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

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.

Mechanisms on spasmolytic and anti-inflammatory effects of a herbal medicinal product consisting of myrrh, chamomile flower, and coffee charcoal.

Inflammatory bowel disease or irritable bowel syndrome are chronic gastrointestinal disorders which are associated with a lifelong therapeutic need. The disease results in physical, psychological, and social problems with an impact on partnership, sexuality, education, and career. Thus, the number of patients and health care professionals relying on traditional and complementary medicines and especially phytotherapy for the treatment of these chronic conditions is increasing over recent years. One traditional herbal medicinal product consisting of chamomile flower, myrrh, and coffee charcoal has been widely used in clinical practice within this indication area. Long-term experience and an increasing understanding of the pharmacological mechanisms substantiate its application and clinical effectiveness. Mainly the spasmolytic and anti-inflammatory effects provide a rationale for its therapeutic application. In addition, synergistic effects between the herbal components contribute to the overall effect of this medication.

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

Recent clinical evidence suggests the efficacy of a traditional herbal medicinal product containing myrrh (Commiphora molmol Engl.), coffee charcoal (Coffea arabica L.) and chamomile flower dry extract (Matricaria chamomilla L.) in the therapy of inflammatory bowel diseases (IBD). However, the mechanisms of action in this context have not been entirely elucidated. The present study aimed to evaluate the effects of myrrh, coffee charcoal and chamomile flower extract on the inflammatory cross talk between immune and intestinal epithelial cells together with the resulting intestinal barrier disorders. A complex co-culture cell model consisting of intestinal epithelial cell (IEC) monolayers (Caco-2, HT29-MTX-E12) and macrophages (THP-1) was established for the simultaneous investigation of these two IBD characteristics. The lipopolysaccharide (LPS) activation of the macrophages led to a pro-inflammatory mediator release and thereby an inflammatory stimulation of IECs with chemokine release and reduced barrier function. The effects of the individual plant extracts and a ternary combination on inflammatory mediator release (IL-6, TNF, IL-8, MCP-1, PGE2) was quantified by ELISA. The transepithelial electrical resistance (TEER) of IEC monolayers was measured to evaluate the effects on the barrier function. Budesonide served as a positive control. All three plant extracts exhibited anti-inflammatory properties via the inhibition of the inflammatory mediator release to a varying extent. An intestinal barrier stabilising effect was observed for myrrh and coffee charcoal. Myrrh exerted the most distinct pharmacological activity. Dose reducing and synergistic interactions emerged within the threefold combination. Thus, our results provide a mechanistic basis for the use of the herbal combination of myrrh, coffee charcoal and chamomile flower extract in IBD treatment and underline the potential benefits of the phytotherapeutic multi-component/multi-target approach in this complex pathogenesis.