Comparative bioavailability of two vitamin B1 preparations: benfotiamine and thiamine mononitrate. Benfotiamine (Sigma-Aldrich) was dissolved in a 200 mM solution of hydroxypropyl--cyclodextrin (HP--CD, Roquette, Lestrem, France) at a concentration of 25 mg/ml. Lipid-soluble thiamine derivatives were developed mainly in Japan for the treatment of beriberi. What is diabetic neuropathy? Though thiamine levels rapidly increased in blood and liver to reach a maximum after one or two hours, no significant increase was observed in the brain. The mice were force-fed with a dose of 100 mg benfotiamine/kg in approximately 100 l using a syringe prolonged by a flexible tube that was inserted into the stomach. Detection of transketolase in bone marrow-derived insulin-producing cells: benfotiamine enhances insulin synthesis and glucose metabolism. PMID: 32987117 DOI: 10.1016/j.exger.2020.111097 Abstract It is well known that patients with Alzheimer's disease (AD) have imbalances in blood thiamine concentrations and lower activity of thiamine-dependent enzymes. Thank you! For use as a nootropic, Sulbutiamine is better because it quickly crosses the blood-brain barrier. I think tolerance is way over-rated and the majority of supplements Ive reviewed do not require cycling. Finally, it seems important to us that, because of different chemical, metabolic and pharmacological properties, a clear distinction should be made between lipophilic thiamine disulfides (derived from allithiamine) and S-acyl derivatives such as benfotiamine. If you are using any of the racetams like Piracetam and Aniracetam you may want to consider adding Sulbutiamine as well.At the very minimum every neurohacker should be using a multivitamin every day that includes Vitamin B1 (thiamine). I believe it was a part of my Myers Cocktail IV some years ago. Benfotiamine does not. All authors read and approved the final manuscript. Detection of transketolase in bone marrow-derived insulin-producing cells: benfotiamine enhances insulin synthesis and glucose metabolism, Burning or shooting pains in the lower legs. The blood-brain barrier is made up of tightly packed cells in the brain's capillaries that prevent harmful substances from entering the brain. Novel Therapies for Kidney Disease in People With Diabetes. It has not been researched much. The thiamine concentration in the commercial Dulbecco's modified Eagle's medium (DMEM) is 10 M [8]. Since the discovery of allithiamine [9], a number of derivatives were synthesized. Effectiveness of omega-3 fatty acid supplementation in patients with Alzheimer disease: A systematic review and meta-analysis. In most samples, we also observed the presence of ThTP and AThTP, but the levels of these compounds in the liver and the brain were not influenced by the treatment (not shown). blood-brain barrier disruption, astrocyte dysfunction, excitotoxicity, . It is therefore likely that, in these cells, the added benfotiamine is at least partially dephosphorylated to S-benzoylthiamine that can enter the cells as in the case of the intestinal mucosa. (2002) Brain activation of monocyte-lineage cells: involvement of interleukin-6. The Japanese got Beriberi because they were on a white rice diet and became severely thiamine deficient. [i] Williams R.R., Cline J.K. Synthesis of Vitamin B1 Journal of the American Chemical Society 1936, 58 (8), pp 15041505 (source), [ii] Wernicke-Korsakoff syndrome. Mild thiamine deficiency affects a significant segment of the population in any country. Benfotiamine supplements help increase thiamine (vitamin B1) levels. Charity, best mosquito repellant on the planet has been my experience. dopamine, anxiety, depression, epilepsy, OCD, nootropics for ADHD, nootropics for social anxiety, etc. The difference is regular Thiamine does not easily cross the blood-brain barrier. Sheline CT, Wei L. Free radical-mediated neurotoxicity may be caused by inhibition of mitochondrial dehydrogenases in vitro and in vivo. These compounds can easily diffuse through plasma membranes thus bypassing the