• Title/Summary/Keyword: Serm effect

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Selective Estrogen Receptor Modulation by Larrea nitida on MCF-7 Cell Proliferation and Immature Rat Uterus

  • Ahn, Hye-Na;Jeong, Si-Yeon;Bae, Gyu-Un;Chang, Minsun;Zhang, Dongwei;Liu, Xiyuan;Pei, Yihua;Chin, Young-Won;Lee, Joongku;Oh, Sei-Ryang;Song, Yun Seon
    • Biomolecules & Therapeutics
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    • v.22 no.4
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    • pp.347-354
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    • 2014
  • Larrea nitida is a plant that belongs to the Zygophyllaceae family and is widely used in South America to treat inflammatory diseases, tumors and menstrual pain. However, its pharmacological activity remains unclear. In this study we evaluated the property of selective estrogen receptor modulator (SERM) of Larrea nitida extracts (LNE) as a phytoestrogen that can mimic, modulate or disrupt the actions of endogenous estrogens, depending on the tissue and relative amount of other SERMs. To investigate the property of SERM of LNE, we performed MCF-7 cell proliferation assays, estrogen response element (ERE)-luciferase reporter gene assay, human estrogen receptor (hER) binding assays and in vivo uterotrophic assay. To gain insight into the active principles, we performed a bioassay-guided analysis of LNE employing solvents of various polarities and using classical column chromatography, which yielded 16 fractions (LNs). LNE showed high binding affinities for $hER{\alpha}$ and $hER{\beta}$ with $IC_{50}$ values of $1.20{\times}10^{-7}$ g/ml and $1.00{\times}10^{-7}$ g/ml, respectively. LNE induced $17{\beta}$-estradiol (E2)-induced MCF-7 cell proliferation, however, it reduced the proliferation in the presence of E2. Furthermore, LNE had an atrophic effect in the uterus of immature rats through reducing the expression level of progesterone receptor (PR) proteins. LN08 and LN10 had more potent affinities for binding on $hER{\alpha}$ and ${\beta}$ than other fractions. Our results indicate that LNE had higher binding affinities for $hER{\beta}$ than $hER{\alpha}$, and showed SERM properties in MCF-7 breast cancer cells and the rat uterus. LNE may be useful for the treatment of estrogen-related conditions, such as female cancers and menopause.

The Effect of human Immunoglobulin and Chorionic Gonadotropin on the Production of Maternal Blocking Antibody (인혈청(人血淸) 면역글로부린 및 융모성성선자극호르몬이 습관성유산환자의 혈청내 '차단항체' 생성에 미치는 영향)

  • Park, Moon-Il
    • Clinical and Experimental Reproductive Medicine
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    • v.20 no.2
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    • pp.149-156
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    • 1993
  • Human chorionic gonadotropin(hCG) and intravenous immunoglobulin(IVIG) treatment were attempted as a novel therapeutic approach for unexplained recurrent spontaneous abortion(RSA). Forty-four and 3 women with a history of RSA were treated with hCG and IVIG, respectively, during pregnancy. Of these patients, serum blocking factor assay was performed before and after each treatment, in 15 patients; 12 cases with hCG and 3 cases with IVIG. The results were as follows: 1. Of 44 women who receive hCG during pregnancy, 24 delivered healthy infants at term, 10 patients suffered repeat abortion, and 10 women are still pregnant under 28 weeks. Over all success rate of hCG treatment was 70.6% (24/34). Although there is no statistical significance, absolute serm blocking level was decreased after treatment(N=12). 2. Of 3 women who receive IVIG during pregnancy, all 3 women are still pregnant under 28 weeks. Serum blocking level was increased after treatment, however, this increment was not statistically significant. Although no conclusion could be extracted from the patients who received IVIG, the therapeutic effect of hCG is comparable to that of the other therapeutic regimens, such as allogeneic leukocytes. It was postulated that actual etiology of unknown RSA would be classified as hormonal origin although combined etiologies are common in Korean women.

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The Effect of Selective Estrogen Receptor Modulators (SERMs) on the Tamoxifen Resistant Breast Cancer Cells

  • Chang, Bo-Yoon;Kim, Sae-Am;Malla, Bindu;Kim, Sung-Yeon
    • Toxicological Research
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    • v.27 no.2
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    • pp.85-93
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    • 2011
  • Selective estrogen receptor modulators (SERMs) are synthetic molecules which bind to estrogen receptors (ER) and can modulate its transcriptional capabilities in different ways in diverse estrogen target tissues. Tamoxifen, the prototypical SERM, is extensively used for targeted therapy of ER positive breast cancers. Unfortunately, the use of tamoxifen is associated with acquired resistance and some undesirable side effects. This study investigated the availability of the conventional SERMs on the TAM-resistance breast cancer cells. SERMs showed more effectiveness in MCF-7 cells than tamoxifen resistant cells, except toremifene and ospemifene. Especially, toremifene was more efficacious in tamoxifen resistant cells than MCF-7. Ospemifene had similar cytotoxic activity on the two types of breast cancers. The other SERMs used in this experiment didn't inhibit efficiently the proliferation of tamoxifen resistant cells. These results support the possibility to usage of toremifene on tamoxifen resistant cancer. The effectiveness by toremifene on tamoxifen resistant cells might be different pathways from the apoptosis and the autophagy. Further study should be needed to elucidate the underlying mechanism of effect of toremifene on tamoxifen resistant cancer.

