Bioavailability of Genistein and Its Glycoside Genistin As Measured in the Portal Vein of Freely Moving Unanesthetized Rats

Steensma, Aukje; Faassen-Peters, Maria; Noteborn, H.P.J.M.; Rietjens, Ivonne M. C. M.

doi:10.1021/jf060783t

Cited by 62 publications

(47 citation statements)

References 32 publications

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“…For example, genistein exposure following normal soybean exposure in Asian has been reported to be 50-100 nM [56]. The AUC (0-24h) values for total genistein and conjugates were 54, 24, and 13 μM for genistein, genistin, and enriched protein soy extract, respectively.…”

Section: ) Other Polyphenolsmentioning

confidence: 99%

“…These results indicate that the bioavailability of genistein is higher for the aglycone than for its aglycoside. Genistin is partly absorbed in its glycosidic form [56]. It is concluded that bioavailability studies based on portal vein plasma levels contribute to insight into the role of the intestine and liver in deglycosylation and uptake characteristics of glycosylated flavonoids [56].…”

Section: ) Other Polyphenolsmentioning

confidence: 99%

“…Genistin is partly absorbed in its glycosidic form [56]. It is concluded that bioavailability studies based on portal vein plasma levels contribute to insight into the role of the intestine and liver in deglycosylation and uptake characteristics of glycosylated flavonoids [56]. The C max of total genistein could reach 5.49 μmol/L when it was administrated at a single dose of 56 μmol/kg of body weight.…”

Section: ) Other Polyphenolsmentioning

confidence: 99%

“…The C max of total genistein could reach 5.49 μmol/L when it was administrated at a single dose of 56 μmol/kg of body weight. Furthermore, when orally administrated genistein at the dose level, phase II conjugates is 20-30 times higher than that of parent compound [56]. In general, isoflavones are certainly the best absorbed flavonoids: plasma concentration of 1.4-4 μmol/L are obtained between 6 and 8h in adults who consume relatively low quantities of soy derivatives supplying ≅ 50 mg isoflavones [57][58][59].…”

Section: ) Other Polyphenolsmentioning

confidence: 99%

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Natural polyphenol disposition via coupled metabolic pathways

Liu¹,

Hu²

2007

Expert Opinion on Drug Metabolism & Toxicology

127

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A major challenge associated with the development of chemopreventive polyphenols is the lack of bioavailability in vivo, which are primarily the result of coupled metabolic activities of conjugating enzymes and efflux transporters. These coupling processes are present in most of tissues and organs in mammals and are efficient for the purposes of drug metabolism, elimination and detoxification. Therefore, it was expected that these coupling processes represent a significant barrier to the oral bioavailabilities of polyphenols. In various studies of this coupling process, it was identified that various conjugating enzymes such as UGT and SULT are capable of producing very hydrophilic metabolites of polyphenols, which cannot diffuse out of the cells and needs the action of efflux transporters to pump them out of the cells. Additional studies have shown that efflux transporters such as MRP2, BCRP and OAT appear to serve as the gate keeper when there is an excess capacity to metabolize the compounds. These efflux transporters may also act as the facilitator of metabolism when there is a product/metabolite inhibition. For polyphenols, these coupled processes enable a duo recycling scheme of enteric and enterohepatic recycling, which allows the polyphenols to be reabsorbed and results in longer than expected apparent plasma half-lives for these compounds and their conjugates. Since the vast majority of polyphenols in plasma are hydrophilic conjugates, more research is needed to determine if the metabolites are active or reactive, which will help explain their mechanism of actions.

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Section: ) Other Polyphenolsmentioning

confidence: 99%

Section: ) Other Polyphenolsmentioning

confidence: 99%

Section: ) Other Polyphenolsmentioning

confidence: 99%

Section: ) Other Polyphenolsmentioning

confidence: 99%

See 2 more Smart Citations

Natural polyphenol disposition via coupled metabolic pathways

Liu¹,

Hu²

2007

Expert Opinion on Drug Metabolism & Toxicology

127

View full text Add to dashboard Cite

show abstract

“…A previous study has proved that the bioavailability of the aglycone form was higher than the glycoside form for isoflavones. 8) A study has shown that glycosylation attenuated the efficiency in inhibiting the xanthine oxidase enzyme and that the aglycone acted as an active chelator of metallic ions. 9) However, to the best of our knowledge, the preventive effect of dietary kaempferol glycoside and its aglycone on diabetes in (type 2) model mice KK-A y has not previously been reported.…”

mentioning

confidence: 99%