rate-limiting transport system required for free thiamine. i.e. This study provides evidence showing that GLUT1 also transports dehydroascorbic acid into the brain. It was suggested that treatment with benfotiamine blocks three major pathways (the hexosamine pathway, the advanced glycation end product formation pathway and the diacylglycerol-protein kinase pathway) of hyperglycemic damage, probably by removal of glyceraldehyde 3-phosphate and fructose 6-phosphate through activation of the pentose phosphate enzyme transketolase [18]. I think I am deficient in stomach acid, since my symptoms go away when I take a whole bunch of betaine hydrochloride capsules with my food, Id like to get to the bottom of this, though. They can guide you on whether it's safe for you and help you determine an appropriate dosage. The data are expressed as mean SEM for 4 experiments. Tablets and capsules are usually 750 mg each. If you are hypothyroid or dealing with Hashimotos there is a very good chance you would benefit from thiamine supplementation. What Happens If I Take Too Much Benfotiamine? the beneficial effects of the drug concern peripheral tissues but not the central nervous system. Charity, Ive never cycled Sulbutiamine and it works great! Published 2021 Mar 9. doi:10.2147/DDDT.S296197, Nwadiugwu MC. The researchers concluded that post-stroke fatigue and related disorders could be a manifestation of mild thiamine deficiency. Highly significant increases of free thiamine and ThMP were also observed in the liver, but not in the brain. Side effects are possible, but they've been rare in studies. I read in various health books that Vitamin B1 is necessary for the production of stomach acid, so I was wondering if all forms of B1 would have that effect or if only thiamine hydrochloride would help produce hydrochloric acid (stomach acid) because of the chloride content. Thiamine vs. Sulbutiamine: Whats the Difference? Side effects reported with benfotiamine included: There are no documented severe side effects of benfotiamine. Was this due to some physiological damage that necessitated much higher doses now to overcome this defect? For that you need Sulbutiamine. Here, the authors demonstrate that brain endothelial . Drug Des Devel Ther. 2023 Dotdash Media, Inc. All rights reserved, Verywell Health uses only high-quality sources, including peer-reviewed studies, to support the facts within our articles. Indeed, it was found effective for the protection of diabetic complications such as diabetic neuropathy [18-23] and alcoholic neuropathy [46]. Personally, Ive found Sulbutiamine to be much better for cognition than standard thiamine. It wasnt until 1897 that Christiaan Eijkman, a military doctor in the Dutch East Indies figured out that the bran removed from white rice was causing problems. Itokawa Y, Nishino K, Igarashi S. Evaluation of thiamin derivatives: human bioavailability, uptake by human blood cells, and conversion to thiamin by rat liver homogenate. https://www.alz.org/alzheimers-dementia/facts-figures. For that reason, a variety of lipophilic thiamine derivatives have been synthesized. As the brain is particularly sensitive to thiamine deficiency, we wanted to test whether intracellular thiamine and thiamine phosphate levels are increased in the brain after oral benfotiamine administration. Brien, I havent the time nor the inclination to debate this with you. . Thus, high-dose thiamine therapy reversed the symptoms of Wernicke's encephalopathy [1] and prevented incipient diabetic nephropathy [4] and diabetic dyslipidaemia [5] in experimental diabetes in the rat. (source). Neuroprotective and Antioxidant Effect of Ginkgo biloba Extract Against AD and Other Neurological Disorders. 