Nutraceuticals.pptx, Herbal Drug Technology

B.Pharm 6th sem.
Unit-2 Nutraceuticals.
As per PCI.

1. PREPARED BY:  MS. SURUCHI AGARWAL   ASSISTANT PROFESSOR KRISHNA INSTITUTE OF PHARMACY & SCIENCES, KANPUR Nutraceuticals

2. Nutraceuticals are derived from the combination of two words “Nutrition” and “Pharmaceuticals” and have been termed by Stephen De Felice in 1989. He defined it as “a food or part of a food that provides pharmacological benefits, including the prevention and treatment of disease”.

3. Health benefits of nutraceuticals Nutraceuticals are useful in various diseases such as coronary heart disease, obesity, diabetes, cancer, osteoporosis, Parkinson's, Alzheimer's diseases, arthritis, sleeping disorders, cold, cough, digestion problems, osteoporosis, blood pressure, pain and depression etc. Dietary fibres: Dietary fibres play critical role in keeping good health in human individuals and animals. Fibres are those parts of the plant, leaves, stem, fruits and seeds which cannot be digested or absorbed in the body. Water-insoluble fibres absorb water to a certain extent and mainly contribute to bulking of stool, and allow quick passage of wastes through the elementary canal. Soluble fibres get dissolved in water and form a gel that binds the stool. It slows down the absorption of glucose and reduces blood cholesterol levels. PUFAs: These are Poly Unsaturated Fatty Acids also called "essential fatty acids". PUFAs are mainly omega-3 fatty acids and omega-6 fatty acids . The PUFA are the known precursors for arachidonic acid (AA), eicosapentaenoic acid (EPA) and docosahexanoic acid (DHA). These fatty acids have been found to regulate blood pressure, heart rate, blood clotting and immune response. It is also present in dark green leafy vegetables, flaxseed oil and in certain vegetable oils.

4. Probiotics: Probiotics (for life) can be described as a live microorganism which when ingested with or without food improves the intestinal microbial balance and consequently the health and functioning of large intestine. Probiotics or friendly bacteria present in the dairy food are another area of functional foods. Probiotics bacteria promote gut health. Bioyoghurts containing Lactobacillus acidophillus and Bifidobacteria lead the probiotics. Probiotics may also help reduce certain food allergies. Prebiotics : Prebiotics are the food components that escape digestion by normal human digestive enzymes and safely in intact form reach the colon after passage through the stomach and small intestine, where they selectively promote the growth of probiotics. They are easier to formulate into regular foods and therefore offer a better chance of success in restoring natural balance of the colonic micro-flora and enriching the health of the large intestine. Insulin as fructosan obtained commercially from Jerusalem artichoke tubers, Helianthus tuberosus , family Compositae or raw chicory is the best known prebiotics.

5. Minerals: Calcium : Calcium is an important element in the treatment of bone loss and prevention. Sufficient intake of calcium and vitamin D postmenopausally can significantly reduce the risk for fracture. Magnesium: Magnesium is an essential element involved in well over 300 enzymatic processes and critical in the proper use and maintenance of calcium. Manganese: Manganese is required in several enzymatic reactions and necessary for proper bone and cartilage formation. Copper : Copper is an essential element needed by all tissues in the body; copper and zinc must be in proper proportion. Zinc: Zinc is one of the most important trace mineral. Zinc supports the body’s overall antioxidant system by scavenging free radicals. It also performs many other vital functions. Phosphorous: Phosphorous is important in maintaining bone structure and modulating plasma and bone formation.

6. Vitamins: Vitamins are the complex substances of organic origin which in small quantities are necessary for the maintenance of human and animal life. Vitamins B 1 or thiamine deficiency is mostly observed in white rice eaters. Ribofalvin-5-phosphate is a cofactor for vitamin B 2 which is beneficial in people who lack the enzyme to convert vitamin B 2 because of nutritional factors or disease condition. Niacinamide deficiency may cause neurological and skin problems. The body can also synthesize niacin from tryptophan. Pantothenic acid -A deficiency affect adrenal gland, immune and cardiovascular system. Vitamin B 6 (Pyridoxine) is crucial for glucose production, hormone modulation and neurotransmitter synthesis. Folic acid is a B complex vitamin which contributes to healthy bone formation. Vitamin C is the body’s main water-soluble antioxidant. It is necessary for proper maintenance of bones. Inositol helps move fatty material from the liver into intestine. Biotin produced by several species of intestinal flora prevents yeast from converting to a more pathogenic fungal form. Choline bitartrate is helpful in moving fat out of liver into the bile.

