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Showing papers in "Anais Da Academia Brasileira De Ciencias in 2018"


Journal ArticleDOI
TL;DR: The analysis of this event using drought indicators as well as meteorological fields shows that since the middle 1990s to 2016, 16 out of 25 years experienced rainfall below normal, which suggests that the recent drought may have in fact started in the middle-late 1990s.
Abstract: This study discusses the climatological aspects of the most severe drought ever recorded in the semiarid region Northeast Brazil. Droughts are recurrent in the region and while El Nino has driven some of these events others are more dependent on the tropical North Atlantic sea surface temperature fields. The drought affecting this region during the last 5 years shows an intensity and impact not seen in several decades in the regional economy and society. The analysis of this event using drought indicators as well as meteorological fields shows that since the middle 1990s to 2016, 16 out of 25 years experienced rainfall below normal. This suggests that the recent drought may have in fact started in the middle-late 1990s, with the intense droughts of 1993 and 1998, and then the sequence of dry years (interrupted by relatively wet years in 2007, 2008, 2009 and 2011) after that may have affected the levels of reservoirs in the region, leading to a real water crisis that was magnified by the negative rainfall anomalies since 2010.

282 citations


Journal ArticleDOI
TL;DR: Studies of fish FR production are preliminary and should be executed to evaluate the effects of ROS on fish, including their beneficial action against pathogens and its deleterious action on the oxidation of cellular components.
Abstract: Molecular oxygen is a necessary compound for all aerobic organisms, although oxygen is a potent oxidant, which can cause oxidative stress (OS). OS occurs when there is an imbalance between the production of oxidant and antioxidants components, are result of normal cell metabolism, and many of these compounds play a fundamental role in several metabolic pathways. The organism produces several reactive oxygen species (ROS), but they are balanced by an antioxidant defense system that maintains the levels of these oxidizing compounds at an acceptable level. Many of these components are essential in the organism defense and their byproducts are considered potent bactericides that actively act in the destruction of invading pathogens. Fish immune system is composed of innate and acquired mechanisms of defense. Phagocytosis is an innate process of defense, which interconnects these two systems, since the pathogens processing by professional phagocytes is a fundamental stage for antibodies production. During phagocytosis there is production of ROS and consequent production of free radicals (FR), these compounds lead to the formation of potent bactericides to combat microorganisms. However, it is known that OS limits the immune response, with an impairment in defense compounds in an attempt to decrease the ROS production. Studies of fish FR production are preliminary and should be executed to evaluate the effects of ROS on fish, including their beneficial action against pathogens and its deleterious action on the oxidation of cellular components.

145 citations


Journal ArticleDOI
TL;DR: This review has an approach to interdisciplinary studies against cancer carried out by many scientists using porphyrin-type substrates as photosensitizers in PDT and other related macrocycles of the phthalocyanine and corrole types have entered in the same "pipeline".
Abstract: This review has two parts. The first one gives an approach to interdisciplinary studies against cancer carried out by many scientists using porphyrin-type substrates as photosensitizers in PDT. Intensive studies were performed for almost six decades. The successes really started in 1993 with the first formulation patented under the trade name Photofrin, which was immediately approved in several countries to treat certain types of cancer. Photofrin is still used although certain negative features soon became well known. That has motivated the search for better new photosensitizers. Several ones were developed, evaluated and a few of them had clinical approval. This group includes porphyrin derivatives and pro-drugs (aminolevulinic acid and its alkyl esters). Oncological, dermatological and ophthalmic applications are now taking place for the benefit of mankind. The second part of this review is related with the work carried out in Aveiro at the authors University on the synthesis and biological evaluation of several potential PDT photosensitizers. Not only new synthetic methodologies mainly for porphyrins and chlorins were developed but also other related macrocycles of the phthalocyanine and corrole types have entered in the same "pipeline". In vivo and in vitro biological evaluations also took place under interdisciplinary studies.

