Application of Polyethylene Glycol Artesunate in Preparation of Anti-hepatic Lesion Medicine

Abstract

The invention provides applications of pegylated artesunate shown as the formula (I) in preparing medicines capable of resisting hepatic pathological changes. According to the applications, pegylated artesunate can obviously reduce the hepatic fibrosis condition and abnormal liver function of hepatic fibrosis rats caused by carbon tetrachloride, reduce the amount of the serum fibrosis markers such as hyaluronidase (HA), laminin (LN) and procollagen III (PC-III), reduce the amount of alamine aminotransferase (ALT) and aspartate aminotransferase (AST) in the serum, reduce the contents of malondialdehyde (MDA) and hydroxyproline (Hyp) of the liver tissue, and effectively prevent the development of liver fibrosis and promote the reversion of liver fibrosis, and has the significant differences compared with artesunate under the same dosage. In addition, the pegylated artesunate is good in water solubility, high in bioavailability, and long in half-life period, and the administration times can be reduced. The formula (I) is shown as follows.

Description

technical field [0001] The invention relates to the technical field of artesunate derivatives, in particular to the application of polyethylene glycol artesunate in the preparation of anti-hepatic lesions drugs. Background technique [0002] Hepatic fibrosis is the pathological basis of liver cirrhosis. Various etiologies (such as viral hepatitis, alcoholic liver disease, non-alcoholic liver disease, drug and chemical factors, etc.) cause liver damage and inflammation, leading to liver fibrosis , and eventually develop into liver cirrhosis. Liver fibrosis is the result of excessive deposition of extracellular matrix, and it is also the main intermediate link in the further development of liver cirrhosis and liver cancer. [0003] Liver cirrhosis has a high morbidity and mortality rate. According to statistics, domestic patients hospitalized due to liver cirrhosis accounted for 0.36% to 0.64% of the hospitalizations in the same period. Chronic liver diseases such as parasit...

AI Technical Summary

Problems solved by technology

Evidence has shown that liver fibrosis and early liver cirrhosis are reversible. Blocking or reversing liver fibrosis is an important goal in the treatment of chronic liver diseases, but there are no approved chemical or biological agents against liver fibrosis in clinical application

However, there is no research on the anti-hepatic fibrosis of polyethylene glycol artesunate

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