Antitumor effect of TW-37, a BH3 mimetic in human oral cancer

• Main Authors: Chi-Hyun Ahn, Won Woo Lee, Yun Chan Jung, Ji-Ae Shin, Kyoung-Ok Hong, Sujung Choi, Neeti Swarup, Jihoon Kim, Min-Hye Ahn, Minjung Jung, Sung-Dae Cho, Bohwan Jin
• Format: Article
• Language: English
• Published: BMC 2019-12-01
• Series: Laboratory Animal Research
• Subjects: TW-37; Apoptosis; Bcl-2; Oral cancer
• Online Access: https://doi.org/10.1186/s42826-019-0028-7

Abstract TW-37 is a small molecule B cell lymphoma-2 (Bcl-2) homology 3 mimetic with potential anticancer activities. However, the in vivo anti-cancer effect of TW-37 in human oral cancer has not been properly studied yet. Here, we attempted to confirm antitumor activity of TW37 in human oral cancer. TW-37 significantly inhibited cell proliferation and increased the number of dead cells in MC-3 and HSC-3 human oral cancer cell lines. TW-37 enhanced apoptosis of both cell lines evidenced by annexin V/propidium iodide double staining, sub-G1 population analysis and the detection of cleaved poly (ADP-ribose) polymerase and caspase-3. In addition, TW-37 markedly downregulated the expression of Bcl-2 protein, while not affecting Bcl-xL or myeloid cell leukemia-1. In vivo, TW-37 inhibited tumor growth in a nude mice xenograft model without any significant liver and kidney toxicities. Collectively, these data reveal that TW-37 may be a promising small molecule to inhibit human oral cancer.