Advances in chemistry and bioactivity of parthenolide

Review covering up to 07/2019(-)-Parthenolide is a germacrane sesquiterpene lactone, available in ample amounts from the traditional medical plant feverfew (Tanacetum parthenium). Acting as a covalently reactive compound, it displays anti-inflammatory, redox-modulating, and epigenetic activities, as...

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Vydáno v:Natural product reports Ročník 37; číslo 4; s. 541
Hlavní autoři: Freund, Robert R A, Gobrecht, Philipp, Fischer, Dietmar, Arndt, Hans-Dieter
Médium: Journal Article
Jazyk:angličtina
Vydáno: England 01.04.2020
ISSN:1460-4752, 1460-4752
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Shrnutí:Review covering up to 07/2019(-)-Parthenolide is a germacrane sesquiterpene lactone, available in ample amounts from the traditional medical plant feverfew (Tanacetum parthenium). Acting as a covalently reactive compound, it displays anti-inflammatory, redox-modulating, and epigenetic activities, as well as selective cytotoxicity towards cancer stem and progenitor cells. Furthermore, parthenolide was found to modulate microtubule dynamics by interfering with the detyrosination of α-tubulin, a specific posttranslational modification of the cytoskeleton. This review interfaces recently achieved parthenolide syntheses with strategies for bioactivity-based derivatization. Furthermore, chemical probe development from parthenolide is discussed, leading to a qualified summary of reported biological activities and implicated or identified targets. Special emphasis is given to parthenolide-induced microtubule modulation and the recently characterized tubulin carboxypeptidase enzymes involved in nerve (re)growth, cardiac muscle cell function, and metastasis development.
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ISSN:1460-4752
1460-4752
DOI:10.1039/c9np00049f