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  • Title: LYG-202, a new flavonoid with a piperazine substitution, shows antitumor effects in vivo and in vitro.
    Author: Zeng S, Liu W, Nie FF, Zhao Q, Rong JJ, Wang J, Tao L, Qi Q, Lu N, Li ZY, Guo QL.
    Journal: Biochem Biophys Res Commun; 2009 Aug 07; 385(4):551-6. PubMed ID: 19481059.
    Abstract:
    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.
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