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.

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 A Novel Estrogen Receptor α-Associated Protein Alters Receptor-Deoxyribonucleic Acid Interactions and Represses Receptor-Mediated Transcription

2004 ◽  
Vol 18 (11) ◽  
pp. 2649-2659 ◽  
Author(s):  
Margaret A. Loven ◽  
Roger E. Davis ◽  
Carol D. Curtis ◽  
Nemone Muster ◽  
John R. Yates ◽  
...  
Keyword(s):  
Estrogen Receptor ◽  
Thyroid Hormone Receptor ◽  
Estrogen Receptor Α ◽  
Target Cells ◽  
Estrogen Response Element ◽  
Response Element ◽  
Estrogen Response ◽  
Mcf 7

Abstract Estrogen receptor α (ERα) serves as a ligand-activated transcription factor, turning on transcription of estrogen-responsive genes in target cells. Numerous regulatory proteins interact with the receptor to influence ERα-mediated transactivation. In this study, we have identified pp32, which interacts with the DNA binding domain of ERα when the receptor is free, but not when it is bound to an estrogen response element. Coimmunoprecipitation experiments demonstrate that endogenously expressed pp32 and ERα from MCF-7 breast cancer cells interact. Although pp32 substantially enhances the association of the receptor with estrogen response element-containing DNA, overexpression of pp32 in MCF-7 cells decreases transcription of an estrogen-responsive reporter plasmid. pp32 Represses p300-mediated acetylation of ERα and histones in vitro and inhibits acetylation of ERα in vivo. pp32 Also binds to other nuclear receptors and inhibits thyroid hormone receptor β-mediated transcription. Taken together, our studies provide evidence that pp32 plays a role in regulating transcription of estrogen-responsive genes by modulating acetylation of histones and ERα and also influences transcription of other hormone-responsive genes as well.

The biologic activity of selenoestrogens

1982 ◽  
Vol 60 (2) ◽  
pp. 152-156 ◽  
Author(s):  
G. Longcope ◽  
T. Arunachalam ◽  
E. Caspi
Keyword(s):  
Estrogen Receptor ◽  
Estrogen Receptors ◽  
Uterine Weight ◽  
Binding Properties ◽  
Active Compounds ◽  
Relative Binding ◽  
Biologic Activity ◽  
Differential Imaging

For differential imaging of mammary tumors with estrogen receptors and without estrogen receptors we required γ-emitting estrogen analogues. In this paper we report on the binding properties of 7α-, 16α-, and 17α-methylselenoestrogens and 17α-phenylselenoestrogens relative to the binding properties of estradiol.The selenium-containing estrogens retained the ability to displace [3H]estradiol from the estrogen receptor of rabbit uterine cytosol, although in most instances the displacement was small (3–7% compared to estradiol).The most active compounds were 16α-phenylselenoestrone, 16α-methylselenoestradiol, and 17α-methylselenomethyl-estradiol which had relative binding of 23, 27, and 31%, respectively, compared with that of estradiol.16α-Methylselenoestradiol was able to translocate the estrogen cytosol receptor to the nucleus, in vitro, but was not able to increase the uterine weight when administered to mice in vivo.

The Effect of Bitter Melon (Momordica charantia) Extract on the Uptake of 99mTc Labeled Paclitaxel: In Vitro Monitoring in Breast Cancer Cells

2020 ◽  
Vol 20 (12) ◽  
pp. 1497-1503 ◽  
Author(s):  
Ayfer Y. Kilcar ◽  
Onur Yildiz ◽  
Tansu Dogan ◽  
Ezgi Sulu ◽  
Gokhan Takan ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Estrogen Receptor ◽  
Cancer Drug ◽  
Breast Carcinoma Cell Line ◽  
Bitter Melon ◽  
Radiolabeled Compounds ◽  
Scientific Attention ◽  
Mcf 7

