Insights into In Vivo Absolute Oral Bioavailability, Biotransformation, and Toxicokinetics of Zearalenone, α-Zearalenol, β-Zearalenol, Zearalenone-14-glucoside, and Zearalenone-14-sulfate in Pigs

104

One of the concerns when using grain ingredients in feed formulation for livestock and poultry diets is mycotoxin contamination. Aflatoxin, fumonisin, ochratoxin, trichothecene (deoxynivalenol, T-2 and HT-2) and zearalenone (ZEN) are mycotoxins that have been frequently reported in animal feed. ZEN, which has raised additional concern due to its estrogenic response in animals, is mainly produced by Fusarium graminearum (F. graminearum), F. culmorum, F. cerealis, F. equiseti, F. crookwellense and F. semitectums, and often co-occurs with deoxynivalenol in grains. The commonly elaborated derivatives of ZEN are α-zearalenol, β-zearalenol, zearalanone, α-zearalanol, and β-zearalanol. Other modified and masked forms of ZEN (including the extractable conjugated and non-extractable bound derivatives of ZEN) have also been quantified. In this review, common dose of ZEN in animal feed was summarized. The absorption rate, distribution (“carry-over”), major metabolites, toxicity and estrogenicity of ZEN related to poultry, swine and ruminants are discussed.

Section: Zen Toxicity and Estrogenic Effect In Livestock Animalsmentioning

confidence: 99%

Zearalenone (ZEN) in Livestock and Poultry: Dose, Toxicokinetics, Toxicity and Estrogenicity

Liu

Applegate

2020

104

“…Both deoxynivalenol (DON, 38) and zearalenone (ZEN, 33) were converted to their corresponding sulfates DON 3-sulfate (126) and ZEN 14-sulfate (127) ( Figure S63) by the fungus Sphaerodes mycoparasitica [87]. ZEN (33) was also found to be converted to ZEN 14-sulfate (127) by pigs [103]. Both DON 3-sulfate (126) and ZEN 14-sulfate (127) were less toxic than DON (38) and ZEN (33), respectively [87].…”

Section: Sulfationmentioning

confidence: 99%

Detoxification of Mycotoxins through Biotransformation

Yin

et al. 2020

Mycotoxins are toxic fungal secondary metabolites that pose a major threat to the safety of food and feed. Mycotoxins are usually converted into less toxic or non-toxic metabolites through biotransformation that are often made by living organisms as well as the isolated enzymes. The conversions mainly include hydroxylation, oxidation, hydrogenation, de-epoxidation, methylation, glycosylation and glucuronidation, esterification, hydrolysis, sulfation, demethylation and deamination. Biotransformations of some notorious mycotoxins such as alfatoxins, alternariol, citrinin, fomannoxin, ochratoxins, patulin, trichothecenes and zearalenone analogues are reviewed in detail. The recent development and applications of mycotoxins detoxification through biotransformation are also discussed.

“…ZEA is mainly biotransformed into α-zearalenol (α-ZEA), which shows the highest binding affinity to human and porcine estrogen receptors, whereas in broilers and rats, β-zearalenol (β-ZEA) with the low affinity to the receptor is predominantly produced [ 103 , 104 , 105 ]. ZEA upregulates mainly mRNA levels of CYP2B6, CYP3A4, CYP1A2 and CYP1A1, followed by CYP3A5 and CYP2C9, together with activation of their transcriptional regulators—aryl the hydrocarbon receptor (AhR), constitutive androstane receptor (CAR), and pregnane X receptor (PXR) [ 106 ].…”

Section: Biotransformation Of Mycotoxinsmentioning

confidence: 99%

Mycotoxins: Biotransformation and Bioavailability Assessment Using Caco-2 Cell Monolayer

Tran

Viktorová

Ruml

2020

The determination of mycotoxins content in food is not sufficient for the prediction of their potential in vivo cytotoxicity because it does not reflect their bioavailability and mutual interactions within complex matrices, which may significantly alter the toxic effects. Moreover, many mycotoxins undergo biotransformation and metabolization during the intestinal absorption process. Biotransformation is predominantly the conversion of mycotoxins meditated by cytochrome P450 and other enzymes. This should transform the toxins to nontoxic metabolites but it may possibly result in unexpectedly high toxicity. Therefore, the verification of biotransformation and bioavailability provides valuable information to correctly interpret occurrence data and biomonitoring results. Among all of the methods available, the in vitro models using monolayer formed by epithelial cells from the human colon (Caco-2 cell) have been extensively used for evaluating the permeability, bioavailability, intestinal transport, and metabolism of toxic and biologically active compounds. Here, the strengths and limitations of both in vivo and in vitro techniques used to determine bioavailability are reviewed, along with current detailed data about biotransformation of mycotoxins. Furthermore, the molecular mechanism of mycotoxin effects is also discussed regarding the disorder of intestinal barrier integrity induced by mycotoxins.