Emodin, the Bioactive Ingredient of Herbal Cascara Sagrada (Rhamnus purshiana) which Protects Our Body Against the Onset of Metabolic Syndrome

By Kyle J. Norton, Master of Nutrition

Emodin, a major bioactive compound found in herbal Cascara Sagrada may be considered an adjunct therapy in the prevention and treatment of metabolic syndrome, some scientists suggested.

Metabolic syndrome is a cluster of conditions associated with the increased risk of diabetes, heart disease and stroke, including high blood pressure and sugar, excess body weight and obesity, abnormally high levels of blood cholesterol or triglyceride levels.

Researchers do not know the exact causes of metabolic syndrome. However, they do know that ethnicity and family history and mutation of genes which causes insulin resistance inherited from the parents are the numbers of risk factor associated with the early onset of the condition.

Certain medical conditions such as polycystic ovarian syndrome and gallstone disease, nonalcoholic fatty livers are also the prevalent risk factors for the development of metabolic syndrome.

It is misleading that metabolic syndrome can only cause heart disease, diabetes, and stroke. According to the National Heart, Lung and Blood Institute, people with metabolic syndrome are also associated with an increased risk of excessive blood clotting and persistent low-grade inflammation throughout the body.

Treatment of metabolic syndrome should be followed closely to the underlining risk factors of abdominal obesity, physical inactivity, and atherogenic/diabetogenic diet and drug therapy for specific metabolic risk factors should be considered for those at high or moderately high 10-year absolute risk of atherosclerotic cardiovascular disease, according to the American Heart Association and the National Heart, Lung, and Blood Institute slightly modifies and clarifies the diagnostic criteria for the metabolic syndrome.

Medication used to reduce the level of progression of metabolic syndrome-related disorders including thiazolidinediones, GLP-1 agonists, and DPP-4 inhibitors may be effective, however, they can induce serious side effects such as edema, weight gain, macular edema, and heart failure.

Some patients who take the medicine may also experience side effects of hypoglycemia, decrease hematocrit and hemoglobin levels and increased bone fracture risk.

Cascara sagrada is a species of buckthorn, genus Rhamnus, belonging to the family Rhamnaceae, native to western North America.

Cascara sagrada bark has been used in traditional medicine for gastrointestinal support. and it is thought to have a laxative and natural cleansing, etc., effect.

The chemical ingredients
Besides the main compound of anthraquinones, other compounds include anthraquinone glycosides, (emodin, frangulin, iso-emodin, aloe-emodin, and chrysophanol), rhein, aloin, malic acid, tannic acid, cascarosides A, B, C, and D, hydroxy anthracene derivatives (HAD).

In the concerns of the side effects of conventional medicine used for the treatment of metabolic syndrome, researchers at the Shanghai Institute of Materia Medica launched an investigation of the effect of emodin, a natural product and active ingredient of various Chinese herbs including Cascara Sagrada in metabolic disorders in diet-induced obese (DIO) mice.

Emodin exerted a significant effect as a potent and selective 11beta-HSD1 inhibitor against insulin resistance and with the IC(50) of 186 and 86 nM for human and mouse 11beta-HSD1, respectively

11β-HSD1, a family of enzymes which have been found to associate with the risk of insulin resistance.

Furthermore, single oral administration of emodin inhibited 11beta-HSD1 activity of liver and fat significantly in mice without reversing the prednisone and dexamethasone-induced insulin resistance.

In DIO mice, oral administration of emodin improved insulin sensitivity and lipid metabolism and lowered blood glucose and hepatic phosphoenolpyruvate carboxykinase (PEPCK), and glucose-6-phosphatase mRNA.

Phosphoenolpyruvate carboxykinase (PEPCK) is associated with the control of hepatic glucose output.

Glucose-6-phosphatase mRNA is increased to some extents in kidney and liver of diabetic rats.

The findings suggested the potential value of analogs of emodin for the treatment of metabolic syndrome or type 2 diabetes.

Moreover, researchers at the extended study of the effect emodin in metabolic syndrome mice associated with 11beta-HSD1 activity also discovered that emodin inhibited the 11β-HSD1 activity in 3T3-L1 adipocytes in concentration- and time-dependent manners (the IC₅₀ values of 7.237 and 4.204 μmol/L, respectively, after 1 and 24 h treatment, through suppressing the 11-dehydrocorticosterone-in the generation of corticosterone without affecting corticosterone-induced adipogenesis in normal tissues..

3T3-L1 adipocytes are used as cell culture model of insulin resistance

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Adipogenesis is the process of cell differentiation from pre-adipocytes to adipocytes.

Moreover, emodin (3 μmol/L) partly reversed the impaired insulin-stimulated glucose uptake and adiponectin secretion induced by 11-dehydrocorticosterone but not those induced by corticosterone.

In ob/ob mice, long-term emodin administration decreased 11β-HSD1 activity in mesenteric adipose tissues, lowered non-fasting and fasting blood glucose levels, and improved glucose tolerance.

Dr. Wang YJ, the lead scientist, after taking into account co and confounders, wrote, "Emodin improves the inactive glucocorticoid-induced adipose tissue dysfunction by selective inhibition on 11β-HSD1 in adipocyte in vitro and improves glycemic control in ob/ob mice".

Taken altogether, Cascara Sagrada bioactive compound emodin may be considered an adjunct supplement used alone for the prevention or combined with other conventional medicine for the treatment of metabolic syndrome without inducing adverse effects.

However, due to the limitation of the above studies, additional data collection large example size and multi-centers studies performed with human consumption of the whole food or its bioactive compound emodin during the course of the disease will be necessary to complete the picture of Cascara sagrada anti-metabolic syndrome possibilities.

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Author Biography
Kyle J. Norton (Scholar, Master of Nutrition, All right reserved)
Health article writer and researcher; Over 10.000 articles and research papers have been written and published online, including worldwide health, ezine articles, article base, health blogs, self-growth, best before it's news, the karate GB daily, etc.,.
Named TOP 50 MEDICAL ESSAYS FOR ARTISTS & AUTHORS TO READ by Disilgold.com Named 50 of the best health Tweeters Canada - Huffington Post
Nominated for shorty award over last 4 years
Some articles have been used as references in medical research, such as international journal Pharma and Bioscience, ISSN 0975-6299.

References
(1). "Emodin, a natural product, selectively inhibits 11beta-hydroxysteroid dehydrogenase type 1 and ameliorates metabolic disorder in diet-induced obese mice" by Feng Y, Huang SL, Dou W, Zhang S, Chen JH, Shen Y, Shen JH, Leng Y. (PubMed)
(2). Emodin, an 11β-hydroxysteroid dehydrogenase type 1 inhibitor, regulates adipocyte function in vitro and exerts the anti-diabetic effect in ob/ob mice. by Wang YJ, Huang SL, Feng Y, Ning MM, Leng Y. (PubMed)