7. Benefits and Role of Nutraceuticals in Prevention of Diabetes Phytochemicals Effective against Diabetes : Vitamins: Vitamin C being antioxidant in nature (ascorbic acid) scavenges reactive oxygen species and thus reduces protein glycation . Vitamin E also has protective action against type 2 diabetes. It acts by stimulating liver glucokinase activity, increasing insulin production, and enhancing glucose uptake in muscle cells. Calcium and Vitamin D: Appropriate levels of calcium and vitamin D suppresses secretion of parathyroid hormone (PTH), hence help to conserve insulin sensitivity, improve glucose tolerance and prevent diabetes mellitus. Vitamin D is immunomodulatory and anti- inflammatory agent. Vitamin D and calcium enhances function of β-cell of pancreas. L- carnitine : It is vitamin like compound, present in mammalian plasma mainly in skeletal and cardiac muscles. L- carnitine helps in fatty acid transport across the inner mitochondrial membrane into the matrix for β-oxidation, detoxification of potentially toxic metabolites, and stabilization of cell membranes. L carnitine helps to fight with oxidative stress and insulin resistance of skeletal muscles. Omega-3 fatty acids: Omega 3 fatty acids supplement lowers triglycerides, VLDL cholesterol, inflammatory markers and blood pressure. It also avoids insulin resistance. It is helpful in treatment of type 2 diabetes. CoQ10: It improves insulin resistance lowers glucose and fasting insulin levels .

8. Minerals: Chromium increases insulin sensitivity and improves glucose tolerance in patients with type 2 diabetes. Thus, it regulates glucose levels. Magnesium is involved in glucose oxidation and glucose transport across cell membranes. Its intake lowers the levels of fasting insulin. It helps to preserve adipocyte insulin sensitivity. Zinc and antioxidants prevents the damage of retina due to oxidative stress. Phytoestrogens : Phytoestrogens and soy proteins reduce adipose tissue and improve glucose uptake Berberine : It is active constituent of the ancient Chinese herb Coptis chinensis Franch which is used to treat diabetes. It decreases in HbA 1c , fasting plasma glucose, post prandial glucose, and plasma triglycerides. Other benefiary effects of Berberine includes reduction of serum cholesterol, triglyceride, LDL-C, systolic and diastolic blood pressures etc. Curcumin : Curcumin , active principle of turmeric, directly interacts with cyclooxygenase-2 (COX-2). DNA polymerase, lipoxygenase (LOX), glycogen synthase kinase 3b (GSK-3b) cytokines (TNF-α). Hence, it has role in prevention of Diabetes. Herbs used in diabetes treatment Babul, bel , Aloe, kalmegh , drumstick, bitter gourd, flax seeds, kadhipatta , green tea, guduchi etc.

9. Benefits and Role of Nutraceuticals in Prevention of Cardiovascular Diseases Curcumin : It is a major component of turmeric (Curcuma longa). It has various therapeutic activities such as anti-carcinogenic, anti-inflammatory, antioxidative , antibacterial, hypoglycemic , and hypocholesterolemic etc. It significantly decreases serum lipid peroxides, increases in HDLC, and decreases total serum cholesterol level. Hence, it acts as anti- hyperlipidemic . It improves functioning of heart and blood vessels and has membrane stabilizing effects. It is good antioxidant hence; it helps to avoid oxidative injury. Coenzyme Q10 (Ubiquinone): Coenzyme Q10 (CoQ10) is an antioxidant naturally produced in the body, present in the heart, kidney, pancreas and liver. It is mainly found in meat and seafood. It takes part in various activities such as free radical scavenger, mitochondrial energy production, regeneration of vitamins E, C and A, inhibition of oxidation of LDL, reduction of total cholesterol, triglycerides, raises HDL-C and protects from ischemic reperfusion injury. Low level Coenzyme Q10 leads to hypertension, CHD, hyperlipidemia , Diabetes, and atherosclerosis. Coenzyme Q10 has protective action against ischemia- reperfusion injury caused during coronary artery bypass graft (CABG) surgery . It avoids myocardial damage caused ischemia reperfusion injury by increasing ATP concentration, enhancing antioxidant capacity, reducing oxidative damage and reducing cardiomyocyte apoptosis .

