The Effect of Formulation on the Bioactivity of Artemisia Preparations for Metabolic Syndrome

Botanicals have been used for thousands of years as therapeutic agents for many diseases and human conditions. “Metabolic syndrome” is currently defined as a condition whose major features consist of obesity, insulin resistance, development of Type 2 diabetes and accelerated cardiovascular disease and continues to grow at epidemic proportions. Our BRC (Botanical Research Center) focuses on botanicals that can be used for the prevention/treatment of metabolic syndrome. One of the primary research objectives of the BRC as a whole focuses on how the constituents of botanicals affect insulin signaling pathways and improve insulin resistance, the underlying metabolic dysregulation associated with metabolic syndrome. While select species of Artemisia are under current evaluation by the BRC, the extract of Artemisia dracunculus L. (PMI-5011) is the most characterized both in terms of its biological activity and its composition of 6 compounds identified as having antidiabetic activity. The bioavailability of active compounds from Artemisia were measured and related to the formulation of the vehicle in C57Bl6J mice. Comparable bioaccessibility (i.e. potential to be bioavailable) of the active compounds was measured using the TNO intestinal model (TIM), a dynamic multi-compartmental, computer-controlled apparatus that closely simulates all in vivo conditions of the upper GI tract of humans. A comparison of test preparations showed significant improvements in the bioaccessibility, bioavailability and bioactivity for specific formulations relative to the extract alone. These effects will have a profound influence on the effective human dose of Artemisia and must be considered when planning clinical studies.