Nutraceutical Compounds PDF

NUTRACEUTICAL COMPOUNDS Red ginseng oil→ unsaturated fatty acids and lipophilic components (root steamed for 1-3hours + drying process→ water extraction process→ RG marc and RG extract→ from marc→ RGO): 1. Antioxidant properties → free radical scavenging and upregulation of antioxidant enzymes....

NUTRACEUTICAL COMPOUNDS Red ginseng oil→ unsaturated fatty acids and lipophilic components (root steamed for 1-3hours + drying process→ water extraction process→ RG marc and RG extract→ from marc→ RGO): 1. Antioxidant properties → free radical scavenging and upregulation of antioxidant enzymes. 2. Anti-inflammatory effects→ inhibition of AP-1 and NFkB 3. Chemopreventive properties→ activation of the nuclear factors E2 related factor 2 (Nrf2); expression of phase II detoxifying and antioxidant enzymes. 4. Antiapoptotic→ protective effects; inhibition of caspase activation, reducing mitochondrial Bax/bcl-2 ratio and P-cJun 5. Anticancer properties 6. Hair growth→ activation of IGF-1, VEGF, Wnt/beta catenin and Sonic hedgehog pathways 7. Other activities→ boost quality and appearance of the skin, immunomodulatory effect and antiatherogenic effects. METABOLIC SYNDROME NUTRACEUTICAL COMPOUNDS Berberine is an alkaloid found in various plants→ Chinese and Ayurvedic system; gastrointestinal issues such as diarrhea and infections. Today metabolic syndrome and cardiovascular health. 1. Hypoglycemic effects→ inhibition of gluconeogenesis, stimulation of glycolysis and increase insulin sensitivity; similar to metformin 2. Lipid lowering effect→ boost of LDL clearance (upregulation of LDL receptor genes and stabilization of LDL receptors in the liver) and inhibition of lipid synthesis. 3. Antihypertensive effect→ promotion of vasodilation (inhibition of ACE enzyme and alpha 1 adrenergic antagonism) Momordica Charantia, is a tropical plant widely used in traditional medicine particularly in Asia. NBCs present: momordicin, charantin, polypeptide p and vicine. It targets key metabolic tissues. 1. Hypoglycemic effects→ promotion of insulin production and sensitivity and reduction of glucose absorption. Poly p is similar to insulin. 2. Hypolipidemic effects 3. Antihypertensive effects Gymnema Sylvestre, commonly known as “sugar destroyer”, is a plant native to India and Africa. Mixture of saponins, acidic glycosides and anthroquinones. 1. Hypoglycemic effects→ gymnemic acids (sweetness inhibitors; reduced sweet craving), combined with insulin helps reducing blood glucose levels, reduction of glucose absorption and enhancement of insulin activity. 2. Hypolipidemic effects Irvingia Gabonensis, commonly known as African mango, native to central and west Africa. The bark has antibiotic properties and used to favor dermal wound healing. Its properties are attributed to its high concentration of dietary fibers and its capacity of modifying the lipid distribution. 1. Hypoglycemic effects 2. Hypolipidemic effects→ inhibition of adipogenesis. Resveratrol is a polyphenolic compound that acts as defense mechanism in plants (phytoalexin). It gained attention following the French paradox. It has poor bioavailability→ carriers 1. Antioxidant properties 2. Metabolic regulation→ interact with SIRT1 and AMPK 3. Antihypertension→ boost of NO synthesis 4. Hypolipidemic 5. Hypoglycemic effects 6. Anti-atherogenic plaque formation. Ursolic acid is a pentacyclic triterpenoid found in the skin of fruits and in herbs. 1. Hypoglycemic effects 2. Lipid metabolism→ reduced adipocytes differentiation and lipolysis; management of obesity. HYPERCHOLESTEROLEMIA Red yeast rice is a traditional Chinese food product made by fermenting rice with M. Purpureus. It contains Monacolin K and monacolin-related compounds (direct and indirect hypolipidemic effect) 1. Hypolipidemic effects→ inhibition of HMG-CoA reductase. Monacolin K is chemically identical to lovastatin→ higher bioavailability and more severe side effects. NB: variability. Omega-3 fatty acids are polyunsaturated fatty acids. New source of omega 3 fatty acids is the krill oil (bound by phospholipids); rich in EPA and DHA and astaxanthin (anti-ox) 1. Lipid lowering effects→ lowering of triglycerides and LDL and increasing of HDL 2. Anti-inflammatory effects 3. Glucose tolerance Annurca apples exhibit a very high polyphenolic content, particularly catechins. 1. Hypolipidemic action→ overexpression of LDL receptors in the liver and increase in HDL Plant sterols and stanols for managing moderate to high cholesterol levels. 1. Hypolipidemic effect→ compete with dietary cholesterol for intestine absorption; potential atherogenic properties. Dietary fibers especially soluble fibers such as psyllium, pectin, guar gum and beta glucans. 