Wang Longyun, Yin Qianqian, Liu Cun, Tang Ying, Sun Changgang, Zhuang Jing
College of Traditional Chinese Medicine, Shandong University of Traditional Chinese Medicine, Jinan, China.
College of First Clinical Medicine, Shandong University of Traditional Chinese Medicine, Jinan, China.
Front Pharmacol. 2021 Jul 5;12:706121. doi: 10.3389/fphar.2021.706121. eCollection 2021.
Ursolic acid (UA) is a natural pentacyclic triterpene derived from fruit, herb, and other plants. UA can act on molecular targets of various signaling pathways, inhibit the growth of cancer cells, promote cycle stagnation, and induce apoptosis, thereby exerting anticancer activity. However, its poor water-solubility, low intestinal mucosal absorption, and low bioavailability restrict its clinical application. In order to overcome these deficiencies, nanotechnology, has been applied to the pharmacological study of UA. In this review, we focused on the absorption, distribution, and elimination pharmacokinetics of UA in vivo, as well as on the research progress in various UA nanoformulations, in the hope of providing reference information for the research on the anticancer activity of UA. Relevant research articles on Pubmed and Web of Science in recent years were searched selectively by using the keywords and subheadings, and were summarized systematically. The improvement of the antitumor ability of the UA nanoformulations is mainly due to the improvement of the bioavailability and the enhancement of the targeting ability of the UA molecules. UA nanoformulations can even be combined with computational imaging technology for monitoring or diagnosis. Currently, a variety of UA nanoformulations, such as micelles, liposomes, and nanoparticles, which can increase the solubility and bioactivity of UA, while promoting the accumulation of UA in tumor tissues, have been prepared. Although the research of UA in the nanofield has made great progress, there is still a long way to go before the clinical application of UA nanoformulations.
熊果酸（UA）是一种天然的五环三萜，来源于水果、草药及其他植物。UA可作用于多种信号通路的分子靶点，抑制癌细胞生长，促进细胞周期停滞并诱导凋亡，从而发挥抗癌活性。然而，其水溶性差、肠道黏膜吸收低以及生物利用度低限制了其临床应用。为克服这些不足，纳米技术已应用于UA的药理学研究。在本综述中，我们重点关注了UA在体内的吸收、分布和消除药代动力学，以及各种UA纳米制剂的研究进展，以期为UA抗癌活性的研究提供参考信息。通过使用关键词和副标题，对近年来PubMed和Web of Science上的相关研究文章进行了选择性检索，并进行了系统总结。UA纳米制剂抗肿瘤能力的提高主要归因于生物利用度的提高和UA分子靶向能力的增强。UA纳米制剂甚至可与计算机成像技术相结合用于监测或诊断。目前，已经制备了多种UA纳米制剂，如胶束、脂质体和纳米颗粒，它们可以增加UA的溶解度和生物活性，同时促进UA在肿瘤组织中的蓄积。尽管UA在纳米领域的研究取得了很大进展，但UA纳米制剂的临床应用仍有很长的路要走。
