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CN-121971503-A - NRF2 targeted composition capable of efficiently releasing sulforaphane and application thereof

CN121971503ACN 121971503 ACN121971503 ACN 121971503ACN-121971503-A

Abstract

The present invention relates to a nutritional targeted composition comprising a component 1 providing glucoraphanin, a component 2 providing myrosinase, vitamin C and magnesium stearate for the efficient release of glucoraphanin and activation of the NRF2 target, and to the use of said composition for the preparation of a product for the prevention or treatment of a disease or disorder that can be prevented or treated with glucoraphanin.

Inventors

  • LI XIAOLONG
  • JIANG LINA

Assignees

  • 深圳福山生物科技有限公司

Dates

Publication Date
20260505
Application Date
20251229

Claims (15)

  1. 1. A composition comprising the following components: 1) Providing component 1 of glucoraphanin; 2) Providing component 2 of myrosinase; 3) Vitamin C, and 4) Magnesium stearate.
  2. 2. The composition of claim 1, wherein said component 1 is selected from the group consisting of crucifers, extracts thereof, and mixtures thereof.
  3. 3. The composition of any one of claims 1 to 2, wherein the cruciferous plant is broccoli.
  4. 4. The composition of any one of claims 1 or 3, wherein the cruciferous plant is selected from the group consisting of a plant whole, a portion of a plant, and combinations thereof.
  5. 5. The composition of any one of claims 1 to 4, wherein the cruciferous plant is selected from the group consisting of a floral ball, a seed, a sprout, and a combination thereof of a plant.
  6. 6. The composition according to any one of claims 1 to 5, wherein the mass ratio of the component 1, the component 2, vitamin C and magnesium stearate is (10-90): 1-90): 0.1-10: 1-10.
  7. 7. The composition of any one of claims 1 to 6, which is in solid form.
  8. 8. The composition of any one of claims 1 to 7 in the form of a powder, granule, capsule or tablet formulation.
  9. 9. The composition of any one of claims 1 to 8, wherein the component 1 is selected from the group consisting of broccoli seed extract, broccoli sprout powder, broccoli bulb lyophilized powder, and combinations thereof, and chemically or biologically synthesized forms of glucoraphanin.
  10. 10. The composition of any one of claims 1 to 9, wherein the component 2 is selected from horseradish, radish, cabbage, juice or serum thereof, and extracts thereof.
  11. 11. Use of a composition according to any one of claims 1 to 10 for the preparation of a product for the prevention or treatment of a disease or condition that can be prevented or treated with sulforaphane.
  12. 12. The use according to claim 11, wherein the disease or condition which can be prevented or treated with sulforaphane is selected from the group consisting of cancer, diabetes, cardiovascular disease, helicobacter pylori infection, autism, schizophrenia, depression, alzheimer's disease and pulmonary fibrosis.
  13. 13. A method for in vitro conversion of glucoraphanin to glucoraphanin, comprising the steps of: 1) The composition according to any one of claim 1 to 12, 2) The composition is mixed with water or an aqueous solution.
  14. 14. A method of supplementing a subject in need thereof with a sulforaphane comprising administering to the subject a composition of any of claims 1 to 13.
  15. 15. A method of promoting the release of glucoraphanin in an aqueous solution comprising the step of mixing a sample comprising component 1 providing glucoraphanin, component 2 providing myrosinase, and vitamin C with magnesium stearate.

Description

NRF2 targeted composition capable of efficiently releasing sulforaphane and application thereof Technical Field The invention belongs to the field of biological medicine, and relates to a composition for efficiently releasing sulforaphane and activating an NRF2 target spot and application thereof in preparation of a product for preventing or treating diseases or symptoms which can be prevented or treated by using the sulforaphane. Background Chronic non-infectious diseases, or chronic diseases, have become a global significant public health challenge, and their control strategies are transitioning from traditional therapies to early prevention and accurate intervention. The nutrition targeting (or accurate nutrition) intervention takes 'nutrition genomics' as a core and combines with 'clinical evidence-based' technology to construct a gene-active ingredient dynamic matching system, and the personalized nutrition intervention landing is promoted by screening dietary active ingredients capable of specifically regulating and controlling the expression or the function of key genes, so that an innovative approach is provided for chronic disease prevention and treatment. Nuclear factor E2 related factor 2 (NRF 2) is a transcription factor for regulating antioxidant stress response by cells, is also a key transcription factor of an endogenous antioxidant system of a human body, can regulate and control more than 500 genes (such as phase II enzyme NQO1, glutathione sulfhydryl transferase and the like) after being activated, enhances endogenous defenses such as detoxification, mitochondrial function, abnormal protein clarity and the like (Pall, M.L., & Levine, S. Acta Physiologica Sinica, 2015, 67 (1), 1-18), and becomes a core target of chronic disease intervention. Based on the activation effect of NRF2 channel, the composition can play a role in treating and preventing gastric ulcer, helicobacter pylori infection, cancer, diabetes, cardiovascular diseases, autism, schizophrenia, depression, alzheimer disease and other diseases. Sulforaphane (Sulforaphane, SFN), also known as sulforaphane, is the strongest activator of NRF2 found in edible plants to date. Compared with plant polyphenols such as curcumin, resveratrol and the like with lower bioavailability, the sulforaphane can effectively activate NRF2 channels in human tissues under the condition of diet allowable dose (Houghton CA, curr Top Med Res.2020; 2:123.). Studies have shown that sulforaphane can induce the expression of cytoprotective genes by efficiently activating NRF2 signaling pathway, exerting durable and more effective antioxidant and chemopreventive effects (Young-Joon S. Science.2003,3,768). The prior art also shows that the sulforaphane and its precursor compound sulforaphane have definite chemoprotective effect on gastric ulcer, helicobacter pylori infection and the like (CN 1935003A; CN1170472C; CN 101208079B). Therefore, the development of compositions capable of efficient delivery and stable release of sulforaphane is of great value for achieving nutritional intervention against NRF2 targets. The cruciferous plant is the main source of glucoraphanin and its precursor compound glucoraphanin, wherein broccoli of Brassica of Brassicaceae is the core source, and the content of glucoraphanin in seeds and sprouts is relatively high. However, broccoli contains biologically inactive glucoraphanin, which is converted to active glucoraphanin by myrosinase in crucifers. However, sulforaphane, which is an isothiocyanate, is unstable in chemical properties, is easily degraded by the influence of oxygen and temperature, and is unfavorable for storage in applications. In view of this limitation, the prior art proposes a solution that the myrosinase and the glucoraphanin raw materials are respectively prepared into solid forms and stored in the form of a premix, so that decomposition of glucoraphanin by enzymes during storage can be avoided, and enzymolysis is completed in a solution environment after administration with water or oral administration, so that effective absorption of glucoraphanin is realized (see CN110946996 a). However, it has been found that for existing products for the prevention of chronic diseases, especially for the mixture of myrosinase in solid form and glucoraphanin raw material (including raw material in the form of broccoli and/or its extract), the release of glucoraphanin in aqueous solution is limited, which affects the degree of utilization of the product. Accordingly, there is a need to overcome the low release rate of glucoraphanin in existing products, and in particular, the limited release of glucoraphanin in aqueous solutions from compositions comprising glucoraphanin and myrosinase, and there is a strong need to provide a composition comprising glucoraphanin and myrosinase that can release glucoraphanin in aqueous solutions with high efficiency, thereby effectively activating the NRF2 target. Disclosure of Invention The