PMID- 30107337 OWN - NLM STAT- MEDLINE DCOM- 20190107 LR - 20190107 IS - 1873-4367 (Electronic) IS - 0927-7765 (Linking) VI - 171 DP - 2018 Nov 1 TI - Angiopep-2 modified PEGylated 2-methoxyestradiol micelles to treat the PC12 cells with oxygen-glucose deprivation/reoxygenation. PG - 638-646 LID - S0927-7765(18)30533-2 [pii] LID - 10.1016/j.colsurfb.2018.08.009 [doi] AB - 2-Methoxyestradiol (2ME2), as a microtubule and hypoxia-inducible factor-1 (HIF-1) inhibitor, can be used to treat cerebral ischemia-reperfusion (I/R) injury. However, its poor water solubility compromises its efficacy as a neuroprotectant. Herein, we synthesized PEGylated 2ME2 and angiopep-2 capped PEGylated 2ME2 and fabricated angiopep-2 modified PEGylated 2ME2 micelles containing free 2ME2 (ANG-PEG-2ME2/2ME2) via emulsion-solvent evaporation method. The effect of the micelles on ischemia-reoxygenation injury was evaluated by oxygen-glucose deprivation/reoxygenation (OGD/R) models with different degrees of PC12 cell damage. In comparison with free 2ME2, the micelles significantly increased the cell viability, inhibited reactive oxygen species (ROS) generation and apoptosis for PC12 cells with 0.5 and 4 h OGD followed by 24 h reoxygenation. Taken together, the angiopep-2 modified 2ME2-loaded micelles could effectively reduce the injury of PC12 cells induced by OGD/R. CI - Copyright (c) 2018 Elsevier B.V. All rights reserved. FAU - Hu, Lijun AU - Hu L AD - School of Pharmacy, Shanghai Jiao Tong University, 800 Dongchuan Road, Shanghai 200240, China. FAU - Wang, Yun AU - Wang Y AD - School of Pharmacy, Shanghai Jiao Tong University, 800 Dongchuan Road, Shanghai 200240, China. FAU - Zhang, Yihui AU - Zhang Y AD - School of Pharmacy, Shanghai Jiao Tong University, 800 Dongchuan Road, Shanghai 200240, China. FAU - Yang, Ning AU - Yang N AD - School of Pharmacy, Shanghai Jiao Tong University, 800 Dongchuan Road, Shanghai 200240, China. FAU - Han, Huijie AU - Han H AD - School of Pharmacy, Shanghai Jiao Tong University, 800 Dongchuan Road, Shanghai 200240, China. FAU - Shen, Yuanyuan AU - Shen Y AD - School of Pharmacy, Shanghai Jiao Tong University, 800 Dongchuan Road, Shanghai 200240, China. Electronic address: shenyuanyuan@sjtu.edu.cn. FAU - Cui, Derong AU - Cui D AD - Department of Anesthesiology, Shanghai Sixth People's Hospital Affiliated to Shanghai Jiao Tong University, Shanghai 200233, China. Electronic address: cuishuning118@163.com. FAU - Guo, Shengrong AU - Guo S AD - School of Pharmacy, Shanghai Jiao Tong University, 800 Dongchuan Road, Shanghai 200240, China. Electronic address: srguo@sjtu.edu.cn. LA - eng PT - Journal Article DEP - 20180808 PL - Netherlands TA - Colloids Surf B Biointerfaces JT - Colloids and surfaces. B, Biointerfaces JID - 9315133 RN - 0 (Angiopep-2) RN - 0 (Micelles) RN - 0 (Peptides) RN - 0 (Reactive Oxygen Species) RN - 3WJQ0SDW1A (Polyethylene Glycols) RN - 6I2QW73SR5 (2-Methoxyestradiol) RN - IY9XDZ35W2 (Glucose) RN - S88TT14065 (Oxygen) SB - IM MH - 2-Methoxyestradiol/chemical synthesis/chemistry/*pharmacology MH - Animals MH - Apoptosis/drug effects MH - Cell Survival/drug effects MH - Glucose/*chemistry/metabolism MH - Micelles MH - Oxidation-Reduction MH - Oxygen/*chemistry/metabolism MH - PC12 Cells MH - Particle Size MH - Peptides/*chemistry MH - Polyethylene Glycols/*chemistry MH - Rats MH - Reactive Oxygen Species/antagonists & inhibitors/metabolism MH - Surface Properties OTO - NOTNLM OT - OGD/R OT - PC12 cells OT - PEGylated 2-methoxyestradiol micelles EDAT- 2018/08/15 06:00 MHDA- 2019/01/08 06:00 CRDT- 2018/08/15 06:00 PHST- 2018/05/16 00:00 [received] PHST- 2018/08/04 00:00 [revised] PHST- 2018/08/07 00:00 [accepted] PHST- 2018/08/15 06:00 [pubmed] PHST- 2019/01/08 06:00 [medline] PHST- 2018/08/15 06:00 [entrez] AID - S0927-7765(18)30533-2 [pii] AID - 10.1016/j.colsurfb.2018.08.009 [doi] PST - ppublish SO - Colloids Surf B Biointerfaces. 2018 Nov 1;171:638-646. doi: 10.1016/j.colsurfb.2018.08.009. Epub 2018 Aug 8.