Method of preparing ATG's analogue, and the application of ATG and it's analogue
View Patent ↗The present invention provides the use of ATG in the preparation of a reagent for adjusting the activity of PP2A; and the use of ATG in increasing the activity of PP2A in 293T cells. The present invention also provides the use of the arctigenin in the preparation of the medicine for reducing the proteinuria of the diabetic mice. The present invention also provides the use of the arctigenin in the preparation of the reagent for inhibiting the expression of the NOX4 gene. The present invention also provides analogs of arctigenin and application thereof. The present invention provides a novel use of ATG for modulating PP2A activity, and ATG can also significantly reduce proteinuria in diabetic mice. At the same time, arctigenin could significantly inhibit the expression of NOX4 in STZ-eNOS −/− mice glomeruli. The ATG analogs of the present invention are more effective than the native ATG.
1. An ATG analogue for regulating the bioactivity of PP2A, NOX4, and reducing diabetic proteinuria, wherein the ATG analogue is at least one compound selected from the group of compounds represented by formula (1-1) and formula (1-2):
wherein in formula (1-1) and formula (1-2):
X is O, Y is N, and Z is N;
R 1 , R 2 , R 3 , R 4 and R 5 are each independently selected from H, aliphatic or aromatic hydrocarbon groups, nitro groups, phosphoric acid groups, sulfide groups, sulfone groups, nitrile groups, heterocyclic group, boronate or boronic acid group, ester group, and amine group.
2. The ATG analogue according to claim 1 , wherein R 2 is H 3 CO— and R 3 is H 3 CO—.
3. The ATG analogue according to claim 1 , wherein R 4 is H 3 CO—.
4. The ATG analogue according to claim 1 , wherein R 2 is H 3 CO—, R 3 is H 3 CO—, and R 4 is H 3 CO—.