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      Antiprotozoal and Antibacterial Activity of Ravenelin, a Xanthone Isolated from the Endophytic Fungus Exserohilum rostratum

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          Abstract

          The natural compound ravenelin was isolated from the biomass extracts of Exserohilum rostratum fungus, and its antimicrobial, antiplasmodial, and trypanocidal activities were evaluated. Ravenelin was isolated by column chromatography and HPLC and identified by NMR and MS. The susceptibility of Gram-positive and Gram-negative bacteria strains to ravenelin was determined by microbroth dilution assay. Cytotoxicity was evaluated in hepatocarcinoma cells (HepG2) and BALB/c peritoneal macrophages by using MTT. SYBR Green I-based assay was used in the asexual stages of Plasmodium falciparum. Trypanocidal activity was tested against the epimastigote and intracellular amastigote forms of Trypanosoma cruzi. Ravenelin was active against Gram-positive bacteria strains, with emphasis on Bacillus subtilis (MIC value of 7.5 µM). Ravenelin’s antiparasitic activities were assessed against both the epimastigote (IC 50 value of 5 ± 1 µM) and the intracellular amastigote forms of T. cruzi (IC 50 value of 9 ± 2 µM), as well as against P. falciparum (IC 50 value of 3.4 ± 0.4 µM). Ravenelin showed low cytotoxic effects on both HepG2 (CC 50 > 50 µM) and peritoneal macrophage (CC 50 = 185 ± 1 µM) cells with attractive selectivity for the parasites (SI values > 15). These findings indicate that ravenelin is a natural compound with both antibacterial and antiparasitic activities, and considerable selectivity indexes. Therefore, ravenelin is an attractive candidate for hit-to-lead development.

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          Rapid colorimetric assay for cellular growth and survival: Application to proliferation and cytotoxicity assays

          A tetrazolium salt has been used to develop a quantitative colorimetric assay for mammalian cell survival and proliferation. The assay detects living, but not dead cells and the signal generated is dependent on the degree of activation of the cells. This method can therefore be used to measure cytotoxicity, proliferation or activation. The results can be read on a multiwell scanning spectrophotometer (ELISA reader) and show a high degree of precision. No washing steps are used in the assay. The main advantages of the colorimetric assay are its rapidity and precision, and the lack of any radioisotope. We have used the assay to measure proliferative lymphokines, mitogen stimulations and complement-mediated lysis.
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            Natural Products as Sources of New Drugs from 1981 to 2014.

            This contribution is a completely updated and expanded version of the four prior analogous reviews that were published in this journal in 1997, 2003, 2007, and 2012. In the case of all approved therapeutic agents, the time frame has been extended to cover the 34 years from January 1, 1981, to December 31, 2014, for all diseases worldwide, and from 1950 (earliest so far identified) to December 2014 for all approved antitumor drugs worldwide. As mentioned in the 2012 review, we have continued to utilize our secondary subdivision of a "natural product mimic", or "NM", to join the original primary divisions and the designation "natural product botanical", or "NB", to cover those botanical "defined mixtures" now recognized as drug entities by the U.S. FDA (and similar organizations). From the data presented in this review, the utilization of natural products and/or their novel structures, in order to discover and develop the final drug entity, is still alive and well. For example, in the area of cancer, over the time frame from around the 1940s to the end of 2014, of the 175 small molecules approved, 131, or 75%, are other than "S" (synthetic), with 85, or 49%, actually being either natural products or directly derived therefrom. In other areas, the influence of natural product structures is quite marked, with, as expected from prior information, the anti-infective area being dependent on natural products and their structures. We wish to draw the attention of readers to the rapidly evolving recognition that a significant number of natural product drugs/leads are actually produced by microbes and/or microbial interactions with the "host from whence it was isolated", and therefore it is considered that this area of natural product research should be expanded significantly.
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              Human malaria parasites in continuous culture.

              Plasmodium falciparum can now be maintained in continuous culture in human erythrocytes incubated at 38 degrees C in RPMI 1640 medium with human serum under an atmosphere with 7 percent carbon dioxide and low oxygen (1 or 5 percent). The original parasite material, derived from an infected Aotus trivirgatus monkey, was diluted more than 100 million times by the addition of human erythrocytes at 3- or 4-day intervals. The parasites continued to reproduce in their normal asexual cycle of approximately 48 hours but were no longer highly synchronous. The have remained infective to Aotus.
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                Author and article information

                Contributors
                Role: Academic Editor
                Journal
                Molecules
                Molecules
                molecules
                Molecules
                MDPI
                1420-3049
                02 June 2021
                June 2021
                : 26
                : 11
                : 3339
                Affiliations
                [1 ]Post-Graduate Program in Chemistry, Federal University of Pará, 66075-110 Belém, Brazil; konanquim@ 123456gmail.com (J.R.S.P.); mcwander@ 123456hotmail.com (J.M.C.); heriberto.ufpa@ 123456gmail.com (H.R.B.); lucianowat@ 123456yahoo.com.br (L.A.W.); pat@ 123456ufpa.br (P.S.B.M.)
                [2 ]Laboratory of Immunomodulation and Protozoology, Oswaldo Cruz Institute, Oswaldo Cruz Foundation, 21040-360 Rio de Janeiro, Brazil; jvssilva89@ 123456gmail.com (J.V.S.-S.); juanfernandes222@ 123456gmail.com (J.M.P.F.); fernandoalsouza@ 123456gmail.com (F.A.-S.); kscalabrese@ 123456gmail.com (K.d.S.C.)
                [3 ]São Carlos Institute of Physics, University of São Paulo, São Carlos, 13566-590 São Paulo, Brazil; guilherme.eduardo.souza@ 123456usp.br (G.E.d.S.); carolcaguiar@ 123456yahoo.com.br (A.C.C.A.); rvcguido@ 123456ifsc.usp.br (R.V.C.G.)
                [4 ]Post-Graduate Program Animal Sciences, State University of Maranhão, 65055-310 São Luís, Brazil
                Author notes
                [* ]Correspondence: andrey@ 123456ufpa.br ; Tel.: +55-91-3201-8050
                [†]

                These authors contributed equally to this work.

                Author information
                https://orcid.org/0000-0002-9576-8981
                https://orcid.org/0000-0001-6080-7170
                https://orcid.org/0000-0003-3278-6688
                https://orcid.org/0000-0002-7187-0818
                https://orcid.org/0000-0003-0047-6159
                https://orcid.org/0000-0002-1884-3765
                https://orcid.org/0000-0002-9368-8574
                Article
                molecules-26-03339
                10.3390/molecules26113339
                8199546
                34199336
                8bd093a3-fd72-4636-9851-d2a46b1da635
                © 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 ( https://creativecommons.org/licenses/by/4.0/).

                History
                : 08 April 2021
                : 11 May 2021
                Categories
                Article

                antimicrobial,antiprotozoan,polyketides,fungi,xanthone
                antimicrobial, antiprotozoan, polyketides, fungi, xanthone

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