scholarly journals Evaluation of estrogenic potential by herbal formula, HPC 03 for in vitro and in vivo

Reproduction ◽  
2018 ◽  
Vol 155 (2) ◽  
pp. 103-113 ◽  
Author(s):  
Bo Yoon Chang ◽  
Dae Sung Kim ◽  
Hye Soo Kim ◽  
Sung Yeon Kim
Keyword(s):  
Estrogen Receptor ◽  
Ovariectomized Rats ◽  
Herbal Formula ◽  
Mineral Density ◽  
Bone Mineral Density Loss ◽  
Ovx Rats ◽  
Estrogenic Potential ◽  
Mcf 7

HPC 03 is herbal formula that consists of extracts from Angelica gigas, Cnidium officinale Makino and Cinnamomum cassia Presl. The present study evaluated the estrogenic potential of HPC 03 by using in vitro and in vivo models. The regulatory mechanisms of HPC 03 in estrogen-dependent MCF-7 cells were assessed. HPC 03 induced the proliferation of estrogen receptor-positive MCF-7 cells, and the proliferation was blocked by the addition of the estrogen antagonist tamoxifen. The estrogen receptorα/β luciferase activities were significantly increased by HPC 03 treatment, which also increased the mRNA expression of the estrogen-responsive genes Psen2, Pgr and Ctsd. Also, we evaluated the ameliorative effects of HPC 03 on menopausal symptoms in ovariectomized rats. HPC 03 treatment in OVX rats significantly affected the uterine weight, increased the expression of estrogen-responsive genes Pgr and Psen2 in uterus, increased bone mineral density loss in the femur and inhibited body weight increase. Serum E2, collagen type 1 and osteocalcin were significantly increased, while serum LH, FSH and ALP were decreased compared with OVX rats. HPC 03 may be a promising candidate for the treatment of menopause, but further research is necessary to determine whether the observed effects also occur in humans.

scholarly journals Osteoprotective Effects of Loganic Acid on Osteoblastic and Osteoclastic Cells and Osteoporosis-Induced Mice

2020 ◽  
Vol 22 (1) ◽  
pp. 233
Author(s):  
Eunkuk Park ◽  
Chang Gun Lee ◽  
Eunguk Lim ◽  
Seokjin Hwang ◽  
Seung Hee Yun ◽  
...  
Keyword(s):  
Osteoclast Differentiation ◽  
Osteoblastic Differentiation ◽  
Common Disease ◽  
Root Extract ◽  
Mouse Bone Marrow ◽  
Mineral Density ◽  
Bone Mineral Density Loss ◽  
In Vivo Experiments

Osteoporosis is a common disease caused by an imbalance of processes between bone resorption by osteoclasts and bone formation by osteoblasts in postmenopausal women. The roots of Gentiana lutea L. (GL) are reported to have beneficial effects on various human diseases related to liver functions and gastrointestinal motility, as well as on arthritis. Here, we fractionated and isolated bioactive constituent(s) responsible for anti-osteoporotic effects of GL root extract. A single phytochemical compound, loganic acid, was identified as a candidate osteoprotective agent. Its anti-osteoporotic effects were examined in vitro and in vivo. Treatment with loganic acid significantly increased osteoblastic differentiation in preosteoblast MC3T3-E1 cells by promoting alkaline phosphatase activity and increasing mRNA expression levels of bone metabolic markers such as Alpl, Bglap, and Sp7. However, loganic acid inhibited osteoclast differentiation of primary-cultured monocytes derived from mouse bone marrow. For in vivo experiments, the effect of loganic acid on ovariectomized (OVX) mice was examined for 12 weeks. Loganic acid prevented OVX-induced bone mineral density loss and improved bone structural properties in osteoporotic model mice. These results suggest that loganic acid may be a potential therapeutic candidate for treatment of osteoporosis.

scholarly journals Identification of the Active Ingredient and Beneficial Effects of Vitex rotundifolia Fruits on Menopausal Symptoms in Ovariectomized Rats

