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Tripterine derivative and application thereof in tumor resistance

A technology for triptolide and derivatives, which is applied in the field of biomedicine, can solve the problems of low water solubility, high myocardial toxicity, influence on application, etc., and achieves broad application prospects and the effect of reducing cytotoxicity

Active Publication Date: 2022-04-26
NINGXIA MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although tripteryglide has significant pharmacological activity, its low water solubility, high myocardial toxicity and strong killing effect on normal cells have seriously affected its clinical application.

Method used

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  • Tripterine derivative and application thereof in tumor resistance
  • Tripterine derivative and application thereof in tumor resistance
  • Tripterine derivative and application thereof in tumor resistance

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] This example shows the application of Phomopsis LGT-5 to transform tripterine, and the tripterine derivative (compound 1) shown in formula (I) was obtained after separation and identification.

[0037] 1) Biological preparation

[0038] Phomopsis LGT-5 was inoculated into a Erlenmeyer flask containing 150 mL of modified Martin liquid medium, and cultured with shaking at 28°C and 180 rpm until it reached the logarithmic growth phase (usually the culture time was 1 day), at which point Phomopsis LGT The concentration of -5 is about 5g dry weight / L culture system. The dry weight measurement method used in this example is as follows: sampling the culture system, collecting the bacteria by centrifugation, washing thoroughly with sterile water, and then drying to dry weight. The formula of the improved Martin's liquid medium (pH 6.2-6.6) described in this example is: 5 g of peptone, 1 g of dipotassium hydrogen phosphate, 0.5 g of magnesium sulfate, 2 g of yeast extract powde...

Embodiment 2

[0055] In this example, a cytotoxicity test was carried out to measure the antitumor activity of Compound 1, and the results of the determination are shown in Figure 9-Figure 13 .

[0056] Test agent: Celastrol (tripterine), compound 1 prepared in Example 1.

[0057] Test cells: U251 cells, A549 cells, KG-1 cells, B16 cells; BV-2 cells; H9c2 cells; PC12 cells.

[0058] Preparation of the test agent solution: Dissolve the test agent in DMSO to obtain a solution with a concentration of 50mmol / mL, then dilute it with complete medium to obtain the test agent with a concentration of 8μmol / L, 5μmol / L, 2μmol / L or 1μmol / L. Test the test drug solution. The complete medium consists of 9 volume parts of DMEM medium and 1 volume part of fetal calf serum.

[0059] Culture conditions: 37°C, 5% CO2.

[0060] experiment procedure:

[0061] 1) Take a 96-well plate and add 100 μL of the cell suspension (containing 5×10 3 cells to be tested), cultivated for 24 hours, and discarded the sup...

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Abstract

The invention provides a tripterine derivative which is obtained by carrying out biotransformation and separation on tripterine by adopting phomopsis (the preservation registration number is CGMCC (China General Microbiological Culture Collection Center) NO.16088). Compared with the tripterine, the antitumor activity of the tripterine derivative has no significant difference, but the cytotoxicity is greatly reduced. The tripterine derivative disclosed by the invention has the potential of being prepared into a novel anti-tumor drug, and a wide application prospect is provided for preparing the tripterine derivative by utilizing a biotechnology on a large scale.

Description

technical field [0001] The invention belongs to the technical field of biomedicine and relates to the preparation and activity detection of tripterygne derivatives, in particular to the preparation of tripteryne derivatives and their antitumor activity by adopting a biotransformation method. Background technique [0002] Tripterygium wilfordii has antibacterial, anti-inflammatory, and tumor cell-inhibiting effects. The active ingredient in tripterygium wilfordii is Celastrol (CSL). Those of ordinary skill in the art can refer to patents CN111848722A, CN103642887B and related technical documents for understanding of the pharmacological activity of tripterine. This patent no longer elaborates on this. Although tripterine has significant pharmacological activity, its low water solubility, high myocardial toxicity and strong killing effect on normal cells have seriously affected its clinical application. Therefore, improving or retaining the pharmacological activity of tripter...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J63/00A61K31/56A61P35/00
CPCC07J63/008A61P35/00
Inventor 吴秀丽杨慧江雨涵王建寰刘成
Owner NINGXIA MEDICAL UNIV
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