Abstract
Hepatitis B virus (HBV) infection is prevalent and continues to be a global health concern. In this study, we determined the anti-hepatitis B virus (HBV) potential of the Socotra-endemic medicinal plant Dracaena cinnabari and isolated and characterized the responsible constituents. A bioassay-guided fractionation using different chromatographic techniques of the methanolic extract of D. cinnabari led to the isolation of two chalcone derivatives. Using a variety of spectroscopic techniques, including 1H-, 13C-, and 2D-NMR, these derivatives were identified as 2,4’-dihydroxy-4-methoxydihydrochalcone (compound 1) and 2,4’-dihydroxy-4-methoxyhydrochalcone (compound 2). Both compounds were isolated for the first time from the red resin (dragon’s blood) of D. cinnabari. The compounds were first evaluated for cytotoxicity on HepG2.2.15 cells and 50% cytotoxicity concentration (CC50) values were determined. They were then evaluated for anti-HBV activity against HepG2.2.15 cells by assessing the suppression of HBsAg and HBeAg production in the culture supernatants and their half maximum inhibitory concentration (IC50) and therapeutic index (TI) values were determined. Compounds 1 and 2 indicated inhibition of HBsAg production in a dose- and time-dependent manner with IC50 values of 20.56 and 6.36 μg/mL, respectively.
Highlights
Infectious disease caused by the hepatitis B virus (HBV) is widespread and continues to be a global health issue
As part of a continuing study of medicinal plants and natural products with antiviral activity, we studied the isolation and structure elucidation of two chalcone derivatives from Dracaena cinnabari with anti-hepatitis activity
A bioassay-guided fractionation, using chromatographic techniques, of the methanolic extract of D. cinnabari led to the isolation of two chalcone derivatives that showed antihepatitis activity
Summary
Infectious disease caused by the hepatitis B virus (HBV) is widespread and continues to be a global health issue. Around two billion people show evidence of infection with hepatitis, and about 250–360 million people are chronically infected and at risk for liver disease, according to statistics. Liver failure, or hepatocellular carcinoma develop in 15–40% of people infected with HBV [1,2,3]. Around 25% of chronically infected adults develop cirrhosis or liver cancer and die as a result of this infection [4,5,6]. The price of these anti-HBV drugs makes them unaffordable for most underdeveloped countries. Continuous research is being conducted to discover novel anti-HBV medications derived from natural sources that have higher efficacy and promise. Several phytocompounds from distinct phytochemical classes have been studied for their potential anti-HBV activity [1,9,10,11,12]
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