Biomolecules ◽  
2021 ◽  
Vol 11 (7) ◽  
pp. 1033
Author(s):  
Ji Hwan Lee ◽  
Sullim Lee ◽  
Quynh Nhu Nguyen ◽  
Hung Manh Phung ◽  
Myoung-Sook Shin ◽  
...  
Keyword(s):  
Weight Gain ◽  
Body Weight Gain ◽  
Animal Experiments ◽  
Ovariectomized Rats ◽  
Biological Functions ◽  
Menopausal Syndrome ◽  
Active Constituents ◽  
Mcf 7

Estrogen replacement therapy is a treatment to relieve the symptoms of menopause. Many studies suggest that natural bioactive ingredients from plants resemble estrogen in structure and biological functions and can relieve symptoms of menopause. The fruit of V. rotundifolia, called “Man HyungJa” in Korean, is a traditional medicine used to treat headache, migraine, eye pain, neuralgia, and premenstrual syndrome in Korea and China. The aim of the present study was to confirm that V. rotundifolia fruit extract (VFE) exerts biological functions similar to those of estrogen in menopausal syndrome. We investigated its in vitro effects on MCF-7 cells and in vivo estrogen-like effects on weight gain and uterine contraction in ovariectomized rats. Using the polar extract, the active constituents of VFE (artemetin, vitexicarpin, hesperidin, luteolin, vitexin, and vanillic acid) with estrogen-like activity were identified in MCF-7 cells. In animal experiments, the efficacy of VFE in ameliorating body weight gain was similar to that of estrogen, as evidenced from improvements in uterine atrophy. Vitexin and vitexicarpin are suggested as the active constituents of V. rotundifolia fruits.

scholarly journals Drug-Herb Interaction Between Selective Estrogen Receptor Modulators and Estrogenic Herbal Medicine Er-Xian Decoction in Bone in Vivo and in Vitro

2020 ◽  
Author(s):  
Ka-Ying Wong ◽  
Liping Zhou ◽  
Wenxuan Yu ◽  
Christina Chui Wa Poon ◽  
Man-Sau Wong
Keyword(s):  
Estrogen Receptor ◽  
Selective Estrogen Receptor Modulators ◽  
Serum Estradiol ◽  
Mineral Density ◽  
Alp Activity ◽  
Estrogen Receptor Modulators ◽  
Combined Use ◽  
Receptor Modulators

Abstract Background: Er-Xian decoction (EXD), a traditional Chinese Medicine for managing menopausal syndrome and osteoporosis in China, could exert osteoprotective action via activation of estrogen receptor (ERs) and regulation of serum estradiol without causing severe side effects. However, no fundamental studies have explored its potential interaction in the combined use of prescription drugs, Selective Estrogen Receptor Modulators (SERMs), regarding the osteogenic and uterotrophic effects. The present study evaluated the estrogenic effects of EXD and its potential interactions with tamoxifen and raloxifene in bone and uterus using a mature ovariectomized (OVX) Sprague-Dawley (SD) rat model and human osteoblastic MG-63 cells. Methods: Six-month-old female SD rats were randomly assigned to Sham-operated group or seven OVX groups: vehicle, 17ß-estradiol (E2, 1.0 mg/kg.day), Tamoxifen (Tamo, 1.0 mg/kg.day), Raloxifene (Ralo, 3.0 mg/kg.day), EXD (EXD, 1.6 g/kg.day), EXD+Tamoxifen (EXD+Tamo) and EXD+Raloxifene (EXD+Ralo). The effect of EXD on bodyweight, bone mineral density (BMD), bone microarchitecture, biochemical analysis of serum and urine, and uterus were evaluated. In addition, Alkaline phosphatase assay and activation of estrogen-responsive element mediated by EXD and in its combination with SERMs were investigated in MG-63 cells. Results: In vivo, EXD could interact with SERMs to modulate the serum estradiol, follicle-stimulating hormone, osteocalcin level as well as BMD and bone properties in OVX rats. Moreover, EXD could relieve the uterotrophic effect of SERMs. In vitro, EXD crude extract and EXD-treated serum could promote ALP activity. In particular, EXD-treated serum could interact with SERMs on regulating ALP activity in MG-63 cells. Conclusion: Our study demonstrated that EXD in vivo and EXD-treated serum in vitro did not weaken the osteogenic effect of SERMs. Interestingly, EXD seems to ameliorate the uterotrophic effects of SERMs. Therefore, the combined use of EXD and SERMs may be considered safe and effective in managing postmenopausal osteoporosis.

