Drug intelligence / Profile preview

obtusifolin

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral, Topical
01

Overview

Obtusifolin is a **small molecule anthraquinone derivative** found primarily in the seeds of *Senna obtusifolia* and *Senna tora*. It has demonstrated anti-inflammatory activities, notably in preclinical models of osteoarthritis and dry eye disease. Its mechanism is mainly through **inhibition of the NF-κB signaling pathway**—reducing phosphorylation of p65 and blocking the expression of downstream inflammatory mediators such as MMP3, MMP13, and COX2 in osteoarthritis[1][3]. Additionally, obtusifolin suppresses ERK/p38 MAPK signaling, further lowering pro-inflammatory cytokine levels (TNF-α, IL-6, MCP-1), and increases IL-10 production[3]. It has shown protective roles in dry eye disease by restoring tear production, reducing conjunctival irritation, and alleviating goblet cell loss[3]. In vitro, obtusifolin also inhibits high glucose-induced mitochondrial apoptosis by modulating ROS generation and apoptotic pathways in endothelial cells[7]. Investigational indications include osteoarthritis and dry eye disease; the compound is not approved for human use and is primarily used in research settings.

Other names
obtusifolin2,8-dihydroxy-1-methoxy-3-methylanthracene-9,10-dione
02

Targets

MIF (Oxidized macrophage migration inhibitory factor)MMP13 (Matrix metalloproteinase-13)MMP3 (Matrix metalloproteinase-3)RELA (Nuclear Factor Kappa B Subunit p65)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)MAPK14 (p38 mitogen-activated protein kinase alpha)ERK

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