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Applications of composition of Schiglautone A derivatives in preparing medicines for resisting hepatic fibrosis

A liver fibrosis and composition technology, applied in the fields of organic synthesis and medicinal chemistry, can solve the problems of lack of clinical treatment methods

Inactive Publication Date: 2016-12-07
NANJING GUANGKANGXIE BIOLOGICAL MEDICAL TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In recent years, some anti-hepatic fibrosis treatments have emerged, including chemical drugs, biological agents, traditional Chinese medicine and gene therapy, etc., but the ideal clinical treatment methods are still lacking (Liu Ping. Strengthen the research on the mechanism of anti-hepatic fibrosis. Chinese liver disease Magazine, 2005, 8(13): 561)

Method used

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  • Applications of composition of Schiglautone A derivatives in preparing medicines for resisting hepatic fibrosis
  • Applications of composition of Schiglautone A derivatives in preparing medicines for resisting hepatic fibrosis
  • Applications of composition of Schiglautone A derivatives in preparing medicines for resisting hepatic fibrosis

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] The preparation of embodiment 1 compound Schiglautone A

[0016] The preparation method of compound Schiglautone A (I) refers to the literature published by Fan-Yu Meng et al. of Schisandra glaucescens. Organic Letters 13(2011) 1502–1505).

[0017]

Embodiment 2

[0018] The synthesis of the O-bromoethyl derivative (II) of embodiment 2 Schiglautone A

[0019] Compound I (502 mg, 1.00 mmol) was dissolved in 15 mL of benzene, and tetrabutylammonium bromide (TBAB) (0.08 g), 1,2-dibromoethane (7.520 g, 40.00 mmol) and 6 mL of 50% sodium hydroxide solution. The mixture was stirred at 35 °C for 8 h. After 8 hours, the reaction solution was poured into ice water, extracted twice with dichloromethane immediately, and the organic phase solutions were combined. Then the organic phase solution was washed with water and saturated brine three times successively, then dried with anhydrous sodium sulfate, and finally concentrated under reduced pressure to remove the solvent to obtain a crude product. The crude product was purified by silica gel column chromatography (mobile phase: petroleum ether / acetone=100:1.0, v / v), the brown concentrated elution band was collected and the solvent was evaporated to obtain a brown powder of Compound II (508mg, 71%...

Embodiment 3

[0024] The synthesis of the O-(triazolyl) ethyl derivative (III) of embodiment 3 Schiglautone A

[0025] Compound II (358 mg, 0.5 mmol) was dissolved in 10 mL of acetonitrile, anhydrous potassium carbonate (345 mg, 2.5 mmol), potassium iodide (84 mg, 0.5 mmol) and 1,2,3-triazole (2760 mg, 40 mmol) were added thereto ), the mixture was heated to reflux for 3h. After the reaction, the reaction solution was poured into ice water, extracted twice with an equal amount of dichloromethane, and the organic phases were combined. The combined organic phases were successively washed with water and saturated brine, dried over anhydrous sodium sulfate, and concentrated under reduced pressure to remove the solvent to obtain a crude product. The crude product was purified by silica gel column chromatography (mobile phase: petroleum ether / acetone=100:1.0, v / v), and the light yellow concentrated elution band was collected to obtain compound III as a yellow colloidal solid (245.7mg, 71%) .

...

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Abstract

The invention relates to the fields of organic synthesis and pharmaceutical chemistry, and discloses and provides a composition prepared from O-(triazolyl) ethyl derivative (III) and O-(di(2-methylthio-ethyl)amino) ethyl derivative (IV) of Schiglautone A at the weight ratio of 70 to 30, and a method for preparing the composition by mixing the two compounds at the weight ratio of 70 to 30. The pharmacological experiment proves that the composition provided by the invention at 20 [mu] g / ml can obviously inhibit the proliferation of NIH / 3T3 and the proliferation of fibroblasts induced by transforming growth factor-beta 1, and has the effect of resisting hepatic fibrosis, and therefore, the invention further provides the applications of the composition prepared from O-(triazolyl) ethyl derivative (III) and O-(di(2-methylthio-ethyl)amino) ethyl derivative (IV) of Schiglautone A at the weight ratio of 70 to 30 in preparing medicines for resisting hepatic fibrosis.

Description

[0001] The invention relates to the fields of organic synthesis and medicinal chemistry, in particular to a composition, a preparation method and an application thereof. Background technique [0002] Liver fibrosis is a dynamic process from chronic liver injury to liver cirrhosis, manifested in the synthesis and secretion of a large amount of extracellular matrix (ECM), while the degradation is absolutely or relatively insufficient, resulting in the diffuse deposition of ECM in the liver. It starts with necrosis of hepatocytes (HC), followed by inflammatory response, release of fibrogenesis mediators, activation of hepatic stellate cells (FSC), and finally, the synthesis and degradation of liver connective tissue components are obviously out of balance. Liver fibrosis is a common pathological process of many chronic liver diseases and an important factor affecting prognosis. [0003] In the past 20 years, the study of liver fibrosis has made great progress, and it has been con...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4192A61K31/195C07D249/04C07C323/25A61P1/16
CPCA61K31/4192A61K31/195C07C323/25C07D249/04A61K2300/00
Inventor 陆贤
Owner NANJING GUANGKANGXIE BIOLOGICAL MEDICAL TECH
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