Abstract
Non-communicable diseases (NCDs) such as cancer, diabetes, and chronic respiratory and cardiovascular diseases continue to be threatening and deadly to human kind. Resistance to and side effects of known drugs for treatment further increase the threat, while at the same time leaving scientists to search for alternative sources from nature, especially from plants. Pentacyclic triterpenoids (PT) from medicinal plants have been identified as one class of secondary metabolites that could play a critical role in the treatment and management of several NCDs. One of such PT is ursolic acid (UA, 3 β-hydroxy-urs-12-en-28-oic acid), which possesses important biological effects, including anti-inflammatory, anticancer, antidiabetic, antioxidant and antibacterial effects, but its bioavailability and solubility limits its clinical application. Mimusops caffra, Ilex paraguarieni, and Glechoma hederacea, have been reported as major sources of UA. The chemistry of UA has been studied extensively based on the literature, with modifications mostly having been made at positions C-3 (hydroxyl), C12-C13 (double bonds) and C-28 (carboxylic acid), leading to several UA derivatives (esters, amides, oxadiazole quinolone, etc.) with enhanced potency, bioavailability and water solubility. This article comprehensively reviews the information that has become available over the last decade with respect to the sources, chemistry, biological potency and clinical trials of UA and its derivatives as potential therapeutic agents, with a focus on addressing NCDs.
Highlights
Non-communicable diseases (NCDs), including cancers, cardiovascular diseases, pulmonary illnesses, and diabetes, account for nearly 71 percent of all fatalities globally, as reported by the WorldHealth Organization
These researchers explored the structure-activity relationship of the synthesized bioactive analogues. They mainly focused their modifications on hydroxyl position C-3 and carboxylic group C-17 of the ursolic acid (UA) parent compound to produce a series of derivatives
Due to its low toxicity, anticancer activities, and commercial availability with various structural modifications, UA is regarded as a pillar through organic semi-synthesis, and this has attracted more researchers to studying and discovering various ursolic acid derivatives [61]
Summary
Non-communicable diseases (NCDs), including cancers, cardiovascular diseases, pulmonary illnesses, and diabetes, account for nearly 71 percent of all fatalities globally, as reported by the World. One group of compounds from plants is called pentacyclic triterpenoids (PT). These are defined as a group of 30 carbon structural compounds with interesting biological activities and great diversity, with more than 100 chemical skeletons of carbon. PT are used in treatment of several cancers without damaging normal cells through toxicity [4] These PT have revealed therapeutic and chemical preventive characteristics in skin, lung, liver and lung disease [5]. This review provides an overview of the structural development of UA and its derivatives, along with their advantages as anti-cancer, anti-inflammatory, antibacterial, anti-diabetic and neuroprotective therapeutic agents, as well as their herbicidal activities
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