Abstract
For centuries, Amaranthus sp. were used as food, ornamentals, and medication. Molecular mechanisms, explaining the health beneficial properties of amaranth, are not yet understood, but have been attributed to secondary metabolites, such as phenolic compounds. One of the most abundant phenolic compounds in amaranth leaves is 2-caffeoylisocitric acid (C-IA) and regarding food occurrence, C-IA is exclusively found in various amaranth species. In the present study, the anti-inflammatory activity of C-IA, chlorogenic acid, and caffeic acid in LPS-challenged macrophages (RAW 264.7) has been investigated and cellular contents of the caffeic acid derivatives (CADs) were quantified in the cells and media. The CADs were quantified in the cell lysates in nanomolar concentrations, indicating a cellular uptake. Treatment of LPS-challenged RAW 264.7 cells with 10 µM of CADs counteracted the LPS effects and led to significantly lower mRNA and protein levels of inducible nitric oxide synthase, tumor necrosis factor alpha, and interleukin 6, by directly decreasing the translocation of the nuclear factor κB/Rel-like containing protein 65 into the nucleus. This work provides new insights into the molecular mechanisms that attribute to amaranth’s anti-inflammatory properties and highlights C-IA’s potential as a health-beneficial compound for future research.
Highlights
In ancient times, the Aztecs were the first to cultivate Amaranthus sp. for food production, as ornamental and medicinal plants [1]
caffeic acid (CA) and CQA are widespread in plants, whereas caffeoylisocitric acid (C-IA) has only been described for the genera Amaranthus and Dactylus
Based on the literature emphasizing the absorption of caffeic acid derivatives (CADs) and in amaranth species, C-IAC-IA
Summary
The Aztecs were the first to cultivate Amaranthus sp. for food production, as ornamental and medicinal plants [1]. Nutrients 2019, 11, 571 preparation of soups or stews, cooked or fried with other green vegetables as a side or main dish, or the young leaves are eaten raw in salads [1,2]. They have been used in various traditional remedies, e.g., Ayurvedic medicine, for the treatment of inflammation [1]. It remains unclear how amaranth-derived preparations facilitate anti-inflammatory action on a molecular basis
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