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Application of aucubin or aglycone thereof to preparation of medicine for inhibiting ferroptosis

A technology of aucubinin and coral in peach leaf, applied in the field of use of traditional Chinese medicine extracts, can solve problems such as unclear molecular mechanism, and achieve the effect of enriching the basis of pharmacological action

Inactive Publication Date: 2020-11-03
PEOPLES HOSPITAL OF HENAN PROV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, whether ferroptosis can be inhibited and the molecular mechanism is still unclear

Method used

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  • Application of aucubin or aglycone thereof to preparation of medicine for inhibiting ferroptosis
  • Application of aucubin or aglycone thereof to preparation of medicine for inhibiting ferroptosis
  • Application of aucubin or aglycone thereof to preparation of medicine for inhibiting ferroptosis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Example 1: Effects of different concentrations of aucubin or its aglycones on the activity of HK-2 cells

[0043] 9000 HK-2 cells were inoculated in 96-well plates per well, and 6 replicate wells were set up for each group. The four weeks were filled with PBS buffer (200 μL per well) to prevent peripheral effects. Incubate in a 37°C, 5% CO2 incubator. After the cells adhered to the wall, discard the old medium, add new DMEM-F12 medium with different concentrations of aucubin or its aglycone (0, 0.1, 1, 10, 100 μM), 200 μL per well, and continue in the incubator Incubate for 48h. Discard the old culture medium after 48 hours, add DMEM-F12 medium (100 μL / well) without aucubin and CCK-8 reagent (10 μL / well), incubate in the incubator for 0.5 hour; The instrument detects the OD value of each well and calculates the cell viability.

[0044] Such as figure 1 As shown, within the experimental range, with the increase of the concentration of aucubin or its aglycon, the act...

Embodiment 2

[0045] Example 2: Effects of different concentrations of aucubin or its aglycones on ferroptosis induced by Erastin in HK-2 cells

[0046] 9000 HK-2 cells were inoculated in 96-well plates per well, and 6 replicate wells were set up for each group. The four weeks were filled with PBS buffer (200 μL per well) to prevent peripheral effects. Incubate in a 37°C, 5% CO2 incubator. Experiments are divided into the following groups:

[0047] Control: PBS, blank control group

[0048] Erastin: 5 μM Erastin

[0049] Fer-1: 5μM Erastin+0.5μM Fer-1

[0050] AU-L: 5μM Erastin+1μM AU (low dose)

[0051] AU-M: 5μM Erastin+10μM AU (medium dose)

[0052] AU-H: 5μM Erastin+100μM AU (high dose)

[0053] AG-L: 5μM Erastin+1μM AG (low dose)

[0054] AG-M: 5μM Erastin+10μM AG (medium dose)

[0055] AG-H: 5μM Erastin+100μM AG (high dose)

[0056] After adding the above drugs, continue to incubate in the incubator for 48h. After 48 hours, discard the old culture medium, add DMEM-F12 mediu...

Embodiment 3

[0058] Example 3: Effects of different concentrations of aucubin or its aglycones on ferroptosis induced by RSL-3 in HK-2 cells

[0059] 9000 HK-2 cells were inoculated in 96-well plates per well, and 6 replicate wells were set up for each group. The four weeks were filled with PBS buffer (200 μL per well) to prevent peripheral effects. Incubate in a 37°C, 5% CO2 incubator. Experiments are divided into the following groups:

[0060] Control: PBS, blank control group

[0061] RSL-3: 2 μM RSL-3

[0062] Fer-1: 5 μM RSL-3 + 0.5 μM Fer-1

[0063] AU-L: 2μM RSL-3+1μM AU (low dose)

[0064] AU-M: 2μM RSL-3+10μM AU (medium dose)

[0065] AU-H: 2μM RSL-3+100μM AU (high dose)

[0066] AG-L: 2μM RSL-3+1μM AG (low dose)

[0067] AG-M: 2μM RSL-3+10μM AG (medium dose)

[0068] AG-H: 2μM RSL-3+100μM AG (high dose)

[0069] After adding the above drugs, continue to incubate in the incubator for 48h. After 48 hours, discard the old culture medium, add DMEM-F12 medium (100 μL / well) ...

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Abstract

The invention discloses an application of aucubin or aglycone thereof to preparation of a medicine for inhibiting ferroptosis, belongs to the field of an application of traditional Chinese medicine extracts, and particularly provides an application of aucubin or aglycone thereof to preparation of the medicine for inhibiting ferroptosis. The invention relates to an application of aucubin, in particular to an application of aucubin or aglycone thereof to preparation of the medicine for preventing or treating diseases related to ferroptosis. The inhibition effect and the molecular mechanism of the aucubin or the aglycone thereof on ferroptosis are disclosed for the first time, the pharmacological action basis of the aucubin or the aglycone thereof is enriched, and a new way is provided for prevention or treatment of diseases related to ferroptosis.

Description

technical field [0001] The invention belongs to the field of use of traditional Chinese medicine extracts, and specifically relates to the application of aucubin or its aglycone in the preparation of ferroptosis-inhibiting drugs, and more specifically relates to the application of aucubin or its aglycone in the preparation of prevention or treatment of ferroptosis-related diseases application in medicines. Background technique [0002] Ferroptosis is a brand-new iron-dependent cell death method discovered by Professor Stockwell, a well-known scholar at Columbia University, in 2012. It is completely different from cell death methods such as apoptosis, necrosis, autophagy, and mitotic catastrophe. In terms of molecular mechanism, the essence of ferroptosis is the metabolic disorder of intracellular lipid peroxide, that is, due to the depletion of glutathione (GSH), the membrane lipid repair enzyme glutathione peroxidase (Glutathione Peroxidase 4, GPX4 ) activity decreases, li...

Claims

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Application Information

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IPC IPC(8): A61K31/7048A61K31/352A61P3/00A61P25/00A61P25/28A61P25/16A61P25/14A61P1/16A61P13/12A61P11/00A61P9/00A61P9/10A61P39/02
CPCA61K31/352A61K31/7048A61P1/16A61P3/00A61P9/00A61P9/10A61P11/00A61P13/12A61P25/00A61P25/14A61P25/16A61P25/28A61P39/02
Inventor 冯晗马培志张伟方凤琴赵飞秦艳闫静静刘凯莉王晓博
Owner PEOPLES HOSPITAL OF HENAN PROV
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