阅读说明：本技术 一种倍半萜类化合物在制备治疗胃肠间质瘤药物中的用途 (Application of sesquiterpene compound in preparation of medicine for treating gastrointestinal stromal tumor ) 是由 李飞 田芝雷 于 2019-09-05 设计创作，主要内容包括：本发明提供一种倍半萜类化合物在制备治疗胃肠间质瘤药物中的用途,其中地丁素B、aristolactone、银袋内酯乙均对胃肠间质瘤具有抑制作用。本发明化合物毒性低,副作用小,具有良好的抑制胃肠间质瘤的效果,扩展了治疗胃肠间质瘤的药物范围,具有稳定性好,释放迅速,提高了药物活性的特点。(The invention provides application of sesquiterpene compounds in preparation of a medicine for treating gastrointestinal stromal tumors, wherein the gerbera din B, aristolactone and the cecrolactone B both have an inhibitory effect on the gastrointestinal stromal tumors. The compound has low toxicity and small side effect, has good effect of inhibiting gastrointestinal stromal tumor, expands the range of medicines for treating the gastrointestinal stromal tumor, and has the characteristics of good stability, quick release and improved medicinal activity.)

1. Application of jalapactone B or aristolactone or dibenin in preparing medicine for treating gastrointestinal stromal tumor is provided.

2. The use according to claim 1, wherein the gylcolide b or aristolactone or dibulin is formulated with a pharmaceutically acceptable carrier to form a pharmaceutical composition.

3. The use of claim 1, wherein the medicament is in the form of tablet, capsule, soft capsule, granule, or injection.

4. The use according to claim 1, wherein the medicament is for use with a second therapeutic agent for the treatment of gastrointestinal stromal tumors.

Technical Field

The invention belongs to the field of medicines. Relates to an application of sesquiterpene compound in preparing medicine for treating gastrointestinal stromal tumor.

Background

Gastrointestinal stromal tumors are a tumor of mesenchymal tissue in the gastrointestinal tract that is often mistaken for a neurological tumor or a smooth muscle tumor. The disease incidence is relatively reduced, about 10 ten-thousandth, and the Chinese medicinal preparation belongs to an unusual disease in Chinese clinical medical diagnosis and treatment. At present, the clinical medical field of China has no definite definition on the pathogenesis and clinical diagnosis and treatment of gastrointestinal stromal tumors. The mainly adopted treatment method is surgical radical excision treatment. At present, the medicines for treating gastrointestinal stromal tumors are expensive and bring heavy burden to patients, and the existing medicines often have serious toxic and side effects and poor compliance of patients. In the prior art, no sesquiterpenoids are developed for treating gastrointestinal stromal tumors, and the invention provides a novel medicament for treating gastrointestinal stromal tumors. At present, drugs for treating gastrointestinal stromal tumors, such as imatinib and the like, are easy to generate drug resistance in the treatment process.

Disclosure of Invention

The invention provides a purpose of sesquiterpene compounds in treating gastrointestinal stromal tumors, which aims to overcome the defects of the prior art.

In order to realize the purpose of the invention, the technical scheme of the invention is as follows:

the sesquiterpene compound provided by the invention selectively uses the gerdinin or the jalapactone B or the aristolactone, and provides a new application of the gerdinin or the jalapactone B or the aristolactone.

Application of DITINOL or YINGBAOLINO B or ARISTOLACTONE in preparing medicine for treating gastrointestinal stromal tumor is provided.

The pharmaceutical composition is prepared from the dilantin or jalapactone B or aristolactone and a pharmaceutically acceptable carrier.

The dosage form of the medicine can be tablets, capsules, soft capsules, granules and injections.

The medicament may be used in combination with a second therapeutic agent for the treatment of gastrointestinal stromal tumors.

The deludinin is selectively deludinin A or deludinin B

The deltoid or jacaralactone, ethyl or aristolactone, is commercially available or synthesized by conventional compound synthesis methods known in the art using commercially available starting materials. After synthesis, the product can be further purified by means of column chromatography, high performance liquid chromatography or crystallization.

Preferably, the medicament is an oral formulation. Experiments show that the medicine prepared from the dibulin or the jalapactone B or the aristolactone has an obvious treatment effect when acting on gastrointestinal stromal tumor cells.

The digenin or the jalapactone or the aristolactone has the effect of enhancing the activity of natural killer cells (NK), can enhance the activity of immune cells, promotes the NK cells to kill tumor cells, and secretes cytokines to regulate other immune cells. And further act together with tumor cells.

The pharmaceutical composition may be formulated in any pharmaceutically acceptable dosage form including: tablets, sugar-coated tablets, film-coated tablets, enteric-coated tablets, capsules, hard capsules, soft capsules, oral liquids, buccal agents, granules, pills, powders, ointments, pellets, suspensions, powders, solutions, injections, suppositories, ointments, plasters, creams, sprays, drops, patches; oral dosage forms are preferred, such as: capsule, tablet, oral liquid, granule, pill, powder, pellet, and unguent. The oral dosage forms may contain conventional excipients such as binders, fillers, diluents, tabletting agents, lubricants, disintegrating agents, coloring agents, flavoring agents and wetting agents, and the tablets may be coated if necessary.

In the present invention, there is no limitation on the type of the binder, and it may be a conventional binder that is pharmaceutically acceptable. In a preferred embodiment of the invention, the binder is selected from hydroxypropyl cellulose.

In the present invention, there is no limitation on the type of the pharmaceutically acceptable lubricant, and it may be magnesium stearate, talc, paraffin, glyceryl monostearate, glyceryl monopalmitate, and the like, which are commonly used in the art. In a preferred embodiment of the invention, the lubricant is selected from magnesium stearate. In the present invention, there is no limitation on the amount of the lubricant, and it may be an amount conventionally used in the art.

In the present invention, the term "pharmaceutically acceptable additive" is used to mean a pharmaceutically acceptable additive that enhances the properties of the formulation. Such additives are well known to those skilled in the art. Wherein the filler is lactose, pregelatinized starch, microcrystalline cellulose, etc. The disintegrant is croscarmellose sodium, crospovidone and sodium carboxymethyl starch. The adhesive is hydroxypropyl cellulose and the like. The lubricant is magnesium stearate, etc.

The second therapeutic agent can be selected from imatinib, sunitinib, and other tinib drugs.

The content of said butin or gycolactone or aristolactone of the present invention in the composition is 0.1 to 200mg, and the therapeutically effective amount thereof is more preferably 5 to 150mg, more preferably 50 to 100mg, and still more preferably 75 mg.

The invention has the following excellent effects:

1. the compound of the invention has low toxicity and small side effect.

2. Has good effect of inhibiting gastrointestinal stromal tumor, and expands the range of medicines for treating gastrointestinal stromal tumor.

3. The tablet of the invention has good stability, quick release and improved drug activity.

Detailed Description

Preferred embodiments of the present invention will be described in detail with reference to the following examples. It is to be understood that the following examples are given for illustrative purposes only and are not intended to limit the scope of the present invention. Various modifications and alterations of this invention will become apparent to those skilled in the art without departing from the spirit and scope of this invention.

The experimental procedures used in the following examples are all conventional procedures unless otherwise specified.

Materials, reagents and the like used in the following examples are commercially available unless otherwise specified.