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Phenylacetyltetrahydro-beta-carboline small molecule compound and application thereof

A technology based on phenylacetyl and carbolines, which is applied in the field of biomedical chemistry and can solve problems such as loss of efficacy

Inactive Publication Date: 2019-07-19
EAST CHINA NORMAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] Invention patent (CN 103223175 A) discloses an anti-scarring and tissue fibrosis oligo-double-stranded nucleotide drug, but the oligo-double-stranded nucleotide is easily degraded by nucleases in the body when used in the human body, thus losing its effect

Method used

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  • Phenylacetyltetrahydro-beta-carboline small molecule compound and application thereof
  • Phenylacetyltetrahydro-beta-carboline small molecule compound and application thereof
  • Phenylacetyltetrahydro-beta-carboline small molecule compound and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Embodiment 1: the preparation of WG-449E

[0051] Place methyl indole-7-carboxylate in a round-bottomed flask, dissolve it with TFA, stir and react for 10 minutes, add the DCM solution in which 1-dimethylamino-2-nitroethylene is dissolved into the flask dropwise, and then React at room temperature for about 2 hours. TLC detection, after the completion of the reaction, the reaction solution was evaporated to the minimum amount, with a little excess saturated NaHCO 3 Neutralize the concentrated solution until the pH is about 8. At this time, a large number of yellow solids are precipitated in the solution, filtered by suction, washed repeatedly, dried and ground to obtain a yellow powder;

[0052] The obtained yellow powder was dissolved in methanol solution, and NaBH was added in batches under ice-cooling conditions. 4 , N 2 protection, react for about 5 hours until the solution becomes colorless; add an appropriate amount of palladium carbon powder (10%), stir for 5 ...

Embodiment 2

[0059] Example 2: WG-449E inhibits gene transcription and protein expression of type I collagen.

[0060] 1. The effect of WG-449E on gene transcription of type I collagen detected by luciferase double reporter gene

[0061]Purpose and principle: Bioluminescent organisms are widely distributed in nature, and the enzymes that catalyze these bioluminescent reactions are called luciferases. Under suitable substrate conditions, luciferase can quickly catalyze the oxidation of the luciferin substrate, and the signal generated during the oxidation process can be captured by a fluorescence detector. The strength of the signal was used to judge the luciferase activity of the sample. Since endogenous luciferase is not distributed in mammalian cells, luciferase is an ideal reporter gene. By cloning the target gene upstream of the luciferase gene, constructing a reporter gene plasmid, transfecting cells, lysing the cells, and measuring the activity of luciferase, the effect of drug add...

Embodiment 3

[0067] Example 3: WG-449E inhibits the proliferation and migration of scar fibroblasts at a non-toxic dose.

[0068] 1. SRB method was used to detect the toxicity of WG-449E of the present invention to normal skin cells and scar fibroblasts.

[0069] Purpose and principle: The absorption peak of sulforhodamine B (SRB) at 540nm wavelength has a linear relationship with the cell mass, so it is often used as a quantitative detection method for cell proliferation ability.

[0070] Method: Add scar fibroblasts into 96-well plate, after the cells adhere to the wall, replace with fresh medium with different concentrations of WG-449E, after 24, 48, 72, and 96 hours of drug treatment, fix the cells, wash them, and air-dry them Add SRB dye solution for staining for 10min, wash off excess dye solution with 1% acetic acid, and air dry. The Tris solution dissolves the SRB bound to the cell protein, and after shaking, the absorbance value of each well at a wavelength of 515nm is measured w...

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Abstract

The invention discloses an application of a phenylacetyltetrahydro-beta-carboline small molecule organic compound or a pharmaceutically acceptable salt as shown in a formula (I), or its pharmaceuticalcomposition for preparing anti-scarring medicine. The invention also discloses the application of the small molecule compound WG-449E or the pharmaceutically acceptable salt in the anti-scarring medicines. In the present invention, the small molecule compound WG-449E or the pharmaceutically acceptable salt has the anti-scarring effect and can be used as a scar inhibitor for the treatment of hypertrophic scars caused by burns, cuts and the like after dermal trauma. The compound prevents or treats the formation and development of hypertrophic scars by inhibiting collagen synthesis, fibroblast proliferation and migration at scar tissue, and has the following advantages: 1. the coumpund can effectively inhibit the formation of scars, and 2. itching can be relieved by inhibiting the migrationof scar fibroblasts.

Description

technical field [0001] The invention belongs to the field of biomedical chemistry and relates to a class of phenylacetyltetrahydro-β-carboline small molecule organic compounds and applications thereof. Background technique [0002] The formation of hypertrophic scar is caused by abnormal wound healing and is a pathological process. Scars usually develop from injuries that reach deep dermal tissue, including burns, cuts, cuts, lacerations, and the like. The fibroblasts in hypertrophic scars are abnormally active and proliferate in large numbers, leading to excessive synthesis of collagen and deposition in the extracellular matrix. Migration of fibroblasts causes unbearable itching and pain in the affected area. It is a serious skin fibroproliferative disease. According to incomplete statistics, worldwide, more than 80 million people are affected by scars every year. In the United States alone, more than 4 million people are severely traumatized each year, more than 2 millio...

Claims

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Application Information

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IPC IPC(8): A61K31/437A61P17/00A61P13/12A61P11/00A61P1/16A61P9/00A61P27/02A61P19/02A61P17/02C07D471/04
CPCA61K31/437A61P1/16A61P9/00A61P11/00A61P13/12A61P17/00A61P17/02A61P19/02A61P27/02C07D471/04
Inventor 刘明耀邵婷唐文舒高丹陈益华易正芳
Owner EAST CHINA NORMAL UNIV
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