Kalpana Kalpana (Editor)

Parthenolide

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Molar mass
  
248.317 g/mol

Parthenolide httpsuploadwikimediaorgwikipediacommonsthu

Parthenolide is a sesquiterpene lactone of the germacranolide class which occurs naturally in the plant feverfew (Tanacetum parthenium), after which it is named. It is found in highest concentration in the flowers and fruit. Feverfew is used in herbalism and is purportedly useful for a variety of aliments. Many vendors of feverfew remedies specify the content of parthenolide in their products, because it is believed to be the primary chemical constituent responsible for biological activity.

Lack of solubility in water and bioavailability limits the potential of parthenolide as a drug. Drug researchers are trying to develop synthetic analogs instead that will be absorbed to a more useful extent. It also inhibits HDAC1 protein without affecting other class I/II HDACs, which leads to sustained DNA damage response in certain cells (required for apoptosis).

In vitro biological activities

Parthenolide has a variety of reported in vitro biological activities, including:

  • Modulation of the NF-κB-mediated inflammatory responses in experimental atherosclerosis.
  • intraneural or systemic application promotes axon regeneration in the peripheral nervous system
  • Inducing apoptosis in acute myelogenous leukemia (AML) cells, leaving normal bone marrow cells relatively unscathed. Moreover, the compound may get at the root of the disease because it also kills stem cells that give rise to AML. Parthenolide is under consideration as a potential cancer drug in combination with sulindac.
  • Activity against a parasite Leishmania amazonensis.
  • Microtubule-interfering activity.
  • Anti-inflammatory and anti-hyperalgesic effects.
  • Blocking lipopolysaccharide-induced osteolysis through the suppression of NF-κB activity.
  • inducing apoptosis and production of reactive oxygen species in high-risk pre-B leukemia cells.
  • Parthenolide induces MITF M isoform downregulation and senescence in MITF-Mhigh melanoma cells
  • Parthenolide has been found to act as an agonist of the adiponectin receptor 2 (AdipoR2).

    References

    Parthenolide Wikipedia