Lysosomal Trapping (Lysosomotropism)

Introduction

Background information:
  • Lysosomes are essential for the degradation of old organelles and engulfed microbes and also play a role in programmed cell death1.
  • Lysosomotropic agents e.g., chloroquine, accumulate preferentially in the lysosomes of cells in the body.
  • These agents tend to have both lipophilic or amphiphilic compounds with basic moieties. Once inside the acidic environment of the lysosome, the drug becomes protonated and trapped in the organelle2.
  • Trapping of drugs in the lysosome may be one mechanism leading to drug-induced phospholipidosis for cationic amphiphilic drugs (CAD).
  • Cyprotex’s lysosomal trapping service is a cell based assay which uses high content screening to identify both lysosomotropism and cytotoxicity according to a recently published method2.

Protocol

Lysosomal Trapping Cell-based Assay Protocol

Data

Data for Lysosomal Trapping

Known lysosomotropic and non-lysosomotropic agents were screened in the lysosomal trapping assay. Data generated were compared to those published in the literature.

References

1) Turk B and Turk V (2009) J Biol Chem 284; 21783-21787
2) Nadanaciva S et al., (2011) Toxicology In Vitro 25; 715-723
3) Kazmi F et al., (2013) Drug Metab Dispos 41; 897-905

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Caroline Bauch

Caroline Bauch

Principal Scientist

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Cyprotex enables and enhances the prediction of human exposure, clinical efficacy and toxicological outcome of a drug or chemical. By combining quality data from robust in vitro methods with contemporary in silico technology, we add value, context and relevance to the ADME-Tox data supplied to our partners in the pharmaceutical or chemical industries.