School of Pharmaceutical Sciences, Qilu University of Technology (Shandong Academy of Sciences), Jinan, Shandong Province, People's Republic of China.
College of TCM, Shandong University of Traditional Chinese Medicine, Jinan, Shandong Province, People's Republic of China.
Drug Des Devel Ther. 2022 Apr 29;16:1255-1272. doi: 10.2147/DDDT.S355059. eCollection 2022.
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.
植物来源的倍半萜内酯是发现抗癌药物的有前途的天然来源。作为一种广泛研究的倍半萜内酯，小白菊内酯（PTL）通过靶向致癌作用中的许多突出信号通路和关键蛋白调节剂，其肿瘤抑制作用已得到阐明。值得注意的是，PTL 也是第一个被报道能够根除癌症干细胞的小分子。然而，PTL 作为抗肿瘤药物的临床应用仍然受到限制，这是由于其一些缺点，如水溶性低和生物利用度差。因此，纳米医学因其将难溶性药物递送到所需部位的巨大潜力而引起了广泛关注。鉴于其与游离小分子类似物相比具有显著优势，纳米颗粒递送系统似乎是解决包括 PTL 在内的疏水性药物递送的潜在解决方案。在这篇综述中，我们总结了 PTL 所依据的关键抗癌机制以及迄今为止合成的工程化 PTL 纳米颗粒。因此，PTL 纳米制剂可能是最大限度发挥 PTL 治疗价值的替代策略。
