Berberine is a very popular glucose disposal agent (GDA) on the market that has caught the interest of many. Berberine is an alkaloid extracted from various plants that plays a role in reducing inflammation, improving intestinal health, possibly reducing cholesterol, as well as being a diabetic aid due to its ability to reduce glucose production in the liver. Its main mechanism os through activation of Adenosine Monophosphate-Activated Protein Kinase (AMPK) while inhibiting Protein-Tyrosine Phosphatase 1B (PTP1B). As it works through AMPK inhibition, it will only reduce blood sugar levels if they are elevated. We typically see berberine being used mainly for its glucose disposal effects so we will focus on that aspect during this article, please note however it has a host of other benefits.
A randomized, parallel controlled, open-label clinical trial was conducted to evaluate the effect of a botanic compound berberine (BBR) on NAFLD from Yan et al. A total of 184 eligible patients with NAFLD were enrolled and randomly received (i) lifestyle intervention (LSI), (ii) LSI plus pioglitazone (PGZ) 15mg qd, and (iii) LSI plus BBR 0.5g tid, respectively, for 16 weeks. Hepatic fat content (HFC), serum glucose and lipid profiles, liver enzymes and serum and urine BBR concentrations were assessed before and after treatment. We also analyzed hepatic BBR content and expression of genes related to glucose and lipid metabolism in an animal model of NAFLD treated with BBR. As compared with LSI, BBR treatment plus LSI resulted in a significant reduction of HFC (52.7% vs 36.4%, p = 0.008), paralleled with better improvement in body weight, HOMA-IR, and serum lipid profiles (all p<0.05). BBR was more effective than PGZ 15mg qd in reducing body weight and improving lipid profile. BBR-related adverse events were mild and mainly occurred in digestive system. Serum and urine BBR concentrations were 6.99ng/ml and 79.2ng/ml, respectively, in the BBR-treated subjects. Animal experiments showed that BBR located favorably in the liver and altered hepatic metabolism-related gene expression. BBR ameliorates NAFLD and related metabolic disorders. The therapeutic effect of BBR on NAFLD may involve a direct regulation of hepatic lipid metabolism (1.)
The second study I wanted us to look at was one from Zhang et al. The objective of the study was to evaluate the efficacy and safety of berberine in the treatment of type 2 diabetic patients with dyslipidemia. One hundred sixteen patients with type 2 diabetes and dyslipidemia were randomly allocated to receive berberine (1.0 g daily) and the placebo for 3 months. The primary outcomes were changes in plasma glucose and serum lipid concentrations. Glucose disposal rate (GDR) was measured using a hyperinsulinemic euglycemic clamp to assess insulin sensitivity. In the berberine group, fasting and postload plasma glucose decreased from 7.0 +/- 0.8 to 5.6 +/- 0.9 and from 12.0 +/- 2.7 to 8.9 +/- 2.8 mm/liter, HbA1c from 7.5 +/- 1.0% to 6.6 +/- 0.7%, triglyceride from 2.51 +/- 2.04 to 1.61 +/- 1.10 mm/liter, total cholesterol from 5.31 +/- 0.98 to 4.35 +/- 0.96 mm/liter, and low-density lipoprotein-cholesterol from 3.23 +/- 0.81 to 2.55 +/- 0.77 mm/liter, with all parameters differing from placebo significantly (P < 0.0001, P < 0.0001, P < 0.0001, P = 0.001, P < 0.0001, and P <0.0001, respectively). The glucose disposal rate was increased after berberine treatment (P = 0.037), although no significant change was found between berberine and placebo groups (P = 0.063). Mild to moderate constipation was observed in five participants in the berberine group. They concluded stating that “Berberine is effective and safe in the treatment of type 2 diabetes and dyslipidemia” (2.)
Now that we know from a literary standpoint that berberine itself is a very potent glucose disposal agent, I wanted to look specifically at Super Berberine, also known as Berberine-Cyclodextrin Complex (this just means that the berberine is complexed with cyclodextrins.) Cyclodextrins are sugar molecules bound into a ring- or doughnut-shape, which can be used to increase the solubility of other compounds by the formation of inclusion complexes. The insoluble compound is held in the hydrophobic cavity, and the cyclodextrin acts as a water-soluble “carrier” molecule. This makes berberine more soluble leading to a greater bioavailabliltiy than normal berberine and also makes it less bitter because the complexed molecules do not interact as fully with our taste buds (3, 4, 5.) As this form of berberine is enhanced, that typically means its a trademarked ingredient (which this is.) That means its typically only found in higher end GDAs. Partition-Elite from Prime Nutrition contains super berberine at a very effective dosage of 50mgs (due to the fact that the bioavailability is enhanced and is combined with eight other GDAs.) So if you’re looking to implement Super Berberine, try out Partition-Elite with a higher carbohydrate meal and monitor as it will increase insulin sensitivity, promotes a positive partitioning environment where you store more calories in muscle cells instead of fat cells, and helps in keeping you growing leaner.
- Efficacy of Berberine in Patients with Non-Alcoholic Fatty Liver Disease. Hong-Mei Yan, Ming-Feng Xia, Yan Wang, Xin-Xia Chang, Xiu-Zhong Yao, Sheng-Xiang Rao, Meng-Su Zeng, Yin-Fang Tu, Ru Feng, Wei-Ping Jia, Jun Liu, Wei Deng, Jian-Dong Jiang, Xin Gao. PLoS One. 2015 (https://www.ncbi.nlm.nih.gov/pubmed/26252777)
- Treatment of type 2 diabetes and dyslipidemia with the natural plant alkaloid berberine. Yifei Zhang, Xiaoying Li, Dajin Zou, Wei Liu, Jialin Yang, Na Zhu, Li Huo, Miao Wang, Jie Hong, Peihong Wu, et al. J Clin Endocrinol Metab. 2008 (https://www.ncbi.nlm.nih.gov/pubmed/18397984)
- Study on the Interaction of β-Cyclodextrin and Berberine Hydrochloride and Its Analytical Application. Jia, B., Li, Y., Wang, D., & Duan, R. (2014). (https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4014474/)
- A simple fluorescence quenching method for berberine determination using water-soluble CdTe quantum dots as probes. Ming Cao, Meigui Liu, Chun Cao, Yunsheng Xia, Linjun Bao, Yingqiong Jin, Song Yang, Changqing Zhu. Spectrochim Acta A Mol Biomol Spectrosc. 2010 (https://www.ncbi.nlm.nih.gov/pubmed/20093069)
- Significant fluorescence enhancement by supramolecular complex formation between berberine chloride and cucurbit(n=7)uril and its analytical application. Nan Dong, Li-na Cheng, Xiu-lin Wang, Qin Li, Chuan-yu Dai, Zhu Tao. Talanta. 2011 (https://www.ncbi.nlm.nih.gov/pubmed/21482268)