10. Flavonoids: These are class of polyphenolic compound mainly present in onion, apples cruciferous vegetables, black grapes, red wine, grapefruits, cherries, berries and herbs etc. Flavonoids block the angiotensin- converting enzyme (ACE), thus reduces blood pressure. It blocks cyclooxygenase enzyme that breaks down prostaglandins and hence prevents platelet aggregation. They also have protective effects on the vascular system and tiny capillaries. Flavonoids present in tea acts by various mechanisms such as suppress free radicals, protect mitochondrial damage, and suppress hyperglycemia . Thus, they reduce hypertension and improve cardiac hypertrophy. Dietary fibers : The consumption of fiber rich food significantly reduces the risk of CVDs. Soluble fiber (gums, fruits) helps to lower blood fat and maintain blood sugar level. Water insoluble fibers such as cellulose, hemicelluloses pass into the digestive tract and trap cholesterol, toxins etc. These fibers bind cholesterol, bile acids, and disrupt the enterohepatic cycle. Also Bile acid biosynthesis needs cholesterol and hence blood cholesterol levels can be reduced.

11. Plant sterols: These are natural compounds found in vegetable oils, nuts, seeds, legume, fruits, vegetables and grains. E.g. sitosterol , campesterol and stigmasterol . It should be consumed 150 to 400 mg/day. Hence, sterols are useful in preventing coronary heart diseases. Nuts: Nuts contains mono- and poly-unsaturated fatty acids, dietary fiber , phytosterols , and polyphenols etc. Nuts reduce levels of LDL cholesterols and thus reduce the risk of CVDs. Omega 3 fatty acids: Omega 3 fatty acids such as eicosapentanoic acid (EPA) and docosahexanoic acid (DHA) protect against CVDs. As per various studies it can be predicted that Omega 3 fatty acids reduces platelet aggregation, blood viscosity, plasma fibrinogen levels, PF4, and thromboglobulin and increase capillary flow. Thus, it can be used to treat CVDs. Rice bran: It lowers the level of LDL and increases the level HDL and hence protect against heart disease. Probiotics: Probiotic bacteria inhibit cholesterol synthesis and enhance cholesterol metabolism. This action is due to short-chain fatty acids produced during carbohydrate fermentation carried out by these bacteria. Probiotics reduce total cholesterol, triglycerides and LDL. Soy Proteins: Soy products are rich in polyunsaturated fatty acids, fibre, vitamins and minerals etc. Soy proteins decrease the micellar content and absorption of lipids. It inhibits angiotensin converting enzyme (ACE) and thereby reduces systolic and diastolic BP.

12. Polyphenols: Polyphenols include number of phytoconstituents such as flavonoids, phenolic acids, stilbenes and lignans etc. food like fruits, vegetables, cereal, legumes, and beverages are main sources of phenolic compounds. Polyphenols improve HDL-C levels. Polyphenols act as anti-atherosclerotic agent by decreasing LDL oxidation, improving endothelial function, increasing nitric oxide release, protection against myocardial ischemia and platelet aggregation. Resveratrol (RES) is a polyphenol, found in grapes, berries and red wine. Various studies have showed that Resveratrol improve skeletal muscle and vascular function, inhibiting LDL-C oxidation, and thereby retards atherosclerosis. It has protective effects, cardiac hypertrophy and heart failure. Spirulina : Spirulina ( Cyanobacterium ) is a type of blue green algae rich in protein, vitamins, minerals, carotenoids and phycocyanins etc. It shows alterations in blood lipid profiles. It reduces TC and LDL-C. α- Tocopherol : It is vitamin E and is fat soluble antioxidant. Being antioxidants it reduces cholesterol, inhibits cancers and manages diabetes. Vitamin D ( Calciferol ): Vitamin D protect against atherosclerosis by inhibition of macrophage cholesterol uptake, foam cell formation, reducing vascular smooth muscle cell proliferation, and avoiding expression of adhesion molecules to endothelial cells Sesame: Various studies have indicated that Sesame lowers serum glucose, LDL-C, increases HDL, reduces oxidative stress markers, lowers BP, reduces inflammation etc.

13. Benefits and Role of Nutraceuticals in Cancer Prevention 1. Polyphenolic compounds: ( a) Epigallocatechin 3 gallate is example of polyphenolic compound present in green tea. It has prominent antitumour properties. (b) Resveratrol is another example of poplyphenolic compounds which are used in treatment of cancer because of its anti-proliferative action. Resveratrol is a stilbenoid , present in skin of grapes, blueberries, peanuts etc. (c) Flavonoids: Flavonoids can affect the mRNA levels of genes important in cell cycle control and apoptosis. They interact with enzymes related to DNA topology. Some flavonoids like genistien modulate topoisomerase II activity. Quercetin , also has anticancer effects. It initiates cell apoptosis, prevent carcinogenesis, and inhibit melanoma, growth, invasion of cancer. (d) Phytoestrogenes are special group of compounds containing isoflavonoids , flavonoids, stilbenes , and lignans and have property to bind estrogen receptors. ( e) Soy protein consists of genistein and daidzein . Soya proteins reduce the levels of luteinizing hormone (LH), follicle stimulating hormone (FSH) and progesterone. It protects from breast cancer or prostate cancer. (f) Blueberries, blackberries and strawberries are polyphenolic compounds and are good antioxidants. These are effective in the prevention of development of cancer cells.

