorption of Iron, • Iodine: proper function of Thyroid gland, • Chromium: with insulin it helps in conversion of carbohydrate and fat into energy, treatment of diabetes,
  • 65. • Selenium: Antioxidant, functioning of heart muscle, part of GPX enzyme, • Zinc: Essential for cell reproduction, for development in Neonates, wound healing, production of sperm and testosterone hormone,
  • 66. • Herbals: • Aloe vera: Anti-inflammatory, emollient, wound healing, • Evening Primrose oil: Dietary supplement of linoleic acid, treatment of atopic eczema, • Garlic: Antibacterial, antifungal, antithrombotic, antiinflammatory, • Ginger: carminative, antiemetic, treatment of dizziness
  • 67. • Ginseng: Adaptogen, • Green tea: Antioxidant, reduces risk of CVD, enhances humoral and cell mediated Immunity, • Vegetables, fruits, whole grain, herbs, nuts and various seeds contain an abundance of phenolic compounds, terpenoids, sulphur compounds, pigments etc. that has been associated with protection / treatment of certain disease conditions,
  • 68. •Phytochemicals: • Phytochemicals could provide health benefits as: 1. Substrate for biochemical reactions 2. Cofactors of enzymatic reactions 3. Inhibitors of enzymatic reactions 4. Absorbents that bind to & eliminate undesirable constituent in the intestine 5. Scavengers of reactive or toxic chemicals
  • 69. 6. Enhance the absorption and / or stability of essential nutrients 7. Selective growth factor for beneficial bacteria 8. Fermentation substrate for beneficial bacteria 9. Selective inhibitors of deleterious intestinal bacteria
  • 70. Various Phytochemicals Phytochemicals Source Role Tocotrienols & tocopherols Grains Suppressed the growth of diverse tumors cell lines via initiation of apoptosis and concomitant arrest of cells in the G1 phase of the cell cycle Carotenoids Fruits & vegetables Antioxidants, protects against uterine, prostate, colorectal, lung and digestive tract cancers, and protection to other antioxidants.
  • 71. Limonoids Citrus fruits Inhibiting phase I enzymes & inducing phase II detoxification enzymes in liver, provide protection to lung tissue. Phytosterols Various plants Exhibit anti-inflammatory, anti-neoplastic, anti- pyretic & immune- modulating activity, decrease cholesterol Phenolic constituents Various plants, wholegrain Antioxidants, lowers the risk of CHD, diabetes, hypertension etc.
  • 72. Flavonoids Grapes, wines Action against free radicals, free radicals mediated cellular signaling, inflammation, allergies, platelet aggregation, & hepatotoxins Catechin & gallic acids Grapes, berries, cocoa, green tea, acacia spp. Antioxidants, free radical scavenging ability, inhibition of eicosanoid synthesis, reduces CHD Isoflavonoids Soybeans Treating cancers & osteoporosis
  • 73. Anthocyanidins Fruits & flowers Antioxidants & anti- mutagenic properties Glucosinolates Cruciferous Activators of liver detoxification enzymes, inhibit the neoplastic effect of various carcinogens Indoles Reduces estrogen- dependent cancer risk, Fiber Various vegetables, fruits, Protects against colorectal diseases,
  • 74. Method to enhance active components in food • Manipulating the diet to get maximum level of active components • Combination of food ingredients rich in nutraceuticals • Fortifying food with active ingredients • By fermentation of food products • Changing food habits to natural type of diet
  • 79. 80 Nutraceutic potential of grape polyphenols. Flavonols Antocianins Pro-antocyanidins Shao et al. (2006). Grape seed proanthocyanidin extract attenuates oxidant injury in cardiomyocytes. Pharmacological Research PoliphenolsPoliphenols contentcontent:: juicejuice >> winewine >> grape/fruitsgrape/fruits “Antioxidant protection of the cardiovascular system”
  • 80. Malvidin-3-O-glucoside 114 mg/100 mL 35% anthocyanins Main active molecules. Myricetin-3-O-glucoside 93 mg/100 mL 27% flavonols Quercetin-3-O-glucuronide 76 mg/100 mL 22% flavonols Quercetin-3-O-glucoside 80 mg/100 mL 23% flavonols AntocianinsAntocianins FlavonolsFlavonols
  • 81. 0.00 100.00 200.00 300.00 400.00 500.00 600.00 700.00 800.00 900.00 1000.00 Phenols Flavonols Anthocyanins 992.00 Âą 2.1 404.77 Âą 1.5 402.41 Âą 0.8 989.80 Âą 1.8 402.05 Âą 1.6 400.12 Âą 0.9 mg/100mL RGJ lioRGJ Red grape juice poliphenolic content before (RGJ) and after lyophilization (lioRGJ). 83
  • 82. 84 Antioxidant activity of red grape juice before (RGJ) and after lyophilization (lioRGJ) FRAP = Antiradical indirect power DPPH = Antiradical direct power
  • 83. “Antioxidant profile and“Antioxidant profile and in vitroin vitro cardiac radicalcardiac radical--scavengingscavenging vsvs propro--oxidant effects ofoxidant effects of commercial red grape juices (commercial red grape juices (VitisVitis viniferavinifera L. cv.L. cv. AglianicoAglianico N.)”N.)” Gian Carlo Tenore, Michele Manfra, Paola Stiuso, Luigi Coppola, Mariateresa Russo, Isabel Maria Gomez Monterrey, Pietro Campiglia Journal of Agricultural and Food Chemistry, 2012 Nutraceutical potential of grape polyphenols.
  • 84. Grape juice: “Functional food → Nutraceutic potential” Possible use as nutraceutical: Support for the treatment of neoplastic diseases. Nutraceutical potential of grape polyphenols. (Jones et al., Int. J. Cancer Res., 10(1), 46-53, 2014)
  • 85. Hyperglicemy: a new therapeutic approach. PPARg (proliferator-activated receptor gamma) a nuclear receptor has a primary role in lipid and carbohydrates metabolism. Problem: PPARg-targeting drugs are characterized by unwanted side effects. Natural products from edible biomaterials are a structurally different resource to easy the complex side effects of common use drugs. It can be adopted a nutritional tailored approach to easy side unwanted effetcts. Amorfrutins, extracted from the edible part of two legumes, namely Glycyrrhiza foetida and Amorpha fruticosa, are new and potent anti diabetes agents. They selectively bond to the PPARg receptor and activate it.
  • 87. “Beyond diet, before drugs” (E. Novellino, 2012) A. Santini, Journal of Food Research, 2014, (4), 1-5. Pro active nutraceutical approach: when and where?
  • 88. “Beyond diet, before drugs” (E. Novellino, 2012) Antonello Santini and Ettore Novellino Current Bioactive Compounds, 2014, 10(1), 1-12.
  • 89. Increasing Nutraceuticular Value of food through Genetic Bio fortification
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  • 133. CONCLUSION • Nutraceuticals are present in most of the food ingredients with varying concentration • Concentration, time and duration of supply of nutraceuticals influence human health • Manipulating the foods, the concentration of active ingredients can be increased • Diet rich in nutraceuticals along with regular exercise, stress reduction and maintenance of healthy body weight will maximise health and reduce disease risk