Amplification of DNA-binding affinities of protoberberine alkaloids by appended polyamines

Ji Yan Pang, Yu Hua Long, Wen Hua Chen*, Zhi Hong Jiang

*Corresponding author for this work

Research output: Contribution to journalJournal articlepeer-review

28 Citations (Scopus)


This communication describes a synthetic approach toward the amplification of the moderate DNA-binding affinities of protoberberine alkaloids. Specifically, three protoberberine derivatives bearing two to six primary amino groups at the 3- and 9-positions of protoberberine were synthesized and characterized by NMR (1H and 13C) and HRMS. Studies on their affinities toward calf thymus (CT) DNA by ethidium bromide (EB) displacement and spectrophotometric titration experiments indicate that these polyamino protoberberines show more than 103-fold enhanced DNA-binding affinities relative to palmatine and thus are exploitable as strong DNA-binders.

Original languageEnglish
Pages (from-to)1018-1021
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Issue number4
Publication statusPublished - 15 Feb 2007

Scopus Subject Areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

User-Defined Keywords

  • DNA-binding
  • EB displacement
  • Multivalency
  • Polyamine
  • Protoberberine


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