Advances on Applications of Bioactive Natural Compounds

This is a reprint of articles from the Special Issue published online in the open access journal Applied Sciences (ISSN 2076-3417) (available at: https://www.mdpi.com/journal/applsci/special issues/Bioactive Natural Compounds).info:eu-repo/semantics/publishedVersio

Secondary Metabolites in Edible Species : Looking beyond Nutritional Value

Secondary metabolites are organic molecules of low molecular weight, biosynthesized by any living being using a wide range of biosynthetic pathways, known as secondary metabolism. In evolutionary terms, secondary metabolism is seen as a set of specialized pathways that use a varied and specialized series of enzymes. Secondary metabolism aims to produce molecules with specific functions that promote the adaptability and survival of the species. However, secondary metabolites are not molecules essential to life, as are the lipids, carbohydrates and amino acids involved in basic life functions and produced by the primary metabolism. Terrestrial plants and algae, because they are sessile species, synthesize an admirable structural diversity of secondary metabolites. […]. (excerpt)This work was funded by FCT-Fundação para a Ciência e a Tecnologia, the European Union, QREN, FEDER, COMPETE, by funding the cE3c centre (UIDB/00329/2020) and the LAQV-REQUIMTE (UIDB/50006/2020) research units, and funded by the project EthnoHERBS (H2020-MSCA-RISE-2018, No. 823973).info:eu-repo/semantics/publishedVersio

Secondary Metabolites and Their Applications

The identification of secondary metabolites present in both terrestrial and marine species continues to be a fundamental and privileged path for the emergence of new and fundamental natural products available on the market with very different applications. For example, aplidine is a new natural anticancer agent, and it was approved in Australia in 2018 to treat multiple myeloma and was isolated from the first time from tunicate “Aplidium albicans” Milne Edwards. (+)-Nootkatone is a natural sesquiterpene compound, found in very small amounts in several species such as “Chamaecyparis nootkatensis” (D. Don) Sudworth, ”Chrysopogon zizanioides” (L.) Roberty and “Citrus paradise” Macfad., which exhibits highly appreciated organoleptic properties and is, therefore, highly demanded as a flavoring agent or adjuvant in the food, pharmaceutical and perfumery industries. This same natural secondary metabolite is applied as insecticide and acaricide, and it was very recently authorized by United Sates Environmental Protection Agency to be include on formulations to control the spread of mosquitoes that transmit infectious diseases as dengue and zika. And who does not know the application of ascorbic acid, found for example in acerola and lemon fruits, as an antioxidant agent, widely used by the food industry? The successful application of secondary metabolites in diverse requests often involves the use of, more or less, complex mixtures of metabolites, extracted by different methods and from different natural sources, but whose chemical composition and active principles are perfectly established. For example, there are the defined botanical mixtures, called natural product botanicals, which are recognized by the FDA as medicinal entities, successfully used in clinical therapy for the treatment of various diseases. This is the case of the mixture of the secondary metabolites of ”Solanum sodomaeum” L., solamargine, solasonine, and mono- and di-glycosides derivatives of solasodine, approved by the European Medicine Agency (trade name Curaderm) for the treatment of basal cell carcinoma of the skin. One area in which the application of secondary metabolites mixtures rather than of pure compounds is common is in the formulation of biopesticides. For example, the insecticide Grandevo® is a mixture of metabolites produced in the fermentation of “Chromobacterium subtsugae”, which includes pigments from the violacein family and proteins that are repellent and antifeeding. Despite the great successes already achieved regarding the secondary metabolites’ identification and the development of new applications for these metabolites, this is an area of research that should not slow down. Research must continue identifying and isolating secondary metabolites in unexplored natural sources; new methodologies for extracting secondary metabolites should be tested and optimized to develop greener and more efficient processes; pure secondary metabolites and chemically characterized mixtures must be tested in different biological activities in order to enhance new applications responding to the growing needs of humanity. The Special Issue of Applied Sciences, “Advances in Applications of Natural Bioactive Compounds”, aims to contribute to the desired continuous advance in this scientific field, bringing together publications focused on the most recent advances in the identification of secondary metabolites from terrestrial and marine sources, in new extractive methodologies, and in proposals for applications that add value to natural resources and contributes to a more sustainable development.his study was financed by Portuguese National Funds, through FCT Fundação para a Ciência e Tecnologia, the European Union, QREN, FEDER, and COMPETE, through funding the cE3c center (UIDB/00329/2020), the LAQV-REQUIMTE (UIDB/50006/2020) and the CICS-UBI (UIDB/00709/2020 and UIDP/00709/2020).info:eu-repo/semantics/publishedVersio

