Effects of Troponoids on Mitochondrial Function and Cytotoxicity

Author:

Bradley Daniel P.12,O’Dea Austin T.1,Woodson Molly E.12,Li Qilan12,Ponzar Nathan L.12,Knier Alaina12,Rogers Bruce L.3,Murelli Ryan P.45,Tavis John E.12ORCID

Affiliation:

1. Saint Louis University School of Medicine, St. Louis, Missouri, USA

2. Saint Louis University Institute for Drug and Biotherapeutic Innovation, St. Louis, Missouri, USA

3. Casterbridge Pharmaceuticals, Woburn, Massachusetts, USA

4. Brooklyn College, City University of New York, New York, New York, USA

5. Ph.D. Program in Chemistry, The Graduate Center of The City University of New York, New York, New York, USA

Abstract

The α-hydroxytropolones (αHTs) are troponoid inhibitors of hepatitis B virus (HBV) replication that can target HBV RNase H with submicromolar efficacies. αHTs and related troponoids (tropones and tropolones) can be cytotoxic in cell lines as measured by 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2 H -tetrazolium (MTS) assays that assess mitochondrial function. Previous studies suggest that tropolones induce cytotoxicity through inhibition of mitochondrial respiration.

Funder

HHS | National Institutes of Health

Small Business Innovation Research

Publisher

American Society for Microbiology

Subject

Infectious Diseases,Pharmacology (medical),Pharmacology

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