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FCY-302, a Novel Small Molecule, Induces Apoptosis in Leukemia and Myeloma Cells by Attenuating Key Antioxidant and Mitochondrial Enzymes

Prasanna Rajagopalan*†, Abdulrahim Hakami*†, Mohammed Ragab*, Ashraf Elbessoumy*‡

* Department of Clinical Laboratory Sciences, College of Applied Medical Sciences, King Khalid University, Abha, Kingdom of Saudi Arabia
† Central Research Laboratory, College of Applied Medical Sciences, King Khalid University, Abha, Kingdom of Saudi Arabia
‡ Department of Biochemistry, Faculty of Science, Alexandria University, Alexandria, Egypt

Oncology Research 2019, 27(8), 957-964. https://doi.org/10.3727/096504019X15555428221646

Abstract

Arylidene analogs are well proven for biological activities. FCY-302, a novel small molecule belonging to this class, was screened for its biological efficacy in leukemia and myeloma cells. FCY-302 selectively inhibited proliferation of cancer cells with GI50 values of 395.2 nM, 514.6 Nm, and 642.4 nM in HL-60, Jurkat, and RPMI-8226 cells, respectively. The compound also increased sub-G0 peak in the cancer cell cycle and favored apoptosis determined by annexin V assay. The compound decreased the antiapoptotic Bcl-2 levels and increased proapoptotic Bax proteins in leukemia and myeloma cell lines. FCY-302 attenuated the mitochondrial membrane-bound Na+ /K+ ATPase, Ca2+ ATPase, and Mg2+ ATPase enzyme activities and significantly decreased activities of antioxidant enzymes like SOD, CAT, GR, and GST in all the three cancer cells tested. Our findings suggest that FCY-302 inhibits the proliferation of leukemia and myeloma cancer cells by altering key mitochondrial and antioxidant enzymes, eventually driving them to apoptosis. These results drive focus on FCY-302 and its analogs to be developed as potential small molecules with bioactivities against cancer.

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APA Style
Rajagopalan, P., Hakami, A., Ragab, M., Elbessoumy, A. (2019). FCY-302, a novel small molecule, induces apoptosis in leukemia and myeloma cells by attenuating key antioxidant and mitochondrial enzymes. Oncology Research, 27(8), 957-964. https://doi.org/10.3727/096504019X15555428221646
Vancouver Style
Rajagopalan P, Hakami A, Ragab M, Elbessoumy A. FCY-302, a novel small molecule, induces apoptosis in leukemia and myeloma cells by attenuating key antioxidant and mitochondrial enzymes. Oncol Res. 2019;27(8):957-964 https://doi.org/10.3727/096504019X15555428221646
IEEE Style
P. Rajagopalan, A. Hakami, M. Ragab, and A. Elbessoumy "FCY-302, a Novel Small Molecule, Induces Apoptosis in Leukemia and Myeloma Cells by Attenuating Key Antioxidant and Mitochondrial Enzymes," Oncol. Res., vol. 27, no. 8, pp. 957-964. 2019. https://doi.org/10.3727/096504019X15555428221646



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