97 citations


Journal ArticleDOI
TL;DR: In this review a special attention will be given to the role of some drug delivery systems to improve the efficiency of tetrapyrrolic photosensitizers to this type of treatment.
Abstract: Photodynamic therapy (PDT) is a modality of cancer treatment in which tumor cells are destroyed by reactive oxygen species (ROS) produced by photosensitizers following its activation with visible or near infrared light. The PDT success is dependent on different factors namely on the efficiency of the photosensitizer deliver and targeting ability. In this review a special attention will be given to the role of some drug delivery systems to improve the efficiency of tetrapyrrolic photosensitizers to this type of treatment.

86 citations


Journal ArticleDOI
TL;DR: The objective of this review is to describe the development of naphthoquinones as antifungals for the treatment of Candida species and to note the most promising compounds.
Abstract: Naphthoquinones are the most commonly occurring type of quinones in nature. They are a diverse family of secondary metabolites that occur naturally in plants, lichens and various microorganisms. This subgroup is constantly being expanded through the discovery of new natural products and by the synthesis of new compounds via innovative techniques. Interest in quinones and the search for new biological activities within the members of this class have intensified in recent years, as evidenced by the evaluation of the potential antimicrobial activities of quinones. Among fungi of medical interest, yeasts of the genus Candida are of extreme importance due to their high frequency of colonization and infection in humans. The objective of this review is to describe the development of naphthoquinones as antifungals for the treatment of Candida species and to note the most promising compounds. By using certain criteria for selection of publications, 68 reports involving both synthetic and natural naphthoquinones are discussed. The activities of a large number of substances were evaluated against Candida albicans as well as against 7 other species of the genus Candida. The results discussed in this review allowed the identification of 30 naphthoquinones with higher antifungal activities than those of the currently used drugs.

72 citations


Journal ArticleDOI
TL;DR: Considering the chemical and biological diversity of Brazil, this review highlights the Brazilian natural products that were successfully used to develop new products and the value of secondary metabolites from Brazilian biodiversity with potential application for new Products and technologies.
Abstract: The development of our society has been based on the use of biodiversity, especially for medicines and nutrition. Brazil is the nation with the largest biodiversity in the world accounting for more than 15% of all living species. The devastation of biodiversity in Brazil is critical and may not only cause the loss of species and genes that encode enzymes involved in the complex metabolism of organisms, but also the loss of a rich chemical diversity, which is a potential source for bioeconomy based on natural products and new synthetic derivatives. Bioeconomy focus on the use of bio-based products, instead of fossil-based ones and could address some of the important challenges faced by society. Considering the chemical and biological diversity of Brazil, this review highlights the Brazilian natural products that were successfully used to develop new products and the value of secondary metabolites from Brazilian biodiversity with potential application for new products and technologies. Additionally, we would like to address the importance of new technologies and scientific programs to support preservation policies, bioeconomy and strategies for the sustainable use of biodiversity.

62 citations


Journal ArticleDOI
TL;DR: Band algorithms in estimating chlorophyll-a (Chl-a) concentration based on bands of two new sensors: Operational Land Imager onboard Landsat-8 satellite (OLI/Landsat- 8), and MultiSpectral Instrument onboard Sentinel-2A (MSI/Sentinel-2 A) were assessed.
Abstract: In this present research, we assessed the performance of band algorithms in estimating chlorophyll-a (Chl-a) concentration based on bands of two new sensors: Operational Land Imager onboard Landsat-8 satellite (OLI/Landsat-8), and MultiSpectral Instrument onboard Sentinel-2A (MSI/Sentinel-2A). Band combinations designed for Thematic Mapper onboard Landsat-5 satellite (TM/Landsat-5) and MEdium Resolution Imaging Spectrometer onboard Envisat platform (MERIS/Envisat) were adapted for OLI/Landsat-8 and MSI/Sentinel-2A bands. Algorithms were calibrated using in situ measurements collected in three field campaigns carried out in different seasons. The study area was the Barra Bonita hydroelectric reservoir (BBHR), a highly productive aquatic system. With exception of the three-band algorithm, the algorithms were spectrally few affected by sensors changes. On the other hands, algorithm performance has been hampered by the bio-optical difference in the reservoir sections, drought in 2014 and pigment packaging.

