CN113813259A - Application of octenidine dihydrochloride in preparation of antitumor drugs - Google Patents
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- SMGTYJPMKXNQFY-UHFFFAOYSA-N octenidine dihydrochloride Chemical compound Cl.Cl.C1=CC(=NCCCCCCCC)C=CN1CCCCCCCCCCN1C=CC(=NCCCCCCCC)C=C1 SMGTYJPMKXNQFY-UHFFFAOYSA-N 0.000 title claims abstract description 55
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
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- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention discloses application of octenidine dihydrochloride in preparation of antitumor drugs. In vitro cell experiments show that octenidine dihydrochloride (OCT) can inhibit the growth and proliferation of tumor cells such as nasopharyngeal carcinoma cells; experiments in mice show that subcutaneous tumor formation in nude mice is obviously inhibited by OCT, which shows that OCT can inhibit nasopharyngeal carcinoma cell growth, and immunohistochemical detection proves the safety of OCT as antitumor drug. Therefore, the OCT can be used for preparing anti-tumor drugs, can be used for treating tumors such as nasopharyngeal carcinoma, esophageal squamous carcinoma, colorectal cancer or lung cancer, and provides a new drug source for the adjuvant therapy of the cancers.
Description
Technical Field
The invention belongs to the technical field of medicines, and particularly relates to application of octenidine dihydrochloride in preparation of antitumor medicines.
Background
Nasopharyngeal carcinoma (NPC) is a regional malignancy with an incidence of 0.4 per 100,000 individuals in the United states and in most new casesNow the middle east south asian countries. In addition, the incidence of nasopharyngeal carcinoma has a certain ethnic and familial inheritance, such as: borneo Bida friends and Nagars in northern India[1]. Nasopharyngeal carcinoma is a malignant tumor that occurs in the outermost epithelial layer of the nasopharyngeal cavity, above the oropharynx and hypopharynx, near the base of the skull.
Conventional treatments for NPC include radiation therapy or chemotherapy or a combination of both. In areas with high incidence of nasopharyngeal carcinoma, limited radiotherapy technologies and surgical facilities hinder the treatment effect, resulting in local residual tumor, further generating tumor recurrence, and greatly reducing the overall survival rate of patients. More importantly, the molecular basis of NPC pathogenesis is still poorly understood, and surgical resection is often the last option for patients with advanced tumor, given the close proximity of the nasopharyngeal site to the brain stem cell area, major blood vessels and nerves. The early stage of NPC has no obvious symptoms, and some symptoms during the onset of the NPC are similar to headache, neuropathic facial pain, neck lumps, epistaxis or nasal obstruction and the like and are easily confused with other diseases, so that misdiagnosis is caused, and the treatment is delayed. The existing therapeutic drugs for patients with advanced nasopharyngeal carcinoma comprise cisplatin, 5-FU, paclitaxel, gemcitabine and the like[2]Although these chemotherapeutic drugs can provide some clinical benefit to patients, there is still a need to develop new drugs with high efficacy and low toxicity to improve the anti-tumor effect.
Octenidine dihydrochloride (OCT), also known as Octenidine dihydrochloride, is an effective antiseptic compound for skin mucosa and wounds, and has a structural formula shown in formula I:
according to related reports, OCT has antibacterial and anti-inflammatory effects[3]It can be used for wound infection and preoperative skin preparation, has obvious inhibiting effect on Staphylococcus aureus, and can interact with bacterial surface structure to cause lysis and death[4]. OCT can also stimulate phagocytosis and growth factor, and is beneficial for wound healing[4]However, the effect of OCT in tumor cells has not been reported yet.
Disclosure of Invention
The invention aims to overcome the defects in the prior art and provide the application of octenidine dihydrochloride in preparing antitumor drugs.
The purpose of the invention is realized by the following technical scheme:
application of octenidine dihydrochloride (OCT) in preparing antitumor drugs is provided.
