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Method for preparing marine organism alkali CDK2 inhibitor and application of marine organism alkali CDK2 inhibitor

A technology of marine alkaloids and inhibitors, which is applied in drug combinations, organic chemistry, antineoplastic drugs, etc., can solve problems such as poor specificity, large side effects, and limitations of its own physical and chemical properties, and achieve simple structure, easy implementation, and significant inhibition active effect

Inactive Publication Date: 2021-03-16
滨州医学院附属医院
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  • Description
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Problems solved by technology

In view of the close correlation and critical importance of CDK2 and the development of tumor cells, using CDK2 as an anticancer target has become a hot spot in the development of anticancer drugs. At present, about a hundred kinds of CDK2 inhibitors have been synthesized one after another, but due to poor specificity , large side effects, and limitations of its own physical and chemical properties, so far there is no CDK2 inhibitor that has been really used in clinical practice

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  • Method for preparing marine organism alkali CDK2 inhibitor and application of marine organism alkali CDK2 inhibitor
  • Method for preparing marine organism alkali CDK2 inhibitor and application of marine organism alkali CDK2 inhibitor
  • Method for preparing marine organism alkali CDK2 inhibitor and application of marine organism alkali CDK2 inhibitor

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Embodiment

[0034] refer to figure 1 As shown, the method for preparing marine alkaloid CDK2 inhibitors described in this embodiment comprises the following steps:

[0035] 1. Raw material processing: the sponge Aaptos suberitoides was collected from the waters of Yongxing Island in Xisha in 2012, and it was stored at -20°C; At room temperature, it was extracted by dynamic cold immersion with methanol 3 times, soaked for 5 days each time; the 3 extracts were combined and concentrated under reduced pressure at 40°C; then, dissolved and desalted with anhydrous methanol 3 times to obtain 162.5g of extract .

[0036] 2. Silica gel column chromatography: Dissolve the extract in 1.5-3 times the weight of pure methanol, then mix the sample with 100-200 mesh silica gel 1-3 times the weight of the extract, and then apply it to the silica gel column (the specification of the filler silica gel is 200 -300 mesh or 300-400 mesh); and then respectively use petroleum ether and acetone in a volume rati...

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Abstract

The invention relates to the technical field of marine organisms and medicines, in particular to a method for preparing a marine organism alkali CDK2 inhibitor and an application of the marine organism alkali CDK2 inhibitor. The method comprises the following steps of: crushing a frozen sponge Aaptos suberitoides sample by using a crusher, and dynamically carrying out cold-soaking and extracting for three times by using methanol at room temperature for 5 days each time; combining the three extracting solutions, and carrying out concentrating under reduced pressure at the temperature of 40 DEGC; then, using absolute methanol to carry out dissolution and desalination for three times, and preparing extract; obtaining the compounds A, B and C through silica gel column chromatography, ODS column chromatography and high performance liquid chromatography separation, wherein the prepared compounds A, B and C have remarkable inhibitory activity on CDK2 kinase, mitosis of tumor cells is prevented by inhibiting the activity of the CDK2 kinase, and the anti-tumor effect is further achieved. Meanwhile, the alkaloid is simple in structure and easy to achieve artificial synthesis, can be used asa novel CDK2 kinase inhibitor, and has important guiding significance for developing CDK2 inhibitor antitumor drugs.

Description

technical field [0001] The invention relates to the technical fields of marine biology and medicine, in particular to a method and application for separating and preparing marine alkaloid CDK2 inhibitors from marine sponge Aaptossuberitoides. Background technique [0002] Tumor is a global problem that endangers human life and health. It has shown a gradual upward trend in the world in recent years. It is estimated that in the next 20 years, new cancer cases will reach 22 million each year, and the number of cancer deaths will rise to 13 million during the same period. Effective research and development Anticancer drugs are still the top priority in tumor treatment. The fundamental feature of tumors is the infinite proliferation of cells, which is due to the disorder of cell cycle regulation. Through the intervention of cell cycle regulation, limiting the infinite proliferation of tumor cells is one of the important means of treating tumors. The main regulator of the cell c...

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D471/06A61P35/00
CPCC07D471/06A61P35/00
Inventor 宫凯凯贺倩倩苗双满玉清
Owner 滨州医学院附属医院
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