Identification of a botanical inhibitor of intestinal diacylglyceride acyltransferase 1 activity via in vitro screening and a parallel, randomized, blinded, placebo-controlled clinical trial

Diacylglyceride acyltransferase 1 (DGAT1) is the enzyme that adds the final fatty acid on to a diacylglyceride during triglyceride (TG) synthesis. DGAT1 plays a key role in the repackaging of dietary TG into circulating TG rich chylomicrons. A growing amount of research has indicated that an exagger...

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Bibliographic Details
Published in:Nutrition & metabolism 2015-08, Vol.12 (1), p.27-27, Article 27
Main Authors: Velliquette, Rodney A, Grann, Kerry, Missler, Stephen R, Patterson, Jennifer, Hu, Chun, Gellenbeck, Kevin W, Scholten, Jeffrey D, Randolph, R Keith
Format: Article
Language:English
Subjects:
Anthocyanin
Care and treatment
Clinical trials
Health aspects
Instrument industry
Medical research
Medicine, Botanic
Medicine, Experimental
Medicine, Herbal
Metabolism
Monounsaturated fatty acids
Nutrition
Obesity
Physiological aspects
Plant metabolites
Polyphenols
Triglycerides
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Summary:Diacylglyceride acyltransferase 1 (DGAT1) is the enzyme that adds the final fatty acid on to a diacylglyceride during triglyceride (TG) synthesis. DGAT1 plays a key role in the repackaging of dietary TG into circulating TG rich chylomicrons. A growing amount of research has indicated that an exaggerated postprandial circulating TG level is a risk indicator for cardiovascular and metabolic disorders. The aim of this research was to identify a botanical extract that inhibits intestinal DGAT1 activity and attenuates postprandial hypertriglyceridemia in overweight and obese humans. Twenty individual phytochemicals and an internal proprietary botanical extract library were screened with a primary cell-free DGAT1 enzyme assay that contained dioleoyl glycerol and palmitoleoyl Coenzyme A as substrates plus human intestinal microsomes as the DGAT1 enzyme source. Botanical extracts with IC50 values 
ISSN:1743-7075
1743-7075
DOI:10.1186/s12986-015-0025-2