Parthenolide - (Feverfew)

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

Cancer Lett. 2017 Dec 1;410:180-190. doi: 10.1016/j.canlet.2017.09.034. Epub 2017 Sep 28.

Pharmacological evidence for the bone-autonomous contribution of the NFκB/β-catenin axis to breast cancer related osteolysis.

Marino S1, Bishop RT2, Logan JG3, Mollat P4, Idris AI5.

Author information


The NFκB signaling pathway is implicated in breast cancer and bone metastasis. However, the bone-autonomous contribution of NFκB to breast cancer-induced osteolysis is poorly understood. Here, we report that pretreatment of osteoblasts with the sesquiterpene lactone Parthenolide (PTN), a verified NFκB inhibitor, prior to exposure to conditioned medium from human and mouse breast cancer cell lines enhanced osteoblast differentiation and reduced osteoblast ability to stimulate osteoclastogenesis.

PTN prevented breast cancer-induced osteoclast formation and reduced the ability of breast cancer cells to prolong osteoclast survival and to inhibit osteoclast apoptosis. In vivo, administration of PTN in immuno-competent mice reduced osteolytic bone loss and skeletal tumour growth following injection of the syngeneic 4T1-BT1 cells and reduced local osteolysis caused by conditioned medium from human and mouse osteotropic breast cancer cell lines.

Mechanistic studies revealed that NFκB inhibition by PTN in osteoblasts and osteoclasts was accompanied by a significant increase in β-catenin activation and expression. Collectively, these results raise the possibility that combined targeting of NFκB and β-catenin signalling in the tumour microenvironment may be of value in the treatment of breast cancer related osteolysis.

Hydrogen peroxide-induced apoptosis of human lens epithelial cells is inhibited by parthenolide.

Shentu XC, Ping XY, Cheng YL, Zhang X, Tang YL, Tang XJ.

Int J Ophthalmol. 2018 Jan 18;11(1):12-17. doi: 10.18240/ijo.2018.01.03. eCollection 2018.



Parthenolide prevents resistance of MDA-MB231 cells to doxorubicin and mitoxantrone: the role of Nrf2.

Carlisi D, De Blasio A, Drago-Ferrante R, Di Fiore R, Buttitta G, Morreale M, Scerri C, Vento R, Tesoriere G.

Cell Death Discov. 2017 Dec 4;3:17078. doi: 10.1038/cddiscovery.2017.78. eCollection 2017.

Crystal Structures and Human Leukemia Cell Apoptosis Inducible Activities of ParthenolideAnalogues Isolated from Piptocoma rufescens.

Ren Y, Gallucci JC, Li X, Chen L, Yu J, Kinghorn AD.

J Nat Prod. 2018 Jan 19. doi: 10.1021/acs.jnatprod.7b01079. [Epub ahead of print]

Regulator of calcineurin 1 modulates vascular contractility and stiffness through the upregulation of COX-2-derived prostanoids.

García-Redondo AB, Esteban V, Briones AM, Díaz Del Campo LS, González-Amor M, Méndez-Barbero N, Campanero MR, Redondo JM, Salaices M.

Pharmacol Res. 2018 Jan 5. pii: S1043-6618(17)31245-8. doi: 10.1016/j.phrs.2018.01.001. [Epub ahead of print]

Acid-Induced Rearrangement of Epoxygermacranolides: Synthesis of Furanoheliangolides and Cadinanes from Nobilin.

De Mieri M, Smieško M, Ismajili I, Kaiser M, Hamburger M.

Molecules. 2017 Dec 18;22(12). pii: E2252. doi: 10.3390/molecules22122252.

The natural sesquiterpene lactones arglabin, grosheimin, agracin, parthenolide, and estafiatin inhibit T cell receptor (TCR) activation.

Schepetkin IA, Kirpotina LN, Mitchell PT, Kishkentaeva АS, Shaimerdenova ZR, Atazhanova GA, Adekenov SM, Quinn MT.

Phytochemistry. 2018 Feb;146:36-46. doi: 10.1016/j.phytochem.2017.11.010. Epub 2017 Dec 22.

Three newly identified lipophilic flavonoids in Tanacetum parthenium supercritical fluid extract penetrating the Blood-Brain Barrier.

Végh K, Riethmüller E, Hosszú L, Darcsi A, Müller J, Alberti Á, Tóth A, Béni S, Könczöl Á, Balogh GT, Kéry Á.

J Pharm Biomed Anal. 2018 Feb 5;149:488-493. doi: 10.1016/j.jpba.2017.11.029. Epub 2017 Nov 16.

Schizonticidal antimalarial sesquiterpene lactones from Magnolia champaca (L.) Baill. ex Pierre: microwave-assisted extraction, HPTLC fingerprinting and computational studies.

