Combined Graphene Oxide with 2-Methoxyestradiol for Effective Anticancer Therapy In-vitro Model

Introduction: This article describes the invention of graphene oxide (GO) or reduced graphene oxide (rGO) functionalised with 2-methoxy estradiol. The presence of polar hydroxyl groups enables the binding of 2-ME to GO/rGO through hydrogen bonds with epoxy and hydroxyl groups located on the surface and carbonyl and carboxyl groups located at the edges of graphene flake sheets.

Methods: The patented method of producing the subject of the invention and the research results regarding its anticancer effectiveness via cytotoxicity in an in vivo model (against A375 melanoma and 143B osteosarcoma cells) are described.

Results: It was shown that the inhibition of PTP1B phosphotyrosine phosphatase is one of the mechanisms of action of GO functionalised with 2-ME (GO-2-ME). This is a very important result, considering the fact that 2-ME itself has no inhibitory properties against this phosphatase.

Discussion: Graphene oxide flakes embroidered with 2-methoxyestradiol molecules may be a promising solution, bringing a new and important effect in the form of improving the bioavailability of the therapeutic substance, ie 2-ME. An appropriate dosage of GO-2-ME/rGO-2-ME, in which GO/rGO is a carrier of 2-methoxyestradiol (2-ME), can ensure effective penetration of the active substance through biological boundaries/membranes and controlled modification of cell signalling, ultimately leading to the selective elimination of malignant cells.