Nutraceuticals

nutraceuticals

1. NUTRACEUTICALS LET FOOD BE YOUR MEDICINE SUBMITTED BY ANUPAM PRAHLAD Dept. of Pharmacology, 1 st year M.Pharm Devaki Amma Memmorial College of Pharmacy

2. CONTENTS Introduction Advantages of nutraceuticals Classifications Clinical uses Regulatory aspects Conclusion

3. “A nutraceutical is any substance that is a food or a part of food and provides medical or health benefits, including the prevention and treatment of disease”. The term “Nutraceutical” was coined from “Nutrition” & “Pharmaceutical” in 1989 by Stephen. A nutraceutical is a pharmaceutical-grade and standardized nutrient.  "Nutraceutical" is creating the concept that extracts from food can be used as drugs, i.e. food supplements.

4. ADVANTAGES OF NUTRACEUTICALS Nutraceutical have the potential to play a role in healthy eating and to contribute to the prevention and treatment of diseases so that how functional components in foods could expand the role of disease prevention and treatment.  The nutraceuticals are preferred due to Since new molecule is difficult to discover and more expensive and risky then ever before, many pharmaceutical companies are now trying to nutraceuticals so that there is undoubtedly a very huge and growing market . The belief among consumers that these “food like substances” are either harmless or least toxic as compared to conventional pharmaceuticals . Increased healthcare costs with conventional pharmaceuticals, recent legislation and scientific discoveries.

5. Inappropriate dietary habits are seen as contributing to the leading cause of deaths of due to coronary heart disease, certain type of cancers etc. the role of nutraceuticals in treating these Conditions is thus speculated. Nutraceuticals are gaining popularity as people are relying on them for safeguarding their health and avoiding side effects associated with drugs as well Long history of use and better patient tolerance as well as public acceptance Plants constitute to be a major source of new lead generation ADVANTAGES OF NUTRACEUTICALS

6. CLASSIFICATION  Nutraceuticals are non specific biological therapies used to promote wellness, prevent malignant process and control systems . These can be grouped into the following three broad categories: Substance with established nutritional functions , such as vitamins , minerals ,amino acids and fatty acids- Nutrients  Herbs or botanicals products as concentrates and extracts – Herbals Reagents derived from other sources( eg . pyruvate , chondroitin sulphate , steroids hormone ,precursors)serving specific functions , such as sports nutrition , weight loss supplements and meal replacements – Dietary supplements.

7.  DIETARY SUPPLEMENTS Probiotics , Prebiotics , Antioxidants , Enzymes, etc HERBAL/ PHYTOCHEMICALS Herbs or Botanical products. NUTRIENTS Vitamins, Minerals , Amino Acids , Fatty acids , etc.

8. probiotics Probiotics are defined as live microorganisms that are believed to provide health benefits when consumed. [ Probiotics are often called "good" or "helpful" bacteria because they help keep your gut healthy. They can help balance your "good" and "bad" bacteria to keep your body working like it should.  Species of Lactobacillus, Bifidobacterium , yeast Saccharomyces cerevisiae, some E. coli and Bacillus species are also used as probiotics 

9. Antibiotics   Alcohol consumption Stress   Problems in digestion Problems in absorption of nutrients in the body Destroy the gut micro flora Emergence of antibiotic resistant strains PROBIOTICS PROBIOTICS WHY ARE PROBIOTICS IMPORTANT FOR HUMAN HEALTH?

10. Key properties of probiotic  Non-pathogenic, non-toxic and non-allergic. Capable of surviving and metabolizing in upper G.I. tract e.g. Resistant to low pH, organic acids, bile juice, saliva and gastric acid . Human in origin, genetically stable and capable of remaining viable for long periods in field condition. Able to modulate immune response and provide resistance to disease through improved immunity or by the production of antimicrobial substance in the guts.

11. Good adhesion/ colonization to human intestinal tract and influence on gut mucosal permeability. Antagonistic against carcinogenic/ pathogenic organisms. Clinically proven health benefit, e.g. gastrointestinal disorders, diarrhea, clostridium difficle colitis, antibiotics associated diarrhea, acute gastroenteritis. Technologic properties for commercial viability such as stability of desired characteristics during processing, storage and transportation.

