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Isopentenyl substituted coumarin compound and preparation method and application thereof

A technology of coumarin and isopentenyl, applied in the application of antitumor drugs, the field of preparation of isopentenyl substituted coumarin compounds, can solve the problem of rare chemical components and pharmacological activities of jackfruit fruit

Pending Publication Date: 2021-09-07
HAINAN NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So far, there are few research reports on the chemical constituents and pharmacological activities of jackfruit fruit

Method used

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  • Isopentenyl substituted coumarin compound and preparation method and application thereof
  • Isopentenyl substituted coumarin compound and preparation method and application thereof
  • Isopentenyl substituted coumarin compound and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Embodiment one: the preparation method of compound artoheteronin

[0021] A. The dried Jackfruit pulp (10.7kg, Hainan) was pulverized and extracted four times by cold soaking with 75% ethanol solution, each time for one week, filtered, and the filtrate was collected and concentrated under reduced pressure to obtain the ethanol extract;

[0022] B. The ethanol extract was added with distilled water to make a suspension, which was sequentially extracted with petroleum ether and ethyl acetate, and the petroleum ether extract was concentrated under reduced pressure to obtain 518.8 g of petroleum ether extract;

[0023] C. Purify the petroleum ether extract by column chromatography:

[0024] (1) The petroleum ether extraction extract was separated by silica gel column chromatography, and gradient elution was carried out with petroleum ether-ethyl acetate (volume ratios of 83:17, 68:32 and 55:45) as the eluent, and collected Petroleum ether-ethyl acetate (volume ratio 68:32)...

Embodiment 2

[0030] Embodiment two: the preparation method of compound artoheteronin

[0031] A. The dried jackfruit pulp (100.8kg, Hainan) was pulverized and then extracted four times by cold immersion in methanol, each time for one week, filtered, the filtrate was collected, and concentrated under reduced pressure to obtain a methanol extract;

[0032] B. The methanol extract was added with distilled water to make a suspension, which was sequentially extracted with petroleum ether and ethyl acetate, and the petroleum ether extract was concentrated under reduced pressure to obtain 5218.7 g of petroleum ether extract;

[0033] C. Purify the petroleum ether extract by column chromatography:

[0034] (1) Use silica gel column chromatography to separate the extract from petroleum ether, use petroleum ether-ethyl acetate (83:17, 68:32 and 55:45 by volume) as the eluent for gradient elution, and collect petroleum Ether-ethyl acetate (volume ratio 68:32) eluate;

[0035] (2) Take petroleum eth...

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Abstract

The invention relates to the field of natural medicines, and discloses an isopentenyl-substituted coumarin compound which is derived from artocarpus heterophyllus and has a novel chemical structure, a preparation method of the isopentenyl-substituted coumarin compound and application of the isopentenyl-substituted coumarin compound in anti-tumor medicines, and various in-vitro anti-tumor activity evaluation results of the compound artoheterronin show that the compound has remarkable anti-tumor activity, has the protein tyrosine kinase inhibition activity equivalent to that of a positive control drug, can be further developed into an anti-tumor drug taking protein tyrosine kinase as a target, can be applied to the anti-tumor drug, is simple in separation and purification process and mild in reaction condition, and has practical significance.

Description

technical field [0001] The invention belongs to the field of natural medicines, and in particular relates to a preparation method of an isopentenyl-substituted coumarin compound derived from jackfruit and having a novel chemical structure and its application in antitumor drugs. Background technique [0002] Malignant tumor is a frequently-occurring disease with a high mortality rate. It is currently seriously threatening human life and health, and is gradually becoming the number one killer of human life and health. The treatment of malignant tumors in modern medicine mainly includes surgical treatment, chemical drug therapy, radiotherapy and biological therapy, with chemical drug therapy as the main treatment. Even if surgical treatment is adopted, it is often necessary to routinely use chemical drugs for adjuvant treatment after surgery . With the rapid development of life sciences, the mechanism of malignant tumors has been elucidated, and new anti-tumor targets have bee...

Claims

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Application Information

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IPC IPC(8): C07D311/16A61K36/60A61P35/00
CPCC07D311/16A61K36/60A61P35/00
Inventor 刘艳萍付艳辉于绡梅乔泽华李娟唐浩轩
Owner HAINAN NORMAL UNIVERSITY
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