Estrogenic and mutagenic activities of Crotalaria pallida measured by recombinant yeast assay and Ames test
TL;DR: Considering the excellent estrogenic activity performed by stigmasterol in the RYA associated with the absence of mutagenic activity when evaluated by the Ames test, stig masterol becomes a strong candidate to be used in hormone replacement therapy during menopause.
Abstract: Crotalaria pallida Ailton is a plant belonging to the Fabaceae family, popularly known as “rattle or rattlesnake” and used in traditional medicine to treat swelling of the joints and as a vermifuge. Previous pharmacological studies have also reported anti-inflammatory, antimicrobial and antifungal activities. Nevertheless, scientific information regarding this species is scarce, and there are no reports related to its possible estrogenic and mutagenic effects. Thus, the purpose of the present study was to investigate the estrogenic potential of C. pallida leaves by means of the Recombinant Yeast Assay (RYA), seeking an alternative for estrogen replacement therapy during menopause; and to reflect on the safe use of natural products to assess the mutagenic activity of the crude extract from C. pallida leaves, the dichloromethane fraction and stigmasterol by means of the Ames test. The recombinant yeast assay with the strain BY4741 of Saccharomyces cerevisiae, was performed with the ethanolic extract, dichloromethane fraction and stigmasterol isolated from the leaves of C. pallida. Mutagenic activity was evaluated by the Salmonella/microsome assay (Ames test), using the Salmonella typhimurium tester strains TA100, TA98, TA97 and TA102, with (+S9) and without (-S9) metabolization, by the preincubation method. All samples showed estrogenic activity, mainly stigmasterol. The ethanolic extract from C. pallida leaves showed mutagenic activity in the TA98 strain (-S9), whereas dichloromethane fraction and stigmasterol were found devoid of activity. Considering the excellent estrogenic activity performed by stigmasterol in the RYA associated with the absence of mutagenic activity when evaluated by the Ames test, stigmasterol becomes a strong candidate to be used in hormone replacement therapy during menopause.
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TL;DR: A comprehensive summary of more than 450 estrogenic chemicals including estrogenic endocrine disruptors is provided here to understand the complex and profound impact of estrogen action.
193 citations
TL;DR: Applications of estrogenic terpenes and terpenoids are categorized into cancer treatment and prevention, cardioprotection, endocrine toxicity/reproductive dysfunction, food/supplement/traditional medicine, immunology/inflammation, menopausal syndromes and neuroprotection, where their benefits are discussed based on their availability, stability and variations.
55 citations
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...Stigmasterol (E) ER/Traditional medicine Boldrin et al. (2013) (R)...
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Cites background from "Estrogenic and mutagenic activities..."
...The raw leaves are very useful for abortion since it has stigmasterol which affects estrogenic activity (Boldrin et al., 2013)....
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TL;DR: The leaves of Tridax procumbens were screened for the presence of bioactive molecules and the results showed that they had high flavonoids, alkaloids, hydroxycinnamates, tannins and phytosterols, moderate benzoic acid derivatives and lignans, and low carotenoids contents as discussed by the authors.
Abstract: The leaves of Tridax procumbens were screened for the presence of bioactive molecules. They had high flavonoids, alkaloids, hydroxycinnamates, tannins and phytosterols, moderate benzoic acid derivatives and lignans, and low carotenoids contents. Thirty nine known alkaloids (mainly akuammidine, 68.756%), twenty three known flavonoids (mainly 17.593% kaempferol and 12.538% (-)-epicatechin), five known carotenoids (mainly lutein, 62.608%), four known benzoic acid derivatives (mainly ferulic acid, 46.091%), two phytosterols (mainly stigmasterol, 80.853%) and six known lignans (mainly galgravin, 77.326%) were detected. Also detected were caffeic acid and tannic acid. The medicinal properties of the flavonoids, phytosterols, alkaloids, tannins, hydroxicinnamates, carotenoids, benzoic acid derivatives and lignans that were present in the leaves were discussed herein and proposed to be explored for their potential medicinal values. The great number of potentially active nutrients and their multifunctional properties make Tridax procumbens a perfect candidate for the production of health-promoting food and food supplements.
