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Open AccessArticle

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

1
R&D Safety Science Research, Kao Corporation, 2606 Akabane, Ichikai–Machi, Haga–Gun, Tochigi 321–3497, Japan
2
Drug Safety Testing Center Co., Ltd., 88-75 Shingou, Higashimatsuyama-shi, Saitama 355-0071, Japan
*
Authors to whom correspondence should be addressed.
These authors contributed equally.
Pharmaceuticals 2019, 12(3), 110; https://doi.org/10.3390/ph12030110
Received: 6 June 2019 / Revised: 8 July 2019 / Accepted: 9 July 2019 / Published: 17 July 2019
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Abstract

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-O-caffeoylquinic acid (5-CQA), and its metabolites, 5-O-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 1–100 µM. 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 µM CA with 4-aminopyridine, and area under the curve (AUC) and number of population spike were increased at 10 µM FA with bicuculline, dose dependency was not confirmed, and no significant changes were observed at 1 µM and by CGAs alone. In the Magnus assay, a slight increase in contraction activity was observed at >1 µM FA in the stomach fundi and 100 µM 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. View Full-Text
Keywords: safety pharmacology; chlorogenic acid; caffeoylquinic acid; coffee; adverse effects; bioactive compounds; cardiovascular system; central nervous system; gastrointestinal system safety pharmacology; chlorogenic acid; caffeoylquinic acid; coffee; adverse effects; bioactive compounds; cardiovascular system; central nervous system; gastrointestinal system
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Amano, Y.; Honda, H.; Nukada, Y.; Ikeda, N.; Yamane, M.; Nakano, K.; Kameyama, A.; Morita, O. Safety Pharmacological Evaluation of the Coffee Component, Caffeoylquinic Acid, and Its Metabolites, Using Ex Vivo and In Vitro Profiling Assays. Pharmaceuticals 2019, 12, 110.

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