阅读说明：本技术 2,5-呋喃二甲醇在制备抗肿瘤药物中的应用 (Application of 2, 5-furandimethanol in preparation of antitumor drugs ) 是由 冯昆 侯亚男 郑春辉 王雅溶 于 2019-09-17 设计创作，主要内容包括：本发明属于医药领域,公开了一种2,5-呋喃二甲醇在制备抗肿瘤药物中的应用,所述肿瘤包括神经母细胞瘤、肺癌、胃腺癌和结直肠腺癌。一种抗肿瘤药物,所述抗肿瘤药物包括2,5-呋喃二甲醇。所述抗肿瘤药物还包括药学上可接受的辅料。所述抗肿瘤药物的给药方式为口服或注射。本发明首次公开了2,5-呋喃二甲醇的新的医药用途,即可用于制备抗肿瘤药物,给治疗肿瘤提供了一种新的途径和手段。本发明指出2,5-呋喃二甲醇的毒副作用小,可对多种类型的肿瘤产生显著的抑制作用,具有良好的临床应用价值。(The invention belongs to the field of medicines, and discloses application of 2, 5-furandimethanol in preparation of antitumor drugs, wherein tumors comprise neuroblastoma, lung cancer, gastric adenocarcinoma and colorectal adenocarcinoma. An anti-tumor drug, which comprises 2, 5-furandimethanol. The anti-tumor medicine also comprises pharmaceutically acceptable auxiliary materials. The administration mode of the anti-tumor medicine is oral administration or injection. The invention discloses a new medical application of 2, 5-furandimethanol for the first time, namely the 2, 5-furandimethanol can be used for preparing anti-tumor medicaments, and provides a new way and means for treating tumors. The invention indicates that the 2, 5-furandimethanol has small toxic and side effects, can generate obvious inhibition effect on various tumors, and has good clinical application value.)

The application of 2, 5-furandimethanol in preparing antitumor drugs is characterized in that tumors comprise neuroblastoma, lung cancer, gastric adenocarcinoma and colorectal adenocarcinoma.

2. An antitumor agent characterized by comprising 2, 5-furandimethanol.

3. the antitumor agent as claimed in claim 2, wherein the mass content of 2, 5-furandimethanol in the antitumor agent is 5-30%.

4. The antitumor drug as claimed in claim 2, further comprising a pharmaceutically acceptable excipient.

5. the antitumor agent as claimed in claim 4, wherein said pharmaceutically acceptable adjuvant comprises at least one of an osmotic pressure regulator, a pH regulator, a solubilizer, a solubilizing agent, an antioxidant, a bacteriostatic agent, an emulsifier, a binder and a suspending agent.

6. The antitumor drug as claimed in claim 2, wherein the antitumor drug is formulated in the form of a gel, a soft capsule, an oral preparation, an injection solution, a lyophilized powder for injection or a bolus injection.

7. The antitumor drug as claimed in claim 2, wherein the administration mode of the antitumor drug is oral or injection, and the injection mode is intravenous injection, intramuscular injection, intraperitoneal injection or subcutaneous injection.

Technical Field

The invention belongs to the field of medicines, and particularly relates to application of 2, 5-furandimethanol in preparation of antitumor drugs.

Background

Tumor is one of the major diseases seriously harming human health, and has better treatment means for early tumor, but for malignant tumor, the malignant tumor is mainly treated to improve the life quality of patients and prolong the survival time, and is difficult to eradicate without relapse. Although many important achievements have been made on the research of the anti-tumor drugs in recent decades, most of the anti-tumor drugs used clinically at present kill normal body cells while killing tumor cells, thereby not only affecting the treatment effect, but also bringing great pain to tumor patients. Therefore, there is still a need to continuously research and develop novel antitumor drugs.

2, 5-Furandimethanol is commonly used as an intermediate for preparing medicaments to synthesize medicaments for treating neurodegenerative diseases, such as medicaments for preventing and treating the neurodegenerative diseases Parkinson's disease and the like (Japanese Bin and the like, the research on the biological activity and safety of a common component 5-hydroxymethyl-2-furfural in traditional Chinese medicines and foods progresses [ J ] Chinese pharmacist, 2018,21: 1456-. The 5-hydroxymethyl-2-furfural serving as a downstream product of the 2, 5-furandimethanol also exists in dogwood, polygonum multiflorum, schisandra chinensis and codonopsis pilosula, and has the functions of resisting myocardial ischemia, resisting oxidation, reducing blood pressure and blood sugar and improving learning and memory.

