Parthenolide and its Analogues: A New Potential Strategy for the Treatment of Triple-Negative Breast Tumors

Abstract

Triple negative breast cancers (TNBC) are heterogeneous and aggressive pathologies, with distinct morphological and clinical characteristics associated with their genetic diversity, epigenetics, transcriptional changes and aberrant molecular patterns. Treatment with anti-neoplastic drugs exerts systemic effects with low specificity, and incipient improvement in overall survival due to chemoresistance and recurrence. New alternatives for TNBC treatment are urgent and parthenolide or its analogues have been explored. Parthenolide is a sesquiterpene lactone with promising antitumor effects against TNBC cell lines. This review highlights the importance of parthenolide and its analogue drugs in TNBC treatment.

Identification of a small molecule as inducer of ferroptosis and apoptosis through ubiquitination of GPX4 in triple negative breast cancer cells

“…Sesquiterpene lactone PTL showed moderate activity against breast cancer [30]. To improve the anticancer effect of parthenolide, we designed and synthesized a series of parthenolide derivatives.…”

Production of Plant Sesquiterpene Lactone Parthenolide in the Yeast Cell Factory

“…It contains an α-methylene-γ-butyrolactone group and an epoxide group, which show strong nuclear factor-kappaB (NF-κB)- and signal transduction and activation of transcription (STAT)-inhibition-mediated transcriptional suppression of pro-apoptotic genes . Parthenolide has been reported to inhibit pathogenicity in various types of cancer, such as myeloma, colorectal, breast, cervical, and prostate cancer. − However, parthenolide cannot achieve a proportional effect to its administered dose due to its low solubility in body fluids . ACT001 is a fumarate salt form of dimethylaminomicheliolide (DMAMCL) chemically synthesized from parthenolide. , It can rapidly distribute to tissues after oral administration and diffuse through the blood–brain barrier .…”

Generation of multicellular tumor spheroids with micro-well array for anticancer drug combination screening based on a valuable biomarker of hepatocellular carcinoma

“…It is an NF- κB inhibitor, that inhibits histone deacetylase 1 (HDAC-1) and DNA methyltransferase 1 (DMT-1) ( Bork et al, 1997 ; Freund et al, 2020 ). It has also been found to have anti-cancer activity in a variety of tumors, such as breast tumors, colorectal cancer, renal cell carcinoma, and et al ( Araújo et al, 2020 ; Liu D. et al, 2021 ; Liu X. et al, 2021 ). Combination treatment with Parthenolide and 5-FU provides synergistic anti-cancer effects in vitro and in vivo ( Kim S.-L. et al, 2013 ; Liu Dajun et al, 2013 ; Ding et al, 2019 ).…”