title: 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.
authors.affiliation: Biotechnology Laboratory, Department of Chemistry, Sacred Heart College, Kochi, 682 013, India.
authors.forename: Franklin
authors.initials: F
authors.lastname: John
authors.forename: Jinu
authors.initials: J
authors.lastname: George
authors.forename: Supriya V
authors.initials: SV
authors.lastname: Vartak
authors.forename: Mrinal
authors.initials: M
authors.lastname: Srivastava
authors.forename: P A
authors.initials: PA
authors.lastname: Hassan
authors.forename: V K
authors.initials: VK
authors.lastname: Aswal
authors.forename: Subhas S
authors.initials: SS
authors.lastname: Karki
authors.forename: Sathees C
authors.initials: SC
authors.lastname: Raghavan
mesh_terms: D017209:Apoptosis / Q000187:drug effects; D049109:Cell Proliferation / Q000187:drug effects; D053903:DNA Breaks, Double-Stranded / Q000187:drug effects; D059766:DNA End-Joining Repair / Q000187:drug effects*; D004357:Drug Synergism; D006801:Humans; D061986:MCF-7 Cells; D009369:Neoplasms / Q000188:drug therapy*; D011060:Poloxalene / Q000008:administration & dosage* / Q000737:chemistry; D011743:Pyrimidines / Q000008:administration & dosage* / Q000737:chemistry; D012545:Schiff Bases / Q000008:administration & dosage* / Q000737:chemistry
chemical_list: C578537:5,6-bis(benzylideneamino)-2-mercaptopyrimidin-4-ol; D011743:Pyrimidines; D012545:Schiff Bases; C464484:pluronic block copolymer P123; D011060:Poloxalene
keywords: SCR7; pluronic block copolymer; polymeric micelles