28 citations
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...Stigmasterol has anti-osteoarthritic, anti-hypercholestrolemic, cytotoxicity, antitumor, thyroid inhibiting, hypoglycemic, anti-mutagenic, antioxidant, anti-inflammatory, anticonvulsant and sedative [69], chemopreventive, anticancer, estrogenic [70] activities....
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TL;DR: Results suggest that two hydroxyls (in positions 7 and 8) or 7-methoxy substituents are essential for the antiestrogenic activity of flavonoids.
199 citations
"Estrogenic and mutagenic activities..." refers background in this paper
...The presence of these hydroxyl groups is essential for the estrogenic activity because they mimic the hydroxyl at the 3 and 17 position, found in the 17-β-estradiol molecule [28]....
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TL;DR: The soy isoflavones, biochanin A and genistein, showed the most potent estrogenic activity, with a dose-response effect up to 10−7 M, while luteolin and naringenin displayed the strongest estrogenicity, while apigenin had a relatively strong progestational activity.
Abstract: Soy isoflavones have been studied extensively for estrogenic and antiestrogenic properties. Other flavonoids, found in fruits, vegetables, tea and wine, have been much less tested for steroid hormone activity. We therefore assessed the estrogenic, androgenic and progestational activities of 72 flavonoids and structurally-related compounds. These compounds were tested on BT-474 human breast cancer cells at concentrations of 108–10−5 M, with estradiol (estrogen), norgestrel (progestin) and dihydrotestosterone (androgen) used as positive controls, and ethanol (solvent) as a negative control. pS2, an estrogen-regulated protein, and prostate-specific antigen (PSA), regulated by androgens and progestins, were quantified in tissue culture supernatants using ELISA-type immunofluorometric assays developed in-house. Of the 72 compounds tested, 18 showed estrogenic activity at 10−5 M. Of this subset, seven also showed progestational activity at this concentration. The soy isoflavones, biochanin A and genistein, showed the most potent estrogenic activity, with a dose-response effect up to 10−7 M. Of all other flavonoids, luteolin and naringenin displayed the strongest estrogenicity, while apigenin had a relatively strong progestational activity. Based on our data, we have formulated a set of structure/function relationships between the tested compounds. Flavonoids, therefore, exhibit significant steroid hormone activity, and may have an effect in the modification of cancer risk by diet, or in cancer therapeutics and prevention.
193 citations
"Estrogenic and mutagenic activities..." refers background in this paper
...Furthermore, the presence of a double bond between carbons 2 and 3 of the ring C is essential for the estrogenic activity [26]....
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...[26] reported that hydroxyl at the 6, 7 or 4’ positions of the flavonoid provides greater estrogenic activity and more potent compounds with 2–4 hydroxyl groups, namely, at least one in the 7 position of the ring A and another in the 4’ position of ring B....
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...Flavonoids have some structural similarities to the natural estrogen 17-β-estradiol, as well as to other steroid hormones and steroid hormone antagonists [26], and can interact with the ER and induce gene expression similar to that induced by estrogens, albeit at a lower affinity [27]....
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TL;DR: The pendulum swung back from its peak negative sentiment following more detailed data from the WHI study that demonstrated the importance of the age at initiation and the good safety profile of HRT in women younger than 60 years.
Abstract: The past decade has seen marked fluctuations in opinions concerning the merits and risks of postmenopausal hormone replacement therapy (HRT). In July 2002, menopause management faced a major turnin...
183 citations
"Estrogenic and mutagenic activities..." refers background in this paper
...during menopause, without the undesirable effects of estrogen, such as the elevation of breast cancer incidence [9,10]....
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