Natural Compounds : A Dynamic Field of Applications

Nature represents an amazing source of inspiration since it produces a great diversity of natural compounds selected by evolution, which exhibit multiple biological activities and applications. A large and very active research field is dedicated to identifying biosynthesized compounds, to improve/develop new methodologies to produce/reuse natural compounds and to assess their potential for pharmaceutical, cosmetic and food industries, among others, and also to understand their mechanism of action. Here, the main results presented in each work are highlighted. The applications suggested are mostly related to pharmacological uses and involve mainly pure natural compounds and essential oils. These works are significant contributions and reinforce the dynamic field of natural products applications.This research was funded by FCT–Fundação para a Ciência e a Tecnologia, the European Union, QREN, FEDER, COMPETE, by funding the cE3c centre (UIDB/00329/2020) and the LAQV-REQUIMTE (UIDB/50006/2020) research units, and by the Spanish Ministry Science and Research (MINECO RTI2018-094356-B-C21).info:eu-repo/semantics/publishedVersio

Biological activity and applications of natural compounds

(This book is a printed edition of the Special Issue Biological Activity and Applications of Natural Compounds that was published in Applied Sciences).Nature represents an amazing source of inspiration since it produces a great diversity of natural compounds selected by evolution, which exhibit multiple biological activities and applications. A large and very active research field is dedicated to identifying biosynthesized compounds, to improve/develop new methodologies to produce/reuse natural compounds and to assess their potential for pharmaceutical, cosmetic and food industries, among others, and also to understand their mechanism of action.info:eu-repo/semantics/publishedVersio

O maravilhoso mundo dos metais

A secção UAciência é coordenada pelo Professor Universitário Armindo Rodrigues.A grande maioria dos elementos químicos existentes na natureza correspondem a categoria dos metais. São elementos muito heterogéneos, mas com propriedades comuns: tonalidade prateada (a maioria), brilhantes (brilho metálico), suaves ao toque, mais densos que a água e bons condutores de eletricidade. A maioria são sólidos a temperatura ambiente, mas o metal mercúrio e líquido e tão denso que o chumbo flutua sobre a sua superfície. São de uma versatilidade estonteante. Por exemplo o cobre, exibe aplicações de grande valor económico quer na sua forma pura (como um dos melhores condutores de eletricidade) quer combinado com estanho dando origem ao bronze a partir do qual se fazem grandes obras de arte que perduram no tempo. Alguns metais puros resistem estoicamente à ação do tempo sem sofrerem qualquer reação de degradação como o ouro e a platina cujo brilho permanece indefinidamente, enquanto outros, como o ferro, reagem espontaneamente com o oxigénio do ar, na presença de água, mesmo vestigial, originando a ferrugem, uma reação praticamente impossível de parar e que acarreta perdas económicas imensas, como por exemplo, o desgaste de estruturas de portos, carros, barcos, pontes, etc. […].info:eu-repo/semantics/publishedVersio

Protein-ligand docking study: diterpenes from Juniperus brevifolia as anticancer and antimicrobial agentes

