Berberine-piperazine conjugates as potent influenza neuraminidase blocker

Ganuskh Enkhtaivan, Doo Hwan Kim, Gyun Seok Park, Muthuraman Pandurangan, Daniel A. Nicholas, So Hyun Moon, Avinash A. Kadam, Rahul V. Patel, Han Seung Shin, Bhupendra M. Mistry

Research output: Contribution to journalArticlepeer-review

15 Scopus citations

Abstract

In these studies, we analyzed substituted piperazine based berberine analogs conjugated through a pentyloxy side chain for their in vitro and in silico biological effects. All the final analogs were screened for their in vitro antiviral action against a collection of different influenza virus strains using the CPE assay and SRB assay. Moreover, their cytotoxicity towards non-cancer cell lines was examined employing Madin–Darby canine kidney (MDCK) cell lines. The anti-influenza activities of berberine-piperazine derivatives (BPD) were evaluated in the range from 35.16 μg/mL to 90.25 μg/mL of the IC50s along with cytotoxicity level which was observed in the range 44.8 μg/mL to 3890.6 μg/mL of CC50s towards MDCK cells. In an effort to know the mechanism of action of BPD1-BPD23, results of Neuraminidase inhibition assay and Molecular docking studies carried out against neuraminidase as the target enzyme revealed that titled compounds are potential neuraminidase inhibitors that merge to the active site of neuraminidase, with moderate to high binding energy.

Original languageEnglish
Pages (from-to)1204-1210
Number of pages7
JournalInternational Journal of Biological Macromolecules
Volume119
DOIs
StatePublished - Nov 2018

Keywords

  • Berberine-piperazine derivatives
  • Docking
  • Influenza virus
  • Neuraminidase inhibitors

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