Bioprospection of Natural Sources of Polyphenols with Therapeutic Potential for Redox-Related Diseases

Abstract

Plants are a reservoir of high-value molecules with underexplored biomedical applications. With the aim of identifying novel health-promoting attributes in underexplored natural sources, we scrutinized the diversity of (poly)phenols present within the berries of selected germplasm from cultivated, wild, and underutilized Rubus species. Our strategy combined the application of metabolomics, statistical analysis, and evaluation of (poly)phenols’ bioactivity using a yeast-based discovery platform. We identified species as sources of (poly)phenols interfering with pathological processes associated with redox-related diseases, particularly, amyotrophic lateral sclerosis, cancer, and inflammation. In silico prediction of putative bioactives suggested cyanidin–hexoside as an anti-inflammatory molecule which was validated in yeast and mammalian cells. Moreover, cellular assays revealed that the cyanidin moiety was responsible for the anti-inflammatory properties of cyanidin–hexoside. Our findings unveiled novel (poly)phenolic bioactivities and illustrated the power of our integrative approach for the identification of dietary (poly)phenols with potential biomedical applications.

Assessing the Intestinal Permeability and Anti-Inflammatory Potential of Sesquiterpene Lactones from Chicory

“…The low IC 50 value for Crz1 inhibition by 11β,13-dihydrolactucin suggests that the low absorption rate observed may still provide the potential for modulation of Crz1 activity. The ability of 11β,13-dihydrolactucin to modulate Crz1 activity is very significant and comparable to the well described immunosuppressant drug FK506, known for inhibition of calcineurin and also already described to be active in the yeast system [27].…”

“…Cells were washed and resuspended in 5 µL of 1,4-Diazabicyclo[2.2.2]octane (DABCO, triethylenediamine) DABCO solution (200 mM DABCO in 75% ( v / v ) glycerol, 25% ( v / v ) PBS) (Sigma-Aldrich). The preparations were monitored for GFP fluorescence as previously described [ 27 ] using a Zeiss Imager Z2 (Zeiss, Germany) fluorescence microscope. Photographs were taken with an Axiocam 506 mono (Zeiss).…”

“…The qRT-PCR analyses were performed as previously described [ 27 ]. Briefly, total RNA was extracted using the RNeasy Mini kit (QIAGEN).…”

“…The preparations were monitored for GFP fluorescence as previously described [27] using a Zeiss Imager Z2 (Zeiss, Germany) fluorescence microscope. Photographs were taken with an Axiocam 506 mono (Zeiss).…”

Extracts of Digested Berries Increase the Survival of Saccharomyces cerevisiae during H2O2 Induced Oxidative Stress

“…For instance, increasing mRNA levels of heme oxygenase 1 (HO-1) and consequently protecting retinal cells from diabetes-induced oxidative stress [ 15 ]. It has also been suggested that differences in polyphenol composition between berry species may account for differences in bioactivity against a range of disorders [ 16 ]. However, anthocyanins are sensitive to physicochemical conditions encountered during gastrointestinal digestion, and may also be modified during absorption and metabolism, leading to structural changes into anthocyanin derivatives with different biochemical properties.…”