Chemical and Pharmacological Aspects of Caffeic Acid and Its Activity in Hepatocarcinoma

Caffeic acid (CA) is a phenolic compound synthesized by all plant species and is present in foods such as coffee, wine, tea, and popular medicines such as propolis. This phenolic acid and its derivatives have antioxidant, anti-inflammatory and anticarcinogenic activity. and studies have demonstrated...

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Vydáno v:Frontiers in oncology Ročník 9; s. 541
Hlavní autoři: Espíndola, Kaio Murilo Monteiro, Ferreira, Roseane Guimarães, Narvaez, Luis Eduardo Mosquera, Silva Rosario, Amanda Caroline Rocha, da Silva, Agnes Hanna Machado, Silva, Ana Gabrielle Bispo, Vieira, Ana Paula Oliveira, Monteiro, Marta Chagas
Médium: Journal Article
Jazyk:angličtina
Vydáno: Switzerland Frontiers Media S.A 21.06.2019
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ISSN:2234-943X, 2234-943X
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Abstract Caffeic acid (CA) is a phenolic compound synthesized by all plant species and is present in foods such as coffee, wine, tea, and popular medicines such as propolis. This phenolic acid and its derivatives have antioxidant, anti-inflammatory and anticarcinogenic activity. and studies have demonstrated the anticarcinogenic activity of this compound against an important type of cancer, hepatocarcinoma (HCC), considered to be of high incidence, highly aggressive and causing considerable mortality across the world. The anticancer properties of CA are associated with its antioxidant and pro-oxidant capacity, attributed to its chemical structure that has free phenolic hydroxyls, the number and position of OH in the catechol group and the double bond in the carbonic chain. Pharmacokinetic studies indicate that this compound is hydrolyzed by the microflora of colonies and metabolized mainly in the intestinal mucosa through phase II enzymes, submitted to conjugation and methylation processes, forming sulphated, glucuronic and/or methylated conjugates by the action of sulfotransferases, UDP-glucotransferases, and o-methyltransferases, respectively. The transmembrane flux of CA in intestinal cells occurs through active transport mediated by monocarboxylic acid carriers. CA can act by preventing the production of ROS (reactive oxygen species), inducing DNA oxidation of cancer cells, as well as reducing tumor cell angiogenesis, blocking STATS (transcription factor and signal translation 3) and suppression of MMP2 and MMP-9 (collagen IV metalloproteases). Thus, this review provides an overview of the chemical and pharmacological parameters of CA and its derivatives, demonstrating its mechanism of action and pharmacokinetic aspects, as well as a critical analysis of its action in the fight against hepatocarcinoma.
AbstractList Caffeic acid (CA) is a phenolic compound synthesized by all plant species and is present in foods such as coffee, wine, tea, and popular medicines such as propolis. This phenolic acid and its derivatives have antioxidant, anti-inflammatory and anticarcinogenic activity. and studies have demonstrated the anticarcinogenic activity of this compound against an important type of cancer, hepatocarcinoma (HCC), considered to be of high incidence, highly aggressive and causing considerable mortality across the world. The anticancer properties of CA are associated with its antioxidant and pro-oxidant capacity, attributed to its chemical structure that has free phenolic hydroxyls, the number and position of OH in the catechol group and the double bond in the carbonic chain. Pharmacokinetic studies indicate that this compound is hydrolyzed by the microflora of colonies and metabolized mainly in the intestinal mucosa through phase II enzymes, submitted to conjugation and methylation processes, forming sulphated, glucuronic and/or methylated conjugates by the action of sulfotransferases, UDP-glucotransferases, and o-methyltransferases, respectively. The transmembrane flux of CA in intestinal cells occurs through active transport mediated by monocarboxylic acid carriers. CA can act by preventing the production of ROS (reactive oxygen species), inducing DNA oxidation of cancer cells, as well as reducing tumor cell angiogenesis, blocking STATS (transcription factor and signal translation 3) and suppression of MMP2 and MMP-9 (collagen IV metalloproteases). Thus, this review provides an overview of the chemical and pharmacological parameters of CA and its derivatives, demonstrating its mechanism of action and pharmacokinetic aspects, as well as a critical analysis of its action in the fight against hepatocarcinoma.
