Drug intelligence / Profile preview

astilbin

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral, Topical, Intravenous
01

Overview

Astilbin is a naturally occurring flavanonol glycoside (a type of flavonoid) found in various plants such as St. John’s wort (Hypericum perforatum), Smilax glabra rhizomes, and Astilbe species. It is used in traditional Chinese medicine and has demonstrated a range of pharmacological activities including anti-inflammatory, immunosuppressive, antioxidant, antibacterial, hepatoprotective effects and potential anticancer properties. Mechanistically, astilbin modulates immune responses by suppressing effector CD4+ T cell function and inflammatory cytokine production (such as TNF-α and IL-6), inhibits NF-κB signaling pathways involved in inflammation and cancer progression, reduces oxidative stress via Nrf2 activation pathways, inhibits enzymes like angiotensin-converting enzyme and aldose reductase relevant to metabolic diseases such as diabetes complications. Preclinical studies suggest efficacy for conditions including arthritis (with less toxicity than cyclosporine A), psoriasis-like skin disease via ferroptosis/cGAS-STING pathway modulation[7], diabetic nephropathy through TGF-β/Smad inhibition[10], burn wound healing[1], radioprotection[9], neurodegenerative diseases[4], gastric cancer apoptosis induction[3] among others.

Other names
Taxifolin 3-O-rhamnosideTaxifolin3-O-rhamnosideTaxifolin-3-O-rhamnosideDihydroquercitrin(2R-cis)-isomer of astilbin(2S-cis)-isomer of astilbinisoastilbinneoisoastilbin
02

Targets

CYP1B1 (Cytochrome P450 1B1)KLF4 (Krüppel-like factor 4)CTGF (Connective tissue growth factor)IL (Interleukins)MMP12 (Macrophage Metalloelastase)NOS1 (nNOS)NFE2L2 (Nuclear factor (erythroid-derived 2)-like 2)NF-κBPPARG (Peroxisome proliferator-activated receptor gamma)TNFA (Tumor necrosis factor alpha (soluble))

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