Possible molecular targets for therapeutic applications of caffeic acid phenethyl ester in inflammation and cancer

Abstract

Of the various derivatives of caffeic acid, caffeic acid phenethyl ester (CAPE) is a hydrophobic, bioactive polyphenolic ester obtained from propolis extract. The objective in writing this review article was to summarize all published studies on therapeutics of CAPE in inflammation and cancer to extract direction for future research. The possible molecular targets for the action of CAPE, include various transcription factors such as nuclear factor-κB, tissue necrosis factor-α, interleukin-6, cyclooxygenase-2, Nrf2, inducible nitric oxide synthase, nuclear factor of activated T cells, hypoxia-inducible factor-1α, and signal transducers and activators of transcription. Based on the valuable data on its therapeutics in inflammation and cancer, clinical studies of CAPE should also be conducted to explore its toxicities, if any.

Phytotherapeutics: The Emerging Role of Intestinal and Hepatocellular Transporters in Drug Interactions with Botanical Supplements

“…The molecular transport systems involved in nutrient uptake into the liver are well documented [ 12 ]. Apart from transporters involved in nutrient uptake, the intestine and the liver cells express other transporters that mediate the uptake of xenobiotics, for example flavonoids [ 13 , 14 , 15 ].…”

“…Another study described the estrone-3-sulfate uptake inhibition by the green tea catechins EGCG and ECG in the cells expressing OATP1A2, OATP1B1 and OATP2B1 [ 62 ]. It is also found in cytotoxicity studies that EGCG is transported by OATO1B3 [ 15 ]. Remarkably, the average concentration of EGCG and ECG in the brewed green tea was approximately 400 μM, so that the maximal concentrations were in the low millimolar range [ 62 ].…”

Induction of Cell Cycle Arrest and Apoptotic Response of Head and Neck Squamous Carcinoma Cells (Detroit 562) by Caffeic Acid and Caffeic Acid Phenethyl Ester Derivative

“…Organic phenolic compounds including caffeic acid (CA) and its derivative caffeic acid phenethyl ester (CAPE) are known to be highly bioactive components extracted from honeybee hive propolis [ 12 , 13 ]. Recent studies indicate that they exhibit cytotoxic, antiproliferative [ 14 , 15 ], anti-inflammatory, immunomodulatory [ 16 , 17 ], antioxidative [ 17 – 20 ], and antibacterial properties [ 17 , 21 ].…”

A novel nanoparticle loaded with methyl caffeate and caffeic acid phenethyl ester against Ralstonia solanacearum—a plant pathogenic bacteria

“…6B, the expression levels of phcA in the blank and API groups were 1.3 and 1.9 times those of the nanoparticle group, respectively. CAPE has a certain inhibitory effect on the various transcription factors (such as interleukin-6 and cyclooxygenase-2) and transcriptional activators in cells, 46 which may lead to the decreased expression of phcA. Further, the decreased expression of phcA might be one of the reasons for the decreased motility and the formation of a biolm.…”