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Berberine and its Role in Lowering Cholesterol

Writer's picture: Sharad JaiswalSharad Jaiswal

Berberine

  • Berberine has been utilized for an exceptionally long time in traditional medicine, especially in Chinese and Ayurveda.

  • Due to its potential therapeutic benefits for many diseases, including cancer, cardiovascular problems, metabolic syndrome, and diabetes, berberine has lately attracted a lot of attention. In this article, we will examine the biology of berberine and go over some of its health advantages.

  • Berberine's many complex biological characteristics have been the focus of in-depth study. Antibacterial, anti-inflammatory, antioxidant, and anti-cancer effects of berberine have been demonstrated.

  • One of its primary modes of action is the capacity of berberine to interact with a range of molecular targets, including receptors, signaling pathways, and enzymes, leading to a variety of pharmacological effects [1].

  • Adenosine monophosphate-activated protein kinase, a crucial enzyme involved in cellular energy management, is activated by berberine and has been found to enhance insulin sensitivity and glucose metabolism.

  • Berberine stimulates insulin signaling, lowers hepatic glucose synthesis, raises skeletal muscle glucose absorption, and improves glycemic control by activating AMPK.

  • Additionally, it has been demonstrated that berberine has lipid-lowering properties. It reduces the production of triglycerides and cholesterol by inhibiting the enzyme acetyl-CoA carboxylase, which is crucial for the synthesis of fatty acids. [2].

Hypercholesterolemia

  • Hypercholesterolemia is a disorder that can result from an excessively high blood cholesterol level. The biology of hypercholesterolemia, including its origins, physical consequences, and risk factors for people, will be examined in this essay.

  • A disorder known as hypercholesterolemia is characterized by unusually high cholesterol levels in the blood. Lipoproteins, which are molecules made of proteins and lipids, carry cholesterol in the blood. Low-density lipoprotein (LDL) and high-density lipoprotein are the two basic forms of lipoproteins. (HDL) [3].

  • Both inherited and acquired hypercholesterolemia exist. A hereditary condition called familial hypercholesterolemia is handed down over generations. It is brought on by abnormalities in genes that control blood levels of LDL cholesterol, such as the LDL receptor gene.

  • Elevated levels of LDL cholesterol are the result of poor LDL cholesterol removal from circulation. On the other side, acquired hypercholesterolemia is not inherited and is typically brought on by lifestyle factors such as poor diet, inactivity, smoking, and binge drinking.

  • Several reasons might cause hypercholesterolemia. A history of ailments in the family is one of the most important risk factors. A person’s chance of acquiring familial hypercholesterolemia is raised if they have a close relative with the disorder, such as a parent or sibling.

  • A diet heavy in saturated and trans fats, inactivity, smoking, binge drinking, obesity, and certain medical disorders like diabetes, hypothyroidism, and renal disease is additional risk factors.

  • Hypercholesterolemia can have substantial and protracted repercussions on the body. LDL cholesterol buildup in artery walls can cause atherosclerosis, a significant risk factor for cardiovascular conditions [4].

How does Berberine Regulates Cholesterol Levels?

  • It has been demonstrated that the natural substance berberine HCl, which is present in several plants including goldenseal, Oregon grape, and barberry, has cholesterol-lowering properties. There are numerous ways that berberine HCl lowers cholesterol levels, some of them are as follows:

  • Berberine HCl has been found to inhibit HMG-CoA reductase, an enzyme that is essential to produce cholesterol in the liver. Berberine HCl lowers blood cholesterol levels by blocking this enzyme, which lowers the liver's production of cholesterol [5].

  • Enhancing LDL receptor expression: It has been demonstrated that the liver cell-specific expression of LDL (low-density lipoprotein) receptors can be increased by berberine HCl.

  • By attaching to LDL cholesterol, sometimes known as "bad" cholesterol, and encouraging its uptake into liver cells for additional processing and elimination, LDL receptors oversee eliminating it from the bloodstream. Lower cholesterol levels are the result of enhanced LDL receptor expression since it increases the removal of LDL cholesterol from the bloodstream.

