Polyphenols and Sesquiterpene Lactones from Artichoke Heads: Modulation of Starch Digestion, Gut Bioaccessibility, and Bioavailability following In Vitro Digestion and Large Intestine Fermentation

Abstract

Artichoke is a relevant source of health-promoting compounds such as polyphenols and sesquiterpene lactones. In this study, the bioaccessibility and gut bioavailability of artichoke constituents were evaluated by combining in vitro digestion and large intestine fermentation, metabolomics, and Caco-2 human intestinal cells model. Moreover, the ability of artichoke polyphenols to modulate the in vitro starch digestibility was also explored. An untargeted metabolomic approach based on liquid chromatography quadrupole-time-of-flight (UHPLC/QTOF) mass spectrometry coupled with multivariate statistics was used to comprehensively screen the phytochemical composition of raw, digested, and fermented artichoke. Overall, a large abundance of phenolic acids and sesquiterpene lactones was detected, being 13.77 and 11.99 mg·g−1, respectively. After 20 h of in vitro large intestine fermentation, a decrease in polyphenols and sesquiterpene lactones content was observed. The most abundant compounds characterizing the raw material (i.e., chlorogenic acid and cynaropicrin equivalents) showed an average % bioaccessibility of 1.6%. The highest % bioaccessibility values were recorded for flavonoids such as anthocyanin and flavone equivalents (on average, 13.6%). However, the relatively high bioavailability values recorded for flavonols, phenolic acids, and sesquiterpene lactones (from 71.6% up to 82.4%) demonstrated that these compounds are able to be transported through the Caco-2 monolayer. The phenolic compounds having the highest permeation rates through the Caco-2 model included low molecular weight phenolics such as tyrosol and 4-ethylcatechol; the isoflavonoids 3′-O-methylviolanone, equol 4′-O-glucuronide, and hydroxyisoflavone; together with the methyl and acetyl derivatives of glycosylated anthocyanins. Therefore, although human in vivo confirmatory trials are deemed possible, current findings provide insights into the mechanistic effects underlying artichoke polyphenols and sesquiterpenoids bioavailability following gastrointestinal and large intestine processes.

Functional implications of bound phenolic compounds and phenolics–food interaction: A review

“…Generally, in vitro digestion methods are the most exploited to simulate both gastric and small intestinal phases, followed or not by Caco‐2 cells uptake evaluations (Rocchetti, Giuberti, et al., 2020; Rocchetti, Rizzi, et al., 2020). In this regard, PCs bioaccessibility is usually assessed using the in vitro static gastrointestinal method, first harmonized by Minekus et al.…”

Phytochemical Profile, Mineral Content, and Bioactive Compounds in Leaves of Seed-Propagated Artichoke Hybrid Cultivars

“…The mass spectrometer was set to operate in full-scan mode and positive polarity, acquiring ions in the range of 100–1200 m/z . The analytical conditions for the analysis of bioactive compounds in these food matrices were optimized in previous experiments [ 6 ]. Briefly, the chromatographic separation was achieved using a Knauer Blue Orchid C18 column (100 mm × 2 mm i.d., 1.8 μm) and a mixture of water and acetonitrile (both LC-MS grade, VWR, Milan, Italy) as mobile phase.…”

“…The artichoke is well known as a valuable source of various bioactive compounds (such as polyphenols), soluble dietary fiber (e.g., inulin), vitamins, and minerals [ 1 , 4 ]. Specifically, leaf extracts are rich in phenolic acids (e.g., isomers of caffeoylquinic acid), flavones (such as glycosidic forms of luteolin and apigenin), anthocyanins (mainly glycosidic derivatives of cyanidin), and lower-molecular-weight phenolics [ 5 , 6 ]. Sesquiterpene lactones are also an important class of bioactive compounds that characterize artichoke and its beneficial properties.…”

Effect of Shading on the Sesquiterpene Lactone Content and Phytotoxicity of Cultivated Cardoon Leaf Extracts

“…12 Moreover, the phytotoxic activity of C. cardunculus leaves has been correlated with the joint action of STLs, with synergistic and antagonistic interactions identified between them. 13 STLs have also been identified in fresh heads 19 but not in roots and inflorescence stems. 20 Furthermore, cynaropicrin, the major compound found in Cynara species, has been reported as an anti-inflammatory 21 agent, a cytotoxic compound against several types of cancer cells 22,23 and as an antispasmodic.…”