Serotonin: The chemistry of Well-Being Overview and Experiments Update The Magic Ingredient of Our Success Formula During the past 25 years, the Pharmaceutical industry has invested billions of dollars on the marketing of antidepressants. An indirect results are that the terms “increase in serotonin level” and “serotonin as a chemistry of well being” has become part of our mainstream vocabulary. The industry funding has been essential for identifying the serotonin/dopamine transporters as a target for the development of antidepressants. Our study shows that in oral form, 100% water soluble serotonin and dopamine have insignificant absorption rates. In this case the notion that oral water-soluble ingredients should work as well as oral bioavailable is not working. Optimization of oral bioavailability is a continuing challenge for the pharmaceutical industry. We have created such a transporter. The transporter completely mimics the natural way of serotonin absorption as well as numerous other ingredients. The bioavailability of the new natural serotonin is raised up to 3,000 times. Under these circumstances it becomes possible to market an oral supplement (capsules, gel, and chewing gum) with the brand “Natural serotonin”. Our R&D are co-operated with 4 Groups of Scientists with 40years experience with serotonin related health problems led by: Dr. Lubovtseva Lubov Histological studies of serotonin in the tissues Dr. Moshkin MikhailSeasonal affective disorder Dr. Simonenkov Alexey-Use of serotonin drugs in clinical practice Dr. Popova Nina – Serotonin behavioral neurogenetics The second challenge is to exploit well-established use and brand of serotonin as a chemistry of well-being The third marketing success challenge is to come in under the radar with efficacy not only beyond the competition, but ahead of an entire industry, giving no chance to our competitors to clone it. Despite a reduction in attrition due to pharmacokinetics issues, efficacy has not improved, since 1991. We discovered an universal solution for many ingredients, which mimics existing natural delivery system of active substances in the body at the cellular level. In comparison with 100% water soluble Serotonin we increse it efficacy in oral form by 3000 times!!! Mannanoligosaccharide (MOS) Supramollecular with Serotonin Macrophages envelope Mannan Oligosaccharides like mycobacteria Serotonin (Also known as 5-HT, or 5hydroxytryptamine) • Serotonin is the most ubiquitous neurotransmitter of all • It’s found in the central and peripheral nervous systems, it is located in the GI tract, platelets, mast cells and macrophages • ~95% of all serotonin in the body is in the gut Functions of serotonin • • • • • • • • • • • • • • • • Happiness Sociability/boosts self-esteem/overcomes shyness Social phobias Makes you full and feel sleepy Impulsive eating disorders Impulse control Helps to control pain pathways Nausea, vomiting, gastric motility Generalized anxiety disorder Aggression Premenstrual disorders Migraines Erections Prevent bleeding Immune control Provide Thermoregulation Serotonin in skin regulates thermogenesis Typical metabolism The serotonin and smooth muscle • • • • Serotonin is the leading factor responsible for stimulation of the smooth muscles contraction The smooth muscles can contract without conscious control Serotonin is considered as an “energy” factor the smooth muscles contraction Smooth muscle is found within the walls of all blood vessels, including the smallest arteria, in lymphatic vessels, the urinary bladder, uterus, male and female reproductive tracts, GI tract, respiratory tract, arrector pili, closing up the skin’s pores, the eye’s ciliary muscle that controls accommodation for viewing objects at varying distances, the iris of the eye, which is responsible to the amount of light entering the eye The Second Brain...serotonin and the gut • GUT CHECK: A complex, independent nervous system lines the gastrointestinal tract that has been dubbed the "second brain” influences Mood and Well-Being Age related Serotonin decrease Different serotonin receptors and the serotonin transporter decline with age coursing that can be treated by Newly developed Serotonin supplement: • low energy levels • reduced initiative • decrease in sex drive • reduced visual acuity • development of varicose and spider veins • uncontrolled weight gain • reduction of erections in the morning • depression • bleeding gums • reduced thermo genesis • weather sensitive problems • low tolerance for alcohol Serotonin is major factor of Thermoregulation • • • The vasomotor response and total body