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

Amano, Yuki; Honda, Hiroshi; Nukada, Yuko; Ikeda, Naohiro; Yamane, Masayuki; Nakano, Koji; Kameyama, Akiyo; Morita, Osamu

doi:10.3390/ph12030110

Cited by 18 publications

(10 citation statements)

References 34 publications

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“…Therefore, the importance of the extraction process cannot be overlooked; nevertheless, the kind of coffee roast may have a significant impact. Coffee and its bioactive compounds are known to exert various beneficial pharmacological effects on humans (22). These biological effects might be attributed to their various micronutrients including caffeine, chlorogenic acid, trigonelline, tryptophan alkaloids, diterpenes, and other secondary metabolites.…”

Section: Discussionmentioning

confidence: 99%

Shifting of Physicochemical and Biological Characteristics of Coffee Roasting Under Ultrasound-Assisted Extraction

et al. 2021

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Ultrasound-assisted extraction (UAE) is an effective tool for the extraction of natural antioxidants. Thus, differentially roasted Arabica-coffee beans known as light (LC), medium (MC), and dark coffee (DC) were prepared and extracted under the influence of UAE. Following that, they were examined specifically on theirs physicochemical and biological characteristics: nutritional values, pH, °Brix, antioxidant activities, polyphenol content, caffeine, and chlorogenic-acid levels. Various parameters, such as extraction temperatures (20, 40, and 80°C) and extraction time periods (5, 10, and 20 min), were examined. DC extract was less acidic than those on MC and LC extracts. LC showed higher moisture content than the MC and DC (1.56, 1.3, and 0.92%, respectively). MC displayed the highest polyphenol content and potent antioxidant activity. Caffeine and chlorogenic acid contents trend to decrease during roasting. The maximum caffeine level was found in MC at 80°C for 5 min (27.65 mg/g extract). The highest chlorogenic acid content was in LC at 80°C for 10 min (16.67 mg/g extract). The caffeine and chlorogenic acid contents were related to the polyphenol content and depended on the roasting and extraction conditions. These results suggest that the UAE at various temperature and extraction time period may alter the physicochemical and biological characteristics of different coffee roasts.

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Section: Discussionmentioning

confidence: 99%

Shifting of Physicochemical and Biological Characteristics of Coffee Roasting Under Ultrasound-Assisted Extraction

et al. 2021

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“…As a result, the pharmacologi-cal/toxicological evaluation of 5-CQA has become increasingly important. To this end, Amano et al (2019) used in vitro and ex vivo profiling assays according to ICH S7A guideline to evaluate the safety of 5-CQA; and found that 5-CQA and its metabolites were safe to use and could have beneficial effects as a pharmaceutical.…”

Section: Pharmacological Safety Evaluationmentioning

confidence: 99%

Chlorogenic acid: A comprehensive review of the dietary sources, processing effects, bioavailability, beneficial properties, mechanisms of action, and future directions

Tian

Cui

et al. 2020

Comp Rev Food Sci Food Safe

258

179

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Chlorogenic acids (CGAs), a group of hydroxycinnamates, are generally abundant in everyday foods and beverages, most prominently in certain coffee drinks. Among them, the chlorogenic acid (CGA), also termed as 5-O-caffeoylquinic acid (5-CQA), is one of the most abundant, highly functional polyphenolic compounds in the human diet. The evidence of its health benefits obtained from clinical studies, as well as basic research, indicates an inverse correlation between 5-CQA consumption and a lower risk of metabolic syndromes and chronic diseases. This review focuses on the beneficial properties for health and mechanisms of action of 5-CQA, starting with its history, isomers, dietary sources, processing effects, preparation methods, pharmacological safety evaluation, and bioavailability. It also provides the possible molecular mechanistic bases to explain the health beneficial effects of 5-CQA including neuroprotective, cardiovascular protective, gastrointestinal protective, renoprotective, hepatoprotective, glucose and lipid metabolism regulatory, and anticarcinogenic effects. The information summarized here could aid in the basic and clinical research on 5-CQA as a natural dietary additive, potential drug candidate, as well as a natural health promoter.

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“…GRN 000869). Also, Amano et al have reported that minor gastrointestinal side effects can be observed only in very high dose of 5-CQA (>100 μM), whereas 1 g of STEE has approximately 13.86 μM of 5-CQA ( Amano et al, 2019 ). Therefore, daily intake of these polyphenols is unlikely to cause any serious side effects.…”

Section: Discussionmentioning

confidence: 99%

Sugarcane (Saccharum officinarum L.) Top Extract Ameliorates Cognitive Decline in Senescence Model SAMP8 Mice: Modulation of Neural Development and Energy Metabolism

Iwata

Ferdousi

et al. 2020

Front. Cell Dev. Biol.

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Age-related biological alterations in brain function increase the risk of mild cognitive impairment and dementia, a global problem exacerbated by aging populations in developed nations. Limited pharmacological therapies have resulted in attention turning to the promising role of medicinal plants and dietary supplements in the treatment and prevention of dementia. Sugarcane ( Saccharum officinarum L.) top, largely considered as a by-product because of its low sugar content, in fact contains the most abundant amounts of antioxidant polyphenols relative to the rest of the plant. Given the numerous epidemiological studies on the effects of polyphenols on cognitive function, in this study, we analyzed polyphenolic constituents of sugarcane top and examined the effect of sugarcane top ethanolic extract (STEE) on a range of central nervous system functions in vitro and in vivo . Orally administrated STEE rescued spatial learning and memory deficit in the senescence-accelerated mouse prone 8 (SAMP8) mice, a non-transgenic strain that spontaneously develops a multisystemic aging phenotype including pathological features of Alzheimer’s disease. This could be correlated with an increased number of hippocampal newborn neurons and restoration of cortical monoamine levels in STEE-fed SAMP8 mice. Global genomic analysis by microarray in cerebral cortices showed multiple potential mechanisms for the cognitive improvement. Gene set enrichment analysis (GSEA) revealed biological processes such as neurogenesis, neuron differentiation, and neuron development were significantly enriched in STEE-fed mice brain compared to non-treated SAMP8 mice. Furthermore, STEE treatment significantly regulated genes involved in neurotrophin signaling, glucose metabolism, and neural development in mice brain. Our in vitro results suggest that STEE treatment enhances the metabolic activity of neuronal cells promoting glucose metabolism with significant upregulation of genes, namely PGK1 , PGAM1 , PKM , and PC . STEE also stimulated proliferation of human neural stem cells (hNSCs), regulated bHLH factor expression and induced neuronal differentiation and astrocytic process lengthening. Altogether, our findings suggest the potential of STEE as a dietary intervention, with promising implications as a novel nutraceutical for cognitive health.

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

Cited by 18 publications

References 34 publications

Shifting of Physicochemical and Biological Characteristics of Coffee Roasting Under Ultrasound-Assisted Extraction

Shifting of Physicochemical and Biological Characteristics of Coffee Roasting Under Ultrasound-Assisted Extraction

Chlorogenic acid: A comprehensive review of the dietary sources, processing effects, bioavailability, beneficial properties, mechanisms of action, and future directions

Sugarcane (Saccharum officinarum L.) Top Extract Ameliorates Cognitive Decline in Senescence Model SAMP8 Mice: Modulation of Neural Development and Energy Metabolism

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