Ferulic Acid Is Quickly Absorbed from Rat Stomach as the Free Form and Then Conjugated Mainly in Liver

Zhao, Zhaohui; Egashira, Yukari; Sanada, Hiroo

doi:10.1093/jn/134.11.3083

Cited by 195 publications

(187 citation statements)

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“…The acute oral LD 50 of FA in male and female F344 rats was 2445 mg.kg -1 and 2133 mg.kg , respectively (Tada et al, 1999). Both free and linked FA are quickly absorbed from the stomach without modification due to acid pH, according to studies carried out in situ in the rat stomach, but it was verified that only the free form of the acid was absorbed by the intestine after administration of 8 µmol FA / kg body weight (Zhao et al, 2004).…”

Section: Preclinical Pharmacokineticmentioning

confidence: 99%

Section: Preclinical Pharmacokineticmentioning

confidence: 99%

“…Only 0.5-0.8% is found in feces of mice (Zhao et al, 2003). After absorption, about 50% of FA reaches the liver, and the remainder is distributed in the bloodstream, gastric mucosa and peripheral tissues (Adam et al, 2002;Zhao et al, 2004;Silberberg et al, 2006). Chang et al (1993) administered pure FA in Wistar rats and found that the free acid did not enter the enterohepatic circulation.…”

mentioning

confidence: 99%

“…Conjugation was required for its distribution in the organism. The conjugation reactions of FA occur mainly in the liver but may also occur in the intestinal mucosa or kidney, catalyzed by sulfotransferases (EC 2.8.2.1) and UDP glucuronosyl transferases (EC 2.4.1.17) (Piskula, Terao, 1998;Kern et al, 2003;Zhao et al, 2004). Studies in humans and rats showed that after oral intake of FA, the most abundant metabolites generated in plasma were FA-glucuronide (FA conjugate with glucuronic acid) and FA-sulfoglucuronide (FA conjugate with sulfate and glucuronide) in addition to unmodified FA.…”

mentioning

confidence: 99%

“…Studies in humans and rats showed that after oral intake of FA, the most abundant metabolites generated in plasma were FA-glucuronide (FA conjugate with glucuronic acid) and FA-sulfoglucuronide (FA conjugate with sulfate and glucuronide) in addition to unmodified FA. The studies indicated that concentrations of metabolites derived from FA ingestion are a function of several factors such as the dose and route administered, as well as the animal species (Zhao et al, 2003(Zhao et al, , 2004.Free phenolic acids can be absorbed via paracellular transport and active transport mediated by monocarboxylic acids transporters (MCT) in the gastrointestinal mucosa. According to Konishi et al (2006) the absorption efficiency of each phenolic acid depends on its affinity for the MCT.…”

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confidence: 99%

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Ferulic acid and derivatives: molecules with potential application in the pharmaceutical field

Brenelli

Goldbeck

Santos

et al. 2013

Braz. J. Pharm. Sci.

