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Indole alkaloid compound as well as preparation method, pharmaceutical composition and application thereof

A technology of indole alkaloids and compositions, which is applied in the direction of drug combinations, organic chemistry, antineoplastic drugs, etc., can solve the problems of no relevant activity and no indole alkaloids, and achieve simple operation, low cost, and low cost of raw materials Effects from a wide range of sources

Active Publication Date: 2022-04-05
KUNMING INST OF BOTANY - CHINESE ACAD OF SCI +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, there is no report of the indole alkaloid shown in the formula (I) in the prior art, nor is there any report of its related activity

Method used

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  • Indole alkaloid compound as well as preparation method, pharmaceutical composition and application thereof
  • Indole alkaloid compound as well as preparation method, pharmaceutical composition and application thereof
  • Indole alkaloid compound as well as preparation method, pharmaceutical composition and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] 1.2 kg of dried seeds of Kopsia arborea, heated and refluxed with methanol to extract three times, each time for 3 hours, combined the extracts, recovered methanol under reduced pressure, kneaded the concentrated extract with 10% hydrochloric acid aqueous solution and adjusted the pH value 2 to 3, extract three times with petroleum ether, then adjust the pH value to 9 to 10 with 10% NaOH solution, and use CH 2 Cl 2 Extraction obtains total base part 154g, total base part utilizes silica gel column chromatography, petroleum ether-acetone gradient elution obtains five parts (Fr.A-E), Fr C (38g) utilizes silica gel column chromatography, petroleum ether / acetone (10: 1→5:1, v / v), reverse phase chromatography C-18 (acetonitrile / water, 30:70→80:20) and SephadexLH-20 (methanol) separate and obtain the indole alkaloid 1 of structure shown in formula II (6.5mg, yield 0.004%, purity 98%, colorless crystals), 2 (12mg, yield 0.008%, purity 98%, pale yellow oil) and 3 (8.7mg, yield...

Embodiment 2

[0071] Mix the indole alkaloid prepared in Example 1 and water for injection evenly, perform fine filtration, potting and sterilization in sequence to obtain the indole alkaloid injection.

Embodiment 3

[0073] Preparation of medically acceptable salts of indole alkaloids:

[0074] The indole alkaloids prepared in Example 1 are respectively reacted with tartaric acid, citric acid, formic acid, acetic acid, oxalic acid, hydrochloric acid, hydrobromic acid, nitric acid, sulfuric acid with a mass concentration of 4%, to obtain the tartaric acid of indole alkaloids respectively Salt, citrate, formate of indole alkaloid, acetate of indole alkaloid, oxalate of indole alkaloid, hydrochloride of indole alkaloid, hydrogen bromide of indole alkaloid Salts of indole alkaloids, nitrates of indole alkaloids, sulfates of indole alkaloids.

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Abstract

The invention provides indole alkaloid as well as a preparation method, a pharmaceutical composition and application thereof, and belongs to the technical field of medicines. The indole alkaloid or the pharmaceutically acceptable salt thereof provided by the invention has relatively remarkable inhibitory activity on CDK kinases (CDK4 / 6 and CDK5), and is a candidate drug which has development potential and can be used for treating various diseases (tumors and neurodegenerative diseases) related to cyclin-dependent kinases. The compound and the pharmaceutical composition thereof can be used for preparing medicines for treating various diseases related to cyclin-dependent kinases, medicines for treating breast cancer, non-small cell lung cancer, liver cancer, intestinal cancer and pancreatic cancer, medicines for treating neurodegenerative diseases, medicines for treating AD, PD, Huntington's disease and amyotrophic lateral sclerosis, medicines for treating acute myopathy and acute myopathy, medicines for treating acute myopathy and acute myopathy, medicines for treating acute myopathy and acute myopathy, and medicines for treating acute myopathy and acute myopathy. And preparing a CDK kinase inhibitor.

Description

Technical field: [0001] The invention relates to the technical field of medicines, in particular to an indole alkaloid or a pharmaceutically acceptable salt thereof, a preparation method and application thereof, an indole alkaloid pharmaceutical composition and an application thereof. Background technique: [0002] Cyclin-dependent kinases (CDKs) are a class of serine / threonine kinases, which are important signal transduction molecules in cells and participate in cell growth, proliferation, and apoptosis. The dysregulation of CDKs can lead to the occurrence of various diseases (tumors, neurodegenerative diseases, etc.), therefore, CDKs have become effective and important targets in drug development. Among them, CDK4 / 6 is the key protein kinase for the occurrence and development of most malignant tumors. Its inhibitors can inhibit the continuous proliferation of tumor cells by inhibiting the transition of the cell cycle from G1 phase to S phase. In addition, CDK5, another me...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D519/00A61P35/00A61P25/28A61P25/16A61P25/14A61P21/00A61P25/00A61K31/475
CPCY02A50/30
Inventor 张于罗荣灿郝小江姚永刚
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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