The structural formula of the octenidine dihydrochloride is shown as a formula I:
the tumors comprise nasopharyngeal carcinoma, esophageal squamous carcinoma, colorectal cancer, lung cancer and the like; nasopharyngeal carcinoma is preferred.
The effective concentration of the octenidine dihydrochloride is 0-5 mu M (excluding 0); preferably 0.8 to 5. mu.M.
The medicine contains one or more pharmaceutically acceptable carriers or auxiliary materials.
The auxiliary material is at least one of a sustained release agent, an excipient, a filler, an adhesive, a wetting agent, a disintegrating agent, an absorption enhancer, a surfactant and a lubricant; preferably edible oil; more preferably corn oil.
The medicine can be further prepared into a pharmaceutical preparation by adopting a conventional method in the field; comprises oral administration pharmaceutical preparations, such as capsules, pills, tablets, oral liquid, granules and the like.
Application of octenidine dihydrochloride in preparation of medicines for inhibiting growth and/or proliferation of nasopharyngeal carcinoma cells.
The nasopharyngeal carcinoma cells comprise at least one of nasopharyngeal carcinoma cells CNE-1 and SUNE-1.
Compared with the prior art, the invention has the following advantages and effects: the invention combines in vitro and in vivo experiments to find that the octenidine dihydrochloride has the functions of resisting inflammation and sterilizing on the surface of skin and inhibiting the growth and proliferation of nasopharyngeal carcinoma cells, so that the octenidine dihydrochloride can be used for treating tumors and provides a new medicine source for the adjuvant treatment of cancers.
Drawings
FIG. 1 is a graph showing the effect of OCT on nasopharyngeal carcinoma cell proliferation; wherein A is the influence of OCT on nasopharyngeal carcinoma cells CNE-1; and B is the influence of OCT on nasopharyngeal carcinoma cells CNE-1.
FIG. 2 is a graph showing the effect of OCT on CNE-1 apoptosis in nasopharyngeal carcinoma; wherein A is a flow cytometry detection result; b is the apoptosis condition.
FIG. 3 is a graph showing the effect of OCT on the tumorigenic capacity of nasopharyngeal carcinoma cells in mice; wherein A is a tumor picture; b is the tumor volume; c is tumor weight.
FIG. 4 is a graph showing the results of measurement of glutamic oxaloacetic transaminase and glutamic pyruvic transaminase in serum of mice after OCT treatment of the mice; wherein, A is the activity condition of serum glutamic-oxalacetic transaminase; b is the activity of serum glutamic pyruvic transaminase.
FIG. 5 is a graph showing the results of immunohistochemical detection of heart, liver, lung and kidney tissues and tumors of mice treated with OCT.
Detailed Description
The present invention will be described in further detail with reference to examples, but the embodiments of the present invention are not limited thereto. Reagents, methods and apparatus used in the present invention are conventional in the art unless otherwise indicated. The test methods in the following examples, in which specific experimental conditions are not specified, are generally performed according to conventional experimental conditions or according to the experimental conditions recommended by the manufacturer. Unless otherwise specified, reagents and starting materials for use in the present invention are commercially available.
Octenidine dihydrochloride (OCT) in an embodiment of the invention was purchased from Targetmol corporation (https:// www.targetmol.com).
Nasopharyngeal carcinoma cells CNE-1 and SUNE-1 in the examples of the present invention were purchased from cell banks of Chinese academy of sciences.
Example 1 in vitro experiments
(1) Detection of the effect of OCT on cell proliferation: the cells CNE-1 and SUNE-1 were plated on separately96-well plates, 5000 cells per well, cultured at 37 ℃ in CO2In an incubator with the content of 5%, after 24 hours, OCT (with the final concentration of 0, 0.2, 0.4, 0.8, 1.6 and 3.2 mu M) with different concentrations is used for processing, the processing time is 24 hours, the cell activity is detected by a CCK-8 cell proliferation detection kit (Targetmol), and the influence of OCT with different concentrations on the proliferation of nasopharyngeal carcinoma cells is researched.
