Optimized 2-methoxyestradiol invasomes fortified with apamin: a promising approach for suppression of A549 lung cancer cells
Zuhier Awan, Shareefa A. AlGhamdi, Nabil A. Alhakamy, Solomon Z. Okbazghi, Mohamed A. Alfaleh, Shaimaa M. Badr-Eldin, Hibah M. Aldawsari, Mohammed A. S. Abourehab, Hani Z. Asfour, Shadi A. Zakai, Mohammad W. Alrabia, Aya A. Negm, Mohamed A. El‐Moselhy, Sara S. Sharkawi, Waleed Y. Rizg
Abstract
5.6 ± 0.2 µg/mL). Post 2ME-INVA-APA administration, a significant rise in cell death and necrosis was seen among the A549 cells compared to those treated with plain formula or 2ME alone. This effect was indicated by increased Bax expression and reduced Bcl-2 expression, as well as mitochondrial membrane potential loss. Moreover, the cell cycle analysis showed that 2ME-INVA-APA arrests the G2-M phase of the A549 cells. Additionally, it was observed that the micellar formulation of the drug increased the cell count in pre-G1, thereby exhibiting phenomenal apoptotic potential. Furthermore, it up-regulates caspase-9 and p53 and downregulates TNF-α and NF-κβ. Collectively, these findings showed that our optimized 2ME-INVA-APA could easily seep through the cell membrane and induce apoptosis in relatively low doses.