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 ◽  
...  
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 ◽  
...  

2003 ◽  
pp. 351-362 ◽  
Author(s):  
D Seidlova-Wuttke ◽  
O Hesse ◽  
H Jarry ◽  
V Christoffel ◽  
B Spengler ◽  
...  

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.


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 ◽  
...  

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.


Metabolism ◽  
2006 ◽  
Vol 55 (5) ◽  
pp. 605-613 ◽  
Author(s):  
Christian Lemieux ◽  
Yves Gélinas ◽  
Josée Lalonde ◽  
Fernand Labrie ◽  
Denis Richard ◽  
...  

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