Anxiolytic marcgraviaceae compositions containing betulinic acid, betulinic acid derivatives, and methods
View Patent ↗Pharmaceutical compositions for preventing or treating anxiety, comprising betulinic acid or derivatives thereof are provided. Methods for preventing or treating anxiety with betulinic acid or derivatives thereof are also provided. The invention further provides betulinic-acid containing preparations of plants of the family Marcgraviaceae having anxiolytic activity and methods for making such extracts and using them to prevent or treat anxiety in a subject.
1. A method for treating anxiety in a subject comprising administering to a subject in need thereof a therapeutically effective amount of a compound selected from betulinic acid, methyl dihydrobetulinate, 3-acetoxy betulinic acid, methyl betulinate, methyl 3-acetoxybetulinate, betulinic acid amide, betulinic acid benzylamide, betulinic acid anilide, betulinic acid pyrrolidine amide, betulonic acid isobutyl amide, betulinic acid isobutyl amide, betulinic acid glycine methyl ester amide, betulinic acid glycine amide, dihydrobetulinic acid, ethyl betulinate, 3-acetoxy betulinic acid hydroxylamine, and any one of compounds 18-23 from Table 1, or a pharmaceutically acceptable salt thereof.
2. The method according to claim 1 , wherein said compound is selected from methyl dihydrobetulinate, 3-acetoxy betulinic acid, methyl betulinate, methyl 3-acetoxybetulinate, betulinic acid amide, betulinic acid benzylamide, betulinic acid anilide, betulinic acid pyrrolidine amide, betulonic acid isobutyl amide, betulinic acid isobutyl amide, betulinic acid glycine methyl ester amide, betulinic acid glycine amide, dihydrobetulinic acid, ethyl betulinate, 3-acetoxy betulinic acid hydroxylamine, and pharmaceutically acceptable salts thereof.
3. The method according to claim 1 , wherein said compound is selected from methyl betulinate and ethyl betulinate.
4. The method according to claim 1 , wherein said compound is administered in an amount of from about 0.1 to about 2.5 mg per kg of body weight per dose.
5. The method according to claim 1 , wherein said compound is administered in an amount of from about 0.1 to about 0.25 mg per kg of body weight per dose.
6. The method according to claim 1 , wherein said anxiety is acute anxiety.
7. The method according to claim 1 , wherein said anxiety is chronic anxiety.
8. The method according to claim 1 , wherein said compound is administered orally.
9. The method according to claim 1 , wherein said compound is the sole anxiolytic agent administered.
10. The method according to claim 1 , wherein said compound is betulinic acid, or a pharmaceutically acceptable salt thereof.
11. The method according to claim 10 , wherein said betulinic acid or pharmaceutically acceptable salt thereof is administered in an amount of from 0.1 to 2.5 mg/kg of body weight of said subject per dose.
12. The method according to claim 10 , wherein said betulinic acid or pharmaceutically acceptable salt thereof is administered in an amount of from 0.1 to 0.25 mg/kg of body weight of said subject per dose.
13. The method according to claim 10 , wherein said anxiety is acute anxiety.
14. The method according to claim 10 , wherein said anxiety is chronic anxiety.
15. The method according to claim 10 , wherein said betulinic acid or pharmaceutically acceptable salt thereof is administered daily for a period of at least 21 days.
16. The method according to claim 10 , wherein betulinic acid is the sole anxiolytic agent administered.