Use of tandospirone and analogues thereof for the preparation of a medicament against skin tumors and pharmaceutical compositions
By using tandospirone and its analogues with psychotropic drugs such as amitriazine to prepare anti-skin tumor drugs, especially anti-melanoma drugs, the problems of drug toxicity and drug resistance in existing treatment regimens have been solved, and significant inhibition of melanoma cell proliferation and control of tumor growth have been achieved.
Patent Information
- Authority / Receiving Office
- CN · China
- Patent Type
- Patents(China)
- Current Assignee / Owner
- XIANGYA HOSPITAL CENT SOUTH UNIV
- Filing Date
- 2022-10-14
- Publication Date
- 2026-08-04
AI Technical Summary
Current melanoma treatment options face challenges such as drug toxicity and postoperative recurrence due to drug resistance, and there is a lack of effective anti-skin tumor drugs.
Tandospirone and its analogues, along with psychotropic drugs such as amitriazine, are used to prepare anti-skin tumor drugs, especially anti-melanoma drugs, which achieve anti-tumor effects by inhibiting the proliferation of skin tumor cells.
Tandospirone and its analogues have a significant inhibitory effect on the proliferation of melanoma cells, effectively inhibiting tumor growth, and have shown good therapeutic effects in in vitro and in vivo experiments, with no obvious toxic side effects.
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Figure CN117180279B_ABST
Abstract
Description
[0001] This application is a divisional application of Chinese Patent Application No. 202211258886.0, filed on October 14, 2022, entitled "Use of psychotropic drugs in the preparation of anti-skin tumor drugs and pharmaceutical compositions". Technical Field
[0002] This invention relates to the field of biomedical technology, and in particular to the use of tandospirone and its analogues in the preparation of anti-skin tumor drugs and pharmaceutical compositions. Background Technology
[0003] Cancer is a leading cause of death worldwide, and skin tumors, especially melanoma, are among the most malignant of all cancer types. According to the WHO's GLOBOCAN 2012 database, 250,178 new cases of cutaneous melanoma were diagnosed globally in 2015. Currently, the Clark classification is used for the clinical histological subtyping of melanoma, including four types: malignant lentigines-like melanoma; superficial diffuse melanoma; acral lentigines-like melanoma / mucosal melanoma; and nodular melanoma.
[0004] Clinical symptoms of malignant melanoma of the skin include bleeding, itching, tenderness, and ulceration. Generally speaking, the symptoms of melanoma are related to the age of onset. Young patients usually present with itching, changes in the color of the lesions, and enlargement of the borders, while elderly patients usually present with ulceration of the lesions, which usually indicates a poor prognosis.
[0005] While treatment options for melanoma are rapidly evolving, the toxic side effects of drugs and postoperative recurrence due to drug resistance pose significant challenges. With the emergence of the concept of "drug repurposing," a growing number of doctors and scientists believe that if basic and clinical validation can be achieved, existing, widely used non-anti-tumor drugs can be explored for development into new anti-cancer agents. This would save on new drug development costs and time, while also ensuring certain levels of assurance regarding the drug's physicochemical properties, pharmacokinetics, and safety. Summary of the Invention
[0006] Based on this, one aspect of the present invention provides the use of tandospirone and its analogues in the preparation of anti-skin tumor drugs, particularly anti-melanoma drugs.
[0007] The technical solution provided by this invention is as follows:
[0008] The use of tandospirone and its analogues in the preparation of an anti-skin tumor drug, wherein the tandospirone and its analogues comprise one or more of tandospirone, a pharmaceutically acceptable salt of tandospirone, and a pharmaceutically acceptable ester of tandospirone.
[0009] The inventors discovered that the aforementioned psychotropic drugs tandospirone, pharmaceutically acceptable salts of tandospirone, and pharmaceutically acceptable esters of tandospirone have a significant inhibitory effect on the proliferation of skin tumor cells, effectively inhibiting the growth of skin tumor cells and thus playing an anti-skin tumor role.
[0010] In some embodiments, the tandospirone and its analogues are one or more of tandospirone, a pharmaceutically acceptable salt of tandospirone, and a pharmaceutically acceptable ester of tandospirone.
