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

Laurus azorica : Valorization through Its Phytochemical Study and Biological Activities

Laurus azorica (Seub.) Franco is an endemic species from the Azores, traditionally used in all the islands as a seasoning in cooking. The studies carried out with this species refer mainly to its essential oils. The study that was developed here allowed, for the first time, to determine the chemical composition and biological activities of the ethanol extract, fractions, and pure compounds from L. azorica. The hexane fraction was analyzed by GC–MS and revealed the presence of 48 compounds, comprising mainly fatty acids, fatty alcohols and terpenes, the family of fatty alcohols identified here for the first time in the genus Laurus. Three sesquiterpene lactones—costunolide, 11,13-dehydrosantonin and reynosin—were isolated for the first time in L. azorica from the same fraction, and structurally characterized using spectroscopic techniques. The compounds identified belong to families known to have relevant medicinal and nutritional properties. Regarding antioxidant activities, the results obtained showed a moderate radical scavenging effect of extracts and fractions, while in the β-carotene bleaching assay, costunolide was shown to be the most active (IC₅₀ = 4.08 ± 0.76 μg/mL), about 3.6 times more active than the standard, gallic acid, which presented IC₅₀ = 14.56 ± 0.13 μg/mL. Although the inhibition of extracellular matrix-degrading enzymes was not detected, the ethanol extract showed good inhibitory activity of tyrosinase, with an IC₅₀ of 12.04 ± 0.23 μg/mL, only 6.6-fold lower than the control kojic acid. The results presented deepen the knowledge about a little studied species, opening new perspectives for the development of value-added applications in the food and cosmeceutical fields.This research was funded by project MACBIOPEST (MAC2/1.1a/289), Interreg MAC 2014-2020, co-financed by DRCT (Azores Regional Government), as well as by FCT-Fundacao para a Ciencia e Tecnologia, the European Union, QREN, FEDER and COMPETE, through funding the cE3c center-CHANGE (UIDB/00329/2020) and the LAQV-REQUIMTE (UIDB/50006/2020).info:eu-repo/semantics/publishedVersio

Anti-aging activity of Lobophora variegata ethanolic and methanolic extracts and their fractions

Conference Report XVI International Symposium on Marine Natural Products | XI European Conference on Marine Natural Products, 1-5 September 2019, Peniche, Portugal.Seaweed have promising applications within food, cosmetic and health industries, which led to an increased interest in studying these organisms [1]. In several coastal areas, thousands of tons of macroalgae are cast on beaches and shorelines and it would be very interesting if this biomass could be managed, allowing the extraction of added-value compounds. In this context, polar extracts (methanol and ethanol) of a macroalgal beach cast sample mainly composed of “Lobophora variegate” were prepared and the anti-aging and antioxidant activities were evaluated. The preliminary results showed interesting results, and thus these crude extracts were then fractionated sequentially by their solubility in dichloromethane, acetone and ethyl acetate, resulting in 4 semi-pure fractions each, which were also tested. Fractions A1.1.1 and A1.2.3 were very good tyrosinase inhibitors (IC₅₀ = 37.87 and 24.01 μg/mL, respectively) and fractions A1.1.2 and A1.2.2 presented very good inhibition of elastase (IC₅₀ = 44.76 and 20.86 μg/mL, respectively). However, none of the fractions was active against collagenase. These results show that further purifications of these fractions can lead to the isolation of bioactive added-value compounds.info:eu-repo/semantics/publishedVersio

Asparagopsis Genus : What We Really Know About Its Biological Activities and Chemical Composition

Although the genus Asparagopsis includes only two taxonomically accepted species, the published literature is unanimous about the invasive nature of this genus in different regions of the globe, and about the availability of large amounts of biomass for which it is important to find a commercial application. This review shows that extracts from Asparagospsis species have already been evaluated for antioxidant, antibacterial, antifungal, antiviral, antifouling, cytotoxic, antimethanogenic and enzyme-inhibitory activity. However, the tables presented herein show, with few exceptions, that the activity level displayed is generally low when compared with positive controls. Studies involving pure compounds being identified in Asparagopsis species are rare. The chemical compositions of most of the evaluated extracts are unknown. At best, the families of the compounds present are suggested. This review also shows that the volatile halogenated compounds, fatty acids and sterols that are biosynthesized by the Asparagopsis species are relatively well known. Many other non-volatile metabolites (halogen compounds, flavonoids, other phenolic compounds) seem to be produced by these species, but their chemical structures and properties haven’been investigated. This shows how much remains to be investigated regarding the secondary-metabolite composition of these species, suggesting further studies following more targeted methodologies.This study was financed by ASPAZOR project (DRCT: ACORES-01-0145-FEDER-00060-ASPAZOR); Portuguese National Funds, through FCT-Fundacao para a Ciencia e a Tecnologia, and as applicable co-financed by the FEDER within the PT2020 Partnership Agreement by funding the LAQVREQUIMTE (UIDB/50006/2020) and the cE3c centre (FCT Unit funding (UID/BIA/00329/2019).info:eu-repo/semantics/publishedVersio

Cytotoxic, antibacterial, antioxidant, and anticholinesterasic activity of Juniperus brevifolia extracts

XXIII Encontro Nacional da Sociedade Portuguesa de Química. Aveiro, 12-14 de Junho 2013.The cytotoxic, antibacterial, antioxidant and anticholinesterasic (anti-AChE) activities of the methanol and acetone extracts of Juniperus brevifolia wood and bark were determined. The present study demonstrates that bark extracts of J. brevifolia are the most active and showed good antioxidant activity, lower anti-AChE activity except for the acetone extract, poor cytotoxic and antibacterial activities and absence of activity for Gram (-) bacteria.Azores University, FCT for funding CIBIO Research Unit and to DRCTC for funding CIRN