12. Mechanism of action Bioconversion of, for example, sugars into fermentation products Production of growth substrates, like vitamins B and K, for other bacteria . Direct antagonism by antimicrobial substances: hydrogen peroxide , organic acids, Bacteriocin , acidophilin . Competitive exclusion for binding sites. Improved barrier function . Production of β- D- galactosidase enzymes that break down lactose . Reduction of inflammation, thus altering intestinal properties Stimulation of innate immune response

13. Examples of probiotics Bifidobacteria There are approximately 30 species of bifidobacteria . They are found in the intestinal tract within days of birth, especially in breastfed infants. They help in the improvement of abdominal pain, bloating, bowel dysfunction, incomplete evacuation, straining, and the passage of gas.

14. Lactobacillus There are more than 50 species of lactobacilli. Foods that are fermented, like yogurt, and dietary supplements also contain these bacteria. It helps in preventing yeast infections, urinary tract infection, IBS, traveler's diarrhea , diarrhea resulting from Clostridium difficile, treating lactose intolerance, skin disorders ( feverblisters , eczema,acne ) and prevention of respiratory infections .

15. Saccharomyces The only yeast probiotic. It is effective in treating diarrhea associated with the use of antibiotics and traveler's diarrhea. It has also been reported to prevent the reoccurrence of Clostridium difficile, to treat acne, and to reduce side effects of treatment for Helicobacter pylori.

16. Streptococcus This produces large quantities of the enzyme lactase, making it effective. It helps in the prevention of lactose intolerance. Enterococcus This is normally found in the intestinal tract of humans. Enterococcus faecium SF68 is a specific probiotic strain that has been used in the management of diarrhoeal illnesses.

17.   Leuconostoc Members of Leuconstoc spp. are very often used in production of fermented foods because of their ability to produce lactic acid bacteria and diacetyl . Leuconostoc are used to inhibit Listeria monocytogenes in dairy and meat products.

18. CLINICAL USES Treatment of Antibiotic Associated Diarrhea Probiotics used in prevention and as adjuvant therapy in AAD. Disease Antibiotic treatment Clostridium overgrowth produces toxin  Disturbance of intestinal microbiota  Microbiota imbalance Probiotics

19. 2. Lactose Intolerance Lactase digests lactose commonly present in milk and milk products. Lactose is not digested when there is a deficiency in lactase and results in diarrhea. Supplementation with probiotics has been shown to mitigate the symptoms of lactose intolerance by enzyme β- D- galactosidase. Having yoghurt is a good way for a lactose intolerant person to get calcium.

20. 3. Helicobacter pylori Infections Bifidobacteria and B. subtilis may inhibit the growth or attachment of H. pylori. Possible mechanisms eradicates H. pylori include the ability of the probiotics to bind to gastric epithelial cells, to produce a high quantity of lactic acid, and to proliferate rapidly.

21. 4. Hypercholesterolemia LACTIC ACID BACILLI Increase production of short chain fatty acids. Inhibit cholesterol synthesis. Decreased blood cholesterol Increases bile Bile syn. Increases More cholesterol is used up Decreases cholesterol

22. 5. Probiotics and Cancer Enzymes (Glycosidase, B- glucuronidase , azoreductase , and nitroreductase ) of the intestinal flora convert the precarcinogens to active carcinogens giving rise to colon CA. Probiotics reduce faecal concentrations of enzymes and reduce absorption of harmful mutagens that may contribute to colon carcinogenesis. Activity of L. acidophilus and L. casei supplementation in humans helps to decrease levels of these enzymes

23. PREBIOTICS Prebiotics are food ingredients that induce the growth or activity of beneficial microorganisms (e.g., bacteria and fungi). The most common example is in the gastrointestinal tract, where prebiotics can alter the composition of organisms in the gut microbiome. In diet, prebiotics are typically non-digestible fiber compounds that pass undigested through the upper part of the gastrointestinal tract and stimulate the growth or activity of advantageous bacteria that colonize the large bowel by acting as substrate for them.

