Analysis of 1,3-cyclopentadiones from hops and proanthocyanidins from Acacia nilotica and their combined efficacy in treating metabolic syndrome and hypercholesterolemia

We aimed to determine the identity and percent weight of phytochemicals present in two unique phytochemical extracts. The first is a modified hops (Humulus lupulus var. Nugget) extract consisting of various substituted 1,3-cyclopentadiones (SCPD), the second is an Acacia nilotica bark extract (ABE) comprised almost entirely of proanthocyanidins (PAC). Analytical standards for the predominant SCPD diastereomers and analogs were obtained using high-speed counter-current chromatography (HSCCC). A UPLC method was developed for the analysis of SCPD in modified hops extract.

The identification and isolation of the major components of the ABE began with fractionation into two homogenous fractions: high molecular weight polymeric condensed tannins and small molecules & oligomeric condensed tannins. LC-MS analysis of the small molecule & oligomeric tannin fraction revealed the presence of various mono- and di- galloyl catechins [1].

The significance of these findings relates to the use of these two extracts in combination, as a nutritional therapeutic with clinically demonstrated efficacy. The discovery of this unique combination was initially shown in two in-vitro assays and subsequently confirmed in the db/db mouse. The efficacy of this combination was demonstrated in a 2-arm, open label clinical trial (HMS3) involving 49 subjects with hypercholesterolemia and metabolic syndrome (MetS). The culmination of this research is the development of a proprietary medical food designed to provide nutritional support for the management of conditions associated with metabolic syndrome and cardiovascular disease.

References: 1. El-Toumy, S. A. A., Mahdy, K. A. (2004), Bull Fac. Pharm., Cairo Univ., 42:317–325.