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HQS-3, a newly synthesized flavonoid, possesses potent anti-tumor effect in vivo and in vitro.
- Source :
-
European Journal of Pharmaceutical Sciences . Jul2013, Vol. 49 Issue 4, p649-658. 10p. - Publication Year :
- 2013
-
Abstract
- Abstract: HQS-3 is a newly baicalein derivative with a benzene substitution. We investigated the anticancer effect of HQS-3 in vivo and in vitro. HQS-3 significantly decreased tumor growth in mice inoculated with Heps and HepG2 cells; and had little influence on the state and weight of animals. After treatment with 20mg/kg HQS-3, the inhibitory rate of tumor weight in mice inoculated with Heps and HepG2 cells were 63.62% and 68.03%, respectively. Meanwhile, HQS-3 inhibited the viability of various kinds of tumor cells with IC50 values in the range of 22.98–54.32μM after 48h treatment measured by MTT-assay. HQS-3 remarkably inhibited viability of hepatoma cells in a concentration- and time-dependent manner and induced apoptosis in HepG2 cells by DAPI staining and Annexin V/PI double staining. The apoptosis-induction effect of HQS-3 was attributed to its ability to modulate the activity of caspase-9, caspase-3 and PARP. Moreover, the expression of bax protein was increased while the bcl-2 protein was decreased, leading to an increase in Bax/Bcl-2 ratio. The accumulation of ROS induced by HQS-3 in HepG2 cells was also observed. The further results suggested that HQS-3 induced mitochondrial-mediated apoptosis by increasing ROS level and inhibiting the expression of anti-oxidative protein SOD2. HQS-3 exerted anti-tumor activity both in vitro and in vivo via inducing tumor cells apoptosis, and these results suggested that it deserves further investigation as a novel chemotherapy for human tumors. [Copyright &y& Elsevier]
Details
- Language :
- English
- ISSN :
- 09280987
- Volume :
- 49
- Issue :
- 4
- Database :
- Academic Search Index
- Journal :
- European Journal of Pharmaceutical Sciences
- Publication Type :
- Academic Journal
- Accession number :
- 89344840
- Full Text :
- https://doi.org/10.1016/j.ejps.2013.04.016