Alternative and efficient extraction methods for marine-derived compounds

Marine ecosystems cover more than 70% of the globe's surface. These habitats are occupied by a great diversity of marine organisms that produce highly structural diverse metabolites as a defense mechanism. In the last decades, these metabolites have been extracted and isolated in order to test them in different bioassays and assess their potential to fight human diseases. Since traditional extraction techniques are both solvent- and time-consuming, this review emphasizes alternative extraction techniques, such as supercritical fluid extraction, pressurized solvent extraction, microwave-assisted extraction, ultrasound-assisted extraction, pulsed electric field-assisted extraction, enzyme-assisted extraction, and extraction with switchable solvents and ionic liquids, applied in the search for marine compounds. Only studies published in the 21st century are considered. © 2015 by the authors; licensee MDPI.The authors are grateful for the European Union (FEDER funds through COMPETE) and National Funds (FCT, Fundação para a Ciência e Tecnologia) through project Pest-C/EQB/LA0006/2013, to financial support from the European Union (FEDER funds) under the framework of QREN through Project NORTE-07-0124-FEDER-000069, to CYTED Programme (Ref. 112RT0460) CORNUCOPIA Thematic Network and project AGL2011-23690 (CICYT). Clara Grosso thanks FCT for the FCT Investigator (IF/01332/2014). We acknowledge support by the CSIC Open Access Publication Initiative through its Unit of Information Resources for Research (URICI).Peer Reviewe

Bioactive Marine Drugs and Marine Biomaterials for Brain Diseases

Marine invertebrates produce a plethora of bioactive compounds, which serve as inspiration for marine biotechnology, particularly in drug discovery programs and biomaterials development. This review aims to summarize the potential of drugs derived from marine invertebrates in the field of neuroscience. Therefore, some examples of neuroprotective drugs and neurotoxins will be discussed. Their role in neuroscience research and development of new therapies targeting the central nervous system will be addressed, with particular focus on neuroinflammation and neurodegeneration. In addition, the neuronal growth promoted by marine drugs, as well as the recent advances in neural tissue engineering, will be highlighted.The authors are grateful to the financial support from the European Union (FEDER funds through COMPETE) and National Funds (FCT, Fundação para a Ciência e Tecnologia) through project Pest-C/EQB/LA0006/2013 and from the European Union (FEDER funds) under the framework of QREN through Project NORTE-07–0124-FEDER-000069, to CYTED Programme (Ref. 112RT0460) CORNUCOPIA Thematic Network and project AGL2011–23690 (CICYT). Clara Grosso thanks FCT for the Post-Doc fellowship (SFRH/BPD/63922/2009). We acknowledge support by the CSIC Open Access Publication Initiative through its Unit of Information Resources for Research (URICI)Peer reviewe

Evaluation of the neuroprotective and antidiabetic potential of phenol-rich extracts from virgin olive oils by in vitro assays

In this work, phenol-rich extracts from ‘Cornicabra’ and ‘Picual’ virgin-olive oils (EVOOs) were examined, for the first time, to establish their capacity to inhibit key enzymes involved in Alzheimer's disease (AD) (acetylcholinesterase (AChE), butyrylcholinesterase (BuChE) and 5-lipoxygenase (LOX)), major depressive disorder (MDD) and Parkinson's disease (PD) (monoamine oxidases: hMAO-A and hMAO-B respectively), and diabetes mellitus (DM) (α-glucosidase and α-amylase). ‘Cornicabra’ displayed the best inhibitory activity against all enzymes, when compared to ‘Picual’: BuChE (IC50 = 156 ± 4 and 308 ± 33 mg mL−1), LOX (IC50 = 26 ± 0.5 and 37 ± 3 mg mL−1), hMAO-A (IC50 = 20 ± 2 and 37 ± 0.2 mg mL−1), hMAO-B (IC50 = 131 ± 7 and 215 ± 13 mg mL−1) and α-glucosidase (IC50 = 154 ± 17 and 251 ± 31 mg mL−1), respectively. The behaviour observed can be associated with the higher content of secoiridoids, lignans and phenolic acids in ‘Cornicabra’ EVOO.POCTEP | Ref. 0377_IBERPHENOL_6_EFundação para a Ciência e a Tecnologia | Ref. UID/QUI/50006/2013Norte Portugal Regional Operational Programme | Ref. NORTE-01-0145-FEDER-000024Xunta de Galici

New Insight on the Bioactivity of Solanum aethiopicum Linn. Growing in Basilicata Region (Italy): Phytochemical Characterization, Liposomal Incorporation, and Antioxidant Effects

