Pharmacological action and potential targets of chlorogenic acid

Miao, Mingsan; Xiang, Lin

doi:10.1016/bs.apha.2019.12.002

Cited by 142 publications

(101 citation statements)

References 41 publications

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“…Here, we found CA is effective to depress PDAC cell growth in vitro and in vivo by inducing cell cycle arrest, which was consistent with the tumor suppressive activity of CA in other cancer types (Miao & Xiang, 2020). Importantly, we validated that CA significantly interrupted mitochondrial respiration and slightly repressed aerobic glycolysis which suggested a potential role of CA in modulating cancer cell metabolism and revealed a novel mechanism of CA in cancer therapy.…”

Section: Discussionsupporting

confidence: 88%

“…Previous studies have evaluated potential anti‐tumor activity of CA in multiple cancer types, including lung cancer, breast cancer, colon cancer, and hepatocellular carcinoma (Miao & Xiang, 2020). However, the tumor suppressive activity of CA in pancreatic carcinoma remains to be evaluated.…”

Section: Resultsmentioning

confidence: 99%

“…Presently, multiple groups have found that certain natural compounds showed potential antitumor activity. Among them, chlorogenic Acid (CA) is considered a potentially promising compound for cancer therapy (Miao & Xiang, 2020). CA is one of the main anti‐bacterial and anti‐viral effective pharmacological components of honeysuckle.…”

Section: Introductionmentioning

confidence: 99%

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Chlorogenic acid depresses cellular bioenergetics to suppress pancreatic carcinoma through modulating c‐Myc‐TFR1 axis

Yang

Said

Huang

et al. 2020

Phytotherapy Research

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Pancreatic ductal adenocarcinoma (PDAC) is severe malignant tumor in human, the outcomes of PDAC is extremely poor. Here, we evaluated the potential anti‐tumor activity of chlorogenic Acid (CA) in PDAC. Here, we found CA was effective to suppress PDAC cell growth in vitro and in vivo. Importantly, we found overall oxygen consumption rate was significantly decreased in CA dose‐dependent manner. We also found glycolysis reverse was decreased in CA‐treated cells, while basal glycolysis and glycolytic capacity were not significantly changed. Mechanistically, we demonstrated TFR1 could be a novel downstream target of CA, which is essential for PDAC cell growth and cellular bioenergetics maintenance. Furthermore, we validated that CA‐reduced c‐Myc resulted to down‐regulation of TFR1, which contributes to mitochondrial respiration dysfunction and cell growth delay. Together, this study indicates that CA suppresses PDAC cell growth through targeting c‐Myc‐TFR1 axis and suggests CA could be considered as a promising compound for PDAC treatment.

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Section: Discussionsupporting

confidence: 88%

Section: Resultsmentioning

confidence: 99%

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Chlorogenic acid depresses cellular bioenergetics to suppress pancreatic carcinoma through modulating c‐Myc‐TFR1 axis

Yang

Said

Huang

et al. 2020

Phytotherapy Research

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“…Importantly, coffee has a diversity of other bioactive constituents apart from caffeine, amongst which stem chlorogenic acids 21 . As most polyphenols, chlorogenic acids have been described as potent antioxidants 22 and several studies have shown an ability of chlorogenic acids to affect brain function 23 – 27 . Thus, interventions with diets enriched in chlorogenic acids ameliorate mood 22 , 23 and cognitive function 25 , 26 in volunteers.…”

Section: Introductionmentioning

confidence: 99%

Neuromodulation and neuroprotective effects of chlorogenic acids in excitatory synapses of mouse hippocampal slices

Fernandes

Dobrachinski

Silva

et al. 2021

Sci Rep

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The increased healthspan afforded by coffee intake provides novel opportunities to identify new therapeutic strategies. Caffeine has been proposed to afford benefits through adenosine A2A receptors, which can control synaptic dysfunction underlying some brain disease. However, decaffeinated coffee and other main components of coffee such as chlorogenic acids, also attenuate brain dysfunction, although it is unknown if they control synaptic function. We now used electrophysiological recordings in mouse hippocampal slices to test if realistic concentrations of chlorogenic acids directly affect synaptic transmission and plasticity. 3-(3,4-dihydroxycinnamoyl)quinic acid (CA, 1–10 μM) and 5-O-(trans-3,4-dihydroxycinnamoyl)-D-quinic acid (NCA, 1–10 μM) were devoid of effect on synaptic transmission, paired-pulse facilitation or long-term potentiation (LTP) and long-term depression (LTD) in Schaffer collaterals-CA1 pyramidal synapses. However, CA and NCA increased the recovery of synaptic transmission upon re-oxygenation following 7 min of oxygen/glucose deprivation, an in vitro ischemia model. Also, CA and NCA attenuated the shift of LTD into LTP observed in hippocampal slices from animals with hippocampal-dependent memory deterioration after exposure to β-amyloid 1–42 (2 nmol, icv), in the context of Alzheimer’s disease. These findings show that chlorogenic acids do not directly affect synaptic transmission and plasticity but can indirectly affect other cellular targets to correct synaptic dysfunction. Unraveling the molecular mechanisms of action of chlorogenic acids will allow the design of hitherto unrecognized novel neuroprotective strategies.

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“…Many of these are known not only for their antioxidant properties [ 1 ] but also for their beneficial health effects in traditional medicine and as food supplements, as well as potential application in standard medicine. An important group of such compounds is cinnamic acid and its derivatives, which have antimicrobial, antitumor, anti-inflammatory and other biological activities [ 2 , 3 , 4 , 5 ]. At the molecular level, this is due to their well-known antioxidative properties [ 1 , 6 ] but also specific interactions with protein targets.…”

Section: Introductionmentioning

confidence: 99%

Inhibition of Human Cathepsins B and L by Caffeic Acid and Its Derivatives

Ulčakar

Novinec

2020

Biomolecules

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Caffeic acid (CA) and its derivatives caffeic acid phenethyl ester (CAPE) and chlorogenic acid (CGA) are phenolic compounds of plant origin with a wide range of biological activities. Here, we identify and characterize their inhibitory properties against human cathepsins B and L, potent, ubiquitously expressed cysteine peptidases involved in protein turnover and homeostasis, as well as pathological conditions, such as cancer. We show that CAPE and CGA inhibit both peptidases, while CA shows a preference for cathepsin B, resulting in the strongest inhibition among these combinations. All compounds are linear (complete) inhibitors acting via mixed or catalytic mechanisms. Cathepsin B is more strongly inhibited at pH 7.4 than at 5.5, and CA inhibits its endopeptidase activity preferentially over its peptidyl-dipeptidase activity. Altogether, the results identify the CA scaffold as a promising candidate for the development of cathepsin B inhibitors, specifically targeting its endopeptidase activity associated with pathological proteolysis of extracellular substrates.

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Pharmacological action and potential targets of chlorogenic acid

Cited by 142 publications

References 41 publications

Chlorogenic acid depresses cellular bioenergetics to suppress pancreatic carcinoma through modulating c‐Myc‐TFR1 axis

Chlorogenic acid depresses cellular bioenergetics to suppress pancreatic carcinoma through modulating c‐Myc‐TFR1 axis

Neuromodulation and neuroprotective effects of chlorogenic acids in excitatory synapses of mouse hippocampal slices

Inhibition of Human Cathepsins B and L by Caffeic Acid and Its Derivatives

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