Ginkgetin: A Promising Multitarget Agent for Diverse Diseases

Area of Science:

• Natural Product Chemistry
• Pharmacology
• Medicinal Chemistry

Background:

• Ginkgetin (GK) is a biflavonoid isolated from Ginkgo biloba, structurally distinct due to its 3'-8″-linked biflavone subclass.
• Its unique dimeric architecture enhances membrane permeability and allows for multitarget engagement.

Purpose of the Study:

• To systematically review the chemical characteristics, pharmacological activities, and molecular mechanisms of Ginkgetin (GK).
• To emphasize GK's multitarget actions and therapeutic potential across various disease systems.
• To discuss limitations and future perspectives for GK's clinical translation.

Main Methods:

• Literature review of preclinical studies on Ginkgetin (GK).
• Analysis of GK's chemical structure, pharmacological effects, and molecular targets.
• Synthesis of information on therapeutic potential and challenges in clinical translation.

Main Results:

• GK exhibits pleiotropic effects including anti-inflammatory, antioxidant, anticancer, neuroprotective, and cardioprotective activities.
• Mechanistically, GK modulates key signaling pathways like Nrf2/HO-1, NF-κB, JAK/STAT, MAPKs, AMPK/mTOR, PI3K/Akt, and cGAS-STING.
• GK shows therapeutic potential in cancer, metabolic, cardiovascular, neurological, and musculoskeletal diseases, with emerging antibacterial properties.

Conclusions:

• Ginkgetin (GK) possesses significant multitarget therapeutic potential demonstrated in preclinical studies.
• Challenges in pharmacokinetics, bioavailability, and druggability currently limit its clinical translation.
• Further research and rational development are needed to facilitate GK-based interventions in human medicine.