Abstract
Due to certain differences in terms of molecular structure, isoquinoline alkaloids from Chelidonium majus engage in various biological activities. Apart from their well-documented antimicrobial potential, some phenanthridine and protoberberine derivatives as well as C. majus extract present with anti-inflammatory and cytotoxic effects. In this study, the LC–MS/MS method was used to determine alkaloids, phenolic acids, carboxylic acids, and hydroxybenzoic acids. We investigated five individually tested alkaloids (coptisine, berberine, chelidonine, chelerythrine, and sanguinarine) as well as C. majus root extract for their effect on the secretion of IL-1β, IL-8, and TNF-α in human polymorphonuclear leukocytes (neutrophils). Berberine, chelidonine, and chelerythrine significantly decreased the secretion of TNF-α in a concentration-dependent manner. Sanguinarine was found to be the most potent inhibitor of IL-1β secretion. However, the overproduction of IL-8 and TNF-α and a high cytotoxicity for these compounds were observed. Coptisine was highly cytotoxic and slightly decreased the secretion of the studied cytokines. The extract (1.25–12.5 μg/mL) increased cytokine secretion in a concentration-dependent manner, but an increase in cytotoxicity was also noted. The alkaloids were active at very low concentrations (0.625–2.5 μM), but their potential cytotoxic effects, except for chelidonine and chelerythrine, should not be ignored.
Highlights
Isoquinoline alkaloids contained in Chelidonium majus L. extracts have been found to be some of the most potent molecules against bacteria, viruses, fungi, and protozoa [1]
In an intact tonoplast and vacuole vesicle system, berberine uptake was stimulated by Mg/pyrophosphate, Mg/adenosine triphosphate (ATP), guanosine-50 -triphosphate (GTP), cytidine triphosphate (CTP), and uridine-50 -triphosphate (UTP)
The results of our research indicate that coptisine and sanguinarine had the largest effect in terms of the mechanisms associated with the development of a cytotoxic effect in LPS-stimulated human neutrophils
Summary
Isoquinoline alkaloids contained in Chelidonium majus L. extracts have been found to be some of the most potent molecules against bacteria, viruses, fungi, and protozoa [1]. This group of compounds is represented mostly by phenanthridine, protoberberine, and protopine derivatives. According to the available literature, roots contain up to 4% alkaloids, while the aerial parts contain 0.1–1% (with the exception of coptisine, which is much more abundant, especially in fruits). Due to differences in their molecular structures, C. majus alkaloids engage in different biological activities [1]. Quaternary nitrogen in molecules, e.g., in chelerythrine, sanguinarine, berberine, or coptisine, has been found to be involved in the inhibition of cellular respiration, whereas the presence of an imine moiety in the structures of sanguinarine and chelerythrine determines the ability of these compounds to inhibit the activity of proteins and enzymes [5]
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