Antifertility and hormonal properties of flavones of Striga orobanchioides

Hiremath, S. P.; Badami, Shrishailappa; Hunasagatta, S K; Patil, Sarawathi B

doi:10.1016/s0014-2999(99)00723-2

Cited by 68 publications

(36 citation statements)

References 8 publications

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“…In vitro both compounds can bind to estrogen receptors (Middleton et al, 2000), and in vivo both induce uterus weight increase and antifertility (Hiremath et al, 2000). The mode of action of apigenin is still unclear, but metabolism is the first step that can help to build our knowledge.…”

Section: Discussionmentioning

confidence: 99%

“…Some 5,7,4Ј-hydroxyflavonoids ( Fig. 1) present in the Western diet such as apigenin, luteolin, kaempferol, or naringenin have also been shown to possess estrogenic or antiestrogenic properties in vitro (Breinholt and Larsen, 1998;Le Bail et al, 1998;Middleton et al, 2000;Birt et al, 2001) as well as in vivo Hiremath et al, 2000). They are about 1000 times less estrogenic than genistein (Middleton et al, 2000), but their presence in great amounts could explain the abortive properties of some medicinal plants (Hiremath et al, 2000).…”

Section: Introductionmentioning

confidence: 99%

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Metabolism of Apigenin by Rat Liver Phase I and Phase Ii Enzymes and by Isolated Perfused Rat Liver

Gradolatto¹,

Canivenc-Lavier²,

Basly³

et al. 2004

Drug Metab Dispos

114

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This article is available online at http://dmd.aspetjournals.org ABSTRACT:The metabolism of apigenin, a low estrogenic flavonoid phytochemical, was investigated in rat using liver models both in vitro (subcellular fractions) and ex vivo (isolated perfused liver). In vitro, phase I metabolism led to the formation of three monohydroxylated derivatives: luteolin which was the major metabolite (K m ‫؍‬ 22.5 ؎ 1.5 M; V max ‫؍‬ 5.605 ؎ 0.090 nmol/min/mg protein, means ؎ S.E.M.), scutellarein, and iso-scutellarein. These oxidative pathways were mediated by cytochrome P450 monooxygenases (P450s). The use of P450 inhibitors and inducers showed that CYP1A1, CYP2B, and CYP2E1 are involved. In vitro studies of phase II metabolism indicated that apigenin underwent conjugation giving three monoglucuronoconjugates and one monosulfoconjugate. Luteolin led to the formation of four monoglucuronoconjugates, two sulfoconjugates, and one methylconjugate identified as diosmetin. Ex vivo during the apigenin perfusion of an isolated rat liver, none of the phase I metabolites could be recovered. In contrast, two monoglucuronoconjugates and one of the sulfoconjugates of apigenin already identified in vitro were recovered. Moreover, two new derivatives were isolated and identified as a diglucuronoconjugate and a glucuronosulfoconjugate. This work provides new data about the metabolism of apigenin and shows the interest value of using various experimental models in metabolic studies.

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Metabolism of Apigenin by Rat Liver Phase I and Phase Ii Enzymes and by Isolated Perfused Rat Liver

Gradolatto¹,

Canivenc-Lavier²,

Basly³

et al. 2004

Drug Metab Dispos

114

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“…Oral administration of apigenin was shown to cause a significant increase in uterine weight and overall uterine concentration of estrogen receptor (ER)-· in female mice (63). Apigenin has been shown to decrease intracellular and secreted levels of PSA in androgen-responsive human prostate cancer LNCaP cells (52).…”

Section: Achillea Millefoliummentioning

confidence: 99%

Apigenin and cancer chemoprevention: Progress, potential and promise (Review)

Patel

Shukla²,

Gupta³

2007

Int J Oncol

311

362

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Abstract. Cancer is one of the major public health burdens in the United States and in other developed countries, causing approximately 7 million deaths every year worldwide. Cancer rates vary dramatically in different regions and populations around the globe, especially between developing and developed nations. Changes in cancer prevalence patterns occur within regions as their populations age or become progressively urbanized. Migration has also contributed to such variations as changes in dietary habits influence cancer rates. These epidemiologic findings strongly suggest that cancer rates are influenced by environmental factors including diet, which is largely preventable. Approaches to prevent cancer include overlapping strategies viz. chemoprevention or dietary cancer prevention. Chemoprevention aims at prevention or reversal of the initiation phase of carcinogenesis or arrest at progression of carcinogenesis through the administration of naturally occurring constituents or pharmacological agents. Cancer prevention through diet may be largely achievable by increased consumption of fruits and vegetables. Considerable attention has been devoted to identifying plant-derived dietary agents which could be developed as promising chemopreventives. One such agent is apigenin. A naturally occurring plant flavone (4', 5, 7,-trihydroxyflavone) abundantly present in common fruits and vegetables including parsley, onions, oranges, tea, chamomile, wheat sprouts and some seasonings. Apigenin has been shown to possess remarkable anti-inflammatory, antioxidant and anti-carcinogenic properties. In the last few years, significant progress has been made in studying the biological effects of apigenin at cellular and molecular levels. This review examines the cancer chemopreventive effects of apigenin in an organ-specificity format, evaluating its limitations and its considerable potential for development as a cancer chemopreventive agent.

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“…The ovaries were excised out and the numbers of functional CL were counted under dissecting microscope. Rate of implantation (%) was calculated as the number of implantation sites per functional CL present in the ovary (Hiremath et al 2000) and plotted against each concentration of puerarin to construct a dose-response curve.…”

Section: Antifertility Studiesmentioning

confidence: 99%

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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Antifertility and hormonal properties of flavones of Striga orobanchioides

Cited by 68 publications

References 8 publications

Metabolism of Apigenin by Rat Liver Phase I and Phase Ii Enzymes and by Isolated Perfused Rat Liver

Metabolism of Apigenin by Rat Liver Phase I and Phase Ii Enzymes and by Isolated Perfused Rat Liver

Apigenin and cancer chemoprevention: Progress, potential and promise (Review)

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

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