Abstract
The herbal preparation coffee charcoal is produced by over-roasting and milling green dried Coffea arabica L. seeds, and has a long-standing tradition in the treatment of inflammatory and gastrointestinal disorders. Its therapeutic properties are commonly attributed to adsorptive and astringent effects. This insufficiently explains its mode of action, especially when used in the treatment of inflammatory diseases in lower dosages. Our investigations aimed to identify bioactive secondary plant metabolites affecting cytokine-signaling. Thus, a phytochemical analysis of coffee charcoal extract was conducted using HPLC and LC/MS. Trigonelline, neochlorogenic acid, chlorogenic acid, caffeine, cryptochlorogenic acid, feruloylquinic acid isomers, and a caffeoylquinolacton were identified in the extract. Subsequently, the effects of coffee charcoal extract, chlorogenic acid isomers, their metabolite caffeic acid, caffeine, and trigonelline on cytokine (TNF, IL-6, MCP-1) release from LPS-challenged human THP-1 macrophages were examined to evaluate anti-inflammatory activity. Coffee charcoal showed concentration-dependent mild-to-medium inhibitory effects. The chlorogenic acid isomers and caffeic acid inhibited the TNF release, with cryptochlorogenic acid exerting the most distinct effects, as well as decreasing the release of IL-6 and MCP-1. In addition, scanning electron microscopic images provided an impression of the particle constitution, indicating a larger particle size and less structured surface of coffee charcoal in comparison to activated charcoal. In conclusion, our findings underline that beyond adsorptive effects, coffee charcoal exhibits pharmacological properties, which derive from a spectrum of secondary plant metabolites and support the therapeutic use in inflammatory diseases. Chlorogenic acids, particularly cryptochlorogenic acid, appear as pivotal bioactive compounds.
Highlights
Coffee charcoal, referred to as Coffeae carbo, is a herbal preparation with a long tradition in the treatment of inflammatory disorders
The application of coffee charcoal in the treatment of inflammation and gastrointestinal disorders is based on a long-standing tradition
To gain a better understanding about the mechanisms eliciting the therapeutic qualities of coffee charcoal, this study aimed to identify secondary plant metabolites and examine their influence on pro-inflammatory mediator release from activated macrophages
Summary
Referred to as Coffeae carbo, is a herbal preparation with a long tradition in the treatment of inflammatory disorders. It was introduced into medical practice in 1937 by August G. Coffee charcoal is produced by roasting green dried Coffea arabica L. seeds to blackening on Molecules 2019, 24, 4263; doi:10.3390/molecules24234263 www.mdpi.com/journal/molecules. The name might suggest it, the resulting product is not a charred, carbonized charcoal, but rather over-roasted coffee, which still contains a considerable amount of secondary plant substances like caffeine, trigonelline, chlorogenic acid, and caffeic acid. Traditional areas of application range from angina, paradontosis, and migraine to wound care, diarrhea, and other functional and inflammatory disorders of the gastrointestinal tract [1,2,3,4,5]
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