Institute of Pharmaceutical Biology and Phytochemistry (IPBP), University of Münster, Pharma Campus Correnstraße 48, D-48149 Münster, Germany.
Molecules. 2020 Oct 19;25(20):4804. doi: 10.3390/molecules25204804.
The increasing drug resistance of malaria parasites challenges the treatment of this life-threatening disease. Consequently, the development of innovative and effective antimalarial drugs is inevitable. -tigloylcyclovirobuxeine-B, a -cycloartane alkaloid from L., has shown promising and selective in vitro activity in previous studies against (), causative agent of Malaria tropica. For further investigations, it is indispensable to develop an advanced and efficient isolation procedure of this valuable natural product. Accordingly, we used liquid-liquid chromatography including centrifugal partition chromatography (CPC) to obtain the pure alkaloid on a semi-preparative scale. Identification and characterization of the target compound was accomplished by UHPLC/+ESI-QqTOF-MS/MS, H NMR and C NMR. In conclusion, this work provides a new and efficient method to obtain -tigloylcyclovirobuxeine-B, a valuable natural product, as a promising antiplasmodial lead structure for the development of innovative and safe medicinal agents.
疟原虫的抗药性不断增强，给这种危及生命的疾病的治疗带来了挑战。因此，开发创新、有效的抗疟药物是必然的。-tigloylcyclovirobuxeine-B 是从 L.中提取的一种 -cycloartane 生物碱，在之前的研究中对疟原虫（导致热带疟疾的病原体）表现出了有前景和选择性的体外活性。为了进一步的研究，开发一种先进、高效的这种有价值的天然产物的分离程序是必不可少的。因此，我们使用液-液色谱法，包括离心分配色谱（CPC），在半制备规模上获得纯生物碱。通过 UHPLC/+ESI-QqTOF-MS/MS、1H NMR 和 13C NMR 对目标化合物进行了鉴定和表征。总之，这项工作提供了一种新的、有效的方法来获得 -tigloylcyclovirobuxeine-B，这是一种有价值的天然产物，作为一种有前途的抗疟先导结构，可用于开发创新和安全的药物。
