Description
Reticulol is an isocoumarin derivative produced by certain species of
Streptomyces that inhibits cAMP phosphodiesterase (IC
50 = 41 μM). It also inhibits DNA topoisomerase I when used at a concentration of 45 μM in B16F10 melanoma cells. Reticulol has antifungal activity against
T. mentagrophyes with a MIC of 1.8 μM. It is cytotoxic against A427 human lung and B16F10 mouse melanoma cells at concentrations of 25 and 200 μM, respectively, and inhibits lung metastasis in mice.
Uses
Reticulol is an isocoumarin metabolite shown to inactivate topoisomerase I.
Uses
Reticulol is an isocoumarin metabolite produced by selected species of Streptomyces. Reticulol was first described as a potent inhibitor of cyclic nucleotide phosphodiesterase but more recent research has demonstrated a topoisomerase I inactivation mechanism. Reticulol also causes dose dependent inhibition of lung metastasis in the B16F10 melanoma model.
in vivo
Reticulol (10 mg/kg, 50 mg/kg; iv; day 3 and day 5 after tumor implanted) inhibits tumor growth in mice bearing B16F10 melanoma, and shows lung metastasis-blocking effect[1].
| Animal Model: | Pathogen-free female C57BL/6J mice[1] |
| Dosage: | 10 mg/kg, 50 mg/kg |
| Administration: | IV via the tail vein; day 3 and day 5 after tumor implanted |
| Result: | Inhibited tumor growth.
|
References
[1] L A MITSCHER W M W W Andres. Reticulol, a new metabolic isocoumarin.[J]. Experientia, 1964, 20 5: 258-259. DOI:
10.1007/bf02151790[2] Y FURUTANI. Reticulol, an inhibitor of cyclic adenosine 3’, 5’-monophosphate phosphodiesterase.[J]. Journal of Antibiotics, 1975, 28 7: 558-560. DOI:
10.7164/antibiotics.28.558[3] DAE-SEOG LIM. Topoisomerase I inactivation by reticulol and its in vivo cytotoxicity against B16F10 melanoma.[J]. Chemotherapy, 2003, 49 5: 257-263. DOI:
10.1159/000072451[4] DAE-SEOG LIM. Antitumor efficacy of reticulol from Streptoverticillium against the lung metastasis model B16F10 melanoma. Lung metastasis inhibition by growth inhibition of melanoma.[J]. Chemotherapy, 2003, 49 3: 146-153. DOI:
10.1159/000070621