Mehrotra E, Vishwakarma J, Tripathi AC, Sonar PK, Saraf SK.

Nat Prod Res. 2017 Oct 31:1-5. doi: 10.1080/14786419.2017.1396595. [Epub ahead of print]

Parthenolide suppresses hypoxia-inducible factor-1α signaling and hypoxia induced epithelial-mesenchymal transition in colorectal cancer.

Kim SL, Park YR, Lee ST, Kim SW.

Int J Oncol. 2017 Dec;51(6):1809-1820. doi: 10.3892/ijo.2017.4166. Epub 2017 Oct 18.

Sesquiterpene binding Gly-Leu-Ser/Lys-"co-adaptation pocket" to inhibit lung cancer cell epithelial-mesenchymal transition.

Ai XY, Zhang H, Gao SY, Qin Y, Zhong WL, Gu J, Li M, Qiao KL, Tian Q, Cui ZH, Yang JH, Bi Z, Xiao T, Chen S, Liu HJ, Zhou HG, Sun T, Yang C.

Oncotarget. 2017 Jul 26;8(41):70192-70203. doi: 10.18632/oncotarget.19599. eCollection 2017 Sep 19.

Pharmacological evidence for the bone-autonomous contribution of the NFκB/β-catenin axis to breast cancer related osteolysis.

Marino S, Bishop RT, Logan JG, Mollat P, Idris AI.

Cancer Lett. 2017 Dec 1;410:180-190. doi: 10.1016/j.canlet.2017.09.034. Epub 2017 Sep 28.

Osteopontin plays a unique role in resistance of CD34+/CD123+ human leukemia cell lines KG1a to parthenolide.

Mohammadi S, Zahedpanah M, Ghaffari SH, Shaiegan M, Nikbakht M, Nikugoftar M.

Life Sci. 2017 Nov 15;189:89-95. doi: 10.1016/j.lfs.2017.09.019. Epub 2017 Sep 19.

Smad4 re-expression increases the sensitivity to parthenolide in colorectal cancer.

Li X, Yang H, Ke J, Liu B, Lv X, Li X, Zhang Y.

Oncol Rep. 2017 Oct;38(4):2317-2324. doi: 10.3892/or.2017.5929. Epub 2017 Aug 29.

Parthenolide Promotes Differentiation of Osteoblasts Through the Wnt/β-Catenin Signaling Pathway in Inflammatory Environments.

Zhang X, Chen Q, Liu J, Fan C, Wei Q, Chen Z, Mao X.

J Interferon Cytokine Res. 2017 Sep;37(9):406-414. doi: 10.1089/jir.2017.0023. Epub 2017 Aug 22.

Anticancer activity profiling of parthenolide analogs generated via P450-mediated chemoenzymatic synthesis.

Alwaseem H, Frisch BJ, Fasan R.

Bioorg Med Chem. 2017 Aug 8. pii: S0968-0896(17)30909-4. doi: 10.1016/j.bmc.2017.08.009. [Epub ahead of print]

Parthenolide attenuates 7,12-dimethylbenz[a]anthracene induced hamster buccal pouch carcinogenesis.

Baskaran N, Selvam GS, Yuvaraj S, Abhishek A.

Mol Cell Biochem. 2017 Aug 12. doi: 10.1007/s11010-017-3151-5. [Epub ahead of print]

Hepatoprotective and cytotoxic activities of Anvillea garcinii and isolation of four new secondary metabolites.

Perveen S, Al-Taweel AM, Yusufoglu HS, Fawzy GA, Foudah A, Abdel-Kader MS.

J Nat Med. 2018 Jan;72(1):106-117. doi: 10.1007/s11418-017-1118-1. Epub 2017 Aug 9.

DMAPT inhibits NF-κB activity and increases sensitivity of prostate cancer cells to X-rays in vitro and in tumor xenografts in vivo.

Mendonca MS, Turchan WT, Alpuche ME, Watson CN, Estabrook NC, Chin-Sinex H, Shapiro JB, Imasuen-Williams IE, Rangel G, Gilley DP, Huda N, Crooks PA, Shapiro RH.

Natural or plant products for the treatment of neurological disorders: current knowledge.

Parvez MK.

Curr Drug Metab. 2017 Jul 10. doi: 10.2174/1389200218666170710190249. [Epub ahead of print]

Correction to: Bahabadi M, et al., Hepatoprotective effect of parthenolide in rat model of nonalcoholic fatty liver disease.

[No authors listed]

Immunopharmacol Immunotoxicol. 2017 Oct;39(5):x. doi: 10.1080/08923973.2017.1352255. Epub 2017 Jul 10. No abstract available.

643 Chapel Street South Yarra 3141 Australia

T: +61 3 9826 9898  E:  

All rights reserved 2020