We all understand the struggle of maintaining a truly healthy lifestyle. The unfortunate yet familiar results of eating too much or too poorly, coupled with lack of exercise and sometimes genetic predisposition often result in metabolic diseases such as diabetes, obesity, fatty liver disease, and atherosclerosis -- an illness where the arteries get clogged up with fat -- which can lead to heart disease or even heart attack.
According to a survey done by Council for Responsible Nutrition, 76 percent of adults in the U.S take dietary supplements as a way to boost and maintain their health in order to avoid these and other conditions (1).
However, in spite of numerous products on the market, people concerned about their metabolic condition (e.g. high cholesterol, high sugar, overweight) are seemingly at a loss, as most agents (shown in the graphic) that are sold for metabolic improvement are not effective and may even cause side effects.
But there is one particular compound found in nature that has attracted attention of scientific community due to its powerful metabolic effects, and it was never
commercially available to the general public – until now.
This compound is called betulin (from Latin Betula – birch, that derives from Sanskrit bhrajate - to shine; bright, white). It is one of the major components of the bark of birch tree, and in fact, is responsible for the tree’s characteristic white color (6). For centuries, people around the world have been using the bark, sap and leaves of the birch tree for their antimicrobial and anti-inflammatory properties.
That is until 2011, when a seminal article from the highly rated scientific journal Cell Metabolism uncovered incredible metabolic effects of betulin.
Background facts:
Our metabolism is a complicated network of interconnected biochemical reactions used by our cells to harness energy, store it and use it to maintain vital functions. You can think of it as a street map in a big city with constantly moving traffic.
Keeping metabolism in balance requires coordinated interplay of multiple key regulators — often proteins — that act like “traffic controllers”.
One aspect of metabolism is the breakdown and production of fat, and a critical “traffic controller” for this process is a protein called SREBP (for Sterol Regulatory Element-Binding Protein).
When SREBP is turned “on” or “off”, it will cause lipid (fat) levels to go up or down which will translate into multiple downstream effects on the entire body.
The Study:
Scientists found that when SREBP is acted on by betulin, it is “turned off,” leading to reduction of the amount of fatty molecules (lipids, triglycerides and cholesterol) in the cell. Even more intriguingly, they discovered that cells treated with betulin had a higher sensitivity to insulin, meaning they were able to more effectively take up sugar from the bloodstream for use as an energy source.
The scientists went further and conducted an experiment on three groups of mice that were put on a high fat, aptly called westernized, diet for six weeks. Each group was treated with either lovastatin, betulin, or placebo (control).
The findings (7):
- Mice treated with Betulin:
- Had reduced levels of cholesterol, triglycerides and fatty acids.
- Diminished rate of atherosclerotic plaque formation (harmful build ups of fat in the arteries).
- Decreased fat and weight gain,
- Decreased resting blood sugar level.
Amazingly, in all these tests betulin performed equally well or better compared to lovastatin, the first US FDA approved medicine in a family of drugs called statins that are prescribed to over 35 million people in the USA alone for high cholesterol and prevention/treatment of heart disease (8, 9).
What does this mean?
According to one of the most credible, top-rated scientific journals called Nature, it means that betulin “may offer advantages over existing therapeutic strategies” for prevention and treatment of metabolic symptoms — often partly caused by a common diet in the USA that is high in saturated fat — such as obesity, heart disease, non-alcoholic fatty liver disease, and diabetes/prediabetes. Type II Diabetes expert and M.D, Dr. Anupam Ghose, predicts that “[betulin] might replace statin drugs, while reducing the need for oral anti-diabetic drugs or insulin” (10)
Many additional studies in animal models have confirmed betulin’s and betulinic acid’s (another compound from birch bark) potential for specific conditions that affect an astounding number of people and bring billions of dollars to the pharmaceutical industry each year.
Safety:
Betulin belongs to the class of natural compounds called triterpenes which are found in a great variety of fruits, vegetables and medicinal plants and are therefore part of the human diet.