Background: Bitter Melon Extract (BME) is widely used for the treatment of various diseases worldwide due to its rich phytochemical and antioxidant content. The well-known anti-cancer drug Paclitaxel (PAC) plays a major role in the treatment of various cancer types such as ovarian, breast, and lung cancer. Technetium-99m (99mTc) radiolabeled paclitaxel is emerging as an imaging probe for breast cancer in vivo. 99mTc labeled compounds have been attracting more scientific attention since the achievement of earlier researches in Nuclear Medicine. People consume several types of diets of plant origin without knowing the interaction with radiolabeled compounds or radiopharmaceuticals. Objectives: In the current study, we aimed to monitor the potential effects of the BME on the uptake of 99mTc labeled Paclitaxel (99mTc-PAC) against MCF-7 (ER+) and MDA-MB-231 (ER-) cell lines by using in vitro methods. Methods: BME was obtained by the extraction of BM seeds by 80% ethanol. PAC was labeled with 99mTc by stannous chloride (SnCl2) as a reducing agent. Cytotoxicity and incorporation assays were performed on MCF-7 and MDA-MB-231 cells within the cell culture studies. Results: The uptake value of 99mTc-PAC on MCF-7 cells at 240 minutes was 6.20% and BME treated 99mTc- PAC value was 17.39%. Conclusion: It is observed that BME treatment has a significant effect on the uptake of 99mTc-PAC on MCF-7 cells which is a known estrogen receptor-positive breast carcinoma cell line. It is concluded that this effect could be due to the estrogen receptor-dependent interaction of BME.

Ergosterol (Major Sterol of Baker’s and Brewer’s Yeast Extracts) Inhibits the Growth of Human Breast Cancer Cells in vitro and the Potential Role of its Oxidation Products

2003 ◽  
Vol 73 (1) ◽  
pp. 19-23 ◽  
Author(s):  
M. T. Ravi Subbiah ◽  
W. Abplanalp
Keyword(s):  
Breast Cancer ◽  
Estrogen Receptor ◽  
Cancer Cells ◽  
Breast Cancer Cells ◽  
Oxidation Products ◽  
Brewer’S Yeast ◽  
Brewer's Yeast ◽  
Mcf 7

The derivation of chemopreventive agents from dietary sources has been the subject of considerable attention in recent years. Yeast extracts have been used as nutritional supplements for a number of years. In this communication we show that ergosterol (a 28-carbon sterol found in baker’s and brewer’s yeast) can prevent growth of breast cancer cells in vitro in the presence of estradiol-17beta. Estrogen receptor (+) MCF-7 cells appear to be more sensitive to ergosterol than estrogen receptor (–) MDA-231 cells. However, MDA-231 cells were more sensitive to ergosterol in terms of apoptotic effects than MCF-7 cells, indicating that other mechanisms (antiestrogenic activity) may also be operative in estrogen receptor (+) cells. Compared to freshly prepared ergosterol, stored preparations were more potent in inhibiting growth of cancer cells, indicating that oxidation product(s) of ergosterol may be responsible for the noted effects. Further studies on in vivo effects of ergosterol and lipid extracts of yeast in animal models are warranted to determine their potential for use as supplements in humans.

A Novel Triazole Derivative Drug Presenting In Vitro and In Vivo Anticancer Properties

2018 ◽  
Vol 18 (17) ◽  
pp. 1483-1493
Author(s):  
Ricardo Imbroisi Filho ◽  
Daniel T.G. Gonzaga ◽  
Thainá M. Demaria ◽  
João G.B. Leandro ◽  
Dora C.S. Costa ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cancer Cells ◽  
Cell Line ◽  
Cancer Cell ◽  
Cancer Cell Line ◽  
Hepatic Function ◽  
Anticancer Properties ◽  
Mcf 7

