Modified pectins, compositions and methods related thereto
View Patent ↗The present invention provides compositions of modified pectin and methods for preparing and using them.
1. A biologically active pectin made by a process consisting essentially of:
(a) passing an aqueous solution comprising 1-20 mg/mL pectin and 7.5%-25% w/w ethanol through a tangential flow filter with a pore size of less than 1.0 μm to provide a permeate and a retentate, wherein said permeate consists essentially of biologically active pectin having an average molecular weight from 10 kDa to 250 kDa and an IC 50 less than 200 μg/mL in a cancer cell apoptosis model; and
(b) collecting said biologically active pectin.
2. A biologically active partially de-esterified pectin made by a process consisting essentially of:
(a) treating a first aqueous solution comprising 1-20 mg/mL pectin with acid, base, or both, to partially de-esterify the pectin,
(b) neutralizing the first solution to form a second aqueous solution comprising partially de-esterified pectin,
(c) passing a third solution comprising the second aqueous solution and 7.5%-25% w/w ethanol through a tangential flow filter with a pore size of less than 1.0 μm to provide a permeate and a retentate, wherein said permeate consists essentially of iologically active partially de-esterified pectin having an average molecular weight from 10 kDa to 250 kDa and an IC 50 less than 200 μg/mL in a cancer cell apoptosis model, and wherein the degree of esterification in the biologically active partially de-esterified pectin is between 10% and 60%, and
(d) collecting said biologically active partially de-esterified pectin.
3. A biologically active pectin made by a process consisting essentially of the steps:
(a) passing an aqueous solution comprising 1-20 mg/mL pectin and 7.5%-25% w/w ethanol through a tangential flow filter with a pore size of 0.1 μm to 1.0 μm to provide a permeate and a retentate, wherein said permeate consists essentially of biologically active pectin having an average molecular weight from 10 kDa to 250 kDa and an IC 50 less than 200 μg/mL in a cancer cell apoptosis model; and
(b) collecting said biologically active pectin.
4. A biologically active partially de-esterified pectin made by a process consisting essentially of the steps:
(a) treating a first aqueous solution comprising 1-20 mg/mL pectin with acid, base, or both, to partially de-esterify the pectin,
(b) neutralizing the first aqueous solution to form a second aqueous solution comprising partially de-esterified pectin,
(c) passing a third aqueous solution comprising the second aqueous solution and 7.5%-25% w/w ethanol through a tangential flow filter with a pore size of 0.1 μm to 1.0 μm to provide a permeate and a retentate, wherein said permeate consists essentially of biologically active partially de-esterified filtered pectin having an average molecular weight from 10 k Da to 250 kDa and an IC 50 less than 200 μg/mL in a cancer cell apoptosis model, and wherein the degree of esterification in the biologically active partially de-esterified pectin is between 10% and 60%, and
(d) collecting said biologically active partially de-esterified pectin.
5. The biologically active pectin of claim 1 , wherein the pore size is about 0.2 μm.
6. The biologically active pectin of claim 1 , wherein the aqueous solution has a pectin concentration of 1 to 10 mg/mL.
7. The biologically active pectin of claim 1 , wherein the aqueous solution has a pH in the range of 2.5 to 7.5.
8. The biologically active pectin of claim 1 , wherein the average molecular weight of the biologically active pectin is selected from the group consisting of 50 kDa-200 kDa, 80 kDa-150 kDa, 70 kDa-150 kDa and 80 kDa-100 kDa.
9. The biologically active pectin of claim 1 , wherein the biologically active pectin inhibits cancer cell proliferation in a cancer cell apoptosis model with an IC 50 less than 100 μg/mL.
10. The biologically active pectin of claim 1 , wherein 10%-20% w/w ethanol or 15%-25% w/w ethanol is present in the aqueous solution.
11. The biologically active pectin of claim 1 , wherein the pectin in the aqueous solution is citrus pectin.
12. The biologically active pectin of claim 1 , wherein the pectin in the aqueous solution has one or more mannose subunits.
13. The biologically active pectin of claim 12 , wherein the pectin in the aqueous solution has galactose side chains.
14. The biologically active pectin of claim 13 , wherein the pectin in the aqueous solution has a galactose content of greater than or equal to 5%.
15. The biologically active pectin of claim 13 , wherein the galactose side chains are linked to one or more of the mannose subunits.
16. The biologically active partially de-esterified pectin of claim 2 , wherein the pore size is about 0.2 μm.
17. The biologically active partially de-esterified pectin of claim 2 , wherein the first aqueous solution has a pectin concentration of 1 to 10 mg/mL.
18. The biologically active partially de-esterified pectin of claim 2 , wherein the first aqueous solution has a pH in the range of 2.5 to 7.5.
19. The biologically active partially de-esterified pectin of claim 2 , wherein the average molecular weight of the biologically active partially de-esterified pectin is selected from the group consisting of 50 kDa-200 kDa, 80 kDa-150 kDa, 70 kDa-150 kDa and 80 kDa-100 kDa.
20. The biologically active partially de-esterified pectin of claim 2 , wherein the biologically active partially de-esterified pectin inhibits cancer cell proliferation in a cancer cell apoptosis model with an IC 50 less than 100 μg/mL.
21. The biologically active partially de-esterified pectin of claim 2 , wherein 10%-20% w/w ethanol or 15%-25% w/w ethanol is present in the third aqueous solution.
22. The biologically active partially de-esterified pectin of claim 2 , wherein the pectin in the first aqueous solution is citrus pectin.
23. The biologically active pectin of claim 2 , wherein the pectin in the aqueous solution has one or more mannose subunits.
24. The biologically active pectin of claim 23 , wherein the main in the aqueous solution has galactose side chains.
25. The biologically active pectin of claim 24 , wherein the pectin in the aqueous solution has a galactose content of greater than or equal to 5%.
26. The biologically active pectin of claim 24 , wherein the galactose side chains are linked to one or more of the mannose subunits.
27. The biologically active pectin of claim 3 , wherein the pectin in the aqueous solution has one or more mannose subunits.
28. The biologically active pectin of claim 27 , wherein the pectin in the aqueous solution has galactose side chains.
29. The biologically active pectin of claim 28 , wherein the pectin in the aqueous solution has a galactose content of greater than or equal to 5%.
30. The biologically active pectin of claim 28 , wherein the galactose side chains are linked to one or more of the mannose subunits.