Alantolactone

Synonyms: helenin, helenine

Alantolactone, a naturally occurring eudesmane-type sesquiterpene lactone (SL), could induce activin/SMAD3 signaling and disrupt Cripto-1/activin receptor type II A interaction.

Alantolactone Chemical Structure

Alantolactone Chemical Structure

CAS No. 546-43-0

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Biological Activity

Description Alantolactone, a naturally occurring eudesmane-type sesquiterpene lactone (SL), could induce activin/SMAD3 signaling and disrupt Cripto-1/activin receptor type II A interaction.
Targets
STAT3 [1] activin/SMAD3 [3]
In vitro
In vitro Alantolactone selectively suppresses STAT3 activation and exhibits potent anticancer activity in MDA-MB-231 cells. Alantolactone effectively suppressed both constitutive and inducible STAT3 activation at tyrosine 705. It decreased STAT3 translocation to the nucleus, its DNA-binding, and STAT3 target gene expression. Alantolactone significantly inhibits STAT3 activation with a marginal effect on MAPKs and on NF-κB transcription; however, this effect is not mediated by inhibiting STAT3 upstream kinases. SHP-1, SHP-2, and PTEN, which are protein tyrosine phosphatases (PTPs) were not affected by alantolactone. Alantolactone treatment resulted in the inhibition of migration, invasion, adhesion, and colony formation[1]. Alantolactone could induce activin signaling and activin target gene expression. Alantolactone activated the activin signaling pathway in a cancer cell line. It could promote SMAD2/3 nuclear translocation in a very short time[3].
Cell Research Cell lines MDA-MB-231 and MCF-7 cells
Concentrations 15 μM
Incubation Time 24 h
Method

Cell viability was evaluated using MTT assay. The cells were seeded into 96-well plates and maintained at 37 °C for 24 h. The cells were treated with alantolactone for 24 h. The MTT solution (0.5 mg/mL) was added to each well, and the cells were incubated for another 3 h. The MTT formazan crystals were dissolved in DMSO. The results were obtained by measuring the absorbance at a wavelength of 540 nm using a microplate reader.

In Vivo
In vivo In vivo administration of alantolactone inhibited the growth of human breast xenograft tumors[1]. Alantolactone exerts no toxic effect on liver and kidneys in vivo, The drug was well tolerated by mice and no mortality or any sign of pharmacotoxicity was found at a dose of 100 mg/kg during all the experimental periods. Alantolactone can cross blood-brain barrier[2].
Animal Research Animal Models athymic BALB/c nude mice
Dosages 2.5 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 232.32 Formula

C15H20O2

CAS No. 546-43-0 SDF Download Alantolactone SDF
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 46 mg/mL ( (198.0 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 46 mg/mL

Water : Insoluble


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In vivo
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