The Emerging Potential of Parthenolide Nanoformulations in Tumor Therapy.

The Emerging Potential of Parthenolide Nanoformulations in Tumor Therapy.
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DOI:
10.2147/dddt.s355059
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发表时间:
2022
期刊:
Drug design, development and therapy
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中科院分区:
其他
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植物源倍半萜内酯是发现抗癌药物的重要天然来源。作为一种被广泛研究的倍半萜内酯,parthenolide (PTL)的抑瘤作用已被阐明,它通过靶向肿瘤发生过程中一些重要的信号通路和关键的蛋白调节因子。值得注意的是,PTL也是第一个被报道可以根除癌症干细胞的小分子。然而,由于其水溶性低、生物利用度差等缺点,PTL作为抗肿瘤药物的临床应用仍然有限。因此,纳米医学吸引了很多人的兴趣,因为它具有将难溶性药物运送到所需身体部位的巨大潜力。鉴于其相对于自由的小分子递送系统的显著优势,纳米颗粒递送系统似乎是解决包括PTL在内的疏水药物递送的潜在解决方案。本文综述了PTL的主要抗癌机制以及迄今为止合成的工程化PTL纳米颗粒。因此,PTL纳米制剂可能是一种替代策略,以最大化PTL的治疗价值。
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.
倍半萜结合Gly-Leu-Ser/Lys-“共适应袋”抑制肺癌细胞上皮-间质转化
DOI: 10.18632/oncotarget.19599
发表时间: 2017-09-19
期刊: Oncotarget
影响因子: --
作者:
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
通讯作者: Yang C