scholarly journals Estrogen modulates the recruitment of myelopoietic cell progenitors in rat through a stromal cell-independent mechanism involving apoptosis

Blood ◽  
1996 ◽  
Vol 87 (7) ◽  
pp. 2683-2692 ◽  
Author(s):  
NK Shevde ◽  
JW Pike
Keyword(s):  
Estrogen Receptor ◽  
Ovarian Function ◽  
Morphological Changes ◽  
Estrogen Treatment ◽  
Ovariectomized Rats ◽  
Terminal Deoxynucleotidyl Transferase ◽  
Protective Effects ◽  
Hematopoietic Stem

Loss of ovarian function leads to a significant increase in the number of bone-resorbing osteoclasts. Estrogen replacement is known to manifest bone protective effects in the treatment of postmenopausal osteoporosis. In the present study, we used ovariectomized rats to examine the effects of estrogen loss at the osteoclast progenitor colony forming unit-granulocyte macrophage (CFU-GM) level. A significant increase in CFU-GM number was observed as early as 7 days following ovariectomy, and correlated directly with an increase in the number of osteoclast-like cells generated in marrow cultures. The increase in CFU-GM following ovariectomy was abrogated in animals that received estrogen treatment in vivo. A similar suppressive effect was observed on CFU-GM number when ovariectomized rat marrow was treated with estrogen in vitro. This effect was blocked in the presence of the estrogen antihormone ICI 164,384. Thus, the data suggest the possibility that estrogen exerts a direct effect on osteoclast progenitors, and does so through the estrogen receptor-mediated mechanism. Ovariectomy also led to an increase in the early hematopoietic stem/progenitor cell population (Thy 1.1+ cells) as determined by FLOW cytometry methods. Morphological changes as well as terminal deoxynucleotidyl transferase assays revealed that estrogen treatment negated growth factor-induced proliferation of these early progenitors by promoting apoptosis. The cellular effects of estrogen in vitro together with the immunocytochemical detection of the estrogen receptor in these cells, strongly support the contention that in addition to osteoclast progenitors such as CFU-GM, earlier hematopoietic progenitors are also unique cellular targets for estrogen action.

scholarly journals The Preventive Effect of Biochanin A on Bone Loss in Ovariectomized Rats: Involvement in Regulation of Growth and Activity of Osteoblasts and Osteoclasts

2013 ◽  
Vol 2013 ◽  
pp. 1-10 ◽  
Author(s):  
Shu-Jem Su ◽  
Yao-Tsung Yeh ◽  
Huey-Wen Shyu
Keyword(s):  
Bone Loss ◽  
Mrna Expression ◽  
Biological Effects ◽  
Biochanin A ◽  
Ovariectomized Rats ◽  
Tartrate Resistant Acid Phosphatase ◽  
Type I ◽  
Mineral Density ◽  
Ovx Rats

