/ Contact
Articles on
and Healing
Videos about
& Prevention

From Wikipedia, the free encyclopedia

CAS number 633-66-9
PubChem 2353
ChemSpider 2263

Molecular formula C20H18NO4+
Molar mass 336.36122 g/mol
Except where noted otherwise, data are given for materials in their standard state (at 25 °C, 100 kPa)

Berberine is a quaternary ammonium salt from the group of isoquinoline alkaloids. It is found in such plants as Berberis, goldenseal (Hydrastis canadensis), and Coptis chinensis, usually in the roots, rhizomes, stems, and bark. Berberine is strongly yellow colored, which is why in earlier times berberis species were used to dye wool, leather and wood. Wool is still today dyed with berberine in Northern India. Under ultraviolet light, berberine shows a strong yellow fluorescence.[1] Because of this it is used in histology for staining heparin in mast cells.[2]  

* 1 Traditional use
* 2 Biosynthesis
* 3 Diabetes, dyslipidemias and cardiovascular conditions
* 4 Cancer
* 5 Mental health
* 6 Intestinal disorders
* 7 HIV

1) Traditional use

As a traditional medicine or dietary supplement, berberine has showed some activity against fungal infections, Candida albicans, yeast, parasites, and bacterial/viral infections.[3][4] Berberine seems to exert synergistic effects with fluconazole even in drug-resistant Candida albicans infections.[5] Some research has been undertaken into possible use against MRSA infection.[6]

Berberine is considered an ineffective antibiotic. However, when applied in vitro and in combination with methoxyhydnocarpin, an inhibitor of multidrug resistance pumps, berberine inhibits growth of Staphylococcus aureus.[7]

Berberine is a component of some eye drop formulations. There is some evidence that it is useful in the treatment of trachoma,[8] and it has been a standard treatment for leishmaniasis.[9] Berberine prevents and suppresses proinflammatory cytokines, E-selectin,[10] and genes, and increases adiponectin expression[11] which partly explains its versatile health effects. Berberine is a nucleic acid-binding isoquinolone alkaloid with wide potential therapeutic properties.[12]

2) Biosynthesis

Biosynthesis of Berberine

The alkaloid berberine has a tetracyclic skeleton that is derived from a benzyltetrahydroisoquinoline system with the incorporation of an extra carbon atom provided by S-Adenosyl methionine (SAM) via an N-methyl group. Formation of the berberine bridge is readily rationalized as an oxidative process in which the N-methyl group is oxidized to an iminium ion, and a cyclization to the aromatic ring occurs by virtue of the phenolic group.[13]

It is known that the immediate precursor of protoberberine alkaloids in plants is (S)-reticuline.[14] Berberine is an alkaloid derived from tyrosine. L-DOPA and 4-hydroxypyruvic acid both come from L-Tyr. Although two tyrosine molecules are used in the biosynthetic pathway, only the phenylethylamine fragment of the tetrahydroisoquinoline ring system is formed via DOPA, the remaining carbon atoms come from tyrosine via 4-hydroxyphenylacetaldehyde. L-DOPA loses carbon dioxide to form dopamine 1. Likewise, 4-hydroxypyruvic acid also loses carbon dioxide to form 4-hydroxyphenyl-acetaldehyde 2. Dopamine 1 then reacts with 4-hydroxy-phenylacetaldehyde 2 to form (S)-norcolaurine 3 in a reaction similar to the Mannich reaction. After oxidation and methylation by SAM, (S)-reticuline 4 is formed. (S)-reticuline serves as a pivotal intermediate to other alkaloids. Oxidation of the tertiary amine then occurs and an iminium ion is formed 5. In a Mannich-like reaction the ortho position to the phenol is nucleophilic, and electrons are pushed to form 6. Product 6 then undergoes keto-enol tautomerism to form (S)-scoulerine which is then methylated by SAM to form (S)-tetrahydrocolumbamine 7. Product 7 is then oxidized to form the methylenedioxy ring from the ortho-methoxyphenol, via an O2-, NADPH- and cytochrome P-450-dependent enzyme. giving (S)-canadine 8. (S)-canadine is then oxidized to give the quaternary isoquinolinium system of berberine. This happens in two separate oxidation steps, both requiring molecular oxygen, with H2O2 and H2O produced in the successive processes.[15]

