Method for enhancing tyrosinase inhibitory activity

Patent metadata

Field	Value
Publication number	US-12383571-B2
Application number	US-202117546180-A
Country	US
Kind code	B2
Filing date	Dec 9, 2021
Priority date	Jun 19, 2019
Publication date	Aug 12, 2025
Grant date	Aug 12, 2025

Abstract

The disclosure provides a method for enhancing tyrosinase inhibitory activity, and belongs to the technical field of intensive and deep processing of fruits and vegetables. The disclosure improves an inhibitory effect of a tyrosinase inhibitor on tyrosinase in manner of heating treatment; the tyrosinase inhibitor consists of a phenolic acid with a concentration of 0.6-1.8 mg/mL and a saponin with a concentration of 0.5-1.5 mg/mL; and the heating treatment conditions are as follows: the heating temperature is 130-170° C., and the heating time is 30-120 min. The disclosure compounds polyphenols and the saponin into the tyrosinase inhibitor, tyrosinase relative activity after treatment can be as low as 5%, and a three-component polyphenol can produce a synergistic effect; high temperature will make the saponin deglycosylated to produce substances with a powerful tyrosinase inhibitory effect, such as a polyphenol polymer, thus greatly improving the inhibitory effect of the tyrosinase inhibitor on the tyrosinase.

First claim

What is claimed is:

1. A method for enhancing tyrosinase inhibitory activity, which comprises:
heating a tyrosinase inhibitor,
wherein the tyrosinase inhibitor consists of a phenolic acid and a saponin;
wherein the phenolic acid consists of one of the following:
(a) 5 mM quercetin, 5 mM cinnamic acid, and 5 mM ferulic acid;
(b) 5 mM quercetin, 0.5 mM cinnamic acid, and 5 mM ferulic acid;
(c) 5 mM quercetin, 0.5 mM gallic acid, and 5 mM ferulic acid;
(d) 5 mM quercetin, 0.5 mM gallic acid, and 0.5 mM isorhamnetin;
(e) 5 mM quercetin, 5 mM cinnamic acid, and 0.5 mM isorhamnetin; or
(f) 5 mM quercetin, 5 mM ferulic acid, and 0.5 mM isorhamnetin;
wherein the saponin is protodioscin or sarsasapogenin with a concentration of 0.5 mg/mL to 1.5 mg/ml; and
wherein heating is performed at 130° C. to 170° C. for 30 minutes, and wherein the tyrosinase inhibitor synergistically increases tyrosinase inhibitory activity compared to a tyrosinase inhibitor when heated at a temperature outside of the 130° C. to 170° C. temperature range.

2. A tyrosinase inhibitor, wherein the tyrosinase inhibitor consists of a phenolic acid and a saponin;
wherein the phenolic acid consists of one of the following:
(a) 5 mM quercetin, 5 mM cinnamic acid, and 5 mM ferulic acid;
(b) 5 mM quercetin, 0.5 mM cinnamic acid, and 5 mM ferulic acid;
(c) 5 mM quercetin, 0.5 mM gallic acid, and 5 mM ferulic acid;
(d) 5 mM quercetin, 0.5 mM gallic acid, and 0.5 mM isorhamnetin;
(e) 5 mM quercetin, 5 mM cinnamic acid, and 0.5 mM isorhamnetin; or
(f) 5 mM quercetin, 5 mM ferulic acid, and 0.5 mM isorhamnetin; and
wherein the saponin is protodioscin or sarsasapogenin with a concentration of 0.5 mg/mL to 1.5 mg/mL.

3. The method according to claim 1 , wherein the phenolic acid is selected from (a), (b), (d), (e), or (f), and wherein the saponin is protodioscin with a concentration of 0.5 mg/mL to 1.5 mg/mL.

4. The method according to claim 1 , wherein the phenolic acid is (c) 5 mM quercetin, 0.5 mM gallic acid, and 5 mM ferulic acid, and wherein the saponin is sarsasapogenin with a concentration of 0.5 mg/mL to 1.5 mg/mL.

5. The method according to claim 1 , wherein the phenolic acid is selected from (b), (d), (e), or (f), and wherein the saponin is protodioscin with a concentration of 0.5 mg/mL to 1.5 mg/mL.

6. The method according to claim 1 , wherein the phenolic acid is (b) or (d), and wherein the saponin is protodioscin with a concentration of 0.5 mg/mL to 1.5 mg/mL.

7. The method according to claim 1 , wherein the phenolic acid is selected from (a), (e), or (f), and wherein the saponin is protodioscin with a concentration of 0.5 mg/mL to 1.5 mg/mL.

8. The method according to claim 3 , wherein the saponin is protodioscin with a concentration of 1.0 mg/mL.

9. The method according to claim 4 , wherein the saponin is sarsasapogenin with a concentration of 1.5 mg/mL.

10. The method according to claim 5 , wherein the saponin is protodioscin with a concentration of 1.0 mg/mL.

11. The method according to claim 6 , wherein the saponin is protodioscin with a concentration of 1.0 mg/mL.

12. The method according to claim 7 , wherein the saponin is protodioscin with a concentration of 1.0 mg/mL.

13. The tyrosinase inhibitor according to claim 2 , wherein the phenolic acid is selected from (a), (b), (d), (e), or (f), and wherein the saponin is protodioscin with a concentration of 0.5 mg/mL to 1.5 mg/mL.

14. The tyrosinase inhibitor according to claim 2 , wherein the phenolic acid is (c) 5 mM quercetin, 0.5 mM gallic acid, and 5 mM ferulic acid, and wherein the saponin is sarsasapogenin with a concentration of 0.5 mg/mL to 1.5 mg/mL.

15. The tyrosinase inhibitor according to claim 2 , wherein the phenolic acid is selected from (b), (d), (e), or (f), and wherein the saponin is protodioscin with a concentration of 0.5 mg/mL to 1.5 mg/mL.

16. The tyrosinase inhibitor according to claim 2 , wherein the phenolic acid is (b) or (d), and wherein the saponin is protodioscin with a concentration of 0.5 mg/mL to 1.5 mg/mL.

17. The tyrosinase inhibitor according to claim 2 , wherein the phenolic acid is selected from (a), (e), or (f), and wherein the saponin is protodioscin with a concentration of 0.5 mg/mL to 1.5 mg/mL.

18. The tyrosinase inhibitor according to claim 13 , wherein the saponin is protodioscin with a concentration of 1.0 mg/mL.

19. The tyrosinase inhibitor according to claim 14 , wherein the saponin is sarsasapogenin with a concentration of 1.5 mg/mL.

20. The method according to claim 15 , wherein the saponin is protodioscin with a concentration of 1.0 mg/mL.

Assignees

• Univ Jiangnan

Inventors

• Fan Liuping
• Yu Qun
• Li Jinwei

Classifications

• A61K31/352

  condensed with carbocyclic rings, e.g. methantheline  {(cannabinoids A61K31/658)} · CPC title

• A61K31/192 Primary

  having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid  {(cannabinoids A61K31/658)} · CPC title

• A61K31/704 Primary

  attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin {(digitoxin A61K31/7048)} · CPC title

• A23B2/733

  Compounds of undetermined constitution obtained from animals or plants · CPC title

• A61K2800/5922

  At least two compounds being classified in the same subclass of A61K8/18 · CPC title