An iGlu Receptor Antagonist and Its Simultaneous Use with an Anticancer Drug for Cancer Therapy

Autor:	Kim Truc Nguyen, Chung Yen Ang, Pei-Zhou Li, Zhong Luo, Si Yu Tan, Yanli Zhao
Přispěvatelé:	School of Materials Science & Engineering, School of Physical and Mathematical Sciences
Rok vydání:	2015
Předmět:	medicine.drug_class Antineoplastic Agents Pharmacology Receptors Ionotropic Glutamate Catalysis Mice chemistry.chemical_compound Science::Biological sciences::Human anatomy and physiology [DRNTU] Drug Delivery Systems Cell Line Tumor medicine Animals Humans Doxorubicin Receptor Melanoma Chemistry Organic Chemistry Glutamate receptor Cancer Drug Synergism General Chemistry Glutathione Silicon Dioxide Receptor antagonist medicine.disease Drug Combinations Neuroprotective Agents Drug delivery NIH 3T3 Cells Nanoparticles Spermine Ionotropic effect medicine.drug
Zdroj:	Chemistry - A European Journal. 21:6123-6131
ISSN:	0947-6539
DOI:	10.1002/chem.201406527
Popis:	Glutamate receptor antagonists have been known to play a crucial role in the treatment of many neuronal diseases. Recently, these antagonists have also shown therapeutic effects in the treatment of cancer. In this study, an ionotropic glutamate (iGlu) receptor antagonist, 4-hydroxyphenylacetyl spermine (L1), was used concurrently with a common anticancer drug, doxorubicin (Dox), for simultaneous cancer therapy. Mesoporous silica nanoparticles (MSNPs) were employed as the delivery vehicle for both L1 and Dox by conjugating the iGlu receptor antagonist on the surface and encapsulating Dox within the mesopores. Dox was then trapped within the mesopores by functionalizing a redox-cleavable capping group on the MSNP surface, and it could be released upon exposure to the reductive glutathione. In vitro studies on B16F10 and NIH3T3 cell lines revealed that the iGlu receptor antagonist L1 exhibited therapeutic as well as targeting effects. In addition, the simultaneous use of therapeutic L1 and Dox proved to be synergistic in the treatment of cancer. The present work demonstrated the feasibility of employing a delivery system to deliver both neuroprotective drug and anticancer drug for efficient anticancer treatment.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4c1f00e8a3aa798b15c9274945529cc9 https://doi.org/10.1002/chem.201406527 Zobrazit plný text záznamu Plný text ve formátu PDF Plný text ve formátu HTML
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