The Emerging Potential of Parthenolide Nanoformulations in Tumor Therapy

Abstract

Plant-derived sesquiterpene lactones are promising natural sources for the discovery of anti-cancer drugs. As an extensively studied sesquiterpene lactone, the tumor suppression effect of parthenolide (PTL) has been clarified by targeting a number of prominent signaling pathways and key protein regulators in carcinogenesis. Notably, PTL was also the first small molecule reported to eradicate cancer stem cells. Nevertheless, the clinical application of PTL as an antitumor agent remains limited, owing to some disadvantages such as low water solubility and poor bioavailability. Thus, nanomedicine has attracted much interest because of its great potential for transporting poorly soluble drugs to desired body sites. In view of the significant advantages over their free small-molecule counterparts, nanoparticle delivery systems appear to be a potential solution for addressing the delivery of hydrophobic drugs, including PTL. In this review, we summarized the key anticancer mechanisms underlined by PTL as well as engineered PTL nanoparticles synthesized to date. Therefore, PTL nanoformulations could be an alternative strategy to maximize the therapeutic value of PTL.

Sesquiterpene Lactones and Cancer: New Insight into Antitumor and Anti-inflammatory Effects of Parthenolide-Derived Dimethylaminomicheliolide and Micheliolide

“…Some disadvantages have been cited by the previously published data. For instance, in a study, there are some disadvantages such as poor bioavailability and low water solubility [ 25 ]. Another disadvantage is that these biological extracts are obtained from the plants.…”

Research status of indole-modified natural products

“…32 Parthenolide is a natural product of sesquiterpene lactones, which is derived from the flower buds of Tanacetum balsamita and possesses anti-tumor activity. 33 Bommagani et al designed and synthesized a series of parthenolide-indole derivatives, hoping to obtain promising drugs against hematological tumors. Derivative 11 (Fig.…”

“…Biological activity of triterpenoid-indole derivatives[23][24][25][26][27][28][29][30][31][32][33][34][35][36] …”

Liposomes as Multifunctional Nano-Carriers for Medicinal Natural Products

“…3,5-Dipentadecyloxybenzamidine hydrochloride (TRX-20)-modified liposomes encapsulating triptolide significantly improved the anti-inflammatory effects in the membranous nephropathic model ( Yuan et al, 2017 ). Due to the scaffold of α -methylene- γ -lactone, parthenolide has high electrophilicity to alkylate proteins and thus processes various bioactivities ( Jin et al, 2018 ; An et al, 2022 ). pH-sensitive liposomes PTL-Lips encapsulating parthenolide have enhanced its antitumor efficacy ( Gao et al, 2020a ).…”