Toxicological evaluation of the isoflavone puerarin and its glycosides

Chung, Hyuk Jin; Chung, Mi Ja; Houng, Soung Jin; Jeun, Jungae; Kweon, Dong Keon; Choi, Chung; Park, Jong-Tae; Park, Kwan Hwa; Lee, Sung Joon

doi:10.1007/s00217-009-1156-3

Cited by 33 publications

(18 citation statements)

References 26 publications

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“…It is also important to note that the bioavailability of puerarin in vivo is often limited by its insolubility. A recent report documents that enzymatic modification of puerarin to puerarin glycoside increases the solubility O100-fold (Chung et al 2009); however, it remains to be ascertained if the pregnancy-terminating potential of puerarin is retained by its glycosidic form. Moreover, puerarin nanoparticles are reported to have good stability, enhanced intestinal absorption and increased bioavailability after oral administration (Liu et al 2009, Wu et al 2009).…”

Section: Discussionmentioning

confidence: 99%

“…But a recent report on toxicological evaluation in rats demonstrates that puerarin and its glycosides are not mutagenic, rather they exert anti-mutagenic effects and do not have significant toxic effects at doses of up to 250 mg/kg per day for 28 days (Chung et al 2009). The high MED of puerarin in rats, therefore, should not be a major strategic constraint in exploring its future potential as antifertility agent.…”

Section: Discussionmentioning

confidence: 99%

“…The high MED of puerarin in rats, therefore, should not be a major strategic constraint in exploring its future potential as antifertility agent. Moreover, puerarin and puerarincontaining plants have many therapeutic applications in traditional medicine (Chung et al 2009), which suggests that this drug is not unacceptably toxic. The present findings, however, raise the issue if therapeutic uses of puerarin are contraindicated in pregnancy.…”

Section: Discussionmentioning

confidence: 99%

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Puerarin, a selective oestrogen receptor modulator, disrupts pregnancy in rats at pre-implantation stage

Saha¹,

Saraswat²,

Chakraborty³

et al. 2012

Reproduction

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The tubers of Pueraria tuberosa have folkloric repute as emmenagogue. The n-BuOH fraction of the ethanolic extract of tubers exhibits significant antifertility activity in laboratory animals. The present investigation explored the active principle(s) of the tuber extract with reference to contragestive effects in rats and probed the possible mechanism of action. Bioactivity-guided fractionation identified puerarin as the major constituent that exerted pregnancy-terminating effects. Oral administration of puerarin at R300 mg/kg per day for days (D) 1-2 post-coitus resulted in complete implantation failure. Serum oestradiol levels during D2-D5 and progesterone (P 4 ) level on D5 remained unaffected, but the endometrial expression of oestrogen receptor a (ERa) and ERb was adversely modulated that disrupted the implantation-specific characteristic endometrial oestrogenic milieu. The eventual consequence was loss of endometrial receptivity characterised by down-regulation of the uterine expression of P 4 receptor (PR) and attenuation of endometrial expression of leukaemia inhibitory factor, vascular endothelial growth factor and cyclo-oxygenase-2, the three important signalling molecules involved in the process of implantation. Light microscopic examination of the embryos demonstrated no untoward effect of puerarin on the development of embryos until D4, but D5 blastocysts underwent gross morphological distortion. The findings taken together are interpreted to suggest that puerarin adversely impacts the uterine expression of ER and PR that disrupts the implantation-conducive uterine milieu and prevents implantation. In conclusion, puerarin may be envisaged as a prospective molecule that merits further exploration for the development of non-steroidal post-coital contraceptive for women.

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Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

See 1 more Smart Citation

Puerarin, a selective oestrogen receptor modulator, disrupts pregnancy in rats at pre-implantation stage

Saha¹,

Saraswat²,

Chakraborty³

et al. 2012

Reproduction

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“…and i.g. LD 50 of Puerariae total flavones was up to 5.97 and 10.11 g/kg for rats . The LD 50 and approximate lethal dosage (ALD) of Radix Puerariae water extract in both female and male ICR mice were found to be over 2000 mg/kg .…”

Section: Toxicitymentioning

confidence: 99%

RadixPuerariae: An overview of Its Chemistry, Pharmacology, Pharmacokinetics, and Clinical Use

Zhang

Lam

Zuo

2013

The Journal of Clinical Pharmacology

192

130

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Radix Puerariae has been traditionally used for the treatment of diarrhea, acute dysentery, deafness and cardiovascular diseases. Yege (Gegen or Radix Puerariae lobatae), the dried root of Pueraria lobata (Wild.) Ohwi, has been widely used in China and, to a lesser extent, in Japan, Korea, and the United States. Although they have been classified into different categories in Chinese Pharmacopoeia, Yege is often used interchangeably in practice with Fenge (Radix Puerariae thomsonii), which is the dried root of Pueraria thomsonii Benth. Among various commercially available products of Radix Puerariae, injection of puerarin, the major isoflavone from Radix Puerariae, has been most widely used as a vasodilator for the treatment of angina and myocardial infarction. Considering the extensive clinical usage and recent alert of fatal herb-drug interaction of Radix Puerariae, the current review is proposed to cover its traditional applications, pharmacological activities, pharmacokinetics, clinical efficacy, and potential herb-drug interactions aiming to fill in the information gaps of this herb for frontline practitioners. Although various small, poorly designed clinical trials have demonstrated the safety, efficacy, and significant clinical benefits of Radix Puerariae, prospective randomized controlled clinical trials are needed to further establish its effective and safe use.

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“…The Er:YAG powder was obtained by a nitrate-citrate solgel method [11]. Aqueous solutions of Y(NO 3 O) 2 M, in a molar ratio citric acid: nitrates of 3:1.…”

Section: Methodsmentioning

confidence: 99%

Nanocrystalline Er:YAG thin films prepared by pulsed laser deposition: An electron microscopy study

Stanoi

Popescu

Ghica

et al. 2007

Applied Surface Science

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Toxicological evaluation of the isoflavone puerarin and its glycosides

Cited by 33 publications

References 26 publications

Puerarin, a selective oestrogen receptor modulator, disrupts pregnancy in rats at pre-implantation stage

Puerarin, a selective oestrogen receptor modulator, disrupts pregnancy in rats at pre-implantation stage

RadixPuerariae: An overview of Its Chemistry, Pharmacology, Pharmacokinetics, and Clinical Use

Nanocrystalline Er:YAG thin films prepared by pulsed laser deposition: An electron microscopy study

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