Caffeic acid (CA) is a phenolic compound synthesized by all plant species and is present in foods such as coffee, wine, tea, and popular medicines such as propolis. This phenolic acid and its derivatives have antioxidant, anti-inflammatory and anticarcinogenic activity. In vitro and in vivo studies have demonstrated the anticarcinogenic activity of this compound against an important type of cancer, hepatocarcinoma (HCC), considered to be of high incidence, highly aggressive and causing considerable mortality across the world. The anticancer properties of CA are associated with its antioxidant and pro-oxidant capacity, attributed to its chemical structure that has free phenolic hydroxyls, the number and position of OH in the catechol group and the double bond in the carbonic chain. Pharmacokinetic studies indicate that this compound is hydrolyzed by the microflora of colonies and metabolized mainly in the intestinal mucosa through phase II enzymes, submitted to conjugation and methylation processes, forming sulphated, glucuronic and/or methylated conjugates by the action of sulfotransferases, UDP-glucotransferases, and o-methyltransferases, respectively. The transmembrane flux of CA in intestinal cells occurs through active transport mediated by monocarboxylic acid carriers. CA can act by preventing the production of ROS (reactive oxygen species), inducing DNA oxidation of cancer cells, as well as reducing tumor cell angiogenesis, blocking STATS (transcription factor and signal translation 3) and suppression of MMP2 and MMP-9 (collagen IV metalloproteases). Thus, this review provides an overview of the chemical and pharmacological parameters of CA and its derivatives, demonstrating its mechanism of action and pharmacokinetic aspects, as well as a critical analysis of its action in the fight against hepatocarcinoma.
Caffeic acid (CA) is a phenolic compound synthesized by all plant species and is present in foods such as coffee, wine, tea, and popular medicines such as propolis. This phenolic acid and its derivatives have antioxidant, anti-inflammatory and anticarcinogenic activity. In vitro and in vivo studies have demonstrated the anticarcinogenic activity of this compound against an important type of cancer, hepatocarcinoma (HCC), considered to be of high incidence, highly aggressive and causing considerable mortality across the world. The anticancer properties of CA are associated with its antioxidant and pro-oxidant capacity, attributed to its chemical structure that has free phenolic hydroxyls, the number and position of OH in the catechol group and the double bond in the carbonic chain. Pharmacokinetic studies indicate that this compound is hydrolyzed by the microflora of colonies and metabolized mainly in the intestinal mucosa through phase II enzymes, submitted to conjugation and methylation processes, forming sulphated, glucuronic and/or methylated conjugates by the action of sulfotransferases, UDP-glucotransferases, and o-methyltransferases, respectively. The transmembrane flux of CA in intestinal cells occurs through active transport mediated by monocarboxylic acid carriers. CA can act by preventing the production of ROS (reactive oxygen species), inducing DNA oxidation of cancer cells, as well as reducing tumor cell angiogenesis, blocking STATS (transcription factor and signal translation 3) and suppression of MMP2 and MMP-9 (collagen IV metalloproteases). Thus, this review provides an overview of the chemical and pharmacological parameters of CA and its derivatives, demonstrating its mechanism of action and pharmacokinetic aspects, as well as a critical analysis of its action in the fight against hepatocarcinoma.Caffeic acid (CA) is a phenolic compound synthesized by all plant species and is present in foods such as coffee, wine, tea, and popular medicines such as propolis. This phenolic acid and its derivatives have antioxidant, anti-inflammatory and anticarcinogenic activity. In vitro and in vivo studies have demonstrated the anticarcinogenic activity of this compound against an important type of cancer, hepatocarcinoma (HCC), considered to be of high incidence, highly aggressive and causing considerable mortality across the world. The anticancer properties of CA are associated with its antioxidant and pro-oxidant capacity, attributed to its chemical structure that has free phenolic hydroxyls, the number and position of OH in the catechol group and the double bond in the carbonic chain. Pharmacokinetic studies indicate that this compound is hydrolyzed by the microflora of colonies and metabolized mainly in the intestinal mucosa through phase II enzymes, submitted to conjugation and methylation processes, forming sulphated, glucuronic and/or methylated conjugates by the action of sulfotransferases, UDP-glucotransferases, and o-methyltransferases, respectively. The transmembrane flux of CA in intestinal cells occurs through active transport mediated by monocarboxylic acid carriers. CA can act by preventing the production of ROS (reactive oxygen species), inducing DNA oxidation of cancer cells, as well as reducing tumor cell angiogenesis, blocking STATS (transcription factor and signal translation 3) and suppression of MMP2 and MMP-9 (collagen IV metalloproteases). Thus, this review provides an overview of the chemical and pharmacological parameters of CA and its derivatives, demonstrating its mechanism of action and pharmacokinetic aspects, as well as a critical analysis of its action in the fight against hepatocarcinoma.
