CN-122005517-A - Application of famoxadone derivative in preparation of glioma drugs

Abstract

The invention discloses an application of a famoxadone derivative in preparing a glioma drug, and belongs to the technical field of medicines. The compound has remarkable inhibitory activity on various glioma cell lines such as SF126, T98G, A172, U-87 MG and U251, has activity superior to that of a common glioma-resistant drug temozolomide in clinic and has low toxicity on normal brain cells. The invention also provides a preparation method of the compound and a pharmaceutical composition containing the compound, and the pharmaceutical composition can be prepared into various dosage forms such as injection, tablet and the like. The invention provides a new effective drug choice for glioma treatment, has mature preparation process and various drug dosage forms, and has wide clinical application prospect.

Inventors

• XIAO QIANQIAN
• WANG ZHIWEI
• WANG SONGSONG

Assignees

• 山东第一医科大学(山东省医学科学院)

Dates

Publication Date

20260512

Application Date

20260414

Claims (4)

1. 1. The application of the pennisetum alopecuroide derivative in preparing glioma medicaments is characterized in that gliomas comprise human brain tumor cells, human brain glioma cells, human glioblastoma cells and human brain astroglioblastoma cells.
2. 2. A medicament for treating glioma, which is characterized by comprising the famoxadone derivative according to claim 1 and pharmaceutically acceptable auxiliary materials.
3. 3. The medicament of claim 2, wherein the pharmaceutically acceptable excipients comprise one or more of diluents, binders, disintegrants, lubricants, cosolvents, emulsifiers, flavoring agents, colorants, or preservatives.
4. 4. The medicament according to claim 2, wherein the medicament is in the form of a tablet, capsule, granule, injection, oral liquid, suspension, ointment or gel.

Description

Application of famoxadone derivative in preparation of glioma drugs Technical Field The invention relates to the technical field of medicines, in particular to an application of a pennisetum alopecuroides lactone derivative in preparation of glioma medicines. Background Gliomas are the most common malignant neoplasms in the central nervous system, accounting for about 40% -50% of intracranial tumors. It has the characteristics of strong invasiveness, rapid growth, high recurrence rate, poor prognosis and the like, and seriously threatens the life and health of human beings. At present, the treatment means of glioma mainly comprise comprehensive therapies such as surgical excision, radiation therapy, chemical drug therapy and the like, but the clinical treatment effect is still not satisfactory. The operation excision is difficult to thoroughly remove the tumor tissue, the residual tumor cells are easy to cause recurrence, the radiation treatment can inhibit the tumor growth to a certain extent, but the radiation treatment also causes damage to normal brain tissue and causes a series of adverse reactions, and the chemical drug treatment is an important means for postoperative adjuvant treatment and advanced glioma treatment, however, the existing chemotherapy drugs have the problems of poor targeting, large toxic and side effects, easy drug resistance and the like, and limit the clinical application effect. Therefore, the development of a novel anti-glioma drug with the characteristics of high efficiency, low toxicity, strong targeting and the like becomes an important subject to be solved urgently in the current medical field. Disclosure of Invention Aiming at the problems of insufficient curative effect, large side effect, difficult acquisition of natural active compounds and the like of the traditional glioma therapeutic drugs, the invention provides a derivative of the nomame lactone, which is prepared by taking nomame lactone alcohol extracted from the nomame extract of the plant genus nomame of the family Compositae as a core raw material through artificial chemical synthesis and structural modification, and does not directly use the natural extracted nomame lactone alcohol. The compound has simple synthetic route, can be prepared in large quantity, has high-efficiency inhibitory activity on glioma cells, and can be used for preparing medicines for treating glioma. The invention provides an application of a pennisetum alopecuroide derivative in preparing a medicine for treating glioma, wherein the pennisetum alopecuroide derivative is used for preparing the medicine for treating glioma, and the glioma comprises human brain tumor cells (SF 126), human brain glioma cells (T98G), human glioblastoma cells (A172) and human brain astroglioblastoma cells (U-87 MG). By the technical scheme, the application has the beneficial effects that: The invention discovers that the 12-methylamino-parinolide ring-opening product (compound A) of the parinolide derivative has remarkable anti-glioma activity, has inhibition effect on SF126, T98G, A, U-87 MG, U251 and other glioma cell lines, has better inhibition activity than the clinical common anti-glioma drug temozolomide, and has lower toxicity to normal brain cells (such as human brain astrocytes) and better safety. The preparation method of the compound is mature, the reaction parameters are clear, the yield is stable, the purity is controllable, the compound is beneficial to industrial production, the medicine prepared by taking the compound as an active ingredient can be prepared into various dosage forms according to clinical requirements, the use is convenient, a new effective choice is provided for glioma treatment, and the compound has wide clinical application prospect. Drawings FIG. 1 is a schematic diagram of the chemical structure of a skatole derivative provided by the examples of the present invention; FIG. 2 is a chemical structural schematic of a process for preparing a ring-opening product of 12-methylamino-homopterolide (Compound A). Detailed Description The invention is illustrated by the following examples. Example 1: preparation of ring-opening product of 12-methylamino-homonymolactone alcohol (Compound A): The target derivative compound A is prepared by taking the natural extract of the plant of the genus Tianming of the family Compositae as a starting material and performing chemical modification synthesis. As shown in FIG. 2, the reaction end point (developing agent: dichloromethane-methanol=100:3, ultraviolet lamp 254 nm) was detected by TLC, and when the raw material spots completely disappeared, the product spots were clear and no new impurity spots appeared, the reaction was judged to be ended, by dissolving the skatole (50 mg,1.95×10 -1 mmol) in methanol (1.5 mL), then slowly dropping an aqueous KOH solution (0.25 mL,0.1 mol/L) into the reaction system, stirring at room temperature for 30 min, further adding methylamine hydrochloride (52.65m