Topic: Berberine benefits and a caution (drug interaction)
Marnie
Frequent Contributor (5K+ posts)
Member # 773
posted
Berberine numerous benefits and a warning (regarding use in conjunction with other Rx�s due to liver enzymes involved)
First what is it?
The berberine alkaloid can be found in the roots, rhizomes, stem, and bark of the plants. Berberine-containing plants are used medicinally in many traditional medical systems, including Ayurvedic herbal and Chinese herbal medicine..
Alkaloids are a group of naturally occurring chemical compounds that contain mostly basic nitrogen atoms.
How might Berberine be helpful to us?
1. MS (experimental autoimmune encephalomyelitis is the way to mimic MS in mice):
Regulation of Th1 and Th17 Cell Differentiation and Amelioration of Experimental Autoimmune Encephalomyelitis by Natural Product Compound Berberine
We found that as soon as we injected the material from the human brain, the rat became forgetful. It didn�t remember a task that we had taught it to remember, and in that experiment,
after a few hours, the a-beta cleared out of the rat brain and the rat was back to normal.
*** dnalc.org � unable to post link to lymenet
Don�t we all have fleeting moments of forgetfulness � especially as we age?
The liver produces amyloid beta too! In the intestine, it binds with ApoB.
And what is beta amyloid, anyway? Turns out this pesky accumulating plaque protein actually seems to help the brain use pyruvate as fuel in lieu of glucose.
Why the heck would that happen? ApoE can signal the brain to change from glucose as a primary fuel to fats (ketone bodies) and pyruvate.
It is postulated this switch is caused when the brain is under microbial attack.
In this theory, amyloid beta is not a cause of Alzheimer's, but rather a defense against it. (5) .
More evidence for this theory comes from a case study that MCT oil seemed to be protective or reverse symptoms of Alzheimers (6).
There is also a theory that Alzheimer's patients suffer from a poor ability to use glucose as fuel in the brain, so that a change to a ketogenic metabolism is exceptionally helpful (7).
Unable to link on lymenet...evolutionarypsychiatry.blogspot.com
ApoE forms a *stable complex* with amyloid β (Aβ) peptides
in vitro
and that the state of apoE lipidation influences the fate of brain Aβ, i.e.,
5. Alleviates fatty liver caused by high fat diet (in rats).
Berberine reduces methylation of the MTTP (Microsomal triglyceride transfer protein promoter and alleviates fatty liver induced by a high-fat diet in rats.
Causes of a fatty liver: alcoholism, metabolic abnormalities, excess body weight, insulin resistance, high triglycerides in the blood, many drugs, aspirin, corticosteroids, tamoxifen, tetracycline, pregnancy, toxins, viruses.
***Merckmanuals.com � unable to post link to lymenet
Elevated plasma homocysteine concentrations as a predictor of steatohepatitis in patients with non-alcoholic fatty liver disease.
The plasma homocysteine concentrations were significantly higher in patients with non-alcoholic fatty liver disease, while the concentrations were not affected by chronic viral hepatitis.
Plasma homocysteine is a parameter for discriminating steatohepatitis from simple steatosis. Determining the plasma homocysteine concentrations may facilitate selection of steatosis patients in whom a liver biopsy should be performed.
BBR (berberine) also downregulated several hepatic proinflammatory genes, including TNF-α, IL-6, and ***serum amyloid A3*** (SAA3; Fig. 4D), which have been proposed to play a role in the development of steatohepatitis (12).
GW9662 (PPARgamma antagonist) aggravated LPS-induced (and reversed BBR-attenuated) COX-2 expression. The findings showed that BBR ameliorated COX-2 overexpression partially via modulation of p38 and PPARγ pathways during acute endotoxemia.
PPAR-γ2 (mostly found in adipose tissue and the intestine). PPARG regulates fatty acid storage and glucose metabolism. The genes activated by PPARG stimulate lipid uptake and adipogenesis (= preadipocytes become adipocytes) by fat cells.
The enzyme Cyclooxygenase-2 (COX-2) is abundantly expressed in colon cancer cells and plays a key role in colon tumorigenesis. We found that berberine�.effectively inhibits COX-2 transcriptional acitivty in colon cancer cells in a dose and time dependent manner�.The present findings may further explain the mechanism of anti-inflammatory and anti-tumor promoting effects of berberine.
