A Reduction-responsive Amphiphilic Methotrexate-Podophyllotoxin Conjugate for Targeted Chemotherapy
© 2019 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim..
Owing to the naturally high toxicity, poor water solubility, and other side effects of podophyllotoxin (PPT), its applications are limited. To address these issues, we developed a new PPT delivery system, in which the hydrophilic drug methotrexate (MTX) and the hydrophobic drug PPT were linked by a reduction-responsive disulfide bond to form an amphiphilic drug-drug conjugate prodrug (MTX-SS-PPT). The conjugate could self-assemble into spherical nanoaggregates in aqueous solution and self-deliver to tumor tissues. In addition, MTX could target to folate-receptor-positive cells. Over-expression of glutathione in tumor cells broke the disulfide bonds and released the free drug. In vitro and in vivo experiments indicated that the nanodrug could effectively improve the biocompatibility and reduce the toxicity of PPT.
| Medienart: |
E-Artikel |
|---|
| Erscheinungsjahr: |
2019 |
|---|---|
| Erschienen: |
2019 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:14 |
|---|---|
| Enthalten in: |
Chemistry, an Asian journal - 14(2019), 21 vom: 04. Nov., Seite 3840-3844 |
| Sprache: |
Englisch |
|---|
| Beteiligte Personen: |
Hou, Meili [VerfasserIn] |
|---|
| Links: |
|---|
| Themen: |
Amphiphilic molecules |
|---|
| Anmerkungen: |
Date Completed 06.11.2019 Date Revised 08.01.2020 published: Print-Electronic Citation Status PubMed-not-MEDLINE |
|---|
| doi: |
10.1002/asia.201901070 |
|---|
| funding: |
|
|---|---|
| Förderinstitution / Projekttitel: |
|
| PPN (Katalog-ID): |
NLM301605092 |
|---|
| LEADER | 01000naa a22002652 4500 | ||
|---|---|---|---|
| 001 | NLM301605092 | ||
| 003 | DE-627 | ||
| 005 | 20231225104958.0 | ||
| 007 | cr uuu---uuuuu | ||
| 008 | 231225s2019 xx |||||o 00| ||eng c | ||
| 024 | 7 | |a 10.1002/asia.201901070 |2 doi | |
| 028 | 5 | 2 | |a pubmed24n1005.xml |
| 035 | |a (DE-627)NLM301605092 | ||
| 035 | |a (NLM)31552698 | ||
| 040 | |a DE-627 |b ger |c DE-627 |e rakwb | ||
| 041 | |a eng | ||
| 100 | 1 | |a Hou, Meili |e verfasserin |4 aut | |
| 245 | 1 | 2 | |a A Reduction-responsive Amphiphilic Methotrexate-Podophyllotoxin Conjugate for Targeted Chemotherapy |
| 264 | 1 | |c 2019 | |
| 336 | |a Text |b txt |2 rdacontent | ||
| 337 | |a ƒaComputermedien |b c |2 rdamedia | ||
| 338 | |a ƒa Online-Ressource |b cr |2 rdacarrier | ||
| 500 | |a Date Completed 06.11.2019 | ||
| 500 | |a Date Revised 08.01.2020 | ||
| 500 | |a published: Print-Electronic | ||
| 500 | |a Citation Status PubMed-not-MEDLINE | ||
| 520 | |a © 2019 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim. | ||
| 520 | |a Owing to the naturally high toxicity, poor water solubility, and other side effects of podophyllotoxin (PPT), its applications are limited. To address these issues, we developed a new PPT delivery system, in which the hydrophilic drug methotrexate (MTX) and the hydrophobic drug PPT were linked by a reduction-responsive disulfide bond to form an amphiphilic drug-drug conjugate prodrug (MTX-SS-PPT). The conjugate could self-assemble into spherical nanoaggregates in aqueous solution and self-deliver to tumor tissues. In addition, MTX could target to folate-receptor-positive cells. Over-expression of glutathione in tumor cells broke the disulfide bonds and released the free drug. In vitro and in vivo experiments indicated that the nanodrug could effectively improve the biocompatibility and reduce the toxicity of PPT | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a amphiphilic molecules | |
| 650 | 4 | |a chemotherapy | |
| 650 | 4 | |a podophyllotoxin | |
| 650 | 4 | |a reduction-responsive | |
| 650 | 4 | |a target | |
| 700 | 1 | |a Li, Shanshan |e verfasserin |4 aut | |
| 700 | 1 | |a Xu, Zhigang |e verfasserin |4 aut | |
| 700 | 1 | |a Li, Baosheng |e verfasserin |4 aut | |
| 773 | 0 | 8 | |i Enthalten in |t Chemistry, an Asian journal |d 2006 |g 14(2019), 21 vom: 04. Nov., Seite 3840-3844 |w (DE-627)NLM169728706 |x 1861-471X |7 nnns |
| 773 | 1 | 8 | |g volume:14 |g year:2019 |g number:21 |g day:04 |g month:11 |g pages:3840-3844 |
| 856 | 4 | 0 | |u http://dx.doi.org/10.1002/asia.201901070 |3 Volltext |
| 912 | |a GBV_USEFLAG_A | ||
| 912 | |a GBV_NLM | ||
| 951 | |a AR | ||
| 952 | |d 14 |j 2019 |e 21 |b 04 |c 11 |h 3840-3844 | ||