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Application of 3, 4-dihydro-2H-benzo-[1, 4] oxazine drugs or salt of oxazine in preparing drugs for inhibiting iron death

A technology of ferroptosis and drugs, which is applied in the field of medicine, can solve the problems of short half-life and high toxicity, and achieve good therapeutic effect, high safety and definite effect

Pending Publication Date: 2019-11-19
SHANDONG NORMAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, these two compounds have the disadvantages of short half-life and high toxicity respectively.

Method used

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  • Application of 3, 4-dihydro-2H-benzo-[1, 4] oxazine drugs or salt of oxazine in preparing drugs for inhibiting iron death
  • Application of 3, 4-dihydro-2H-benzo-[1, 4] oxazine drugs or salt of oxazine in preparing drugs for inhibiting iron death
  • Application of 3, 4-dihydro-2H-benzo-[1, 4] oxazine drugs or salt of oxazine in preparing drugs for inhibiting iron death

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Example 1: Quantitative calculation of 3,4-dihydro-2H-benzo-[1,4]oxazines:

[0042] The study found that conjugation is beneficial to the antioxidant activity of amine-containing compounds. Therefore, the inventors purchased amine-containing compounds with different p-π* conjugates from a reagent company. The structure of the compound was optimized by Gaussian software, and the natural bonding orbital analysis of the optimized structure was carried out by NBO6.0W. The results showed that the oxygen lone pair electron had the strongest conjugation effect on the benzene ring, and its E(2) values ​​were 27.05 and 28.18, respectively. Kcal / mol; significantly higher than the E(2) value of sulfur (respectively 18.34 and 19.46Kcal / mol); and the C atom has no p-π* conjugation effect because it has no lone pair of electrons. Using Gaussian software to calculate the thermodynamic parameters of the reaction of these compounds with lipid free radicals, the results show that 3,4-dih...

Embodiment 2

[0047] Example 2: In vitro anti-ferroptosis activity test experiment and cytotoxicity experiment of the target compound

[0048] In vitro anti-ferroptosis activity test method:

[0049] Erastin was used to induce human fibroblastosarcoma cells HT-1080 to establish a cell ferroptosis model, and the inhibitory activity of the compound on cell ferroptosis was determined. Briefly, HT-1080 was treated with a lethal concentration of Erastin (10 [mu]M) in the presence of various concentrations of compounds (1-12). Cell viability was detected by MTT assay after continuing to culture for 48 hours. Each experiment was set up with six replicate wells at the same concentration and repeated three times independently. The effective concentration of the compound to inhibit ferroptosis (EC 50 ) was defined as the concentration at which cell viability was reduced by 50% compared to the control group. The activity results are shown in Table 3.

[0050] Cytotoxicity test method

[0051] HC...

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Abstract

The invention relates to application of 3, 4-dihydro-2H-benzo-[1, 4] oxazine or salt of the oxazine in preparing drugs for inhibiting iron death, especially to application of 3, 4-dihydro-2H-benzo-[1,4] oxazine compounds or salt of the oxazine in preparing drugs for treating diseases associated with iron death, and the diseases associated with iron death include brain trauma, stroke, cardiovascular diseases, liver and kidney failure, inflammation and neurodegenerative diseases such as Parkinson's disease and schizophrenia.

Description

technical field [0001] The invention belongs to the technical field of medicine. It specifically relates to the application of 3,4-dihydro-2H-benzo-[1,4]oxazines or salts thereof in the preparation of medicines for treating diseases related to ferroptosis, more specifically, 3, 4-dihydro-2H-benzo-[1,4]oxazine compound or its salt is used in the preparation of medicines for treating traumatic brain injury, stroke, cardiovascular, liver and kidney failure, inflammation and neurodegenerative diseases Applications. Background technique [0002] The information disclosed in this background section is only intended to increase the understanding of the general background of the present invention, and is not necessarily taken as an acknowledgment or any form of suggestion that the information constitutes the prior art already known to those skilled in the art. [0003] Ferroptosis is a recently discovered new programmed cell death that is different from apoptosis, necrosis and aut...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/538A61P25/18A61P25/16A61P25/28A61P9/10A61P9/00A61P1/16A61P13/12A61P29/00
CPCA61K31/538A61P25/18A61P25/16A61P25/28A61P9/10A61P9/00A61P1/16A61P13/12A61P29/00
Inventor 盛卸晃霍宝琪李文静曾嘉成
Owner SHANDONG NORMAL UNIV
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