8. Has some anti-bacterial and anti-fungal and anti-viral effects. It is considered an antibiotic and inhibits the growth of Staphyloccus aureus, Microcystis aerigompsa. A toxic cyanobacterium.
Protective Effects of Berberine in an Experimental Rat Osteoarthritis Model
In *IL-1β-induced* rat articular chondrocytes,
berberine decreased IL-1β-induced GAG (glycosaminoglycan) release and NO production.
Meanwhile, high-dose berberine exhibited an anticatabolic effect in an IL-1β-induced rat osteoarthritis (OA) model. These findings suggest that berberine may play a protective role in the development of OA and may be useful in the treatment of OA.
Glycosaminoglycans (GAG) - This family of carbohydrates is essential or important for life. Some examples of glycosaminoglycan uses in nature include heparin as an anticoagulant, hyaluronan as a component in the synovial fluid lubricant in body joints, and chondroitins, which can be found in connective tissues, cartilage and tendons.
Members of the glycosaminoglycan family vary in the type of hexosamine, hexose or hexuronic acid unit they contain (e.g. glucuronic acid, iduronic acid, galactose, galactosamine and glucosamine.
11. May act as an anti-depressant and impacts several neurotransmitters (in mouse test). Taken together, theses findings demonstrate that berberine exerted antidepressant-like effect in various behavioural paradigms of despair possibly by modulating brain biogenic amines (norepinephrine, serotonin and dopamine).
Further, nitric oxide pathway and/or sigma receptors are involved in mediating its antidepressant-like activity in mouse forced swim test.
12. May be heart protective (raisanberine is a derivative of berberine)
Conclusion: Raisanberine relieved hypoxic/oxidant insults to the pulmonary artery and cardiac myocytes of rats by suppressing activated NADPH oxidase and increased calcium influx.
13. Use in conjunction with Rx for treatment of lung cancer
As potential adjuvants to chemotherapy for non-small cell lung cancer, COP and BER increase ROS production, reduce MDR, and enhance the inhibitory effects of chemotherapeutic agents on A549 cell growth.
Coptis extract (COP), a Chinese medicinal herb, and its major constituent, berberine (BER), have anticancer properties.
14. Potential anti-inflammatory use to protect the heart
Berberine ameliorates inflammation in patients with acute coronary syndrome following percutaneous coronary intervention. (May lower LDL and triglycerides without impacting HDL.)
In the berberine-treated group, matrix metalloproteinase (MMP)-9, intercellular adhesion molecule (ICAM)-1, vascular cell adhesion molecule (VCAM)-1, C-reactive protein, interleukin-6 and monocyte chemoattractant protein-1 were significantly reduced relative to baseline values.
Sixty-one patients were treated with berberine (300 mg, t.i.d., for 30 days)
�revealed that berberine-induced cytotoxicity in breast cancer cells involves dysregulation of protein folding, proteolysis, redox regulation, protein trafficking, cell signaling, electron transport, metabolism and centrosomal structure.
This study suggests that the anticancer effect of berberine on HeLa cells was a complex process based on affecting multiple protein expression and acting on an interaction network. Our work could be helpful to elucidate the mechanism of berberine's anticancer activity on HeLa cells. HSPA8 (heat shock protein) and annexin A5 might be the targets.
The results revealed that berberine significantly decreased fasting blood glucose, insulin levels, total cholesterol, triglyceride levels, urinary protein excretion, serum creatinine (Scr) and blood urea nitrogen (BUN) in diabetic rats.
The histological examinations revealed amelioration of diabetes-induced glomerular pathological changes following treatment with berberine.
In addition, the protein expressions of nephrin and podocin were significantly increased. It seems likely that in rats berberine exerts an ameliorative effect on renal damage in diabetes induced by high-fat diet and streptozotocin.
The possible mechanisms for the renoprotective effects of berberine may be related to inhibition of glycosylation and improvement of antioxidation that in turn upregulate the expressions of renal nephrin and podocin.
These results suggest that berberine improves insulin sensitivity by inhibiting fat store and adjusting adipokine profile in human preadipocytes and metabolic syndrome patients.
