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BH3模拟物TW-37对人口腔癌的抗肿瘤作用

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

作者信息

Ahn Chi-Hyun, Lee Won Woo, Jung Yun Chan, Shin Ji-Ae, Hong Kyoung-Ok, Choi Sujung, Swarup Neeti, Kim Jihoon, Ahn Min-Hye, Jung Minjung, Cho Sung-Dae, Jin Bohwan

机构信息

1Department of Oral Pathology, School of Dentistry and Dental Research Institute, Seoul National University, Seoul, 03080 Republic of Korea.

2Laboratory Animal Center, CHA University, CHA Biocomplex, Sampyeong-dong, Seongnam, 13488 Republic of Korea.

出版信息

Lab Anim Res. 2019 Dec 4;35:27. doi: 10.1186/s42826-019-0028-7. eCollection 2019.

DOI:10.1186/s42826-019-0028-7
PMID:32257914
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7081630/
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-G 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.

摘要

TW-37是一种具有潜在抗癌活性的小分子B细胞淋巴瘤-2（Bcl-2）同源结构域3模拟物。然而，TW-37在人类口腔癌中的体内抗癌作用尚未得到充分研究。在此，我们试图证实TW-37在人类口腔癌中的抗肿瘤活性。TW-37显著抑制MC-3和HSC-3人类口腔癌细胞系的细胞增殖并增加死亡细胞数量。通过膜联蛋白V/碘化丙啶双染色、亚G期细胞群分析以及检测裂解的聚（ADP-核糖）聚合酶和半胱天冬酶-3证明，TW-37增强了这两种细胞系的凋亡。此外，TW-37显著下调Bcl-2蛋白的表达，而不影响Bcl-xL或髓样细胞白血病-1。在体内，TW-37在裸鼠异种移植模型中抑制肿瘤生长，且无任何明显的肝肾毒性。总体而言，这些数据表明TW-37可能是一种有前景的抑制人类口腔癌的小分子。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6836/7081630/192b88d1c14f/42826_2019_28_Fig6_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6836/7081630/dcee2f2729d0/42826_2019_28_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6836/7081630/6b6a03761b7a/42826_2019_28_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6836/7081630/711f0db85f91/42826_2019_28_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6836/7081630/85874a650fb3/42826_2019_28_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6836/7081630/023d1b3d6a85/42826_2019_28_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6836/7081630/192b88d1c14f/42826_2019_28_Fig6_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6836/7081630/dcee2f2729d0/42826_2019_28_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6836/7081630/6b6a03761b7a/42826_2019_28_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6836/7081630/711f0db85f91/42826_2019_28_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6836/7081630/85874a650fb3/42826_2019_28_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6836/7081630/023d1b3d6a85/42826_2019_28_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6836/7081630/192b88d1c14f/42826_2019_28_Fig6_HTML.jpg

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