63 / 2021-10-10 17:18:04

Antimalarial Marine Natural Products: A Comprehensive Overview and Emphasized Targets for Malaria Treatment

Antimalarial Marine Natural Products,Malaria Targets,Blue Drug Bank

Malaria remains a significant public health challenge in regions of the world. Especially, the control of malaria has been severely compromised due to the widespread resistance of Plasmodium falciparum to nearly all frontline therapeutics.^[1,2] Focusing on the strategy of “Blue Drug Bank”, the molecules highlighted can be used as inspiration for medicinal chemistry campaigns.^[3]

This review covers developments of antimalarial marine lead compounds between 1972 and July 2021.They are divided into seven categories, polyketide (16%), terpenoid (29%), alkaloid (26%), macrolide (16%), peptide (7%), steroid (3%) and others (3%). We selected 60 representative potential molecules from 361 compounds and highlighted the structure-activity relationships, molecular mechanisms of target, drug-like properties in order to assess their drug potential. We counted 107 clinically targets and determined the subcellular location of the relevant target proteins, which linked the molecules to the target proteins at the subcellular level. Encouragingly, the development of new antimalarial drugs in combination with drug targets has also been successfully applied. We hope that the examples we have summarized can be applied to the huge treasure house of marine natural products.

This work was supported by the Program of National Natural Science Foundation of China (Nos. U1706210, 41776141, 41906090, 42006092 and 41322037), the Program of Natural Science Foundation of Shandong Province of China (No. ZR2019BD047), the Marine S&T Fund of Shandong Province for Pilot National Laboratory for Marine Science and Technology (Qingdao) (No. 2018SDKJ0403-2), and the Taishan Scholars Program, China (No. tsqn20161010).