Berberine, is an alkaloid from Hydrastis canadensis L., Chinese herb Huanglian, and many other plants. It is widely used in traditional Chinese medicine as an antimicrobial in the treatment of dysentery and infectious diarrhea. This manuscript describes cardiovascular effects of berberine and its derivatives, tetrahydroberberine and 8‐oxoberberine. Berberine has positive inotropic, negative chronotropic, antiarrhythmic, and vasodilator properties. Both derivatives of berberine have antiarrhythmic activity. Some of cardiovascular effects of berberine and its derivatives are attributed to the blockade of K+ channels (delayed rectifier and KATP) and stimulation of Na+‐Ca2+ exchanger. Berberine has been shown to prolong the duration of ventricular action potential. Its vasodilator activity has been attributed to multiple cellular mechanisms. The cardiovascular effects of berberine suggest its possible clinical usefulness in the treatment of arrhythmias and/or heart failure
Berberine, an alkaloid initially isolated from Chinese herbal medicine exhibited the ability to induce morphological changes and internucleosomal DNA fragmentation, characteristic of apoptosis in promyelocytic leukemia HL-60 cells. Cell cycle studies showed that only about 20% of the cells underwent apoptosis at the early time (6 h) of berberine (25 μg/ml) treatment; these appeared to be cells in S phase at the time of berberine treatment. At extended time (6–48 h), cells were cell cycle arrested, the number of cells of each phase, particularly the cells of S phase decreased and much more (> 50%) of the cells appeared with DNA content less than G1. Attempts were also made to isolate possible berberine-DNA complexes from cell cultures treated with berberine (25 μg/ml; 2–24 h). Shifts of absorption maxima of berberine in the direction of longer wavelengths were observed in the isolated berberine-DNA complexes. Palmatine, an analog of berberine, which was not able to induce apoptosis, also complexed with DNA in cells treated with palmatine (25 μg/ml; 2–24 h). Our results suggest that some important cellular processes other than the intracellular DNA-interacting action of berberine may be involved in the berberine-induced apoptosis in HL-60 cells
Type 2 diabetes vs Glucophage
Berberine has been shown to regulate glucose and lipid metabolism in vitro and in vivo. This pilot study was to determine the efficacy and safety of berberine in the treatment of type 2 diabetes mellitus patients. In study A, 36 adults with newly diagnosed type 2 diabetes mellitus were randomly assigned to treatment with berberine or metformin (0.5 g 3 times a day) in a 3-month trial. The hypoglycemic effect of berberine was similar to that of metformin. Significant decreases in hemoglobin A1c (from 9.5% ± 0.5% to 7.5% ± 0.4%, P < .01), fasting blood glucose (from 10.6 ± 0.9 mmol/L to 6.9 ± 0.5 mmol/L, P < .01), postprandial blood glucose (from 19.8 ± 1.7 to 11.1 ± 0.9 mmol/L, P < .01), and plasma triglycerides (from 1.13 ± 0.13 to 0.89 ± 0.03 mmol/L, P < .05) were observed in the berberine group. In study B, 48 adults with poorly controlled type 2 diabetes mellitus were treated supplemented with berberine in a 3-month trial. Berberine acted by lowering fasting blood glucose and postprandial blood glucose from 1 week to the end of the trial. Hemoglobin A1c decreased from 8.1% ± 0.2% to 7.3% ± 0.3% (P < .001). Fasting plasma insulin and homeostasis model assessment of insulin resistance index were reduced by 28.1% and 44.7% (P < .001), respectively. Total cholesterol and low-density lipoprotein cholesterol were decreased significantly as well. During the trial, 20 (34.5%) patients experienced transient gastrointestinal adverse effects. Functional liver or kidney damages were not observed for all patients. In conclusion, this pilot study indicates that berberine is a potent oral hypoglycemic agent with beneficial effects on lipid metabolism
Berberine, an isoquinoline alkaloid, has a wide range of pharmacological effects, including anti-inflammation, yet the exact mechanism is unknown. Because cyclooxygenase-2 (COX-2) plays a key role in prostaglandins (PGs) synthesis, which is elevated in inflammation, we examined whether the anti-inflammatory mechanism of berberine is mediated through COX-2 regulation. In oral cancer cell line OC2 and KB cells, a 12 h berberine treatment (1, 10, and 100 μM) reduced prostaglandin E2 (PGE2) production dose-dependently with or without 12-O-tetradecanoylphorbol-13-acetate (TPA, 10 nM) induction. This berberine induced effect occurred rapidly (3 h) as a result of reduced COX-2 protein, but not enzyme activity. The electrophoretic mobility shift assay revealed that activator protein 1 (AP-1) binding was decreased in oral cancer cells treated with berberine for 2 h. Further analysis showed that berberine inhibited AP-1 binding directly. These anti-inflammatory effects paralleled to the in vivo results where berberine pretreatment of Wistar rat inhibited the production of exudates and PGE2 in carrageenan induced air pouch.
