scholarly journals Evidence for selective estrogen receptor modulator activity in a black cohosh (Cimicifuga racemosa) extract: comparison with estradiol-17beta

2003 ◽  
pp. 351-362 ◽  
Author(s):  
D Seidlova-Wuttke ◽  
O Hesse ◽  
H Jarry ◽  
V Christoffel ◽  
B Spengler ◽  
...  
Keyword(s):  
Gene Expression ◽  
Estrogen Receptor ◽  
Selective Estrogen Receptor Modulator ◽  
Ovariectomized Rats ◽  
Tartrate Resistant Acid Phosphatase ◽  
Complement Protein ◽  
Cimicifuga Racemosa ◽  
Mineral Density ◽  
Receptor Modulator ◽  
Igf I

OBJECTIVE: Some phytoestrogens are believed to have selective estrogen receptor modulator (SERM) activity with no action in the uterus but beneficial effects in the hypothalamo/pituitary unit and in the bone and are presently the focus of clinical interest. In the present experiments, the effects of the clinically used Cimicifuga racemosa (CR) extract BNO 1055 in the uterus, in the bone and on serum luteinizing hormone (LH) were compared with the effects of estradiol-17beta (E(2)) under acute and chronic conditions in ovariectomized rats. METHODS: Ovariectomized rats were treated either acutely (6 h) or chronically (3 Months) with E(2) or the CR extract. Gene expression of some estrogen-regulated genes in the metaphysis of the tibia and the uterus was determined. Furthermore, bone mineral density was measured by quantitative computer tomography. RESULTS: When given acutely, both E(2) and the CR extract inhibited LH secretion and slightly stimulated gene expression of IGF-I, collagen-1alpha1, osteoprotegerin and osteocalcin (all osteoblast products), and of tartrate-resistant acid phosphatase (TRAP, an osteoclast product) in the metaphysis of the femur. While E(2) stimulated uterine weight and expression of progesterone receptor (PR), the complement protein (C3) and IGF-I genes, and inhibited gene expression of the estrogen receptor beta (ERbeta) in the uterus, no such effect was observed under acute CR treatment. After chronic application with pelleted food over 3 Months E(2) had profound effects in the uterus on weight and gene expression (ERbeta, PR, C3 and IGF-I) which were not seen in the CR-treated animals. Within 3 Months after ovariectomy, control rats had lost more than 50% of the metaphyseal bone mass of the tibia, an effect prevented by E(2) and partially by CR supplementation. CONCLUSIONS: These data confirm the concept that the CR extract BNO 1055 contains as yet unidentified substances with SERM properties which act in the hypothalamo/pituitary unit and in the bone but not in the uterus.

scholarly journals Selective estrogen receptor modulator lasofoxifene suppresses spondyloarthritis manifestation and affects characteristics of gut microbiota in zymosan-induced SKG mice

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Hyemin Jeong ◽  
In Young Kim ◽  
Eun-Kyung Bae ◽  
Chan Hong Jeon ◽  
Kwang-Sung Ahn ◽  
...  
Keyword(s):  
Estrogen Receptor ◽  
Gut Microbiota ◽  
Small Animal ◽  
Joint Inflammation ◽  
Fecal Calprotectin ◽  
Selective Estrogen Receptor Modulator ◽  
Mineral Density ◽  
Receptor Modulator ◽  
Significant Difference ◽  
Microbiota Diversity

AbstractAnkylosing spondylitis is a male-predominant disease and previous study revealed that estrogens have an anti-inflammatory effect on the spondyloarthritis (SpA) manifestations in zymosan-induced SKG mice. This study aimed to evaluate the effect of selective estrogen receptor modulator (SERM) lasofoxifene (Laso) on disease activity of SpA. Mice were randomized into zymosan-treated, zymosan + 17β-estradiol (E2)-treated, and zymosan + Laso-treated groups. Arthritis was assessed by 18F-fluorodeoxyglucose (18F-FDG) small-animal positron emission tomography/computed tomography and bone mineral density (BMD) was measured. Fecal samples were collected and 16S ribosomal RNA gene sequencing was used to determine gut microbiota differences. Both zymosan + E2-treated mice and zymosan + Laso-treated mice showed lower arthritis clinical scores and lower 18F-FDG uptake than zymosan-treated mice. BMD was significantly higher in zymosan + E2-treated mice and zymosan + Laso-treated mice than zymosan-treated mice, respectively. Fecal calprotectin levels were significantly elevated at 8 weeks after zymosan injection in zymosan-treated mice, but it was not significantly changed in zymosan + E2-treated mice and zymosan + Laso-treated mice. Gut microbiota diversity of zymosan-treated mice was significantly different from zymosan + E2-treated mice and zymosan + Laso-treated mice, respectively. There was no significant difference in gut microbiota diversity between zymosan + E2-treated mice and zymosan + Laso -treated mice. Laso inhibited joint inflammation and enhanced BMD in SKG mice, a model of SpA. Laso also affected the composition and biodiversity of gut microbiota. This study provides new knowledge regarding that selected SpA patients could benefit from SERM treatment.

