Enhanced efficacy of pluronic copolymer micelle encapsulated SCR7 against cancer cell proliferation.

Abstract:

:5,6-Bis(benzylideneamino)-2-mercaptopyrimidin-4-ol (SCR7) is a new anti cancer molecule having capability to selectively inhibit non-homologous end joining (NHEJ), one of the DNA double strand break (DSB) repair pathways inside the cells. In spite of the promising potential as an anticancer agent, hydrophobicity of SCR7 decreases its bioavailability. Herein the entrapment of SCR7 in Pluronic copolymer is reported. The size of the aggregates was determined by transmission electron microscopy (TEM) and dynamic light scattering (DLS) which yields an average diameter of 23 nm. SCR7 encapsulated micelles (ES) were also characterized by small-angle neutron scattering (SANS). Evaluation of its biological properties by using a variety of techniques, including Trypan blue, MTT and Live-dead cell assays, reveal that encapsulated SCR7 can induce cytotoxicity in cancer cell lines, being more effective in breast cancer cell line. Encapsulated SCR7 treatment resulted in accumulation of DNA breaks within the cells, resulting in cell cycle arrest at G1 phase and activation of apoptosis. More importantly, we found ≈ 5 fold increase in cell death, when encapsulated SCR7 was used in comparison with SCR7 alone.

journal_name

Macromol Biosci

authors

John F,George J,Vartak SV,Srivastava M,Hassan PA,Aswal VK,Karki SS,Raghavan SC

doi

10.1002/mabi.201400480

subject

Has Abstract

pub_date

2015-04-01 00:00:00

pages

521-34

issue

4

eissn

1616-5187

issn

1616-5195

journal_volume

15

pub_type

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