Anti-cholesterolemic compounds and methods of use

Abstract

The present invention provides novel compounds with hypocholesteremic activity from crude Embilica officinialis (EO) extracts and methods of use. The invention also provides nutraceuticals.

1 .- 47 . (canceled) 
     
     
         48 . A pharmaceutical composition for the treatment or prevention of an elevated blood lipid level-related disease or disorder comprising one or more gallic acid derivatives and a pharmaceutically acceptable excipient. 
     
     
         49 . The pharmaceutical composition of  claim 48 , wherein the gallic acid derivative is derived from EuMil. 
     
     
         50 . The pharmaceutical composition of  claim 48 , wherein the one or more gallic acid derivatives is selected from the group comprising: methyl gallate, ethyl gallate, glycerol-1-gallate, glucose-1-gallate (GG1), glucose-6-gallate (GG6), glucose-1,6-digallate (DGG16), mucic acid-2-gallate, 1-methyl mucate-2-gallate, mucic acid 1,4-lactone 5-gallate, geraniin, corilagin, chebilc acid, and m-digallic acid with minor p-digallic acid. 
     
     
         51 . The pharmaceutical composition of  claim 48 , comprising a combination of gallic acid derivatives selected from the group consisting of: Compound 4+Compound 5+Compound 2a, Compound 4+Compound 8+Compound 2a, Compound 4+Compound 5+Compound 7, Compound 4+Compound 2a, Compound 4+Compound 2b, Compound 7+Compound 2b, Compound 5+Compound 8, and Compound 5+Compound 7. 
     
     
         52 . The pharmaceutical composition of  claim 48 , wherein the at least one gallic acid derivative is present in an amount from about 10 mg-500 mg. 
     
     
         53 . The pharmaceutical composition of  claim 52 , wherein the at least one gallic acid derivative is present in an amount from about 40 mg-200 mg. 
     
     
         54 . The pharmaceutical composition of  claim 48 , further comprising a one or more second agents. 
     
     
         55 . The pharmaceutical composition of  claim 54 , wherein the one or more second agents is a therapeutic agent. 
     
     
         56 . The pharmaceutical composition of  claim 55 , wherein the therapeutic agent is selected from the group consisting of: inhibitors of cholesterol metabolism, inhibitors of triglyceride synthesis, beta blockers, diuretics, inhibitors of platelet aggregation, angiogenesis inhibitors, arthritis medication, toxins, anti-inflammatory agents. 
     
     
         57 . The pharmaceutical composition of  claim 55 , wherein the therapeutic agent is attached to the gallic acid derivative by a covalent linkage. 
     
     
         58 . The pharmaceutical composition of  claim 48 , wherein the composition is administered in a dosage form selected from the group consisting of a: food composition, tablet, pill, gel, capsule, suspension tablet, liquid, solution, patch, aqueous emulsion powder, lozenge, sachet, cachet, elixir, suspension, emulsion, solution, syrup, aerosol, ointment, soft gelatin capsule, and hard gelatin capsule, suppository, creams, lotions, solutions, gels, pastes, powder, and suspension. 
     
     
         59 . The pharmaceutical composition of  claim 58 , wherein the food composition is a health food product, a food product made from cereal flour, gums, a dairy product, a soup, a broth, a paste, a sauce, a beverage, a powder, a vitamin complex, a food rich in cholesterol, salt, or pepper. 
     
     
         60 . The pharmaceutical composition of  claim 58 , wherein the dosage form is further selected from the group consisting of immediate release, sustained release, and delayed release. 
     
     
         61 . The pharmaceutical composition of  claim 58 , wherein the dosage comprises about 0.1% to about 95% gallic acid derivative weight to weight of the composition. 
     
     
         62 . A kit comprising a pharmaceutical composition according to  claim 48 , and instructions for use. 
     
     
         63 . A kit comprising one or more gallic acid derivatives and instructions for use. 
     
     
         64 . The kit of  claim 63 , wherein the one or more gallic acid derivatives is selected from the group comprising: methyl gallate, ethyl gallate, glycerol-1-gallate, glucose-1-gallate (GG1), glucose-6-gallate (GG6), glucose-1,6-digallate (DGG16), mucic acid-2-gallate, 1-methyl mucate-2-gallate, mucic acid 1,4-lactone 5-gallate, geraniin, corilagin, chebilc acid, and m-digallic acid with minor p-digallic acid, and instructions for use. 
     
     
         65 . The kit of  claim 64 , comprising a combination of gallic acid derivatives selected from the group consisting of: Compound 4+Compound 5+Compound 2a, Compound 4+Compound 8+Compound 2a, Compound 4+Compound 5+Compound 7, Compound 4+Compound 2a, Compound 4+Compound 2b, Compound 7+Compound 2b, Compound 5+Compound 8, and Compound 5+Compound 7. 
     
     
         66 . The kit of  claim 63 , wherein said kit is for use in preventing or treating an elevated blood lipid level related disease or disorder in a subject, for use in preventing or treating inflammation in a subject, for use in preventing or treating a stress response in a subject, for use in reducing cholesterol biosynthesis in a subject, for use in increasing the cellular efflux of cholesterol in a subject, or for use in inhibiting the cellular uptake of cholesterol in a subject. 
     
     
         67 . The kit of  claim 63 , wherein the one or more gallic acid derivatives is administered as a nutraceutical.