(2) Detecting apoptosis by flow cytometry: before detection by a flow cytometer, cells CNE-1 are treated by OCT, namely the CNE-1 cells are paved in a six-hole plate for culture, the number of the cells reaches 70% of each hole after 24 hours, then the CNE-1 cells are treated by OCT (final concentration is 0, 0.4, 0.8 and 1.6 mu M) with different concentrations for 24 hours, then the cells are treated by an annexin V-FITC apoptosis detection kit (Biyunyan), the treatment method is carried out according to the instruction provided by the kit, and then the detection is carried out by the flow cytometer to study the influence of the OCT with different concentrations on the apoptosis of nasopharyngeal carcinoma cells.
The results of the cell level experiments are shown in figures 1 and 2: in FIG. 1, the cell activity of nasopharyngeal carcinoma decreased with increasing OCT concentration; in FIG. 2, the level of apoptosis of nasopharyngeal carcinoma CNE-1 cells increased with increasing OCT concentration. Indicating that the OCT can inhibit the proliferation of human nasopharyngeal carcinoma cells and promote apoptosis.
Example 2 in vivo experiments
(1) Constructing a nasopharyngeal carcinoma mouse model: selecting a male mouse NCG (purchased from Nanjing model animal research center) with age of 6 weeks, and constructing a nasopharyngeal carcinoma mouse model by adopting a subcutaneous injection mode, namely, mixing a cell suspension (nasopharyngeal carcinoma cells CNE-1) and Matrigel (Corning Matrigel Matrix) according to a volume ratio of 1: 1 mix, 2X10 per mouse6Individual cells (mice were injected subcutaneously with resuspended cells picked up with a 25G needle microinjector). Following subcutaneous injection, the tumor size reached 5x5mm for subsequent experiments.
(2) The experiment was divided into three groups: low concentration drug treatment group (5, injection amount 3 mg/kg); high concentration drug treatment group (5, injection amount 6 mg/kg); control group (5, injected with an equal volume of regular commercially available corn oil as the treated group).
(3) OCT processing: after subcutaneous injection, when the tumor size reaches 5 multiplied by 5mm, OCT treatment is started, and the administration is carried out in a gastric lavage mode, namely OCT is dissolved in corn oil and administered at the concentration of 3mg/kg and 6mg/kg, once every two days, and the administration is carried out for 10 times in total; the control group was given an equal volume of corn oil in the same manner. After 3 weeks, mice were euthanized and tumors were removed for observation and measurement, while heart, liver, lung, and kidney were removed for HE staining by a biological company (hubei baios biotechnology limited, guangzhou) and tumors were also sent to the same biological company for immunohistochemical staining (Ki-67 staining).
The results are shown in FIGS. 3 to 5: FIG. 3 shows the results of subcutaneous tumor formation in mice, which can significantly inhibit the growth of nasopharyngeal carcinoma cells CNE-1 after OCT gastric lavage of mice; the growth curve of the tumor volume and the statistics of the tumor quality show that subcutaneous tumor formation in a nude mouse is obviously inhibited by OCT, which shows that OCT can inhibit the growth of nasopharyngeal carcinoma cells; FIG. 4 shows that there is no great difference in serum glutamic-oxaloacetic transaminase and glutamic-pyruvic transaminase measurements of two groups of mice; FIG. 5 is a pathological tissue section detection result of a mouse, and the heart, liver, lung and kidney tissues of an experimental mouse are subjected to immunohistochemical detection, so that no obvious difference exists between the experimental group and the control group, and the safety of the use of the OCT as an anti-tumor drug is proved. The results of in vivo experiments show that OCT can inhibit the growth of nasopharyngeal carcinoma cell transplantation tumor in mice.