24. Prebiotics- examples Garlic, Onions Chicory root Asparagus Wheat Rye Barley breast milk Tomatoes berries bananas

25. Established Prebiotics Inulin Extraction from chicory root, Wheat, banana, onions, garlic Fructo -oligosaccharides Tranfructosylation from sucrose, or hydrolysis of chicory inulin  Galacto -oligosaccharides Produced from lactose by b-galactosidase SOS (soy-oligosaccharides) Extracted from soya bean whey XOS ( xylo -oligosaccharides) Enzymic hydrolysis of xylan   IMO ( isomalto oligosaccharides) Transgalactosylation of maltose Pyrodextrins Pyrolysis of potato or maize starch

26. Oligosaccharides Oligosaccharide is the main constituent of prebiotic food products. Oligosaccharides stimulate the growth of benefic bacteria and increase the resistance to invading pathogens. The functional oligosaccharides include; Fructooligosaccharides (FOS), Glucooligosaccharides (GOS), Inulin, Isomaltooligosaccharides (IMO), Soybeanmeal oligosaccharides (SMO), Mannan oligosaccharides(MOS), Galactooligosaccharides , Maltooligosaccharides (MO), Xylooligosaccharides (XOS), Pectin-derived acidic oligosaccharides ( pAOS ).

27. Fructo -oligosaccharide Fructo oligosaccharides is a group of oligosaccharides, or a group of connected simple sugars. Sources include onions and chicory root also garlic. It helps in the stimulate production of beneficial bacteria, minimal effect on blood sugar, also help strengthen the immune system. Inulin Inulin is a dietary fibre that is found in many common foods such as leeks, kiwi, asparagus, onions, garlic, bananas, wheat, rhubarb, dairy products etc. There are several benefits of inulin apart from weight- management, it even increases calcium absorption, improved bone health. It can also be used to replace sugar and fat as a food additive to improve taste. Soybean-oligosaccharide They found in soy milk, soy oil,bean curd, ice cream. Promote the growth of Bifidobacteria in the intestinal tract,lowering cholesterol.

28. Xylo -oligosaccharide They are naturally present in fruits, vegetables, bamboo, milk and honey. It help to improve blood sugar levels and fat absorption, re- establish normal colonic flora. It also increase mineral absorption and vitamin B creation. Galacto -oligosaccharide Galacto -oligosaccharides, otherwise called( GOS), are found naturally in breast milk but are added to foods such as infant formula, fruit drinks, dairy products, breakfast cereals and biscuit crackers. Increases the good bacteria boosts the immune system. Promote intestinal health by keeping unfriendly bacteria such as E.coli, vaginal, urinary infections at bay.

29. Uses of Prebiotic Enhance bone density and increase Calcium absorption. Improve immune function in both the gut and body. Establish a healthier balance of bacteria in the gut. Promote regular bowel movements. Suppress appetite. Reduces the risk of an intestinal infection. Increase in mineral absorption and improvement of bone health. Modulation of gastro-intestinal peptides production, energy metabolism and satiety. Initiation (after birth) and regulation/modulation of immune functions.

30. Health Benefits of Prebiotic Immune System Strength Prebiotic fiber promotes the growth and colonization of beneficial bacteria in the gut. These bacteria aid the immune system in fighting illness-causing bacteria and viruses. Normal Bowel Function Irritable bowel syndrome, which is characterized by bloating, gas, stomach pain, cramping, bouts of constipation and diarrhea, is caused by food being digested improperly. , prebiotic fiber causes foods to be digested normally, over a normal period of time, not too quickly or too slowly.

31. Cancer Prevention Bifidobacteria digests inulin in the gut flora and produces short chain fatty-acids: acetic acid, propionic acid, and butyric acid. Within the intestine, it is believed that these acids can help prevent certain forms of cancer. Colon Cancer The insoluble fiber from prebiotics, some experts believe, are actually doing a part in preventing colon cancer by sweeping up carcinogens and other dangerous toxins before they can be absorbed into the bloodstream where they can do damage

32. Antioxidants An antioxidant is a molecule that inhibits the oxidation of other molecules. Antioxidants terminate these chain reactions by removing free radical intermediates, and inhibit other oxidation reactions and in turn oxidizing themselves.  Dietary antioxidants and some accessory molecules, such as zinc and certain vitamins are important in maintaining free radical scavenging systems, biosynthetic capacity, membranes, enzymes . Antioxidants are found in the vegetable oils. e.g.- Soybean oil, canola oil, corn oil, oat oil, wheat germ oil, palm oil, evening prime rose oil. Like tocopherols (vitamin E) it lower the susceptibility of LDL oxidation and also reduce platelet’s role in thrombus formation.

