Egas Moniz School of Health & Science, University Campus, Quinta da Granja Monte da Caparica, 2829-511 Caparica, Portugal.
Egas Moniz Center for Interdisciplinary Research (CiiEM), Egas Moniz School of Health & Science, University Campus, Quinta da Granja Monte da Caparica, 2829-511 Caparica, Portugal.
Molecules. 2024 May 15;29(10):2316. doi: 10.3390/molecules29102316.
Malaria remains an important and challenging infectious disease, and novel antimalarials are required. Benzyl isothiocyanate (BITC), the main breakdown product of benzyl glucosinolate, is present in all parts of L. () and has antibacterial and antiparasitic activities. To our knowledge, there is no information on the effects of BITC against malaria. The present study evaluates the antimalarial activity of aqueous extracts of BITC and seeds, leaves, and stems. We used flow cytometry to calculate the growth inhibition (GI) percentage of the extracts and BITC against unsynchronized cultures of the chloroquine-susceptible 3D7 - GFP strain. Extracts and/or compounds with at least 70% GI were validated by IC50 estimation against 3D7 - GFP and Dd2 (chloroquine-resistant strain) unsynchronized cultures by flow cytometry, and the resistance index (RI) was determined. aqueous extracts showed some antimalarial activity that was higher in seeds than in leaves or stems. BITC's GI was comparable to chloroquine's. BITC's IC50 was similar in both strains; thus, a cross-resistance absence with aminoquinolines was found (RI < 1). BITC presented features that could open new avenues for malaria drug discovery.
疟疾仍然是一种重要且具有挑战性的传染病，因此需要新型抗疟药物。苄基异硫氰酸酯（BITC）是苄基葡萄糖硫苷的主要分解产物，存在于 L. 的各个部位，具有抗菌和抗寄生虫活性。据我们所知，尚无关于 BITC 抗疟作用的信息。本研究评估了 BITC 水溶液提取物以及 种子、叶子和茎对疟疾的抗疟活性。我们使用流式细胞术计算提取物和 BITC 对氯喹敏感的 3D7-GFP 菌株未同步培养物的生长抑制（GI）百分比。通过流式细胞术，对至少 70%GI 的提取物和化合物进行 IC50 估计，对 3D7-GFP 和 Dd2（氯喹抗性株）未同步培养物进行验证，并确定耐药指数（RI）。 水提物表现出一定的抗疟活性，在种子中的活性高于叶子或茎。BITC 的 GI 与氯喹相当。BITC 在两种菌株中的 IC50 相似；因此，发现与氨基喹啉类药物无交叉耐药性（RI<1）。BITC 具有可开辟疟疾药物发现新途径的特征。
