Abstract
Ursolic acid is a pharmacologically active pentacyclic triterpenoid derived from medicinal plants, fruit, and vegetables. The pharmacological activities of ursolic acid have been extensively studied over the past few years and various reports have revealed that ursolic acid has multiple biological activities, which include anti-inflammatory, antioxidant, anti-cancer, etc. In terms of cancer treatment, ursolic acid interacts with a number of molecular targets that play an essential role in many cell signaling pathways. It suppresses transformation, inhibits proliferation, and induces apoptosis of tumor cells. Although ursolic acid has many benefits, its therapeutic applications in clinical medicine are limited by its poor bioavailability and absorption. To overcome such disadvantages, researchers around the globe have designed and developed synthetic ursolic acid derivatives with enhanced therapeutic effects by structurally modifying the parent skeleton of ursolic acid. These structurally modified compounds display enhanced therapeutic effects when compared to ursolic acid. This present review summarizes various synthesized derivatives of ursolic acid with anti-cancer activity which were reported from 2015 to date.
Highlights
At present, cancer remains a significant health problem and is the second leading cause of death worldwide
The ursolic acid-based derivatives containing at least an OH and NH moiety in the hydroxamate part displayed good cytotoxicity and were significantly less selective to the cancer cells when compared to the oleanolic acid-based compounds
Jiang et al synthesized a series of Ursolic acid (UA) derivatives as inhibitors of Nuclear factor kappa B (NF-κB) by introducing long-chain amide moieties at the C-28 position, and the β-hydroxy group C-3 was protected by an acetyl group
Summary
Cancer remains a significant health problem and is the second leading cause of death worldwide. Extensive research has been performed to study the therapeutic effect of drugs derived from plants against a number of cancers, and the outstanding results indicate that most natural active compounds have potent anticancer effects [5]. In terms of biological perspectives, the large group of pentacyclic triterpenoids with basic molecular structures with five membered rings have attracted the attention of many researchers due to their notable broad spectrum of pharmacological activities including anticancer, anti-inflammatory, antioxidant, antiviral, antimicrobial, etc.
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