Lipid-lowering effect of berberine in human subjects and rats
Keywords: Berberine Obesity Hyperlipidemia Osteoporosis Human Rat Pilot study
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 pane1, 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, TNFa, 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.
[C] 2012 Elsevier GmbH. All rights reserved.
The obesity epidemic has emerged as a severe health threat to the population worldwide. The Centers for Disease Control and Prevention (CDC) reported that 33.8% of U.S. adults and approximately 17% of children and adolescents aged 2-19 years were obese in 2010. The prevalence of obesity has tremendously increased the risk of many other disorders such as hyperlipidemia, type II diabetes, and osteoarthritis (Malnick and Knobler 2006). According to NIH guidelines (NH-I 1998); a low calorie diet, increased physical activity, and behavior therapy are the fundamental treatments for obese individuals. If the combined lifestyle modification isn't effective, pharmacological therapy should be considered for individuals with a BMI [greater than or equal to]30 kg/[m.sup.2] or patients with a BMJ [greater than or equal to]27 kg/[m.sup.2] with concomitant obesity-related risk factors or diseases.
An unfortunate fact of obesity pharmacotherapy is that even though more than one dozen anti-obesity medications have been introduced into market, the majority of them have been withdrawn or discontinued due to serious adverse effects (loannides-Demos et al. 2011). The most recent examples are rimonabant and sibutramine which were withdrawn in 2009 and suspended in 2010 respectively....