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F16 Hybrids Derived from Steviol or Isosteviol Are Accumulated in the Mitochondria of Tumor Cells and Overcome Drug Resistance. | LitMetric

F16 Hybrids Derived from Steviol or Isosteviol Are Accumulated in the Mitochondria of Tumor Cells and Overcome Drug Resistance.

Molecules

Hematology/Oncology, Medical Faculty, University Clinic for Internal Medicine IV, Martin-Luther University Halle-Wittenberg, Ernst-Grube Str. 40, D-06120 Halle (Saale), Germany.

Published: January 2024

AI Article Synopsis

  • Steviol and isosteviol were transformed into lipophilic F16 hybrids using the sweetener stevioside, and their cytotoxic effects were tested through SRB assays.
  • The effectiveness of these compounds depended on the specific aromatic substitutions and the length of the spacer, with one compound showing an IC (A2780) value of 180 nM, outperforming similar rhodamine hybrids.
  • Some F16 hybrids also demonstrated the ability to overcome drug resistance in specific cancer models and exhibited a similar accumulation pattern in mitochondria and other cellular areas.

Article Abstract

Steviol and isosteviol were prepared from the commercially available sweetener stevioside and converted into lipophilic F16 hybrids. Their cytotoxicity was determined in SRB assays and showed to depend on both the substitution pattern of the aromatic substituent as well as on the spacer length. Therefore, compound held an IC (A2780) of 180 nM, thus surpassing the activity of comparable rhodamine hybrids. Several of the compounds were also able to overcome drug resistance in the A2780/A2780cis model. Extra staining experiments showed a similar subcellular accumulation pattern of the F16 hybrids as a well-established mitocan, hence proving preferential mitochondrial accumulation but also some other accumulation in other cellular areas.

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Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC10821019PMC
http://dx.doi.org/10.3390/molecules29020381DOI Listing

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