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Norcantharidin derivative and activity testing method and application thereof

A technology for norcantharidin and derivatives, which is applied in biochemical equipment and methods, microbial determination/inspection, organic active ingredients, etc., can solve the problems of unsatisfactory pharmacological test results, loss of inhibitory effect, etc., and achieve good anti-tumor effects. active effect

Inactive Publication Date: 2010-10-20
SHAOXING UNIVERSITY
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  • Abstract
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  • Claims
  • Application Information

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Problems solved by technology

There can also be a double bond between 5-C and 6-C; the 7-oxygen bridge is indispensable, which may be due to the formation of hydrogen bonds between the oxygen atom and PP1 and PP2A; 2) the reduction of the anhydride on the anhydride ring will Loss of inhibition of PP1 and PP2A
[0004] The modification of cantharidin structure 5-C or 6-C generally only introduces substituents, but the results of pharmacological tests are not ideal

Method used

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  • Norcantharidin derivative and activity testing method and application thereof
  • Norcantharidin derivative and activity testing method and application thereof
  • Norcantharidin derivative and activity testing method and application thereof

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Embodiment 1

[0047] Example 1: The effect of the 32 compounds on the activity of human lung adenocarcinoma cell A549 was analyzed by cell counting kit-8.

[0048] (1) The cultured A549 cells were digested with trypsin and then centrifuged, resuspended with new medium, and then planted 300 A549 cells with a volume of 50ul in each well of a 384-well plate with a liquid dispenser mutidrop;

[0049] (2) At 37°C, 5% CO 2 After culturing under the condition for 24 hours, the automatic liquid handling system Bravo was used to dispense drugs for stimulation. The treatment concentrations of various compounds were: 16uM 8uM 4uM 2uM 1uM 0.5uM 0.25uM 0.125uM, and each treatment had four repetitions;

[0050] (3) After 48 hours, use the CCK-8 kit to detect the activity of the cells: add 5ul of CCK-8 solution to each well, and use a microplate reader to read the absorption value of each well at a wavelength of 450nm; continue in the cell culture incubator Incubate for 100 min, and read the absorbance a...

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Abstract

The invention discloses a norcantharidin derivative and an activity testing method and an application thereof and relates to the field of cantharidin derivatives. The norcantharidin derivative has two kinds, one is a norcantharidin dimer derivative, and the other is a heterocyclic substituted norcantharidin derivative. Cell counting kit-8 is used to analyze the influence of the compound on the activity of human lung adenocarcinoma cells A549. The norcantharidin derivative has good anti-tumor activity.

Description

Technical field: [0001] The invention belongs to the field of cantharidin derivatives, and more specifically relates to a norcantharidin dimer derivative, a heterocyclic substituted norcantharidin derivative and a synthesis method and application thereof. Background technique: [0002] Cantharidin (cantharidin) is a folk medicine in my country, and it is an active ingredient of a drug for treating malignant tumors. Modern studies have proved that it has a certain curative effect on primary liver cancer, and has the advantages of increasing white blood cells and not suppressing the immune system. Therefore, it has high medicinal research value and has attracted widespread attention. But the toxicity of cantharidin is bigger, and synthesis is very complicated, recent research shows, in norcantharidin (norcantharidin), two methyl groups of 2 and 3 positions are missing, and norcantharidin not only keeps strong antitumor activity and The unique effect of increasing white blood ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D519/00C07D498/22C07D491/22C12Q1/02G01N21/31A61K31/424A61K31/4162A61K31/427A61P35/00
Inventor 邓莉平
Owner SHAOXING UNIVERSITY
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