Medicine for treating cancer and application

Through the combination of Xiaoduicin C and sorafenib, the problems of poor treatment effect, high recurrence rate and large side effects in existing cancer treatment methods have been solved, and effective treatment of multiple cancers has been achieved and reduced. Side effects of toxicity.

CN119424410APending Publication Date: 2025-02-14THE HONG KONG POLYTECHNIC UNIV
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Patent Information

Application Number
CN202310973290.7
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2023-08-03
Publication Date
2025-02-14

AI Technical Summary

Technical Problem

The existing cancer treatment methods have problems such as poor treatment effect, high recurrence rate and large side effects, and an effective therapeutic drug with lower toxic and side effects is needed.

Method used

Using a combination of small dimethin C and sorafenib, by testing the activity of different types of cancer cells, it was found that they had significant cancer cell toxic activity and showed synergistic effects in drug combination experiments.

Benefits of technology

When treating various types of cancer, the combination of Xiaoduicin C and sorafenib significantly improves the anti-cancer activity, reduces toxic side effects, and proves its inhibitory effect on tumors and on mice in animal experiments. Safety of the organs.

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Abstract

The invention provides a medicine containing helenin C and sorafenib for treating cancers. The medicine comprises helenin C and sorafenib. Compared with the prior art, the medicine for treating cancer provided by the invention has the advantages that the composition of the helenin C and the sorafenib has remarkable anti-cancer activity and synergistic effect, the cancer can be more effectively treated, and meanwhile, the toxic and side effects are reduced.
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Description

Technical Field

[0001] The present invention belongs to the field of biomedical technology, and in particular relates to a medicine for treating cancer and its application. Background Art

[0002] Cancer is a leading cause of death worldwide. According to statistics from the World Health Organization, nearly 10 million deaths (or nearly one-sixth) worldwide are caused by cancer each year, and about one-third of cancer deaths come from China. It can be seen that China has become a cancer superpower. Cancer originates from cells in various organs and tissues, and it is usually divided into two types: carcinoma in situ and metastatic cancer. When a malignant tumor first occurs, it will stay in the basal layer of the primary site. Since it does not infiltrate adjacent tissues, it is defined as carcinoma in situ, while metastatic cancer refers to a malignant tumor that has been transferred from another cancer (primary cancer).

[0003] Cancer treatment depends on many factors, including the type, size, location, stage of the cancer and the patient's overall health. Common cancer treatment options include: surgical resection, organ transplantation, chemotherapy, radiation therapy and interventional therapy.

[0004] However, these treatments have many challenges, such as poor treatment effects and low average survival rates; high recurrence rates. Even if patients undergo surgery, radiotherapy or chemotherapy, there is still a high possibility of recurrence. This is because cancer cells are highly heterogeneous, and different cancer cells have different drug resistance and growth rates, which leads to unstable treatment effects and increased recurrence rates; large side effects. Cancer treatment is often accompanied by many adverse reactions and side effects, such as nausea, vomiting, diarrhea, loss of appetite, etc., which have a negative impact on the patient's quality of life and physical health. Therefore, more research and innovation are needed to further improve the treatment effect and prognosis of cancer. Summary of the invention

[0005] In view of this, the technical problem to be solved by the present invention is to provide a drug for treating cancer with lower toxic side effects.

[0006] The invention provides a medicine for treating cancer, comprising heliconia tin C.

[0007] Microhelenin C is an extract of goosegrass, with the molecular formula of C 20 H 26 O5, the molecular structure is shown in formula (I), and the molecular weight is 346.42.

[0008]

[0009] The present invention tests the activity of different cancer cells and finds that the survival rate of the corresponding cancer cells is close to 50% after adding 10 μM of the compound helicin C and 24 hours. The experimental results show that the compound helicin C has significant cancer cell toxicity.

[0010] In the present invention, the cancer cells include but are not limited to one or more of liver cancer cells, colon cancer cells, breast cancer cells, gastric cancer cells and melanoma cells.

[0011] Specifically in the present invention, the cancer cells are one or more of liver cancer cells HepG2, colon cancer cells HCT116, breast cancer cells MCF-7, gastric cancer cells MGC803 and melanoma cells A375.

[0012] Further preferably, the drug for treating cancer also includes sorafenib. Sorafenib is a multi-target kinase inhibitor that can simultaneously inhibit multiple intracellular kinases that exist in tumor cells and participate in tumor cell signal transduction, angiogenesis and apoptosis, and can also inhibit cell surface kinases.

[0013] The present invention has found that the mass ratio of chrysanthemumin C and sorafenib is preferably 1: (0.5-2), more preferably 1: (0.8-1.5), more preferably 1: (0.8-1.2), and most preferably 1: 1 through drug combination experiments.

[0014] The present invention also tested the drug combination experiment and found that the combination of the compound heliconiaceae C and sorafenib at a ratio of 1:1, after 24 hours of treatment with the combination of heliconiaceae C 10 μM plus sorafenib 10 μM, had a synergistic effect (synergistic index CI<1).

[0015] Therefore, the present invention provides a drug for treating cancer comprising helicin C and sorafenib. Compared with the prior art, the combination of helicin C and sorafenib in the cancer treatment drug provided by the present invention has significant anti-cancer activity and synergistic effect, can treat cancer more effectively, and reduce toxic side effects.

[0016] The present invention also provides the use of scutellarin C in preparing drugs for treating cancer.

[0017] In the present invention, the cancer includes but is not limited to one or more of liver cancer, colon cancer, breast cancer, gastric cancer and melanoma.

[0018] The present invention also provides the use of scutellarin C and sorafenib in preparing a drug for treating cancer.

[0019] Specifically, in the present invention, the mass ratio of the helicin C to sorafenib is preferably 1:(0.5-2), more preferably 1:(0.8-1.5), further preferably 1:(0.8-1.2), and most preferably 1:1.

[0020] In the present invention, the cancer includes but is not limited to one or more of liver cancer, colon cancer, breast cancer, gastric cancer and melanoma.

[0021] The present invention takes mice inoculated with liver cancer tumors as an example to prove that helicin C and sorafenib have strong inhibitory effects on tumor cells and will not have toxic side effects on various organs of mice.

[0022] The total dosage of the helicin C and sorafenib in mice is preferably 10-30 mg / kg, more preferably 15-25 mg / kg, and even more preferably 20 mg / kg. BRIEF DESCRIPTION OF THE DRAWINGS

[0023] Figure 1 This is a volume comparison diagram of tumor tissue in Example 5 of the present invention;

[0024] Figure 2 This is the HE staining picture of the animal section experiment in Example 5 of the present invention;

[0025] Figure 3 This is a graph comparing the activities of the combination drug of compound scutellarin C and sorafenib in Example 5 of the present invention and the single drug use. DETAILED DESCRIPTION

[0026] The following will be combined with the embodiments of the present invention to clearly and completely describe the technical solutions in the embodiments of the present invention. Obviously, the described embodiments are only part of the embodiments of the present invention, not all of the embodiments. Based on the embodiments of the present invention, all other embodiments obtained by ordinary technicians in this field without making creative work are within the scope of protection of the present invention.

[0027] The DMEM culture medium used in the examples is Gibco DMEM culture medium.

[0028] Example 1: Inhibitory effects of scutellarin C, sorafenib and their combination on HepG2 liver cancer cells

[0029] Human hepatoma cells HepG2 were inoculated into 96-well plates, with 100 μL of cell suspension per well. The culture medium was DMEM culture medium supplemented with 10% FBS and 2 mM glutamate. After 24 hours of inoculation, scutellarin C, sorafenib, and a combination of scutellarin C and sorafenib were added, respectively, and the control group culture medium did not add drugs. After 24 hours of addition, the cell survival rate was evaluated by the MTT method. Tumor cell survival rate = experimental group OD value / control group OD × 100%; Calcusyn software was used to calculate the synergistic index (CI) of the combination of scutellarin C and sorafenib. The results are shown in Table 1.

[0030] Table 1 Survival rate test results of liver cancer cell HepG2

[0031]

[0032] Example 2: Inhibitory effects of scutellarin C, sorafenib and their combination on colon cancer cells HCT116

[0033] Human colon cancer cells HCT116 were inoculated into 96-well plates, with 100 μL of cell suspension per well. The culture medium was DMEM culture medium supplemented with 10% FBS and 2 mM glutamate. After 24 hours of inoculation, scutellarin C, sorafenib, and a combination of scutellarin C and sorafenib were added, respectively, and the control group culture medium did not add drugs. After 24 hours of addition, the cell survival rate was evaluated by the MTT method. Tumor cell survival rate = experimental group OD value / control group OD × 100%; Calcusyn software was used to calculate the synergistic index (CI) of the combination of scutellarin C and sorafenib. The results are shown in Table 2.

[0034] Table 2 Survival test results of human colon cancer cell HCT116

[0035]

[0036] Example 3: Inhibitory effects of scutellarin C, sorafenib and their combination on breast cancer cells MCF-7

[0037] Human breast cancer cells MCF-7 were inoculated into 96-well plates, with 100 μL of cell suspension per well. The culture medium was DMEM culture medium supplemented with 10% FBS and 2 mM glutamate. After 24 hours of inoculation, scutellarin C, sorafenib, and a combination of scutellarin C and sorafenib were added, respectively, and no drug was added to the control group culture medium. After 24 hours of addition, the cell survival rate was evaluated by the MTT method. Tumor cell survival rate = OD value of the experimental group / OD value of the control group × 100%; Calcusyn software was used to calculate the synergistic index (CI) of the combination of scutellarin C and sorafenib. The results are shown in Table 3.

