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Updated: Aug 17, 2026

Ookluc: A Plasmodium berghei Line for Identifying Transmission-blocking Compounds
Published on: July 11, 2025
Isoneocryptolepine, a synthetic indoloquinoline alkaloid, as an antiplasmodial lead compound
Sabine Van Miert1, Steven Hostyn, Bert U W Maes
1Department of Pharmaceutical Sciences, University of Antwerp, Belgium.
Abstract:
The antiprotozoal activities of three naturally occurring isomeric indoloquinoline alkaloids, i.e., cryptolepine (1), neocryptolepine (2), and isocryptolepine (3), and two dimeric indoloquinoline alkaloids, cryptoquindoline (6) and biscryptolepine (7), originally obtained from the plant Cryptolepis sanguinolenta, were compared with those of a new synthetic indoloquinoline isomer, isoneocryptolepine (4), and a quaternary derivative, N-methyl-isocryptolepinium iodide (5). The latter compounds showed a high antiplasmodial activity against the chloroquine-resistant Plasmodium falciparum strain K1 (IC50 of 0.23 +/- 0.04 and 0.017 +/- 0.004 microM, respectively), while the cytotoxicity (L6 cells) was 4.32 +/- 0.04 and 12.7 +/- 2.0 microM, respectively. Isoneocryptolepine (4) was found to act as an inhibitor of beta-hematin formation and as a DNA-intercalating agent.
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