Application of 7-hydroxy-1-indanone

By using 7-hydroxy-1-indanone as a novel targeted therapy drug, the problem of high recurrence rate of gastric cancer has been solved, achieving more efficient treatment results for gastric cancer, improving patient survival rate and quality of life, and promoting the development of the pharmaceutical industry.

CN120938976APending Publication Date: 2025-11-14HEILONGJIANG ACAD OF TCM
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Patent Information

Application Number
CN202511074055.1
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2025-08-01
Publication Date
2025-11-14

AI Technical Summary

Technical Problem

Gastric cancer has a high recurrence rate, current treatment options are not very effective, the 5-year survival rate is low, and patients have poor prognosis. There is a need to develop more effective targeted therapies.

Method used

Using 7-hydroxy-1-indanone as a novel targeted therapy drug, apoptosis of gastric cancer cells was induced, and the growth and migration of gastric cancer cells were inhibited, so as to develop personalized treatment plans for gastric cancer.

Benefits of technology

It has improved the treatment effect of gastric cancer, reduced the recurrence rate and mortality rate, provided more precise treatment options, reduced the economic and psychological burden on patients, and promoted the development of the pharmaceutical industry.

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Abstract

The invention discloses application of 7-hydroxy-1-indanone, and relates to an application method of the 7-hydroxy-1-indanone. In order to solve the problems of high recurrence rate of gastric cancer and poor treatment after healing, in-vitro cell experiments verify that 7-hydroxy-1-indanone can effectively inhibit proliferation and invasion of gastric cancer cells and induce apoptosis of the gastric cancer cells, and has the effect of resisting gastric cancer tumors. The invention belongs to the technical field of effective components of medicines.
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Description

Technical Field

[0001] This invention relates to the application of 7-hydroxy-1-indanone. Background Technology

[0002] Gastric cancer ranks fifth in incidence and third in mortality among malignant tumors worldwide. In my country, approximately 20% of gastric cancer cases are diagnosed at an early stage, with most patients diagnosed at a locally advanced or advanced stage, resulting in poor prognosis. Gastric cancer has complex subtypes and strong spatiotemporal heterogeneity. Currently, Western medicine commonly uses a combination of fluorouracil and platinum-based molecularly targeted therapy, which uses specific inhibitors to bind to molecules on the surface of tumor cells, inhibiting tumor proliferation, invasion, and metastasis. However, the overall efficacy of this treatment is unsatisfactory, with a 5-year survival rate of only 35.1%. Gastric cancer has an insidious onset and rapid progression; most patients are already in advanced stages when admitted to the hospital, and the recurrence rate after surgery is high. Summary of the Invention

[0003] The purpose of this invention is to solve the technical problem of high recurrence rate and poor treatment prognosis of gastric cancer, and to provide an application of 7-hydroxy-1-indanone.

[0004] 7-Hydroxy-1-indanone can be used to induce apoptosis in gastric cancer cells and inhibit their growth and migration.

[0005] The structural formula of 7-hydroxy-1-indanone is as follows: Figure 11 As shown.

[0006] The application of the 7-hydroxy-1-indanone is to inhibit the proliferation, invasion, and migration of gastric cancer cells (MFC) and to promote apoptosis of gastric cancer cells.

[0007] 7-Hydroxy-1-indanone can effectively inhibit the proliferation and invasion of gastric cancer cells and induce apoptosis, thus exhibiting anti-gastric cancer effects. Developing novel targeted therapies for gastric cancer using 7-hydroxy-1-indanone can improve treatment efficacy and reduce recurrence and mortality rates. This will provide more personalized and precise treatment options for gastric cancer patients, alleviate the economic and psychological burden on patients and their families, and improve their quality of life. Simultaneously, it will promote the development of the pharmaceutical industry and foster technological innovation and economic growth in related fields. Attached Figure Description

[0008] Figure 1 This is a graph showing the half-maximal inhibitory rate of CCK-8 cytotoxicity in Experiment 1.

[0009] Figure 2 This is a graph showing the cell migration and healing rate in the scratch test in Experiment 2;

[0010] Figure 3 This is a comparison chart showing the effect of different drug doses on cell viability in the CCK8 toxicity test in Experiment 3;

[0011] Figure 4 This is a control diagram showing the activity of 7-hydroxy-1-indanone against mouse gastric cancer cells in Experiment 4;

[0012] Figure 5 These are stained images of gastric cancer cells in the blank group, cisplatin group, high-dose group, medium-dose group, and low-dose group of Experiment 5.

[0013] Figure 6 These are cell scratch healing photos taken at 0h, 12h, and 24h in the blank group, cisplatin group, high-dose group, medium-dose group, and low-dose group in Experiment 6.

[0014] Figure 7 These are comparative photographs of the changes in morphology and expression area of ​​MFC cells observed under an optical X-ray microscope using the Rb a Caspase-1 P10 antibody in Experiment 7.

[0015] Figure 8 These are comparative photographs of changes in the morphology and expression area of ​​MFC cells observed under an optical X-ray microscope using cyclin D10 Rabbit pAb antibody in Experiment 7.

