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.
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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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TL;DR: This review summarizes the current studies on ethnomedicinal practices, phytochemistry, pharmacological studies and a potential study of Acalypha indica in different locations around the world to provide a useful and basic knowledge platform for anyone interested in gaining information about this plant.
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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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References
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TL;DR: Aveloz is a plant of the genus Euphorbia (Euphorbiaceae) and it has been popularly used in South America for treating ulcer, cancer, tumor, wart and other diseases as discussed by the authors.
Abstract: Folk medicinal plants have been analyzed and assayed to confirm their possible antitumoral and anticarcinogenic properties. Aveloz is a plant of the genus Euphorbia (Euphorbiaceae) and it has been popularly used in South America for treating ulcer, cancer, tumor, wart and other diseases. However, some researches have shown opposite effects. Due to these contradictory results, the aim of this work was to test the antimutagenic potential of Euphorbia tirucalli latex in Aspergillus nidulans methionine system. Two concentrations of the latex were used in conidia treatment: 0.1% and 0.2% (v/v). The treatment was developed by collecting quiescent conida from five days old colonies in latex solution, during 24 hours. The results have indicated that both concentrations show antimutagenic effect because the mutation frequency of the treated conidia was smaller than mutation frequency of the control
20 citations
TL;DR: A significant increase in the frequencies of both cytogenetic events was observed when proliferating cells were treated for 4 h with harmine followed by irradiation with UV light for 3 min.
Abstract: The photodynamic effect of harmine and UV light was studied by measuring the number of sister-chromatid exchanges and micronuclei induced by this treatment in Allium cepa meristematic cells. A significant increase in the frequencies of both cytogenetic events was observed when proliferating cells were treated for 4 h with harmine followed by irradiation with UV light for 3 min.
18 citations
TL;DR: Results indicate that the crotafuran B inhibition of NO production involves a decrease in the iNOS gene expression via the inhibition of NF-{kappa}B activation through the increase in I{kapp}B{alpha} synthesis.
13 citations
TL;DR: Their low toxicity towards mice fibroblasts at maximal concentrations, their antioxidant activity, comparable or even higher than that of ascorbic acid as determined by direct quenching of the DPPH radical, and their potential for significantly altering total and LDL cholesterol levels, suggest that these conjugates merit further studies in the treatment of cardiovascular or other related diseases.
Abstract: Synthesis, detailed structural characterization (X-ray, NMR, MS, IR, elemental analysis), and studies of toxicity, antioxidant activity and bioavailability of unique potent anti-atherosclerotic succinobucol-steroid conjugates are reported. The conjugates consist of, on one side, the therapeutically important drug succinobucol ([4-{2,6-di-tert-butyl-4-[(1-{[3-tert-butyl-4-hydroxy-5-(propan-2-yl)phenyl]sulfanyl}ethyl)sulfanyl]phenoxy}-4-oxo-butanoic acid]) possessing an antioxidant and anti-inflammatory activity, and on the other side, plant stanol/sterols (stigmastanol, β-sitosterol and stigmasterol) possessing an ability to lower the blood cholesterol level. A cholesterol-succinobucol prodrug was also prepared in order to enhance the absorption of succinobucol through the intestinal membrane into the organism and to target the drug into the place of lipid metabolism—The enterohepatic circulation system. Their low toxicity towards mice fibroblasts at maximal concentrations, their antioxidant activity, comparable or even higher than that of ascorbic acid as determined by direct quenching of the DPPH radical, and their potential for significantly altering total and LDL cholesterol levels, suggest that these conjugates merit further studies in the treatment of cardiovascular or other related diseases. A brief discussion of succinobucol’s ability to quench the radicals, supported with a computational model of the electrostatic potential mapped on the electron density surface of the drug, is also presented.
10 citations
"Estrogenic and mutagenic activities..." refers background in this paper
...The advantages of phytosteroids result from its biodegradability, the ability to affect numerous biological processes through membranes, to bind to specific hormone receptors and to be modified by synthetic methods [32-34]....
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01 Jan 2011
TL;DR: Da viele Pyrrolizidinalkaloide mutagene und einige auch kanzerogene Wirkungen besitzen, beschaftigen sich europaische and internationale Aufsichtsbehorden mit der Frage nach moglichen Ruckstanden in Lebensmitteln tierischen Ursprungs.
Abstract: Pyrrolizidinalkaloide sind Pflanzentoxine, die in mehr als 6000 Pflanzenarten vorkommen. Die Seneciose der landwirtschaftlichen Nutztiere stellt eine Vergiftung mit Pyrrolizidinalkaloiden von Pflanzen der Gattung Senecio dar. Sie ist seit Ende des 19.Jahrhunderts in Deutschland, den USA, Kanada und Neuseeland bekannt und wird vor allem durch Senecio jacobaea und verwandte Senecio spp. bei landwirtschaftlichen Nutztieren einschlieslich Geflugel hervorgerufen. Tiervergiftungen mit Pyrrolizidinalkaloiden spielen weltweit eine grose Rolle. In unseren Breiten findet vor allem die Vergiftung von Pferden und Rindern durch das Jakobskreuzkraut ( Senecio jacobaea ), die als Schweinsberger Krankheit bekannt wurde, erneut besondere Beachtung in der Tiermedizin. Sie tritt fast immer als chronische Vergiftung auf und endet in der Regel todlich. Endgultige Ursache ist die Bildung von toxischen Metaboliten der Pyrrolizidinalkaloide in der Leber, die mit Nukleinsauren und Proteinen kovalente Bindungen eingehen und zur Leberzirrhose fuhren. Da viele Pyrrolizidinalkaloide mutagene und einige auch kanzerogene Wirkungen besitzen, beschaftigen sich europaische und internationale Aufsichtsbehorden mit der Frage nach moglichen Ruckstanden in Lebensmitteln tierischen Ursprungs. Die Ubersichtsarbeit befasst sich in Teil1 mit Aspekten des Vorkommens, der Chemie und der Toxikologie von Pyrrolizidinalkaloiden sowie mit den durch sie hervorgerufenen Pflanzenvergiftungen bei landwirtschaftlichen Nutztieren. Im zweiten Teil der Ubersicht erfolgt eine Darstellung des klinischen Verlaufs der Seneciose bei Tieren, von Behandlungsmasnahmen, der erheblichen Speziesunterschiede sowie eine kritische Bewertung so genannter ungiftiger Aufnahmemengen von Senecio-Pflanzen im Tierfutter auf der Grundlage kumulativer letaler Toxindosen.
8 citations