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Application of picrasma quassioides alkaloid serving as STAT3 (Signal Transducer and Activator of Transcription 3) signal specificity inhibitor

An alkaloid, specific technology, applied in the field of medical applications, can solve the problems such as drugs that have not yet appeared

Inactive Publication Date: 2012-07-04
白银博赛宁生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the development of drugs targeting STAT3 has become recognized as an important solution for the treatment of certain tumors, but no ideal drug has yet been used in clinical practice.

Method used

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  • Application of picrasma quassioides alkaloid serving as STAT3 (Signal Transducer and Activator of Transcription 3) signal specificity inhibitor
  • Application of picrasma quassioides alkaloid serving as STAT3 (Signal Transducer and Activator of Transcription 3) signal specificity inhibitor
  • Application of picrasma quassioides alkaloid serving as STAT3 (Signal Transducer and Activator of Transcription 3) signal specificity inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Embodiment 1, the preparation of bitter wood tablet

[0029] Formula: DHCD (purity greater than 95%) 20.0g

[0030] Filler 180.0g

[0031] Disintegrant 10.0g

[0032] Adhesive 6.0g

[0033] Lubricant 3.0g

[0034] Total 200.0g

[0035] Process: 1000 tablets were made according to the conventional process for preparing tablets, each containing 20 mg of DHCD.

Embodiment 2

[0036] Embodiment 2: the preparation of bitter wood capsule

[0037] Formula: DHCD (purity greater than 95%) 50.0g

[0038] Filler 85.0g

[0039] Adhesive 5.0g

[0040] Lubricant 10.0g

[0041] Total 200.0g

[0042] Process: make 1000 capsules according to the conventional process for preparing capsules, and each capsule contains 50 mg of DHCD.

Embodiment 3

[0043] The preparation of embodiment 3, DHCD injection

[0044] Formula: DHCD (purity greater than 95%) 100.0g

[0045] Citric acid 1.0g

[0046] Sodium citrate 0.5g

[0047] Sodium chloride 18.0g

[0048] Water for injection 2000ml

[0049] Process: According to the conventional process for preparing injections, a total of 1000 2ml injections were made, each with 100 mg of DHCD.

[0050] The fillers, disintegrants, binders, lubricants and other auxiliary materials in the above-mentioned embodiments are the most conventional auxiliary materials in pharmacy.

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Abstract

The invention provides a novel medical application of picrasma quassioides alkaloid, i.e., an application of picrasma quassioides alkaloid serving as a STAT3 (Signal Transducer and Activator of Transcription 3) signal specificity inhibitor. As proved by a cell model screening experiment and Western-Blot detection, the picrasma quassioides alkaloid has high STAT3 inhibiting activity and can be used for effectively inhibiting the expression of relevant genes regulated and controlled by STAT3, so that the growth of tumor cells dependent on STAT3 signals can be inhibited effectively. The picrasma quassioides alkaloid is taken as an active ingredient for preparing an antitumor medicament based on the target spot of STAT3; and antitumor medicaments such as various oral preparations, injections and the like of various dosage forms are prepared from pharmaceutically-acceptable processes and auxiliary materials by taking picrasma quassioides alkaloid as an active ingredient.

Description

technical field [0001] The invention belongs to the field of medical applications, and relates to the medical use of eucalyptus alkaloids, in particular to the application of eucalyptus alkaloids as specific inhibitors of STAT3 signals. Background technique [0002] Bitterwood (Picrasma quassioides) has high medicinal value, and the processed or extracted active ingredients can be used for auxiliary treatment of various diseases including tumors. Dehydrocrenatidine (chemical name: 1-vinyl-4,8-dimethoxy-9H-β-carboline, English name: 1-Ethenyl-4,8-dimethoxy-9H-β-carboline; CAS No: 65236-62-6, abbreviated as DHCD) is an alkaloid extracted from bitter wood with the molecular formula C 15 h 14 N 2 o 2 , molecular weight 254.3, its structural formula is: [0003] [0004] DHCD was first isolated by T. Ohmoto et al. (Chem. Pharm. Bull., 1985, 33(8), 3356-3360), but there is no clear monomer application report yet. [0005] STAT3 is one of the important members of a series ...

Claims

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Application Information

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IPC IPC(8): A61K31/437A61P35/00
Inventor 杜宇平陈星王勤杨金波
Owner 白银博赛宁生物科技有限公司
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