2020;78(3):989-1010. doi: 10.3233/JAD-200896. already noted that benfotiamine was sparingly soluble in organic solvents such as benzene, chloroform and methanol, but was readily soluble in aqueous media at pH 8.0 [31]. I read we build up tolerance against sulbutiamine pretty fast, is it true? As mentioned above, the thiamine concentration in most commercial culture media is about 10 M, one or two orders of magnitude higher than the Km for the high affinity thiamine transport present in most cells [8,28,29]. Your blood-brain barrier (BBB) is a protective layer that lines the inner surfaces of the blood vessels inside your brain. Laboratory for Mitochondrial Biology and Metabolic Dysfunction in Neurodegeneration, Assistant Medical Director; Director, Neurorehabilitation. Other reports suggested that thiamine may protect against free-radical mediated neurotoxicity [6] and that it may have a cytoprotective effect on cultured neonatal rat cardiomyocytes under hypoxic insult [7]. FOIA Structures of the S-acyl derivative benfotiamine and the disulfide compounds allithiamine, fursultiamine and sulbutiamine. Efectividad de la suplementacin de cidos grasos omega-3 en pacientes con enfermedad de Alzheimer: revisin sistemtica con metaanlisis. Federal government websites often end in .gov or .mil. 2004 Sep;10(9):RA199-203. As treatment with benfotiamine did not yield elevated brain thiamine levels, we wanted to test whether this molecule is able to easily cross cell membranes in cultured cells. Taking regular Thiamine on the off days if cycling wont make a difference. 2019;14:1303-1317. This cycle breaks fatty acids, amino acids and monosaccharides into smaller molecules that produce adenosine triphosphate (ATP) energy within your mitochondria. Can TTFD also cross the blood brain barrier easily? And of course there were problems right from the start. It then enters the bloodstream as S-benzoylthiamine that is converted to thiamine in erythrocytes and in the liver. Gibson GE, Luchsinger JA, Cirio R, et al. 1Center for Cellular and Molecular Neurobiology, University of Lige, Avenue de l'Hpital, 1, 4000 Lige, Belgium, 2Laboratory of Pharmaceutical Technology, Department of Pharmacy, University of Lige, Avenue de l'Hpital, 1, 4000 Lige, Belgium. Both Benfotiamine (BF) and Lipothiamine (LP) are what is known as open ring forms of thiamine. Therefore, once the cells were nearly confluent, DMEM was replaced by a saline containing 10 M of either thiamine or benfotiamine. So to get its benefits you must get it from food, or take it as a supplement. Fig.1)1) [12] and O-isobutyrylthiamine disulfide ("sulbutiamine", Fig. One more thing about this miracle B-vitamin. National Institutes of Health, National Institute on Aging. The blood-brain barrier (BBB) is a semipermeable and extremely selective system in the central nervous system of most vertebrates, that separates blood from the brain's extracellular fluid. Bitsch R, Wolf M, Moller J, Heuzeroth L, Gruneklee D. Bioavailability assessment of the lipophilic benfotiamine as compared to a water-soluble thiamin derivative. Advanced glycation end products (AGEs), which are toxic protein modifications indicative of altered glucose metabolism and aging, typically increase in the brains of Alzheimers patients, but benfotiamine treatment significantly reduced this increase. A small sample size limited this trial. It is generally assumed that the symptoms arise from decreased activity of thiamine diphosphate (ThDP) dependent enzymes such as transketolase and pyruvate and oxoglutarate dehydrogenases, with subsequent impairment of carbohydrate metabolism in the brain. These lipophilic disulfides are often referred to as "allithiamines", in our opinion an improper denomination as they are synthetic molecules not present in Allium species and do not possess any allyl group. And provide the building blocks of the molecules needed to produce brain cells. No safe or effective dosage recommendations have been established for benfotiamine as a treatment for any condition. If you're looking for better brain health, balanced blood sugar, and a memory boost then look no further than benfotiamine! I hope that thiamine will work more as a tonic, ie, something that builds up the body to the point where digestion will function normally without betaine. The data were analyzed by MANOVA (Wilk's Lambda, p = 0.0002, 0.0145 and 0.27 for