ANTI-CANCER EFFECTS OF A NOVEL TAMOXIFEN ANALOG (SP-1) ON U87 GLIOBLASTOMA CELL LINE

• Published in: The Ohio journal of science Vol. 117; no. 1; pp. A28 - A29
• Main Authors: Frendo, Samson M, Aulthouse, Amy L, Kinder, David H
• Format: Journal Article
• Language: English
• Published: Columbus Ohio Academy of Science 01.04.2017
• Subjects: Anticancer properties; Brain; Brain cancer; Brain tumors; Cancer; Cell morphology; Colonies; Cytology; Cytotoxicity; Estrogens; Glioblastoma; Glioblastoma cells; Low temperature; Mitosis; Monolayers; Morphology; Receptors; Tamoxifen; Toxicity
• ISSN: 0030-0950; 2471-9390

Glioblastoma is the most common and deadliest form of malignant primary brain tumors. The Sigma-2 receptor is known to be present in glioblastoma cells, and agonists of sigma-2 receptors are known to have cytotoxic and anti-proliferative effects on cancer cells. A unique compound designed to bind sigma-2 receptors, SP-1, with structural similarities to the drug Tamoxifen, was synthesized with the removal of the estrogen receptor binding portions. U87 glioblastoma cells were grown in monolayer or a single-cell suspension in low temperature agarose. They were then fed DMEM containing 10% FCS and incubated at 37°C. Cells in agarose were treated with Tamoxifen (5pM, 10pM) and SP-1 (18pM, 35pM) with triplicate cultures per treatment. Cell morphology, mitotic activity, and cytotoxicity were noted at half-week intervals for a period of 1.5 weeks. All agarose cultures were stained with trypan blue to assess viability; living and nonliving single cells and colonies with dead were counted. Statistical comparisons were made using a t-test and reported as significant at or below the 95% CI. As noted in monolayer, cellular processes occurred in single cells and colonies in agarose under vehicle and normal controls. Process extension significantly decreased over time as treatment concentrations increased. Continuous exposure to vehicle control (0.1% DMSO) did not have a significant effect on mitosis or cell viability when compared to untreated controls. The Tamoxifen and SP-1 treatments at all concentrations showed significant cytotoxic and antimitotic effects after 1.5 weeks. Future studies will elucidate the mechanism by which cytotoxicity and antimitotic activity occur.