Metabolic syndrome = increased blood pressure, a high blood sugar level, excess body fat around the waist or abnormal cholesterol levels � that occur together, increasing your risk of heart disease, stroke and diabetes.
20. One form of berberine maybe protective in Parkinson�s Disease
Collectively, the blockade of neuronal K(ATP) channels by THB in SNc DA neurons is a novel pharmacological mechanism of THB, which may contribute to its neuroprotective effects in PD.
In enzymology tetrahydroberberine oxidase is an enzyme that catalyzes the follow chemical reaction. (S)-tetrahydroberberine + 2 O2 <-> berberine + 2 H2O2
Sandyk, R. And Pardeshi, R. (1990) Pyridoxine Improves Drug-Induced Parkinsonism And Psychosis In A Schizophrenic Patient. Int. J. Neurosci. 52, 225-232
21. May protect from endothelial dysfunction
Berberine prevents hyperglycemia-induced endothelial injury and enhances vasodilatation via adenosine monophosphate-activated protein kinase and endothelial nitric oxide synthase.
Berberine concentration dependently enhanced phosphorylation of endothelial nitric oxide synthase (eNOS) at Ser1177 and promoted the association of eNOS with heat shock protein 90 (HSP90), leading to an increased production of nitric oxide.
Furthermore, berberine attenuated high glucose-induced generation of reactive oxygen species, cellular apoptosis, nuclear factor-kB activation, and expression of adhesion molecules, thus suppressing monocyte attachment to endothelial cells.
In mouse aortic rings, berberine elicited endothelium-dependent vasodilatations and alleviated high glucose-mediated endothelial dysfunction.
All these beneficial effects of berberine on the endothelium were abolished by either pharmacological inhibition of adenosine monophosphate-activated protein kinase (AMPK) or adenovirus-mediated overexpression of a dominant negative version of AMPK.
�berberine works by targeting an ancient regulator of metabolism, the activated protein kinase (AMPK) enzyme.
AMPK regulates the uptake of glucose by your cells and the synthesis of glucose transporters�which help move glucose out of your blood and into your cells, where it belongs.
Berberine may also increase the number and activity of the insulin receptors on your cells, promoting insulin sensitivity.
On top of that, AMPK facilitates the burning of fatty acids in your cells, which is why it�s a powerful tool for helping keep blood lipid levels in check.
*** drwhitaker.com � unable to post link to lymenet
Repeating�berberine targets *activated* AMPK. One mechanism by which AMPK regulates lipid metabolism is phosphorylation and
inactivation of acetyl CoA carboxylase (ACC),
an important rate-controlling enzyme for the synthesis of malonyl-CoA.
ACC is both a critical precursor for biosynthesis of fatty acids and a potent inhibitor of long-chain fatty acyl-CoA transport to mitochondria for β-oxidation.
That is B6/PLP/P5P. (Which lowers homocysteine also.)
Chemical Inhibition of Acetyl-CoA Carboxylase Induces Growth Arrest and Cytotoxicity Selectively in Cancer Cells
ACC activity in cancer cells is essential for proliferation and survival.
Together, these findings indicate that cancer cells have become dependent on ACC activity to provide the cell with a sufficient supply of fatty acids to permit proliferation and survival, introducing the concept of using small-molecule ACC inhibitors as therapeutic agents for cancer.
PLP plays a role in the conversion of dopa into dopamine,allows the conversion of the excitatory neurotransmitter glutamate to the inhibitory neurotransmitter GABA, and allows SAM to be decarboxylated to form propylamine, which is a precursor to polyamines.
These results are consistent with previous studies that found that: (1) pyridoxal kinase had a very low activity in children with autism and (2) pyridoxal 5 phosphate (PLP) levels are unusually low in children with autism.
Thus, it appears that the low conversion of pyridoxal and pyridoxine to PLP results in low levels of PLP, which is the active cofactor for 113 known enzymatic reactions, including the formation of many key neurotransmitters.
CONCLUSIONS: Total vitamin B6 is abnormally high in autism, consistent with previous reports of an
impaired pyridoxal kinase
for the conversion of pyridoxine and pyridoxal to PLP.
