Basic research on anti-trypanosomal drug discovery using bioactive substances derived from insect

甲虫防御素衍生肽对布氏锥虫的作用方式为攻击细胞膜。我们开发了一种多功能材料，将防御素衍生肽共价结合在材料表面，并从腐殖酸中纯化了一种抗锥虫物质。令人惊讶的是，活性物质被鉴定为核黄素，称为维生素B2。口服核黄素可显著延迟锥虫感染小鼠的死亡和寄生虫的增殖。然而，静脉或腹腔注射核黄素并不影响寄生虫的死亡率和增殖。

The mode of action of beetle-defensin derived peptides against Trypanosoma brucei brucei was revealed that the peptides attack cellular membrane of the parasites. We developed multi-functional materials on which the defensin derived peptides were covalently bound on the surface.We purified an anti-trypanosomal substance from Bombyx pupae. Surprisingly, the active substance was identified as riboflavin, known as vitamin B2. Oral administration of riboflavin significantly delayed death of trypanosome-infected mice and proliferation of parasites. However, intravenous or intraperitoneal injection of riboflavin did not affect mortality and proliferation of parasites.