Study summary · research use only
Antiviral activity of sertindole, raloxifene and ibutamoren against transcription and replication-competent Ebola virus-like particles
Plain-language summary
Paraphrased from the published abstract below — not a verdict on whether anything works.
In this cell-based study (species not specified), a chemical library of drug-like compounds was screened using a transcription and replication-competent Ebola virus-like particle system. The abstract reports dose-dependent inhibition of Ebola replication by 15 hit compounds, mostly targeting G protein-coupled receptors, grouped by chemical structure into diphenylmethane derivatives, promazine derivatives, and a third group including sertindole, raloxifene, and ibutamoren, which showed antiviral effects, downregulated viral VP40 matrix protein and envelope glycoprotein expression, and reduced EBOV-derived minigenome RNA in progeny particles. Ibutamoren, a growth hormone secretagogue receptor agonist, is reported as having the most prominent antiviral activity among the tested compounds, with a 50% concentration value of 0.2 μM against replication, a 50% cytotoxic concentration of 42.4 μM, and a selectivity index of 222.8.
Abstract
A chemical library comprising 2,354 drug-like compounds was screened using a transcription and replication-competent viruslike particle (trVLP) system implementing the whole Ebola virus (EBOV) life cycle. Dose-dependent inhibition of Ebola trVLP replication was induced by 15 hit compounds, which primarily target different types of G protein-coupled receptors (GPCRs). Based on the chemical structure, the compounds were divided into three groups, diphenylmethane derivatives, promazine derivatives and chemicals with no conserved skeletons. The third group included sertindole, raloxifene, and ibutamoren showing prominent antiviral effects in cells. They downregulated the expression of viral proteins, including the VP40 matrix protein and the envelope glycoprotein. They also reduced the amount of EBOV-derived tetracistronic minigenome RNA incorporated into progeny trVLPs in the culture supernatant. Particularly, ibutamoren, which is a known agonist of growth hormone secretagogue receptor (GHSR), showed the most promising antiviral activity with a 50% effective concentration of 0.2 μM, a 50% cytotoxic concentration of 42.4 μM, and a selectivity index of 222.8. Here, we suggest a strategy for development of anti-EBOV therapeutics by adopting GHSR agonists as hit compounds. [BMB Reports 2020; 53(3): 166-171].
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