Here it is proposed that lack of the vitamin B6 derivative pyridoxal 5'-phosphate might contribute to the appearance of pancreatic islet autoimmunity and type I diabetes onset.
In one study, fourteen women with gestational diabetes were given 100 mg of vitamin b6 each day for two weeks, which resulted in eliminating the diagnosis in twelve out of the fourteen women.
***naturalpedia.com � unable to post link to lymenet
I�m here to tell you�B6/PLP/P5P stops my son�s seizures which began at puberty. God�s truth.
But I suspect he has a MTHFR defect and may have a hard time converting folic acid -> L-methylfolate. When homocysteine levels go too high� B6,sublingual, to the rescue. Yes..
Even though seizures can be controlled with pyridoxal 5'-phosphate, neurological problems such as developmental delay and learning disorders may still occur. (Link above). Yup�he didn�t talk until age 2 and indeed had/has learning disabilities!
Even with that gene defect (MTHFR):
For example, carrying the 5,10-methylene-tetrahydrofolate reductase (MTHFR) thermal-labile variant has been shown to be a risk factor for colorectal adenomatous polyps, but
only in the context of low-folate, vitamin B12, and vitamin b6 intake.
Given that a goal of the field of nutrition is the prevention and treatment of disease, genetic markers may aid in this effort by identifying population subgroups at high risk of disease in the presence of particular dietary exposures.
***naturalpedia.com � unable to post link to lymenet
PLP and inflammation:
Vitamin B6 deficiency associated with inflammation
In order to make DHA and EPA, your body must have sufficient vitamin B6, vitamin B3, vitamin C, magnesium, and zinc.
*** naturalpedia.com � unable to post link to lymenet
DHA is structural, EPA is functional (anti-inflammatory).
Vitamin B6 serves as a coenzyme of approximately 100 enzymes that catalyse essential chemical reactions in the human body. It plays an important role in protein, carbohydrate and lipid metabolism.
Its major function is the production of serotonin from the amino acid trytophan in the brain and other neurotransmitters, and so it has a role in the regulation of mental processes and mood.
Furthermore, it is involved in the conversion of tryptophan to the vitamin niacin, the formation of haemoglobin and the growth of red blood cells, the absorption of vitamin B12, the production of prostaglandines and hydrochloric acid in the gastrointestinal tract, the sodium-potassium balance, and in histamine metabolism.
As part of the vitamin B-complex it may also be involved in the downregulation of the homocysteine blood level.
Vitamin B6 also plays a role in the improvement of the immune system.
All three forms of vitamin B6 (pyridoxine, pyridoxal and pyridoxamine) are readily absorbed in the small intestine by an energy dependent process.
All three are converted to pyridoxal phosphate in the liver, a process which requires zinc and riboflavin.
For large-scale population surveys there is another method of assessing a pyridoxine deficiency state: the tryptophan load test.
Vitamin B6 participates in the conversion of tryptophan to the vitamin niacin.
A pyridoxine deficiency blocks this process, producing more xanthurenic acid.
If the administration of tryptophan leads to an increased excretion of xanthurenic acid, a pyridoxine deficiency can be diagnosed.
(My daughter had hyperemesis gravidarum � serious and ongoing.
She was NOT given B6, but instead given $$$ Zofran. I took Bendectin = B6 + doxylamine succinate = Unisom sleep TABS + B6 when I was pregnant with her.)
Deficiencies in pyridoxal kinase result in reduced synthesis of PLP and are associated with seizure disorders related to a reduction in the synthesis of GABA.
Other symptoms that may appear with deficiency in vitamin B6 include nervousness, insomnia, skin eruptions, loss of muscular control, anemia, mouth disorders, muscular weakness, dermatitis, arm and leg cramps, loss of hair, slow learning, and
Great� methionine <-> homocysteine via folic acid (B9) and B12. Assuming those little creatures don�t have a problem converting folic acid to its usable form L-Methylfolate and have consumed adequate folic acid and B12 from their foods.
While mice are omnivores (they eat both plants and meat), grain comprises much of their normal diet. Not exactly like our fast food American diets!
For example, some depression patients have a genetic pyrrole disorder which renders them grossly depleted in vitamin B-6.
These individuals cannot efficiently create serotonin since B-6 is an important co-factor in the last step of its synthesis.
