title: Dihydroartemisinin and transferrin dual-dressed nano-graphene oxide for a pH-triggered chemotherapy.
abstract: Dihydroartemisinin (DHA) is a unique anti-malarial drug isolated from the plant Artemisia annua. Recently, it has been studied as an alternative modality for cancer therapy, utilizing its reactive oxygen species (ROS) yielding mechanism from interacting with Ferrous ion (Fe (II)). In this work, a novel nanodrug (DHA-GO-Tf) is constructed based on nanoscale Graphene oxide (GO) dual-dressed with DHA and Transferrin (Tf). Tf dually functions as a pilot for the nanoparticle to target tumor cell with over expressed Transferrin receptor (TfR) and a ferric ion carrier. Upon tumor cellular endocytosis, Ferric ion (Fe(III)) is released from the Tf, triggered by the low pH in the lysosomes of the tumor cell. The intracellular Fe (III) is reduced to Fe (II) and interacts with DHA to increase its cytotoxicity. The potential of this alternative anti-tumor modality is demonstrated both in vitro and in vivo. Comparing with DHA alone, the nanodrug DHA-GO-Tf resulted in a significantly enhanced tumor delivery specificity and cytotoxicity, and achieved a complete tumor cure in mice with minimal side-effects.
authors.affiliation: MOE Key Laboratory of Laser Life Science & Institute of Laser Life Science, College of Biophotonics, South China Normal University, Guangzhou, 510631, PR China.
authors.forename: Lijuan
authors.initials: L
authors.lastname: Liu
authors.affiliation: MOE Key Laboratory of Laser Life Science & Institute of Laser Life Science, College of Biophotonics, South China Normal University, Guangzhou, 510631, PR China. Electronic address: weiyanchun@scnu.edu.cn.
authors.forename: Yanchun
authors.initials: Y
authors.lastname: Wei
authors.affiliation: MOE Key Laboratory of Laser Life Science & Institute of Laser Life Science, College of Biophotonics, South China Normal University, Guangzhou, 510631, PR China.
authors.forename: Shaodong
authors.initials: S
authors.lastname: Zhai
authors.affiliation: MOE Key Laboratory of Laser Life Science & Institute of Laser Life Science, College of Biophotonics, South China Normal University, Guangzhou, 510631, PR China.
authors.forename: Qun
authors.initials: Q
authors.lastname: Chen
authors.affiliation: MOE Key Laboratory of Laser Life Science & Institute of Laser Life Science, College of Biophotonics, South China Normal University, Guangzhou, 510631, PR China; Joint Laboratory of Laser Oncology with Cancer Center of Sun Yat-sen University, South China Normal University, Guangzhou, 510631, PR China. Electronic address: xingda@scnu.edu.cn.
authors.forename: Da
authors.initials: D
authors.lastname: Xing
mesh_terms: D000818:Animals; D000971:Antineoplastic Combined Chemotherapy Protocols / Q000008:administration & dosage* / Q000737:chemistry; D037621:Artemisinins / Q000008:administration & dosage*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D003692:Delayed-Action Preparations / Q000008:administration & dosage / Q000737:chemistry*; D004058:Diffusion; D005260:Female; D006108:Graphite / Q000737:chemistry*; D006863:Hydrogen-Ion Concentration; D051379:Mice; D008807:Mice, Inbred BALB C; D053769:Nanocapsules / Q000008:administration & dosage* / Q000737:chemistry / Q000648:ultrastructure; D009374:Neoplasms, Experimental / Q000737:chemistry / Q000188:drug therapy* / Q000473:pathology; D010087:Oxides / Q000737:chemistry; D010316:Particle Size; D014168:Transferrin / Q000008:administration & dosage / Q000737:chemistry; D016896:Treatment Outcome
chemical_list: D037621:Artemisinins; D003692:Delayed-Action Preparations; D053769:Nanocapsules; D010087:Oxides; D014168:Transferrin; C039060:artenimol; D006108:Graphite
keywords: Chemotherapy; Dihydroartemisinin; Graphene oxide; Reactive oxygen species; Transferrin