It has a long history of medicinal use, as several cultures all around the world have used the bark and sap of the birch tree in teas and other concoctions for kidney and bladder health, and for their anti-inflammatory and antimicrobial properties (19, 20). Betulinic acid is also present in a historically widely consumed mushroom called chaga, which grows on birch trees (21)
But the most stringent evaluation of betulin’s safety came from animal studies that specifically addressed its potential toxicity by administering increasing amounts, at doses up to 16 g/kg, of the pure compound into mice (23). Even at the highest dose studied - which is 10,000 times higher than what is provided in a single BETULEX™ capsule – scientists were unable to detect any signs of toxicity externally or in any internal organs (22, 23). These data places betulin squarely into the safest, “non-toxic” class according to any international scale of toxicity of chemical agents (24). Special study of betulin at the genetic level determined no mutagenic effects of the compound (25).
In some countries, betulin has been approved for use in food industry, specifically as a natural preservative in meat products to prolong shelf life (26, 27, 28). Overall, it can be confidently concluded that betulin is a safe compound.
What this means for you:
Based on over 2,000 articles published since 1900 (28), whether you’re looking to maintain your healthy lifestyle as you age or trying to minimize the risk of developing metabolic symptoms, betulin can benefit you. It’s unique profile of being a safe natural compound that has specific biological activity, rivaled only by expensive pharmaceutical drugs, puts it on the very top of the list of truly active supplements.
References:
1. “Dietary Supplement Usage Increases, Says New Survey.” Dietary Supplement Usage Increases, Says New Survey | Council for Responsible Nutrition, 19 Oct. 2017, www.crnusa.org/newsroom/dietary-supplement-usage-increases-says-new-survey.
2. “Office of Dietary Supplements - Selenium.” NIH Office of Dietary Supplements, U.S. Department of Health and Human Services, 11 Mar. 2020, ods.od.nih.gov/factsheets/Selenium-HealthProfessional/.
3. “Office of Dietary Supplements - Chromium.” NIH Office of Dietary Supplements, U.S. Department of Health and Human Services, 1 Oct. 2020, ods.od.nih.gov/factsheets/Chromium-HealthProfessional/.
4. “Cinnamon.” National Center for Complementary and Integrative Health, U.S. Department of Health and Human Services, May 2020, www.nccih.nih.gov/health/cinnamon.
5. Pekala, Jolanta, et al. “L-Carnitine - Metabolic Functions and Meaning in Humans Life.” Current Drug Metabolism, vol. 12, no. 7, 2011, pp. 667–678, https://doi.org/10.2174/138920011796504536
6. Green, Brian, et al. “Isolation of Betulin and Rearrangement to Allobetulin. A Biomimetic Natural Product Synthesis.” Journal of Chemical Education, vol. 84, no. 12, 2007, pp. 1895–2031, https://doi.org/10.1021/ed084p1985
7. Tang, Jing-jie, et al. “Inhibition of SREBP by a Small Molecule, Betulin, Improves Hyperlipidemia and Insulin Resistance and Reduces Atherosclerotic Plaques.” Cell Metabolism, vol. 13, no. 1, 2011, pp. 44–56, https://doi.org/10.1016/j.cmet.2010.12.004
8. “Lovastatin: MedlinePlus Drug Information.” MedlinePlus, U.S. National Library of Medicine, 15 Dec. 2017, medlineplus.gov/druginfo/meds/a688006.html.
9. Salami, Joseph A, and Haider Warraich. “National Trends in Statin Use and Expenditures in the US Adult Population From 2002 to 2013: Insights From the Medical Expenditure Panel Survey.” JAMA Cardiology, vol. 2, no. 1, 1 Jan. 2017, pp. 56–65, https://doi.org/10.1001/jamacardio.2016.4700
10. Ghose, Anupam. 1 Aug. 2019, www.anupamghose.com/type-2-diabetes-is-betulin-from-birch-bark-a-future-treatment-for-type-2-diabetes/.
11. Hai, Yan Quan, et al. “Betulinic Acid Alleviates Non-Alcoholic Fatty Liver by Inhibiting SREBP1 Activity via the AMPK–MTOR–SREBP Signaling Pathway.” Biochemical Pharmacology, vol. 85, no. 9, 2013, https://doi.org/10.1016/j.bcp.2013.02.007
12. “Nonalcoholic Fatty Liver Disease.” American Liver Foundation, 11 June 2020, liverfoundation.org/for-patients/about-the-liver/diseases-of-the-liver/non-alcoholic-fatty-liver-disease/.