oxygen consumption are clearly reduced in intensity with age. Serotonin controls the vasomotor mechanism, how you blood vessels dilate and constrict. Internal body temperature is controlled through sweat production and the rate of blood flowing through the network of blood vessels within the skin. Serotonin supplements is the Natural Way to Improve Thermo genesis. Serotonin treatment of Meteo-dependent People Increased sensitivity to weather changes affected primarily the elderly and vegetatively unstable people. They respond not only to changes in weather, but the high humidity, temperature fluctuations, low pressure, electrical voltage in the atmosphere of various ailments: headaches, migraines, sleep disorders, anxiety states, depression, insomnia. Serotonin improve skin via blood circulation Improves Skin The pores of the skin through which sweat is excreted get clogged due to the use of creams, deodorants and dead skin cells. These clogged pores cause skin problems like acne, pimple and blackheads. The serotonin supplement opens up these pores, and the sweat flushes out of them, thus carrying poisonous substances out of the body. Improves Blood Circulation The serotonin supplement activates the blood vessels that ensures that there is proper supply of blood even by the thinnest of the capillaries. Proper blood supply brings fresh nutrients to the cells and ensures complete removal of waste out of them. Serotonin expelling toxins in the blood Serotonin prevent bleeding. The natural chemistry to treat bleeding gums Serotonin increases visual acuity in the 0.2-0.3 units per course of treatment (10-20 capsules of 10 mg) mg) Serotonin removes varicose and spider veins Serotonin may rank people 10 mg 200 mg Morning wood is a good indicator of healthy serotonin levels Team spirit Here we have a solitary and lonely creature, the desert locust. But just give them a little serotonin, and they go and join a gang Serotonin linked to estrogen and menstrual migraines Serotonin and depression What do women do when we’re depressed? We eat! In addition to increasing serotonin in the brain, chocolates (boost) anandamide—a substance that closely resembles marijuana Weight loss The weight loss drugs target the satiety center in the hypothalamus— boost serotonin that tells you – “stop eating, you’re full” The SRI’s (serotonin reuptake inhibitors) 1987—the first selective serotonin reuptake inhibitor marketed Prozac The SRIs—side effects • Increasing serotonin may result in decreased dopamine • Dopamine gives you some zip to your doo-dah in the bedroom • SRIs may result in anorgasmia, loss of libido and premature ejaculation • Inhibit platelets • Course bleeding gums Serotonin syndrome Overdose of SSRIs Drugs associated with serotonin syndrome Experimental part Membrane potential is the difference in electrical potencial between the interior and the exterior of a biological cell with synthetic serotonin (green) and Sea-backthorn extract (red). Serotonin from sea-backtorn Serotonin content 1-2% - Neurotransmitter Serotonin Melatonin - “Happiness“ Hormone - Increase Activity - Awakening from sleep Triptophan Dietary sourses Serotonin Melatonin -Circadian rhythm - Sleep - Seasonal affective disorders - Depression - Decrease in activity The comparitive study of the natural (ОбП) and synthetic serotonin (Сер). Morphological and neurochemical benefits of its consumption for Djungarian hamster Dosage: synthetic serotonin – 28.5 mg/per hamster*per day; natural serotonin – 300 mg - equivalent for 28.5 mg of synthetic serotonin/per hamster*per day Duration : A) 02.11.2010-15.01.2011 B) 02.11.2011 – 15.01.2012 Djungarian hamster : seasonal changes •Seasonal colour changes •Weight reduction •Motion activity reduction •Temperature regulation changes • Immune response suppression Research objectives: A comparison study of morphofunctional changes for two groups of animals: •Screening group (K) и •Group fed with serotonin enhanced supplement (ССВО) All the tests were carried out in shorter daylight hours. Animal’s weight 1 30 Масса тела, г Duration, days -1 -2 At the end of experiment * - p=0.04 20 -3 К -4 ССВО -5 10 -6 0 1 3 5 7 К 9 ССВО Groups of animals 4 Animal’s fatness 3 Индекс Changes in body weight 0 Weight 2 1 0 К ССВО Groups of animals Spontaneous motion activity before the experiment and within 1st -3rd weeks of experiment 500 450 400 ССВО 350 300 250 200 150 100 50 19 19 20 20 21 21 21 22 22 23 23 24 24 25 25 26 26 26 27 27 28 28 29 29 30 30 31 31 32 32 32 33 33 34 34 35 35 36 36 37 37 37 38 38 39 39 40 40 41 41 42 42 43 43 0 0 3 1 2 Test equipment to register