Alantolactone

Catalog No.S8318 Synonyms: helenin, helenine, Eupatal

Alantolactone Chemical Structure

Molecular Weight(MW): 232.32

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

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  • Colon cancer cell lines (A) SW620, (B) HCT116, and (C) HT29 were treated with different concentrations (60, 12, 2.4, 0.48, and 0.098 μM) of nifuroxazide (nifu), niclosamide (nicl), cryptotanshinone (cry), and a lantolactone (ala), respectively, for 72 h. Cell proliferation in each group was detected by MTT assay. (D) HCT116, SW620, and HT29 cell lines were suppressed with niclosamide treatment at different concentrations (20, 10, 5, 2.5, and 1.25 μM) for 72 h. Subsequently, cell proliferation in each group was detected by MTT assay. The data were obtained from 3 independent experiments.

    Onco Targets Ther, 2017, 10:1767-1776. Alantolactone purchased from Selleck.

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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

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].

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].

Protocol

Cell Research:[1]
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  • 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.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: athymic BALB/c nude mice
  • Formulation: DMSO 0.1% v/v(PBS)
  • Dosages: 2.5 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 46 mg/mL (198.0 mM)
Ethanol 46 mg/mL (198.0 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 232.32
Formula

C15H20O2

CAS No. 546-43-0
Storage powder
Synonyms helenin, helenine, Eupatal

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID