Identification of Free-B-Ring flavonoids as potent COX-2 inhibitors
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
A01N-065/00
A61K-031/7048
A61K-036/539
A61K-031/353
출원번호
US-0970283
(2013-08-19)
등록번호
US-9061039
(2015-06-23)
발명자
/ 주소
Jia, Qi
Nichols, Timothy C.
Rhoden, Eric E.
Waite, Scott
출원인 / 주소
Unigen, Inc.
대리인 / 주소
Seed IP Law Group PLLC
인용정보
피인용 횟수 :
0인용 특허 :
77
초록▼
The present invention provides a novel method for inhibiting the cyclooxygenase enzyme COX-2. The method is comprised of administering a composition containing a Free-B-Ring flavonoid or a composition containing a mixture of Free-B-Ring flavonoids to a host in need thereof. The present also includes
The present invention provides a novel method for inhibiting the cyclooxygenase enzyme COX-2. The method is comprised of administering a composition containing a Free-B-Ring flavonoid or a composition containing a mixture of Free-B-Ring flavonoids to a host in need thereof. The present also includes novel methods for the prevention and treatment of COX-2 mediated diseases and conditions. The method for preventing and treating COX-2 mediated diseases and conditions is comprised of administering to a host in need thereof an effective amount of a composition containing a Free-B-Ring flavonoid or a composition containing a mixture of Free-B-Ring flavonoids and a pharmaceutically acceptable carrier.
대표청구항▼
1. A method for reducing joint dysfunction, comprising administering to a human or animal having joint pain, joint stiffness, or impaired physical function due to joint dysfunction a therapeutically effective amount of a composition comprising a Scutellaria extract enriched for a Free-B-Ring flavono
1. A method for reducing joint dysfunction, comprising administering to a human or animal having joint pain, joint stiffness, or impaired physical function due to joint dysfunction a therapeutically effective amount of a composition comprising a Scutellaria extract enriched for a Free-B-Ring flavonoid or a mixture of Free-B-Ring flavonoids, wherein the method inhibits peroxidase activity which reduces joint dysfunction in the human or animal. 2. The method according to claim 1, the Free-B-Ring flavonoid or mixture of Free-B-Ring flavonoids are compounds having a structure as follows: wherein R1, R2, R3, R4, and R5 are independently a —H, —OH, —SH, —OR, —SR, —NH2, —NHR, —N(R)2, —N(R)3+X−; a carbon, oxygen, nitrogen or sulfur glycoside of a single or a combination of multiple sugars selected from aldopentose, methyl-aldopentose, aldohexose, or ketohexose;wherein R is an alkyl group having 1-10 carbon atoms; andX is hydroxyl, chloride, fluoride, iodide, sulfate, phosphate, acetate, or carbonate. 3. The method according to claim 1, wherein the Scutellaria is Scutellaria baicalensis, Scutellariae lateriflora, Scutellariae radix, or Scutellariae orthocalyx. 4. The method according to claim 1, wherein the Scutellaria extract enriched for a Free-B-Ring flavonoid or mixture of Free-B-Ring flavonoids is extracted from a plant part selected from stems, stem barks, twigs, tubers, roots, root barks, young shoots, seeds, rhizomes, flowers, leaves, or other aerial parts. 5. The method according to claim 1, wherein the joint dysfunction is associated with systemic lupus erythematosis, rheumatoid arthritis, or osteoarthritis. 6. The method according to claim 1, wherein the Scutellaria extract enriched for a Free-B-Ring flavonoid or mixture of Free-B-Ring flavonoids comprises baicalin. 7. The method according to claim 1, wherein the Scutellaria extract enriched for a Free-B-Ring flavonoid or mixture of Free-B-Ring flavonoids is formulated as a composition comprising a pharmaceutically acceptable carrier, excipient, or both. 8. The method according to claim 7, wherein the composition comprises 0.01% to 100% Free-B-Ring flavonoid or mixture of Free-B-Ring flavonoids. 9. The method according to claim 7, wherein the composition is administered at a dose of 0.01 to 200 mg/kg of body weight of the human or animal. 10. A method for reducing joint dysfunction, comprising administering to a human or animal having joint pain, joint stiffness, or impaired physical function due to joint dysfunction a therapeutically effective amount of a composition comprising an anti-oxidant enhancing Scutellaria extract enriched for a Free-B-Ring flavonoid or a mixture of Free-B-Ring flavonoids, wherein the method has anti-oxidant enhancing activity which inhibits peroxidase activity and reduces joint dysfunction in the human or animal. 11. The method according to claim 10, the Free-B-Ring flavonoid or mixture of Free-B-Ring flavonoids are compounds having a structure as follows: wherein R1, R2, R3, R4, and R5 are independently a —H, —OH, —SH, —OR, —SR, —NH2, —NHR, —N(R)2, —N(R)3+X−; a carbon, oxygen, nitrogen or sulfur glycoside of a single or a combination of multiple sugars selected from aldopentose, methyl-aldopentose, aldohexose, or ketohexose;wherein R is an alkyl group having 1-10 carbon atoms; andX is hydroxyl, chloride, fluoride, iodide, sulfate, phosphate, acetate, or carbonate. 12. The method according to claim 10, wherein the Scutellaria is Scutellaria baicalensis, Scutellariae lateriflora, Scutellariae radix, or Scutellariae orthocalyx. 13. The method according to claim 10, wherein the Scutellaria extract enriched for a Free-B-Ring flavonoid or mixture of Free-B-Ring flavonoids is extracted from a plant part selected from stems, stem barks, twigs, tubers, roots, root barks, young shoots, seeds, rhizomes, flowers, leaves, or other aerial parts. 14. The method according to claim 10, wherein the joint dysfunction is associated with systemic lupus erythematosis, rheumatoid arthritis, or osteoarthritis. 15. The method according to claim 10, wherein the human or animal has impaired physical function due to joint dysfunction. 16. The method according to claim 10, wherein the Scutellaria extract enriched for a Free-B-Ring flavonoid or mixture of Free-B-Ring flavonoids comprises baicalin. 17. The method according to claim 10, wherein the Scutellaria extract enriched for a Free-B-Ring flavonoid or mixture of Free-B-Ring flavonoids is formulated as a composition comprising a pharmaceutically acceptable carrier, excipient, or both. 18. The method according to claim 17, wherein the composition comprises 0.01% to 100% Free-B-Ring flavonoid or mixture of Free-B-Ring flavonoids. 19. The method according to claim 17, wherein the composition is administered at a dose of 0.01 to 200 mg/kg of body weight of the human or animal.
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