1. Hypolipidemic effects→ bile acid sequestration, enhance of LDL receptors and increased LDL clearance 2. Inhibition of hepatic fatty acids synthesis 3. Reduced macronutrient absorption 4. Improved intestinal motility Polyphenols are compounds characterised by many phenolic groups. It comprise flavonoids and catechins. 1. Hypocholesterolemic effects→ inhibition of key enzymes and boost of LDL clearance T2D It’s characterised by insulin deficiency and insulin resistance→ enhancing glucose uptake and modulating glucose transporter. Amorfrutins are isoprenoid-substituted benzoic acid derivatives. They work as thiazolidinediones; distinct gene expression pattern. 1. Hypoglycemic effects→ activation of PPARgamma→ glucose metabolism, lipid storage and insulin sensitivity 2. No side effects like fat storage or hepatotoxicity. Morus alba leaves effects are similar to Glibenclamide. Main compound is 1-deoxynojirimycin. 1. Hypoglycemic effects→ alpha glucosidase inhibitor and increase liver sensitivity to insulin 2. Inhibition of CYP450 enzymes→ altered drug metabolism. Dietary lipids are among omega 3 and 6 fatty acids. 1. Hypoglycemic effect→ activation of the PPARgamma HYPERTENSION Beetroot juice is a primary source of dietary nitrates. Dietary nitrates→ absorbed in small intestine→ salivary glands→ reduced to nitrites→ stomach→ NO or re-ox to nitrates. 1. Antihypertensive effects→ conversion of nitrates into NO (vasodilation) Olive oil has an higher consumption of monounsaturated fatty acids (MUFAs) 1. Lipid lowering effects→ reduced risk of coronary heart disease; reduced LDL 2. Antihypertensive effects→ no clear connection Garlic-based nutraceuticals particularly those containing S-allyl cysteine and organosulfides. Ex. aged garlic extract. 1. Antihypertensive effects→ stimulation of endogenous hydrogen sulfide production in vascular system→ eNO regulation and hyperpolarization of SMCs (membrane ionic channels) 2. Cardiovascular effects→ Organoselenium compounds, steroid saponins, sapogenins, B6/12, flavonoids, lectins and N- fructosyl aa INFLAMMATION Curcumin is a polyphenolic diarylheptanoid responsible for the yellow pigment. 1. Targets many inflammatory pathways→ COX2, STAT3, LOX5, pro-inflammatory cytokines and so on. 2. Upregulation of PPAR gamma→ inflammation reduction and promotion tissue repair 3. Low bioavailability→ new formulations; administered with Piperine Polyphenols have a high antioxidant capacity. 1. ROS scavenging 2. Enhance antioxidant enzymes 3. Enhances glutathione levels Flavonoids are secondary metabolites. Anthocyanins, pigments responsible for the color of many plants. They consist of 2 phenyl rings and a heterocyclic ring. Low bioavailability→ gastrointestinal and liver metabolism. They are classified according to the extent of oxidation and the presence of substituents. An example is Myricetin→ bark of Myrica nagi thumb in India; yellow coloured crystal dye. 1. Anti-inflammatory effects→ inhibition of COX enzymes + prevent NF-kb activation 2. Anti-oxidant effects→ increase levels of superoxide dismutase 3. Prevention of periodontitis→ inhibit expression of genes coding important virulence factors of porphyromonas gingivalis Propolis, often referred to as bee glue, is a resinous substance. The 13^th group is the red propolis; 300 compounds→ terpenes, flavonoids, aromatic acids, fatty acids and inorganic elements + Neovestitol→ isoflavonoid 1. Antioxidant effects 2. Anti-inflammatory effects → modulation of NO pathway and IL-6 release 3. Anticaries 4. Antimicrobial properties Fenugreek is a medical herb, whose therapeutic potential is mainly attributed to its high content of flavonoids, saponins and polyphenols. 1. Anti-inflammatory effects → suppression of TNF alfa 2. Managing metabolic syndrome 3. Managing neuroinflammation 4. Antipyretic properties 5. Antioxidant properties→ accelerate wound healing Frankincense contains a variety of resins (boswellic acids), gums and essential oil (terpens + sesquiterpens). 1. Anti-inflammatory effects→ inhibition of 5-LOX, Cox2 overexpression, modulation of NFkb and interference with calcium  2. Pain-relieving properties→ essential oil 3. Anti-oxidant properties→ gums 4. Antitumor and antibacterial→essential oils Mirtle contains terpenoids, tannins and flavonoids. 1. Astringent, tonic and antiseptic properties→ wound healing as well as treating disorders of digestive and urinary systems 2. Anti-catarrhal properties→ respiratory diseases 3. Anti-inflammatory effects→ inhibition of ROS, elastase, COX and 5 LOX 4. Antiproliferative effects Ginger is a traditional medicine, its primarily active compound is the gingerol, then zingerone, zingiberene, polysaccharides, raw fibers, lipids and organic acids. 