Description
ACTIVE MOLECULES DESCRIPTION
The most important biologically active principles are the sesquiterpene lactones, the principal one being parthenolide. More than 30
sesquiterpene lactones have been identified in this herb. In general, there are 5 different types of sesquiterpene lactones, which may be classified by chemical ring structures. Feverfew
contains eudesmanolides, germacranolides, and guaianolides. Parthenolide is a germacranolide.
The following flavonoids have been isolated: 6 hydroxykaempferol 3,6-dimethyl ether, 6 hydroxykaempferol 3,6,4′-trimethyl ether
(tanetin), quercetagetin 3,6-dimethyl ether,
quercetagetin 3,6,3′-trimethyl ether (accompanied by isomeric 3,6,4′-trimethylether), quercetin, apigenin, and luteolin.
ANTI-INLAMMATORY ACTIVITY
• Parthenolide binds to and inhibits IκB kinase complex
(IKK)β
• Parthenolide inhibits prostaglandine synthetase
• Parthenolide reduces human neutrophil oxidative burst
activity
Parthenolide, a sesquiterpene lactone, expresses multiple anti
cancer and anti inflammatory activities.
EFFECTS ON PLATELETS
Extracts of feverfew inhibit platelet 5-HT secretion via neutralisation of sulfhydryl groups inside or outside the cell. The
sesquiterpenes in feverfew contain the alpha methylenebutyrolactone unit capable of reacting with sulfhydrylgroups. Feverfew extracts are not only potent inhibitors of
serotonin release from platelets but also of polymorphonuclear leukocyte granules.
The Feverfew plant derived compounds parthenolide enhances platelet production and attenuates platelet activation through NF
kB inhabitation. INHIBITION OF HISTAMINE RELEASE A chloroform extract of feverfew inhibited histamine release from rat peritoneal mast cells in a different manner from established mast cell inhibitors, such as cromoglycate and quercetin. The exact mechanism of action has not been determined but may be mediated by entry of calcium into mast cells.
Anticancer activity – Mechanisms of action may include: – Cytotoxic action associated with interruption of DNA replication by the highly reactive lactone ring, epoxide, and methylene groups of parthenolide through inhibition of thymidine into DNA oxidative stress, and intracellular thioldepletion, endoplasmic reticulum stress, and mitochondrial dysfunction.Parthenolide and similar lactones displayed anticancer activity against several
human cancer cell lines, including human fibroblasts, human laryngeal carcinoma, human cells transformed with simian virus, human epidermoid cancer of the
nasopharynx, and anti Epstein Barr early antigen activity .Migraine headache, prophylactic treatment – Inhibition of prostaglandin synthesis, decrease of vascular smooth muscle spasm, and blockage of platelet granule secretion. Effects on vascular smooth muscle – Treatment with parthenolide significantly decreased the [(3)H]thymidine
incorporation into DNA by 30%~56%. Addition of parthenolide also increased cell population at G(0)/G(1) phase and decreased cell population at S phase, which is
consistent with its stimulatory effects on p21 and p27. In addition, parthenolide also increased IkappaBalpha expression and reduced Cox-2 expression in a time
dependent manner. Research shows that Parthenolide inhibits proliferation of vascular smooth muscle cells
through induction of Go/G1 phase cycle arrest.