Author Espíndola, Kaio Murilo Monteiro
Silva Rosario, Amanda Caroline Rocha
Vieira, Ana Paula Oliveira
Monteiro, Marta Chagas
da Silva, Agnes Hanna Machado
Ferreira, Roseane Guimarães
Narvaez, Luis Eduardo Mosquera
Silva, Ana Gabrielle Bispo
AuthorAffiliation 1 Laboratory of In Vitro Tests, Immunology and Microbiology-LABEIM, Exact and Natural Sciences Institute, Federal University of Pará/UFPA , Belém , Brazil
3 Laboratory of In Vitro Tests, Immunology and Microbiology-LABEIM, Health Science Institute, Federal University of Pará/UFPA , Belém , Brazil
2 Laboratory of In Vitro Tests, Immunology and Microbiology-LABEIM, Biological Sciences Institute, Federal University of Pará/UFPA , Belém , Brazil
AuthorAffiliation_xml – name: 1 Laboratory of In Vitro Tests, Immunology and Microbiology-LABEIM, Exact and Natural Sciences Institute, Federal University of Pará/UFPA , Belém , Brazil
– name: 3 Laboratory of In Vitro Tests, Immunology and Microbiology-LABEIM, Health Science Institute, Federal University of Pará/UFPA , Belém , Brazil
– name: 2 Laboratory of In Vitro Tests, Immunology and Microbiology-LABEIM, Biological Sciences Institute, Federal University of Pará/UFPA , Belém , Brazil
Author_xml – sequence: 1
  givenname: Kaio Murilo Monteiro
  surname: Espíndola
  fullname: Espíndola, Kaio Murilo Monteiro
– sequence: 2
  givenname: Roseane Guimarães
  surname: Ferreira
  fullname: Ferreira, Roseane Guimarães
– sequence: 3
  givenname: Luis Eduardo Mosquera
  surname: Narvaez
  fullname: Narvaez, Luis Eduardo Mosquera
– sequence: 4
  givenname: Amanda Caroline Rocha
  surname: Silva Rosario
  fullname: Silva Rosario, Amanda Caroline Rocha
– sequence: 5
  givenname: Agnes Hanna Machado
  surname: da Silva
  fullname: da Silva, Agnes Hanna Machado
– sequence: 6
  givenname: Ana Gabrielle Bispo
  surname: Silva
  fullname: Silva, Ana Gabrielle Bispo
– sequence: 7
  givenname: Ana Paula Oliveira
  surname: Vieira
  fullname: Vieira, Ana Paula Oliveira
– sequence: 8
  givenname: Marta Chagas
  surname: Monteiro
  fullname: Monteiro, Marta Chagas
BackLink https://www.ncbi.nlm.nih.gov/pubmed/31293975$$D View this record in MEDLINE/PubMed
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ContentType Journal Article
Copyright Copyright © 2019 Espíndola, Ferreira, Narvaez, Silva Rosario, da Silva, Silva, Vieira and Monteiro. 2019 Espíndola, Ferreira, Narvaez, Silva Rosario, da Silva, Silva, Vieira and Monteiro
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Keywords caffeic acid
anticarcinogenic activity
antioxidant activity
catechol group
hepatocarcinoma
Language English
License This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) and the copyright owner(s) are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.
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This article was submitted to Pharmacology of Anti-Cancer Drugs, a section of the journal Frontiers in Oncology
Edited by: Huizi Jin, Shanghai Jiao Tong University, China
Reviewed by: Feng Qian, Shanghai Jiao Tong University, China; Marcello Locatelli, Università degli Studi G. d'Annunzio Chieti e Pescara, Italy
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Snippet Caffeic acid (CA) is a phenolic compound synthesized by all plant species and is present in foods such as coffee, wine, tea, and popular medicines such as...
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SubjectTerms anticarcinogenic activity
antioxidant activity
caffeic acid
catechol group
hepatocarcinoma
Oncology
Title Chemical and Pharmacological Aspects of Caffeic Acid and Its Activity in Hepatocarcinoma
URI https://www.ncbi.nlm.nih.gov/pubmed/31293975
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https://pubmed.ncbi.nlm.nih.gov/PMC6598430
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