Application of ginkgetin in preparation of GRP78 protein inhibitor

By using ginkgo as a GRP78 protein inhibitor, endoplasmic reticulum stress and autophagy are induced, the problem of lack of effective targeted drugs in osteosarcoma treatment is solved, and effective inhibition and treatment effect on osteosarcoma cells are achieved.

CN120000640APending Publication Date: 2025-05-16SHANGHAI FIRST PEOPLES HOSPITAL
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Patent Information

Application Number
CN202510171958.5
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2025-02-17
Publication Date
2025-05-16

AI Technical Summary

Technical Problem

The prior art lacks effective targeted drugs in the treatment of osteosarcoma, resulting in limited therapeutic effects and greater side effects.

Method used

Ginkgo or its pharmaceutically acceptable salts are used as GRP78 protein inhibitors to affect its ATPase activity and thermal stability, thereby inducing endoplasmic reticulum stress and autophagy, and inhibiting the proliferation and invasion of osteosarcoma cells.

Benefits of technology

Ginkgo significantly inhibits the proliferation, invasion and apoptosis of osteosarcoma cells, slows tumor growth and metastasis, and provides a new targeted therapeutic solution.

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Abstract

The invention relates to the field of biological medicine, in particular to application of ginkgetin in preparation of a GRP78 protein inhibitor. The ginkgetin has a structure as shown in a formula (I): # imgabs0 #. A thermal displacement experiment proves that the ginkgetin interacts with an LYS-296 site of GRP78, so that the ginkgetin can be used as a GRP78 protein inhibitor to influence ATP enzyme activity and thermal stability of the GRP78 protein inhibitor; after the ginkgetin treats the tumor cells, the expression of the marker protein of the endoplasmic reticulum stress of the tumor cells is up-regulated, which indicates that the ginkgetin can induce the endoplasmic reticulum stress generation; the function antagonism of an autophagy inhibitor chloroquine and ginkgetin shows that ginkgetin can induce tumor cell autophagy.
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