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Journal ArticleDOI

Estrogenic and mutagenic activities of Crotalaria pallida measured by recombinant yeast assay and Ames test

04 Sep 2013-BMC Complementary and Alternative Medicine (BioMed Central)-Vol. 13, Iss: 1, pp 216-216

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.

AbstractCrotalaria 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.

Topics: Ames test (59%), Stigmasterol (54%)

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Citations
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Journal ArticleDOI
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.
Abstract: 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. First, estrogenic chemicals are categorized by structure as well as their applications, usage and effects. Second, estrogenic signaling is examined by the molecular mechanism based on the receptors, signaling pathways, crosstalk/bypassing and autocrine/paracrine/homeostatic networks involved in the signaling. Third, evaluation of estrogen action is discussed by focusing on the technologies and protocols of the assays for assessing estrogenicity. Understanding the molecular mechanisms of estrogen action is important to assess the action of endocrine disruptors and will be used for risk management based on pathway-based toxicity testing.

144 citations


Journal ArticleDOI
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.
Abstract: Terpenes are made of the isoprene unit (C5), and along with their derivatives, terpenoids, they are widely distributed in plants as active ingredients involved in anti-inflammation, anti-carcinogenesis and neuroprotection Estrogenic terpenes and terpenoids are an important category of phytoestrogens and have been used as traditional medicines The comprehensive list of estrogenic terpenes and terpenoids includes hemi-, mono-, sesqui-, di-, tri-, tetra- and polyterpenes, their derivatives, and meroterpenes, along with the signaling pathways and cellular functions on which their estrogenicity is exerted Signaling pathways are further classified as bidirectional or unidirectional, the latter being further divided into two types depending upon the presence of both ligands, or the absence of one or both ligands Although estrogenic activity of terpenes and terpenoids was evaluated by ligand-binding assays, yeast two-hybrid assays, reporter-gene assays, transcription assays, protein assays, cell assays and animal testing, the mechanism of estrogenic activity is still not fully understood 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

31 citations


Additional excerpts

  • ...Stigmasterol (E) ER/Traditional medicine Boldrin et al. (2013) (R)...

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Journal ArticleDOI
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.
Abstract: Ethnopharmacological relevance Acalypha indica is an herbal plant that grows in wet, temperate and tropical region, primarily along the earth’s equator line. This plant is considered by most people as a weed and can easily be found in these regions. Although this plant is a weed, Acalypha indica has been acknowledged by local people as a useful source of medicine for several therapeutic treatments. They consume parts of the plant for many therapeutics purposes such as anthelmintic, anti-ulcer, bronchitis, asthma, wound healing, anti-bacterial and other applications. As this review was being conducted, most of the reports related to ethnomedicinal practices were from Asian and African regions. The aim of the review The aim of this review is to summarize the current studies on ethnomedicinal practices, phytochemistry, pharmacological studies and a potential study of Acalypha indica in different locations around the world. This review updates related information regarding the potential therapeutic treatments and also discusses the toxicity issue of Acalypha indica. Materials and methods This review was performed through a systematic search related to Acalypha indica including the ethnomedicinal practices, phytochemistry and pharmacological studies around the world. The data was collected from online journals, magazines, and books, all of which were published in English, Malay and Indonesian. Search engine websites such as Google, Google Scholar, PubMed, Science Direct, Researchgate and other online collections were utilized in this review to obtain information. Results The links between ethnomedicinal practices and scientific studies have been discussed with a fair justification. Several pharmacological properties exhibited certain potentials based on the obtained results that came from different related studies. Based on literature studies, Acalypha indica has the capability to serve as anthelmintic, anti-inflammation, anti-bacterial, anti-cancer, anti-diabetes, anti-hyperlipidemic, anti-obesity, anti-venom, hepatoprotective, hypoxia, and wound healing medicine. For the traditional practices, the authors also mentioned several benefits of consuming the raw plant and decoction. Conclusion This review summarizes the current studies of Acalypha indica collected from many regions. This review hopefully will provide a useful and basic knowledge platform for anyone interested in gaining information regarding Acalypha indica.