Biochanin A (BCA) is a major isoflavone abundant in red clover (Trifolium pretense). The protective effect of BCA on bone loss in an ovariectomized (OVX) animal model has never been clarified. The objective of this study was to investigate the biological effects of BCA on bone loss in OVX ratsin vivoand on the development of osteoblasts and osteoclastsin vitro. Ovariectomy resulted in a marked increase in body weight and a decrease in femoral bone mineral density and trabecular bone volume that was prevented by BCA or 17β-estradiol (E2) treatment. However, an increase in uterine weight was observed in E2-treated OVX rats, but not in response to BCA treatment. Treatment with BCA increased the mRNA expression of osterix, collagen type I, alkaline phosphatase (ALP), and osteocalcin and decreased the mRNA expression of tartrate-resistant acid phosphatase (TRAP) and the receptor activator of nuclear factor-κB ligand (RANKL)/osteoprotegerin (OPG) ratio in the femur of OVX rats. Treatment with BCA or E2 prevented the OVX-induced increase in urinary deoxypyridinoline (DPD) and serum tumor necrosis factorα(TNF-α) and interleukin-1β(IL-1β).In vitro, BCA induced preosteoblasts to differentiate into osteoblasts and increased osteoblast mineralization. BCA inhibited preosteoclasts and osteoclast proliferation and decreased osteoclast bone resorption. These findings suggest that BCA treatment can effectively prevent the OVX-induced increase in bone loss and bone turnover possibly by increasing osteoblastic activities and decreasing osteoclastic activities.

scholarly journals Selective Estrogen Receptor Modulator-Like Activities of Herba epimedii Extract and its Interactions With Tamoxifen and Raloxifene in Bone Cells and Tissues

2021 ◽  
Vol 11 ◽  
Author(s):  
Liping Zhou ◽  
Ka-Ying Wong ◽  
Wenxuan Yu ◽  
Christina Chui-Wa Poon ◽  
Huihui Xiao ◽  
...  
Keyword(s):  
Estrogen Receptor ◽  
Bone Cells ◽  
Sex Hormone ◽  
Hormone Deficiency ◽  
Ovariectomized Rats ◽  
Dependent Manner ◽  
Protective Activity ◽  
Mineral Density ◽  
Alp Activity ◽  
Ovx Rats

Herbaepimedii (HEP), a kidney-tonifying herb, has been commonly used alone or in formula for strengthening kidney function and treating bone disorders. Its bone protective activity has been demonstrated to be via estrogen receptor (ERs). HEP activates the phosphorylation of ERα in an estrogen response element- (ERE-) dependent manner. We examined the bone protective effects of HEP and its potential interactions with Selective Estrogen Receptor Modulators (SERMs, such as tamoxifen and raloxifene) as they act via the same ERs. Six-month-old mature Sprague Dawley sham-operated (Sham) or ovariectomized (OVX) rats were treated with either vehicle, 17ß-estradiol (1.0 mg/kg.day), tamoxifen (Tamo, 1.0 mg/kg.day), raloxifene (Ralo, 3.0 mg/kg.day), HEP (0.16 g/kg.day), or its combinations with respective SERMs (HEP + Tamo; HEP + Ralo) for 12 weeks. HEP and SERMs as well as their combinations significantly restored changes in bone mineral density (BMD), trabecular bone properties, and bone turnover biomarkers induced by ovarian sex hormone deficiency in ovariectomized rats. Besides the increase in serum estradiol, inhibition on follicle stimulating hormone (FSH) might also be involved in the osteoprotective activities of HEP and SERMs. HEP interacted with SERMs to protect bones from ovarian sex hormone deficiency without altering SERMs’ bone protective activities. HEP neither induced changes in uterus weight nor altered the uterotrophic activity of SERMs in OVX rats. In human osteosarcoma MG-63 cells, HEP-treated serum (HEP-Ts) significantly promoted alkaline phosphatase (ALP) activity like the crude HEP extract did but did not stimulate ERE activity. Our study also reported that biologically activated HEP interacted with SERMs to promote ALP activity without altering the action of SERMs at most of the concentrations tested in MG-63 cells. HEP exerted bone protective activity and the use of HEP did not alter the bone protective activities of SERMs when they were used simultaneously in an estrogen-deficient rat model.

