FCY-302, a novel small molecule, induces apoptosis in leukemia and myeloma cells by attenuating key anti-oxidant and mitochondrial enzymes.

FCY-302, a novel small molecule, induces apoptosis in leukemia and myeloma cells by attenuating key anti-oxidant and mitochondrial enzymes. Oncol Res. 2019 Apr 17;: Authors: Rajagopalan P, Hakami A, Ragab M, Elbessoumy A Abstract Arylidene analogues 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 anti-apoptotic Bcl-2 levels and increased pro apoptotic Bax proteins in leukemia and myeloma cell lines. FCY-302attenuated 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, GST in all the three cancer cells tested. Our findings suggest FCY-302 to inhibit the proliferation of leukemia and myeloma cancer cells by altering key mitochondrial and anti-oxidant enzymes, eventually driving them to apoptosis. These results drive focus on FCY-302 and its analogues to be developed as potential small molecules with bioactivities against cancer. PMID: 31046873 [PubMed - as supplied by publisher]
Source: Oncology Research - Category: Cancer & Oncology Tags: Oncol Res Source Type: research