Establishment of a luciferase assay-based screening system for detecting estrogen receptor agonists in plant extracts

Du, Jinyan; Wei, Yan-Jie; Peng, Cheng; Ran, Xia; Zhang, Hong; Jiang, Yi-Ping; Rahman, Khalid; Qin, Lu-Ping

doi:10.1016/j.bone.2011.05.028

Cited by 5 publications

(5 citation statements)

References 43 publications

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“…Currently, estrogen is one of the most commonly used treatment strategies for treating postmenopausal osteoporosis (6). However, studies have demonstrated that estrogen treatment could result in serious adverse effects, such as endometrial carcinoma, breast cancer and cardiovascular disease (4,7). It is therefore key to identify novel strategies with low toxicity for treating osteoporosis.…”

Section: Introductionmentioning

confidence: 99%

Polydatin possesses notable anti-osteoporotic activity via regulation of OPG, RANKL and β-catenin

Zhou¹,

Ru-zi²,

Yang³

et al. 2016

Molecular Medicine Reports

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This study was designed to investigate the anti‑osteoporotic activity of polydatin and its possible underlying mechanism. Osteoporosis was induced in mice by ovariectomy (OVX) and the mice were divided into 5 groups: An OVX only group, polydatin groups (10, 20 and 40 mg/kg) and a sham group (n=10/group). After 12 weeks of treatment, body weight, uterine index and the dry weight of thigh‑bones were recorded. In addition, the serum calcium, serum phosphorus, alkaline phosphatase (ALP) and osteoprotegerin (OPG) levels were also determined. Western blot analysis was then conducted to investigate the possible mechanism underlying the effect of polydatin via determining the expression of OPG, receptor activators of nuclear factor‑κB ligand (RANKL) and β‑catenin in the ST2 cell line. The results indicated that intraperitoneal injection of polydatin (10, 20 and 40 mg/kg/day) decreased body weight, and increased uterine index and dry weights of thigh‑bones of ovariectomized mice (P<0.05), and polydatin also significantly increased the serum calcium, phosphorus, ALP and OPG of ovariectomized mice (P<0.05). Results of western blot analysis showed that polydatin upregulated the ratio of OPG/RANKL (P<0.05) and β‑catenin protein in ST2 cells. In conclusion, the results demonstrated that polydatin exhibits anti‑osteoporotic activity via regulating osteoprotegerin, RANKL and β‑catenin.

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Section: Introductionmentioning

confidence: 99%

Polydatin possesses notable anti-osteoporotic activity via regulation of OPG, RANKL and β-catenin

Zhou¹,

Ru-zi²,

Yang³

et al. 2016

Molecular Medicine Reports

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“…The estrogen replacement therapy (ERT) is one of the commonly used treatments for preventing osteoporosis in postmenopausal women, and is considered to be the most effective therapy for osteoporosis (Ma et al, 2013;Qin et al, 2008). However, serious and undesirable adverse effects were found in ERT treatment, including endometrial cancer, breast carcinoma, and cardiovascular diseases (Du et al, 2011). Furthermore, there are many other synthetic agents that could be used to prevent or treat osteoporosis, but many side effects also exist as ERT (Canalis et al, 1998;Genant et al, 1998).…”

Section: Introductionmentioning

confidence: 99%

Anti-osteoporotic activity of puerarin 6″-O-xyloside on ovariectomized mice and its potential mechanism

Li¹,

Bing-pu²,

Pang

et al. 2015

Pharmaceutical Biology

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Context: Osteoporosis is one of the most common bone diseases, and radix of Pueraria lobata (Willd.) Ohwi possesses an obvious therapeutical effect on postmenopausal osteoporosis. Objective: This study investigates the anti-osteoporotic activity of the puerarin 6 00 -O-xyloside (PXY) on ovariectomized mice and its related mechanism. Materials and methods: Osteoporotic mice model was established by ovariectomy (OVX). A total of 50 mice were divided into five groups (n ¼ 10): sham, OVX group, PXY treatment groups (20, 40, and 60 mg/kg/d, i.p.). After 12 weeks' treatment, body weights were recorded. Then, mice were sacrificed, and serum samples were collected to determine the blood calcium, blood phosphorus, alkaline phosphatase (ALP), and osteoprotegerin (OPG) concentrations and uterine index was assayed. The thigh-bones of mice were collected to evaluate histopathological changes. In the in vitro experiment, the effect of PXY on osteoblasts' proliferation was evaluated and western blotting was performed to determine expressions of OPG and the receptor activators of NF-B ligand (RANKL), as well as the ratio of OPG/RANKL. Results: PXY (40 and 60 mg/kg/d, i.p.) obviously decreased body weights and increased uterine index of OVX (p50.05), and improved osteoporotic syndromes of OVX mice; PXY also significantly increased the concentrations of blood calcium, blood phosphorus, ALP, and OPG of OVX mice (p50.05); moreover, PXY obviously up-regulated the ratio of OPG/RANKL (p50.05). Conclusion: Our results demonstrated that the puerarin 6 00 -O-xyloside possesses significant anti-osteoporotic activity on ovariectomy mice.

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“…This procedure was adapted from previously reported methodologies [ 19 , 20 ]. Briefly, ethanol extracts were dissolved in ethanol to produce stock solutions at 100 mg/mL.…”

Section: Methodsmentioning

confidence: 99%

Estrogen and Thyroid Hormone Receptor Activation by Medicinal Plants from Bahia, Brazil

et al. 2018

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Background: A number of medicinal plants are traditionally used for metabolic disorders in Bahia state, Brazil. The aim of this study was to evaluate the estrogen receptor (ER) and thyroid receptor (TR) activation of crude extracts prepared from 20 plants. Methods: Species were extracted and assayed for receptor activation through both ER and TR gene-reporter assays, using 17β-estradiol and triiodothyronine (T3), respectively, as the positive controls. Results: Cajanus cajan (Fabaceae), Abarema cochliacarpus (Fabaceae), and Borreria verticillata (Rubiaceae) were able to activate ER as much as the positive control (17β-estradiol). These three plant species were also assayed for TR activation. At the concentration of 50 µg/mL, C. cajans exerted the highest positive modulation on TR, causing an activation of 59.9%, while B. verticillata and A. cochliacarpus caused 30.8% and 23.3%, respectively. Conclusions: Our results contribute towards the validation of the traditional use of C. cajans, B. verticillata, and A. cochliacarpus in the treatment of metabolic disorders related to ER and TR functions. The gene-reporter assay was proven effective in screening crude plant extracts for ER/TR activation, endorsing this methodology as an important tool for future bioprospection studies focused on identifying novel starting molecules for the development of estrogen and thyroid agonists.

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Establishment of a luciferase assay-based screening system for detecting estrogen receptor agonists in plant extracts

Cited by 5 publications

References 43 publications

Polydatin possesses notable anti-osteoporotic activity via regulation of OPG, RANKL and β-catenin

Polydatin possesses notable anti-osteoporotic activity via regulation of OPG, RANKL and β-catenin

Anti-osteoporotic activity of puerarin 6″-O-xyloside on ovariectomized mice and its potential mechanism

Estrogen and Thyroid Hormone Receptor Activation by Medicinal Plants from Bahia, Brazil

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