Abstract
Background: 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. Objective: 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. Methods: 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. Key finding: 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. Conclusion: 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.
Highlights
A Close Connection Between Ursolic acid (UA) and CancerCancer is a complex disease caused by the abnormal proliferation of cells under the action of multiple factors (Yu et al, 2018)
The results showed that the UA release of the UA-loaded polymer micellar delivery system (UA-PMs) was significantly comparable and there was no obvious initial outburst, indicating that the micelles had controlled release behavior and could increase the accumulation of UA at tumor sites to some extent
Reduce the angiogenesis in chicken chorioallantoic membrane (CAM) of fertilized eggs; (CH-UA-containing polycaprolactone nanoparticles (UA-NPs) at 2μg/CAM could effectively reduce angiogenesis as compared with that of control group.) Inhibit the H22 tumor growth through antiangiogenesis induced by vascular endothelial growth factor (VEGF) signaling pathway blocking. (The volume of tumors of nanoparticle-treated group and control group was 1.12 ± 0.12 and 2.36 ± 0.32 cm3) Effectively diminish off-target effects and increase local drug concentrations of UA Induce overproduction of reactive oxygen species (ROS) and destruction of mitochondrial membrane potential, and resulted in the irreversible apoptosis in cancer cells. (The tumor weight of Folic acid (FA)-CS-UA-NPS group, UA group and normal saline control group was 2.1 ± 1.02 g, 3.48 ± 0.24 g and 5.26 ± 1.69g, respectively.) Reduce the cell viability in 70% after 72 h
Summary
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. 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
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