Food extract’s biological effect and its improvement using nanotechnologies is one of the challenges of the last and the future decades; for this reason, the antioxidant effect of scarlet eggplant extract liposomal incorporation was investigated. Scarlet eggplant (Solanum aethiopicum L.) is a member of the Solanaceae family, and it is one of the most consumed vegetables in tropical Africa and south of Italy. This study investigated the antioxidant activity and the phytochemical composition of S. aethiopicum grown in the Basilicata Region for the first time. The whole fruit, peel, and pulp were subjected to ethanolic exhaustive maceration extraction, and all extracts were investigated. The HPLC-DAD analysis revealed the presence of ten phenolic compounds, including hydroxycinnamic acids, flavanones, flavanols, and four carotenoids (one xanthophyll and three carotenes). The peel extract was the most promising, active, and the richest in specialized metabolites; hence, it was tested on HepG2 cell lines and incorporated into liposomes. The nanoincorporation enhanced the peel extract’s antioxidant activity, resulting in a reduction of the concentration used. Furthermore, the extract improved the expression of endogenous antioxidants, such as ABCG2, CAT, and NQO1, presumably through the Nrf2 pathway

Jasonia glutinosa (L.) DC., a traditional herbal medicine, reduces inflammation, oxidative stress and protects the intestinal barrier in a murine model of colitis

Jasonia glutinosa (L.) DC., known as rock tea (RT), is traditionally used in Spain as a digestive due to its beneficial properties in bowel disorders. The pharmacological nature of these properties has not been established yet. The aim of this work was to evaluate the therapeutic utility of RT in experimental colitis and to identify chemical constituents with anti-inflammatory and/or anti-oxidative properties. RT extract was prepared with ethanol in a Soxhlet apparatus and analysed by HPLC–DAD. Superoxide radical scavenging properties, xanthine oxidase and lipoxygenase (5-LOX) inhibitory activity, and capability to lower nitric oxide (NO) and tumor necrosis factor a (TNF-a) levels were measured in cell-free and cell-based assays. In the 2.5%-dextran-sodium sulphate (DSS) injury-repair model of ulcerative colitis (UC), mice were daily treated with sulfasalazine (SSZ, as reference drug, 100 mg/kg bw), RT (5, 25 and 50 mg/kg bw, p.o.), or vehicle over 20 days. Colitis was scored daily. Colon samples were examined macroscopically and histopathologically. Protein levels of myeloperoxidase (MPO), interleukins 6, and 10 (IL-6, IL-10), inducible NO synthase (iNOS), and cyclooxygenase-2 (COX-2) were studied as markers of oxidative stress and inflammatory activity. The integrity of the apical epithelial layer was assessed by immunofluorescence staining of zonula ocludens-1 (ZO-1). Finally, intestinal contractility was also evaluated by isometric myography. Fifteen phenolic compounds and three pigments were identified and quantified, of which caffeoylquinic acids, and the flavonoid, quercetin-3-O-galactoside, were the most abundant. RT extract significantly scavenged superoxide radicals, inhibited 5-LOX activity, and lowered NO and TNF-a levels. DSS-treated mice receiving RT scored clinically lower than controls during the first 3 days of DSS treatment and during the recovery period. SSZ was less effective than RT. Anatomical and histological examination of colon samples revealed that RT significantly prevented colon shortening, increased colon thickness, and lowered the macroscopic damage score. RT also significantly prevented the increase of MPO activity, IL-6 levels, iNOS and COX-2 expression, the loss of ZO-1 apical expression, and normalized contractility disturbances. In conclusion, daily administration of RT showed therapeutic properties in the DSS-model of UC. The benefits of RT can likely be attributed to its anti-inflammatory and antioxidant phenolic and flavonoid constituents

Improving the knowledge on Piper betle: Targeted metabolite analysis and effect on acetylcholinesterase

9 páginas, 3 figuras, 4 tablas.-- et al.Piper betle is a species growing in South East Asia, where its leaves are economically and medicinally important. To screen the highest possible number of volatile and semivolatile components, the leaves were subjected to headspace solid-phase microextraction, hydrodistillation and Soxhlet extraction, prior to analysis by GC/MS. Fifty compounds (identified by comparison with standard compounds or tentatively by National Institute of Standards and Technology database) were determined, 23 being described for the first time in this matrix. An aqueous extract was also analysed, in which only seven compounds were characterized. The organic acids' composition of this extract was determined by HPLC/UV and eight compounds are reported for the first time in P. betle. This extract also displayed acetylcholinesterase inhibitory capacity.The authors acknowledge Fundaçäo para a Ciência e Tecnologia (FCT) for financial support (PTDC/AGR-AAM/ 64150/2006). C. Belo acknowledges Ministério da Educaçäo e Cultura da República Democrática de Timor-Leste and to Instituto Portugués de Apoio ao Desenvolvimento (IPAD).Peer reviewe

Alternative and Efficient Extraction Methods for Marine-Derived Compounds

Marine ecosystems cover more than 70% of the globe’s surface. These habitats are occupied by a great diversity of marine organisms that produce highly structural diverse metabolites as a defense mechanism. In the last decades, these metabolites have been extracted and isolated in order to test them in different bioassays and assess their potential to fight human diseases. Since traditional extraction techniques are both solvent- and time-consuming, this review emphasizes alternative extraction techniques, such as supercritical fluid extraction, pressurized solvent extraction, microwave-assisted extraction, ultrasound-assisted extraction, pulsed electric field-assisted extraction, enzyme-assisted extraction, and extraction with switchable solvents and ionic liquids, applied in the search for marine compounds. Only studies published in the 21st century are considered

