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Novel dimeric alkaloid as well as preparation and application thereof

A dimerized, alkaloid technology, applied in the field of alkaloids, can solve the problems of interfering with normal physiological functions, affecting gene expression and regulation, etc.

Active Publication Date: 2022-04-12
SHANGHAI UNIV OF ENG SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, studies have shown that most anti-tumor drugs target DNA in vivo and directly act on DNA, interfering with its normal physiological functions, thereby affecting gene expression and regulation, and achieving the effect of inhibiting or killing tumor cells

Method used

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  • Novel dimeric alkaloid as well as preparation and application thereof
  • Novel dimeric alkaloid as well as preparation and application thereof
  • Novel dimeric alkaloid as well as preparation and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Embodiment 1: Extraction and separation of novel alkaloids

[0033] 1.1 Experimental medicinal materials:

[0034] Bitter bean fruit was provided by Zhengzhou Zhongguan Jianye Biotechnology Co., Ltd.

[0035] 1.2 Extraction and separation of new alkaloids from the seeds of Sophora aphorae:

[0036] Get 50Kg of bitter bean seeds and grind into powder for subsequent use. Use 75% ethanol as the solvent to heat and reflux at 85°C for three times, each time for 2.5 hours, the ratio of solid to liquid is 1:10, and combine and concentrate the filtrate to obtain the medicinal solution for later use.

[0037] Dissolve the extracted medicinal liquid with as little water as possible, adjust the pH to 10.5 with sodium hydroxide solution, and the volume ratio of the aqueous solution dissolved in chloroform and medicinal liquid is 1:1, place it in a separatory funnel, shake it, and let it stand until the layers are separated Clear, the chloroform part is in the lower layer, take t...

Embodiment 2

[0041] Example 2: Investigate the structural identification and analysis of new alkaloid compounds

[0042] The novel alkaloid compound that above-mentioned embodiment 1 obtains carries out structural test analysis, obtains following test data:

[0043] Formula I compound: C 26 h 38 N 4 o 3 It is light yellow amorphous powder, slightly soluble in DMSO. HR-ESI-MS (m / z439.3058[M+H] + , calculated value 439.3073). Through HSQC and HMBC spectrum, combined with 1 H NMR and 13The information given by the C NMR spectrum assigns the hydrocarbon information of the above-mentioned new compounds, as shown in Table 1. In the HMBC spectrum, δ H 7.39(H-4') and δ C 151.6(C-6'), δ C 162.1 (C-2') correlation, δ H 6.22(H-3') and δ C 104.0(C-5’) related, δ H 5.76(H-5') and δ C 34.1(C-7'), δ C 115.1(C-3'), δ C 151.6 (C-6') correlation, δ H 3.76(H-10') and δ C 25.6(C-8'), δ C 27.3(C-9'), δ C 57.6 (C-11') correlation, δ H 2.68(H-2) and δ C 57.6 (C-11') correlatio...

Embodiment 3

[0053] Embodiment 3: the inhibition Topo I activity experiment of novel alkaloid compound

[0054] 3.1 Experimental materials:

[0055] The new alkaloids used in the experiment were prepared by the method of the above-mentioned Example 1, weighed accurately, dissolved and diluted with DMSO to a concentration of 1 mM. EDTA (Shanghai Adamas Reagent Co., Ltd.); EB (Sigma-Aldrich Trading Co., Ltd.); Agarose (Shanghai Adamas Reagent Co., Ltd.); pBR322DNA (Baoric Medical Biotechnology Co., Ltd.); DNA topoisomerase I (Baoriyi Biotechnology Co., Ltd.); DNA Loading Buffer (6×) (Shanghai Biyuntian Biotechnology Co., Ltd.).

[0056] 3.2 Experimental method:

[0057] (1) Preparation of 1% agarose gel:

[0058] Accurately weigh 0.5g of agarose powder, dissolve it with 50mL of 1×TAE buffer at high temperature, cool to 60°C and pour it into the horizontal tank of gel electrophoresis.

[0059] (2) Preparation of 1×Topo I Buffer:

[0060] Pipette 10 μL of 10×Topo I Buffer and dilute with ...

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Abstract

The invention relates to a novel dimeric alkaloid and preparation and application thereof, the chemical structural formula of the novel dimeric alkaloid is shown in the specification, the alkaloid is a cytisine type dimeric alkaloid newly found in sophora alopecuroides, and the activity of Topo I can be obviously inhibited; the natural topoisomerase inhibitor with high selectivity can be designed and developed into a novel anti-tumor drug, and has a wide application prospect in the field of research and development of new drugs.

Description

technical field [0001] The invention belongs to the technical field of alkaloids, and relates to a novel dimer alkaloid and its preparation and application. Background technique [0002] Tumor has always been a disease that plagues the world, as determined by the statistical report of the International Agency for Research on Cancer (GLOBOCAN), its morbidity and mortality remain high. Currently common treatments include chemotherapy, radiotherapy, immunotherapy, etc. However, there are problems such as side effects and drug resistance in clinical practice. Therefore, when developing new anti-tumor drugs, it is more inclined to use small molecules targeting different biological targets Drugs to help research about cell proliferation. In addition, the sources of most antineoplastic drugs are directly or indirectly related to natural medicinal plants. [0003] Bitter bean is a plant with high medicinal value, which has been continuously studied by scholars in the past ten year...

Claims

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Application Information

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IPC IPC(8): C07D519/00A61P35/00
Inventor 尹小英孟陈婷
Owner SHANGHAI UNIV OF ENG SCI
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