[0011] In some embodiments, the anti-skin tumor drug further includes one or more of mirtrin, a pharmaceutically acceptable salt of mirtrin, and a pharmaceutically acceptable ester of mirtrin. That is, it can also be a mixture of one or more of tandospirone, a pharmaceutically acceptable salt of tandospirone, and a pharmaceutically acceptable ester of tandospirone with one or more of mirtrin, a pharmaceutically acceptable salt of mirtrin, and a pharmaceutically acceptable ester of mirtrin.
[0012] In some embodiments, the anti-skin tumor drug is an anti-melanoma drug. Experimental studies have found that tandospirone and its analogues have significant inhibitory effects on melanoma cell lines, demonstrating significant efficacy against melanoma.
[0013] In some embodiments, the anti-melanoma drug is a drug that inhibits the proliferation of melanoma SK-MEL-5 cells.
[0014] In some embodiments, the anti-melanoma drug is a drug that inhibits the proliferation of melanoma B16F10 cells.
[0015] In some embodiments, tandospirone and its analogues serve as the active pharmaceutical ingredient of the anti-skin tumor drug.
[0016] In some embodiments, pharmaceutically acceptable salts of the tandospirone include tandospirone methanesulfonate.
[0017] In some embodiments, pharmaceutically acceptable esters of tandospirone include straight-chain or branched alkyl esters of tandospirone, cycloalkyl esters of tandospirone, aromatic alkyl esters of tandospirone, and phosphate esters of tandospirone.
[0018] In some embodiments, the dosage form of the anti-skin tumor drug includes any one of injection, oral, and topical formulations.
[0019] In another aspect, the present invention provides a pharmaceutical composition comprising one or more of tandospirone, a pharmaceutically acceptable salt of tandospirone, and a pharmaceutically acceptable ester of tandospirone, and one or more of ametria, a pharmaceutically acceptable salt of ametria, and a pharmaceutically acceptable ester of ametria.
[0020] This invention proposes a novel use of tandospirone and its analogues in the preparation of anti-skin tumor drugs, particularly anti-melanoma drugs. The tandospirone and its analogues include one or more of tandospirone, pharmaceutically acceptable salts of tandospirone, and pharmaceutically acceptable esters of tandospirone. Experimental verification shows that the above-mentioned tandospirone and its analogues have significant inhibitory effects on the proliferation of melanoma cell lines, demonstrating significant efficacy against melanoma. Attached Figure Description
[0021] Figure 1 The results show the inhibitory effects of amitriazine mesylate in Example 1 and tandospirone in Example 2 on human malignant melanoma SK-MEL-5 at a concentration of 10 μmol / L.
[0022] Figure 2 These are comparative photos of tumor volumes in 5 mice from the control group and 5 mice from the amiodarone mesylate group after the experiment in Example 3 of this invention.
[0023] Figure 3 This is a comparison curve of tumor volume changes between the control group and the amiodarone mesylate group in Example 3 of the present invention;
[0024] Figure 4 This is a comparison chart of the changes in body weight of mice in the control group and the amiodarone mesylate group in Example 3 of the present invention;
[0025] Figure 5 These are comparative photos of tumor volumes in five mice from the control group and five mice from the tandospirone group after the experiment in Example 4 of this invention.
[0026] Figure 6 This is a comparison curve of tumor volume changes between the control group and the tandospirone group in Example 4 of the present invention;
[0027] Figure 7 This is a comparison chart of the weight changes of mice in the control group and the tandospirone group in Example 4 of the present invention. Detailed Implementation
[0028] To make the above-mentioned objects, features, and advantages of the present invention more apparent and understandable, specific embodiments of the present invention will be described in detail. Many specific details are set forth in the following description to provide a thorough understanding of the present invention. However, the present invention can be practiced in many other ways different from those described herein, and those skilled in the art can make similar modifications without departing from the spirit of the present invention. Therefore, the present invention is not limited to the specific embodiments disclosed below.
