Advances in chemistry and bioactivity of parthenolide.
Nat Prod Rep
; 37(4): 541-565, 2020 04 01.
Article
in En
| MEDLINE
| ID: mdl-31763637
ABSTRACT
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.
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Sesquiterpenes
Limits:
Animals
/
Humans
Language:
En
Journal:
Nat Prod Rep
Journal subject:
QUIMICA
Year:
2020
Document type:
Article
Affiliation country: