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LYG-202, a new flavonoid with a piperazine substitution, shows antitumor effects in vivo and in vitro.

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.
AuthorsShi Zeng, Wei Liu, Fei-Fei Nie, Qing Zhao, Jing-Jing Rong, Jia Wang, Lei Tao, Qi Qi, Na Lu, Zhi-Yu Li, Qing-Long Guo
JournalBiochemical and biophysical research communications (Biochem Biophys Res Commun) Vol. 385 Issue 4 Pg. 551-6 (Aug 7 2009) ISSN: 1090-2104 [Electronic] United States
PMID19481059 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Antineoplastic Agents
  • Flavones
  • Flavonoids
  • LYG 202
  • Piperazines
  • piperazine
Topics
  • Animals
  • Antineoplastic Agents (chemistry, pharmacology)
  • Apoptosis
  • Cell Line, Tumor
  • Cell Proliferation (drug effects)
  • Cell Survival (drug effects)
  • Flavones (chemistry, pharmacology)
  • Flavonoids (chemistry, pharmacology)
  • Humans
  • Male
  • Membrane Potential, Mitochondrial (drug effects)
  • Mice
  • Mice, Inbred ICR
  • Piperazines (chemistry, pharmacology)
  • Signal Transduction (drug effects)
  • Xenograft Model Antitumor Assays

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