[0029] Unless otherwise defined, all technical and scientific terms used herein have the same meaning as commonly understood by one of ordinary skill in the art to which this invention pertains. The terminology used herein in the description of the invention is for the purpose of describing particular embodiments only and is not intended to limit the invention. Unless otherwise specifically stated, all raw materials, reagents, instruments, and equipment used in this invention are commercially available or can be prepared by existing methods.
[0030] Psychotropic drugs are a class of medications primarily used to treat schizophrenia, manic episodes, and other severe mental disorders. Amitriazine, pharmaceutically acceptable salts of amitriazine, pharmaceutically acceptable esters of amitriazine, tandospirone, pharmaceutically acceptable salts of tandospirone, and pharmaceutically acceptable esters of tandospirone are all classified as psychotropic drugs.
[0031] Almitrine mesylate is a pharmaceutically acceptable salt of amitriazine. Its CAS number is 29608-49-9, and its molecular formula is C2. 28 H 37 F2N7O6S2, with a molecular weight of 669.76, has the following structural formula:
[0032]
[0033] Tandospirone has the CAS number 87760-53-0 and the molecular formula C. 21 H 29 N5O2, with a molecular weight of 383.49, has the following structural formula:
[0034]
[0035] There are currently no reports on the application of the aforementioned psychotropic drugs in the preparation of drugs for treating skin tumors, especially melanoma.
[0036] One embodiment of the present invention provides the use of a psychotropic drug in the preparation of an anti-skin tumor drug, wherein the psychotropic drug is one or more of amitriazine, a pharmaceutically acceptable salt of amitriazine, a pharmaceutically acceptable ester of amitriazine, tandospirone, a pharmaceutically acceptable salt of tandospirone, and a pharmaceutically acceptable ester of tandospirone.
[0037] Clinically non-antitumor drugs such as amitriazine, pharmaceutically acceptable salts of amitriazine, pharmaceutically acceptable esters of amitriazine, tandospirone, pharmaceutically acceptable salts of tandospirone, and pharmaceutically acceptable esters of tandospirone have been used to treat melanoma cells, exhibiting cell proliferation inhibitory effects. Therefore, the aforementioned psychotropic drugs can be used as active pharmaceutical ingredients in anti-melanoma drugs.
[0038] Specifically, pharmaceutically acceptable salts of amitriazine can be, for example, amitriazine mesylate.
[0039] Studies have found that amitriazine mesylate at a concentration of 10 μmol / L in DMEM medium significantly inhibited the proliferation of melanoma SK-MEL-5 cells. Similarly, tandospirone at a concentration of 10 μmol / L in DMEM medium also significantly inhibited the proliferation of melanoma SK-MEL-5 cells.
[0040] Other embodiments of the present invention also provide a pharmaceutical composition for treating skin tumors, the pharmaceutical composition comprising one or more of amitriazine, a pharmaceutically acceptable salt of amitriazine, a pharmaceutically acceptable ester of amitriazine, tandospirone, a pharmaceutically acceptable salt of tandospirone, and a pharmaceutically acceptable ester of tandospirone, and further comprising pharmaceutically acceptable excipients.
[0041] In this pharmaceutical composition, amitriazine, a pharmaceutically acceptable salt of amitriazine, a pharmaceutically acceptable ester of amitriazine, tandospirone, a pharmaceutically acceptable salt of tandospirone, and a pharmaceutically acceptable ester of tandospirone are the active components of the pharmaceutical composition, which can effectively inhibit the proliferation of melanoma cells and play a major role in the treatment of melanoma.
[0042] It is understood that psychotropic drugs can be amitriazine alone, a pharmaceutically acceptable salt of amitriazine, or a pharmaceutically acceptable ester of amitriazine; or a mixture of two or more of amitriazine, a pharmaceutically acceptable salt of amitriazine, or a pharmaceutically acceptable ester of amitriazine; or tandospirone alone, a pharmaceutically acceptable salt of tandospirone, or a pharmaceutically acceptable ester of tandospirone; or a mixture of two or more of tandospirone, a pharmaceutically acceptable salt of tandospirone, or a pharmaceutically acceptable ester of tandospirone; or a mixture in combination with one or more of amitriazine, a pharmaceutically acceptable salt of amitriazine, or a pharmaceutically acceptable ester of amitriazine and tandospirone, a pharmaceutically acceptable salt of tandospirone, or a pharmaceutically acceptable ester of tandospirone.