However, no relevant data of pharmacological activity and toxicity of 2, 5-furandimethanol exists at home and abroad at present, no report on whether the 2, 5-furandimethanol has the effect of inducing cancer cell apoptosis exists, and no precedent for using the 2, 5-furandimethanol in preparation of antitumor drugs exists.

Disclosure of Invention

Aiming at the defects of the prior art, the invention provides the application of 2, 5-furandimethanol in preparing antitumor drugs. The 2, 5-furandimethanol has good inhibition effect on various tumors (such as neuroblastoma, lung cancer, gastric adenocarcinoma and colorectal adenocarcinoma), and has small adverse reaction.

The application of 2, 5-furandimethanol in preparing antitumor drugs, wherein tumors comprise neuroblastoma, lung cancer, gastric adenocarcinoma and colorectal adenocarcinoma.

An anti-tumor drug, which comprises 2, 5-furandimethanol.

The anti-tumor medicine is a human anti-tumor medicine or an animal anti-tumor medicine.

Preferably, the mass content of the 2, 5-furandimethanol in the antitumor medicament is 5-30%.

preferably, the anti-tumor medicine further comprises pharmaceutically acceptable auxiliary materials.

Further preferably, the pharmaceutically acceptable auxiliary materials comprise at least one of osmotic pressure regulator, pH regulator, solubilizer, cosolvent, antioxidant, bacteriostatic agent, emulsifier, binder and suspending agent.

The pharmaceutically acceptable excipients include, but are not limited to, the following classes: span, tween, polylactic acid, starch, ethanol, sodium carboxymethyl starch, magnesium stearate, polyethylene glycol and carbomer.

preferably, the preparation form of the anti-tumor medicament is gel, soft capsule, oral preparation, injection, freeze-dried powder injection or infusion solution. The large infusion solution refers to a liquid sterilization preparation which has the capacity of more than or equal to 50mL and is directly infused into the body by intravenous drip.

Preferably, the administration mode of the anti-tumor drug is oral administration or injection, and the injection mode is intravenous injection, intramuscular injection, intraperitoneal injection or subcutaneous injection.

The anti-tumor drug is a tumor cell growth inhibitor. The effective activity of the 2, 5-furandimethanol in the antitumor drug can inhibit the growth of tumor cells and induce the tumor cells to generate apoptosis.

The invention adopts neuroblastoma, lung cancer cell, gastric adenocarcinoma and colorectal adenocarcinoma cell to carry out in-vitro tumor cell test, and the test result shows that the 2, 5-furandimethanol can induce various tumor cells to apoptosis and has good anti-tumor effect. Meanwhile, the toxicity test of the 2, 5-furandimethanol on animals is carried out, and the result shows that the 2, 5-furandimethanol has small toxic and side effects, does not influence the normal activities of the animals, and does not cause the pathological changes of body organs.

Compared with the prior art, the invention has the following beneficial effects:

1. The invention provides a new application of 2, 5-furandimethanol in preparing antitumor drugs, and the 2, 5-furandimethanol has good growth inhibition and killing effects on various tumors and has wide clinical application prospect;

2. Toxicity experiments of rats show that adverse reactions and toxic and side effects generated by the gavage of the 2, 5-furandimethanol solution are slight, normal activities of the rats are not influenced, and obvious lesions of organs are not caused.

The 3.2, 5-furandimethanol has a simple structure and low acquisition difficulty, and the 2, 5-furandimethanol is applied to preparation of antitumor drugs, so that the cost of the drugs can be controlled.

Drawings

FIG. 1 is a pathological section of liver, kidney and spleen of rats of the blank control group, the middle dose group and the high dose group after 14d of intragastric administration in example 5.

Detailed Description

in order to make the technical solutions of the present invention more apparent to those skilled in the art, the following examples are given for illustration. It should be noted that the following examples are not intended to limit the scope of the claimed invention.