[0016] Figure 9 This is a comparison chart of the percentage of positive Rb a Caspase-1 P10 antibodies in each group in Experiment 7;

[0017] Figure 10 This is a comparison chart of the percentage of positive cyclin D10 Rabbit pAb antibodies in each group during Experiment 7;

[0018] Figure 11 It is the molecular structural formula of 7-hydroxy-1-indanone. Detailed Implementation

[0019] The technical solution of the present invention is not limited to the specific embodiments listed below, but also includes any combination of the specific embodiments.

[0020] Specific Implementation Method 1: Application of 7-hydroxy-1-indanone, wherein the 7-hydroxy-1-indanone is used to induce apoptosis of gastric cancer cells and inhibit the growth and migration of gastric cancer cells.

[0021] The following experiments were used to verify the effectiveness of the invention:

[0022] Experiment 1:

[0023] CCK-8—Cytotoxicity and Cell Proliferation Assay:

[0024] The effects of 7-hydroxy-1-indanone on the cytotoxicity and proliferation of MFC cells were investigated. Four × 10⁴ MFC cells (200 μL per well) in the logarithmic growth phase were seeded into 96-well plates, with three replicates per group. Cells were cultured for 4 days. Two hours after the addition of cck-8, absorbance (A) was measured at 450 nm. The average values ​​were used to plot growth curves, and the cell proliferation rate of each group was calculated.

[0025] Depend on Figure 1 The results showed that at a drug concentration of 0.14 mg / ml, half of the cells died, indicating that this concentration achieved the half-maximal inhibitory rate of the drug on MFC cells.

[0026] Experiment 2:

[0027] MFC cell migration assay:

[0028] Draw even lines on the back of a 6-well plate with a marker pen, spaced 0.5 cm apart, across the wells. MFC gastric cancer cells were digested with trypsin, resuspended, and counted. The cells were diluted to 1.0 × 10⁶ / mL and seeded into 6-well plates. After culturing for 24 h in a cell culture incubator, the culture medium was discarded. Using a 200 μl sterile pipette tip, a vertical scratch was made in the center of the bottom monolayer of cells in each well, perpendicular to the marker line. The scraped suspended and dead cells were gently washed away with PBS. Cells were then administered according to the following groups: blank group; cisplatin group; and high, medium, and low doses of 7-hydroxy-1-indanone (high 0.14 mg / ml, medium 0.07 mg / ml, low 0.035 mg / ml). Cell migration towards the scratched area was observed under a microscope at the same location at 0, 6, 12, and 24 h. Each experiment was repeated three times.

[0029] After spreading the cells to cover the surface, a 200 μL pipette tip was used to streak the cells vertically to the bottom of the dish. The blank area was measured at 0, 12, 24, and 36 hours, and the migration rate was calculated.

[0030] Depend on Figure 2 It was found that in the 7-hydroxy-1-indanone group, both high and medium doses could effectively inhibit the migration of gastric cancer cells, and the degree of inhibition of healing was similar to that of the positive control drug cisplatin, indicating that 7-hydroxy-1-indanone has a good inhibitory effect on gastric cancer cells.

[0031] The above experiments show that 7-hydroxy-1-indanone has significant anti-tumor activity, and its mechanism of action mainly includes inducing apoptosis of gastric cancer cells, inhibiting the growth and migration of gastric cancer cells, and thus has an anti-gastric cancer effect.

[0032] Experiment 3:

[0033] CCK8 toxicity test:

[0034] Experimental content: To determine the half-maximal inhibitory rate (ICP-C) of 7-hydroxy-1-indanone against mouse gastric cancer cells, and to determine the dosage range for subsequent experiments.

[0035] Experimental results: The high dose of single-agent administration is approximately 0.16 mg / ml.

[0036] Experiment 4:

[0037] CCK8 activity assay:

[0038] Experimental content: Detection of the activity of 7-hydroxy-1-indanone against mouse gastric cancer cells.

[0039] Experimental results: The P values ​​of all experimental groups were less than 0.05, and all showed statistical differences from the blank-treated cells.

[0040] Table 1 (CCK8 activity assay: cell mortality rate in each group after drug administration)

[0041]

[0042] Experiment 5:

[0043] Cell morphology observation - He staining

[0044] Experimental content: The morphological changes of gastric cancer in mice were observed by staining cells with different doses of eosin and hematoxylin.

[0045] Experimental results: Under the same cell dosage, cell morphology shrank and cell number began to decrease with different drug dosages.

[0046] Experiment Six:

[0047] Cell scratch

[0048] Experimental procedure: Cells were seeded in a six-well cell culture plate. After growth, the culture medium was discarded. A 200 μl pipette tip was used to make a scratch in the well plate. The scratch healing rate was calculated using ImageJ software.

[0049] Experimental results:

[0050] Table 2. Healing rate of MFC gastric cancer cells after 24 hours

[0051]

[0052] Experiment 7: Immunohistochemistry

[0053] 1. Experimental procedure: After incubating with antibodies against Rb a Caspase-1 P10 and cyclin D1 Rabbit pAb, observe the changes in the morphology and expression area of ​​MFC cells under an optical X-ray microscope.

[0054] 2. Experimental Results:

[0055] Table 3. Caspase1 protein expression in each group

[0056]

[0057] Table 4. Cyclin D1 protein expression in each group

[0058]

Claims

The application of 1,7-hydroxy-1-indanone, characterized in that... The 7-hydroxy-1-indanone is used to induce apoptosis in gastric cancer cells and inhibit their growth and migration.