[0043] Among them, pharmaceutically acceptable salts of amitriazine can be pharmaceutically common types of salts, such as mesylate salts; pharmaceutically acceptable esters of amitriazine can also be pharmaceutically common types of esters, such as straight-chain or branched alkyl esters, cycloalkyl esters, aromatic alkyl esters, phosphate esters, etc.; pharmaceutically acceptable salts of tandospirone can be pharmaceutically common types of salts, such as mesylate salts; pharmaceutically acceptable esters of tandospirone can also be pharmaceutically common types of esters, such as straight-chain or branched alkyl esters, cycloalkyl esters, aromatic alkyl esters, phosphate esters, etc.
[0044] In one specific example of the invention, the pharmaceutically acceptable salt of amitriazine is amitriazine mesylate.
[0045] In some embodiments, pharmaceutically acceptable excipients include, but are not limited to, excipients, binders, disintegrants, lubricants, coating agents, solvents, solubilizers, suspending agents, thickeners, and surfactants. Appropriate excipients may be selected depending on the dosage form of the pharmaceutical composition.
[0046] It is understood that excipients, adhesives, disintegrants, lubricants, coating agents, solvents, cosolvents, suspending agents, thickeners, surfactants, etc., can all be corresponding agents conventionally used in the art, and the specific types of each agent are not limited in this invention.
[0047] Specifically, the dosage form of the pharmaceutical composition may include, but is not limited to, any one of injections, oral medications, and topical medications. Multiple dosage forms can be used as needed to meet the requirements of different administration methods. For example, the pharmaceutical composition can be formulated as an injection for convenient injection administration; it can be formulated as tablets, granules, pills, capsules, etc., for convenient oral administration; and it can also be formulated as ointments, patches, powders, etc.
[0048] In some other embodiments, the pharmaceutical composition may also be a compound formulation. That is, the above-mentioned amitriazine, pharmaceutically acceptable salts of amitriazine, pharmaceutically acceptable esters of amitriazine, tandospirone, pharmaceutically acceptable salts of tandospirone, and pharmaceutically acceptable esters of tandospirone may be used in combination with other pharmaceutically active ingredients.
[0049] It should be noted that the contents of amitriazine, pharmaceutically acceptable salts of amitriazine, pharmaceutically acceptable esters of amitriazine, tandospirone, pharmaceutically acceptable salts of tandospirone, and pharmaceutically acceptable esters of tandospirone in the pharmaceutical composition can be determined within a suitable range based on actual production and usage conditions, and are not specifically limited in this invention.
[0050] The present invention will be further described below with reference to specific embodiments, but these should not be construed as limiting the scope of protection of the present invention.
[0051] Example 1: In vitro experiment on the inhibition of human melanoma SK-MEL-5 cell proliferation by amitriazine mesylate.
[0052] 1. Experimental Materials
[0053] 1.1 Cell lines
[0054] The SK-MEL-5 melanoma cell line was obtained from the Department of Dermatology Laboratory of Xiangya Hospital, Central South University. It was cultured in DMEM (dulbecco's modified eagle medium) containing 10% FBS (fetal bovine serum) at a constant temperature of 37°C and with a CO2 concentration of 5%.
[0055] 1.2 Reagents
[0056] One 500mL bottle of DMEM medium (purchased from Biological Industries); fetal bovine serum (purchased from Biological Industries); trypsin digestion solution (purchased from Beyotime); PBS powder (purchased from Servicebio); penicillin antibiotics (purchased from Biological Industries); amiotric acid stock solution (10mmol / L, dissolved in DMSO) (purchased from MCE); CCK8 reagent (purchased from Bimake).
[0057] 2. Instruments and Consumables
[0058] 2.1 Instruments
[0059] Clean bench; cell culture incubator; centrifuge; cell counter; negative pressure aspirator; enzyme-linked immunosorbent assay (ELISA) reader.