scholarly journals Estrogen directly and specifically downregulates NaPi-IIa through the activation of both estrogen receptor isoforms (ERα and ERβ) in rat kidney proximal tubule

2015 ◽  
Vol 308 (6) ◽  
pp. F522-F534 ◽  
Author(s):  
Dara Burris ◽  
Rose Webster ◽  
Sulaiman Sheriff ◽  
Rashma Faroqui ◽  
Moshe Levi ◽  
...  
Keyword(s):  
Estrogen Receptor ◽  
Proximal Tubule ◽  
Rat Kidney ◽  
Ovariectomized Rats ◽  
Kidney Cortex ◽  
Kidney Proximal Tubule ◽  
Receptor Isoforms ◽  
Ovx Rats ◽  
Estrogen Receptor Isoforms

We have previously demonstrated that estrogen (E2) downregulates phosphate transporter NaPi-IIa and causes phosphaturia and hypophosphatemia in ovariectomized rats. In the present study, we examined whether E2directly targets NaPi-IIa in the proximal tubule (PT) and studied the respective roles of estrogen receptor isoforms (ERα and ERβ) in the downregulation of NaPi-IIa using both in vivo and an in vitro expression systems. We found that estrogen specifically downregulates NaPi-IIa but not NaPi-IIc or Pit2 in the kidney cortex. Proximal tubules incubated in a “shake” suspension with E2for 24 h exhibited a dose-dependent decrease in NaPi-IIa protein abundance. Results from OVX rats treated with specific agonists for either ERα [4,4′,4″;-(4-propyl-[1 H]-pyrazole-1,3,5-triyl) trisphenol, PPT] or ERβ [4,4′,4″-(4-propyl-[1 H]-pyrazole-1,3,5-triyl) trisphenol, DPN] or both (PPT + DPN), indicated that only the latter caused a sharp downregulation of NaPi-IIa, along with significant phosphaturia and hypophosphatemia. Lastly, heterologous expression studies demonstrated that estrogen downregulated NaPi-IIa only in U20S cells expressing both ERα and ERβ, but not in cells expressing either receptor alone. In conclusion, these studies demonstrate that rat PT cells express both ERα and ERβ and that E2induces phosphaturia by directly and specifically targeting NaPi-IIa in the PT cells. This effect is mediated via a mechanism involving coactivation of both ERα and ERβ, which likely form a functional heterodimer complex in the rat kidney proximal tubule.

Ethanol Extract of Fructus ligustri lucidi Increased Circulating 1,25(OH)2D3Levels, but Did Not Improve Calcium Balance in Mature Ovariectomized Rats

2016 ◽  
Vol 44 (06) ◽  
pp. 1237-1253 ◽  
Author(s):  
Xiao-Li Dong ◽  
Si-Si Cao ◽  
Li-Ping Zhou ◽  
Liya Denney ◽  
Man-Sau Wong ◽  
...  
Keyword(s):  
Proximal Tubule ◽  
Mineral Metabolism ◽  
Ovariectomized Rats ◽  
Calcium Balance ◽  
Vitamin D Metabolism ◽  
Dihydroxyvitamin D ◽  
Fructus Ligustri Lucidi ◽  
Ovx Rats

Our previous studies found that different extracts or fractions of Fructus ligustri lucidi (FLL) played different roles in altering the regulation of bone and mineral metabolism in different animal models. The present study was designed to compare the actions of FLL ethanol (EE) and water extracts (WE) on bone and mineral metabolism in a 6-month-old mature ovariectomized (OVX) rat model. Our results showed that FLL extracts did not significantly improve systematic Ca balance in mature OVX rats. However, EE, but not WE treatment, significantly increased serum 1,25(OH)2D3levels in mature OVX rats. An in vitro study using human proximal tubule (HKC-8) cells showed that EE, but not WE, significantly enhanced renal 25-dihydroxyvitamin D3-1[Formula: see text]-hydroxylase (1-OHase) mRNA expressions and simultaneously repressed renal 25-dihydroxyvitamin D3-24-hydroxylase (24-OHase) mRNA expressions. Further investigation indicated that EE could significantly induce the protein expression of 1-OHase, but did not alter 24-OHase expression in HKC-8 cells. Our results demonstrated that EE increased circulating 1,25(OH)2D3levels in OVX rats, possibly via upregulation of renal 1-OHase expressions in renal proximal tubule cells. Our study indicates that FLL is a natural oral agent that could directly regulate renal vitamin D metabolism in vivo and in vitro.

