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Helix Self-Assembly Behavior of Amino Acid-Modified Camptothecin Prodrugs and Its Antitumor Effect
Guo,Zhaopei1,2; Lin,Lin1; Hao,Kai1; Wang,Dianwei1; Liu,Feng1; Sun,Pingjie1; Yu,Haiyang1; Tang,Zhaohui1; Chen,Meiwan2; Tian,Huayu1,3; Chen,Xuesi1,3
Source PublicationACS Applied Materials and Interfaces

For effective antitumor treatment, it is important to increase the water solubility of hydrophobic antitumor drugs and improve their cell absorption efficiency and nuclear transmission capacity. Here, we use endogenous hydrophilic arginine to modify camptothecin (CPT) to increase its water solubility. Surprisingly, the modified CPT can self-assemble into helical nanofibers through intermolecular π-πstacking and hydrophilic-hydrophobic interactions. Prodrug-based nanofibers were better endocytosed into the nucleus than their nonassembled CPT. Moreover, in vivo, such nanofibers had a longer blood circulation time and a better ability to accumulate in the tumor site. Further, we found that the cationic nanofibers can be combined with the anionic cisplatin-polyglutamic acid through electrostatic interaction to achieve a combined antitumor effect. This provides a new idea for achieving more effective cancer chemotherapy effects.

KeywordAntitumor Camptothecin Prodrug Self-aggregate Π-πstack
URLView the original
Indexed BySCIE
WOS Research AreaScience & Technology - Other Topics ; Materials Science
WOS SubjectNanoscience & Nanotechnology ; Materials Science, Multidisciplinary
WOS IDWOS:000514256400069
Scopus ID2-s2.0-85079358568
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Cited Times [WOS]:12   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionUniversity of Macau
Corresponding AuthorChen,Meiwan; Tian,Huayu
Affiliation1.Key Laboratory of Polymer Ecomaterials,Changchun Institute of Applied Chemistry,Chinese Academy of Sciences,Changchun,130022,China
2.State Key Laboratory of Quality Research in Chinese Medicine,Institute of Chinese Medical Sciences,University of Macau,Taipa,999078,Macao
3.Jilin Biomedical Polymers Engineering Laboratory,Changchun,130022,China
First Author AffilicationInstitute of Chinese Medical Sciences
Corresponding Author AffilicationInstitute of Chinese Medical Sciences
Recommended Citation
GB/T 7714
Guo,Zhaopei,Lin,Lin,Hao,Kai,et al. Helix Self-Assembly Behavior of Amino Acid-Modified Camptothecin Prodrugs and Its Antitumor Effect[J]. ACS Applied Materials and Interfaces,2020,12(6):7466-7476.
APA Guo,Zhaopei,Lin,Lin,Hao,Kai,Wang,Dianwei,Liu,Feng,Sun,Pingjie,Yu,Haiyang,Tang,Zhaohui,Chen,Meiwan,Tian,Huayu,&Chen,Xuesi.(2020).Helix Self-Assembly Behavior of Amino Acid-Modified Camptothecin Prodrugs and Its Antitumor Effect.ACS Applied Materials and Interfaces,12(6),7466-7476.
MLA Guo,Zhaopei,et al."Helix Self-Assembly Behavior of Amino Acid-Modified Camptothecin Prodrugs and Its Antitumor Effect".ACS Applied Materials and Interfaces 12.6(2020):7466-7476.
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