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Use of equol for treating androgen mediated diseases

a technology of androgen mediated diseases and equol, which is applied in the direction of hair cosmetics, drug compositions, metabolic disorders, etc., can solve the problems of not testing for testosterone and unclear whether inhibition of 5-reductase will have a deleterious impact on the system, and achieve the effect of preventing dht binding

Inactive Publication Date: 2006-06-08
CHILDRENS HOSPITAL MEDICAL CENT CINCINNATI +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The present invention relates to a method of using an enantiomeric equol to treat and prevent conditions mediated by androgens in a mammal. The equol can bind with free 5α-dihydrotestosterone, thereby inhibiting its binding to the androgen receptors. The invention also relates to a method of regulating the level of LH in vivo by contacting the DHT of the mammal with enantiomeric equol. The invention further relates to a use of enantiomeric equol as a diagnostic agent for androgen-related disorders and a use of equol in a competitive binding assay.

Problems solved by technology

However, these isoflavone molecules do not exist at high levels in their biologically active form in soy foods, but rather are at high abundance in a precursor form.
Equol, however, is not a phytoestrogen, because it is not a natural constituent of plants.
However, testosterone is not the major androgen responsible for growth of the prostate.
However, it is unclear whether inhibition of 5α-reductase will have a deleterious impact on the system, as evidenced by contraindications arising from reported side effects of conventional treatments using 5α-reducatse inhibitors.

Method used

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  • Use of equol for treating androgen mediated diseases
  • Use of equol for treating androgen mediated diseases
  • Use of equol for treating androgen mediated diseases

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0159] This example demonstrates the in vivo effects of equol on prostate size and hormone secretion. Male Sprague-Dawley rats (400-500 grams) are obtained from Charles Rivers Laboratories (Wilmington, Mass., USA). Rats are caged in pairs and maintained on a 12-hour dark 12-hour light schedule (lights on at 0700 h) with ad libitum access to food and water.

[0160] One week following arrival, animals are given subcutaneous (sc) injections (1 / day for 4 days) of either dimethylsulfoxide (DMSO) (vehicle control) or racemic equol (0.25 mg / kg). Eighteen hours after the final injection, animals are killed via decapitation and trunk blood and prostate are collected for analysis.

[0161] A significant reduction in prostate weight is observed in intact males injected subcutaneously with equol in comparison to intact control males. Additionally, luteinizing hormone (LH) in these same intact males is significantly increased in equol compared to control treated males. These finding are shown in FI...

example 2

[0162] In addition to equol's effects on prostate racemic equol blocks the effects of DHT in other tissues, and decreases body weight. One week following arrival, intact males are given subcutaneous injections of either DMSO (control) or equol (0.5 mg / kg) once / day for 7 days. Following treatments animals are weighed and then killed via decapitation and tissue collection (prostate, testes, epididymis, and pituitary).

[0163] A significant weight decrease in the DHT-sensitive epididymis is observed in racemic equol-treated males compared to controls. However, racemic equol did not affect testes weight or pituitary weight. Body weight during this relatively brief treatment period does not differ significantly between racemic equol and control treatments. These results are presented in Table 2.

TABLE 2Tissue weights from intact males given subcutaneouslyinjections of either DMSO (control) or racemic equol.Prostate (g)Epididymis (g)Testes (g)Pituitary (g)Body (g)DMSO (Control)0.58 (±0.05...

example 3

[0164] Adult male Sprague-Dawley rats are randomly assigned to three groups and receive daily injections of either DMSO, a racemic mixture of equol at 0.250 mg / kg / day), R-equol at 0.250 mg / kg / day, or S-equol at 0.250 mg / kg / day. The total volume of each injection is 0.3 cc, administered sc at the nape of the rat's neck After seven consecutive days of treatment, the rats are killed and the body weight gain during the injection period is determined. Rats injected with R-equol have a significant decrease in body weight gain compared to control rats, as shown in Table 3.

TABLE 3Body Weight Gained in Male Sprague-Dawley Rats Treated with Equol.Treatment GroupProstate (g)Epididymis (g)Body Wt Gain (g)Control0.38 (±0.01)0.96 (±0.03)59.4 (±3.4)Racemic Equol (0.25 mg / kg)0.35 (±0.02)0.89 (±.03) 56.1 (±3.7)R-equol (0.25 mg / kg) 0.31 (±0.02)* 0.85 (±0.04)* 45.6 (±5.5)*S-equol (0.25 mg / kg)0.35 (±0.03)0.86 (±0.05)56.1 (±3.1)

*Significant reduction compared to control

[0165] Testis and pituitary gla...

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Abstract

Equol (7-hydroxy-3(4′hydroxyphenyl)-chroman), the major metabolite of the phytoestrogen daidzein, specifically binds and blocks the hormonal action of 5α-dihydrotestosterone (DHT) in vitro and in vivo. Equol can bind circulating free DHT and sequester it from the androgen receptor, thus altering growth and physiological hormone responses that are regulated by androgens. These data suggest a novel model to explain equol's biological properties. The significance of equol's ability to specifically bind and sequester DHT from the androgen receptor have important ramifications in health and disease and may indicate a broad and important usage for equol in the treatment and prevention of androgen-mediated pathologies. Thus, equol can specifically bind DHT and prevent DHT's biological actions in physiological and pathophysiological processes.

Description

CROSS-REFERENCE TO RELATED APPLICATIONS [0001] The present application claims priority to co-pending U.S. provisional patent application No. 60 / 422,469, filed Oct. 29, 2002.GOVERNMENT INTERESTS [0002] This invention was made with Government support under Grant No. NS39951, awarded by the National Institute of Health (NH), and Grant No. NRI 2002-00798, awarded by the U.S. Dept. of Agriculture (USDA). The Government has certain rights in this invention.BACKGROUND OF THE INVENTION [0003] This invention relates equol and its mechanism of action and use as a therapeutic compound for treating and preventing physiological and pathophysiological conditions mediated by androgens. [0004] In recent years phytoestrogens have received increased investigative attention due to their potential protective effects against age-related diseases (e.g. cardiovascular disease and osteoporosis) and hormone-dependent cancers (i.e., breast and prostate cancer). There are three main classifications of phytoes...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/353A61KA61K31/35
CPCA61K31/35A61K31/353A61K31/352A61P3/00A61P3/04A61P3/06A61P3/10A61P5/14A61P5/16A61P5/24A61P5/26A61P5/28A61P5/30A61P5/50A61P9/00A61P9/12A61P13/08A61P15/08A61P15/12A61P17/00A61P17/08A61P17/10A61P17/14A61P17/16A61P25/00A61P25/20A61P25/22A61P25/24A61P25/28A61P35/00A61P43/00A23L33/10A23V2002/00A61K8/498A61K9/0014A61K9/0053A61Q7/00A61Q19/08
Inventor LEPHART, EDWIN DOUGLASLUND, TRENT D.SETCHELL, KENNETH DAVID REGINALDHANDA, ROBERT J.
Owner CHILDRENS HOSPITAL MEDICAL CENT CINCINNATI
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