REDCAT: Natural Products and related Redox Catalysts: Basic Research and Applications in Medicine and Agriculture, Aveiro, 25-27 Novembro de 2012.From leaves of Juniperus brevifolia, an endemic conifer from Azores, were isolated and structurally characterized, several dehydroabietane and sandaracopimarane derivatives. Some of them (1-4), displayed antiproliferative activity against cancer cell lines (HeLa, A-549 and MCF-7) and bactericidal effect against Bacillus cereus at different concentrations tested. However, it is not known how these compounds interact with most often proteins involved in the antimicrobial and cytotoxic mechanisms. Protein-ligand docking is mainly used to predict (energy and conformation wise) how small molecules bind to a protein of known 3D structure and to predict possible molecular targets for a set of compounds. In this work, the docking studies were performed, using the FlexScreen program, in order to pick molecular targets from a large set of common anticancer (63) and antimicrobial (39) targets to the selected compounds 1-4. The predicted interactions established between the compounds under study and the anticancer targets revealed that the compounds 1 and 3 interact preferentially with phosphatidylinositol-3,4,5-trisphosphate 5-phosphatase 2, whereas compounds 2 and 4 interact preferentially with human mitochondrial peptide deformylase and -tubulin, respectively. Studying the interactions between the compounds 1 and 3 and the antimicrobial targets we predict that these compounds interact preferentially with RNA polymerase and peptide deformylase. These results provide additional understanding of the cytotoxic and antimicrobial effects of diterpenes studied. These preliminary computational docking predictions of therapeutic targets were established working with just 4 compounds, and to obtain more reliable predictions the number of compounds needs to be increased.Thanks are due to the University of Azores, FCT, FEDER, BIOPHARMAC - MAC/1/C104 and Project PEst-OE/QUI/UI0674/2011

Tabela Periódica: a composição química do universo num quadro com 18 colunas e 7 linhas

A secção CÊ de ciência é coordenada pela Professora Universitária Ana Teresa Alves.De que é feito tudo o que existe no universo? Pode parecer mentira, mas a resposta a esta questão é curta: No universo existem apenas 91 elementos químicos diferentes (substâncias puras que não podem ser separadas em substâncias mais simples). Tudo o que existe no universo é composto por um ou mais elementos de entre estes 91. Queres saber quais são? Então olha para uma tabela periódica!info:eu-repo/semantics/publishedVersio

Isómeros : compostos iguais com diferenças

A secção UAciência é coordenada pelo Professor Universitário Armindo Rodrigues.Em 1831, o prestigiado químico Jacob Berzelius introduziu o conceito de isómeros: Compostos que possuem os mesmos átomos nas mesmas proporções, mas em que esses átomos se ligam uns aos outros de diferentes formas (diferentes arranjos entre eles). O exemplo discutido à época foi o ácido fulmínico (H-C=N-O) (sais deste ácido são usados como detonadores primários) e o ácido ciânico (H-O-C N) (líquido incolor e venenoso). O conceito de isomeria permanece como essencial em química tendo ao longo dos anos sido aprofundado e alargado, sendo possível encontrar na natureza e no laboratório um largo conjunto de exemplos de compostos isómeros com propriedades e aplicações práticas muito distintas. […].info:eu-repo/semantics/publishedVersio

Uncharted Source of Medicinal Products : The Case of the Hedychium Genus

A current research topic of great interest is the study of the therapeutic properties of plants and of their bioactive secondary metabolites. Plants have been used to treat all types of health problems from allergies to cancer, in addition to their use in the perfumery industry and as food. Hedychium species are among those plants used in folk medicine in several countries and several works have been reported to verify if and how effectively these plants exert the effects reported in folk medicine, studying their essential oils, extracts and pure secondary metabolites. Hedychium coronarium and Hedychium spicatum are the most studied species. Interesting compounds have been identified like coronarin D, which possesses antibacterial, antifungal and antitumor activities, as well as isocoronarin D, linalool and villosin that exhibit better cytotoxicity towards tumor cell lines than the reference compounds used, with villosin not affecting the non-tumor cell line. Linalool and α-pinene are the most active compounds found in Hedychium essential oils, while β-pinene is identified as the most widespread compound, being reported in 12 different Hedychium species. Since only some Hedychium species have been investigated, this review hopes to shed some light on the uncharted territory that is the Hedychium genus.This research was funded by project MACBIOPEST (MAC2/1.1a/289), program Interreg MAC 2014–2020 co-financed by DRCT (Azores Regional Government), supporting W.R. Tavares’s grant, as well as by FCT—Fundação para a Ciência e Tecnologia, the European Union, QREN, FEDER, and COMPETE, through funding the cE3c center (UIDB/00329/2020) and the LAQV-REQUIMTE (UIDB/50006/2020).info:eu-repo/semantics/publishedVersio