blood, liver and brain respectively) followed by ANOVA for each thiamine compound (*, p < 0.05; **, p < 0.01). How does Vitamin B1 (Thiamine) work in the Brain? doi:10.1016/B978-0-323-35868-2.00013-X, Allowitz KV, Yoo JJ, Taylor JR, Baloch OA, Harames K, Ramana KV. Whilst different studies show that administration of benfotiamine leads to higher thiamine blood levels than administration of water-soluble thiamine [10,24-27], practically no information is available concerning its effects on the brain. It is known that free thiamine is transported across plasma membranes by high affinity carriers [8], but the rate of transport is generally slow. Creatine Supplementation and Brain Health. When the dishes were nearly confluent (5 10 mg of protein/dish), the culture medium was replaced by 10 ml of saline (145 mM NaCl, 5 mM KCl, 1 mM MgCl2, 1 mM CaCl2, 10 mM glucose, 10 mM Hepes-Tris, pH 7.3) containing either 10 M benfotiamine or 10 M thiamine. Tetrahydrofurfuryl disulfide (TTFD) (Fursultiamine): TTFD is a disulfide derivative of thiamine developed in Japan for treating Beriberi. This clinical trial was supported by the National Institutes of Health (NIH) and the Alzheimers Drug Discovery Foundation. Most clinical studies use thiamine doses from 300 up to 1800 mg per day. Careers, Unable to load your collection due to an error. And contributes to the production of the enzyme pyruvate dehydrogenase (PDH) which is essential in making the neurotransmitter acetylcholine. It has nothing to do with sulfur. Salem, Benfotiamine does not easily cross into the brain. (Fig.2).2). Yikes! Shindo H, Okamoto K, Tohtsu J, Takahashi I. We propose that benfotiamine only penetrates the cells after dephosphorylation by intestinal alkaline phosphatases. In the present work, we show that after oral administration of benfotiamine to mice, free thiamine appears in the liver at a fast rate, reaching a maximum after one hour, while in the blood the maximum is reached only after two hours (Fig. The antitrypanosomal drug melarsoprol competitively inhibits thiamin uptake in mouse neuroblastoma cells. Which form of thiamine is best to take if you have chronic hep c. Vanessa, I cannot make a recommendation specifically for Hepatitis. Concerning fursultiamine, it is not clear whether it has specific effects on brain function [12] but it exerts a positive inotropic effect in heart muscle [15-17]. Schmid U, Stopper H, Heidland A, Schupp N. Benfotiamine exhibits direct antioxidative capacity and prevents induction of DNA damage in vitro. A new thiamine derivative, S-benzoylthiamine O-monophosphate. The facilitative glucose transporter, GLUT1, is expressed on endothelial cells at the blood-brain barrier, and is responsible for glucose entry into the brain. The vascular blood-brain barrier is a highly regulated interface between the blood and brain. Front Public Health. Her work is regularly featured in media such as First For Women, Woman's World, and Natural Health. Medline Plus Medical Encyclopedia nlm.nih.gov/medlineplus Retrieved April 7, 2016 (source), [iii] Martin P.R., Singleton C.K., Hiller-Sturmhofel S. The Role of Thiamine Deficiency in Alcoholic Brain Disease National Institute on Alcohol Abuse and Alcoholism nih.gov Retrieved April 7, 2016 (source), [iv] Singleton C.K., Martin P.R. https://www.ayurtimes.com/liv-52-benefits-uses-dosage-side-effects/ When using thiamine, is it necessary to also use a b-complex supplement (so that there is no depletion of certain vitamins)? Thanks. Lipid-soluble thiamine precursors have a much higher bioavailability than genuine thiamine and therefore are more suitable for therapeutic purposes. Its a synthetic form of thiamine naturally occurring in garlic. Bettendorff L. The compartmentation of phosphorylated thiamine derivatives in cultured neuroblastoma cells. Advanced neurohackers add Sulbutiamine to their stack instead of standard Vitamin B1 (thiamine) because its better absorbed and used by your brain than B1. Thiamine deficiency decreases cerebral glucose utilization which results in mitochondrial