Berberine is a novel cholesterol-lowering drug working through a unique mechanism distinct from statins
Weijia Kong, Jing Wei, Parveen Abidi, Meihong Lin, Satoru Inaba, Cong Li, Yanling Wang, Zizheng Wang, Shuyi Si, Huaining Pan, Shukui Wang, Jingdan Wu, Yue Wang, Zhuorong Li, Jingwen Liu & Jian-Dong Jiang
Nature Medicine volume 10, pages1344–1351(2004)Cite this article
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We identify berberine (BBR), a compound isolated from a Chinese herb, as a new cholesterol-lowering drug. Oral administration of BBR in 32 hypercholesterolemic patients for 3 months reduced serum cholesterol by 29%, triglycerides by 35% and LDL-cholesterol by 25%. Treatment of hyperlipidemic hamsters with BBR reduced serum cholesterol by 40% and LDL-cholesterol by 42%, with a 3.5-fold increase in hepatic LDLR mRNA and a 2.6-fold increase in hepatic LDLR protein. Using human hepatoma cells, we show that BBR upregulates LDLR expression independent of sterol regulatory element binding proteins, but dependent on ERK activation. BBR elevates LDLR expression through a post-transcriptional mechanism that stabilizes the mRNA. Using a heterologous system with luciferase as a reporter, we further identify the 5′ proximal section of the LDLR mRNA 3′ untranslated region responsible for the regulatory effect of BBR. These findings show BBR as a new hypolipidemic drug with a mechanism of action different from that of statin drugs.
Did you know that as low as 5-20% of the nutrients you orally ingest from food or supplements will enter your systemic circulation? Why you may ask? The reason for this is first-pass metabolism. This refers to the metabolic breakdown of a drug/supplement whereby the concentration and bioavailability of the substance ingested is greatly reduced before it reaches systemic circulation (bloodstream). Bioavailability refers to the fraction absorbed into systemic circulation. After a supplement is consumed, it is absorbed by the digestive system (mainly small intestine) and enters the hepatic portal system to the liver. In individuals who do not have cirrhosis/liver damage, the smooth endoplasmic reticulum of the liver metabolizes most substances, significantly reducing the bioavailability of the supplement.
Since foods and drugs/supplements get metabolized in the small intestine prior to getting broken down in the liver, resulting in significantly decreased bioavailability (and thereby significantly decreased desired effect) the goal is to increase absorption into the small intestine and into the systemic circulation (prior to degradation in the liver) as much as possible.
Black pepper is one of the most widely used spices throughout the world, known namely for its antioxidant and gastrointestinal absorption enhancing properties. BioPerine® is a patented extract obtained from black pepper fruits (Piper nigrum) standardized minimum to 95% Piperine. BioPerine® is the only patented piperine extracted from black pepper and the only source from piperine to have undergone several clinical studies in the U.S. to substantiate its safety and efficacy for nutritional use.
BioPerine® has been found to enhance gastrointestinal absorption of nutrients by at least 30% in double blind and in vivo studies. BioPerine® has been clinically tested with several nutrient groups, including fat-soluble vitamins (ß-carotene), water-soluble vitamins (vitamin B6, vitamin C), curcumin, coenzyme Q10. It was shown to significantly enhance the bioavailability of these supplemented nutrients through increased gastrointestinal absorption. Studied nutrients were measured by amounts present in the blood when administered with BioPerine® as compared to the control group receiving the above nutrients alone.
Research suggests black pepper extract enhances nutrient digestion and absorption by increasing blood flow to the digestive tract through thermogenesis , thus significantly increasing bioavailability of other important nutrients. Bioavailability of Curcumin when co-administered with 20mg BioPerine® is enhanced by 20-fold or 2000% compared to bioavailability of Curcumin alone and selenium by 30%. Selenium, Curcumin and BioPerine® are all included in Joint Edge Rx to work synergistically together for the best results possible.
