RRC ID 43652
著者 Nakase I, Konishi Y, Ueda M, Saji H, Futaki S.
タイトル Accumulation of arginine-rich cell-penetrating peptides in tumors and the potential for anticancer drug delivery in vivo.
ジャーナル J Control Release
Abstract We investigated the biodistribution of arginine-rich cell-penetrating peptides (CPPs) in tumor-xenografted nude mice after intravenous injection of fluorescently labeled CPPs using in vivo imaging. The CPPs used included HIV-1 Tat (48-60), penetratin, and the L- and D-enantiomers of oligoarginines (8, 12, and 16 residues), all of which are reported to have high cell penetration. Among the tested peptides, high accumulation in tumors was observed for the D-form of octaarginine (r8), and glycosaminoglycans played a key role. Injection of an r8-doxorubicin conjugate (4mg doxorubicin/kg) effectively suppressed tumor proliferation, with no significant decrease in mouse weight, whereas administration of doxorubicin itself (6mg/kg), yielding a similar degree of tumor-growth suppression, resulted in significant weight loss. These results suggest the potential of r8 as a prototypic tumor-targeting vector.
巻・号 159(2)
ページ 181-8
公開日 2012-4-30
DOI 10.1016/j.jconrel.2012.01.016
PII S0168-3659(12)00021-1
PMID 22285548
MeSH Animals Antineoplastic Agents / administration & dosage* Antineoplastic Agents / pharmacokinetics Antineoplastic Agents / therapeutic use CHO Cells Carrier Proteins / chemistry Cell Proliferation / drug effects Cell Survival / drug effects Cell-Penetrating Peptides / chemistry Cell-Penetrating Peptides / pharmacokinetics* Cricetinae Doxorubicin / administration & dosage* Doxorubicin / pharmacokinetics Doxorubicin / therapeutic use Drug Carriers / chemistry Drug Carriers / pharmacokinetics* Female HeLa Cells Humans Mice Mice, Inbred BALB C Mice, Nude Microscopy, Confocal Oligopeptides / chemistry* Peptide Fragments / chemistry Stereoisomerism Time Factors Tissue Distribution Xenograft Model Antitumor Assays tat Gene Products, Human Immunodeficiency Virus / chemistry
IF 7.727
引用数 93
WOS 分野 PHARMACOLOGY & PHARMACY CHEMISTRY, MULTIDISCIPLINARY
リソース情報
ヒト・動物細胞 HeLa(RCB0007)