Anti-tumor activity and mechanism of T03 in vitro and in vivo.
- Author:
Ke TANG
;
Han-Ze YANG
;
Yan LI
;
Kang TIAN
;
Chao LI
;
Wan-Qi ZHOU
;
Fei NIU
;
Zhi-Qiang FENG
;
Xiao-Guang CHEN
- Publication Type:Journal Article
- MeSH:
Animals;
Antineoplastic Agents;
pharmacology;
Apoptosis;
drug effects;
Carcinoma, Hepatocellular;
pathology;
Cell Cycle Checkpoints;
drug effects;
Cell Proliferation;
drug effects;
Hep G2 Cells;
drug effects;
Humans;
Liver Neoplasms;
pathology;
Signal Transduction;
drug effects;
Xenograft Model Antitumor Assays
- From:
Acta Pharmaceutica Sinica
2014;49(6):861-868
- CountryChina
- Language:Chinese
-
Abstract:
The purpose of this study is to investigate the activity and mechanism of a new anti-tumor agent T03. MTT and colony formation assay were performed to determine anti-proliferation activity of T03 in vitro. Antitumor activity was observed by Renca xenograft model in vivo. The effect of T03 on cell cycle and apoptosis were measured by FCM analysis. Western blotting was performed to investigate the expression level of proteins in HepG2 cell lines treated with T03. T03 had anti-tumor activity by inhibiting tumor cell growth and colony formation in vitro, especially on hepatocellular carcinoma cells (HCC). At the concentration of 10 micromol x L(-1), T03 induced cell apoptosis and cell cycle arrest in HCC. Moreover, it proved that T03 reduced the tumor weight with the rate of 42.30% without any obviously side effect in Renca xenograft model. At the concentration of 2.0 micromol x L(-1), T03 was able to reduce the level of p-c-Raf (Ser259), and thus blocked Raf/MEK/ERK and AKT signaling in HepG2 cell lines. The result suggested that T03 has the potential to inhibit cell proliferation and induce cell apoptosis both in vitro and in vivo, particularly active against HCC, indicating T03 and its analogues may serve as a new anti-cancer drug against hepatocellular carcinoma.