damage. Youll feel more awake and alert. MLV and SS performed most of the experimental part of the work. In erythrocytes, it was shown that fursultiamine, a lipophilic disulfide, is rapidly incorporated into the cells while benfotiamine is not [41]. Drug Alcohol Depend. Other studies in clinical populations have used doses ranging from 200600 mg/day [7; 10; 11]. Benfotiamine, a therapeutic drug that raises blood vitamin B1, levels very high, was recently tested as a pilot clinical study conducted by the Gibson Lab at the Burke Neurological Institute. Thiamine occurs in your body as free thiamine and as various phosphorylated forms: thiamine monophosphate (TMP), thiamine triphosphate (TTP), and thiamine pyrophosphate (TPP), which is also known as thiamine diphosphate. Schreeb KH, Freudenthaler S, Vormfelde SV, Gundert-Remy U, Gleiter CH. Thiamine deficiency disorders: diagnosis, prevalence, and a roadmap for global control programs. If you eat certain raw, fresh-water fish, raw shellfish and ferns you are at a greater risk of thiamine deficiency. Likely because this nootropic helps boost the activity of acetylcholine, GABA and glutamate in the brain. We therefore propose that most of the S-benzoylthiamine present in the mesenteric blood is captured by the liver and transformed into thiamine. But because its more bioavailable its more effective than thiamine. Shindo H, Okamoto K, Wada T, Koike H, Kumakura S. Studies on the absorption of S-benzoylthiamine O-monophosphate: (III) Mechanism of the intestinal absorption. The Japanese population were severely thiamine-deficient from this rice-only diet. In the blood, thiamine levels rapidly increased, reaching a maximum after 120 min and slowly decreasing thereafter (Fig. I havent tried it yet, its just arrived. These effects have not been reported with thiamine. Published 2021 May 21. doi:10.3390/ijms22115418. Benfotiamine (S-benzoylthiamine O-monophosphate) is a synthetic S-acyl derivative of thiamine. Is it safe to supplement b1 without taking other b vitamins at the same time? I have researched this a bit more and have read that benfotiamine does not cross the blood brain barrier. However, the benfotiamine concentrations used were 50 100 M, much higher than in our study. "High blood levels of thiamine can be achieved rapidly with oral thiamine hydrochloride. But Ive come across study after study, and reports on forums, where lab tests showed thiamine and thiamine pyrophosphate within range. So you must get it from food including beef, brewers yeast, legumes (beans, lentils), milk, nuts, oats, oranges, pork, rice, seeds, wheat, whole-grain cereals, and yeast. It is two B1 molecules chemically bonded together. Mouse neuroblastoma cells (Neuro 2a) were grown as previously described in 100 mm Petri dishes containing 10 ml Dulbecco's modified Eagle's medium (DMEM, N.V. Invitrogen SA, Merelbeke, Belgium), supplemented with 10% fetal calf serum [29]. Gary E Gibson, Jos A Luchsinger, Rosanna Cirio, Huanlian Chen, Jessica Franchino-Elder, Joseph A Hirsch, Lucien Bettendorff, Zhengming Chen, Sarah Flowers, Linda Gerber, Thomas Grandville, Nicole Schupf, Hui Xu, Yaakov Stern, Christian Habeck, Barry Jordan, Pasquale Fonzetti. Published 2022 Feb 3. doi:10.1136/bmjopen-2021-057142, Manzardo AM, Pendleton T, Poje A, Penick EC, Butler MG. Change in psychiatric symptomatology after benfotiamine treatment in males is related to lifetime alcoholism severity. Without the side effects youd get from stimulants like caffeine. Sources of Benfotiamine & What to Look For, The 6 Best Supplements for Depression, According to a Dietitian, Human immunodeficiency virus (HIV) or AIDS, Therapeutic potential of benfotiamine and its molecular targets. Its a synthetic form of thiamine naturally occurring in garlic.