155

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Ferulic acid is a phenolic acid widely distributed in the plant kingdom. It presents a wide range of potential therapeutic effects useful in the treatments of cancer, diabetes, lung and cardiovascular diseases, as well as hepatic, neuro and photoprotective effects and antimicrobial and anti-inflammatory activities. Overall, the pharmaceutical potential of ferulic acid can be attributed to its ability to scavenge free radicals. However, recent studies have revealed that ferulic acid presents pharmacological properties beyond those related to its antioxidant activity, such as the ability to competitively inhibit HMG-CoA reductase and activate glucokinase, contributing to reduce hypercholesterolemia and hyperglycemia, respectively. The present review addresses ferulic acid dietary sources, the pharmacokinetic profile, antioxidant action mechanisms and therapeutic effects in the treatment and prevention of various diseases, in order to provide a basis for understanding its mechanisms of action as well as its pharmaceutical potential.Uniterms: Ferulic acid/properties. Ferulic acid/antioxidant activity. Ferulic acid/dietary sources. Ferulic acid/therapeutic effects. Natural products. Pharmacognosy.O ácido ferúlico é um ácido fenólico amplamente distribuído no reino vegetal. Ele apresenta uma ampla gama de potenciais efeitos terapêuticos utéis no tratamento do câncer, diabetes, doenças pulmonares e cardiovasculares, bem como efeitos hepáticos, neuro e fotoprotetores, atividades antimicrobianas e antiinflamatórias. O potencial farmacêutico do ácido ferúlico pode ser atribuído à sua capacidade em sequestrar radicais livres. No entanto, estudos recentes revelaram que o ácido ferúlico apresenta propriedades farmacológicas, além da sua atividade antioxidante, como a capacidade de inibir competitivamente a HMG-CoA redutase e ativar a glucoquinase, contribuindo para reduzir a hipercolesterolemia e hiperglicemia, respectivamente. A presente revisão aborda as fontes dietéticas de ácido ferúlico, o perfil farmacocinético, os mecanismos de ação como antioxidante e efeitos terapêuticos no tratamento e prevenção de várias doenças, de modo a proporcionar uma base para a compreensão dos seus mecanismos de ação, bem como os seus potenciais farmacêuticos.Unitermos: Ácido ferúlico/propriedades. Ácido ferúlico/atividade antioxidante. Ácido ferúlico/fontes dietéticas. Ácido ferúlico/efeitos terapêuticos. Produtos naturais. Farmacognosia. INTRODUCTIONNatural antioxidants exhibit therapeutic potential for a variety of diseases such as cancer, diabetes, and cardiovascular and neurodegenerative diseases (Kayahara et al., 1999;Kim et al., 2003;Soobrattee et al., 2005) where free radicals play a key role in development (Prior et al., 1998). Recently there has been increased public and scientific interest in employing natural antioxidants instead of synthetic antioxidants, due to their potential adverse effects on health which may include carcinogenicity (Ito et al., 1983;Würtzen, 1990;Osawa et al., 1990).Antioxidants found in vegetables can ac...

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Section: Preclinical Pharmacokineticmentioning

confidence: 99%

Section: Preclinical Pharmacokineticmentioning

confidence: 99%

mentioning

confidence: 99%

mentioning

confidence: 99%

mentioning

confidence: 99%

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Ferulic acid and derivatives: molecules with potential application in the pharmaceutical field

Brenelli

Goldbeck

Santos

et al. 2013

Braz. J. Pharm. Sci.

155

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Bioavailability of Flavanols and Phenolic Acids

Poquet

Clifford

Williamson

2009

Plant Phenolics and Human Health

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Role, Importance and Biosynthesis of Cell Wall‐Bound Phenolic Acids in Cereals

Hassan

Burton

2018

Annual Plant Reviews Online

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Ferulic acid (FA) and p ‐coumaric acid (pCA) are the most abundant phenolic acids in cereals contributing 70–80% of the total phenolic acid pool (Harris and Hartley, 1980; Van Hung, 2016). They have roles in human health and nutrition (Van Hung, 2016) and cell wall cross‐linking in planta (de O Buanafina, 2009). These compounds are mainly bound to arabinoxylan polysaccharides and lignin polymers in cereals (Molinari et al., 2013). Such linkages may affect properties of the cell wall including adhesion and rigidity (Barrière et al., 2004), and might also limit the availability of wall polysaccharides in downstream processes due to the formation of polysaccharide–polysaccharide and polysaccharide–lignin complexes (Iiyama et al., 1990; Jung et al., 2012). Biosynthetic pathways that lead to the production of these phenolic compounds and their incorporation into the plant cell walls are complicated and there is still much to be understood. This article will cover the applications of cell wall‐bound phenolic acids, focusing on health benefits, and will discuss the possible routes currently thought to exist for the generation and incorporation of these compounds into the cell wall.

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Ferulic Acid Is Quickly Absorbed from Rat Stomach as the Free Form and Then Conjugated Mainly in Liver

Cited by 195 publications

References 32 publications

Ferulic acid and derivatives: molecules with potential application in the pharmaceutical field

Ferulic acid and derivatives: molecules with potential application in the pharmaceutical field

Bioavailability of Flavanols and Phenolic Acids

Role, Importance and Biosynthesis of Cell Wall‐Bound Phenolic Acids in Cereals

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