Medical Mycology: Open Access

Inhibition of VEGF mediated neovascularization, up-regulation of BAX and down regulation of Bcl2 in MDA-MB-231 cell line; Naphthalene chalcone

Synthesis and characterization of (2E)-3-(2-bromo-6-hydroxy- 4-methoxyphenyl)-1-(naphthalene-2-yl) prop-2-en-1- one (d1) by the Claisen–Schmidt condensation method and the resultant compound was characterized by 1H NMR and 13C NMR spectral studies. Compound d1 exhibits incredible anticancer activity on MDA-MB-231 with the IC50 estimations of 6.555 to 10.14 μM. The cell cycle analysis and Annexin V-FITC/PI, treated with d1, confirmed tremendous inhibiting capabilities in the cell cycle and activated apoptosis. The further apoptotic related examination has been finished for the expression level of Caspase 9, and Caspase 3. Supporting this, we overview the in vivo adversary of tumor development and antiangiogenic action of d1 in Ehrlich Ascites Carcinoma (EAC). The d1 treatment inhibited the tumor development and expanded the life expectancy of the EAC-bearing mice without appearing symptoms on healthy mice, as uncovered by histological parameters. The results of compounds d1 showed significant activity at 8.153 μM concentrations in MDA-MB-231 and arrested the G0/ G1 cell cycle. The apoptosis induced in early apoptotic phase and Caspase activation at specified concentration showed significant apoptotic activity. In vivo models in EAC for antiangiogenic models also showed promising activity at a specified concentration. The present study revealed that the d1 showed significant tumor-inhibiting capabilities even in lesser concentrations in both in vitro as well as in vivo suggested that our d1 as a potent anticancer drug.

Author(s):

Abstract | PDF

Share this