3) Diabetes, dyslipidemias and cardiovascular conditions

During the last few decades, many studies have shown that berberine has various beneficial effects on the cardiovascular system and significant anti-inflammatory activities.[16] A Canadian report suggests that berberine can effectively reduce intracellular superoxide levels in LPS-stimulated macrophages. Such a restoration of cellular redox by berberine is mediated by its selective inhibition of gp91phox expression and enhancement of SOD activity.[17] Berberine exerts up-regulating activity on both low-density-lipoprotein receptor (LDLR) and insulin receptor (InsR). This one-drug-multiple-target characteristic might be suitable for the treatment of metabolic syndrome.[18][19] Berberine has been tested and used successfully in experimental[20][21] and human diabetes mellitus.[22][23][24][25] Berberine has been shown to lower elevated blood glucose as effectively as metformin.[26] The mechanisms of action include activation of PPAR-gamma [27], inhibition of aldose reductase,[28] inducing glycolysis,[29] preventing insulin resistance[30] through increasing insulin receptor expression[23] and acting like incretins.[31] A new study suggest that berberine may overcome insulin resistance via modulating key molecules in insulin signaling pathway, leading to increased glucose uptake in insulin resistant cells.[32] Berberine inhibits Foxo1,[33] which integrates insulin signaling with mitochondrial function. Inhibition of Foxo1 can improve hepatic metabolism during insulin resistance and the metabolic syndrome.[34] Berberine might exert its insulinotropic effect in isolated rat islets by up-regulating the expression of hepatocyte nuclear factor 4 alpha, which probably acts solely or together with other HNFs to modulate glucokinase activity, rendering β cell more sensitive to glucose fluctuation and response more effectively to glucose challenge.[35] Berberine seems to inhibit human dipeptidyl peptidase-4 (DPP IV) as well as the pro-diabetic target human protein tyrosine phosphatase 1B (h-PTP 1B), which explain at least some of its anti-hyperglycemic activities.[36] Berberine suppresses intestinal disaccharidases with beneficial metabolic effects in diabetic states.[37] A recent comprehensive metabonomics method, applied to 60 type 2 diabetics, suggests that administration of berberine down-regulates the high level of free fatty acids which are known to be toxic to the pancreas and cause insulin resistance. These results suggest that berberine might play a pivotal role in the treatment of type 2 diabetes, conclude the authors.[22]

Berberine has been shown to boost the effects of metformin and 2,4-thiazolodinedione (THZ) and can partly replace the commercial drugs, which could lead to a reduction in toxicity and side effects of the latter.[38]

Berberine lowers elevated blood total cholesterol, LDL cholesterol, triglycerides and aterogenic apolipoproteins (apo B) (Apo B),[39] but the mechanism of action is distinct from statins.[40][41][42] Berberine reduces LDL cholesterol by upregulating LDLR mRNA expression posttranscriptionally while downregulating the transcription of proprotein convertase subtilisin/kexin type 9 (PCSK9), a natural inhibitor of LDL receptor (LDLR), [43] and increasing in the liver the expression of LDL receptors through extracellular signal-regulated kinase (ERK) signaling pathway,[44] while statins inhibit cholesterol synthesis in the liver by blocking HMG-CoA-reduktase. This explains why berberine does not cause side effects typical to statins. Berberine and plant stanols synergistically inhibit cholesterol absorption in hamsters.[45] Berberin seems to improve the arterial endothelial function in humans.[24][46] Berberine activates AMP-activated protein kinase (AMPK),[47] specifically extracellular signal-regulated kinases (ERK),[48] which plays a central role in glucose and lipid metabolism,[49][50] suppresses proinflammatory cystokines,[51] and reduces MMP-9 and EMMPRIN expression,[52] which are all beneficial changes for heart health. Morevover, berberine reduces hepatic fat content in the rats of non-alcoholic fatty liver disease (NAFLD).[53] Berberine also prevents proliferation of hepatic stellate cells (HSCs), which are central for the development of fibrosis during liver injury.[33]

Experimental[54][55][56] and clinical studies[57][58] suggest that berberine may be useful for patients with severe congestive heart failure.