Macroalgae from S. Miguel Island as a potential source of antiproliferative and antioxidant products

Ulva compressa, Gelidium microdon, Osmundea pinnatifida, Fucus spiralis and Cystoseira abies-marina from the coast of S. Miguel Island were screened for their in vitro cytotoxicity against HeLa tumour cell line, antioxidant potential and total phenolic content. From each alga, the hexane fraction (HF) of the methanol extract, the methanol residue (MF) and the dichloromethane extract (DE), were obtained and evaluated. The highest antiproliferative activity against HeLa cell line was found in C. abies-marina and F. spiralis DE (IC50 8.8 μg/mL and 10.7 μg/mL, respectively), and presented selective cytotoxicity, when tested against Vero cell line. Fluorescence microscopy studies of the two most active extracts suggest an apoptosis-inducing activity. Concerning the antioxidant activity, high values were found on F. spiralis MF and HF (EC50 0.62 μg/mL and 2.01 μg/mL, respectively), even higher than those obtained for trolox and quercetin. This high antioxidant activity in F. spiralis MF can be explained by its content in phenolic compounds, but not for HF, where the antioxidant compounds must be less polar. These results suggest that some macroalgae from the Azorean sea have great potential which could be considered for future applications in medicine, food production or cosmetics industry

Diversity of plant growth-promoting bacteria associated with sugarcane

The sugarcane (Saccharum spp) presents economic importance, mainly for tropical regions, being an important Brazilian commodity. However, this crop is strongly dependent on fertilizers, mainly nitrogen (N). This study assessed the plant growth-promoting bacteria (PGPB) associated with sugarcane that could be used as a potential inoculant to the crop. We evaluated the genetic diversity of PGPB in the plant tissue of sugarcane varieties (RB 867515, RB 1011, and RB 92579). The primer BOX-A1R was used to differentiate the similar isolated and further sequencing 16S rRNA ribosomal gene. The 16S rRNA gene showed the presence of seven different genera distributed into four groups, the genus Bacillus, followed by Paenibacillus (20%), Burkholderia (14%), Herbaspirillum (6%), Pseudomonas (6%), Methylobacterium (6%), and Brevibacillus (3%). The molecular characterization of endophytic isolates from sugarcane revealed a diversity of bacteria colonizing this plant, with a possible biotechnological potential to be used as inoculant and biofertilizers

A Green and Simple Protocol for Extraction and Application of a Peroxidase-Rich Enzymatic Extract

Recently there is a great social expectation that scientists should produce more sustainable and environmentally friendly chemical processes. Within this necessity, biocatalysis presents many attractive features because reactions are often performed in water, under mild conditions, the catalyst is biodegradable and can be obtained from renewable raw materials. In this work, we propose a simple, rapid and low-cost method for the preparation and application of an enzymatic extract from turnip root. The protocol described includes (1) the preparation of the enzymatic extract, (2) the procedure for the assessment of the more favorable working parameters (temperature, pH) and (3) the methodology for the application of the extract as the catalyst for biotransformation reactions. We anticipate that the protocol in this research will provide a simple way for obtaining an enzymatic extract which can operate efficiently under mild conditions and can effectively catalyze the biotransformation of simple phenols.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), the LAQV-REQUIMTE (UIDB/50006/2020) and QOPNA (FCT UID/QUI/00062/2019) research units.info:eu-repo/semantics/publishedVersio

Chemical and biological studies from an Azorean macroalga: Ulva rigida

3rd Portuguese Meeting on Medicinal Chemistry and 1st Portuguese-Spanish-Brazilian Meeting on Medicinal Chemistry, Aveiro, 28-30 Novembro 2012.New drugs from natural sources have been targets of the drug discovery program and some bioactive compounds from macroalgae such as sulfated polysaccharides, steroids and diterpens have found their applications in the pharmaceutical industry.[1,2] Consequently, we have investigated the chemical composition and the in vitro antitumor potential of the metabolites isolated from the macroalga Ulva rigida, collected from the Azorean coast, an environmentally healthy habitat with a high level of biodiversity. We hereby describe isolation of isofucosterol (1) and 7(E)-3ẞ-hidroxy-5α, 6α-epoxymegastigmane (2) from the methanol extract of Ulva rigida, collected in May of 2011 in the Sea of St Miguel Island - Azores archipelago. The process of isolation of these metabolites involved chlorophylls elimination by the method previously described[3] and fractionation by column chromatography. The structures of 1 and 2 were established by 1D and 2D NMR spectral analysis and specific rotation as well as comparison of their spectral data with those described in the literature.[4,5] Compounds 1 and 2 were evaluated for their capacity to inhibit the in vitro growth of three human cancer cell lines: MCF-7 (breast adenocarcinoma), NCI-H460 (non-small cell lung cancer) and A375-C5 (human skin cell line), using the protein binding dye SRB method. The results showed that compound 1 exhibited only a weak activity against MCF-7 (GI50 = 122.2 ± 17.9 μM), NCI-H460 (GI50 = 128.4 ± 32.4 μM), A375-C5 (GI50 = 119.2 ± 28.9 μM), while compound 2 was inactive against all the three cell lines (GI50 >200 μM).This work was financially supported by the project, Bioactive products in marine algae of Azores (PTDC/MAR/100482/2008) from Fundação para a Ciência e a Tecnologia (FCT). Madalena Silva thanks FCT for the young researcher scholarship under PTDC/MAR/100482/2008 project