Claims
- 1. A therapeutic composition prepared by the method comprising:
peracetylating a Boswellia serrata pentacyclic terpene acidic fraction extract to provide a peracetylated product; and optionally oxidizing said peracetylated product with a mild oxidizing agent, to provide a product having a major portion by weight of 3-β-acetoxy-11-keto-β-boswellic acid.
- 2. A composition according to claim 1, wherein said oxidizing agent is a peroxide.
- 3. A composition according to claim 1, wherein said peroxide is tert-butyl hydroperoxide.
- 4. A composition according to claim 1, wherein said oxidizing agent is a metal oxide.
- 5. A composition according to claim 4, wherein said metal oxide is chromium trioxide.
- 6. A composition according to claim 4, wherein said oxidizing agent is an active halogen.
- 7. A composition according to claim 6, wherein said active halogen is an N-substituted halogen.
- 8. A composition according to claim 7, wherein said N-substituted halogen is N-bromo succinimide.
- 9. A method of treating a mammalian host for neoplasia, or inflammation, said method comprising:
administering to said mammalian host a therapeutically effective amount of a composition or its physiologically acceptable salts, prepared according to the method comprising:
peracetylating a Boswellia serrata pentacyclic terpene acidic fraction extract to provide a peracetylated product having a ratio of AKBA to the other boswellic acid components in boswellin increased compared to said acidic fraction.
- 10. A method for treating a mammalian patient for neoplasia, or inflammation, said method comprising:
administering to said mammalian host a therapeutically effective amount of a composition according to claim 1 or its physiologically acceptable salts.
- 11. A method for enhancing the therapeutic activity of the pentacyclic acidic fraction from Boswellia serrata, said method comprising:
peracetylating said acidic fraction with an acetylating agent to provide a peracetylated product; and optionally oxidizing said peracetylated product with a mild oxidizing agent, whereby producing AKBA having enhanced therapeutic activity compared to said pentacyclic acidic fraction.
- 12. A method according to claim 11, wherein said mild oxidant is a peroxide.
- 13. A method according to claim 11, wherein said mild oxidant is a metal oxide
- 14. A method according to claim 11, wherein said mild oxidant is an active halogen.
- 15. A therapeutic composition, comprising:
a mixture of boswellic acids having AKBA in an amount greater than about 20% of the total boswellic acids by weight; a solubilizing agent; and a physiologically compatible carrier.
- 16. The composition of claim 15, wherein said AKBA is present in an amount greater than about 50% of the total boswellic acids in said mixture.
- 17. The composition of claim 15, wherein said AKBA is present in an amount greater than about 85% of the total boswellic acids in said mixture.
- 18. The composition of claim 15, wherein said AKBA is increased by a factor of at least about 90% compared to an unenhanced boswellin.
- 19. The composition of claim 15, wherein said AKBA is present in an amount of about 100% of the total boswellic acids in said mixture.
- 20. A tablet comprising the composition of claim 15 and a binder.
- 21. A capsule comprising the composition of claim 15.
- 22. A solution comprising the composition of claim 15.
- 23. A method for treating a mammal suspected of having neoplasia or inflammation, comprising the steps of:
administering to said mammal a therapeutically active amount of a composition of boswellic acids having AKBA or physiologically acceptable salts thereof in an amount greater than about 20% by weight of the total boswellic acids.
- 24. A method for decreasing production of products of arachidonic acid in a mammal, comprising the step of administering to said mammal a therapeutically effective amount of the composition of claim 15 or one or more of its physiologically acceptable salt.
- 25. A method for treating inflammation in a mammal, comprising the step of administering to said mammal a therapeutically effective amount of the composition of claim 15 or its physiologically acceptable salts.
- 26. A method for treating neoplasia in a mammal, comprising the step of administering to said mammal a therapeutically effective amount of the composition of claim 15 or its physiologically acceptable salts.
- 27. A therapeutic composition, comprising:
a mixture of boswellic acids having BA in an amount less than about 40% of the total boswellic acids by weight and having AKBA in an amount greater than about 20% by weight; and a physiologically compatible carrier.
- 28. A therapeutic composition, comprising:
a mixture of boswellic acids having ABA in an amount less than about 25% of the total boswellic acids by weight and having AKBA in an amount greater than about 20% by weight; and a physiologically compatible carrier.
- 29. A therapeutic composition, comprising:
a mixture of boswellic acids having KBA in an amount less than about 15% of the total boswellic acids by weight and having AKBA in an amount greater than about 20% by weight; and a physiologically compatible carrier.