[0060] 2.2 Consumables
[0061] Cell culture dish; 96-well plate; 15 mL centrifuge tube; cell counting plate.
[0062] 3. Experimental Methods and Results
[0063] 3.1 Cell proliferation experiment
[0064] The experimental procedure was as follows: melanoma SK-MEL-5 cells were cultured at a rate of 3 × 10⁻⁶ cells / year. 3 Each well was seeded with 10% FBS / DMEM (37°C, 5% CO2) and cultured in 96-well plates. The plates were divided into experimental and control groups, with 5 replicates per group. After 14–16 hours of culture, 10 mmol / L stock solution of amitriazine mesylate was added to the culture medium in the experimental group to achieve a final concentration of 10 μmol / L. The control group received only culture medium without amitriazine mesylate. At 48 hours, CCK8 was added to both the experimental and control groups, and the plates were incubated for 2 hours. The absorbance (OD) of each well was then measured at 450 nm using a microplate reader.
[0065] 3.2 Experimental Results
[0066] The inhibitory effect of amitriazine mesylate on the proliferation of melanoma cells was detected using CCK8 assay. The results of the inhibitory effect of amitriazine mesylate at a concentration of 10 μmol / L on human malignant melanoma SK-MEL-5 are as follows: Figure 1 As shown. Figure 1 In this context, "Control" represents the control group.
[0067] Depend on Figure 1 It is evident that amitriazine mesylate significantly inhibits the proliferation of human malignant melanoma SK-MEL-5 cells. After the addition of 10 μmol / L amitriazine mesylate, the survival rate of human malignant melanoma SK-MEL-5 cells in the experimental group was only 24.6%; while in the control group, which only received culture medium without amitriazine mesylate, the survival rate of human malignant melanoma SK-MEL-5 cells was 100%.
[0068] Example 2: In vitro experiment on the inhibition of human melanoma SK-MEL-5 cell proliferation by tandospirone
[0069] 1. Experimental Materials
[0070] 1.1 Cell lines
[0071] The SK-MEL-5 melanoma cell line was obtained from the Department of Dermatology Laboratory of Xiangya Hospital, Central South University. It was cultured in DMEM medium containing 10% FBS at a constant temperature of 37°C and under conditions of 5% CO2 concentration.
[0072] 1.2 Reagents
[0073] One 500mL bottle of DMEM medium (purchased from Biological Industries); fetal bovine serum (purchased from Biological Industries); trypsin digestion solution (purchased from Beyotime); PBS powder (purchased from Servicebio); penicillin antibiotics (purchased from Biological Industries); tandospirone stock solution (10mmol / L, dissolved in DMSO) (purchased from MCE); CCK8 reagent (purchased from Bimake).
[0074] 2. Instruments and Consumables
[0075] 2.1 Instruments
[0076] Clean bench; cell culture incubator; centrifuge; cell counter; negative pressure aspirator; enzyme-linked immunosorbent assay (ELISA) reader.
[0077] 2.2 Consumables
[0078] Cell culture dish; 96-well plate; 15 mL centrifuge tube; cell counting plate.
[0079] 3. Experimental Methods and Results
[0080] 3.1 Cell proliferation experiment
[0081] The experimental procedure was as follows: melanoma SK-MEL-5 cells were cultured at a rate of 3 × 10⁻⁶ cells / year. 3 Each well was seeded with 10% FBS / DMEM (37°C, 5% CO2) and cultured in 96-well plates. The plates were divided into experimental and control groups, with 5 replicates per group. After 14–16 hours of culture, tandospirone stock solution (10 mmol / L) was added to the culture medium in the experimental group to achieve a final concentration of 10 μmol / L. The control group received only culture medium without tandospirone. At 48 hours, CCK8 was added to both the experimental and control groups, and the plates were incubated for 2 hours. The absorbance (OD) of each well was then measured at 450 nm using a microplate reader.
