A M Metabolics. inventing the future of healthcare

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Transcription:

A M Metabolics inventing the future of healthcare

Metabolic Disease Control Flavonoid-Based Amelioration of Carbohydrate Dysfunctional Metabolism December 2013 Daryl L. Thompson and M. Joseph Ahrens

2002 Ahrens & Thompson designed Scripps grapefruit weight loss study Fresh fruit, juice, dehydrated powder Patients lost weight over 3 months Glucose response decreased Insulin levels affected

Naringin early candidate

Led to the discovery of a class of compounds more effective than naringin Understanding naringin structure and effect Understanding carbohydrate chemistry Awareness of Metabolic Syndrome, Diabetes

To control carbohydrate chemistry Complex sugars to simple sugars Absorption from gut Absorption to fat and muscle tissue New glucose from storage or mfg Fat storage Insulin sensitivity and/or production

No one getting diabetes eating mangoes, other sweet tropical fruits Survey of diabetes Survey of the plant kingdom Overlap

Rational Drug Design Candidate metabolic targets Naringin-like phytochemicals Drug-likeness Optimal solubility Balance in number of hydrogen bonds Smaller molecular weight Lipinski s Rule of Five Not more than 5 hydrogen bonds No more than 10 hydrogen bond acceptors MW less than 500 g/mole Partition log coefficient log P less than 5

Computer-Assisted Drug Design BRENDA Supercomputers IPAM & IBI

Glucosidase inhibition by myricetin

ATPase inhibition by quercetin

Alpha-amylase inhibition by chlorogenic acid

Rodent Study by Eurofins Labs STZ treated rats, stabilized at 300 ul/dl Formulation & Dose Fasting & mid-day glucose & OGT response decreased by 18%, 27%, and 24%, respectively Several rats became non-diabetic

I have never seen anything perform like this in this severe of a model, other than insulin itself you may be regenerating B-cells Dr. Gary Grover, Principle Investigator Director, Eurofins Product Safety Laboratories

40 patients type 2 diabetics Half on metformin Half on no control Half of each group received placebo Half of each group received Emulin 250mg with each meal

Change in Fasting Glucose 30% 20% 10% 0% -10% -20% -30% 0 7 PLACEBO EMULIN DRUG E + DRUG

Change in 2 Hr Postprandial Glucose 10% 5% 0% -5% -10% -15% -20% -25% 0 7 PLACEBO EMULIN DRUG E + DRUG

Change in AUC 15% 10% 5% 0% -5% -10% -15% -20% -25% 0 7 PLACEBO EMULIN DRUG E + DRUG

Emulin does a better job at reducing blood sugar levels in type II diabetes than metformin, the most commonly prescribed drug. Emulin [is] a genuine breakthrough. Dr. Mark Kipnes, Principle Investigator Director, dgdresearch/cetero Labs

The Science Behind Emulin Three naturally-occurring phytochemicals that do not occur together in nature Each with specific major activity toward a key control point in carbohydrate metabolism, but with some overlap 3 skeleton keys that together unlock or lock a group of related metabolic pathways

Inhibits several α-glucosidases Inhibits α-amylase Inhibits release of pancreatic α-amylase

Non-competitively inhibit GLUT2 No effect on GLUT5 & SGLT1

Stimulates GLUT4 expression in muscle tissue via beta endorphin-like immunoactivity

A broad category Increases insulin receptor expression in muscle tissue Competes with rosiglitazone Stimulates glucose uptake by muscle in the presence of insulin

Stimulates GLP-1, via camp, promoting IDX-1, maintaining β cells responsiveness to glucose. Stimulates islets to release insulin via non Ca ++, K channels

Inhibits GLUT4 in adipocytes by: inhibiting protein kinase C phosphorylation of receptor sites Suppressing translocation of GLUT4

Inhibits at G1 cell expansion phase Inhibits maturation via activation of AMPK pathway

Inhibits the growth of helicobacter in GI Promotes healthy upper and lower GI lining Ameliorates colitis and diarrhea

Plants high in simple carbohydrates evolved to: Provide a buffer or carbohydrate manager for higher life forms to be consumed with their high sugar load Higher life forms co-evolved to use these carb managers in carbohydrate metabolism Consuming refined sugars without these components results in an inflammatory response The components of Emulin have been left out of the modern diet, resulting in the obesity and diabetes epidemics

COMPOSITION AND METHOD FOR TREATING DIABETES AND METABOLIC DISORDERS USP 7,943,164 and 8,198,319 CIP 13/961524 and worldwide Others Pending Food Additive Food Supplement Functional Food Pharmaceutical Composition Unique Combination not found in Nature No digestive issues Equal to or greater efficacy than current drugs

Currently available at GNC and online Seeking to license/sell IP in other channels Glucose control foods Sports Drinks/Bars Replacement meals Diet aid Diet Foods & Beverages Diabetic Treatment No drug claims at present Medical Foods