The above embodiments are preferred embodiments of the present invention, but the present invention is not limited to the above embodiments, and any other changes, modifications, substitutions, combinations, and simplifications which do not depart from the spirit and principle of the present invention should be construed as equivalents thereof, and all such changes, modifications, substitutions, combinations, and simplifications are intended to be included in the scope of the present invention.
Reference documents:
[1]Sun Z,Wang X,Wang J,Wang J,Liu X,Huang R,et al.Key radioresistance regulation models and marker genes identified by integrated transcriptome analysis in nasopharyngeal carcinoma. Cancer medicine.2021.
[2]Xing X,Zhou X,Yang Y,Li Y,Hu C,Shen C.The impact of body composition parameters on severe toxicities in patients with locoregionally advanced nasopharyngeal carcinoma undergoing neoadjuvant chemotherapy.Annals of translational medicine.2021；9:1180.
[3]Kramer A,Dissemond J,Kim S,Willy C,Mayer D,Papke R,et al.Consensus on Wound Antisepsis:Update 2018.Skin pharmacology and physiology.2018；31:28-58.
[4]Hubner NO,Siebert J,Kramer A.Octenidine dihydrochloride,a modern antiseptic for skin, mucous membranes and wounds.Skin pharmacology and physiology.2010；23:244-58。
Claims (10)
1. application of octenidine dihydrochloride in preparation of antitumor drugs.
2. Use according to claim 1, characterized in that: the tumor is nasopharyngeal carcinoma, esophageal squamous carcinoma, colorectal cancer or lung cancer.
3. Use according to claim 2, characterized in that: the tumor is nasopharyngeal carcinoma.
4. Use according to claim 1, characterized in that: the effective concentration of the octenidine dihydrochloride is 0-5 mu M, and 0 is excluded.
5. Use according to claim 4, characterized in that: the effective concentration of the octenidine dihydrochloride is 0.8-5 mu M.
6. Use according to any one of claims 1 to 5, characterized in that: the medicine contains one or more pharmaceutically acceptable carriers or auxiliary materials; the auxiliary material is at least one of a sustained release agent, an excipient, a filler, an adhesive, a wetting agent, a disintegrating agent, an absorption enhancer, a surfactant and a lubricant.
7. Use according to claim 6, characterized in that: the auxiliary material is edible oil.
8. Use according to claim 7, characterized in that: the auxiliary material is corn oil.
9. Use according to claim 6, characterized in that: the medicine is further prepared into capsules, pills, tablets, oral liquid or granules.
10. Application of octenidine dihydrochloride in preparation of medicines for inhibiting growth and/or proliferation of nasopharyngeal carcinoma cells.
Priority Applications (2)
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| CN202111001060.1A CN113813259A (en) | 2021-08-30 | 2021-08-30 | Application of octenidine dihydrochloride in preparation of antitumor drugs |
| PCT/CN2021/121943 WO2023029141A1 (en) | 2021-08-30 | 2021-09-29 | Use of octenidine dihydrochloride in preparation of antitumor drug |
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| CN202111001060.1A CN113813259A (en) | 2021-08-30 | 2021-08-30 | Application of octenidine dihydrochloride in preparation of antitumor drugs |
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| EP3714069A1 (en) * | 2017-11-20 | 2020-09-30 | Tolremo Therapeutics AG | Diagnostic method |
| US11286171B2 (en) * | 2019-11-01 | 2022-03-29 | Regina VERTELOVA | Therapeutic metallic nanoparticle composition and method of use and manufacture thereof |
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Non-Patent Citations (2)
| Title |
|---|
| LIHONG LI: "Virtual screening based identification of miltefosine and octenidine as inhibitors of heat shock protein 90", 《NAUNYN-SCHMIEDEBERG"S ARCHIVES OF PHARMACOLOGY》 * |
| 刘涛: "17-丙烯胺基-17-去甲氧基格尔德霉素对鼻咽癌细胞VEGF和Survivin表达的影响", 《延安大学学报》 * |
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