- 30. A therapeutic composition, comprising:
a mixture of boswellic acids; and one or more compounds selected from the group consisting of resveratrol, resveratrolosides, genistein, licochalcone A and baicalin; wherein the combination of said compounds produces an effect greater than the sum of the effects of each compound individually.
- 31. The composition of claim 30, wherein said effect is anti-neoplastic and/or anti-inflammatory.
- 32. A method for treating neoplasia in a mammal, comprising the step of administering to said mammal a therapeutically effective amount of the composition of claim 27 or at least one of its physiologically acceptable salts.
- 33. A method for treating neoplasia in a mammal, comprising the step of administering to said mammal a therapeutically effective amount of the composition of claim 30 or at least one of its physiologically acceptable salts.
- 34. The method of claim 32, wherein said neoplasia is selected from the group consisting of lymphoblastic leukemia, prostate cancer, lung cancer, melanoma, and breast cancer.
- 35. A method for inhibiting the production of tumor necrosis factor alpha (TNF-α), comprising exposing to a TNF-α-producing cell, a pharmacologically effective amount of a boswellic acid.
- 36. The method of claim 35, wherein said boswellic acid is AKBA-enriched boswellin.
- 37. A method for treating an mammal for a condition characterized by abnormally increased production of TNF-α, comprising administering to said mammal, a therapeutically effective amount of a boswellic acid composition having a concentration of AKBA greater than that present in a pentacyclic acidic fraction of boswellin.
- 38. A method for treating an animal suffering from neoplasia, comprising administering to said mammal, an amount of AKBA-enriched boswellin sufficient to produce a therapeutic effect in said mammal.
- 39. The method of claim 38, wherein said therapeutic effect is a decrease in tumor size.
- 40. The method of claim 38, wherein said therapeutic effect is increase in survival time.
- 41. The composition of claim 27, wherein said boswellic acids include at least one salt that is solubilized in cyclodextrin.
- 42. The composition of claim 30, wherein said boswellic acids include at least one salt that is solubilized in cyclodextrin.
- 43. A method for commercial production of boswellic acids, comprising:
(a) dissolving a crude extract of Boswellia serrata in an organic solvent forming an organic extract; (b) treating said organic extract with a base and water forming an aqueous layer; (c) acidifying said aqueous layer forming an acidified aqueous extract; (d) adding a filtration agent and magnesium sulfate to said acidified aqueous extract; and (e) filtering said extract produced by step (d).
- 44. A method for commercial peracetylation of a boswellic acid extract, comprising:
(a) adding a pyridine and an acetic anhydride to a commercial extract of boswellic acids forming a peracetylated boswellic acid fraction in a solvent; (b) extracting said peracetylated boswellic acid fraction with an inorganic acid and a salt; (c) adding a filtration agent and magnesium sulfate to said peracetylated boswellic acid fraction; (d) exchanging said solvent with acetic acid and water, forming a precipitate; and (d) collecting said precipitate.
- 45. A method for commercial oxidation of boswellic acids, comprising:
(a) adding calcium carbonate to a peracetylated boswellic acid fraction; (b) adding methyl cyclohexene to said preparation obtained in step (a); (c) adding N-bromosuccinimide to the preparation obtained in step (b); and (d) irradiating said preparation obtained in step (c).
- 46. A method for forming a sodium salt of peracetylated boswellic acid, comprising:
(a) adding ethyl acetate and ethanol to a preparation of peracetylated boswellic acid; and (b) adding sodium hydroxide to the preparation obtained in step (a) until a pH of 8 to 9 is reached and a sodium salt of said peracetylated boswellin forms.
- 47. A method for improving the solubility of boswellic acids, comprising
(a) adding (2-hydroxypropyl)-gamma-cyclodextrin to peracetylated boswellin forming a mixture; (b) finely dividing the mixture obtained in step (a); and (c) adding a solution of saturated sodium bicarbonate in water to said finely divided mixture until said mixture dissolves.
- 48. A composition, comprising:
a mixture of boswellic acids enriched in AKBA compared to an pentacyclic terpene acidic fraction of boswellic acids; at least one other phytochemical selected from the group consisting of resveratrol, resveratrolosides, genistein, licochalcone A and baicalin; and a physiologically compatible lipophilic carrier.
RELATED APPLICATION
[0001] This application claims priority under 35 U.S.C. §119 to U.S. Provisional Patent Application Serial No: 60/364,299, filed Mar. 13, 2002, incorporated herein fully by reference.
Provisional Applications (1)
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Number |
Date |
Country |
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60364299 |
Mar 2002 |
US |