Drug intelligence / Profile preview

alantolactone

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral (experimental), Topical (experimental)
01

Overview

**Alantolactone** is a natural sesquiterpene lactone isolated predominantly from *Inula helenium* and *Radix inulae*.[1][3][4][5][7][9] It has demonstrated multiple pharmacological activities, including **anticancer**, **anti-inflammatory**, **antifungal**, **antibacterial**, **anthelmintic**, **antimicrobial**, **neuroprotective**, and **antitrypanosomal** effects.[3][4][5][7] Its anticancer actions involve inhibition of cell proliferation and induction of apoptosis through mitochondrial and endoplasmic reticulum stress, oxidative stress (ROS), and cell cycle arrest.[1][5][7] Alantolactone inhibits transcription factor **STAT3 activation**—by promoting STAT3 glutathionylation—and suppresses **NF-κB p65 nuclear translocation**.[1][3][13] It also disrupts the **Cripto-1/Activin receptor II complexes**, leading to activation of **SMAD3 signaling**.[4] The compound can downregulate pro-inflammatory cytokines (e.g., TNF-α, IL-1β, IL-6, IL-8, IL-17A, IL-23), attenuate hyperproliferation in psoriatic keratinocyte models, and modulate cancer-associated pathways such as MAPK, Aurora-A kinase, and YAP/TAZ.[3][5][7] Development strategies include improving oral bioavailability via combination with other agents and nano-formulations.[5] The compound is primarily researched in preclinical models, with no approved pharmaceutical formulation.[2][4][5][9]

Brand names
heleninEupatal
Other names
alantolactoneheleninEupatalalant camphor
02

Targets

STAT3 (Signal Transducer and Activator of Transcription 3)SMAD3 (SMAD family member 3)YAP1/TAZ (Yes-associated protein 1/Transcriptional coactivator with PDZ-binding motif complex)TDGF1 (Teratocarcinoma-derived growth factor 1)NLRP3 (Nod-like receptor family pyrin domain-containing protein 3)RELA (Nuclear Factor Kappa B Subunit p65)

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