Protoberberine Alkaloids as Antimalarials

Jonathan L. Vennerstrom, Daniel L. Klayman

Research output: Contribution to journalArticlepeer-review

107 Scopus citations


The protoberberine alkaloids berberine (1), palmatine (2), jatrorrhizine (3), and several berberine derivatives (4-10) were tested for antimalarial activity in vitro against Plasmodium falciparum and in vivo against Plasmodium berghei. The berberine derivatives 4-10 were designed and synthesized to maximize structural diversity within a modest set of compounds. Palmatine (2) and jatrorrhizine (3) were isolated as their chlorides from Enantia chlorantha. None of the protoberberine alkaloids was active in vivo, although compounds 1, 2, 3, 5, and 6 exhibited a potency comparable to that of quinine in vitro.

Original languageEnglish (US)
Pages (from-to)1084-1087
Number of pages4
JournalJournal of Medicinal Chemistry
Issue number6
StatePublished - Feb 1 1988
Externally publishedYes

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery


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