WO-2026091179-A1 - USE OF NOVEL NANO-FORMULATION CONTAINING GINGERENONE A IN PREPARATION OF ANTI-TUMOR DRUG

Abstract

Disclosed in the present invention is a use of a novel nano-formulation containing gingerenone A in the preparation of an anti-tumor drug. The nano-formulation comprises aminated dendritic mesoporous silica and gingerenone A loaded on the aminated dendritic mesoporous silica.

Inventors

• QUAN, Chunshan
• LIU, JUNFENG
• ZHANG, LIYING
• ZENG, ZHENG
• PAN, Xiaofei
• MEI, XIAODAN
• CHEN, YUSONG

Assignees

• 陈玉松

Dates

Publication Date

20260507

Application Date

20241112

Priority Date

20241028

Claims (10)

1. The application of a novel nano-formulation containing gingerone A in the preparation of antitumor drugs is characterized in that the nano-formulation comprises aminated dendritic mesoporous silica and gingerone A loaded on the aminated dendritic mesoporous silica.
2. According to the application of claim 1, the tumor is characterized in that it comprises one or more of the following: melanoma, lymphohematopoietic system tumor, endocrine tumor, lung and mediastinal tumor, breast tumor, digestive system tumor, urinary and male reproductive system tumor, female reproductive system tumor, head and neck tumor, central nervous system tumor, skin tumor, and bone and soft tissue tumor.
3. According to claim 1, the dosage form of the drug includes tablets, capsules, pills, injections, sustained-release preparations, or controlled-release preparations. The routes of administration of the antitumor drugs include one or more of the following: intravenous injection, intraperitoneal injection, intramuscular injection, subcutaneous injection, oral administration, rectal administration, skin and mucous membrane administration, and inhalation administration.
4. According to claim 1, the nano-formulation is used in the antitumor drug at a dose of 100 mg/kg to 400 mg/kg.
5. According to the application described in claim 1, the antitumor drug is a drug that inhibits tumor growth or inhibits tumor cell proliferation.
6. According to the application described in claim 1, the antitumor drug is characterized in that it promotes or induces apoptosis of tumor cells.
7. According to claim 1, the antitumor drug is a drug that inhibits the growth of transplanted tumors.
8. The application according to any one of claims 1-7 is characterized in that the antitumor drug further comprises a pharmaceutically acceptable carrier, excipient and/or excipient.
9. According to the application of claim 1, the method for preparing the nano-formulation comprises: Shogaol A is dissolved in a solvent to obtain a shogaol A solution. The shogaol A solution and aminated dendritic mesoporous silica are added to a buffer solution to react and load the shogaol A onto the aminated dendritic mesoporous silica to obtain the nano-formulation.
10. An antitumor drug, characterized in that the active ingredient is a novel nano-formulation containing gingerone A; the nano-formulation is the nano-formulation used in any one of claims 1-9.

Description

Application of a novel nano-formulation containing gingerone A in the preparation of antitumor drugs Technical Field This invention relates to the field of pharmaceutical technology, and more specifically, to the application of a novel nano-formulation containing gingerone A in the preparation of antitumor drugs. Background Technology Currently, the incidence and mortality rates of malignant tumors in my country continue to rise, with annual medical expenses exceeding 220 billion yuan. Existing treatments for tumors mainly involve surgical resection, chemotherapy, and radiotherapy, but all have limitations such as strong side effects and a high recurrence rate. Therefore, screening for novel, safe, and effective anti-tumor drugs is of great clinical significance. Gingerenone A (GA) is a natural phytochemical extracted from ginger with broad medicinal value, including anti-tumor, antioxidant, anti-aging, anti-inflammatory, antiviral, and blood sugar control effects. Studies have shown that GA can promote anti-proliferation and senescence of breast cancer cells induced by oxidative stress (Gingerenone A Induces Antiproliferation and Senescence of Breast Cancer Cells. Antioxidants.; Tzu-Jung Yu.; et al.). Simultaneously, GA selectively kills cancer cells by dual inhibition of JAK2 and S6K1 (Identification of a Dual Inhibitor of Janus Kinase 2 (JAK2) and p70 Ribosomal S6 Kinase 1 (S6K1) Pathways.; Sanguine Byun.; et al.), making it an effective anti-tumor active ingredient. However, due to the poor solubility, permeability, stability and absorption of gingerone A, it is difficult to achieve an effective therapeutic concentration and thus the expected effect, which greatly limits its application scope. Summary of the Invention The purpose of this invention is to overcome the aforementioned deficiencies in the existing technology and provide a novel nano-formulation containing gingerone A for the preparation of antitumor drugs. This nano-formulation utilizes aminated dendritic mesoporous silica to load gingerone A, resulting in a novel nano-formulation with high drug loading capacity, high encapsulation efficiency, and high biocompatibility. This formulation exhibits low cytotoxicity, can be rapidly taken up by tumor cells, significantly enhances the ability of gingerone A to clear tumor cells, and effectively inhibits tumor proliferation in vivo. Its therapeutic effect is superior to that of the commonly used clinical antitumor drug dabrafenib, and it has broad application prospects. To achieve the above objectives, the technical solution of the present invention is as follows: The application of a novel nanoformulation containing gingerone A in the preparation of antitumor drugs, wherein the nanoformulation comprises aminated dendritic mesoporous silica and gingerone A loaded on the aminated dendritic mesoporous silica. Optionally, the tumor includes one or more of the following: melanoma, lymphohematopoietic system tumors, endocrine tumors, lung and mediastinal tumors, breast tumors, digestive system tumors, urinary and male reproductive system tumors, female reproductive system tumors, head and neck tumors, central nervous system tumors, skin tumors, and bone and soft tissue tumors. Optionally, the dosage form of the drug includes tablets, capsules, pills, injections, sustained-release formulations, or controlled-release formulations. Optionally, the route of administration of the antitumor drug includes one or more of the following: intravenous injection, intraperitoneal injection, intramuscular injection, subcutaneous injection, oral administration, rectal administration, skin and mucous membrane administration, and inhalation administration. Optionally, the dosage of the nano-formulation in the antitumor drug is 100 mg/kg to 400 mg/kg. Optionally, the antitumor drug is a drug that inhibits tumor growth or tumor cell proliferation. Optionally, the antitumor drug is a drug that promotes or induces apoptosis in tumor cells. Optionally, the antitumor drug is a drug that inhibits the growth of transplanted tumors. Optionally, the antitumor drug may also contain pharmaceutically acceptable carriers, excipients, and/or excipients. Optionally, the loading of gingerone A in the nano-formulation is 15% to 30%. Optionally, the encapsulation rate of gingerone A in the nano-formulation is 11% to 35%. Optionally, the particle size of the nano-formulation is 50 nm to 200 nm. Optionally, the specific surface area of the nano-formulation is 800 m² /g to 1000 m² /g. Optionally, the particle size of the aminated dendritic mesoporous silica is 50 nm to 200 nm. Optionally, the pore size of the aminated dendritic mesoporous silica is 2 nm to 10 nm. Optionally, the specific surface area of the aminated dendritic mesoporous silica is 300 m² /g to 1000 m² /g. Optionally, the preparation method of the nano-formulation includes: Shogaol A is dissolved in a solvent to obtain a shogaol A solution. The shogaol A solution and aminated d