| Item type |
文献 / Documents(1) |
| 公開日 |
2021-12-02 |
| アクセス権 |
|
|
アクセス権 |
open access |
| 資源タイプ |
|
|
資源タイプ識別子 |
http://purl.org/coar/resource_type/c_6501 |
|
資源タイプ |
journal article |
| 出版社版DOI |
|
|
|
識別子タイプ |
DOI |
|
|
関連識別子 |
https://doi.org/10.3390/ph14010022 |
|
|
言語 |
ja |
|
|
関連名称 |
10.3390/ph14010022 |
| 出版タイプ |
|
|
出版タイプ |
VoR |
|
出版タイプResource |
http://purl.org/coar/version/c_970fb48d4fbd8a85 |
| タイトル |
|
|
タイトル |
Synthesis and In Vitro Assessment of pH-Sensitive Human Serum Albumin Conjugates of Pirarubicin |
|
言語 |
en |
| 著者 |
ツキガワ, ケンジ
イモト, シュウヘイ
ヤマサキ, ケイシ
ニシ, コウジ
ツツミ, トシヒコ
ヨコヤマ, ショウコ
異島, 優
オタギリ, マサキ
|
| 抄録 |
|
|
内容記述タイプ |
Abstract |
|
内容記述 |
In a previous study, we reported on the development of a synthetic polymer conjugate of pirarubicin (THP) that was formed via an acid-labile hydrazone bond between the polymer and the THP. However, the synthetic polymer itself was non-biodegradable, which could lead to unexpected adverse effects. Human serum albumin (HSA), which has a high biocompatibility and good biodegradability, is also a potent carrier for delivering antitumor drugs. The objective of this study was to develop pH-sensitive HSA conjugates of THP (HSA-THP), and investigate the release of THP and the cytotoxicity under acidic conditions in vitro for further clinical development. HSA-THP was synthesized by conjugating maleimide hydrazone derivatives of THP with poly-thiolated HSA using 2-iminothiolane, via a thiol-maleimide coupling reaction. We synthesized two types of HSA-THP that contained different amounts of THP (HSA-THP2 and HSA-THP4). Free THP was released from both of the HSA conjugates more rapidly at an acidic pH, and the rates of release for HSA-THP2 and HSA-THP4 were similar. Moreover, both HSA-THPs exhibited a higher cytotoxicity at acidic pH than at neutral pH, which is consistent with the effective liberation of free THP under acidic conditions. These findings suggest that these types of HSA-THPs are promising candidates for further development. |
|
言語 |
en |
| キーワード |
|
|
言語 |
en |
|
主題Scheme |
Other |
|
主題 |
pirarubicin (THP) |
| キーワード |
|
|
言語 |
en |
|
主題Scheme |
Other |
|
主題 |
human serum albumin (HSA) |
| キーワード |
|
|
言語 |
en |
|
主題Scheme |
Other |
|
主題 |
HSA-drug conjugates |
| キーワード |
|
|
言語 |
en |
|
主題Scheme |
Other |
|
主題 |
pH-sensitive |
| キーワード |
|
|
言語 |
en |
|
主題Scheme |
Other |
|
主題 |
drug release |
| キーワード |
|
|
言語 |
en |
|
主題Scheme |
Other |
|
主題 |
cytotoxicity |
| 書誌情報 |
en : Pharmaceuticals
巻 14,
号 1,
p. 22,
発行日 2020-12-30
|
| 収録物ID |
|
|
収録物識別子タイプ |
ISSN |
|
収録物識別子 |
14248247 |
| 出版者 |
|
|
出版者 |
MDPI |
|
言語 |
en |
| 権利情報 |
|
|
言語 |
en |
|
権利情報 |
This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). |
| EID |
|
|
識別子 |
374278 |
|
識別子タイプ |
URI |
| 言語 |
|
|
言語 |
eng |
ph_14_1_22.pdf (1.83 MB)
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