[0082] 3.2 Experimental Results
[0083] The inhibitory effect of tandospirone on the proliferation of melanoma cells was detected using CCK8 assay. The results of the inhibitory effect of tandospirone at a concentration of 10 μmol / L on human malignant melanoma SK-MEL-5 are as follows: Figure 1 As shown. Figure 1 In this context, "Control" represents the control group.
[0084] Depend on Figure 1 It is evident that tandospirone significantly inhibits the proliferation of human malignant melanoma SK-MEL-5 cells. After the addition of 10 μmol / L tandospirone, the survival rate of human malignant melanoma SK-MEL-5 cells in the experimental group was only 38%; while in the control group, which only received culture medium without the addition of amitrin mesylate, the survival rate of human malignant melanoma SK-MEL-5 cells was 100%.
[0085] Example 3: Effect of amitriazine mesylate on tumor growth in B16F10 tumor-bearing C57BL / 6 mice
[0086] 1. Experimental Materials
[0087] 1.1 Cell lines
[0088] The B16F10 melanoma cell line was obtained from the Department of Dermatology Laboratory of Xiangya Hospital, Central South University. It was cultured in RPMI-1640 medium (RPMI stands for Roswell Park Memorial Institute) containing 10% FBS at a constant temperature of 37°C and with a CO2 concentration of 5% in the environment.
[0089] 1.2 Reagents
[0090] RPMI-1640 medium, 500 mL each (purchased from Biological Industries); fetal bovine serum (purchased from Biological Industries); trypsin digestion solution (purchased from Beyotime); PBS powder (purchased from Servicebio); penicillin antibiotics (purchased from Biological Industries); amitriazine mesylate (purchased from MCE).
[0091] 2. Instruments and Consumables
[0092] 2.1 Instruments
[0093] Clean bench; cell culture incubator; centrifuge; cell counter.
[0094] 2.2 Consumables
[0095] Cell culture dish; 15mL centrifuge tube; cell counting chamber.
[0096] 3. Experimental Methods and Results
[0097] Experimental Procedure: Ten C57BL / 6 mice were used. After shaving their backs, subcutaneous tumor formation was achieved using mouse melanoma cells (B16F10). Once the tumors were palpable, the mice were randomly divided into two groups of five mice each. The groups were: ① control group and ② amantadine mesylate group. The control group was treated daily with corn oil (corn oil was used as a solvent control in the amantadine mesylate group because it was dissolved in corn oil); the amantadine mesylate group was treated daily by gavage with amantadine mesylate (15 mg / kg). The weight and tumor volume of the mice were measured every other day until the study endpoint.
[0098] Experimental results:
[0099] Figure 2 This is a comparison photograph of the tumor volume of 5 mice in the control group and 5 mice in the amitrin mesylate group after the experiment. Figure 3 This is a comparison curve of tumor volume changes between the control group and the amitriazine mesylate group. Figure 3 The horizontal axis represents the number of days after treatment, and the vertical axis represents the tumor volume.
[0100] Depend on Figure 3 The results showed that as the number of treatment days increased, the tumor volume of mice in the amiodarone mesylate group increased significantly less than that in the control group, indicating that amiodarone mesylate can effectively inhibit tumor growth in mice.
[0101] The body weight of mice in each group was measured, and the weight changes of mice in the control group and the amiodarone mesylate group were compared as shown in the figure below. Figure 4 As shown. Figure 4 The horizontal axis represents the number of days after treatment, and the vertical axis represents the body weight of the mice. Repeated experimental data are expressed as mean (N=5) ± SD; *P < 0.05. Figure 4 It can be seen that the treatment with amiotric acid had little effect on the body weight of mice, indicating that amiotric acid had no obvious toxic side effects on mice.
[0102] Example 4: Effect of tandospirone on tumor growth in B16F10 tumor-bearing C57BL / 6 mice
[0103] 1. Experimental Materials
[0104] 1.1 Cell lines
[0105] The B16F10 melanoma cell line was obtained from the Department of Dermatology Laboratory of Xiangya Hospital, Central South University. It was cultured in RPMI-1640 medium containing 10% FBS at a constant temperature of 37°C and with a CO2 concentration of 5% in the environment.