33. Vitamins like vitamin C, vitamin E and carotenoids are collectively known as antioxidant vitamins. These vitamins act both singly as well as synergistically for the prevention of oxidative reactions leading to several degenerative diseases including cancer, cardiovascular diseases, cataracts etc. These vitamins are abundant in many fruits and vegetables and exert their protective action by free-radical scavenging mechanisms. Vitamin E which comprises of tocopherols together with tocotrienols transfer hydrogen atom and scavenge singlet oxygen and other reactive species thus protecting the peroxidation of PUFA within the biological membrane and LDL.

34.  Vitamin E and selenium has a synergistic role against lipid peroxidation. Vitamin C, better known as ascorbic acid donates hydrogen atom to lipid radicals, quenches singlet oxygen radical and removes molecular oxygen. Scavenging of aqueous radicals by the synergistic effect of ascorbic acid along with tocopherol supplementation is a well known antioxidant mechanism. Carotenoids like lycopene, β- carotene, lutein, zeaxanthin are known to be the most efficient singlet oxygen quencher in the biological systems without the production of any oxidizing products. β- carotene traps peroxy free radicals in tissues at low oxygen concentrations. Hence β- carotene complements the antioxidant properties of vitamin E.

35. Dietary fibre Dietary fibre is the food material, more precisely the plant material that is not hydrolyzed by enzymes secreted by the digestive tract, but digested by microflora in the gut. Dietary fibres mostly include non-starch polysaccharides (NSP) such as celluloses, hemicelluloses, gums and pectins , lignin, resistant dextrins and resistant starches. Foods rich in soluble fibre include fruits, oats, barley and beans  Chemically dietary fibre means carbohydrate polymers with a degree of polymerization not lower than 3, which are neither digested nor absorbed in the small intestine.

36. Based on their water solubility, dietary fibres may be divided into two forms: Insoluble dietary fibre (IDF)- which includes celluloses, some hemicelluloses and lignins which is fermented to a limited extend in the colon. Soluble dietary fibre (SDF)- which includes β- glucans , pectins , gums, mucilages and hemicelluloses that are fermented in the colon. The IDF and SDF compounds are collectively known as non-starch polysaccharides (NSP).

37. The soluble components of dietary fibre by virtue of their bulking and viscosity producing capabilities, retards the gastric emptying of the stomach This affects the rate of digestion and the uptake of nutrients and creates a feeling of satiety. Soluble fibre has been shown to lower selectively serum LDL cholesterol and to improve glucose tolerance They also enhance insulin receptor binding and improve glycaemic response. In colon, dietary fibre increases faecal bulking due to increased water retention, increased transit time and increased faecal bacterial mass caused by soluble fibre fermentation. The fibre also promotes the growth of Bifidobacteria in the gut. 

38.  Persons consuming generous amounts of dietary fibre , compared to those who have minimal fibre intake, are having low risk of CHR , stroke ,hypertension, diabetes, obesity and certain gastrointestinal disorders . Increase in the intake of high fibre food improves serum lipoprotein values , lowers blood pressure level , improves blood glucose control for diabetes, aids weight loss.

39. Polyunsaturated fatty acids (PUFA) PUFAs are also called “essential fatty acids” as these are crucial to the body’s function and are introduced externally through the die. PUFAs have two subdivisions: omega-3- (n-3) fatty acids and omega-6-(n-6) fatty acids. The major omega-3-fatty acids are α- linolenic acid (ALA), eicosapentanoic acid (EPA), docosahexanoic acid (DHA). ALA is the precursor of EPA and DHA. EPA and DHA are found mainly in fatty fishes such as mackerel, salmon, herring, trout, blue fin tuna and in fish-oils. Principal sources of ALA are mainly flaxseed, soybeans, canola, some nuts (e.g. walnuts) and red/black currant seeds.