According to a Chinese report, combined use of berberine with ciclosporin A (CsA) could markedly increase the blood concentration of CsA in heart transplanted recipients and reduce the dosage of CsA required, save the cost for medical service, and shows no obvious adverse reaction.[59]

4) Cancer

Berberine has drawn extensive attention towards its antineoplastic effects.[60][61] It seems to suppress the growth of a wide variety of tumor cells including breast cancer,[62] leukemia, melanoma,[63] epidermoid carcinoma, hepatoma, pancreatic cancer[64], oral carcinoma, tongue carcinoma,[65] glioblastoma, prostate carcinoma, gastric carcinoma.[66][67] Animal studies have shown that berberine can suppress chemical-induced carcinogenesis, clastogenesis [68], tumor promotion, tumor invasion,[69][70][71][72][73] prostate cancer,[74][75][76][77] neuroblastoma,[78][79] and leukemia.[46][80] It is a radiosensitzer of tumor cells but not of normal cells. 

How berberine mediates these effects is not fully understood, but its ability to inhibit angiogenesis and to modulate Mcl-1, Bcl-xL, cyclooxygenase (COX)-2, MDR, tumor necrosis factor (TNF)- and IL-6 , iNOS, IL-12, intercellular adhesion molecule-1 and ELAM-1 expression, MCP-1 and CINC-1, cyclin D1,[81] activator protein (AP-1), HIF-1 , PPAR- , and topoisomerase II has been shown. By using yeast mutants, berberine was found to bind and inhibit stress-induced mitogen-activated protein kinase kinase activation. Because apoptotic, carcinogenic, and inflammatory effects and various gene products (such as TNF-α, IL-6, COX-2, adhesion molecules, cyclin D1, and MDR) modulated by berberine are regulated by the transcription factor nuclear factor- B (NF- B), it is postulated that this pathway plays a major role in the action of berberine.[82] 

Berberine suppressed NF-κB activation induced by various inflammatory agents and carcinogens. This alkaloid also suppressed constitutive NF-κB activation found in certain tumor cells. It seems to protect against side effects of radiation therapy in lung cancer.[83] Berberine, 300 mg three times a day orally, also seems to inhibit complication of abdominal or pelvic radiation, called radiation-induced acute intestinal symptoms (RIAISs).[84] The studies suggest that its use in clinical development may be more as a cytostatic agent than a cytotoxic compound.

5) Mental health

Berberine seems to act as an herbal antidepressant and a neuroprotector against neurodegenerative disorders.[85][86][87][88] Berberine inhibits prolyl oligopeptidase (POP) in a dose-dependent manner. Berberine is also known to bind to sigma receptors like many synthetic antidepressant drugs. As berberine is a natural compound that has been safely administered to humans, preliminary results suggest the initiation of clinical trials in patients with depression, bipolar affective disorder, schizophrenia, or related diseases in which cognitive capabilities are affected, with either the extract or pure berberine. New experimental results suggest that berberine may have a potential of inhibition and prevention of Alzheimer's disease (AD) mainly through both cholinesterase (ChEs)inhibitory and β-amyloids pathways,[89][90] and additionally through antioxidant capacities.[91]

Berberine, an active constituent of bloodroot, is showing promise in fighting brain tumors and many other cancers.

6) Intestinal disorders

Berberine can ameliorate pro-inflammatory cytokines induced intestinal epithelia tight junction damage in vitro, and berberine may be one of the targeted therapeutic agents that can restore barrier function in intestinal disease states.[92]
[edit] HIV

A new study identified a key cellular mechanism underlying the protective effect of berberine on HIV PI-induced inflammatory response in macrophages. Modulation of the Endoplasmic reticulum(ER) stress response represents a potential therapeutic target for various inflammatory diseases and metabolic syndrome including HIV PI-associated atherosclerosis. The report shows the potential application of berberine as a complementary therapeutic agent for HIV infection.[93]

Related articles....

Articles about Temu Lawak Temulawak rhizome contains xanthorrhizol, germakren, allo-aromadendren, tricyclin, and isofurogermakren. Curcumoid and xanthorrizol are the most active component.

39 Surprising Benefits Of Ginger For Skin And Health Ginger is considered the ‘chest of medicine’ in Ayurveda due to its various health benefits. Its powerful therapeutic and preventive effects make it usable in the treatment of various ailments.

Galangal. Galangal is a generic name that often describes several varieties of the ginger root families Zingiberaceae, haling from Southeast Asia, all of which grow in Indonesia. Most forms of ginger posses anti-cancer qualities, to varying degrees and qualifications.

