Nanoformulations of Ursolic Acid: A Modern Natural Anticancer Molecule

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.

Efficacy of Ursolic Acid-Enriched Water-Soluble and Not Cytotoxic Nanoparticles against Enterococci

“…Meticulous literature research to find UA-based polymer formulations as possible antimicrobial agents revealed to us that, while there are numerous articles on the in vitro antimicrobial activity of unformulated UA or its derivatives, articles regarding the in vitro antimicrobial activity of UA-based polymer formulations are practically absent. Most of the previously prepared NPs loaded with UA have, in fact, been studied for their anti-inflammatory [57,58] or antitumor activity [59][60][61][62]. To the best of our knowledge, except for our previous article on UA-loaded dendrimer NPs whose antibacterial activity was not attributable to UA [55], the only article on the antimicrobial activity of a UAliquid crystalline systems-based formulation established the improvement of the antifungal activity of UA [63].…”

Exploring potential targets of Actinidia Chinensis Planch root against hepatocellular carcinoma based on network pharmacology and molecular docking and development and verification of immune-associated prognosis features for hepatocellular carcinoma

“…In our study, 2 active ingredients, namely UA and quercetin, were found to act on BIRC5 protein targets. Ursolic acid (UA), also known as 3beta-hydroxyurs-12-en-28-oic acid, is a natural pentacyclic terpenoid with broad anti-cancer activity (40,41). Previous studies have discovered that UA can promote the apoptosis of liver cancer cells by activating caspase-3 and blocking the PI3K/Akt/survivin signaling pathway (42)(43)(44).…”

Extracts of Knoxia roxburghii (Spreng.) M. A. Rau Induce Apoptosis in Human MCF-7 Breast Cancer Cells via Mitochondrial Pathways

“…Many studies have shown that triterpenoids have obvious inhibitory effects on breast cancer, lung cancer, rectal cancer, and cancers of the central nervous system [ 18 , 19 , 20 ]. Ursolic acid, damnacanthal, bergapten, and 2α,3α,24-trihydroxy-12-alkene-28-ursolic acid have been isolated from KR [ 21 , 22 ], and have been proven to have anti-tumor effects [ 14 , 23 , 24 , 25 , 26 , 27 , 28 ].…”