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RESEARCH PRODUCT
The effects of the macrocyclic lactone bryostatin-1 on leukemic cells in vitro.
Robert PettitCitarrella PVincenzo MiserendinoVittorio GebbiaRoberto ValenzaStratford W. MayAntonio PestaNicolò Borsellinosubject
Cancer ResearchBryostatin 1LymphomaHL60Antineoplastic AgentsAntileukemic agent030218 nuclear medicine & medical imaging03 medical and health scienceschemistry.chemical_compoundLactones0302 clinical medicinehemic and lymphatic diseasesmedicineTumor Cells CulturedHumansClonogenic assayTumor Stem Cell AssayLeukemiaChemistryMyeloid leukemiaGeneral Medicinemedicine.diseaseBryostatinsHaematopoiesisLeukemiaOncology030220 oncology & carcinogenesisCancer researchMacrolidesDrug Screening Assays AntitumorK562 cellsdescription
The macrocyclic lactone bryostatin-1 was found to exert in vitro antineoplastic activity against several leukemic cell lines, including human K562 erythroleukemia, HL60 promyelocytic leukemia, REH and MOLT-4 lymphoblastic leukemias, CCRFCEM lymphoma, KG-1 myeloid leukemia, and murine P388 lymphocytic leukemia. No statistically significant difference in sensitivity to bryostatin-1 was found between adriamycin-resistant P388 and K526 subclones and their sensitive counterparts. Freshly explanted clonogenic leukemic cells showed a variable sensitivity to bryostatin-1 in 10/12 tested samples. The IC50 of clonogenic leukemic cells was 4 × 10–3 M bryostatin-1, and that of normal marrow CFU-GM was 10–5 M. Leukemic cells exposed to bryostatin-1 showed a variable degree of monocytic differentiation as evaluated by ANAE staining and morphology. Bryostatin-1 is also able to inhibit the growth of CFU-GM from myelodysplastic marrow and to shorten the duration of dysplastic hematopoiesis in liquid culture. In conclusion, these data suggest that bryostatin-1 is a potent antileukemic agent in vitro that may be potentially useful for clinical studies.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 1992-06-01 | Tumori |