4.7 Article

Anti-Hepatitis B Virus Effects of Dehydrocheilanthifoline from Corydalis saxicola

Journal

AMERICAN JOURNAL OF CHINESE MEDICINE
Volume 41, Issue 1, Pages 119-130

Publisher

WORLD SCIENTIFIC PUBL CO PTE LTD
DOI: 10.1142/S0192415X13500092

Keywords

Dehydrocheilanthifoline; Corydalis saxicola; Hepatitis B Virus; cccDNA; pgRNA

Funding

  1. Twelfth Five-Year National Science and Technology Support Program [2012BA129B06]
  2. Natural Science Foundation of China [81274170]
  3. Project of State Key Laboratory Cultivation Base for the Chemistry and Molucular Engineering of Medicinal Resources, Ministry of Science and Technolgy of China [CMEMR2011-04]
  4. State Key Laboratory of Natural and Biomimetic Drugs [K20120208]

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In this report, the anti-hepatitis B virus (HBV) activity of dehydrocheilanthifoline (DHCH), a quaternary ammonium alkaloid isolated from the traditional Chinese medicine Corydalis saxicola Bunting (Papaveraceae), was determined in vitro. Following six days of treatment, DHCH efficiently suppressed the secretions of HBsAg and HBeAg in HepG2.2.15 cell cultures, with a half-maximal inhibitory concentration (IC50) of 15.84 and 17.12 mu M, and with a therapeutic index (TI) of 7.32 and 6.77, respectively. Further studies revealed that DHCH reduced the levels of extracellular DNA, intracellular DNA and covalently closed circular DNA (cccDNA) of HBV in a dose-dependent and time-dependent manner, with IC50 values of 15.08, 7.62 and 8.25 mu M, respectively after six days of treatment. In contrast, the level of viral pre-genomic RNA (pgRNA) increased 6.13-fold after treatment with DHCH. Together, it was demonstrated for the first time that DHCH could significantly inhibit the replication of HBV, which warrants further studies on the antiviral mechanisms of DHCH, and suggests that it may be a promising candidate in the therapy of HBV infection.

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