Personal note�son was tested�not that genetic disorder.
Okay�back to Berberine�
22. May act as a skin anti-aging substance and anti-oxidative
Berberine is a plant ingredient that has anti-inflammatory and anti-oxidative effects. Matrix metalloproteinase-9 (MMP-9) and interleukin-6 (IL-6) are known to be highly induced by ultraviolet (UV) light and may play important roles in UV-induced skin inflammation and the skin aging process.
In this study, we investigated the effects of berberine on MMP-9 and IL-6 expression in normal human keratinocytes (NHK).
Our results demonstrated that berberine dose-dependently inhibited basal and TPA-induced expression and activity of MMP-9, and also suppressed TPA-induced IL-6 expression.
Berberine prevented TPA-induced ERK activation and AP-1 DNA binding activity.
Therefore, berberine may be used as an effective ingredient for anti-skin aging products, which can prevent skin inflammation and the degradation of extracellular matrix proteins, including collagen, by MMPs.
Hubby took high doses of oregon grape root tincture (great source of berberine) for several years to prevent candida. It seemed to work, but then when we started using flagyl I stopped it due to using so many herbs with alcohol.
Bea Seibert
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Marnie
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Bea...did you catch the berberine - PLP/P5P action re: ACC?
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Carol in PA
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posted
I looked through all that, and it looks like berberine may be able to fix alot of the damage caused by the Lyme bacteria.
I think that many many medical problems are caused by systemic Lyme infection. Heart disease, high cholesterol, diabetes, pancreatitis, many forms of cancer. Arthritis, asthma, cataracts, autoimmune, osteoporosis, dementia.
We chase each of these as though it's its own entity, but I suspect that most of them are related to the effects of a systemic infection.
For example, my mother weighed nine pounds at birth. I believe her mother had gestational diabetes, which happens to some women when pregnant and causes the baby to gain weight. (The baby is exposed to higher blood sugar.) My grandmother later had arthritis, and then breast cancer, dying at age 60.
She grew up in southern Bavaria, a part of Germany where even today you can read about the problems with getting tick borne infections at local alpine resort areas.
Farther south of my grandmother's birthplace, the Ice Man was found in a glacier, 5300 years old. He had evidence of the Lyme bacteria in his cells, and had joint changes that showed arthritis.
He had changes in his heart and blood vessels that showed he had heart disease, which researchers now know is related to systemic inflammation, the immune system's response to an ongoing bodywide infection such as Lyme.
Mycoplasma infections, like Cpn, Chlamydia pneumonia, may also be to blame. They also live within our cells to survive, and are associated with chronic diseases.
[ 05-06-2012, 12:32 AM: Message edited by: Carol in PA ]
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ukcarry
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Funnily enough, I yesterday started a berberine supplement by Metagenics for suspected SIBO following food poisoning in March. Tha supplement is Candibactin-BR and it contains coptis, oregon grape, berberine, as well as smaller amounts of phellodendron,, Chinese skullcap, ginger, Chines licorice and Chinese rhubarb.
I am taking 2, 30 minutes before each meal [ie 6 per day]. It certainly leaves a strong, bitter taste!
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Carol in PA
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Featuring berberine hydrochloride and extracts of Oregon grape and coptis roots, the formula encourages a healthy intestinal environment and supports detoxification function of the liver and gallbladder.
All that berberine should do something good for you. I saw that Amazon.com carries it too. Let us know your results.
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ukcarry
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On Amazon, Metagenics products seem to be discontinued, so I got it from the above. It is pretty expensive, but there are decent amounts of the herb in it. If it works, it will be cheap at the price!
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posted
Anyone have heartburn or hypoglycemia aggravated by this suppliment?
I had to reduce my homeopathic drops of Berberine to once a day because of the acid reflux. I also started to get shakiness/trembling and joint cracking alot more while on this. I know it is used for diabetes to lower blood sugar and insulin resistance, so would this be contradicted for those with hypoglycemia?
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Keebler
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- amk33,
Sorry to hear of that experience.
True homeopathics drops should not cause heartburn as only one - 5 drops are absorbed under the tongue.
Still, even a tiny bit of alcohol can burn the throat and on down. Rather than the homeopathic drops, the PELLETS may be best.
