Safety Pharmacological Evaluation of the Coffee Component, Caffeoylquinic Acid, and Its Metabolites, Using Ex Vivo and In Vitro Profiling Assays

• Main Authors: Yuto Amano (Author), Hiroshi Honda (Author), Yuko Nukada (Author), Naohiro Ikeda (Author), Masayuki Yamane (Author), Koji Nakano (Author), Akiyo Kameyama (Author), Osamu Morita (Author)
• Format: Book
• Published: MDPI AG, 2019-07-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.
• Notes: 1424-8247; 10.3390/ph12030110
• Keywords: safety pharmacology; chlorogenic acid; caffeoylquinic acid; coffee; adverse effects; bioactive compounds; cardiovascular system; central nervous system; gastrointestinal system; Medicine; R; Pharmacy and materia medica; RS1-441
• Source: Pharmaceuticals, Vol 12, Iss 3, p 110 (2019)

Although coffee components have gained interest for use as pharmaceuticals, little is known about their safety pharmacological effects. Hence, we aimed to evaluate the safety pharmacological effects of a chlorogenic acid (CGA)-related compound contained in coffee, 5-<i>O</i>-caffeoylquinic acid (5-CQA), and its metabolites, 5-<i>O</i>-feruloylquinic acid (5-FQA), caffeic acid (CA), and ferulic acid (FA). Langendorff perfused heart assay, electrophysiological assay of acute rat hippocampal slices, and in vitro Magnus assay of gastrointestinal tracts were conducted at 1&#8722;100 &#181;M. Moreover, in vitro profiling assays against 38 major targets were conducted. In the Langendorff assay, no significant adverse effects were observed. In the electrophysiological assay, although epileptiform discharge rates were increased at 10 &#181;M CA with 4-aminopyridine, and area under the curve (AUC) and number of population spike were increased at 10 &#181;M FA with bicuculline, dose dependency was not confirmed, and no significant changes were observed at 1 &#181;M and by CGAs alone. In the Magnus assay, a slight increase in contraction activity was observed at &gt;1 &#181;M FA in the stomach fundi and 100 &#181;M 5-CQA in the ileum, suggesting enterokinesis promotion. No significant interactions were observed in the in vitro profiling assays. Therefore, CGAs could have a fundamental function as safe pharmaceuticals.