[xii]. Sulbutiamine is a synthetic version of Vitamin B1 (Thiamine). (Fig.6).6). Cathy Wong is a nutritionist and wellness expert. High-dose thiamine therapy was started. I use a variety of supplements to support my liver because I am chelating toxic metals. If you want to try benfotiamine supplements, talk to your healthcare provider. This experiment confirms that thiamine enters Neuro 2a cells more rapidly than benfotiamine. Babaei-Jadidi R, Karachalias N, Ahmed N, Battah S, Thornalley PJ. Hi. I am really curious to find out. Shinozaki H. Cardiac action of thiamine derivatives in guinea pig atria. Here's the latest evidence supporting these claims. Sulbutiamine: Sulbutiamine is my preferred form of Vitamin B1 (Thiamine) for cognitive enhancement. And experienced improvement in their symptoms at a dose of 1500 mg. None of the patients experienced side effects.[viii]. And can ultimately (and very rapidly) lead to coma and death.[ii]. Benfotiamine can boost thiamine levels and help prevent these effects. Official dosages aren't yet established. Babaei-Jadidi R, Karachalias N, Kupich C, Ahmed N, Thornalley PJ. Thanks for trying to answer my question, but Im still puzzled why the small amount of thiamine in unpolished rice was able to prevent beriberi in the first place. It may have been possible to maintain adequate levels of thiamine to prevent problems by using whole food back then. 2016;32(6):591-596. doi:10.1007/s12264-016-0067-0. https://www.distacart.com/en-au/products/himalaya-liv-52-ds?variant=14281879584813, i want to use b1 for my silent acid reflux, i knew it help with autonomic nervous system and managing the stomach acid. https://pubchem.ncbi.nlm.nih.gov/compound/Benfotiamine. Thiamine taken as a supplement does not easily cross the blood-brain barrier according those Japanese scientists and could not cure Beriberi. Thanks! Prescription medications furosemide (Lasix) and fluorouracil (Adrucil) lower the levels of thiamin in the body, so those medicines might also make benfotiamine less effective. Results are pending, but more research is needed before conclusions can be drawn. Vitamin B1 (Thiamine) Improves Symptoms of Fibromyalgia, Vitamin B1 (Thiamine) for Chronic Fatigue, Vitamin B1 (Thiamine) and Hashimotos Thyroiditis, https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5613172/, https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7210561/, https://www.frontiersin.org/articles/10.3389/fnut.2016.00016/full, https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2435522/, https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1225099/, https://www.ayurtimes.com/liv-52-benefits-uses-dosage-side-effects/, https://www.distacart.com/en-au/products/himalaya-liv-52-ds?variant=14281879584813, https://nootropicsexpert.com/sulbutiamine/#sulbutiamine-side-effects, https://pubmed.ncbi.nlm.nih.gov/32987117/, https://www.ncbi.nlm.nih.gov/labs/pmc/articles/PMC6073388/, Thiamine also contributes to the production of the enzyme, Patient 1: 3% reduction in fatigue; 80% reduction in pain, Patient 2: 37% reduction in fatigue; 50% reduction in pain, Patient 3: 7% reduction in fatigue; 60% reduction in pain, Alcoholic liver disease and withdrawal 100 mg injections of thiamine hydrochloride, Thiamine deficiency due to nutrition 100 mg injections, Wernicke-Korsakoff Syndrome 5 200 mg injections. I am glad you interpreted those 2 links, its a bit difficult for me. But more thiamine is needed in your brain than anywhere else in your body. official website and that any information you provide is encrypted Thiamine hydrochloride (HCl): Most Vitamin B1 (Thiamine) supplements available from online retailers and vitamin shops come as Thiamine hydrochloride (HCl). Sorry I dont see an option to edit my reply. This article reviews the current evidence about benfotiamine's effectiveness. You need to use it every day to make sure there is enough in your system to repel the mosquitos. [1] Dosage is up to 900 mg per day. Two small clinical trials suggest that benfotiamine treatment slows cognitive decline in people with mild cognitive impairment or mild Alzheimers disease, but they need to be confirmed by larger, long-term studies. In contrast to the above-mentioned derivatives it is not a disulfide but an S-acyl derivative.
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