Alkaloids. Alkaloids have significant therapeutic value and form the ingredients of many important medicines. The alkaloids also comprise strong vegetable toxics and sedatives. Substances like caffeine and theobromine that are closely associated with natural purine (substance that can be converted to uric acid in the body) compounds are normally categorized as alkaloids.

Turmeric, Curcumin Naturally Block Cancer Cells. Curcumin has previously been found to reduce tumors by 81%, which also gives credence to the natural anti-cancer benefits of turmeric and curcumin intake.

Blood Root used in BSI Compounds. Some of the more important alkaloids present in bloodroot include sanguinarine, chelerythrine, and protopine have been isolated from roots and rhizomes of Sanguinaria canadensis. Berberine is also an important alkaloid present in bloodroot.

Bereberine Alkaloid in BSI Medicines. Berberine suppresses the growth of a wide variety of tumor cells including breast cancer, leukemia, melanoma, epidermoid carcinoma, hepatoma, pancreatic cancer, oral carcinoma, tongue carcinoma, glioblastoma, prostate carcinoma, gastric carcinoma. Animal studies have shown that berberine can suppress chemical-induced carcinogenesis, clastogenesis, tumor promotion, tumor invasion, prostate cancer, neuroblastoma, and leukemia. It is a radiosensitzer of tumor cells but not of normal cells.

Sanguinarine. If applied to the skin, sanguinarine kills cells and can destroy (diseased) tissue. In turn, the bleeding wound may produce a scab, called an Eschar. For this reason, sanguinarine is termed an escharotic.

Master Index of Health-Related Articles on BSI.International

It's not just about killing cancer....

But also about ending the causes of cancer
so it is no longer needed by the body.
The body expels disease when properly nourished.

Alternative web sites often are lost, are made illegal in the current political climate.

Because of the intrinsic value of this information for the reader, we at BSI, in addition to providing a link to the reference, also reprint it here for safe keeping. We kindly invite the author to contact us.

It appears obvious in many cancer-related publications, the author may be leery of liability. As such one must often read-between-the-lines, to understand what is revealed there. 

"Everything is backwards; everything is upside down. Doctors destroy health, lawyers destroy justice, universities destroy knowledge, governments destroy freedom, and the major media destroy information." ~ Michael Ellner

"Anti-dandruf shampoos cause dandruf and scalp disorders. Weight loss foods and drugs cause weight gain. Prescription drugs cause disease. Health insurance destroys health. Television and advertising kill individuality and inspiration." ~ I Wayan Nyepih




A few of the 60+ natural medicines we manufacture at BSI....

Traditional Bloodroot Salve
Compound A
Blood Root Jahe Yellow Powder
Compound B
Blood Root Jahe Magnesium
Yellow Salve

Compound BVC
Goldenseal Comfrey Aloe
Healing Salve

Compound C
Blood Root Jahe Salve
Compound D
Bromelain Papain Powder
Compound G
Jintan Hitam Beet Powder
Compound J
Cancer Killer
Compound K
Manggis Sirsap Powder
Compound L
Colloidal Minerals
Compound M
Noni Mint Powder
Compound NP
Poison Control
Compound S
Digestive Toner and Cleanse
Compound VL
Lung and Sinus Steamer Solution
Compound B Tincture
DMSO Vit C Bloodroot Bicarbonate Magnesium Iodine Jahe
Compound 1-5
Bone & Ligament Rebuilder
Compound O
Oral Parasite Medicine
Compound W
Lung & Sinus Tonic
Compound TL
Jamu BSI

Compound Z

Infusion Enhancement

Compound IZ
Nigella Sativa
Infusion Enhancement

Compound IN
Healing Eye Drops
Vitamin C - Silver - Magnesium - Electrolyte Healing for eyes

Compound ED
Tumor Direct Injection
Compound A-20
Vitamin C and Electrolytes Infusion
Compound IAA
Silver Hydrosol
Infusion Enhancement and Tumor Injection

Compound IS
Lemon Bath and Body Oil
Compound SO
Vita Bath
Healing Bath Salts

Compound V
Trace Elements Body Detox and Skin Purifier
Natural Insect Repellant
Bug Juice
Oral Healing Oils
Compound SOS
Trace Elements Face & Scalp Healing Conditioner
Oral Healing Kit
Oral Kit
Body Detox
and Healing Kit

Body Kit

Sorry, the medicines we make are sold only to our patients.