13. “Non-Alcoholic Fatty Liver Disease (NAFLD) - Hunterdon Gastroenterology Associates: Digestive Health Specialists - Flemington, NJ.” Hunterdon Gastroenterology Associates | Digestive Health Specialists - Flemington, NJ, 25 Sept. 2018, hunterdongastro.com/non-alcoholic-fatty-liver-disease-nafld/.
14. K.D, Kim, et al. “Betulinic Acid Inhibits High-Fat Diet-Induced Obesity and Improves Energy Balance by Activating AMPK.” Nutrition, Metabolism and Cardiovascular Diseases, vol. 29, no. 4, 2019, pp. 409–420, https://doi.org/10.1016/j.numecd.2018.12.001
15. “Study Finds Obesity Itself Raises Risk of Diabetes and Cardiovascular Disease.” Health Essentials from Cleveland Clinic, Health Essentials from Cleveland Clinic, 9 Oct. 2020, health.clevelandclinic.org/study-finds-obesity-itself-raises-risk-of-diabetes-and-cardiovascular-disease/.
16. “Type 2 Diabetes.” Centers for Disease Control and Prevention, Centers for Disease Control and Prevention, 30 May 2019, www.cdc.gov/diabetes/basics/type2.html.
17. Kim, Soo Jung, et al. “Beneficial Effect of Betulinic Acid on Hyperglycemia via Suppression of Hepatic Glucose Production.” Journal of Agricultural and Food Chemistry, vol. 62, no. 2, 2014, pp. 434–442. https://doi.org/10.1021/jf4030739
18. “How Diabetes Affects Your Vision.” Versant Health, 3 Mar. 2020, versanthealth.com/blog/how-diabetes-affects-your-vision/.
19. Rastogi, Subha et al. “Medicinal plants of the genus Betula--traditional uses and a phytochemical-pharmacological review.” Journal of ethnopharmacology vol. 159 (2015): 62-83. https://doi.org/10.1016/j.jep.2014.11.010
20. Dadakova, Eva & Vrchotová, Naděžda & Triska, Jan. (2010). “Content of selected biologically active compounds in tea infusions of widely used European medicinal plants.” Journal of AGROBIOLOGY J Agrobiol. 27. 27-34. https://doi.org/10.2478/s10146-009-0003-2
21. Géry, Antoine et al. “Chaga ( Inonotus obliquus), a Future Potential Medicinal Fungus in Oncology? A Chemical Study and a Comparison of the Cytotoxicity Against Human Lung Adenocarcinoma Cells (A549) and Human Bronchial Epithelial Cells (BEAS-2B).” Integrative cancer therapies vol. 17,3 (2018): 832-843. https://doi.org/10.1177/1534735418757912
22. Jäger, Sebastian et al. “A preliminary pharmacokinetic study of betulin, the main pentacyclic triterpene from extract of outer bark of birch (Betulae alba cortex).” Molecules (Basel, Switzerland) vol. 13,12 3224-35. 18 Dec. 2008, doi:10.3390/molecules13123224
23. Makarova, MN, et al. “Evaluation of acute toxicity of betulin.” Planta Medica, vol. 77, no.12, 2011. 4. https://doi.org/10.3390/molecules13123224
24. Berezovskaya, I.V. Classification of Substances with Respect to Acute Toxicity for Parenteral Administration. Pharmaceutical Chemistry Journal 37, 139–141 (2003). https://doi.org/10.1023/A:1024586630954
25. Yoshida, Edson Hideaki et al. “Evaluation of Betulin Mutagenicity by Salmonella/Microsome Test.” Advanced pharmaceutical bulletin vol. 6,3 (2016): 443-447. https://doi.org/10.15171/apb.2016.057
26. Ilyina, A., et al. “Effect of Betulin-containing Extract from Birch Tree Bark on α-Amylase Activity In vitro and on Weight Gain of Broiler Chickens In vivo.” Plant Foods Human Nutrition, vol. 69, 2014 https://doi.org/10.1007/s11130-014-0404-2
27. Jiang, Jiang, and Youling L Xiong. “Natural antioxidants as food and feed additives to promote health benefits and quality of meat products: A review.” Meat science vol. 120 (2016): 107-117. https://doi.org/10.1016/j.meatsci.2016.04.005
28. Amiri, Shayan, et al. “Betulin and Its Derivatives as Novel Compounds with Different Pharmacological Effects .” Biotechnology Advances , vol. 38, 2020. https://doi.org/10.1016/j.biotechadv.2019.06.008
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