31 citations


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: HEBB might be used as a safe alternative to estrogen replacement therapies and induced cell proliferation and all the dilutions except <500μg/ml have significantly increased cell multiplication.
Abstract: Focus of the study is to identify a safe alternate to Hormone Replacement Therapy by identifying the presence of β-sitosterol and stigmasterol in the hydroalcoholic extract of Bambusa bambos using HPTLC and RP-HPLC-PDA; by evaluating the estrogenic effects of extract containing β-sitosterol and stigmasterol on the growth of MCF-7 cells in vitro. Plant material was identified by DNA sequencing analysis. Presence of β-sitosterol and stigmasterol was confirmed by HPTLC and direct RP-HPLC-PDA. Peaks with retention time about 19.13 and 21.16min were found to be stigmasterol and β-sitosterol in extract. Extract was not cytotoxic to MCF-7 cells in any of the dilutions. It induced cell proliferation and all the dilutions except <500μg/ml have significantly increased cell multiplication. 15.6, 31.2, 62.5 and 125μg/ml of HEBB have shown influence on the proliferation rates similar to the standard 17β-estradiol. The results suggest that HEBB might be used as a safe alternative to estrogen replacement therapies.

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References
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Journal ArticleDOI
TL;DR: Two new tester strains, a frameshift strain and a strain carrying an ochre mutation on a multicopy plasmid (TA102), are added to the standard tester set and two substitutions are made in diagnostic mutagens to eliminate MNNG and 9-aminoacridine.
Abstract: The methods for detecting carcinogens and mutagens with the Salmonella mutagenicity test were described previously (Ames et al., 1975b). The present paper is a revision of the methods. Two new tester strains, a frameshift strain (TA97) and a strain carrying an ochre mutation on a multicopy plasmid (TA102), are added to the standard tester set. TA97 replaces TA1537. TA1535 and TA1538 are removed from the recommended set but can be retained at the option of the investigator. TA98 and TA100 are retained. We discuss other special purpose strains and present some minor changes in procedure, principally in the growth, storage, and preservation of the tester strains. Two substitutions are made in diagnostic mutagens to eliminate MNNG and 9-aminoacridine. Some test modifications are discussed.

7,045 citations


"Estrogenic and mutagenic activities..." refers methods in this paper

  • ...Ames (Berkeley, CA, USA), with (+S9) and without (−S9) metabolization, using the preincubation method [23]....

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Book
28 Jan 2014
TL;DR: Screening of Unknown Commercial Drugs and Thin-Layer Chromatography Analysis of Herbal Drug Mixtures for Pungent-Tasting Principles.
Abstract: Alkaloid Drugs.- Drugs Containing Anthracene Derivatives.- Bitter Drugs.- Cardiac Glycoside Drugs.- Coumarin Drugs.- Drugs Containing Essential Oils (Aetherolea), Balsams and Oleo-Gum-Resins.- Flavonoid Drugs Including Ginkgo Biloba and Echinaceae Species.- Drugs Containing Arbutin, Salicin and Salicoyl Derivatives.- Drugs Containing Cannabinoids and Kavapyrones.- Drugs Containing Lignans.- Drugs Containing 1,4-Naphthoquinones Droserae herba, Dionaeae herba.- Drugs Containing Pigments.- Drugs with Pungent-Tasting Principles.- Saponin Drugs.- Drugs Containing Sweet-Tasting Terpene Glycosides.- Drugs Containing Triterpenes.- Drugs Containing Valepotriates (Valerianae radix).- Screening of Unknown Commercial Drugs.- Thin-Layer Chromatography Analysis of Herbal Drug Mixtures.

1,996 citations


"Estrogenic and mutagenic activities..." refers methods in this paper

  • ...The extracts were monitored using TLC-silica gel 60-F254 precoated Al sheets, using chloroform: methanol: n-propanol:water (5:6:1:4, v:v) as developing solvent, visualized using UV (254 and 366 nm) and anisaldehyde sulphuric acid spray [16], until total depletion of the drug....

