Advantages

- Exhibits selective cytoprotective activity against ferroptosis without affecting apoptosis
- Silicon substitution in the polycyclic quinone structure confers stronger ferroptosis-inhibitory activity than the non-silicon analog and existing inhibitors

Technology Overview & Background

Ferroptosis is a form of programmed cell death distinct from apoptosis and is characterized by iron-dependent lipid peroxidation. In recent years, ferroptosis has attracted growing attention as a therapeutic target because it has been implicated in a wide range of pathological conditions, including neurodegenerative diseases, ischemia-reperfusion injury, and acute kidney injury.
Many currently known ferroptosis inhibitors fall into the categories of antioxidants or free radical scavengers, leaving room for improvement in potency, selectivity, and translational potential. In this study, a series of compounds capable of effectively suppressing ferroptosis was identified from the University of Osaka’s original chemical library, and silicon-containing polycyclic quinone compounds showed particularly strong inhibitory activity in vitro. These compounds represent a novel scaffold distinct from conventional free radical scavenger-type inhibitors and are expected to provide a promising basis for further lead optimization and therapeutic development.

Data

- In an ML162-induced ferroptosis model in HK-2 cells, the compounds showed stronger cytoprotective activity than edaravone.
- Consistent protective effects were observed against ferroptosis induced by agents with different mechanisms of action.
- No protective effect was observed under apoptosis-inducing conditions, supporting selective activity against ferroptosis.

Expectations

The University of Osaka is seeking pharmaceutical or biotech partners for collaboration and licensing opportunities related to the development of therapeutics based on this technology.
- Lead optimization and preclinical development using these silicon analogs and related compounds as starting points.
- Collaborative research to expand the silicon-containing polycyclic compound framework to other drug targets.
Upon expression of interest, an online meeting and technical briefing can be arranged to introduce the detailed data package and discuss fit with your company’s R&D needs.

Principal Investigator

Mitsuhiro ARISAWA, Professor（Graduate School of Pharmaceutical Sciences, The University of Osaka）
Takujiro HOMMA, Junior Associate Professor（Graduate School of Medicine, Osaka Metropolitan University）

Patents and Publications

Patent application filed (unpublished)
The publication information related to this project is provided in the downloadable materials.