55 citations


Journal ArticleDOI
TL;DR: In this paper, essential oils from Citrus aurantifolia leaves and fruit peel were obtained by hydrodistillation by a Clevenger-type apparatus, whereas their chemical composition was analyzed by gas chromatography-flame ionization detector (GC-FID) and GC-MS.
Abstract: Tooth decay is a major public health problem which affects a large number of people in several countries. Even though more than 700 bacterial species have been detected in the oral cavity, Streptococcus and Lactobacillus stand out as the genera that cause tooth decay and other periodontal diseases. In this study, essential oils from Citrus aurantifolia leaves (CL-EO) and fruit peel (CP-EO) were obtained by hydrodistillation by a Clevenger-type apparatus whereas their chemical composition was analyzed by gas chromatography-flame ionization detector (GC-FID) and gas chromatography-mass spectrometry (GC-MS). Limonene (77.5 %), linalool (20.1 %), citronellal (14.5 %) and citronellol (14.2 %) were the main constituents found in the essential oils from C. aurantifolia leaves and fruit peel. Antibacterial activity of essential oils was evaluated in terms of its minimum inhibitory concentration (MIC) values by the broth microdilution method in 96-well microplates. Both CL-EO and CP-EO displayed some activity against all oral pathogens under investigation; MIC values ranged from 20 to 200 µg/mL. CL-EO and CP-EO not only had promising activity against Streptococcus mutans (MIC = 20 µg/mL) and Lactobacillus casei (31.25 µg/mL), but also displayed antibacterial activity against all studied cariogenic bacteria. Efficacy of essential oils against S. mutans and L. casei is noteworthy and should be further investigated.

55 citations


Journal ArticleDOI
TL;DR: CC50 value for AgNPs-TA suggested that TA attenuates nanosilver toxicity comparatively to its precursor (Ag+), which can contribute to the development of new, green, and fast produced drugs aiming at leishmaniasis treatment.
Abstract: Gold (Au0) and silver (Ag0) nanoparticles were synthesized using tannic acid (TA) as both reducing and stabilizer. Nanoparticles formation, stability, and interaction with TA were compared to citrate-coated nanoparticles and monitored by UV-Vis, zeta potential, and transmission electron microscopy. TA coating resulted in a red-shift and broadening of bands compared to citrate-coated nanoparticles (NPs-Cit). AgNPs-TA and AuNPs-TA are negatively charged with mean surface charge of -29.4 mV and -29.6 mV, respectively. TEM images showed polydispersety of AuNPs-TA (6-42 nm) and aggregation of AgNPs-TA (12-71 nm). In vitro assays of Leishmania amazonensis promastigotes showed an increment of antileishmanial activity for AgNPs-TA in relation to AgNPs-Cit, while AuNPs-TA and AuNPs-Cit did not affect the protozoas at tested concentrations. CC50 value for AgNPs-TA suggested that TA attenuates nanosilver toxicity comparatively to its precursor (Ag+). This investigation can contribute to the development of new, green, and fast produced drugs aiming at leishmaniasis treatment.

48 citations


Journal ArticleDOI
TL;DR: This review describes the drugs based on artemisinin and its derivatives, including hybrid derivatives and dimers, trimers and tetramers that contain an endoperoxide bridge, of extreme importance for the discovery of new drugs to treat malaria.
Abstract: According to the World Health Organization, malaria remains one of the biggest public health problems in the world. The development of resistance is a current concern, mainly because the number of safe drugs for this disease is limited. Artemisinin-based combination therapy is recommended by the World Health Organization to prevent or delay the onset of resistance. Thus, the need to obtain new drugs makes artemisinin the most widely used scaffold to obtain synthetic compounds. This review describes the drugs based on artemisinin and its derivatives, including hybrid derivatives and dimers, trimers and tetramers that contain an endoperoxide bridge. This class of compounds is of extreme importance for the discovery of new drugs to treat malaria.

45 citations


Journal ArticleDOI
TL;DR: A comprehensive review of the advent and impact of continuous flow chemistry with regard to the synthesis of natural products and drugs, important pharmaceutical products and definitely responsible for a revolution in modern healthcare is presented.
Abstract: We present a comprehensive review of the advent and impact of continuous flow chemistry with regard to the synthesis of natural products and drugs, important pharmaceutical products and definitely responsible for a revolution in modern healthcare. We detail the beginnings of modern drugs and the large scale batch mode of production, both chemical and microbiological. The introduction of modern continuous flow chemistry is then presented, both as a technological tool for enabling organic chemistry, and as a fundamental research endeavor. This part details the syntheses of bioactive natural products and commercial drugs.