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TL;DR: A scholarly review of the published literature on menopausal hormonal therapy (MHT), make scientifically valid assessments of the available data, and grade the level of evidence available for each clinically important endpoint to arrive at major conclusions.
Abstract: Objective: Our objective was to provide a scholarly review of the published literature on menopausal hormonal therapy (MHT), make scientifically valid assessments of the available data, and grade the level of evidence available for each clinically important endpoint. Participants in Development of Scientific Statement: The 12-member Scientific Statement Task Force of The Endocrine Society selected the leader of the statement development group (R.J.S.) and suggested experts with expertise in specific areas. In conjunction with the Task Force, lead authors (n = 25) and peer reviewers (n = 14) for each specific topic were selected. All discussions regarding content and grading of evidence occurred via teleconference or electronic and written correspondence. No funding was provided to any expert or peer reviewer, and all participants volunteered their time to prepare this Scientific Statement. Evidence: Each expert conducted extensive literature searches of case control, cohort, and randomized controlled tria...

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"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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TL;DR: A small number of adequately controlled human intervention studies suggest that some, but not allpolyphenol extracts or high polyphenol diets may lead to transitory changes in the antioxidative capacity of plasma in humans, but none of these studies have adequately considered long-term effects on DNA or the chromosome.
Abstract: Polyphenols are a large and diverse class of compounds, many of which occur naturally in a range of food plants. The flavonoids are the largest and best-studied group of these. A range of plant polyphenols are either being actively developed or currently sold as dietary supplements and/or herbal remedies. Although, these compounds play no known role in nutrition (non-nutrients), many of them have properties including antioxidant, anti-mutagenic, anti-oestrogenic, anti-carcinogenic and anti-inflammatory effects that might potentially be beneficial in preventing disease and protecting the stability of the genome. However not all polyphenols and not all actions of individual polyphenols are necessarily beneficial. Some have mutagenic and/or pro-oxidant effects, as well as interfering with essential biochemical pathways including topoisomerase enzyme activities, prostanoid biosynthesis and signal transduction. There is a very large amount of in vitro data available, but far fewer animal studies, and these are not necessarily predictive of human effects because of differences in bacterial and hepatic metabolism of polyphenols between species. Epidemiological studies suggest that high green tea consumption in the Japanese population and moderate red wine consumption in the French population may be beneficial for heart disease and cancer, and these effects may relate to specific polyphenols. A small number of adequately controlled human intervention studies suggest that some, but not all polyphenol extracts or high polyphenol diets may lead to transitory changes in the antioxidative capacity of plasma in humans. However, none of these studies have adequately considered long-term effects on DNA or the chromosome and unequivocally associated these with polyphenol uptake. Furthermore, clinical trials have required intravenously administered polyphenols at concentrations around 1400mg/m(2) before effects are seen. These plasma concentrations are unlikely to be achieved using the dietary supplements currently available. More focused human studies are necessary before recommending specific polyphenolic supplements at specific doses in the human population.

561 citations


"Estrogenic and mutagenic activities..." refers background in this paper

  • ...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: Findings from Epidemiologic and experimental studies suggest that dietary PS may offer protection from the most common cancers in Western societies, such as colon, breast and prostate cancer, and the possible mechanisms by which PS offer this protection are summarized.
Abstract: Phytosterols (PS) or plant sterols are structurally similar to cholesterol. The most common PS are beta-sitosterol, campesterol and stigmasterol. Epidemiologic and experimental studies suggest that dietary PS may offer protection from the most common cancers in Western societies, such as colon, breast and prostate cancer. This review summarizes the findings of these studies and the possible mechanisms by which PS offer this protection. These include the effect of PS on membrane structure and function of tumor and host tissue, signal transduction pathways that regulate tumor growth and apoptosis, immune function of the host and cholesterol metabolism by the host. In addition, suggestions for future studies to fill the gaps in our knowledge have been given.

548 citations


"Estrogenic and mutagenic activities..." refers background in this paper

  • ...The exact mechanism by which phytosteroids offer protection against cancer is not understood, but there are theories proposing their effect on the structure of cell membranes, on the fluidity of cell membranes, on enzymes bound to membranes, on signal transduction pathways, on apoptosis, on membrane integrity, on the immune function, on the estrogenic properties on the tissue and on acids and neutral steroids in the colon [31]....

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  • ...Chemically, they are alcohols consisting of 28 or 29 carbon atoms, similar to cholesterol [31]....

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