title: A core cross-linked polymeric micellar platium(IV) prodrug with enhanced anticancer efficiency.
abstract: A core cross-linked polymeric micellar cisplatin(IV) conjugate prodrug is prepared by attaching the cisplatin(IV) to mPEG-b-PLL biodegradable copolymers to form micellar nanoparticles that can disintegrate to release the active anticancer agent cisplatin(II) in a mild reducing environment. Moreover, in vitro studies show that this cisplatin(IV) conjugate prodrug displays enhanced cytotoxicity against HepG2 cancer cells compared with cisplatin(II). Further studies demonstrate that the high cellular uptake and platinum-DNA adduct of this cisplatin(IV) conjugate prodrug can induce more cancer-cell apoptosis than cisplatin(II), which is responsible for its enhanced anticancer activity.
authors.affiliation: China-Japan Union Hospital of Jilin University, Changchun, P R China.
authors.forename: Jie
authors.initials: J
authors.lastname: Hou
authors.forename: Jincai
authors.initials: J
authors.lastname: Shang
authors.forename: Chengbin
authors.initials: C
authors.lastname: Jiao
authors.forename: Peiyue
authors.initials: P
authors.lastname: Jiang
authors.forename: Huijie
authors.initials: H
authors.lastname: Xiao
authors.forename: Lan
authors.initials: L
authors.lastname: Luo
authors.forename: Tongjun
authors.initials: T
authors.lastname: Liu
mesh_terms: D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000737:chemistry; D063566:Biodegradable Plastics / Q000737:chemistry / Q000494:pharmacology; D002945:Cisplatin / Q000008:administration & dosage* / Q000737:chemistry; D018736:DNA Adducts / Q000008:administration & dosage / Q000737:chemistry; D056945:Hep G2 Cells; D006801:Humans; D008823:Micelles; D053758:Nanoparticles / Q000008:administration & dosage* / Q000737:chemistry; D011092:Polyethylene Glycols / Q000737:chemistry; D011107:Polylysine / Q000031:analogs & derivatives / Q000737:chemistry; D011108:Polymers / Q000008:administration & dosage* / Q000737:chemistry; D011355:Prodrugs / Q000008:administration & dosage* / Q000737:chemistry
chemical_list: D000970:Antineoplastic Agents; D063566:Biodegradable Plastics; D018736:DNA Adducts; D008823:Micelles; D011108:Polymers; D011355:Prodrugs; C117924:mPEG-block-PLL; D011107:Polylysine; D011092:Polyethylene Glycols; D002945:Cisplatin
keywords: anticancer efficiency; core cross-linked materials; micellar nanoparticles; platinum(IV) conjugated; prodrugs