The Imidazacridine Derivative LPSF/AC-05 Induces Apoptosis, Cell Cycle Arrest, and Topoisomerase II Inhibition in Breast Cancer, Leukemia, and Lymphoma.

التفاصيل البيبلوغرافية
العنوان:	The Imidazacridine Derivative LPSF/AC-05 Induces Apoptosis, Cell Cycle Arrest, and Topoisomerase II Inhibition in Breast Cancer, Leukemia, and Lymphoma.
المؤلفون:	de Oliveira Chagas MB; Laboratory for Immunomodulation and New Therapeutic Approaches, Federal University of Pernambuco (UFPE), Brazil., Mendonça da Costa VC; Laboratory for Immunomodulation and New Therapeutic Approaches, Federal University of Pernambuco (UFPE), Brazil., Montenegro C; Laboratory for Immunomodulation and New Therapeutic Approaches, Federal University of Pernambuco (UFPE), Brazil., Alves de Lima MDC; Laboratory for Planning and Drug Synthesis, Federal University of Pernambuco (UFPE), Brazil., Melgarejo da Rosa M; Laboratory for Immunomodulation and New Therapeutic Approaches, Federal University of Pernambuco (UFPE), Brazil., Pereira MC; Laboratory for Immunomodulation and New Therapeutic Approaches, Federal University of Pernambuco (UFPE), Brazil., Barreto de Melo Rêgo MJ; Laboratory for Immunomodulation and New Therapeutic Approaches, Federal University of Pernambuco (UFPE), Brazil., Pitta MGDR; Laboratory for Immunomodulation and New Therapeutic Approaches, Federal University of Pernambuco (UFPE), Brazil.
المصدر:	Current cancer drug targets [Curr Cancer Drug Targets] 2024 Jul 05. Date of Electronic Publication: 2024 Jul 05.
Publication Model:	Ahead of Print
نوع المنشور:	Journal Article
اللغة:	English
بيانات الدورية:	Publisher: Bentham Science Publishers Country of Publication: Netherlands NLM ID: 101094211 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1873-5576 (Electronic) Linking ISSN: 15680096 NLM ISO Abbreviation: Curr Cancer Drug Targets Subsets: MEDLINE
أسماء مطبوعة:	Original Publication: Hilversum, The Netherlands ; Boca Raton, FL : Bentham Science Publishers, c2001-
مستخلص:	Introduction: Cancer is the major cause of morbidity and mortality worldwide. Current treatments for both solid and hematological tumors are associated with severe adverse effects and drug resistance, necessitating the development of novel selective antineoplastic drugs. Methods: The present study describes the antitumor activity of the imidazacridine derivative 5-acridin-9-ylmethylidene-2-thioxoimidazolidin-4-one (LPSF/AC05) in breast cancer, leuke-mia, and lymphoma cells. Cytotoxicity assays were performed in PBMC and in breast cancer, leukemia, and lymphoma cell lines using the MTT method. Changes in cell cycle progression and apoptosis were assessed using flow cytometry. Moreover, topoisomerase II inhibition as-says were performed. LPSF/AC05 exhibited cytotoxicity in six of the nine cell lines tested. Results: The best results for leukemia and lymphoma were observed in the Toledo, Jurkat, and Raji cell lines (IC50 = 27.18, 31.04, and 33.36 M, respectively). For breast cancer, the best re-sults were observed in the triple-negative cell line MDA-MB-231 (IC50 = 27.54 μM). The compound showed excellent selectivity, with no toxicity to normal human cells (IC50 > 100M; selectivity index > 3). Cell death was primarily induced by apoptosis in all cell lines. Furthermore, LPSF/AC05 treatmentinduced cell cycle arrest at the G0/G1 phase in leuke-mia/lymphoma and at the G2/M phase in breast cancer. Conclusion: Finally, topoisomerase II was inhibited. These results indicate the potential ap-plication of LPSF/AC05 in cancer therapy. (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)
فهرسة مساهمة:	Keywords: Cancer therapy; LPSF/AC05; antineoplastic drugs; imidazacridine derivative; solid and hematological tumors.
تواريخ الأحداث:	Date Created: 20240710 Latest Revision: 20240710
رمز التحديث:	20240710
DOI:	10.2174/0115680096290753240613114122
PMID:	38982694
قاعدة البيانات:	MEDLINE

الوصف
تدمد:	1873-5576
DOI:	10.2174/0115680096290753240613114122