Caffeic acid phenethyl ester, a promising component of propolis with a plethora of biological activities: A review on its anti-inflammatory, neuroprotective, hepatoprotective, and cardioprotective effects

IUBMB Life ◽  
2013 ◽  
Vol 65 (8) ◽  
pp. 699-709 ◽  
Author(s):  
Mai F. Tolba ◽  
Samar S. Azab ◽  
Amani E. Khalifa ◽  
Sherif Z. Abdel-Rahman ◽  
Ashraf B. Abdel-Naim
2011 ◽  
Vol 2011 ◽  
pp. 1-6 ◽  
Author(s):  
Giovana Duzzo Gamaro ◽  
Edna Suyenaga ◽  
Milene Borsoi ◽  
Joice Lermen ◽  
Patrícia Pereira ◽  
...  

Rosmarinic acid is commonly found in species of the Boraginaceae and the subfamily Nepetoideae (Lamiaceae). It has a number of interesting biological activities, for example, antiviral, antibacterial, anti-inflammatory, and antioxidant. The aim of the present study was to investigate the effect of the i.p. administration of caffeic and rosmarinic acid (5 and 10 mg/kg) on anti-inflammatory and nociceptive response using carrageenan-induced pleurisy model and tail-flick assay in rats. The analysis of cells in the pleural exudates revealed a reduction of 66% of the number of leukocytes that migrated to the pleural cavity in the animals treated with 5 mg/kg caffeic acid, and of 92.9% for the animals treated with 10 mg/kg in comparison with the control group. These exudates showed a balanced distribution of polymorphonuclear (PMN) and mononuclear (MN) cells, differently from the control group, in which PMN cells were predominant. The analysis to tail-flick latency was increased in the group treated with 10 mg/kg caffeic acid characterizing a nociceptive response. While there was no difference between control group and animals treated with rosmarinic.


2020 ◽  
Vol 11 ◽  
Author(s):  
Henrique Silva ◽  
Nuno Miguel F. Lopes

Caffeic acid (CA) and its phenethyl ester (CAPE) are naturally occurring hydroxycinnamic acids with an interesting array of biological activities; e.g., antioxidant, anti-inflammatory, antimicrobial and cytostatic. More recently, several synthetic analogs have also shown similar properties, and some with the advantage of added stability. The actions of these compounds on the cardiovascular system have not been thoroughly explored despite presenting an interesting potential. Indeed the mechanisms underlying the vascular effects of these compounds particularly need clarifying. The aim of this paper is to provide a comprehensive and up-to-date review on current knowledge about CA and its derivatives in the cardiovascular system. Caffeic acid, CAPE and the synthetic caffeic acid phenethyl amide (CAPA) exhibit vasorelaxant activity by acting on the endothelial and vascular smooth muscle cells. Vasorelaxant mechanisms include the increased endothelial NO secretion, modulation of calcium and potassium channels, and modulation of adrenergic receptors. Together with a negative chronotropic effect, vasorelaxant activity contributes to lower blood pressure, as several preclinical studies show. Their antioxidant, anti-inflammatory and anti-angiogenic properties contribute to an important anti-atherosclerotic effect, and protect tissues against ischemia/reperfusion injuries and the cellular dysfunction caused by different physico-chemical agents. There is an obvious shortage of in vivo studies to further explore these compounds’ potential in vascular physiology. Nevertheless, their favorable pharmacokinetic profile and overall lack of toxicity make these compounds suitable for clinical studies.


Biomolecules ◽  
2020 ◽  
Vol 11 (1) ◽  
pp. 31
Author(s):  
Liza Ulčakar ◽  
Marko Novinec

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.


2021 ◽  
Author(s):  
Esra DEMİR ◽  
Feyza Otan ÖZDEN ◽  
Bahattin AVCI

Abstract Caffeic acid phenethyl ester (CAPE) is an active component of propolis extracts and has anti-inflammatory, antioxidant, immunomodulatory activities. This study aims to investigate the anti-inflammatory effect of two different dosages of CAPE on lipopolysaccharide-induced experimental periodontitis (EP). Forty Sprague Dawley rats were randomly divided into four groups: control, EP, EP treated with 5 µmol/kg/day of CAPE (EP + CAPE 5), and EP treated with 10 µmol/kg/day of CAPE (EP + CAPE 10). Followed by the EP, CAPE was administered intraperitoneally to the EP + CAPE groups for 28 days. Samples were investigated biochemically using an enzyme linked immunoassay (ELISA) kit and alveolar bone loss was measured morphometrically. In both of the CAPE groups, the levels of IL-1β and TNF-α in the gingiva were significantly lower than those in the EP group (p < 0.001). The decrease in tissue levels of TNF-α was greater in the EP + CAPE 10 group than in the EP + CAPE 5 group in a dose-dependent manner. Serum analysis of the cytokines showed no significant difference between the groups. Within the limits of this study, CAPE showed its anti-inflammatory effect by reducing pro-inflammatory cytokines in gingiva and is claimed to be a novel agent in improving the results of periodontal therapy without any known side effects.


2014 ◽  
Vol 2014 ◽  
pp. 1-13 ◽  
Author(s):  
Luana Chiquetto Paracatu ◽  
Carolina Maria Quinello Gomes Faria ◽  
Camila Quinello ◽  
Camila Rennó ◽  
Patricia Palmeira ◽  
...  

Numerous anti-inflammatory properties have been attributed to caffeic acid phenethyl ester (CAPE), an active component of propolis. NADPH oxidases are multienzymatic complexes involved in many inflammatory diseases. Here, we studied the importance of the CAPE hydrophobicity on cell-free antioxidant capacity, inhibition of the NADPH oxidase and hypochlorous acid production, and release of TNF-α and IL-10 by activated leukocytes. The comparison was made with the related, but less hydrophobic, caffeic and chlorogenic acids. Cell-free studies such as superoxide anion scavenging assay, triene degradation, and anodic peak potential(Epa)measurements showed that the alterations in the hydrophobicity did not provoke significant changes in the oxidation potential and antiradical potency of the tested compounds. However, only CAPE was able to inhibit the production of superoxide anion by activated leukocytes. The inhibition of the NADPH oxidase resulted in the blockage of production of hypochlorous acid. Similarly, CAPE was the more effective inhibitor of the release of TNF-α and IL-10 byStaphylococcus aureusstimulated cells. In conclusion, the presence of the catechol moiety and the higher hydrophobicity were essential for the biological effects. Considering the involvement of NADPH oxidases in the genesis and progression of inflammatory diseases, CAPE should be considered as a promising anti-inflammatory drug.


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