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Tetra-arylborate lipophilic anions as targeting groups
Kishore K Gaddale Devanna1, Justyna M Gawel, Tracy A Prime
1School of Chemistry, University of Glasgow, Glasgow, G12 8QQ, UK. Richard.Hartley@glasgow.ac.uk.
Chemical Communications (Cambridge, England)
|February 26, 2021
Summary
Tetraphenylborate (TPB) anions cross cell membranes but avoid mitochondria. TPB-conjugates enter cells and accumulate in lysosomes, enabling novel probes and bioactive molecules.
Area of Science:
- Biochemistry
- Cell Biology
- Membrane Transport
Background:
- Tetraphenylborate (TPB) anions are known to cross cell membranes.
- Mitochondrial membrane potential (Δψ) typically excludes TPB anions.
- The behavior of TPB-conjugates in cellular uptake was previously uncharacterized.
Purpose of the Study:
- To investigate the cellular distribution of tetraphenylborate (TPB) anions and their conjugates.
- To determine the influence of mitochondrial membrane potential (Δψ) on TPB-conjugate localization.
- To explore the potential of TPB-conjugates for targeted delivery to intracellular organelles.
Main Methods:
- Utilized TPB-conjugates for cellular uptake studies.
- Monitored distribution across cell membranes in response to membrane potential (Δψ).
- Investigated intracellular accumulation using fluorescence microscopy and endocytosis pathway analysis.
Main Results:
- TPB-conjugates rapidly entered cells, contrary to the exclusion of TPB anions from mitochondria.
- Accumulation of TPB-conjugates was observed within lysosomes following endocytosis.
- Lysosomal targeting was independent of pH, indicating a distinct mechanism.
Conclusions:
- TPB-conjugates exhibit unique cellular uptake and localization properties.
- Lysosomal accumulation of TPB-conjugates offers a novel, pH-independent targeting strategy.
- This finding opens avenues for developing new lysosome-targeted probes and bioactive molecules.
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