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Mitochondrial delivery of mastoparan with transferrin liposomes equipped with a pH-sensitive fusogenic peptide for selective cancer therapy.

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Title: Mitochondrial delivery of mastoparan with transferrin liposomes equipped with a pH-sensitive fusogenic peptide for selective cancer therapy.
Authors: Yamada, Yuma Browse this author
Shinohara, Yasuo Browse this author
Kakudo, Tomoyuki Browse this author
Chaki, Shinji Browse this author
Futaki, Shiroh Browse this author
Kamiya, Hiroyuki Browse this author
Harashima, Hideyoshi Browse this author
Keywords: mastoparan
transferrrin liposomes
GALA
mitochondrial delivery
anticancer therapy
apoptosis
Issue Date: 13-Oct-2005
Publisher: Elsevier
Journal Title: International journal of pharmaceutics
Volume: 303
Issue: 1-2
Start Page: 1
End Page: 7
Publisher DOI: 10.1016/j.ijpharm.2005.06.009
PMID: 16139452
Abstract: Mastoparan (MP), a potent facilitator of mitochondrial permeability transition (PT), could be used as an antitumor agent, if it were encapsulated in a tumor selective delivery system. We recently developed transferrin-modified liposomes (Tf-L) with a pH-sensitive fusogenic peptide (GALA), which delivers an encapsulated fluorescent marker into cytosol efficiently. In this study, we encapsulated MP into Tf-L with GALA for the selective delivery to mitochondria of tumor cells. The MP showed potent PT activity at concentrations above 25 microM in a homogenate of K 562 cells as well as in isolated mitochondria in the presence of phosphate. Tf-L equipped with cholesteryl GALA can release encapsulated sulforhodamine B, while Tf-L failed, as evidenced by confocal laser scanning microscopy. The MP, which was delivered with Tf-L with GALA, released cytochrome c (cyt c) from mitochondria to the cytosol, while free MP released cyt c not only to the cytosol but also extracellulary. These results demonstrate the utility of MP in Tf-L with GALA for cancer therapy.
Type: article (author version)
URI: http://hdl.handle.net/2115/48155
Appears in Collections:薬学研究院 (Faculty of Pharmaceutical Sciences) > 雑誌発表論文等 (Peer-reviewed Journal Articles, etc)

Submitter: 山田 勇磨

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