Bioactive Plant Compounds in Coffee Charcoal (Coffeae carbo) Extract Inhibit Cytokine Release from Activated Human THP-1 Macrophages

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.

Caffeic Acid Modulates Processes Associated with Intestinal Inflammation

“…Unlike IL-8, caffeic acid lacked the capacity to reduce the IL-1β-induced biosynthesis of IL-6 and MCP-1. These results are in contrast with those reported in other cells lines such as THP-1-derived macrophages [ 40 ]. This suggests that caffeic acid can modulate the inflammatory response in a range of different cell types at the intestinal level, highlighting the importance of the study of different cell lines.…”

Anti-Inflammatory and Barrier-Stabilising Effects of Myrrh, Coffee Charcoal and Chamomile Flower Extract in a Co-Culture Cell Model of the Intestinal Mucosa

“…The phytochemical composition of the other two extracts has been previously investigated and described. Caffeine, trigonelline, chlorogenic acid, neochlorogenic acid, cryptochlorogenic acid, feruloylquinic acid isomers and a caffeoylquinolactone were reported as compounds of the coffee charcoal extract [ 15 ], while the extract characterization of the chamomile flower extract indicated apigenin and its glycosides as its main components, accompanied by (iso) ferulic acid glycosides [ 12 ].…”

“…The coffee charcoal extract was prepared, lyophilized and stored as previously described by Weber et al [ 15 ].…”

“…Since the phytochemical composition of the chamomile flower [ 12 ] and coffee charcoal extract [ 15 ] have been described before, the phytochemical extract characterization in this study was limited to the myrrh extract. To gain further reference substances besides furanoeudesma-1,3-diene ( 1 ) and curzerenone ( 2 ), the dried myrrh extract was separated in a liquid–liquid partition between n-heptane and methanol.…”

Adsorption Capacity of Vitamin B12 and Creatinine on Highly-Mesoporous Activated Carbons Obtained from Lignocellulosic Raw Materials

“…Among the simplest and most efficient methods of human body detoxification is enterosorption [ 4 , 5 ], a procedure for the immobilization and elimination of endogenous and exogenous metabolites from the human body [ 6 , 7 , 8 ]. Today, this method is largely employed by the majority of health clinics, the removal of poisonous species relying usually on activated carbons, lignocellulosic charcoals, animal bone charcoals, inorganic porous minerals, bone polymeric and silicon-based resins [ 9 , 10 , 11 , 12 , 13 , 14 , 15 , 16 , 17 ].…”