Use of equol for treating androgen mediated diseases

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.

1 - 22 . (canceled)  
   
   
       23 . A method of modulating physiological and pathophysiological conditions mediated by androgens in a mammal, comprising the step of administering to the mammal an effective amount of an enantiomeric equol that can bind with free 5α-dihydrotestosterone, thereby inhibiting the binding of 5α-dihydrotestosterone with the androgen receptors in the mammal and mediating the conditions mediated by the androgen.  
   
   
       24 . The method according to  claim 23 , wherein the physiological and pathophysiological conditions is selected from the group consisting of: benign prostatic hyperplasia, prostate cancer, male and female pattern baldness, facial and body hair, acne, excessive secretion of sebum from the sebaceous glands, skin effects, anti-aging, anti-photoaging, skin integrity, skin pigmentation, skin whitening, Alzheimer's disease, emotions and mental health, depression, anxiety, Tourette's disease, Kennedy's syndrome, congenital defects in steroidal hormone synthesis and metabolism involving androgens, obesity, body weight, lipid and cholesterol levels, lipogenesis, lipolysis, inhibiting insulin resistance, blood pressure, thyroid function, and cardiovascular disease.  
   
   
       25 . The method according to  claim 23  wherein the equol is administered as an oral composition comprising at least 1 mg enantiomeric equol.  
   
   
       26 . The method according to  claim 23  wherein the equol is administered as a topical composition comprising at least 0.1% enantiomeric equol.  
   
   
       27 . The method according to  claim 23 , wherein the equol is administered as a composition comprising essentially the R-equol enantiomer.  
   
   
       28 . The method according to  claim 23 , wherein the equol is administered as a composition comprising essentially the S-equol enantiomer.  
   
   
       29 . The method according to  claim 23  wherein the equol is administered as a composition comprising a non-racemic mixture of R-equol and S-equol enantiomers.  
   
   
       30 . A method of treating and preventing an androgen-related disease in a mammal, comprising the step of administering to the mammal an effective amount of an enantiomeric equol that can bind with free 5 α-dihydrotestosterone, thereby inhibiting the binding of the 5α-dihydrotestosterone with the androgen receptors in the mammal.  
   
   
       31 . The method according to  claim 30 , wherein the androgen-related disease is selected from the group consisting of: benign prostatic hyperplasia, prostate cancer, male and female pattern baldness, facial and body hair, acne, excessive secretion of sebum from the sebaceous glands, skin effects, anti-aging, anti-photoaging, skin integrity, skin pigmentation, Alzheimer's disease, abnormal emotions and mental health, depression, anxiety, Tourette's disease, Kennedy's syndrome, congenital defects in steroidal hormone synthesis and metabolism involving androgens, obesity, body weight, abnormal lipid and cholesterol levels, excessive lipogenesis, lipolysis, inhibiting insulin resistance, high blood pressure, thyroid function, and cardiovascular disease.  
   
   
       32 . The method according to  claim 30 , wherein the equol is administered as a composition comprising essentially the R-equol enantiomer.  
   
   
       33 . The method according to  claim 30 , wherein the equol is administered as a composition comprising essentially the S-equol enantiomer.  
   
   
       34 . The method according to  claim 30  wherein the equol is administered as a composition comprising a non-racemic mixture of R-equol and S-equol enantiomers.  
   
   
       35 . The method according to  claim 30  wherein the equol is administered as an oral composition comprising at least 1 mg enantiomeric equol.  
   
   
       36 . The method according to  claim 30  wherein the equol is administered as a topical composition comprising at least 0.1% enantiomeric equol.  
   
   
       37 . The method according to  claim 30  wherein said composition does not comprise a significant amount of any other androgen-receptor binding compound.  
   
   
       38 . A method of treating and preventing a combination of an androgen-related condition and an estrogen-related condition in a mammal, comprising the step of administering to a mammal an effective amount of a mixture of R-equol and S-equol, that can bind with free 5α-dihydrotestosterone, and with free 5α-dihydrotestosterone and the estrogen receptor, respectively, thereby inhibiting the binding of the 5α-dihydrotestosterone with the androgen receptors, and affecting binding of the estrogen receptors.  
   
   
       39 . The method according to  claim 38  wherein the combination of androgen-related and estrogen-related conditions comprises an age-related androgen/estrogen hormonal balance, the method further comprising the step of determining the mammal's endocrine androgen/estrogen hormone balance, and wherein administering the mixture of R-equol and S-equol can modulate the hormone balance of 5α-dihydrotestosterone and estrogen.  
   
   
       40 . The method according to  claim 38  wherein the mixture of equol is administered as an oral composition comprising at least 1 mg equol.  
   
   
       41 . The method according to  claim 38  wherein the mixture of equol is administered as a topical composition comprising at least 0.1% equol.  
   
   
       42 . The method according to  claim 38  wherein the mixture of equol is administered as a composition comprising a non-racemic mixture of R-equol and S-equol enantiomers.  
   
   
       43 . The method according to  claim 39  wherein the mixture of equol is administered as a composition comprising a non-racemic mixture of R-equol and S-equol enantiomers.  
   
   
       44 . The method according to  claim 38  wherein the composition does not comprise a significant amount of any other androgen-receptor binding compound.