PUBLICATION
Characterization, bioactivity and pharmacokinetic study of a novel carbohydrate-peptide polymer: Glycol-split heparin-endostatin2 (GSHP-ES2)
- Authors
- Sun, F., Wang, Z., Yang, Z., Li, Y., Cui, H., Liu, C., Gao, D., Wang, F., Tan, H.
- ID
- ZDB-PUB-190103-1
- Date
- 2019
- Source
- Carbohydrate Polymers 207: 79-90 (Journal)
- Registered Authors
- Keywords
- Anti-angiogenesis, ES2, Glycol-split heparin, Stability, Zebra fish
- MeSH Terms
-
- Angiogenesis Inhibitors/chemical synthesis
- Angiogenesis Inhibitors/pharmacokinetics
- Angiogenesis Inhibitors/pharmacology*
- Angiogenesis Inhibitors/toxicity
- Animals
- Cell Line
- Cell Movement/drug effects
- Chickens
- Drug Stability
- Endostatins/chemical synthesis
- Endostatins/pharmacokinetics
- Endostatins/pharmacology*
- Endostatins/toxicity
- Female
- Glycopeptides/chemical synthesis
- Glycopeptides/pharmacokinetics
- Glycopeptides/pharmacology*
- Glycopeptides/toxicity
- Half-Life
- Heparin/chemistry*
- Humans
- Mice, Inbred BALB C
- Oligopeptides/chemical synthesis
- Oligopeptides/pharmacokinetics
- Oligopeptides/pharmacology*
- Oligopeptides/toxicity
- Zebrafish
- PubMed
- 30600066 Full text @ Carbohydr. Polym.
Citation
Sun, F., Wang, Z., Yang, Z., Li, Y., Cui, H., Liu, C., Gao, D., Wang, F., Tan, H. (2019) Characterization, bioactivity and pharmacokinetic study of a novel carbohydrate-peptide polymer: Glycol-split heparin-endostatin2 (GSHP-ES2). Carbohydrate Polymers. 207:79-90.
Abstract
Endostatin (ES) has attracted considerable attention for the treatment of anti-angiogenesis-related disorders. An 11-amino-acid peptide (ES2, IVRRADRAAVP) from the amino terminal of ES is of interest because it is the main active fragment of ES. However, both ES and ES2 have a poor stability and a short half-life, and other disadvantages need to be further resolved. Thus, we conjugated ES2 to glycol-split heparin derivatives (GSHPs) to yield the polymer-peptide conjugate, GSHP-ES2. This study showed that GSHP-ES2 exhibited increased stability, a wider pH activity range, better inhibition of endothelial cell proliferation, migration and tube formation in vitro, better anti-angiogenic activity and a longer half-life in vivo compared with ES2. These results also indicate that GSHP-ES2 has good potential for the treatment of angiogenesis-related diseases, either alone or in combination with other chemicals.
Genes / Markers
Expression
Phenotype
Mutations / Transgenics
Human Disease / Model
Sequence Targeting Reagents
Fish
Orthology
Engineered Foreign Genes
Mapping