RT Journal Article
T1 Discovery of New Compounds Active against Plasmodium falciparum by High Throughput Screening of Microbial Natural Products.
A1 Pérez-Moreno, Guiomar
A1 Cantizani, Juan
A1 Sánchez-Carrasco, Paula
A1 Ruiz-Pérez, Luis Miguel
A1 Martín, Jesús
A1 El Aouad, Noureddine
A1 Pérez-Victoria, Ignacio
A1 Tormo, José Rubén
A1 González-Menendez, Víctor
A1 González, Ignacio
A1 de Pedro, Nuria
A1 Reyes, Fernando
A1 Genilloud, Olga
A1 Vicente, Francisca
A1 González-Pacanowska, Dolores
AB Due to the low structural diversity within the set of antimalarial drugs currently available in the clinic and the increasing number of cases of resistance, there is an urgent need to find new compounds with novel modes of action to treat the disease. Microbial natural products are characterized by their large diversity provided in terms of the chemical complexity of the compounds and the novelty of structures. Microbial natural products extracts have been underexplored in the search for new antiparasitic drugs and even more so in the discovery of new antimalarials. Our objective was to find new druggable natural products with antimalarial properties from the MEDINA natural products collection, one of the largest natural product libraries harboring more than 130,000 microbial extracts. In this work, we describe the optimization process and the results of a phenotypic high throughput screen (HTS) based on measurements of Plasmodium lactate dehydrogenase. A subset of more than 20,000 extracts from the MEDINA microbial products collection has been explored, leading to the discovery of 3 new compounds with antimalarial activity. In addition, we report on the novel antiplasmodial activity of 4 previously described natural products.
YR 2016
FD 2016-01-06
LK http://hdl.handle.net/10668/9706
UL http://hdl.handle.net/10668/9706
LA en
DS RISalud
RD Sep 26, 2025