scholarly journals Raloxifene, a Selective Estrogen Receptor Modulator, Reduces Carrageenan-Induced Acute Inflammation in Normal and Ovariectomized Rats

Endocrinology ◽  
2005 ◽  
Vol 146 (8) ◽  
pp. 3301-3308 ◽  
Author(s):  
Emanuela Esposito ◽  
Anna Iacono ◽  
Giuseppina Mattace Raso ◽  
Maria Pacilio ◽  
Anna Coppola ◽  
...  
Keyword(s):  
Estrogen Receptor ◽  
Acute Inflammation ◽  
Selective Estrogen Receptor Modulator ◽  
Ovariectomized Rats ◽  
Receptor Modulator

scholarly journals Idoxifene: A Novel Selective Estrogen Receptor Modulator Prevents Bone Loss and Lowers Cholesterol Levels in Ovariectomized Rats and Decreases Uterine Weight in Intact Rats

Endocrinology ◽  
1998 ◽  
Vol 139 (12) ◽  
pp. 5224-5234 ◽  
Author(s):  
Mark E. Nuttall ◽  
Jeremy N. Bradbeer ◽  
George B. Stroup ◽  
Daniel P. Nadeau ◽  
Sandra J. Hoffman ◽  
...  
Keyword(s):  
Estrogen Receptor ◽  
Bone Loss ◽  
Selective Estrogen Receptor Modulator ◽  
Ovariectomized Rats ◽  
Uterine Weight ◽  
Receptor Modulator ◽  
Cholesterol Levels ◽  
Intact Rats

scholarly journals Selective Estrogen Receptor Modulator LY353381.HCl-Mediated Neuroprotection and BCL-2 Expression After Experimental Stroke

Stroke ◽  
2001 ◽  
Vol 32 (suppl_1) ◽  
pp. 327-327
Author(s):  
Mark Rossberg ◽  
Nabil J Alkayed ◽  
Hung D Joh ◽  
Stephanie J Murphy ◽  
Richard J Trastman ◽  
...  
Keyword(s):  
Blood Flow ◽  
Estrogen Receptor ◽  
Selective Estrogen Receptor Modulator ◽  
Ovariectomized Rats ◽  
Experimental Stroke ◽  
Ribonuclease Protection Assay ◽  
Cerebral Tissue ◽  
Doppler Flowmetry ◽  
Receptor Modulator ◽  
Ovx Rats

62 Estrogen replacement in ovariectomized rats reduces cerebral tissue infarction sustained after experimental stroke. We hypothesized that LY353381.HCl, a selective estrogen receptor modulator (SERM), reduces cerebral tissue infarction after middle cerebral artery occlusion (MCAO), and that the mechanism of protection is not related to preservation of blood flow. After 5–9 days of treatment with LY353381.HCl (LY) or vehicle (VEH), ovariectomized rats were subjected to 2 hours of MCAO under halothane anesthesia, followed by 22 hours of recovery. Ischemia was confirmed by laser-Doppler flowmetry. MAP, blood gases, and rectal and temporalis muscle temperature were controlled. Infarct volumes were measured by 2,3,5-triphenyltetrazolium chloride (TTC) staining and digital image analysis. Ovariectomized (OVX) rats treated with LY (n=16) had smaller infarct volumes in the caudoputamen (CP) than VEH (n=14) treated rats, 49%±6% vs. 64%±4% of ipsilateral CP, respectively, P <0.05. Cerebral cortical (CTX) infarct size was not statistically different between treatment groups (7%±3% vs. 13%±4% for LY vs. VEH, respectively). In a second cohort of OVX rats, end ischemic regional cerebral blood flow (CBF) was measured by 14 C-iodoantipyrine autoradiography in LY (n=4) and VEH (n=3) treated rats. Absolute ischemic CBF and tissue volume distribution to low flow zones were similar in both groups. In a final cohort, 22 hours post MCAO, tissue was sampled from representative regions of CTX and CP in OVX (n=5) and LY (n=4) treated groups and analyzed for BCL-2 mRNA expression using ribonuclease protection assay. LY increased BCL-2 mRNA in both ipsilateral CTX and CP. We conclude that LY353381.HCl confers protection from focal cerebral ischemia by mechanisms that are not related to CBF but may involve increased BCL-2 expression.

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