the spontaneous motion activity Spontaneous motion activity 250 Average nightly activity changes, per week Motion activity dynamics (average nightly per week) 200 К 150 ССВО 100 50 0 0 -50 1 2 3 4 Duration, weeks 5 6 7 9 Oxygen intake dynamics 15 minutes animals exposure to cold, into the helium oxygen environment (HELOX) Oxygen intake, ml* 18 15 12 Контроль ССВО 9 1 2 3 4 5 6 7 8 9 Test duration, minutes 10 11 12 13 14 15 An equipment to register the oxygen intake Oxygen intake 15 minutes animals exposure to cold, into the helium oxygen environment (HELOX) К 200 17 Ml/g weight Ml/g weight ССВО 100 11 0 5 Суммарное * p= 0.03 Mаксимальное Mинимальное Energy loss 15 minutes animals exposure to cold, into the helium oxygen environment (HELOX) Total energy loss during the test Body thermal conductivity 90 3.0 * р = 0.005 J/weight, g/temperature 0С * p =0.001 J/weight, g 60 2.0 1.0 30 Контроль ССВО Контроль ССВО 38 Body temperature before and after exposure to cold in HELOX К * Body temperature , C ССВО 36 34 * - p = 0.018 32 До теста К После теста ССВО Scatterplot: S_MOC vs. dTb (Casewise MD deletion) dTb = 4.3391 - .0295 * S_MOC Correlation: r = -.2581 1 Scatterplot: dTb S_MOC vs. dTb (Casewise MD deletion) = -20.20 + .08914 * S_MOC Correlation: r = .95259 1 0 0 -2 -1 -3 dTb dTb Temperature changes -1 -2 -4 -5 -3 -6 -4 155 160 165 170 Total oxygen intake 175 180 S_MOC 185 190 195 200 205 95% confidence -7 160 170 180 190 200 S_MOC 210 220 230 240 95% confidence Erythrocytes Type Erythrocytes RBC/HCT Haematocrite Haemoglobin HGB/RBC HGB/HCT Контроль ×1012 c/l 9,54±0,20 фл 46,14±0,55 % 43,84±0,65 g/l 16,84±0,37 17,64±0,22 38,40±0,32 СВВО 9,23±0,19 45,90±0,55 42,33±0,97 16,56±0,33 17,98±0,18 39,17±0,35 Leukocytes Type Leukocytes Lymphocytes Контроль 9,89±1,20 ×109/l 6,24±0,71 СВВО 7,90±0,80 5,32±0,41 MID# 1,97±0,54 1,08±0,15 Granular leukocytes Thrombocytes Thrombocryte 1,64±0,26 ×109 c/l 225,0±7,0 % 0,21±0,01 1,56±0,25 226,7±11,4 0,21±0,01 Visceral organs weight Animals group Name, weight, mg Suprarenal capsule 5,10±0,38 Brown fat Thymus gland Spleen К Android glands 56,0±16,5 140,7±20,9 20,3±5,4 61,1±10,7 ССВО 34,0±2,54 4,43±0,43 107,0±20,8 17,3±5,1 40,0±3,5 1400 50 Spontaneous motion Immune response 25 Number of АОК/spleen weight, mg Energy changes, (average per night per week, sec/hour) Immune response to the antigen intake (sheep red blood cell) 0 К -25 ССВО -50 -75 1050 * 700 350 -100 0 -125 0 1 2 3 4 Time after antigen intake, days 5 6 К ССВО Группы животных * - р=0,0509 (Mann-Whitney U тест) Serotonin enhanced supplement consumption: 1.Considerably reduced weight 2. Increased spontaneous motion activity within first four weeks of the experiment 3. Kept summer type of thermal regulation it means that more energy wasted to compensate exposure to cold. 4. Increased immune response to the sheep red blood cells intake. Nuclear Magnetic Resonance Spectroscopy of cerebrum metabolites Recording area 17,5 мм3 (2 х 3,5 х 2,5) : Categ. Box & Whisker Plot: Cr+Pcr Categ. Box & Whisker Plot: Lactate/Cr 30 28 1,6 Cr. + Pcr Lactate/Cr. 1,4 sagittal 26 1,2 Lactate/Cr Cr+Pcr 24 22 20 18 1,0 * 0,8 axial 16 * 14 12 0,6 Контр 1 2ОбП Mean ±SE ±SD Сер 3 Контр 1 0,4 Gr_mod ОбП 2 Mean ±SE ±SD Сер 3 Gr_mod Biological energy Categ. Box & W hisker Plot: Taurine C ateg. Box & W hisker Plot: Glutam ate C ateg. Box & W hisker Plot: Glutam ine 3,2 14 46 3,4 44 Glutamine 3,0 42 2,8 40 2,6 Glutamate 12 Taurine 10 38 2,4 Glutamate Glutamine 2,0 1,8 1,6 34 32 8 6 30 1,4 28 1,2 * 1,0 0,8 0,6 0,4 Taurine 36 2,2 Контр 1 ОбП 2 Gr_m od Сер 3 * 4 26 24 22 Mean 20 ±SE ±SD 2 Контр 1 ОбП 2 Сер 3 Gr_m od Antidepressants Mean 0 ±SE ±SD Контр 1 ОбП 2 Gr_mod Сер3 Me ±S ±S Colour and brown fat seasonal change Colour seasonal change of Djungarian hamsters масса при забое Categ. Box & Whisker Plot: 26 25 24 масса при забое 23 22 21 20 19 02.11.2011 – 0 week 28.11.2011 – 3rd week 10.01.2012 – 9th week 18 Контр 1 ОбП Сер 3 2 Me ±SE ±SD Группа бурый жир, мг Categ. Box & Whisker Plot: 200 Colour change: 0- 3 нед Categ. Box & Whisker Plot: 2.0 P=0.057, LSD тест Colour change: 0- 9 нед Categ. Box & Whisker Plot: ИзмОкр9_0 ИзмОкр3_0 2.2 180 3.5 H=8.6, p=0.014, Kruskal-Wallis H=2.9, p=0.24, Kruskal-Wallis 160 3.0 1.8 1.6 бурый жир, мг 1.2 2.0 1.0 ИзмОкр9_0 ИзмОкр3_0 140 2.5 1.4 0.8 0.6 1.5 120 100 1.0 0.4 * 80 0.2 0.5 0.0 60 -0.2 0.0 -0.4 -0.6 Контр 1 2 ОбП Группа 3 Сер Mean ±SE ±SD 40 -0.5 Контр 1 ОбП 2 Группа Сер 3 Mean ±SE ±SD 1 Контр 2 ОбП Группа 3 Сер Mea ±SE ±SD Tissue distribution of SEROTONIN-3H and DOPAMINE-3H in male mice ICR * - p<0.05 in comparison with serotonin -3Н (test Mann-Whitney)