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ESTROGENIC EXTRACTS OF Astragalus membranaceus Fisch. Bge. Var. mongolicus Bge. of the Leguminosae Family AND USES THEREOF

a technology of astragalus membranaceus and extracts, which is applied in the field of plant extract compositions, can solve the problems of unsatisfactory effects, 35% increased breast cancer risk, and recent women's health initiative (whi) study abruptly halted, so as to reduce the risk of one or more estrogen receptors and increase the risk or likelihood

Inactive Publication Date: 2009-03-12
BIONOVO
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The present invention aims to provide estrogenic compositions that can treat diseases associated with the estrogen receptor without increasing the risk of other diseases. These compositions should also be readily obtained from natural sources and have methods of making and using them. The technical effects of this invention include reducing the risk of estrogen receptor-mediated diseases while treating another one, and providing a safer alternative to traditional estrogen therapy.

Problems solved by technology

The patent text discusses the need for estrogenic compositions that can be obtained from natural sources and used for treating various conditions such as osteoporosis, cardiovascular disease, and breast cancer. The text also describes a method for making and using such compositions. The technical problem addressed is the need for safer and more cost-effective alternatives to synthetic estrogen replacement therapy and selective estrogen receptor modulators.

Method used

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  • ESTROGENIC EXTRACTS OF Astragalus membranaceus Fisch. Bge. Var. mongolicus Bge. of the Leguminosae Family AND USES THEREOF
  • ESTROGENIC EXTRACTS OF Astragalus membranaceus Fisch. Bge. Var. mongolicus Bge. of the Leguminosae Family AND USES THEREOF
  • ESTROGENIC EXTRACTS OF Astragalus membranaceus Fisch. Bge. Var. mongolicus Bge. of the Leguminosae Family AND USES THEREOF

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0083]ERβ is weaker than ERα at activating ERE-tkLuc: The effects of E2 on transcriptional activation were examined by transfecting a plasmid containing a classical ERE upstream of the minimal thymidine kinase (tk) promoter linked to the luciferase reporter cDNA and an expression vector for ERα or ERβ. E2 produced a 10-fold greater activation of the ERE in the presence of ERα compared to ERβ in human monocytic U937 cells, but the

[0084]EC50 values were similar.

example 2

[0085]ERβ is more effective than ERα at repressing the TNF-RE-tkLuc: The effects of effects of E2 on ERα and ERβ-mediated transcriptional repression were then compared using the −125 to −82 region of the TNF-α promoter, known as the tumor necrosis factor-response element (TNF-RE). TNF-α produced a 5-10-fold activation of 3 copies of the TNF-RE (−125 to −82) upstream of the tk promoter (TNF-RE tkLuc). E2 repressed TNF-α activation of TNF-RE tkLuc by 60-80% in the presence of ERα and ERβ. However, ERβ was approximately 20 times more effective than ERα at repression (IC50 of 241 pM for ERα versus 15 pM for and ERβ, respectively). It was also found that ERβ is more effective than ERα at repressing the native −1044 to +93 TNF-α promoter. Thus, ERα is much more effective than ERβ at transcriptional activation, whereas ERβ is more effective than ERα at transcriptional repression. In contrast to E2, the antiestrogens, tamoxifen, raloxifene and ICI 182, 780 produced a 2-fold activation of TN...

example 3

[0086]ERβ inhibits ERα-mediated transcriptional activation of ERE-tkLuc: Surprisingly, when ERα or ERβ were coexpressed in U937 cells, the activation by ERα is markedly inhibited (FIG. 1). These data show that ERβ exerts a repressive effect on ERα activation of ERE-tkLuc. Similar results were observed in the breast cancer cell line, MDA-MB-435 (FIG. 2). Other investigators have found a similar repressive effect of ERβ on ERα transactivation in different cell types. These studies indicate that the different activation of ERα and ERβ on ERE-tkLuc and the repressive effect of ERβ on ERα-mediated-transcription are not cell-type specific and results from intrinsic properties of the ERs. The repression of ERα by ERβ requires the formation of an ERα / ERβ heterodimer, because mutations in helix 11 of ERβ that prevent dimerization inhibit its repression activity (data not shown).

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Abstract

Estrogenic extracts of Astragalus membranaceus Fisch. Bge. Var. mongolicus Bge. of the Leguminosae Family are provided. Also provided are methods of using said extracts to achieve an estrogenic effect, especially in a human, e.g. a female human. In some embodiments, the methods include treatment of climacteric symptoms. In some embodiments, the methods include treatment of estrogen receptor positive cancer, such as estrogen responsive breast cancer. In some embodiments, the methods include treatment or prevention of osteoporosis.

Description

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Claims

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Application Information

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Owner BIONOVO
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