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Application of andrographolide derivatives and their 3,19 esters in the preparation of anti-hepatic fibrosis drugs

A kind of andrographolide, anti-liver fibrosis technology, applied in the field of medicine

Active Publication Date: 2019-04-19
ZHENGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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  • Application of andrographolide derivatives and their 3,19 esters in the preparation of anti-hepatic fibrosis drugs
  • Application of andrographolide derivatives and their 3,19 esters in the preparation of anti-hepatic fibrosis drugs
  • Application of andrographolide derivatives and their 3,19 esters in the preparation of anti-hepatic fibrosis drugs

Examples

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Embodiment 1

[0073] Example 1 The compounds of the present invention inhibit the migration of human hepatic stellate cells LX-2.

[0074] Under the stimulation of various inflammatory mediators, growth factors and other cytokines, hepatic stellate cells migrate to the inflammatory site of the damaged liver tissue, and then proliferate, activate, and synthesize ECM components such as collagen, which is the key to the development of liver fibrosis. Therefore, the scratch injury method was used to evaluate the anti-hepatic fibrosis effect of the compound of the present invention.

[0075] 1 Cell culture and drug treatment

[0076] Using human hepatic stellate cells LX-2 (provided by Beijing Beina Chuanglian Institute of Biotechnology), compared with andrographolide, the in vitro anti-hepatic fibrosis effect of the compound of the present invention was studied. The LX-2 cells were cultured in a culture flask containing RPMI1640 culture medium containing 10% fetal bovine serum (Zhejiang Tianha...

Embodiment 2

[0084] Embodiment 2 The compound of the present invention significantly reduces carbon tetrachloride (CCl 4 ) induced the degree of liver fibrosis in SD rats

[0085] CCl 4 Induced liver fibrosis model is a traditional classic animal model, because it is very similar to human liver fibrosis in many aspects such as morphology and pathophysiology. It not only has the characteristics of liver fibrosis induced by toxic substances, but also It is also similar to the pathological features after hepatitis B virus infection, and can well simulate the pathological changes of human liver fibrosis. low dose CCl 4 After long-term stimulation, not only the abnormal liver function of animals is very similar to that of human liver cirrhosis, but also the molecular mechanism of fibrosis, serum markers after injury, and pathological changes of liver tissue are very similar to humans. Therefore, CCl 4 The induced liver fibrosis model is now widely used in the study of the pathogenesis of li...

Embodiment 3

[0095] Example 3 The compound of the present invention significantly reduces the degree of liver fibrosis induced by pig serum in Wistar rats

[0096] Immune liver fibrosis is mainly a disease caused by the immune response of the liver itself, and liver fibrosis caused by other factors (viruses, alcohol, schistosomiasis and certain chemical substances, etc.) is often accompanied by different degrees of immune response. Repeated intraperitoneal injection of heterogeneous serum or protein (pig serum g, schistosomiasis serum, human or bovine serum albumin, etc.) to experimental animals is the main modeling method at present. The uniqueness of this method is that the xenogeneic serum mainly activates the liver stem cells HSC through MHC Ⅱ molecules and inflammatory factors to generate an immune response to the liver injury. During this process, liver fibrosis and immune response persist, which can well reproduce the effects of other models. The possible process and mechanism of li...

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Abstract

The invention belongs to the technical field of medicines, discloses applications of andrographolide derivatives in preparation of medicines preventing and treating hepatic fibrosis, and relates to 15-benzylidene-14-deoxy-11,12-dehydroandrographolide derivatives and 3,19 esterified compounds thereof. Experiments prove that the compounds significantly inhibit human hepatic stellate cell LX-2 metastasis and activation, significantly reduce the fibrosis level of hepatic tissues of rats affected with hepatic fibrosis, reduce contents of extracellular matrix protein (ECM) related components, significantly reduce the level of immune inflammation correlation factors of rats affected with hepatic fibrosis, effectively inhibit immuno-inflammatory responses, inhibit hepatic stellate cell activation in hepatic tissues, and promote collagen degradation. The compounds are used as active components for preparing the anti-hepatic fibrosis medicines, and are efficient and low in toxicity, thus providing a novel medicine route for hepatic fibrosis treatment and prevention, and expanding the optional range of clinical medicine application. The compounds and the applications have good development prospects.

Description

technical field [0001] The invention relates to the application of andrographolide derivatives as anti-hepatic fibrosis drugs, in particular to 15-benzylidene-14-deoxy-11,12-dehydroandrographolide derivatives, belonging to the technical field of medicine. Background technique [0002] Globally, the incidence of liver fibrosis (Hepatic fibrosis, HF) is about 100 / 100,000 people, more common in adults aged 35-50, more men than women, and higher in rural areas than in cities. HF refers to the abnormal proliferation of extracellular matrix (ECM) and connective tissue after liver cells are damaged. HF can lead to changes in the structure and function of liver tissue. When the extracellular matrix accumulates for a long time, fibrous hyperplasia forms a network space that hinders the normal material and energy exchange between liver cells and blood, and a large number of liver cells appear necrotic. Form liver cirrhosis (Liver cirrhosis, LC). According to the definition of the Wo...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D307/60C07D405/12A61K31/365A61K31/443A61P1/16
CPCC07D307/60C07D405/12
Inventor 戴桂馥杨卫马翠云徐海伟赵进巫凤娟王亚可高小雪胡洋洋沈鹏鹏蒋坤坤
Owner ZHENGZHOU UNIV
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