Comparison of oral bioavailability of genistein and genistin in rats

Kwon, Suk Hyung; Kang, Myung Joo; Huh, Jin Seo; Ha, Kyung Wook; Lee, Jeong Rai; Lee, Sang Kil; Lee, Bong Sang; Han, In Hee; Lee, Min Suk; Lee, Min Won; Lee, Jaehwi; Choi, Young Wook

doi:10.1016/j.ijpharm.2006.12.046

Cited by 99 publications

(66 citation statements)

References 24 publications

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“…Pharmacokinetic analysis showed that the serum half-life of genistein was 4.53 ± 1.40 hours in rats. 23 In the present study, the t 1/2 of genistein was 4.60 ± 0.59 hours.…”

Section: Discussionsupporting

confidence: 48%

“…For example, genistein 40 mg/kg was orally administered in a pharmacokinetic rat model, 23 and a dose of 480 mg/kg was used in another study to investigate toxicity. 24 In the present study, an intermediate dose of 100 mg/kg was administered.…”

Section: Discussionmentioning

confidence: 99%

“…A similar observation has been reported by other investigators. 23,27 In conclusion, genistein, the principal soy isoflavone, is a molecule of great interest as a lead compound in anticancer drug design and an innovative chemotherapeutic agent. However, genistein is poorly soluble in water, and the dissolution and bioavailability of the drug from the solid oral preparations are different and not reproducible.…”

Section: Discussionmentioning

confidence: 99%

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Eudragit nanoparticles containing genistein: formulation, development, and bioavailability assessment

Tang¹,

Xu²,

Ji³

et al. 2011

IJN

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Background: Genistein, one of the major isoflavones, has received great attention as a phytoestrogen and potential cancer chemoprevention agent. However, the dissolution and bioavailability of genistein from solid oral preparations is low due to its poor water solubility. Methods: In order to improve the oral bioavailability of genistein, genistein nanoparticles were prepared by the nanoprecipitation technique using Eudragit ® E100 as carriers and an optimized formulation of mass ratio (genistein:Eudragit E100, 1:10). The mean particle size of genistein nanoparticles was approximately 120 nm when diluted 100 times with distilled water. The drugloaded nanoparticles were spherical on observation by transmission electric microscopy. Results: Encapsulation efficiency and drug loading of the genistein nanoparticles were approximately 50.61% and 5.02%, respectively. Release of drug from the genistein nanoparticles was two times greater than that from the conventional capsules. After administration of genistein suspension or genistein nanoparticles at a single dose of 100 mg/kg to fasted rats, the relative bioavailability of genistein from the nanoparticles compared with the reference suspension was 241.8%. Conclusion:These results suggested that a nanoparticle system is a potentially promising formulation for the efficient delivery of poorly water-soluble drugs by oral administration.

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“…Pharmacokinetic analysis showed that the serum half-life of genistein was 4.53 ± 1.40 hours in rats. 23 In the present study, the t 1/2 of genistein was 4.60 ± 0.59 hours.…”

Section: Discussionsupporting

confidence: 48%

Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

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Eudragit nanoparticles containing genistein: formulation, development, and bioavailability assessment

Tang¹,

Xu²,

Ji³

et al. 2011

IJN

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“…Different results on the effects of glycosylation may be explained by different bioavailabilities and/or stabilities (30). Indeed, it has been reported that genistin, a glycosylated form of genistein, has greater bioavailability and greater potency in antitumor effect than its aglycon (30,31).…”

Section: Discussionmentioning

confidence: 99%

Chrysophanol-8-O-glucoside, an Anthraquinone Derivative in Rhubarb, Has Antiplatelet and Anticoagulant Activities

et al. 2012

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Abstract. Rhubarb is a widely used traditional medicine and has been reported to elicit a number of biological effects including anti-inflammatory and antiplatelet effects. In the present study, we investigated the effects of anthraquinone derivatives isolated from rhubarb on platelet activity. Of four anthraquinone derivatives isolated from rhubarb examined, chrysophanol-8-O-glucoside (CP-8-O-glc) was found to have the most potent inhibitory effect on collagen-and thrombin-induced platelet aggregation. CP-8-O-glc-treated mice showed significantly prolonged bleeding times. Furthermore, CP-8-O-glc was found to have a significant inhibitory effect on rat platelet aggregation ex vivo and on thromboxane A 2 formation in vitro. In coagulation tests, CP-8-O-glc did not alter prothrombin time, and it prolonged the activated partial thromboplastin time. However, CP-8-O-glc only inhibited platelet phosphatidylserine exposure, but not exert direct inhibition on intrinsic factors. This study demonstrates the antiplatelet and anticoagulant effects of CP-8-O-glc and suggests that this compound might be of therapeutic benefit for the prevention of plateletrelated cardiovascular diseases.

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“…The half-lives of daidzein and genistein were reported to be 9.3 and 7.1 h respectively, indicating that isoflavones or their metabolites are rapidly excreted. However, despite differences in peak levels and pharmacokinetics, whether circulating isoflavone levels differ between aglycones and isoflavone glycosides after their ingestion is still controversial (Cassidy, 2006;Kwon et al, 2007;Nielsen and Williamson, 2007). A recent report even shows a stronger effect of genistin than genistein when orally administered (Jefferson et al, 2009a), suggesting that isoflavone glycosides might be biologically more active than aglycones, despite delayed absorption.…”

Section: Soy Consumption Metabolism and Absorption Of Isoflavonesmentioning

confidence: 99%

Soy, phytoestrogens and their impact on reproductive health

Cederroth

Zimmermann

Nef

2012

Molecular and Cellular Endocrinology

193

117

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a b s t r a c tThere is growing interest in the potential health threats posed by endocrine-disrupting chemicals (EDCs) to the reproductive system. Soybean is the most important dietary source of isoflavones, an important class of phytoestrogen. While consumption of soy food or phytoestrogen supplements has been frequently associated with beneficial health effects, the potentially adverse effects on development, fertility, and the reproductive and endocrine systems are likely underappreciated. Here we review the available epidemiological, clinical and animal data on the effects of soy and phytoestrogens on the development and function of the male and female reproductive system, and weigh the evidence as to their detrimental impact.

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Comparison of oral bioavailability of genistein and genistin in rats

Cited by 99 publications

References 24 publications

Eudragit nanoparticles containing genistein: formulation, development, and bioavailability assessment

Eudragit nanoparticles containing genistein: formulation, development, and bioavailability assessment

Chrysophanol-8-O-glucoside, an Anthraquinone Derivative in Rhubarb, Has Antiplatelet and Anticoagulant Activities

Soy, phytoestrogens and their impact on reproductive health

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