Rather than a homeopathic, might this a tincture?
If so, that could be due to the alcohol content. You might try putting it in more water. Usually, it's best in at least 1/2 cup of water but you can use a cup, or two.
I do best avoiding tinctures unless it's an herb that only works in that form.
Berberine - from whatever source - is available in CAPSULES. Those would be best to avoid the alcohol tinctures.
It's important to know that not all sources of Berberine have the exact same effects. (Search the term in Tillotson's book for detail.)
DGL, a special kind of licorice, can soothe heartburn. See the chapter in that same book about licorice. DGL is explained there.
Many herbs can lower blood sugar, especially if taken on an empty stomach. However, if with a balanced formula of other herbs &/or with a meal, this can usually be managed.
You may need more complex carbs and good fats in your diet so that your food has better longevity. Protein with each meal and every snack will also help stabilize blood glucose.
You may also need to eat more often, every few hours, small amounts so that you can keep your blood sugar more stable.
Most herbs are not intended to be taken alone and usually work much better with others.
If you have a LLND nearby, it's best to have individualized consult. Some of the books here might also help explain how to work with herbs.
Tillotson's THE ONE EARTH HERBAL SOURCEBOOK is good. Just Google the title to find the sight and then read the chapter: The Language of Herbs
================================
It's best to consult with an ILADS-educated LL (lyme literate) doctor who has completed four years of post-graduate medical education in the field of herbal and nutritional medicine -
- and someone who is current with ILADS' research & presentations, past and present. -----------------------
Integrative / Holistic M.D., etc. (Be aware that those in this category can have various levels of formal herbal &/or nutritional education, perhaps even just a short course. Do ask first.)
Links to many articles and books by holistic-minded LL doctors of various degrees . . . .
BASIC HERBAL EDUCATIONAL & SAFETY links -
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Keebler
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- Marnie,
Thanks so much for all the fabulous links and your notes. -
Posts: 48021 | From Tree House | Registered: Jul 2007
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AuntyLynn
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Marnie - That is SOME exhaustive list of links! Thanks!
I know that All of the B Vitamins must be important for Lymies, as they are known as the "anti-stress" vitamins.
I learned about B6 controlling morning sickness from Adele Davis' books - her advice really helped a friend of mine who could only keep watermelon down during the first 5 months of her pregnancy.
Davis said 200 mg of B6 might be necessary to control nausea, once it has begun, but she also warned against allowing your blood sugar to get too low.
Again, thanks for all the great links - they deserve more study.
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Thanks, Keebler. I'm taking Energetics Homeopathics, Bacteria-Chord and Drainage Tone. These do not bother me at all. The Berberine (Core Berberine Blend) is by the same company, but, I guess you're right, it doesn't say homeopathic on the bottle. Rather, "Spagyric Botanical" (whatever that means).
It's definitely the Berberine causing the acid reflux. When I reduced the dose, it improved. I'm not sure if it is causing the increase in tingling/trembling and joint cracking. I have read that it reduces blood sugar for diabetics, but, I can find any info regarding it's effects on hypoglycemics.
I take these three products with Ivermectin to treat FL1953 (perscribed by doctor). While on this protocol, my CD57 has increase from below 100 (starting number 66) to 155, so it seems to be helping the lyme.
I am just worried that the Berberine may be affecting my blood sugar. I moved last year, and lost my blood sugar meter supplies, so I'm not sure if these symptoms are related to blood sugar spikes/drops or not. I do follow a hypoglycemia diet, and eat often throughout the day.
Who knows. I'll keep searching. I may just reduce the Berberine blend to every other day, and see what happens.
Posts: 418 | From NJ | Registered: Sep 2007
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sparkle7
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Spagyric means the plant is burned & the ash is turned into a remedy.
Berberine is good stuff. I have been taking one from Swanson Vitamins. It didn't cost alot. If it is combined with Diflucan, it's supposed to make it work better for drug resistant yeast.
It may be a good idea to take breaks from it every so often. It's a component of goldenseal. It's a good idea to take breaks from taking that herb & not take it all of the time. I'm not sure if the same would be true of berberine.
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Huh, I wonder why they use the ash in these remedies. Gotta look it up. Do you know why you should take breaks from Goldenseal?
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