Aspartyl Protease Inhibitors as Anti-Filarial Drugs.

ABSTRACT: The current treatments for lymphatic filariasis and onchocerciasis do not effectively kill the adult parasitic nematodes, allowing these chronic and debilitating diseases to persist in millions of people. Thus, the discovery of new drugs with macrofilaricidal potential to treat these filarial diseases is critical. To facilitate this need, we first investigated the effects of three aspartyl protease inhibitors (APIs) that are FDA-approved as HIV antiretroviral drugs on the adult filarial nematode, Brugia malayi and the endosymbiotic bacteria, Wolbachia. From the three hits, nelfinavir had the best potency with an IC₅₀ value of 7.78 µM, followed by ritonavir and lopinavir with IC₅₀ values of 14.3 µM and 16.9 µM, respectively. The three APIs have a direct e

SUBMITTER: Beld L 

PROVIDER: S-EPMC9227574 | biostudies-literature | 2022 Jun

REPOSITORIES: biostudies-literature