  • Modulating lipid metabolism: Berberine HCl has been found to influence lipid metabolism by controlling many lipids metabolism-related genes and enzymes. The accumulation of triglycerides and LDL cholesterol in the liver and circulation can be decreased by increasing the activity of enzymes that support fatty acid oxidation.

  • Gut microbiota modulation: Berberine HCl has been demonstrated to affect the billions of bacteria that live in the human digestive tract. According to certain research, berberine HCl can enhance the diversity and composition of the gut microbiota, which will enhance lipid metabolism and lower cholesterol levels [6].

  • Inhibiting pro-inflammatory signaling pathways in the body has been proven to have anti-inflammatory benefits for berberine HCl.

  • Atherosclerosis, a disorder marked by the accumulation of cholesterol-rich plaques in arteries, is a condition whose development is influenced by inflammation. By lowering inflammation, berberine HCl may help prevent or slow the development of atherosclerosis.

  • While berberine HCl has shown promise in lowering cholesterol levels, it is crucial to remember that its effectiveness and safety depend on the individual and other factors and that it should only be used under the supervision of a trained healthcare practitioner.

  • Low blood cholesterol levels, or hypocholesterolemia, can harm one's general health. A particular kind of fat called cholesterol is necessary for the health of the body's cells.

  • It is essential for the synthesis of hormones, food digestion, and the development of cell membranes. However, excessive levels of cholesterol, particularly LDL cholesterol, which is sometimes referred to as "bad" cholesterol, can cause plaques to form in the arteries, raising the risk of cardiovascular disorders including heart attacks and strokes.

  • So general health must maintain ideal cholesterol levels. In recent years, berberine, a natural substance obtained from several plants, has drawn interest due to its application in the treatment of hypocholesterolemia.

  • According to studies, berberine may help lower LDL cholesterol levels, which would enhance the lipid profile overall and lower the risk of cardiovascular illnesses.

  • Berberine lowers cholesterol by reducing the activity of an enzyme known as PCSK9, which is one of the ways it does so. By encouraging the liver's LDL receptors to degrade, PCSK9 is an essential regulator of blood levels of LDL cholesterol.

  • By attaching LDL cholesterol and aiding its absorption into the liver for processing and excretion, LDL receptors oversee eliminating it from circulation.

  • By boosting LDL receptor expression and LDL cholesterol clearance from the blood, berberine decreases levels of LDL cholesterol. By suppressing PCSK9, this is made possible [7].

  • Berberine influences PCSK9 in addition to regulating the expression of genes related to lipid metabolism.

  • By stifling the activity of diacylglycerol acyltransferase (DGAT), an essential enzyme in the synthesis of triglycerides, berberine also lowers the production of triglycerides in the liver [8].

Pre-Clinical and Clinical Trial Data

  • In recent years, berberine, a naturally occurring substance present in several plants, has drawn much interest due to its health advantages, including its impact on hypocholesterolemia, or excessive cholesterol levels.

  • Most of the treatment for hypocholesterolemia has been a class of medications called statins, which are frequently used to reduce cholesterol levels. Alternative forms of treatment are required since certain people may not tolerate or experience negative effects from statins.

  • Because of its antibacterial, anti-inflammatory, and hypoglycemic qualities, berberine has long been utilized in Chinese and Ayurvedic medicine. It can be derived from a variety of plants, including Berberis aristata, Berberis vulgaris, and Coptis chinensis. Recent studies have concentrated on its potential to reduce cholesterol [9].

  • There were 2,010 participants in 23 RCTs that were included in the study. The findings demonstrated that, in comparison to a placebo, berberine dramatically decreased levels of triglycerides, LDL cholesterol, and total cholesterol while significantly raising levels of high-density lipoprotein cholesterol.

  • Comparable results from a different meta-analysis suggested that berberine can successfully lower LDL cholesterol levels [10].

  • Berberine has been shown to have additional positive benefits in hypocholesterolemia in addition to its effects on lipid levels.

  • Human trials have also revealed information on the safety of berberine. The safety of berberine in humans was assessed in a comprehensive study and RCTs meta-analysis, 2,472 people from 27 RCTs were included in the analysis.

  • The findings demonstrated that berberine had a low frequency of negative events and was well tolerated. However, berberine may have adverse effects, just like any medicine, so it is vital to speak with a doctor before beginning any new treatment plan [11].


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