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      Phytochemical Investigation of New Algerian Lichen Species: Physcia Mediterranea Nimis

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          Abstract

          The present study provides new data concerning the chemical characterisation of Physcia mediterranea Nimis, a rare Mediterranean species belonging to the family Physciaceae. The phytochemical screening was carried out using GC-MS, HPLC-ESI-MS-MS, and NMR techniques. Hot extraction of n-hexane was carried out, followed by separation of the part insoluble in methanol: wax (WA-hex), from the part soluble in methanol (ME-hex). GC-MS analysis of the ME-hex part revealed the presence of methylbenzoic acids such as sparassol and atraric acid and a diterpene with a kaurene skeleton which has never been detected before in lichen species. Out of all the compounds identified by HPLC-ESI-MS-MS, sixteen compounds are common between WA-hex and ME-hex. Most are aliphatic fatty acids, phenolic compounds and depsides. The wax part is characterised by the presence of atranorin, a depside of high biological value. Proton 1H and carbon 13C NMR have confirmed its identification. Atranol, chloroatranol (depsides compound), Ffukinanolide (sesquiterpene lactones), leprolomin (diphenyl ether), muronic acid (triterpenes), and ursolic acid (triterpenes) have also been identified in ME-hex. The results suggested that Physcia mediterranea Nimis is a valuable source of bioactive compounds that could be useful for several applications as functional foods, cosmetics, and pharmaceuticals.

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          Coumarin: A Natural, Privileged and Versatile Scaffold for Bioactive Compounds

          Many naturally occurring substances, traditionally used in popular medicines around the world, contain the coumarin moiety. Coumarin represents a privileged scaffold for medicinal chemists, because of its peculiar physicochemical features, and the versatile and easy synthetic transformation into a large variety of functionalized coumarins. As a consequence, a huge number of coumarin derivatives have been designed, synthesized, and tested to address many pharmacological targets in a selective way, e.g., selective enzyme inhibitors, and more recently, a number of selected targets (multitarget ligands) involved in multifactorial diseases, such as Alzheimer’s and Parkinson’s diseases. In this review an overview of the most recent synthetic pathways leading to mono- and polyfunctionalized coumarins will be presented, along with the main biological pathways of their biosynthesis and metabolic transformations. The many existing and recent reviews in the field prompted us to make some drastic selections, and therefore, the review is focused on monoamine oxidase, cholinesterase, and aromatase inhibitors, and on multitarget coumarins acting on selected targets of neurodegenerative diseases.
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            A review of coumarin derivatives in pharmacotherapy of breast cancer.

            The coumarin (benzopyran-2-one, or chromen-2-one) ring system, present in natural products (such as the anticoagulant warfarin) that display interesting pharmacological properties, has intrigued chemists and medicinal chemists for decades to explore the natural coumarins or synthetic analogs for their applicability as drugs. Many molecules based on the coumarin ring system have been synthesized utilizing innovative synthetic techniques. The diversity oriented synthetic routes have led to interesting derivatives including the furanocoumarins, pyranocoumarins, and coumarin sulfamates (COUMATES), which have been found to be useful in photochemotherapy, antitumor and anti-HIV therapy, and as stimulants for central nervous system, antibacterials, anti-inflammatory, anti-coagulants, and dyes. Of particular interest in breast cancer chemotherapy, some coumarins and their active metabolite 7-hydroxycoumarin analogs have shown sulfatase and aromatase inhibitory activities. Coumarin based selective estrogen receptor modulators (SERMs) and coumarin-estrogen conjugates have also been described as potential antibreast cancer agents. Since breast cancer is the second leading cause of death in American women behind lung cancer, there is a strong impetus to identify potential new drug treatments for breast cancer. Therefore, the objective of this review is to focus on important coumarin analogs with antibreast cancer activities, highlight their mechanisms of action and structure-activity relationships on selected receptors in breast tissues, and the different methods that have been applied in the construction of these pharmacologically important coumarin analogs.
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              Ursolic acid in health and disease

              Ursolic acid (UA) is a natural triterpene compound found in various fruits and vegetables. There is a growing interest in UA because of its beneficial effects, which include anti-inflammatory, anti-oxidant, anti-apoptotic, and anti-carcinogenic effects. It exerts these effects in various tissues and organs: by suppressing nuclear factor-kappa B signaling in cancer cells, improving insulin signaling in adipose tissues, reducing the expression of markers of cardiac damage in the heart, decreasing inflammation and increasing the level of anti-oxidants in the brain, reducing apoptotic signaling and the level of oxidants in the liver, and reducing atrophy and increasing the expression levels of adenosine monophosphate-activated protein kinase and irisin in skeletal muscles. Moreover, UA can be used as an alternative medicine for the treatment and prevention of cancer, obesity/diabetes, cardiovascular disease, brain disease, liver disease, and muscle wasting (sarcopenia). In this review, we have summarized recent data on the beneficial effects and possible uses of UA in health and disease managements.
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                Author and article information

                Contributors
                Role: Academic Editor
                Journal
                Molecules
                Molecules
                molecules
                Molecules
                MDPI
                1420-3049
                20 February 2021
                February 2021
                : 26
                : 4
                : 1121
                Affiliations
                [1 ]Laboratory of Vegetal Biology and Environment, Biology Department, Badji Mokhtar University, Annaba 23000, Algeria; kerbouamarwa@ 123456gmail.com (M.K.); serradj.monia@ 123456gmail.com (M.A.A.)
                [2 ]Chemistry Department, University of Beira Interior, 6201-001 Covilha, Portugal; nsevolo.samba@ 123456ubi.pt (N.S.); ra.aitfella@ 123456ubi.pt (R.A.-L.); mlas@ 123456ubi.pt (L.S.)
                [3 ]Department of Clinical Analysis and Public Health, University Kimpa Vita, Uige 77, Angola
                [4 ]Fiber Materials and Environmental Technologies (FibEnTech), University of Beira Interior, 6201-001 Covilhã, Portugal
                [5 ]Laboratory of Valorisation and Conservation of Biological Resources, Biology Department, Faculty of Sciences, University M’Hamed Bougara, Boumerdes 35000, Algeria
                [6 ]Department of Analytical Chemistry, Nutrition and Food Science, Faculty of Chemistry, Chromatographic and mass analysis service (NUCLEUS), University of Salamanca, 37008 Salamanca, Spain; jfbb@ 123456usal.es (J.F.B.); raposo@ 123456usal.es (C.R.)
                Author notes
                [* ]Correspondence: rodilla@ 123456ubi.pt ; Tel.: +351-275-241-306
                Author information
                https://orcid.org/0000-0002-3973-6272
                https://orcid.org/0000-0002-6911-6947
                https://orcid.org/0000-0001-6114-3572
                Article
                molecules-26-01121
                10.3390/molecules26041121
                7924039
                c02a2a0a-4380-4c6c-bf1b-732799236b76
                © 2021 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
                : 21 January 2021
                : 18 February 2021
                Categories
                Article

                algerian lichen,physcia mediterranea nimis,bioactive compounds,n-hexane extract,wax,gc-ms,hplc-esi-ms-ms,nmr

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