Abstract
Coumarins are widely present in a variety of plants and have a variety of pharmacological activities. In this study, we isolated a coumarin compound from Microsorium fortunei (Moore) Ching; the compound was identified as esculetin by hydrogen and carbon spectroscopy. Its anti-hepatitis B virus (HBV) activity was investigated in vitro and in vivo. In the human hepatocellular liver carcinoma 2.2.15 cell line (HepG2.2.15) transfected with HBV, esculetin effecting inhibited the expression of the HBV antigens and HBV DNA in vitro. Esculetin inhibited the expression of Hepatitis B virus X (HBx) protein in a dose-dependent manner. In the ducklings infected with duck hepatitis B virus (DHBV), the levels of DHBV DNA, duck hepatitis B surface antigen (DHBsAg), duck hepatitis B e-antigen (DHBeAg), alanine aminotransferase (ALT) and aspartate aminotransferase (AST) decreased significantly after esculetin treatment. Summing up the above, the results suggest that esculetin efficiently inhibits HBV replication both in vitro and in vivo, which provides an opportunity for further development of esculetin as antiviral drug.
Highlights
The hepatitis B virus (HBV) is a common infectious disease in the world
Real-time PCR was used to detect the level of HBV DNA in the supernatant, and the results showed that esculetin significantly reduced the expression of HBV DNA in the
The results indicated that esculetin can significantly inhibit the secretion of Hepatitis B surface antigen (HBsAg) and Hepatitis Be Antigen (HBeAg) at a non-toxic concentration range, and the inhibitory effect of esculetin on antigen was dose- and time-dependent
Summary
The hepatitis B virus (HBV) is a common infectious disease in the world. There are about 350 million hepatitis B virus carriers worldwide [1,2]. There are a series of figures showing that about one million people worldwide die from complications caused by HBV every year [3], which poses a great threat to human health. The drugs commonly used for anti-HBV are interferon and nucleosides such as IFN-α, lamivudine (3TC), tenofovir, etc. These drugs are prone to drug resistance and have side effects [4]. In the last few years, much clinical and experimental research has verified many Chinese medicines with anti-HBV effects [7]. It is a hot topic in the search for new drugs to find high-efficiency, low-cost and novel anti-HBV drugs from traditional
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