論文 - 詳細
RRC ID | 43652 |
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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) |