Drug intelligence / Profile preview

platanosides

Development stage
Preclinical
Lead developer
Medical University of South Carolina
Modality
Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Intraperitoneal, Oral
01

Overview

Platanosides are a class of plant-derived kaempferol glycosides acylated with p-coumaroyl groups, isolated from the leaves of the American sycamore tree (*Platanus occidentalis*). Developed as a botanical drug candidate, platanosides exist as an equimolar mixture of four geometrical isomers (platanosides 1–4). They exhibit dual therapeutic potential as broad-spectrum antibiotics against multidrug-resistant Gram-positive pathogens (such as methicillin-resistant *Staphylococcus aureus* [MRSA] and *Streptococcus* species) and as hepatoprotective agents. Mechanistically, platanosides act as inhibitors of the Keap1-Nrf2 protein-protein interaction, promoting Nrf2 activation and subsequent mitochondrial biogenesis via PGC1α upregulation. They also inhibit JNK1/2 activation, thereby reducing oxidative stress, inflammation, and cell death. Additionally, they target bacterial enzymes such as FabI (enoyl-ACP reductase) and penicillin-binding proteins (PBP1/2) to exert their antibacterial effects.

Other names
PTSPTSsplatanosideplatanosides 1-4platanosides1-4platanosides-1-4
02

Targets

InhAKEAP1 (Kelch-like ECH-associated protein 1)JNK (Mitogen-activated protein kinase kinase kinase family)PBP1A (Penicillin-binding protein 1A)PBP2 (Penicillin-binding protein 2)

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