ANTILEUKEMIC AND IMMUNOMODULATORY POTENTIAL OF A TRIAZOLOPYRIMIDINE DERIVATIVE IN K-562 CELLS AND HUMAN PERIPHERAL BLOOD MONONUCLEAR CELLS

@article{oliveira2026antileukemic,
  title = {{ANTILEUKEMIC AND IMMUNOMODULATORY POTENTIAL OF A TRIAZOLOPYRIMIDINE DERIVATIVE IN K-562 CELLS AND HUMAN PERIPHERAL BLOOD MONONUCLEAR CELLS}},
  author = {Regiane Costa OLIVEIRA and Gemilson Soares PONTES and Brad Lira SALES and Juniel Assis Crespo NETO and Claudio Lucas Santos CATÃO and Georgyi KOIDAN and Aleksandr KOSTYUK and Anastasia HURIEVA and Allyson Guimarães COSTA},
  journal = {Hematology, Transfusion and Cell Therapy},
  year = {2026},
  month = oct,
  doi = {10.1016/j.htct.2026.107485},
  url = {https://doi.org/10.1016/j.htct.2026.107485},
  note = {CC BY},
}

TY  - JOUR
TI  - ANTILEUKEMIC AND IMMUNOMODULATORY POTENTIAL OF A TRIAZOLOPYRIMIDINE DERIVATIVE IN K-562 CELLS AND HUMAN PERIPHERAL BLOOD MONONUCLEAR CELLS
AU  - Regiane Costa OLIVEIRA
AU  - Gemilson Soares PONTES
AU  - Brad Lira SALES
AU  - Juniel Assis Crespo NETO
AU  - Claudio Lucas Santos CATÃO
AU  - Georgyi KOIDAN
AU  - Aleksandr KOSTYUK
AU  - Anastasia HURIEVA
AU  - Allyson Guimarães COSTA
PY  - 2026
DA  - 2026/10/23
JO  - Hematology, Transfusion and Cell Therapy
DO  - 10.1016/j.htct.2026.107485
UR  - https://doi.org/10.1016/j.htct.2026.107485
AB  - Background: Chronic myeloid leukemia (CML) is a myeloproliferative neoplasm characterized by the presence of the BCR-ABL1 fusion tyrosine kinase, whose constitutive activity activates oncogenic signaling pathways that promote uncontrolled cell proliferation, inhibition of apoptosis, and enhanced survival of myeloid cells. Triazolopyrimidine derivatives have emerged as promising antineoplastic agents due to their ability to regulate cell proliferation, apoptosis, and immune signaling, as well as to modulate the tumor microenvironment, highlighting their potential as novel therapeutic candidates for CML. Aim: Investigate the anti-proliferative and immunomodulatory potential of a triazolopyrimidine-derived in chronic myeloid leukemia cells and peripheral blood mononuclear cells (PBMCs). Materials and methods: The antiproliferative activity of the triazolopyrimidine derivative was determined by the MTT colorimetric assay. K-562 chronic myeloid leukemia cells, healthy human peripheral blood mononuclear cells (PBMCs), and Vero cells (Cercopithecus aethiops) were treated with the compound at concentrations ranging from 3 to 100 μg/mL for 24, 48, and 72 h to evaluate cytotoxicity and selectivity. For immunomodulatory analysis, human PBMCs and K-562 cells were stimulated with lipopolysaccharide (LPS) and subsequently treated with the compound at its IC50 concentration. The levels of the cytokines IFN-γ, TNF-α, IL-4, and IL-10 in cell culture supernatants were quantified by flow cytometry using the Cytometric Bead Array (CBA) assay. Results and discussion: The triazolopyrimidine derivative exhibited potent antileukemic activity against K-562 cells, with an IC50 of 6.72 μM, while showing no significant cytotoxicity toward healthy human peripheral blood mononuclear cells (PBMCs) or Vero cells, indicating selective antitumor activity. In LPS-stimulated human PBMCs and K-562 cells, treatment with the compound at the IC50 concentration significantly reduced the production of the Th1 cytokine IFN-γ and the pro-inflammatory cytokine TNF-α. Conversely, the levels of the Th2 cytokine IL-4 and the regulatory cytokine IL-10 were increased. Although IL-10 can exert immunosuppressive effects in certain tumor contexts, its increase in the present study, associated with the significant reduction in TNF-α and IFN-γ, suggests a balanced immunomodulatory effect, and not a generalized suppression of the immune response. This modulation of the cytokine profile indicates that, in addition to its direct cytotoxic effects, the triazolopyrimidine derivative may influence immune signaling pathways associated with leukemia progression. Conclusion: The triazolopyrimidine derivative demonstrated selective antiproliferative activity against chronic myeloid leukemia cells, combined with a pronounced immunomodulatory effect characterized by suppression of pro-inflammatory cytokines and enhancement of anti-inflammatory mediators. These findings suggest that this compound represents a promising candidate for the development of novel therapeutic strategies targeting hematological malignancies and inflammatory disorders. Nevertheless, further in vivo studies are required to elucidate the underlying mechanisms and confirm its therapeutic efficacy and safety.
SN  - 2531-1379
SN  - 2531-1387
ER  -