Current research also suggests that BioPerine® may play a role in decreasing inflammation, insulin resistance and lipid formation. This can be crucial in helping you in your weight and fat loss goals. However, more research is underway to help solidify these claims. No adverse side effects have been reported with Bioperine®.
⦁ Srinivasan, K. Black pepper and its pungent principle-piperine: a review of diverse physiological effects. Critical reviews in food science and nutrition. 2007; 47.8:735-748.
⦁ Brewer, M. S. Natural antioxidants: sources, compounds, mechanisms of action, and potential applications. Comprehensive Reviews in Food Science and Food Safety. 2011; 10.4:221-247.
⦁ Reanmongkol, Wantana, et al. Effects of piperine on bioenergetic functions of isolated rat liver mitochondria. Biochemical pharmacology. 1988; 37.4:753-757
⦁ Shoba, G, et al. Influence Of Piperine On The Pharmacokinetics Of Curcumin In Animals And Human Volunteers. Planta Med. 1998; 64(4):353-356.
⦁ Badmaev, V, et al. Piperine, An Alkaloid Derived From Black Pepper, Increases Serum Response Of Beta-Carotene During 14-Days Of Oral Beta-Carotene Supplementation. Nutrition Research. 1999; 19(3) 381-388.
⦁ Epstein, William W.; Netz, David F.; Seidel, Jimmy L. (1993). “Isolation of piperine from black pepper”. J. Chem. Ed. 70 (7): 598.
⦁ Badmaev, V, et al. Piperine Derived From Black Pepper Increases The Plasma Levels Of Coenzyme Q10 Following Oral Supplementation. J. Nutr. Biochem. 2000; 11: 109-113.
Posted in Health & Nutrition and tagged bioperine
ABOUT NADIA JAVAID, MD
Board Certified Family Medicine Physician
View all posts by Nadia Javaid, MD →
Published: 25 November 2014
Berberine activates thermogenesis in white and brown adipose tissue
Zhiguo Zhang, Huizhi Zhang, Bo Li, Xiangjian Meng, Jiqiu Wang, Yifei Zhang, Shuangshuang Yao, Qinyun Ma, Lina Jin, Jian Yang, Weiqing Wang & Guang Ning
Nature Communications volume 5, Article number: 5493 (2014) Cite this article
Obesity develops when energy intake exceeds energy expenditure. Promoting brown adipose tissue formation and function increases energy expenditure and hence may counteract obesity. Berberine (BBR) is a compound derived from the Chinese medicinal plant Coptis chinensis. Here we show that BBR increases energy expenditure, limits weight gain, improves cold tolerance and enhances brown adipose tissue (BAT) activity in obese db/db mice. BBR markedly induces the development of brown-like adipocytes in inguinal, but not epididymal adipose depots. BBR also increases expression of UCP1 and other thermogenic genes in white and BAT and primary adipocytes via a mechanism involving AMPK and PGC-1α. BBR treatment also inhibits AMPK activity in the hypothalamus, but genetic activation of AMPK in the ventromedial nucleus of the hypothalamus does not prevent BBR-induced weight loss and activation of the thermogenic programme. Our findings establish a role for BBR in regulating organismal energy balance, which may have potential therapeutic implications for the treatment of obesity.
Due to serious adverse effects and the limited effectiveness of currently available pharmacological therapies for obesity, many research efforts have focused on the development of drugs from natural products. Our previous studies demonstrated that berberine, an alkaloid originally isolated from traditional Chinese herbs, prevented fat accumulation in vitro and in vivo. In this pilot study, obese human subjects (Caucasian) were given 500 mg berberine orally three times a day for twelve weeks. The efficacy and safety of berberine treatment was determined by measurements of body weight, comprehensive metabolic panel, blood lipid and hormone levels, expression levels of inflammatory factors, complete blood count, and electrocardiograph. A Sprague-Dawley rat experiment was also performed to identify the anti-obesity effects of berberine treatment. The results demonstrate that berberine treatment produced a mild weight loss (average 5 lb/subject) in obese human subjects. But more interestingly, the treatment significantly reduced blood lipid levels (23% decrease of triglyceride and 12.2% decrease of cholesterol levels) in human subjects. The lipid-lowering effect of berberine treatment has also been replicated in the rat experiment (34.7% decrease of triglyceride and 9% decrease of cholesterol level). Cortisol, calcitriol, ACTH, TSH, FT4, and SHBG levels were not significantly changed following 12 weeks of berberine treatment. However, there was interestingly, an increase in calcitriol levels seen in all human subjects following berberine treatment (mean 59.5% increase, p = 0.11). Blood inflammatory factors (CRP, IL-6, TNFα, COX-2) and erythrocyte sedimentation rate (ESR) were not significantly affected by treatment with berberine. Tests of hematological, cardiovascular, liver, and kidney function following berberine treatment showed no detrimental side effects to this natural compound. Collectively, this study demonstrates that berberine is a potent lipid-lowering compound with a moderate weight loss effect, and may have a possible potential role in osteoporosis treatment/prevention.
