Cincinnati Children's Hospital Medical Center

Colorado State University Research Foundation

Brigham Young University

Australian Health & Nutrition Association Limited

Girindus America, Inc.

Australian Health & Nutrition Assoc. Ltd.

Ausio Pharmaceuticals, LLC

Farchioni Olii - S.p.a.

Kenneth David Reginald Setchell

Sidney John Cole

Edwin Douglas Lephart

Trent D Lund

Robert J Handa

Victor Dmitrievich Sorokin

Carlo Clerici

A composition for use in making commercial food and skin products comprising 5-equol or mixtures, including both a non-racemic mixture and a racemic mixture, of S-equol and R-equol. The composition can be used to make articles of commerce such as food supplements, pharmaceuticals, and medicaments. The compositions are useful in a method of delivering S-equol to a mammal to prevent or treat a disease or associated condition, including hormone-dependent diseases or conditions such as cardiovascular disease, lipid disorder, osteopenia, osteoporosis, liver disease, and acute ovarian estrogen deficiency. The S-equol enantiomer can be produced in a biological synthesis from the metabolism of an isoflavone by an organism.

Compositions and products containing S-equol, and methods for their making

A composition for use in making commercial food and skin products comprising R-equol. The composition can be used to make articles of commerce such as food supplements, pharmaceuticals, and medicaments. The compositions are useful in a method of delivering R-equol to a mammal to prevent or treat a disease or associated condition, including hormone-dependent diseases or conditions such as cardiovascular disease, lipid disorder, osteopenia, osteoporosis, liver disease, and acute ovarian estrogen deficiency. The R-equol enantiomer can be produced by chiral-phase column separation from a racemic mixture of equol.

Compositions and products containing R-equol, and methods for their making

A composition for use in making commercial food and skin products comprising S-equol or mixtures, including both a non-racemic mixture and a racemic mixture, of S-equol and R-equol. The composition can be used to make articles of commerce such as food supplements, pharmaceuticals, and medicaments. The compositions are useful in a method of delivering S-equol to a mammal to prevent or treat a disease or associated condition, including hormone-dependent diseases or conditions such as cardiovascular disease, lipid disorder, osteopenia, osteoporosis, liver disease, and acute ovarian estrogen deficiency. The S-equol enantiomer can be produced in a biological synthesis from the metabolism of an isoflavone by an organism.

A method for preparing an enantiomeric chromane, by asymmetrically hydrogenating a chromene compound in the presence of an Ir catalyst having a chiral ligand. The method includes the enantioselective preparation of enantiomeric equol. A preferred Ir catalyst has a chiral phosphineoxazoline ligand. Enantiomeric chromanes of high stereoselective purity can be obtained.

Method for enantioselective hydrogenation of chromenes

Equol (7-hydroxy-3(4'hydroxyphenyl)-chroman), the major metabolite of the phytoestrogen daidzein, specifically binds and blocks the hormonal action of 5&#x3b1;-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 of skin and hair. Thus, equol can specifically bind DHT and prevent DHT's biological actions in physiological and pathophysiological processes affecting skin and hair.

Use of equol for treating skin diseases

The invention is directed to a method of preventing or ameliorating a neuropsychiatric or neurodegenerative disease or disorder in a subject. The method includes administering a composition comprising equol in an amount sufficient to prevent or ameliorate the neuropsychiatric or neurodegenerative disease or disorder. The equol may be a racemic mixture of R-equol and S-equol. The equol may be enantiomerically enriched with R-equol or enantiomerically enriched with S-equol.

Use of equol for ameliorating or preventing neuropsychiatric and neurodegenerative diseases or disorders

Equol (7-hydroxy-3(4'hydroxyphenyl)-chroman), the major metabolite of the phytoestrogen daidzein, specifically binds and blocks the hormonal action of 5&#x3b1;-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.

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Cincinnati, OH, United States of America

Kenneth David Reginald Setchell