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Isolation and Characterization of Two Chalcone Derivatives with Anti-Hepatitis B Virus Activity from the Endemic Socotraen Dracaena cinnabari (Dragon's Blood Tree).

Ramzi A A MothanaAhmed H ArbabAli A ElGamalMohammad K ParvezMohammed S Al-Dosari
Published in: Molecules (Basel, Switzerland) (2022)
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 1 H-, 13 C-, 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 (IC 50 ) and therapeutic index (TI) values were determined. Compounds 1 and 2 indicated inhibition of HBsAg production in a dose- and time-dependent manner with IC 50 values of 20.56 and 6.36 μg/mL, respectively.
Keyphrases
  • hepatitis b virus
  • global health
  • liver failure
  • public health
  • oxidative stress
  • structure activity relationship
  • molecular docking
  • high resolution
  • mass spectrometry
  • human health
  • solid state
  • liquid chromatography