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What Do We Know About Berberine? http://healingherbalsnewzealand.com/berberine-containing-herbs/ Antibiotic, Antiviral, Antifungal, Antiparasitic: Berberine has high bacteriostatic activity against Staphylococcus (including MRSA), Streptococcus, Neisseria meningitidis, E coli, Klebsiella, Pseudomonas, Proteus, cholera, Shigella, Salmonella, and tuberculosis (TB). It also exhibits antiviral activity against Influenza A (including ‘Swine Flu’), and antifungal activity against Aspergillus, Candida, and Cryptococcus. It has antiprotozoan activity against Entamoeba and Giardia. Diabetes: Clinical reports have shown that Berberine is safe and effective in treating both Type 2 Diabetes, and its complications. Used on its own, Berberine has been shown to reduce fasting blood glucose by 21-36%, which is comparable to the effects of the drug metformin. When used in combination with glucose-lowering drugs such as metformin or glicazide/glipazide, Berberine has an additive effect. Such reductions in blood glucose appear to be due to increased glucose uptake, reduced liver glucose production, and protective and regenerative effects on pancreatic Beta cells (the cells which secrete insulin). Berberine has been found to have a very good safety profile, even in patients in whom glucose-reducing drugs may be contraindicated. Research in animals has shown that Berberine may be effective in preventing the cardiovascular complications of diabetes, diabetic nephropathy (‘kidney disease’), and diabetic neuropathy (‘nerve’ damage). Berberine has also been reported to have the potential to protect brain tissue from hypoglycaemic events. Nerves: Berberine has been found to have nerve growth factor (NGF) activity, and may therefore assist in nerve repair. It also significantly increases nerve conduction velocity in animal models of diabetic neuropathy (‘nerve’ damage). Berberine appears to have both central and peripheral actions that may account for its protective and pain-relieving effects in animal models of nerve damage and nerve pain. Diarrhea, Irritable Bowel Syndrome, Inflammatory Bowel Disease: Studies in humans have shown that Berberine reduces smooth muscle contraction and intestinal motility, and delays intestinal transit time. Coupled with Berberine’s activity against a wide range of gastro-intestinal pathogens (see ‘Antibiotic’, above), this makes it potentially a very effective treatment for diarrhea of any cause. Cholesterol: With a mechanism that differs from that of statin drugs, Berberine has been shown to reduce total cholesterol levels by 13-31%, LDL cholesterol by 10-25% (‘bad’ cholesterol), triglyceride concentrations by 20-35%, and to elevate HDL cholesterol (‘good’ cholesterol). Unlike statin drugs, Berberine has no adverse effects on liver or muscle tissue. Liver: Berberine reduces liver fat content in animals with nonalcoholic fatty liver disease. It also prevents proliferation of the cells that are central to the development of fibrosis (a bad thing!) during liver injury. Pancreas: Given that Berberine has been shown to protect the pancreas from oxidative stress, and that it has broad-spectrum antibacterial activity, it may have a role in the treatment of pancreatitis. Gallbladder: Berberine has long been known to stimulate bile secretion; it therefore may be useful in the prevention of gallstones, but should never be used in cases of known or suspected gallstones or biliary obstruction. Congestive Heart Failure: In two randomised clinical trials in patients with chronic Congestive Heart Failure, Berberine was added to patients’ established conventional drug regimes. The Berberine treated group showed significant greater increases in left-ventricular-ejection-fraction, exercise capacity, shortness of breath, and fatigue compared with the control group. Additionally, the group treated with Berberine had decreased rates of ventricular premature beats and long-term mortality. Berberine has been shown to possess positive ionotropic, antiarrhythmic, and vasodilatory properties, all of which means, simply put, that it helps the heart to do its job more efficiently. Cardiovascular Antiarrhythmic: In a study of arrhythmic patients treated with Berberine for 1-4 weeks, there was an 89% percent reduction in ventricular premature beats in 62% of patients, and a 50% reduction in the remainder. Berberine has been found to prolong the duration of the ventricular action potential. Clotting: Berberine has anti-platelet activity (as do the drugs aspirin and clopidogrel), decreasing the release of ADP from platelets thus preventing platelet activation and clot formation. Hypertension: In animal models, Berberine has been shown to act on both the endothelium and underlying vascular smooth muscle to induce vasorelaxation, via multiple cellular