Acute supplementation with alpha-glycerylphosphorylcholine augments growth hormone response to, and peak force production during, resistance exercise
Tim Ziegenfuss, Jamie Landis & Jennifer Hofheins
Journal of the International Society of Sports Nutrition volume 5, Article number: P15 (2008) Cite this article
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Many of the positive adaptations resulting from resistance exercise training (i.e., increased muscle mass and strength, decreased fat mass) are thought to be mediated, in part, by exercise-induced increases in growth hormone (GH). One ingredient that has shown clinical promise in elevating GH is the acetylcholine precursor alpha-glycerylphosphorylcholine (A-GPC). The purpose of this study was to examine the effects of a supplement containing primarily A-GPC on serum GH levels, explosive performance, and post-exercise substrate oxidation.
Astragalus Membranaceus (Huangqi)
TA-65, a single chemical entity isolated from the extract of the root of Astragalus membranaceus, leads to an improvement of certain health-span indicators including glucose tolerance, osteoporosis and skin fitness, without significantly increasing global cancer incidence in female mice .
6.1.1 Anti-aging effect of TA-65
Telomeres are essential genetic elements responsible for protecting chromosomes, and short telomeres are associated with aging and many diseases [207-209]. A number of studies have shown that activating telomerase can maintain telomere length, delay aging, and reverse age tissue degeneration [210,211]. TA-65 increased telomerase activity in a telomere shortening cell model – IMR90 cells . TA-65 can also lengthen the red blood cell telomere lengths and produce higher rates of feather renewal in captive zebra finches . Consistent with this, TA-65 can activate telomerase to increase average telomere length in haploinsufficient mouse embryonic fibroblasts and aged mice, decrease the percentage of DNA damage and remodel the relative proportions of circulating leukocytes, reduce the percentage of cells with short telomeres and improve the structure of multiple tissues, at the same time. In old female mice, TA-65 administration for 4 months enhanced the health span, but had no impact on mean or maximum longevity . A randomized, double blind, placebo controlled clinical research involving 117 relatively healthy cytomegalovirus-positive subjects aged 53-87 years old found that TA-65 can lengthen telomeres . A study enrolling 7000 person-years in over a 5-year period, found that TA-65 improves markers of metabolic, bone, and cardiovascular health, with no adverse events, which suggests that TA-65 improves health and may reduce risk of morbidity and mortality .
Anti-vascular disease by AST
AST have positive effects on cardio-cerebrovascular diseases.
Astragalus membranaceus has multiple pharmacological effects, including anti-oxidative-stress, anti-inflammatory, immuno-regulation, vascular protective effects, anti-neurodegeneration, anti-cancer and anti-aging effects via numerous signaling pathways in vital organs and systems. More attention and further studies are needed to evaluate the underlying mechanisms of Astragalus membranaceus’ actions and its targets, in particular, reveal the mechanisms of its metabolism of absorption, distribution, transformation, and excretion. Based on the existing studies and clinical practices, Astragalus membranaceus has a good potential for broad application in aging and aging-related diseases.
Astragalus is usually taken in combination with other herbal supplements. When used appropriately, astragalus appears to be very safe and to have few side effects. Very high doses may suppress the immune system. Hence patients should avoid using astragalus if they are taking immune-suppressing drugs. Pregnant or nursing women should not use the astragalus root. If a person has an immune system disease, such as multiple sclerosis, lupus, rheumatoid arthritis, or another condition known as an “autoimmune disease,” that person should not use the astragalus root.
The results of this study suggest that Ashwagandha root extract reduces psychological and physiological markers of stress, improves mental well-being, and reduces serum cortisol level and food cravings and improves eating behaviors. A statistically significant reduction in body weight and body mass index were observed in patients treated with Ashwagandha root extract compared to placebo. Therefore, we conclude that Ashwagandha root extract can be useful for body-weight management in patients experiencing chronic stress. However, further studies are required to bolster the potential of Ashwagandha to prevent weight gain caused by long-term chronic stress.
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