Phlorotannin extracts from fucales characterized by HPLC-DAD-ESI-MSn: approaches to hyaluronidase inhibitory capacity and antioxidant properties

Purified phlorotannin extracts from four brown seaweeds (Cystoseira nodicaulis (Withering) M. Roberts, Cystoseira tamariscifolia (Hudson) Papenfuss, Cystoseira usneoides (Linnaeus) M. Roberts and Fucus spiralis Linnaeus), were characterized by HPLC-DAD-ESI-MSn. Fucophloroethol, fucodiphloroethol, fucotriphloroethol, 7-phloroeckol, phlorofucofuroeckol and bieckol/dieckol were identified. The antioxidant activity and the hyaluronidase (HAase) inhibitory capacity exhibited by the extracts were also assessed. A correlation between the extracts activity and their chemical composition was established. F. spiralis, the species presenting higher molecular weight phlorotannins, generally displayed the strongest lipid peroxidation inhibitory activity (IC50 = 2.32 mg/mL dry weight) and the strongest HAase inhibitory capacity (IC50 = 0.73 mg/mL dry weight). As for superoxide radical scavenging, C. nodicaulis was the most efficient species (IC50 = 0.93 mg/mL dry weight), followed by F. spiralis (IC50 = 1.30 mg/mL dry weight). These results show that purified phlorotannin extracts have potent capabilities for preventing and slowing down the skin aging process, which is mainly associated with free radical damage and with the reduction of hyaluronic acid concentration, characteristic of the process.The authors are grateful to Fundação para a Ciência e a Tecnologia (FCT) through grant no. PEst-C/EQB/LA0006/2011, to “Consolider Ingenio 2010 Project CSD2007-00063 FUN-C-FOOD” and to “Grupo de excelencia de la región de Murcia 04486/GERM/06”. G. Lopes (SFRH/BD/61565/2009) is indebted to FCT, FSE and POPH for the grant.Peer reviewe

Improved loquat (Eriobotrya japonica Lindl.) cultivars: Variation of phenolics and antioxidative potential

9 páginas, 5 figuras, 3 tablas.-- El PDF es la versión manuscrita de autor.-- et al.Leaves and fruits (peel and flesh) of six improved cultivars (‘Mizuho’, ‘Néctar de Cristal’, ‘Mizauto’, ‘Mizumo’, ‘Centenária’ and ‘NE-3’) of loquat (Eriobotrya japonica Lindl.) were studied for their phenolic composition and antioxidant capacity. The analysis by HPLC-DAD-ESI-MS/MS allowed the identification of 18 compounds (8 hydroxycinnamic acid derivatives and 10 flavonoid glycosides). The quantification of the identified compounds revealed distinct profiles amongst the three analysed materials. Loquat leaves exhibited the lowest amounts of phenolics. 3- And 5-caffeoylquinic, and 5-feruloylquinic acids were the major compounds. Generally, ‘Mizauto’ cultivar presented the highest phenolic content. All loquat materials exhibited DDPH scavenging capacity, in a concentration-dependent manner, the leaves being the most active one. This effect seems to be related to the flavonoid content.D. Gomes is grateful to Fundação para a Ciência e Tecnologia (PTDC/AGR-AAM/64150/2006) for financial support.Peer reviewe

Metabolomic Analysis of Natural Products

20 páginas, 9 figuras, 1 tabla.The metabolome comprises all metabolites in a biological organism, which constitute the end products of its gene expression. Metabolomics consists on the systematic study of the chemical fingerprints resulting from specific cellular processes or, more particularly, the study of an organism’s profile of low molecular weight metabolites. Thus, metabolomics is perhaps the ultimate level of post-genomic analysis as it can reveal changes in metabolite fluxes that are controlled by only minor changes within gene expression. Classical phytochemical approaches often comprised a rather tedious and time consuming process of isolation, dereplication of known substances, followed by structure elucidation and quantification. However, it is important to highlight that, in many situations, the effects of natural products are not due to a single compound, but to a mixture of related and unrelated ones. Thus, metabolomics provides an efficient tool for the quality control and authentication of medicines of natural origin, contributing as well to the characterization of different species. Several combined techniques have been applied in the measurements of intracellular metabolites, whether qualitative or quantitative, which reveal the biochemical status of the organism. This review offers an insight on the methods used in the metabolomics analysis (LC-MS, GC-MS, HPLC-DAD, NMR) of several natural matrices with protective health potential, with special emphasis on the determination of phenolics profiles, once these represent the most abundant and widely spread class of plant natural compounds, additionally exhibiting interesting biological activities.Peer reviewe