| 19481059 |
Zeng S, Liu W, Nie FF, Zhao Q, Rong JJ, Wang J, Tao L, Qi Q, Lu N, Li ZY, Guo QL: LYG-202, a new flavonoid with a piperazine substitution, shows antitumor effects in vivo and in vitro. Biochem Biophys Res Commun. 2009 Aug 7;385(4):551-6. Epub 2009 May 27.
LYG-202 is a newly synthesized flavonoid with a piperazine substitution. We investigated the antitumor effect of LYG-202 in vivo and in vitro. We show that, LYG-202 significantly decreases tumor growth in mice inoculated with S180 sarcoma cells, compared with the control group. Meanwhile, the viabilities of various kinds of tumor cells were inhibited by LYG-202 with IC (50) values in the range of 4.80 to 27.70 microM. Then apoptosis induced by LYG-202 in HepG2 cells was characterized by DAPI staining and Annexin V/PI double staining and degradation of PARP was observed. Activation of the caspase cascade for both the extrinsic and intrinsic pathways was demonstrated, including caspase-8, -9, and -3. The results also showed that the expression of Bcl-2 protein decreased whereas that of Bax protein increased, leading to an increase of the Bax/Bcl-2 ratio. Our results demonstrated that LYG-202 exhibited strong antitumor effect in vivo and in vitro, involving with apoptosis induction. |
1(0,0,0,1) |