mechanisms. Berberine has also been described as having competitive alpha-1 adrenoreceptor-blocking activity, similar to that of the anti-hypertensive drug prazosin. Benign Prostatic Hypertrophy: Alpha-1 adrenoreceptor-blocking drugs are conventional first-line treatments for Benign Prostatic Hypertrophy. Berberine has been described as having competitive alpha-1 adrenoreceptor-blocking activity, similar to that of the drug prazosin. Cancer: In randomised clinical trials of patients undergoing radiation therapy, Berberine has been shown to significantly decrease the incidence of radiation-induced acute intestinal symptoms, and radiationinduced lung injury (both early and late). In vitro, Berberine has been shown to inhibit cell proliferation in various human cancer cell lines, inducing apoptosis, arresting angiogenic processes, inhibiting the diffusion of metastases, and overcoming multi-drug resistance. Apoptotic effect has been shown in brain, nasopharyngeal, oral, lung, breast, liver, colorectal, prostate, bone, epidermoid, lymphoma, and leukaemic cancer cells. Depression, Anxiety, Bipolar Affective Disorder, Schizophrenia: In animal models of depression, Berberine has been shown to have an anti-depressant effects, potentially through modulation of noradrenaline, serotonin and dopamine levels in the brain. Berberine is also reported to have an inhibitory effect on monamine oxidase enzymes (particularly MAO-A), much like some currently available prescription drugs. It also exerts a significant anti-anxiety effect, potentially through activation of 5-HT receptors in the brain. The type of modulatory activity that Berberine has on dopamine receptors also suggest that it may additionally be useful in the treatment of Bipolar Disorder and Schizophrenia. Alzheimer’s Disease: Berberine has been shown to modulate amyloid precursor protein processing in the brain, decreasing Beta Amyloid accumulation, and therefore limiting any of the associated neurotoxicity which has long been associated with Alzheimer’s disease. Berberine is also an excellant central, reversible, acetylcholinesterase inhibitor. These findings suggest that Berberine has exciting potential in the treatment of Alzheimer’s disease. Stroke: In animal models, Berberine has been reported to protect brain tissue against ischaemic, hypoxic, and hypoglycaemic injury. In models of stroke, it has been reported to increase cerebral vasodilation (and therefore blood flow), decrease platelet aggregation, inhibit delayed neuronal death, and ameliorate changes in learning and memory. Epilepsy: Berberine has been found to have protective effects against neuronal injury due to the neurotoxicity of excitatory amino acids, such as glutamate. This may also lend itself to a protective effect on the brain in the recurrent seizures of epilepsy. Anti-inflammatory, Immunosuppressant: Berberine has been shown to reduce the gene expression of pro-inflammatory cytokines including TNF-alpha (TNF-alpha inhibiting drugs are commonly used in Rheumatoid Arthritis), interleukins (IL-6), prostaglandins (PEG2), COX-2 (similarly to NSAID drugs such as Voltaren and ibuprofen), and iNOS. Countering Weight-Gain Related To Antipsychotics: In animal studies, Berberine counters the weightgain associated with the drugs clozapine and risperidone. Labour: Berberine is a well-known uterine stimulant. It should be avoided during pregnancy, but much like the hormone oxytocin, it can be used to strengthen and regulate contractions during labour and delivery, and to reduce the risk of postpartum haemorrhage. My Experiences While normally I have a preference for using whole herbs over isolated phytochemical constituents (due to the potential for the combination of phytochemicals in a plant to provide synergistic effects), the fact remains that all of the plant sources of Berberine described below are significantly more expensive (or alternatively, hard-to-come-by) than commercially-available purified Berberine. Given that this is the case, and the fact that research has shown purified Berberine to be very effective and remarkably safe, I (the author of this article) tend to prescribe the pure product. Oral Berberine has no known toxicity; the gastro-intestinal tract appears to limit excessive absorption (although, what we know about Berberine absorption does seem to be continually debated and frequently revised). High doses of Berberine taken acutely, due to a poor intestinal uptake rate, may cause gastro-intestinal cramping and diarrhea. All Berberine-containing herbs should be avoided during pregnancy because they may cause premature uterine contractions. Briefly, the most common plant sources of Berberine are: Goldenseal: Hydrastis canadensis Barberry: Berberis vulgaris Oregon Grape: Mahonia aquifolium Coptis: Coptis chinensis Yerba Mansa: Anemopsis californica