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      Ursolic Acid and Its Derivatives as Bioactive Agents

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          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.

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          Pentacyclic Triterpene Distribution in Various Plants – Rich Sources for a New Group of Multi-Potent Plant Extracts

          Pentacyclic triterpenes are secondary plant metabolites widespread in fruit peel, leaves and stem bark. In particular the lupane-, oleanane-, and ursane triterpenes display various pharmacological effects while being devoid of prominent toxicity. Therefore, these triterpenes are promising leading compounds for the development of new multi-targeting bioactive agents. Screening of 39 plant materials identified triterpene rich (> 0.1% dry matter) plant parts. Plant materials with high triterpene concentrations were then used to obtain dry extracts by accelerated solvent extraction resulting in a triterpene content of 50 ‑ 90%. Depending on the plant material, betulin (birch bark), betulinic acid (plane bark), oleanolic acid (olive leaves, olive pomace, mistletoe sprouts, clove flowers), ursolic acid (apple pomace) or an equal mixture of the three triterpene acids (rosemary leaves) are the main components of these dry extracts. They are quantitatively characterised plant extracts supplying a high concentration of actives and therefore can be used for development of phytopharmaceutical formulations.
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            Parkinson's Disease and Its Management: Part 1: Disease Entity, Risk Factors, Pathophysiology, Clinical Presentation, and Diagnosis.

            This article-the first of a five-part series-discusses possible causes, symptoms, diagnosis, and goals for treatment of Parkinson's disease. Identifying diseases that have similar presentations is an important component of the diagnostic process.
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              Lupeol, a novel anti-inflammatory and anti-cancer dietary triterpene.

              In the Western world, an average of 250 mg per day of triterpenes (member of phytosterol family), largely derived from vegetable oils, cereals, fruits and vegetables is consumed by humans. During the last decade, there has been an unprecedented escalation of interest in triterpenes due to their cholesterol-lowering properties and evidence of this phenomenon include at least 25 clinical studies, 20 patents and at least 10 major commercially triterpene-based products currently being sold all around the world. Lupeol a triterpene (also known as Fagarsterol) found in white cabbage, green pepper, strawberry, olive, mangoes and grapes was reported to possess beneficial effects as a therapeutic and preventive agent for a range of disorders. Last 15 years have seen tremendous efforts by researchers worldwide to develop this wonderful molecule for its clinical use for the treatment of variety of disorders. These studies also provide insight into the mechanism of action of Lupeol and suggest that it is a multi-target agent with immense anti-inflammatory potential targeting key molecular pathways which involve nuclear factor kappa B (NFkappaB), cFLIP, Fas, Kras, phosphatidylinositol-3-kinase (PI3K)/Akt and Wnt/beta-catenin in a variety of cells. It is noteworthy that Lupeol at its effective therapeutic doses exhibit no toxicity to normal cells and tissues. This mini review provides detailed account of preclinical studies conducted to determine the utility of Lupeol as a therapeutic and chemopreventive agent for the treatment of inflammation and cancer.
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                Author and article information

                Journal
                Molecules
                Molecules
                molecules
                Molecules
                MDPI
                1420-3049
                29 July 2019
                August 2019
                : 24
                : 15
                : 2751
                Affiliations
                [1 ]Department of Chemistry, Faculty of Science and Agriculture, University of Fort Hare, Private Bag X1314, Alice 5700, South Africa
                [2 ]Department of Chemical and Physical Sciences, Faculty of Natural Sciences, Walter Sisulu University, Private Bag X1, Mthatha 5117, South Africa
                [3 ]Department of Human Biology, Faculty of Health Sciences, Walter Sisulu University, Private Bag X1, Mthatha 5117, South Africa
                Author notes
                [* ]Correspondence: ooyedeji@ 123456ufh.ac.za ; Tel.: +27-406-022-362
                Author information
                https://orcid.org/0000-0002-4872-5700
                Article
                molecules-24-02751
                10.3390/molecules24152751
                6695944
                31362424
                d5224106-76ce-4cb8-bfd7-d551fe7b3162
                © 2019 by the authors.

                Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license ( http://creativecommons.org/licenses/by/4.0/).

                History
                : 20 June 2019
                : 25 July 2019
                Categories
                Review

                non-communicable diseases,pentacyclic triterpenoids,ursolic acid,derivatives,sources,biological studies,clinical trials.

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