14. Vitamins and Minerals: Vitamins A, C, E and trace elements like selenium can prevent cancer. Ascorbic acid reported to induce apoptosis through cell cycle arrest, activates the apoptosis factors and interferes with iron uptake in cells. Appropriate dose of supplements like β-carotene, vitamin C, vitamin E and zinc, calcium and vitamin D reduces the chances of bladder cancer, breast and skin cancer. Curcumin : It is chemopreventive in nature. It induces apoptosis in malignant cell lines by suppressing cellular signaling pathways. It suppresses tumour growth by disrupting the activity of several enzymes required for growth and proliferation of cells. Being the potent inhibitor of TNF-α, curcumin suppresses cancer cell proliferation. Curcumin is useful in treatment of colon, stomach, lung, breast, and skin cancers etc.

15. Capsaicin : It is a pungent principle obtained from red chili peppers of Capsicum genus of Solanaceae family. It inhibits growth and induces apoptosis of cancer cells by inhibiting plasma membrane NADH oxidase activity. Gingerol : Gingerol oleoresin isolated from Ginger ( Zingiber officinale ) is commonly used dietary supplement. It has many therapeutic effects such as anti-inflammatory, analgesic, anti-hepatotoxic, antipyretic, and cardiotonic effects. It also suppresses generation of superoxide anion by inhibiting xanthine oxidase. Lycopene : Lycopene is present in Tomatoes have antioxidant properties. It suppress the insulin like growth factor-I (IGF-I), cell cycle progression, reduces the binding capacity of AP-1 transcriptional complex and inhibits proliferation of cells. It is used to treat prostate cancer, gastric cancer, breast cancer, liver and lung cancer etc. Chestnut : Chestnut is antioxidant in nature and is used to treat gastric cancer, and mild prostate cancer and breast cancer. Ginseng : It is used to treat various cancers such as blood, colon, liver, breast and lung being antioxidant in nature. Cruciferous vegetables: Dietary fiber rich cruciferous vegetables like broccoli, cabbage, cauliflower, sprouts, turnip, mustard etc. are used in treatment of cancer

16. Benefits and Role of Nutraceuticals in Prevention of IBD and Other GIT Diseases Dietary Fibers : Fiber improve intestinal transit and decrease constipation being bulking agents. IBS patients are recommended to include soluble fibers in diet. Gas producing foods: IBD can be treated with gas producing food such as alcohol, apricots, bananas, beans, caffeine, carrots, celery, onions, raisins etc. Curcumin : It acts as anti-inflammatory agent and reduces mucosal Injury by inhibition of nuclear factor NF- kB and pro-inflammatory cytokines Curcumin heals peptic ulcers by preventing peroxidase inactivation and enhancing free radical scavenging activity . Zinc : Zinc deficiency causes ulcerations, inflammatory infiltration, oedema of the jejunum, leads to poor absorption of dietary fats, with accumulation of lipids, impairs sodium and water balance and causes intestinal tract damage by free radicals. Zinc supplements improve markers of intestinal permeability and reduce diarrhoea .

17. Probiotic: Probiotics are living microorganisms like species of lactobacilli or bifidobacteria . They maintain good health by improving balance in intestinal microflora . Probiotics also strengthen defence mechanism by strengthening intestinal tight junctions, increasing mucous secretion, enhancing motility, and producing protective nutrients etc. Probiotics have protective effects like prevention of colonic shortening, lowering of liver and thymus weights, and prevent spleen enlargement. Prebiotics: Prebiotics are defined as, "non-digestible polysaccharides like oligosaccharides and insulin which stimulates growth and activity of specific species of bacteria in the colon. It has various beneficiary effects such as improvement in bowel function, increased mineral absorption, altered lipid metabolism, and a reduced risk of colon cancer. They enhance bioavailability and absorption of calcium, magnesium, iron and zinc. Vitamins: Fat soluble vitamins A and D have protective action against IBD. Vitamin D produces protective effects by down regulating pro-inflammatory cytokines like IL-6, IL-21, TNF- α, and IFN-y and by stabilizing the intestinal barrier. Vitamin K protects against IBD and maintains bone health in patients.

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