Beaufay Claire, Ledoux Allison, Jansen Olivia, Bordignon Annélise, Zhao Senzhi, Teijaro Christiana N, Andrade Rodrigo B, Quetin-Leclercq Joëlle, Frédérich Michel
Pharmacognosy Research Group, Louvain Drug Research Institute, Université Catholique de Louvain, Brussels, Belgium.
Laboratory of Pharmacognosy, CIRM, Université de Liège, Liège, Belgium.
Planta Med. 2018 Aug;84(12-13):881-885. doi: 10.1055/a-0644-2723. Epub 2018 Jun 21.
Strychnogucine B is a bisindole alkaloid previously isolated from that possesses promising 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 antimalarial activity was determined intraperitoneally at 30 mg/kg/d in a 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 antitrypanosomal activity but no activity in an acute model. It was also inactive on promastigotes. This highlights its selective antimalarial efficacy and leads to further investigation to assess its potential as new antimalarial lead compound.
马钱子碱B是一种双吲哚生物碱，此前从[具体来源未给出]中分离得到，具有良好的抗疟特性。该化合物以（-）-马钱子碱为原料，经四步合成。由于在最高测试累积剂量60mg/kg时未观察到急性毒性，因此在小鼠模型中以30mg/kg/d的剂量腹腔注射测定其抗疟活性。在彼得斯4天抑制试验中，与赋形剂处理的小鼠相比，该生物碱在第5天可使疟原虫血症抑制近36%，在第7天抑制60%。除了这种有趣的抗疟活性外，它还表现出中度的抗锥虫活性，但在急性模型中无活性。它对前鞭毛体也无活性。这突出了其选择性抗疟功效，并促使进一步研究以评估其作为新型抗疟先导化合物的潜力。
