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Last Updated: January 26, 2022

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Claims for Patent: 8,668,914

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Summary for Patent: 8,668,914
Title:Use of equol for treating skin diseases
Abstract: Equol (7-hydroxy-3(4\'hydroxyphenyl)-chroman), the major metabolite of the phytoestrogen daidzein, specifically binds and blocks the hormonal action of 5.alpha.-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.
Inventor(s): Lephart; Edwin Douglas (Orem, UT), Lund; Trent D. (St. Charles, IL), Setchell; Kenneth David Reginald (Cincinnati, OH), Handa; Robert J. (Phoenix, AZ)
Assignee: Brigham Young University (Provo, UT) Colorado State University Research Foundation (Fort Collins, CO) Children\'s Hospital Medical Center (Cincinnati, OH)
Application Number:12/533,169
Patent Claims:1. A method of mediating androgen hormone action so as to ameliorate at least one condition of the skin or hair of a subject, comprising administering a non-racemic mixture of R- and S-equol, wherein R-equol binds free 5.alpha.-dihydrotestosterone and inhibits its binding with androgen receptor, and wherein at the least one condition of the skin and hair is selected from the group consisting of: a) inducing increased skin integrity by cell renewal; b) enhancing water content or moisture of skin; c) enhancing glycoaminoglycans and hyaluronic acid for improved skin radiance; d) reducing trans epidermal water loss, skin flaking and scaling; e) invigorating for energetically healthy skin; f) improving skin thickness and enhanced cellular durability; g) strengthening skin collagen and improving skin health; h) enhancing skin tensile properties and improving the protective nature of the skin; i) increasing elastin production and improving skin elasticity; j) protecting against and inhibiting elastase; k) protecting against and inhibiting collagenase; I) protecting against and decreasing matrix metalloproteinases; m) improving skin texture and tone; n) reducing skin pores size and enhancing skin smoothness; o) rejuvenating and renewing skin; p) improving the appearance of scars and skin abrasions and enhancing skin repair and wound healing; q) decreasing oily skin by minimizing sebaceous gland secretion and improving sebaceous gland function; r) enhancing hair pigmentation; s) increasing blood flow in the skin; t) improving skin temperature and thermoregulation of the skin; u) inhibiting fibroblast cell apoptosis; v) stabilizing skin color changes and hair pigmentation and enhancing skin lightening; w) treating, ameliorating and protecting against hyperpigmentation, age-spots and photo-aging; x) decreasing or eliminating acne; y) decreasing scalp hair loss or enhancing the retention of scalp hair (in male and female pattern baldness); z) retarding facial and body hair growth, decreasing facial and body hair growth, and reducing hirsutism; aa)reducing vaginal dryness; and bb)attenuating skin and hair abnormalities in steroid hormone synthesis and function and metabolism of steroids and binding steroid receptors involving androgenic and/or estrogenic effects.

2. The method of claim 1, wherein the non-racemic mixture of R- and S-equol comprises at least 5% of R-equol.

3. The method of claim 1, wherein the non-racemic mixture of R- and S-equol comprises at least 10% of R-equol.

4. The method of claim 1, wherein the non-racemic mixture of R- and S-equol comprises at least 20% of R-equol.

5. The method of claim 1, wherein the non-racemic mixture of R- and S-equol comprises at least 25% of R-equol.

6. The method of claim 1, wherein the non-racemic mixture of R- and S-equol comprises S-equol in an amount sufficient to bind estrogen receptor subtypes.

7. A method of ameliorating at least one condition of the skin or hair of a subject, comprising: administering a composition comprising a non-racemic mixture of R- and S-equol, wherein R-equol binds free 5.alpha.-dihydrotestosterone and inhibits its binding with androgen receptors wherein at the least one condition of the skin and hair is selected from the group consisting of: a) inducing increased skin integrity by cell renewal; b) enhancing water content or moisture of skin; c) enhancing glycoaminoglycans and hyaluronic acid for improved skin radiance; d) reducing trans epidermal water loss, skin flaking and scaling; e) invigorating for energetically healthy skin; f) improving skin thickness and enhanced cellular durability; g) strengthening skin collagen and improving skin health; h) enhancing skin tensile properties and improving the protective nature of the skin; i) increasing elastin production and improving skin elasticity; j) protecting against and inhibiting elastase; k) protecting against and inhibiting collagenase; l) protecting against and decreasing matrix metalloproteinases; m) improving skin texture and tone; n) reducing skin pores size and enhancing skin smoothness; o) rejuvenating and renewing skin; p) improving the appearance of scars and skin abrasions and enhancing skin repair and wound healing; q) decreasing oily skin by minimizing sebaceous gland secretion and improving sebaceous gland function; r) enhancing hair pigmentation; s) increasing blood flow in the skin; t) improving skin temperature and thermoregulation of the skin; u) inhibiting fibroblast cell apoptosis; v) stabilizing skin color changes and hair pigmentation and enhancing skin lightening; w) treating, ameliorating and protecting against hyperpigmentation, age-spots and photo-aging; x) decreasing or eliminating acne; y) decreasing scalp hair loss or enhancing the retention of scalp hair (in male and female pattern baldness); z) retarding facial and body hair growth, decreasing facial and body hair growth, and reducing hirsutism; aa)reducing vaginal dryness; and bb)attenuating skin and hair abnormalities in steroid hormone synthesis and function and metabolism of steroids and binding steroid receptors involving androgenic and/or estrogenic effects.

8. The method of claim 7, wherein the non-racemic mixture of R- and S-equol comprises at least 5% of R-equol.

9. The method of claim 7, wherein the non-racemic mixture of R- and S-equol comprises at least 10% of R-equol.

10. The method of claim 7, wherein the non-racemic mixture of R- and S-equol comprises at least 20% of R-equol.

11. The method of claim 7, wherein the non-racemic mixture of R- and S-equol comprises at least 25% of R-equol.

12. The method of claim 7, wherein the composition is administered topically, transdermally, or subdermally.

13. The method of claim 7, wherein the composition is a topical composition comprising from at least about 0.001% to about 10% equol.

14. The method of claim 7, wherein the composition further comprises a pharmaceutical active or an excipient.

15. The method of claim 7, wherein the composition is administered orally at a dose of at least about 0.005 mg of equol per kg body weight.

16. The method of claim 7, wherein the composition is in a delayed or a sustained release formulation.

17. The method of claim 7, wherein the composition is administered via a lotion, a spray solution, a pad, a bandage, or a transdermal patch.

18. The method of claim 7, wherein the non-racemic mixture of R- and S-equol comprises S-equol in an amount sufficient to bind estrogen receptor subtypes.

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