scholarly journals Anti-Osteoporotic Effects of Kukoamine B in Osteoblast and Osteoclast Cells and Ovariectomized Mice

2017 ◽  
Author(s):  
Eunkuk Park ◽  
Jeonghyun Kim ◽  
Mun-Chang Kim ◽  
Subin Yeo ◽  
Jieun Kim ◽  
...  
Keyword(s):  
Osteoblast Differentiation ◽  
Osteoclast Differentiation ◽  
Osteoblastic Differentiation ◽  
Nodule Formation ◽  
Mouse Bone Marrow ◽  
Mineral Density ◽  
Bone Mineral Density Loss ◽  
Ovariectomized Mice

Osteoporosis is an abnormal bone remodeling condition characterized by decreased bone density, which leads to high risks of broken bones. Previous studies have demonstrated that Lycii Radicis Cortex (LRC) extract inhibits bone loss in ovariectomized (OVX) mice by enhancing the osteoblast differentiation. A bioactive compound, Kukoamine B (KB), was identified from a fractionation of LRC extract as a candidate component responsible for an anti-osteoporotic effect. This study investigated the anti-osteoporotic effects of KB using in vitro and in vivo osteoporosis models. KB treatment significantly increased the osteoblastic differentiation and mineralized nodule formation of osteoblastic MC3T3-E1 cells, while it significantly decreased the osteoclast differentiation of primary-cultured monocytes derived from mouse bone marrow. The effects of KB on osteoblastic and osteoclastic differentiations under more physiological conditions were also examined. In the co-culture of MC3T3-E1 cells and monocytes, KB promoted osteoblast differentiation but did not affect osteoclast differentiation. For the in vivo experiments, KB significantly inhibited OVX-induced bone mineral density loss and restored the impaired bone structural properties in osteoporosis model mice. These results suggest that KB may be a potential therapeutic candidate for the treatment of osteoporosis.

scholarly journals 2-Phenylacetamide Isolated from the Seeds of Lepidium apetalum and Its Estrogen-Like Effects In Vitro and In Vivo

Molecules ◽  
2018 ◽  
Vol 23 (9) ◽  
pp. 2293 ◽  
Author(s):  
Mengnan Zeng ◽  
Meng Li ◽  
Miao Li ◽  
Beibei Zhang ◽  
Benke Li ◽  
...  
Keyword(s):  
Estrogen Receptor ◽  
Inductive Effect ◽  
Uterine Weight ◽  
Immature Female ◽  
Main Compound ◽  
Material Basis ◽  
Weight Test ◽  
Mcf 7

The aim of this study was to investigate the estrogen-like effects of 2-phenylacetamide (PA), which is the main compound isolated from the seeds of Lepidium apetalum Willd (LA). Results showed that LA and PA could promote the proliferation of MCF-7 cells. The mouse uterine weight test showed that, LA and PA could increase the uterus index of immature female mice, and the levels of luteinizing hormone (LH) and estrogen (E2). LA could increase the expression of ERα and ERβ, while PA could increase the expression of ERα, ERβ and GPR30 in the uterus and MCF-7 cells. In addition, co-incubation of the estrogen receptor blocker with LA or PA abolished the inductive effect of the proliferation. PA has estrogenic activities and was the material basis of LA that played the estrogenic effect. LA and PA might be used for the treatment of perimenopause syndrome in a novel application.

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