Evaluation of in vitro antibacterial Activity of DWP20373, a Novel Fluoroquinolone (플로오로퀴놀론계 항생제인 DWP20373의 in vitro 항균작용)

  • Kim, Ji-Yeon;Choi, Moon-Jung;Han, Seung-Hee;Kim, Byung-O;Shim, Jeom-Soon;Jung, Yeon-Eui;Lee, Jae-Wok;Yu, Young-Hyo;Park, Myung-Hwan
    • YAKHAK HOEJI
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    • v.40 no.3
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    • pp.357-368
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    • 1996
  • The in vitro antibacterial activity of a novel fluoroquinolone, DWP20373(1-Cyclopropyl-6-fluoro-8-methoxy-7-(2,7-diazabicyclo[3,3,0]oct-4-ene-7-yl)-1,4-dihydro-4 oxoquino line-3carboxylic acid) was compared with those of ciprofloxacin (CPFX), sparfloxacin (SPFX) and ofloxacin (OFLX). DWP20373 was more active than SPFX and OFLX but was less potent than CPFX against gram-negative bacteria. DWP20373 showed an excellent activity against L-MRSA and H-MRSA ($MlC_{90}=0.781{\sim}1.563{\mu}g/ml$).The activity of DWP20373 decreased moderately in the presence of 5mM $Mg^{2+}$. However, pH and serum had no effect on the activity of DWP20373. DWP20373 possessed a rapid bactericidal activity against gram-positive and gram-negative strains.

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GnRH Analogue in Controlled Ovarian Hyperstimulation for Gonadotropin Poor Responder (체외수정시술을 위한 성선자극호르몬 과배란유도에 Poor Response를 나타낸 환자에서 GnRH Analogue의 사용)

  • Kim, Sun-Haeng;Lee, Hee-Kyung;Ku, Pyong-Sahm
    • Clinical and Experimental Reproductive Medicine
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    • v.20 no.1
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    • pp.37-43
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    • 1993
  • In 27 patients with the past history of poor response to the gonadotropin superovulation induction due to poor follicular growth or permature surge of endogenous luteinizing hormone, the effectiveness of pituitary supperssion with the gonadotropin releasing hormone agonist(GnRH-a) in in vitro fertilization(IVF) program was evaluated in 43 cycles using a combination regimen of D-Trp-6 LHRH(Decapeptyl, Ferring)and FSH/hMG from June, 1989 to August, 1990 at Korea University Hospital IVF Clinic. At midluteal phase of menstrual cycle, Decapeptyl-CR was administered by long-term protocol to minimize initial agonistic effect of endogenous gonadotropins. After the confirmation of pituitary suppression, about 2-3 weeks after GNRH-a administration, ovarian follicle growth was stimulated with FSH/hMG and followed by transvaginal ultrasonic measurement of follicle size and by monitoring of serm E2 and LH if necessary. When compared with the control group stimulated with gonadotropin regimen only, the cancellation rate and occurrence rate of premature LH surge during gonadotropin treatment were significantly lower in study group(11.6% and 2.4%, respectively). There is no significant differences in the mean number of aspirated oocytes, fertilization/cleavage rate, embryo transfer(ET) rate, and mean number of embryos transferred between the two groups. The pregnancy rate per treatment cycle, 16.3%, and per ET cycle, 23.3%, were significantly higher in the study group compared with those of control group. These data suggest that GnRH-a therapy is effective for previous poor responder In gonadotropin superovulation induction for IVF.

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Effect of Salt Diets on the Lipid Composition in Serum and Liver of Rats (식염첨가식이(食鹽添加食餌)가 흰쥐의 혈청(血淸) 및 간장(肝臟) 중의 지질성분(脂質成分)에 미치는 영향(影響))

  • Park, Kui-Sun;Kim, Seok-Hwan;Jeung, Jeung-Nam
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.14 no.4
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    • pp.375-380
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    • 1985
  • This experiment was undertaken to investigate and compare the effect of salt on the lipid composition in serm and liver of rats. The average body weight gains and food efficiency ratio were not affected by supplementation with salt in diet. Total cholesterol and free cholesterol levels in serum of all experimental diet group were slightly increased by supplementation with salt, while triglyceride levels were significantly increased. HDL-cholesterol levels of all salt supplementation groups were slightly lower than that of the control group, while LDL, VLDL-cholesterol levels of these groups were higher than that of the control group. The ratio of LDL, VLDL-cholesterol to HDL-cholesterol; so called, atheorgenic index, in serum of salt diet groups was slightly higher than that of the control groups. The ratio of LDL, VLDL-lipoprotein to HDL-lipoprotein in salt diet group were significantly higher than that of the control group. The weight of the liver was not affected by diet, but total cholesterol and triglyceride levels of the liver in salt diet groups were higher than that of the control group.

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