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Application of homoplantaginin and derivatives of homoplantaginin as Nrf-2 activators

A technology of homopsyllogenin and derivatives, which is applied in the preparation of sugar derivatives, sugar derivatives, sugar derivatives, etc., to achieve the effect of anti-oxidation and protection of endothelial cells and endothelial cell damage

Pending Publication Date: 2020-02-14
UNIV OF JINAN
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is no report on the regulation of Nrf2 activity by homopsyllogen and its derivatives.

Method used

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  • Application of homoplantaginin and derivatives of homoplantaginin as Nrf-2 activators
  • Application of homoplantaginin and derivatives of homoplantaginin as Nrf-2 activators
  • Application of homoplantaginin and derivatives of homoplantaginin as Nrf-2 activators

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Example 1: Preparation of Homopsyllogen and Its Derivatives

[0051] The specific operation is as follows:

[0052] 1) Pulverize the raw material of lychee grass, add 10 times the amount of 95% ethanol solution, heat and reflux for extraction twice, each time for 4 hours, combine the extracts, recover ethanol under reduced pressure, and obtain a concentrated solution;

[0053] 2) Extraction and column separation: use ethyl acetate / n-butanol-water as a two-phase solvent system, take the upper layer as the acetyl acetate / n-butanol phase, and the lower layer as the water phase, take the upper layer acetyl acetate / n-butanol phase and concentrate it into For the extract, dilute and filter the above-mentioned concentrated solution with an appropriate amount of water, put it on a macroporous resin column, elute with 30%, 50%, 85%, and 95% ethanol aqueous solution, monitor by thin layer, collect high psyllogenin fractions, concentrate and wash Dehydration;

[0054] 3) Impurit...

Embodiment 2

[0056] Example 2: High psyllogen activates Nrf2

[0057] 1. Experimental method

[0058] Inoculate the endothelial cells in a 96-well culture dish, and when the cell tiled area reaches 80%, set up the control group: culture under normal conditions without serum; experimental group: add concentrations of 0.1 μM and 1 μM under serum-free conditions, respectively. and 10 μM homopsyllogenin S3 and its derivative S1, cultured for 24 hours, fixed with 10% TCA for one hour, rinsed with deionized water for 5 times, and dried naturally, added 50 μL of SRB dye to each well, and shaken to mix After homogenizing for 10 min, rinse with deionized water for 5 times, and after drying naturally, add 100 μL Trisbase to each well to dissolve, and measure the absorbance at 540 nm with a microplate reader. Luci-hela cells (purchased and ATCC) were planted in 96-well plates, and after the cell tiled area reached 80%, set up the control group: culture under normal conditions without serum; experime...

Embodiment 3

[0062] Example 3: Homopsyllogen and its derivatives can activate Nrf2 downstream antioxidant protein HO-1

[0063] 1. Experimental method

[0064] Endothelial cells were inoculated in a culture dish with a diameter of 6 cm. Normal group: under normal conditions without serum, low-density lipoprotein (LDL) was added for culture; control group: under normal conditions without serum, oxidized low-density lipoprotein (ox -LDL) culture; experimental group: cultured with S1 and S3 at concentrations of 0.1 μM, 1 μM and 10 μM respectively under the condition of removing serum. 37°C, CO 2 After culturing in the incubator for 6 hours, the cells were lysed, the cell lysate was collected, centrifuged at 12,000 g at 4°C for 15 min, the supernatant was taken, and the expression level of HO-1 in endothelial cells was detected by western blot.

[0065] 2. Experimental results

[0066] Experimental results such as image 3 As shown, the results showed that: compared with the ox-LDL group o...

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Abstract

The invention relates to the technical field of medicinal use of homoplantaginin and derivatives of homoplantaginin, and specifically discloses application of homoplantaginin and derivatives of homoplantaginin as Nrf-2 activators. It is found through researches that apoptosis, caused by oxidized low-density lipoprotein, of endothelial cells can be inhibited effectively by homoplantaginin and derivatives of homoplantaginin, and effects of oxidation resistance and protection of the endothelial cells are achieved through activation of Nrf2. Theoretical and experimental bases are provided for researches about that prevention of damage to the endothelial cells is achieved through adoption of homoplantaginin and derivatives of homoplantaginin as the activators of Nrf2.

Description

technical field [0001] The invention relates to the technical field of medical applications of homopsyllogenin and its derivatives, and specifically relates to the application of homopsyllogenin and its derivatives as Nrf-2 activators in the preparation of drugs for treating diseases related to Nrf2 signaling pathways. Background technique [0002] The transcription factor Nrf2 belongs to CNC-Bzip (capncollar subfamily of basic leucine-zipper), which is the family of CNC leucine zipper transcription activators. central regulator. By inducing and regulating the constitutive and inducible expression of a series of antioxidant proteins, Nrf2 can reduce the cell damage caused by reactive oxygen species and electrophiles, keep the cells in a stable state, and maintain the body's redox dynamic balance. important access. A large number of studies have shown that Nrf2 is related to the occurrence of various diseases such as inflammation, chronic kidney disease, diabetes, cardiovas...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7048A61P39/06A61P43/00C07H1/08C07H17/07
CPCA61K31/7048A61P39/06A61P43/00C07H1/08C07H17/07
Inventor 孟宁王艳红杨凤英张华欧阳晨曦
Owner UNIV OF JINAN
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