Poly-guanidine shows high cytotoxicity in glioma cell cultures and glioma stem cells

Investigational New Drugs - Tập 40 - Trang 565-575 - 2022
Marcela Márquez1,2, Karl Holmberg Olausson1, Ayodele Alaiya1,3, Sten Nilsson4, Lennart Meurling1, Anders R. Holmberg1
1Department of Oncology-Pathology, Karolinska Institute, Stockholm, Sweden
2Universidad Autónoma de Nuevo León, Centro de Investigación Y Desarrollo en Ciencias de La Salud, Monterrey, Mexico
3Proteomic Unit, Stem Cell and Tissue Re-Engineering Program, King Faisal Specialist Hospital and Research Center, Riyadh, Saudi Arabia
4Department of Oncology Pathology, Karolinska Institute, Stockholm, Sweden

Tóm tắt

Glioblastoma multiforme (GBM) is a malignant CNS tumor with a poor prognosis. GBM shows aberrant glycosylation with hypersialylation. This property is a potential target for therapy. This study investigates the growth inhibitory efficacy of poly-guanidine (GuaDex), with an affinity for sialic acid (Sia). Glioma cell cultures and patient-derived glioma cell lines (PDGCLs) expressing Prominin-1 (CD133) were used. Human fibroblasts and astrocyte-derived cells were used as controls. Temozolomide (standard GBM drug, TMZ) and DMSO were used as a comparison. GuaDex at 1–10 µM concentrations, were incubated for 3.5–72 h and with PDGCLs cells for 6–24 h. The cytotoxicity was estimated with a fluorometric cytotoxicity assay (FMCA). Fluorescence-labelled GuaDex was used to study the cell interactions. Sia expression was confirmed with a fluorescence labelled Sia binding lectin. Expression of glial fibrillary acidic protein was determined. GuaDex induction of growth inhibition was fast, showing after less than 5 min incubation while the control cells were not affected even after 50 min incubation. The growth inhibitory effect on PDGCLs spheroids was persistent still showing after 4 weeks post-treatment. The growth inhibition of GuaDex was induced at low µM concentrations while TMZ induced only a slight inhibition at mM concentrations. GuaDex efficacy appears significant and warrants further studies.

Tài liệu tham khảo

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