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A kind of dichalcone compound and its preparation method and application

A bis-chalcone and compound technology, applied in the field of extraction and separation of traditional Chinese medicine, can solve the problems of complex chemical composition of licorice and difficulty in finding active compounds in licorice, and achieve the effect of good prospects, novel structure and clear method objectives

Active Publication Date: 2022-02-11
DALIAN INST OF CHEM PHYSICS CHINESE ACAD OF SCI
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, due to the extremely complex chemical composition of licorice, which contains hundreds of compounds, it has brought great difficulties to the search for active compounds in licorice. Therefore, how to quickly and accurately separate and identify active compounds has been continuously explored by scholars at home and abroad in recent years. hot issues

Method used

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  • A kind of dichalcone compound and its preparation method and application
  • A kind of dichalcone compound and its preparation method and application
  • A kind of dichalcone compound and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Example 1: Preparation of Compound 6 and Compound 15

[0039]Take 10kg of dried rhizomes of licorice, crush and add methanol with a volume fraction of 50% for reflux extraction for 3 times, two hours each time, and the amount of each extraction solvent is 10, 8, and 6 times the amount of the medicinal material, and the extracts are combined and recovered under reduced pressure. The solvent was evaporated to dryness to obtain the extract, and the extract was re-dissolved in methanol with a volume fraction of 50% to obtain an extraction concentrate; n-heptane was added to extract 3 times by 2 times the volume of the extraction concentrate, and after the organic solvent layers were combined, Concentrated to dryness under reduced pressure to obtain n-heptane extract; the n-heptane extract was separated by normal phase silica gel column chromatography, and eluted with a gradient of dichloromethane: methanol in a volume ratio of 50:1-1:1, The fractions eluted at a ratio of 20...

Embodiment 2

[0050] Example 2: Activity Screening Experiment

[0051] Compound 6 and compound 15 were mixed with human carboxylesterase 2 respectively, incubated at 37°C with shaking for 20 min, and the probe substrate was added to initiate the reaction. After shaking at 37°C for 40 min, an equal volume of acetonitrile was added, and the reaction was terminated after vigorous shaking. The 96-well plate was placed on a fluorescence microplate reader for fluorescence detection (Ex=308nm, Em=392, 528nm), and the fluorescence intensity was calculated. The fluorescence intensity ratio of DMSO group was used to calculate the inhibition intensity of human carboxylesterase 2 ( Figure 5 ).

[0052] Both compound 6 and compound 15 showed strong inhibitory activity against human carboxylesterase 2 (residual activity <20%), and had good application prospects in adjuvant cancer therapy.

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Abstract

The invention provides a class of compounds with a bis-chalcone structure and a preparation method and use thereof. This type of compound has the effect of inhibiting the activity of human carboxylesterase 2, and can be used as an adjuvant drug for the first-line anticancer drug irinotecan, reducing the conversion of irinotecan to SN-38 under the action of human carboxylesterase 2, thereby Alleviate severe adverse reactions such as diarrhea in cancer patients caused by SN‑38.

Description

technical field [0001] The invention belongs to the field of extraction and separation of traditional Chinese medicines, and relates to a class of bischalcone compounds and a preparation method thereof, as well as the application of such compounds as human carboxylesterase 2 inhibitors in assisting irinotecan in anticancer treatment. Background technique [0002] Irinotecan hydrochloride is a first-line drug for the treatment of metastatic colorectal cancer, small cell lung cancer and other solid tumors, but it was found in the process of clinical use that it can cause serious adverse reactions - neutropenia and delayed diarrhea . At present, the diarrhea caused by CPT-11 is generally relieved by taking imontin (loperamide hydrochloride, loperamide) in clinical practice, but because loperamide can also act on opioid receptors, overdose may cause intestinal obstruction, Drowsiness, constipation, muscle tension, mydriasis, slow breathing and other peripheral and central nervo...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C49/84C07C45/78C07C45/79C07C45/80A61K31/12A61P35/00A61P1/12
CPCC07C49/84C07C45/78C07C45/79C07C45/80A61P35/00A61P1/12Y02P20/55
Inventor 梁鑫淼余文怡刘艳芳沈爱金金红利韩阳
Owner DALIAN INST OF CHEM PHYSICS CHINESE ACAD OF SCI
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