Estrogenic activity of a polyphenolic extract of the leaves of Epimedium brevicornum

Ghent University, Faculty of Pharmaceutical Sciences, Laboratory of Pharmacognosy and Phytochemistry, Harelbekestraat 72, B-9000 Ghent, Belgium.
Fitoterapia (Impact Factor: 2.35). 02/2005; 76(1):35-40. DOI: 10.1016/j.fitote.2004.10.002
Source: PubMed


The estrogenic activity of a polyphenolic extract of the leaves of Epimedium brevicornum and five fractions obtained by solid-phase extraction were investigated using estrogen-responsive bioassays, a yeast cell assay and the Ishikawa Var-I assay. The extract was found to exhibit significant estrogenic activity in both assays. Furthermore, bioassay-guided fractionation led to localisation of the estrogenicity in the relatively non-polar fractions of the polyphenolic extract.

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    • "These phytoestrogen flavonoids have been shown to exert protective effects on bone loss in OVX rats and postmenopausal women [12, 13]. However, it has been demonstrated that Epimedium flavonoids are weak estrogen agonists that act via the ERα and ERβ [14]. Phytoestrogens have the ability to interfere with estrogen action either by interacting directly with the estrogen receptor (ER) or indirectly by modulating endogenous estrogen concentrations [15, 16]. "
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    • "The hydrolytic activity was assayed by monitoring the formation of p-nitrophenol following enzymatic hydrolysis of PNPPP [20, 27, 28]. This experimental approach has been applied elsewhere for detection of biological activities of some plant extracts towards PNPPP [29]. The pattern of relaxation produced by the extract that mimics the effect of sildenafil coupled with enzyme substrate inhibitory effect of the extract suggested that phosphodiesterase inhibition was the possible mode of action of the extract on CCSM. "
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    ABSTRACT: Clerodendron capitatum (Willd) (family: verbenaceae) is locally named as Gung and used traditionally to treat erectile dysfunction. Therefore, the current study was designed to investigate the erectogenic properties of C. capitatum. The relaxation effect of this plant was tested on phenylephrine precontracted rabbit corpus cavernosum smooth muscle (CCSM). The effects of C. capitatum were also examined on isolated Guinea pig atria alone, in the presence of calcium chloride (Ca(2+) channel blocker), atropine (cholinergic blocker), and glibenclamide (ATP-sensitive K(+) channel blocker). These effects were confirmed on isolated rabbit aortic strips. The extract, when tested colorimetrically for its inhibitory activities on phosphordiesterase-5 (PDE-5) in vitro towards p-nitrophenyl phenyl phosphate (PNPPP), was observed to induce significant dose-dependent inhibition of PDE-5, with an ID(50) of 0.161 mg/ml (P < .05). In conclusion, our results suggest that C. capitatum possesses a relaxant effect on CCSM, which is attributable to the inhibition of PDE-5, but not mediated by the release calcium, activation of adrenergic or cholinergic receptors, or the activation of potassium channels.
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    • "Briefly, shikonin did not demonstrate estrogenic activity, even at high concentra- tions. Estrogenic activity has been assessed intensively among a great deal of substances including phytocompounds, medicines, pesticides and industrial chemicals using various techniques (De Naeyer et al. 2005; Gutendorf and Westendorf 2001; Sookvanichsilp et al. 2008). According to well-elucidated mechanisms of action (Tsai and O'Malley 1994), in vitro methods use more definitive end points and are more sensitive than in vivo methods. "
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    ABSTRACT: Shikonin, an active component of Lithospermum erythrorhizon Sieb. et Zucc., shows multiple pharmacological properties. However, the estrogenic activity of shikonin is remaining unclear. We assessed the potential estrogenic activity of shikonin with dual-luciferase reporter assay and bioluminescent measurements, by using transient cotransfection with estrogen dependent plasmid pERE-TK-Luc and internal control plasmid pRL-TK in MCF-7 cells. Estrogenic activity of shikonin, even at high concentration did not alter significantly compared to negative control (p > 0.05) and were significantly lower than those with E2 (p < 0.01). Concluding, shikonin demonstrates no estrogenic activity in vitro.
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