[0038] Table 3 Survival rate test results of human breast cancer cell MCF-7

[0039]

[0040] Example 4: Inhibitory effects of scutellarin C, sorafenib and their combination on gastric cancer cell MGC803

[0041] Human gastric cancer cells MGC803 were inoculated into 96-well plates, with 100 μL of cell suspension per well. The culture medium was DMEM culture medium supplemented with 10% FBS and 2 mM glutamate. After 24 hours of inoculation, scutellarin C, sorafenib, and a combination of scutellarin C and sorafenib were added, respectively, and no drug was added to the control group culture medium. After 24 hours of addition, the cell survival rate was evaluated by the MTT method. Tumor cell survival rate = OD value of the experimental group / OD value of the control group × 100%; Calcusyn software was used to calculate the synergistic index (CI) of the combination of scutellarin C and sorafenib. The results are shown in Table 4.

[0042] Table 4 Survival rate test results of human gastric cancer cell MGC803

[0043]

[0044] Example 5: Inhibitory effects of scutellarin C, sorafenib and their combination on melanoma cells A375

[0045] Human melanoma cells A375 were inoculated into 96-well plates, with 100 μL of cell suspension per well. The culture medium was DMEM supplemented with 10% FBS and 2 mM glutamate. After 24 hours of inoculation, scutellarin C, sorafenib, and a combination of scutellarin C and sorafenib were added, respectively, and no drug was added to the control group culture medium. After 24 hours of addition, the cell survival rate was evaluated by the MTT method. Tumor cell survival rate = OD value of the experimental group / OD value of the control group × 100%; Calcusyn software was used to calculate the synergistic index (CI) of the combination of scutellarin C and sorafenib. The results are shown in 5.

[0046] Table 5 Survival rate test results of human melanoma cell A375

[0047]

[0048] Example 5: Effects of scutellarin C, sorafenib and their combination on tumors and toxicity to various organs in nude mice inoculated with liver cancer tumors

[0049] Animal experiments were conducted on chrysanthemumin C, sorafenib, and a combination of chrysanthemumin C and sorafenib. Hepatoma cells Huh7 were inoculated subcutaneously in male nude mice, with 5x10 6 After 7 days, the tumor volume grew to 100mm 3 The control group was given normal saline, the low-dose group of chrysanthemum C was given a dose of 10 mg / kg, the high-dose group of chrysanthemum C was given a dose of 30 mg / kg, the dose of sorafenib was 10 mg / kg, and the combined dose of chrysanthemum C and sorafenib was 10 mg / kg of chrysanthemum C plus 10 mg / kg of sorafenib. Each group was intraperitoneally injected once a day. After 16 days of administration, the experimental mice were killed and the tumors were removed for comparison. The results showed ( Figure 1 , Figure 3 ), the tumor volume of the control group was the largest, while the tumor volumes of the low-dose helicobacter pylori group and the sorafenib group were significantly smaller than those of the control group. The high-dose helicobacter pylori had a better inhibitory effect on tumors, and the combined use of helicobacter pylori and sorafenib had the best effect.

[0050] On the other hand, the results of HE staining from animal slice experiments showed that ( Figure 2 ), pyrenoidin C, sorafenib, and the combination of pyrenoidin C and sorafenib had no toxic side effects on various organs of mice.

[0051] The preferred embodiments of the present invention disclosed above are only used to help explain the present invention, but the present invention is not limited thereto. Those skilled in the art can understand that within the technical concept of the present invention, the technical solution of the present invention can be modified, or some technical features can be combined in any other way. These modifications or combinations do not make the essence of the corresponding technical solution deviate from the spirit and scope of each implementation of the technical solution of the present invention, and should be regarded as the contents disclosed by the present invention, which belong to the protection scope of the present invention.

Claims

1. A drug for treating cancer, characterized in that: Including helicin C.

2. The drug according to claim 1, characterized in that Also includes sorafenib.

3. The drug according to claim 2, characterized in that The mass ratio of the helicin C to sorafenib is 1:(0.5-2).

4. The drug according to claim 2, characterized in that The mass ratio of the helicin C to sorafenib is 1:

1.

5. Application of heliconia tin C in the preparation of drugs for treating cancer.

6. Application of helicin C and sorafenib in the preparation of drugs for treating cancer.

7. The use according to claim 5 or 6, characterized in that: The cancer is selected from one or more of liver cancer, colon cancer, breast cancer, gastric cancer and melanoma.