1. Inhibition of COX enzymes 2. Suppression of inducible NO synthase and TNF alfa → inhibition of NFkb and translocation of PKC alfa 6-gingerol→ 6 shogaol → 6 paradol 3. Zingerone → cleavage reaction → antitumor activity, antihyperlipidemic and antibacterial properties. NEURODEGENERATIVE DISEASES They are caused by a variety of primary insults or triggers such as inflammatory insults, neurodegenerative insults, metabolic insults and ischemic insults. Parkinson disease Mucuna plant is a tropical legume native to Africa and Asia. It contains phenols, polyphenols and tannins. High levels of L-DOPA 1. Rejuvenating effects → nervous system and reproduction system 2. Aphrodisiac and arthritis treatment 3. Antidiabetic effect 4. Antiepileptic effect 5. Antineoplastic effect 6. Antioxidant effect → oxidative stress-related skin conditions 7. Antimicrobial effect Red ginseng contains ginsenosides. 1. Improvement of motor functions 2. Protection of dopaminergic neurons Mitochondrial targeting nutraceuticals: 1. coQ10 2. Curcuminoids and Mucuna compounds→ neuroprotective effects 3. Phosphocreatine Epigallocatechin-3-gallate (EGCG) is found in the green tea, 1. Antioxidant effects 2. Iron chelating capacity 3. ROS scavenging 4. Antiapoptotic actions 5. Activator of AMPK→ neuroprotective effects Alzheimer disease New hypothesis establishes a link between AD and metabolic diseases, with some researchers referring to it as “type 3 diabetes”→ insulin resistance. Key metabolic players are the mTOR, sirtuins and the AMPK. Omega3 fatty acids→ NB: more promising as they ameliorate low chronic inflammation in the early stages. 1. Crucial for brain health and development ( EPA and DHA)→ reduced in AD patients. NB: ALA Polyphenols → flavonoids 1. Neuroprotective benefits EGCG 1. Activation of AMPK B-group vitamins + Vitamin E Herbal medicines→ ginkgo biloba and ginseng MIGRAINE It’s caused by an imbalance of brain activity; causes are the sensitization of trigeminovascular system, imbalances in Ser and energy metabolism in brain. Trigeminal sensory nerve fibers→ brainstem activation → release of vasoactive peptides→ increase of NO, vasodilation, leakage of blood vessels and degranulation of the mast cells→ Pain impulses. Feverfew→ used for the pain, headache and fever. Active ingredient is the parthenolide. 1. Inhibition of the nucleus trigeminal caudalis 2. Inhibition of prostaglandins production 3. Inhibit platelets aggregation 4. Stabilization of Ser levels  5. Inhibition of phospholipase A Butterbur is the active compound of Petadolex; formulation without petasin and hepatotoxic compounds 1. Anti-inflammatory effect→ inhibition of the COX-2 2. Vasodilatatory effects→ inhibition of the L-type voltage gated calcium channels Marijuana 1. Analgesic effects→ action on descending Ser pathways 2. Anti-inflammation properties 3. Inhibition of Ser release Riboflavin is a vitamin that plays a crucial role in mitochondrial energy metabolism. 1. Regulation of mitochondrial energy metabolism Magnesium → intravenous magnesium sulfate and oral magnesium supplementation Coenzyme Q10 1. Improvement of mitochondrial function and energy production PUFAs 1. Reduction of NO production 2. Link with Ser Capsaicin→ intranasal capsaicin Ginkgolide B Phytoestrogens Caffeine DEPRESSION Hypericum perforatum; active compound is the hypericin. 1. MAO inhibition 2. Mild Ser reuptake inhibitor 3. Modulate other neurotransmitters Saffron 1. Anxiolytic properties 2. Antidepressant effect → antioxidant and anti-inflammatory 3. Serotoninergic action 4. Neuroprotective function Curcumin 1. Anti-inflammatory 2. Antioxidant 3. MAO inhibition Omega-3 fatty acids→ major depressive disorder 1. Anti-inflammatory properties 2. Stability and fluidity of the neuronal membrane 3. Restore Ser transport Probiotics 1. Maintain gut microbiota healthy→ gut-brain axis→ neuromodulatory effects Vitamin D → low levels have been associated with an impaired HPA axis 1. Anti-inflammatory effects 2. Modulation of neurotransmitter system 3. Promotion of neuronal growth and survival 4. Regulation of the mood 5. Healthy circadian rhythms CANCER DRUG-RELATED AGENTS → influence various biological pathways Carotenoids→ 600 compounds with antioxidant properties. They are divided into xanthophylls and carotenes 1. Beta carotene and other carotenoids→ converted in retinol→ increased risk of lung, prostate and stomach cancer; but reduced risk of other cancers. Beta-carotene is associated with lung cancer! 2. Lycopene→ reduced risk of prostate cancer. It decreases ROS, induces apoptosis and attenuate metastasis 3. Vitamin D → reduced colorectal cancer 4. Vitamin E and selenium → not currently recommended 5. Curcumin→ anti-colorectal tumor 6. Resveratrol 7. Tea polyphenols 8. Other polyphenols 9. Folc acid→ cofactor in one carbon metabolism