Method for treating oral cancer
AssigneeImam Abdulrahman Bin Faisal University
InventorsFazil AHMAD, Krishna Mohan SURAPANENI, Abeer Mohammed AL-SUBAIE, Balu KAMARAJ
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Abstract
A pharmaceutical composition comprising a tannin selected from 2-O-digalloyl-1,3,4,6-tetra-O-galloyl-β-D-glucose, 3-O-digalloyl-1,2,4,6-tetra-O-galloyl-β-D-glucose, 6-O-digalloyl-1,2,3,4-tetra-O-galloyl-β-D-glucose, 2,6-bis-O-digalloyl-1,3-di-O-galloyl-β-D-glucose, and 6-O-trigalloyl-1,2,3-tri-O-galloyl-β-D-glucose. The tannin may be derived from Quercus infectoria. The pharmaceutical composition is used in a method of treating cancer, particularly oral cancer.
Claims21
1-19. (canceled)
A method of treating oral cancer, comprising:
- administering to a patient in need thereof a therapeutically effective amount of a pharmaceutical composition in solid form,
- wherein the pharmaceutical composition comprises:
- (i) an active ingredient which is 6-O-digalloyl-1,2,3,4-tetra-O-galloyl-β-D-glucose, or a pharmaceutically acceptable salt, solvate, or prodrug thereof, and (ii) a pharmaceutically acceptable carrier and/or excipient, which is at least one selected from the group consisting of a buffer, an inorganic salt, a fatty acid, a vegetable oil, a fatty ester, a surfactant, and a polymer, thereby treating the oral cancer, and (iii) at least one tannin selected from the group consisting of 2-O-digalloyl-1,3,4,6-tetra-O-galloyl-β-D-glucose, 3-O-digalloyl-1,2,4,6-tetra-O-galloyl-β-D-glucose, 2,6-bis-O-digalloyl-1,3-di-O-galloyl-β-D-glucose, and 6-O-trigalloyl-1,2,3-tri-O-galloyl-β-D-glucose,
- wherein the active ingredient accounts for greater than 99% of a total weight of tannins present in the pharmaceutical composition,
- wherein the therapeutically effective amount of the pharmaceutical composition is from 0.1 to 1,000 mg/kg of the active ingredient per body weight of the subject, and
- wherein the treating of the oral cancer reduces a tumor size, by diameter, by at least 5%, relative to the tumor size before the treating.
The method of claim 1, wherein MMP-2 is antagonized by the active ingredient with a binding affinity in a range of from −10.5 to −9.5 to kcal/mol.
The method of claim 1, wherein NF-kB p65 is antagonized by the active ingredient with a binding affinity in a range of from −10.5 to −8.7 kcal/mol.
The method of claim 1, wherein RhoA is antagonized by the active ingredient with a binding affinity in a range of from −11.0 to −8.8 kcal/mol.
The method of claim 1, wherein the administering comprises oral administration, parenteral administration, rectal administration, topical administration, transdermal administration, intralesional administration, and/or inhalation administration.
The method of claim 1, wherein the active ingredient is present in an amount of 1 to 75 wt %, based on a total weight of the pharmaceutical composition.
The method of claim 1, wherein the active ingredient is active against the oral cancer by binding to at least one selected from the group consisting of MMP-2, NF-kB and RhoA.
The method of claim 1, wherein the active ingredient is present in an amount of 2.5 to 70 wt %, based on a total weight of the pharmaceutical composition.
The method of claim 1, wherein the active ingredient is present in an amount of 5 to 65 wt %, based on a total weight of the pharmaceutical composition.
The method of claim 1, wherein the active ingredient is present in an amount of 7.5 to 60 wt %, based on a total weight of the pharmaceutical composition.
The method of claim 1, wherein the active ingredient is present in an amount of 10 to 50 wt %, based on a total weight of the pharmaceutical composition.
The method of claim 1, wherein the pharmaceutical composition is substantially free of saponins, flavonoids, terpenes, cardenolides, phlobatamins, steroids, and glycosides.
The method of claim 1, wherein the pharmaceutical composition is an immediate release composition.
The method of claim 1, wherein the pharmaceutical composition is substantially free of other tannins.
The method of claim 1, wherein the tannin is obtained by ethanolic extraction of Quercus infectoria followed by isolation of the active ingredient.
The method of claim 1, wherein the therapeutically effective amount of the pharmaceutical composition is from 50 to 500 mg/kg of the active ingredient per body weight of the subject.
The method of claim 1, wherein the administering is oral.
The method of claim 1, wherein the administering is parenteral, after dissolving the solid form of the pharmaceutical composition.
The method of claim 1, wherein the administering comprises dissolving 70 to 99.99 wt. % of the active ingredient in a range of from 1 to 20 minutes after entering a stomach of the patient.
The method of claim 1, wherein the administering comprises dissolving 70 to 99.99 wt. % of the active ingredient in an intestine of the patient.
Dependencies are inferred from the claim text.