[0106] 1.2 Reagents
[0107] RPMI-1640 medium, 500 mL per bottle (purchased from Biological Industries); fetal bovine serum (purchased from Biological Industries); trypsin digestion solution (purchased from Beyotime); PBS powder (purchased from Servicebio); penicillin antibiotics (purchased from Biological Industries); tandospirone (purchased from MCE).
[0108] 2. Instruments and Consumables
[0109] 2.1 Instruments
[0110] Clean bench; cell culture incubator; centrifuge; cell counter.
[0111] 2.2 Consumables
[0112] Cell culture dish; 15mL centrifuge tube; cell counting chamber.
[0113] 4. Experimental Methods and Results
[0114] Experimental Procedure: Ten C57BL / 6 mice were used. After shaving their backs, subcutaneous tumor formation was achieved using mouse melanoma cells (B16F10). Once the tumors were palpable, the mice were randomly divided into two groups of five mice each. The groups were: ① control group and ② tandospirone group. The control group received daily PBS treatment; the tandospirone group received daily intraperitoneal injection of tandospirone (3 mg / kg). Mouse weight and tumor volume were measured every other day until the study endpoint.
[0115] Experimental results:
[0116] Figure 5 This is a comparison photograph of the tumor volume of 5 mice in the control group and tandospirone group after the experiment. Figure 6 This is a comparison curve of tumor volume changes between the control group and the tandospirone group. Figure 6 The horizontal axis represents the number of days after treatment, and the vertical axis represents the tumor volume.
[0117] Depend on Figure 6The results showed that as the number of treatment days increased, the tumor volume growth in the tandospirone group was significantly smaller than that in the control group, indicating that tandospirone can effectively inhibit tumor growth in mice.
[0118] The body weight of mice in each group was measured, and the weight changes of mice in the control group and the tandospirone group were compared as shown in the figure below. Figure 7 As shown. Figure 7 The horizontal axis represents the number of days after treatment, and the vertical axis represents the body weight of the mice. Repeated experimental data are expressed as mean (N=5) ± SD; *P < 0.05. Figure 7 It can be seen that tandospirone treatment had little effect on the weight of mice, indicating that tandospirone has no obvious toxic side effects on mice.
[0119] The technical features of the above embodiments can be combined in any way. For the sake of brevity, not all possible combinations of the technical features in the above embodiments are described. However, as long as there is no contradiction in the combination of these technical features, they should be considered to be within the scope of this specification.
[0120] The embodiments described above are merely illustrative of several implementations of the present invention, and while the descriptions are relatively specific and detailed, they should not be construed as limiting the scope of the invention patent. It should be noted that those skilled in the art can make various modifications and improvements without departing from the concept of the present invention, and these all fall within the protection scope of the present invention. Therefore, the protection scope of this invention patent should be determined by the appended claims.
Claims
1. The use of tandospirone or a pharmaceutically acceptable salt thereof in the preparation of an antimelanoma drug, characterized in that, Tandospirone or a pharmaceutically acceptable salt thereof is the sole active pharmaceutical ingredient of the anti-melanoma drug.
2. The use of tandospirone or a pharmaceutically acceptable salt thereof according to claim 1 in the preparation of an anti-melanoma drug, characterized in that, The anti-melanoma drugs also include one or more of amitriazine and pharmaceutically acceptable salts of amitriazine.
3. The use of tandospirone or a pharmaceutically acceptable salt thereof according to claim 1 in the preparation of an anti-melanoma drug, characterized in that, The anti-melanoma drug is at least one of the drugs that inhibits cell proliferation in melanoma SK-MEL-5 cells and melanoma B16F10 cells.
4. The use of tandospirone or a pharmaceutically acceptable salt thereof according to any one of claims 1 to 3 in the preparation of an anti-melanoma drug, characterized in that, Pharmaceutically acceptable salts of tandospirone include tandospirone methanesulfonate.
5. The use of tandospirone or a pharmaceutically acceptable salt thereof according to any one of claims 1 to 3 in the preparation of an anti-melanoma drug, characterized in that, The dosage form of the anti-melanoma drug includes either an injection or an oral formulation.