Cidofovir metabolism and cellular incorporation across keratinocyte models
Cell-based study · SiHa and HeLa cervical carcinoma cells; HaCaT immortalized keratinocytes; primary human keratinocytes (PHKs) [1]
The incorporated fraction was higher in carcinoma and immortalized cells than in PHKs. Active diphosphate levels were not significantly different between PHKs and HPV-positive tumor cells, limiting a preferential-activation explanation.
| Endpoint | Reported result | Reference |
|---|---|---|
| Radiolabel in methanol-insoluble cellular nucleic acid fraction, interpreted by the authors as incorporated CDV | pmol per 10^6 cells; mean ± SD SiHa: 18.39 ± 0.54; HeLa: 13.17 ± 1.43; HaCaT: 8.62 ± 1.11; PHKs: 1.96 ± 0.71; two experiments | [1] |
| Intracellular CDV diphosphate in methanol-soluble fraction | pmol per 10^6 cells; mean ± SD SiHa: 3.50 ± 0.02; HeLa: 2.93 ± 0.08; HaCaT: 1.56 ± 0.01; PHKs: 3.56 ± 0.28; two experiments | [1] |
Literature-Reported Treatment Conditions
- Treatment concentration
- 50 μg/ml final CDV; 10 μCi radiolabeled CDV per flask
- Exposure duration
- 72 h
- Method
- Radiolabeled compound incubation; conditions performed in duplicate
- Vehicle
- Tracer supplied in ethanol/water 1:1; final exposure vehicle proportion not specified
- Reported limits
- No final vehicle fraction is specified in the retrieved method. Two experiments are reported; duplicate conditions are not independent experiment counts.
Methods and source locations
Compound reported in the paper: Cidofovir; Compound label in the paper: [5-3H]-CDV tracer
Radiotracer metabolism experiment; no potency estimate or clinical selectivity claim.
Table 1 and footnote; Methods: Antiviral compound, Cell cultures, Metabolism study with [5-3H]-CDV; Results: Metabolism and incorporation
Radiolabel in methanol-insoluble cellular nucleic acid fraction, interpreted by the authors as incorporated CDV: [5-3H]-CDV exposure followed by fractionation and scintillation counting — Table 1: Incorporated CDV row and footnote; Methods: Metabolism study with [5-3H]-CDV
Intracellular CDV diphosphate in methanol-soluble fraction: Anion-exchange HPLC and radiometric detection — Table 1: CDVpp row and footnote; Results: Metabolism and incorporation