Table 3.
Studies of prodrug application in cell lines or in vivo.
| Study (Year) | Prodrug | Types of Samples Tested | Methodological Approach * | Ref. |
|---|---|---|---|---|
| Steinbach et al. (1995) | 5-ALA | In vitro ● Human urothelial cancer J82 and RT4 cells ● Human normal urothelial HCV29 cells ● Human umbilical cord endothelial cells ● Human fibroblasts |
30–300 µg/mL 5-ALA in serum-containing medium for 4 h at 37 °C | [59] |
| Riesenberg et al. (1996) | 5-ALA | In vitro ● Human urothelial cancer J82 and RT4 cells ● Human normal urothelial HCV29 cells |
25–100 µg/mL 5-ALA in serum-containing RPMI 1640 medium for 4 h at 37 °C | [60] |
| Li et al. (1999) [61] | 5-ALA | In vivo ● Balb/c mice with fibrosarcoma In vitro ● Mouse normal fibroblasts ● Mouse fibrosarcoma cells ● Human bladder carcinoma T24 cells ● Human lung cancer A549 cells |
In vivo ●100–300 mg 5-ALA per kg of body weight, injected intraperitoneally for 3 h In vitro ●3mM 5-ALA in RPMI-1640 medium with 1% FCS for 15 h at 37 °C |
[61] |
| Krieg et al. (2000) | 5-ALA | In vitro ● Human urothelial cancer J82 and RT4 cells ● Human normal urothelial UROtsa cells ● Human fibroblasts |
10–200 µg/mL 5-ALA in serum-free medium for 3 h at 37 °C | [78] |
| Seidl et al. (2001) | 5-ALA | In vitro ● Human urothelial cancer RT4 cells ● Human normal urothelial UROtsa cells |
100 and 200 µg/mL 5-ALA in serum-free medium for 3 and 1 h at 37 °C | [62] |
| Inoue et al. (2009) | 5-ALA | In vitro ● Human urothelial cancer 253J-P, 253J-BV, T24 cells ● Human prostate carcinoma PC-3 and DU145 cells ● Human renal carcinoma ACHN, 786-o and A-498 cells ● Human renal epithelial RPTEC cells |
0–1 mM 5-ALA in serum-free medium for 0-6 h at 37 °C | [80] |
| Chan et al. (2019) | HAL | Ex vivo ● Trypsinized cells (human bladder cancer HT1197 and HT1376; human fibroblast HFF) in suspension |
10–150 µM HAL in serum-free medium for 30 min to 6 h at 37 °C | [71] |
| Shirazi et al. (2020) | HAL | Ex vivo ● Trypsinized cells (human prostate LNCaP; human normal prostate epithelium PNT2) in suspension |
50–150 µM HAL in PBS for 30 min to 2 h at 4, 23 and 37 °C | [82] |
| Crnolatac (2005) | Hypericin and its derivatives | In vitro ● Human bladder carcinoma RT112 cells |
1 µM hypericin/hypericin derivatives in MEM for 2 h at 37 °C | [75] |
* only the conditions for 5-ALA- or HAL-induced PpIX fluorescence measurements were noted. ALA: aminolevulinic acid; HAL: hexyl aminolevulinate or hexaminolevulinate; MAL: methyl aminolevulinate; MEM: minimum essential medium.