title: Patupilone-loaded poly(L-glutamic acid)-graft-methoxy-poly(ethylene glycol) micelle for oncotherapy.
abstract: Patupilone, an original natural anti-cancer agent, also known as epothilone B or Epo906, has shown promise for the treatment of a variety of cancers, however, the systematic side effects of patupilone significantly impaired its clinical translation. Herein, patupilone-loaded PLG-g-mPEG micelles were prepared. Patupilone was grafted to a poly(L-glutamic acid)-graft-methoxy-poly(ethylene glycol) (PLG-g-mPEG) by Steglich esterification reaction to give PLG-g-mPEG/Epo906 that could self-assemble to form patupilone-loaded micelles (Epo906-M). The Epo906-M was able to inhibit the proliferation of A549, MCF-7 cancer cells and BEAs-2B cells in vitro. For in vivo treatment of orthotopic xenograft tumor models (MCF-7), the Epo906-M exhibited higher tumor inhibition efficiency with lower side effects as compared with free Epo906. Seventeen percent of the body weight loss appeared in the group treated with free Epo906 of 0.25 mg kg-1, while the group treated with Epo906-M of 10 mg kg-1showed less than ten percent of body weight loss and displayed stronger tumor inhibiting effect. Therefore, the polypeptide-patupilone conjugate has improved potential for oncotherapy.
authors.affiliation: a Department of Chemistry , Xiangtan University , Xiangtan , PR China.|c Key Laboratory of Polymer Ecomaterials , Changchun Institute of Applied Chemistry, Chinese Academy of Sciences , Changchun , PR China.
authors.forename: Jing
authors.initials: J
authors.lastname: Yan
authors.affiliation: c Key Laboratory of Polymer Ecomaterials , Changchun Institute of Applied Chemistry, Chinese Academy of Sciences , Changchun , PR China.
authors.forename: Dawei
authors.initials: D
authors.lastname: Zhang
authors.affiliation: c Key Laboratory of Polymer Ecomaterials , Changchun Institute of Applied Chemistry, Chinese Academy of Sciences , Changchun , PR China.
authors.forename: Haiyang
authors.initials: H
authors.lastname: Yu
authors.affiliation: c Key Laboratory of Polymer Ecomaterials , Changchun Institute of Applied Chemistry, Chinese Academy of Sciences , Changchun , PR China.
authors.forename: Lili
authors.initials: L
authors.lastname: Ma
authors.affiliation: d College of Chemistry, Northeast Normal University , Changchun , PR China.
authors.forename: Mingxiao
authors.initials: M
authors.lastname: Deng
authors.affiliation: c Key Laboratory of Polymer Ecomaterials , Changchun Institute of Applied Chemistry, Chinese Academy of Sciences , Changchun , PR China.
authors.forename: Zhaohui
authors.initials: Z
authors.lastname: Tang
authors.affiliation: a Department of Chemistry , Xiangtan University , Xiangtan , PR China.|b Key Laboratory of Environmentally Friendly Chemistry and Applications of Ministry of Education, Key Laboratory of Polymeric Materials and Application Technology of Hunan Province , Xiangtan University , Xiangtan , PR China.
authors.forename: Xuefei
authors.initials: X
authors.lastname: Zhang
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology; D001692:Biological Transport; D045744:Cell Line, Tumor; D004337:Drug Carriers / Q000737:chemistry*; D034261:Epothilones / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology; D006801:Humans; D008823:Micelles; D011092:Polyethylene Glycols / Q000737:chemistry*; D011099:Polyglutamic Acid / Q000031:analogs & derivatives* / Q000737:chemistry
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers; D034261:Epothilones; D008823:Micelles; C579712:methoxypoly(ethylene glycol)-block-poly(glutamic acid); D011099:Polyglutamic Acid; D011092:Polyethylene Glycols; C093788:epothilone B
keywords: Patupilone; glutamic acid; micelles; oncotherapy; polypeptide