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Beaufay C , Ledoux A , Jansen O , Bordignon A , Zhao S , Teijaro CN , Andrade RB , Quetin-Leclercq J , Frederich M
In vivo Antimalarial and Antitrypanosomal Activity of Strychnogucine B, a Bisindole Alkaloid from Strychnos icaja
Planta Med. 2018 Aug;84(12-13) :881-885
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Strychnogucine B is a bisindole alkaloid previously isolated from Strychnos icaja that possesses promising in vitro antiplasmodial properties. This compound was synthesized in four steps from (-)-strychnine. As no acute toxicity was observed at the highest tested cumulative dose of 60 mg/kg, its in vivo antimalarial activity was determined intraperitoneally at 30 mg/kg/d in a Plasmodium berghei murine model. In the Peters's 4-d suppressive test, this alkaloid suppressed the parasitaemia by almost 36% on day 5 and 60% on day 7 compared to vehicle-treated mice. In addition to this interesting antimalarial activity, it showed moderate in vitro antitrypanosomal activity but no in vivo activity in an acute Trypanosoma brucei model. It was also inactive in vitro on Leishmania mexicana promastigotes. This highlights its selective antimalarial efficacy and leads to further investigation to assess its potential as new antimalarial lead compound.
1439-0221 Beaufay, Claire Ledoux, Allison Jansen, Olivia Bordignon, Annelise Zhao, Senzhi Teijaro, Christiana N Andrade, Rodrigo B Quetin-Leclercq, Joelle Frederich, Michel Journal Article Germany Planta Med. 2018 Jun 21. doi: 10.1055/a-0644-2723.