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Plasmodium stage-selective antimalarials from Lophira lanceolata stem bark
Phytochemistry ( IF 3.8 ) Pub Date : 2020-06-01 , DOI: 10.1016/j.phytochem.2020.112336
Harouna Soré 1 , Annalisa Lopatriello 2 , Yehenew A Ebstie 3 , Alain R Tenoh Guedoung 3 , Adama Hilou 4 , José A Pereira 5 , Anake Kijjoa 5 , Annette Habluetzel 6 , Orazio Taglialatela-Scafati 7
Affiliation  

Targeting the transmissible stages of the Plasmodium parasite that develop in the human and mosquito host is a crucial strategy for malaria control and elimination. Medicinal plants offer a prolific source for the discovery of new antimalarial compounds. The recent identification of the gametocytocidal activity of lophirone E, obtained from the African plant Lophira lanceolata (Ochnaceae), inspired the evaluation of the plant also against early sporogonic stages of the parasite development. The bioassay-guided phytochemical study led to the isolation of two known lanceolins and of a new glycosylated bichalcone, named glucolophirone C. Its stereostructure, including absolute configuration of the bichalcone moiety, was elucidated by means of NMR, HRMS, ECD and computational calculations. Lanceolin B proved to be a potent inhibitor of the development of Plasmodium early sporogonic stages indicating that the plant produces two different stage-specific antimalarial agents acting on transmissible stages in the human and mosquito host.

中文翻译:

来自 Lophira lanceolata 茎皮的疟原虫阶段选择性抗疟药

针对在人类和蚊子宿主中发展的疟原虫寄生虫的传播阶段是控制和消除疟疾的关键策略。药用植物为发现新的抗疟化合物提供了丰富的资源。最近从非洲植物 Lophira lanceolata (Ochnaceae) 获得的 lophirone E 的杀配子细胞活性的鉴定激发了对该植物的评估,也反对寄生虫发育的早期孢子原阶段。生物测定指导的植物化学研究导致分离出两种已知的披针油菌素和一种新的糖基化双查耳酮,命名为葡糖酮 C。通过 NMR、HRMS、ECD 和计算计算阐明了其立体结构,包括双查耳酮部分的绝对构型。
更新日期:2020-06-01
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