Masquelier’s grape seed extract: from basic flavonoid research to a well-characterized food supplement with health benefits

Abstract

Careful characterization and standardization of the composition of plant-derived food supplements is essential to establish a cause-effect relationship between the intake of that product and its health effect. In this review we follow a specific grape seed extract containing monomeric and oligomeric flavan-3-ols from its creation by Jack Masquelier in 1947 towards a botanical remedy and nutraceutical with proven health benefits. The preparation’s research history parallels the advancing insights in the fields of molecular biology, medicine, plant and nutritional sciences during the last 70 years. Analysis of the extract’s flavanol composition emerged from unspecific colorimetric assays to precise high performance liquid chromatography - mass spectrometry and proton nuclear magnetic resonance fingerprinting techniques. The early recognition of the preparation’s auspicious effects on the permeability of vascular capillaries directed research to unravel the underlying cellular and molecular mechanisms. Recent clinical data revealed a multitude of favorable alterations in the vasculature upon an 8 weeks supplementation which summed up in a health benefit of the extract in healthy humans. Changes in gene expression of inflammatory pathways in the volunteers’ leukocytes were suggested to be involved in this benefit. The historically grown scientific evidence for the preparation’s health effects paves the way to further elucidate its metabolic fate and molecular action in humans.

Vitamin P – Do Certain Polyphenolic IMPS Have a Vital Function?

“…This problem, coupled with the difficulty in attributing a deficiency disease that could clearly be linked to Szent-Györgyi's lemon extracts or to Vitamin P might have led scientists to abandon Vitamin P as a useful hypothesis. Nonetheless, despite the difficulties in understanding the relation of Vitamins C and P, two things have been established: (i) the existence of a distinct biological effect of Vitamin P, i.e., the influence of a series of naturally occurring flavonoids and coumarins ( Figure 1 and Figure S1, Supporting Information) on vascular permeability; and (ii) the influence of these natural products on the anti-scurvy effect of Vitamin C (44,48,65).…”

“…Polyphenolic flavonoid compounds such as flavan-3-ols, flavan-3,4-diols, and oligomeric proanthocyanidins (including procyanidin B1 [15]) have radical scavenging activity and, therefore, have been proposed to serve as "antioxidants". It is now known that vascular function is strongly influenced by oxidative stress and that diminishing oxidative stress also reduces inflammatory stress (65). However, flavonoids and related compounds, as well as extracts containing these compounds, may be involved in a multitude of biological functions and may have multiple (pleiotropic) effects that during evolution have not been selected for a strong effect on a single well-defined target (65,67), but rather the opposite.…”

“…This does not rule out the possibility of specific biological targets, which remain to be determined. In fact, there may be many specific biological targets that are impacted by chemical members of the Vitamin P family (65,67).…”

“…Masquelier's product, called "MASQUELIER's ® Original OPCs", was extracted from the seeds of Vitis vinifera L. This product contained catechins, epicatechins, and OP(A)Cs (dimers to pentamers)(66).Detailed analyses have established that the product is standardized to contain about 85% (w/w) flavonoids, of which 50-60% (w/w) are monomeric and dimeric catechins. The same product was evidently devoid of OP(A)Cs(65,67).…”

“…Early research on the effects of grape seed extracts on the permeability of vascular capillaries was designed to unravel the underlying cellular and molecular mechanisms of action of oligomeric proanthocyanidins and other flavonoids(65).During the 1970's, Masquelier began producing a grape seed extract for medicinal uses as an alternative to the pine-derived Pycnogenol ® . Grape seeds contain a similar, but not identical complement of the oligomeric proanthocyanidins (OPCs; syn OPACs) to pine bark.…”