40. Omega-6-PUFAs mainly consist of linoleic acid (LA), γ- linolenic acid (GLA) and arachidonic acid (ARA). LA occurs mainly in vegetable oils e.g. corn, safflower, soyabean and sunflower. ARA is found in animal products such as meat, poultry and eggs. Omega-3-fatty acids have three major effects on cardiovascular diseases anti-arrhythmic, hypolipidemic and antithrombotic The benefits of omega-3-oils in other areas of health including pre-mature infant health ,asthma, bipolar and depressive disorders, dysmenorrhea and diabetes

41. Phytochemicals Phytochemicals are non-nutritive plant chemicals that have protective or disease preventive properties. 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

42. PHYTOCHEMICALS SOURCE FUNCTIONS 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.

43. 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 Anthocyanin's Fruits & flowers Antioxidants & anti- mutagenic properties Glucosinolates Cruciferous Activators of liver detoxification enzymes, inhibit the neoplastic effect of various carcinogens Indoles Various vegetables, fruits, Reduces estrogen- dependent cancer risk,

44. HERBALS Aloe- vera Anti-inflammatory Emollient Wound healing Garlic Antibacterial Antifungal Antithrombotic Anti-inflammatory Ginger Carminative Antiemetic Treatment of dizziness Ginseng Adaptogen Green tea Antioxidant Reduces risk of CVD Enhances humoral and cell mediated Immunity, Evening Primrose oil Dietary supplement of linoleic acid Treatment of atopic eczema

45. Flax seeds Prevents mammary, colon and rectal cancers. Reduces BP in hypertensive patients. Reduces diabetes and coronary heart diseases.  Spirulina Immunostimulant activity. Management of HIV and other viral infections such as herpes, cytomegalovirus, influenza, mumps. To treat arthritis, atherosclerosis, diabetes and aging process.

46. VITAMINS Vitamin E Antioxidant helps to form blood cells boosts immune system 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 The treatment of certain skin disorders. Vitamin D Essential for formation of bones and teeth Helps the body to absorb and use calcium Vitamin K Essential for blood clotting

47. 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.

48. 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

49. 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  Selenium Antioxidant functioning of heart muscle part of GPX enzyme

50. NUTRACEUTICAL REGULATION Food regulation is aimed at protecting the consumer’s health, increasing economic viability and harmonizing well being. it is also important to be aware that nutritional products intended to treat or prevent disease or to affect the structure or function of the body in a manner apart from what is normally ascribed for food are considered "drugs" under the law.  in India  Food Safety and Standards authority (FSSA) defines Nutraceuticals as “Foods for special dietary uses”. 

51. The Food Safety and Standards Authority of India (FSSAI) has been established under Food Safety and Standards Act, 2006 which consolidates various acts & orders that have handled food related issues in various Ministries and Departments. FSSAI has been created for laying down science based standards for articles of food and to regulate their manufacture, storage, distribution, sale and import to ensure availability of safe and wholesome food for human consumption

52. Dietary Supplement Health Education Act(DSHEA)1994 This law gives the definition and legal requirements necessary for marketing of nutraceuticals in US. The law defines dietary supplement as : a nutraceutical is a product that one or more following dietary ingredients Vitamin Mineral Herbs Amino acids etc. DSHEA also states that nutraceuticals must be the products that are intended for oral administration.

53. Food Safety Standard And Standards Act(FSSA) 2006 This act is laid down in 2006 inorder to form the statuatory body FSSA which regulate the manufacture , storage, distribution, sale and import to ensure the availability of food within the country

54. Regulatory Registration Requirements Product Evaluation : Examination of each active ingredient & additive. Licenses: To get Product registered in India, number of licenses (almost 4 - 5) might be required, depending on the actual product status. Health and label Claims: “Health claims” means any representation that states, suggests or implies that a relationship exists between a food or a constituent of that food and health .

55. 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.

56. REFERENCE Text Book Of Pharmacognosy And Phytochemistry By Biren Shah And A.K.Seth , Pg.No-471-479. Journal Of Food Science And Technology:” Role Of Nutraceuticals In Human Health”. International Journal Of Drug Regulatory Affairs;2015:issn:2321-6794,page:23.

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