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LYG-202, a new flavonoid with a piperazine substitution, shows antitumor effects in vivo and in vitro
- Source :
- Biochemical and biophysical research communications. 385(4)
- Publication Year :
- 2009
-
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.
- Subjects :
- Male
Cell Survival
Poly ADP ribose polymerase
Biophysics
Antineoplastic Agents
Apoptosis
Biochemistry
Piperazines
chemistry.chemical_compound
Mice
In vivo
Annexin
Cell Line, Tumor
Animals
Humans
DAPI
Molecular Biology
Piperazine
Caspase
Cell Proliferation
Flavonoids
Membrane Potential, Mitochondrial
Mice, Inbred ICR
biology
Cell Biology
Flavones
Molecular biology
Xenograft Model Antitumor Assays
In vitro
chemistry
Cell culture
biology.protein
Signal Transduction
Subjects
Details
- ISSN :
- 10902104
- Volume :
- 385
- Issue :
- 4
- Database :
- OpenAIRE
- Journal :
- Biochemical and biophysical research communications
- Accession number :
- edsair.doi.dedup.....35d6b6883571fcf15f8f929bfc5ab5ae