Background: Cancer is a major cause of death worldwide, despite many different drugs available to treat the disease. This high mortality rate is largely due to the complexity of the disease, which results from several genetic and epigenetic changes. Therefore, researchers are constantly searching for novel drugs that can target different and multiple aspects of cancer. Experimental: After a screening, we selected one novel molecule, out of ninety-four triazole derivatives, that strongly affects the viability and proliferation of the human breast cancer cell line MCF-7, with minimal effects on non-cancer cells. The drug, named DAN94, induced a dose-dependent decrease in MCF-7 cells viability, with an IC50 of 3.2 ± 0.2 µM. Additionally, DAN94 interfered with mitochondria metabolism promoting reactive oxygen species production, triggering apoptosis and arresting the cancer cells on G1/G0 phase of cell cycle, inhibiting cell proliferation. These effects are not observed when the drug was tested in the non-cancer cell line MCF10A. Using a mouse model with xenograft tumor implants, the drug preventing tumor growth presented no toxicity for the animal and without altering biochemical markers of hepatic function. Results and Conclusion: The novel drug DAN94 is selective for cancer cells, targeting the mitochondrial metabolism, which culminates in the cancer cell death. In the end, DAN94 has been shown to be a promising drug for controlling breast cancer with minimal undesirable effects.

Derivatives of Deoxypodophyllotoxin Induce Apoptosis Through Bcl-2/Bax Proteins Expression

2020 ◽  
Vol 20 ◽  
Author(s):  
Ya-Nan Li ◽  
Ni Ning ◽  
Lei Song ◽  
Yun Geng ◽  
Jun-Ting Fan ◽  
...  
Keyword(s):  
Annexin V ◽  
Mtt Method ◽  
Anthriscus Sylvestris ◽  
Anti Tumor Activity ◽  
Derivatives Of ◽  
Toxicity In Vitro ◽  
Ht 29 ◽  
Mcf 7

Background: Deoxypodophyllotoxin, isolated from theTraditional Chinese Medicine Anthriscus sylvestris, is well-known because of its significant antitumor activity with strong toxicity in vitro and in vivo. Objective: In this article, we synthesized a series of deoxypodophyllotoxin derivatives, and evaluated their antitumor effectiveness.Methods:The anti tumor activity of deoxypodophyllotoxin derivatives was investigated by the MTT method. Apoptosis percentage was measured by flow cytometer analysis using Annexin-V-FITC. Results: The derivatives revealed obvious cytotoxicity in the MTT assay by decreasing the number of late cancer cells. The decrease of Bcl-2/Bax could be observed in MCF-7, HepG2, HT-29 andMG-63 using Annexin V-FITC. The ratio of Bcl-2/Bax in the administration group was decreased, which was determined by the ELISA kit. Conclusion: The derivatives of deoxypodophyllotoxin could induce apoptosis in tumor cell lines by influencing Bcl-2/Bax.

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.

In vitro evaluation of estrogenic, antiestrogenic and antitumor effects of amentoflavone

2021 ◽  
pp. 096032712199945
Author(s):  
AT Aliyev ◽  
S Ozcan-Sezer ◽  
A Akdemir ◽  
H Gurer-Orhan
Keyword(s):  
Breast Cancer ◽  
Cancer Cells ◽  
Breast Cancer Cells ◽  
Antitumor Effects ◽  
Antiestrogenic Activity ◽  
Er Positive ◽  
In Vivo Effects ◽  
Mcf 7

Apigenin, a flavonoid, is reported to act as an estrogen receptor (ER) agonist and inhibit aromatase enzyme. However, amentoflavone, a biflavonoid bearing two apigenin molecules, has not been evaluated for its endocrine modulatory effects. Besides, it is highly consumed by young people to build muscles, enhance mood and lose weight. In the present study, apigenin was used as a reference molecule and ER mediated as well as ER-independent estrogenic/antiestrogenic activity of amentoflavone was investigated. Antitumor activity of amentoflavone was also investigated in both ER positive (MCF-7 BUS) and triple-negative (MDA-MB-231) breast cancer cells and its cytotoxicity was evaluated in human breast epithelial cells (MCF-10A). Our data confirmed ER agonist, aromatase inhibitory and cytotoxic effects of apigenin in breast cancer cells, where no ER mediated estrogenic effect and physiologically irrelevant, slight, aromatase inhibition was found for amentoflavone. Although selective cytotoxicity of amentoflavone was found in MCF-7 BUS cells, it does not seem to be an alternative to the present cytotoxic drugs. Therefore, neither an adverse effect, mediated by an estrogenic/antiestrogenic effect of amentoflavone nor a therapeutical benefit would be expected from amentoflavone. Further studies could be performed to investigate its in vivo effects.

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