Journal ArticleDOI
TL;DR: This review presented in this review the work done with a special emphasis on the development of dendrimers as a major tool in the combination with drugs, as a potential adjunctive agent in anticancer therapy.
Abstract: Currently, cancer is the second most common cause of death in the United States, exceeded only by heart disease. Chemotherapy traditionally suffers from a non-specific distribution, with only a small fraction of the drug reaching the tumor, in this sense, the use of dendrimers incorporating drugs non-covalently encapsulated inside the dendrimer or covalently conjugated have proven to be effectives against different cancer cell lines. However, at present the dendrimers used as drug-carriers still do not meet the necessary characteristic to be considered as an ideal dendrimer for drug delivery; high toxicity, bio-degradability, low toxicity, biodistribution characteristics, and favorable retention with appropriate specificity and bioavailability have not been fully covered by the current available dendrimers. However, the development and study of new dendrimers drug-carriers continues to be an important tool in the cancer therapy as they can be functionalized with varied ligands to reach the tumor tissue through the different body barriers in the body with minimal loss of activity in the bloodstream, have the ability to selectively kill tumor cells without affecting the normal cells and most important with a release mechanism controlling actively. Given the continuous efforts and research in this area of interest, we presented in this review the work done with a special emphasis on the development of dendrimers as a major tool in the combination with drugs, as a potential adjunctive agent in anticancer therapy.

Journal ArticleDOI
TL;DR: Investigation of the effect of ferrous nano-oxide particles on nutritional compounds of soybean seed found application of 0.75 to 1 g L-1 ferrous Nano-oxide had the best effect on the nutrient composition of soy bean seed.
Abstract: Soybean (Glycine max L.) seed contains amounts of protein, lipid, carbohydrate and mineral elements, which protein and lipid have been known as a main part for soybean's trade value. In this study, in order to investigate the effect of ferrous nano-oxide particles on nutritional compounds of soybean seed, an experiment with 5 treatments and 3 replications was conducted as a randomized complete block design. Treatments were 5 concentrations of ferrous nano-oxide particles including 0, 0.25, 0.5, 0.75 and 1 g L-1 which were sprayed 3 times at 4 and 8 leaves stage and pod initiation. Lipid and protein contents, fatty acids profile, some of mineral elements such as Fe, Mg, Ca and P, chlorophyll a, b and total chlorophyll content were determined. Results showed that solution containing ferrous nano-oxide particles had significant effect on nutritional compounds of soybean seed (P<0.01) compared to control. The highest content of lipid and protein (25.4 and %33.8, respectively) observed by applying 0.75 g L-1 of ferrous nano-oxide and the lowest content was also in control. Changes in the trends of fatty acids profile (palmitic, oleic, linoleic and linolenic acids), some of mineral elements (Fe, Mg, Ca and P) and chlorophyll contents were similar to lipid and protein levels which by increasing in concentration of ferrous nano-oxide from 0 to 0.75 g L-1 all measured parameters also increased, but reduction in all parameters was observed in concentration from 0.75 to 1 g L-1. In conclusion, application of 0.75 to 1 g L-1 ferrous nano-oxide had the best effect on the nutrient composition of soybean seed.

Journal ArticleDOI
TL;DR: This review describes some principles of the controlled synthesis of metal nanoparticles, focusing on how the fundamental understanding of their synthesis in the solution-phase can be put to tailor size, shape, composition, and architecture to enable the tuning of properties.
Abstract: This review describes some principles of the controlled synthesis of metal nanoparticles, focusing on how the fundamental understanding of their synthesis in the solution-phase can be put to tailor size, shape, composition, and architecture. The maneuvering over these parameters not only enable the tuning of properties, but also the maximization and optimization of performances for various applications. Herein, we start with a brief description of metallic nanoparticles, highlighting the motivation for achieving physicochemical control in their synthesis. After that, we turn our attention to some important definitions and classifications as well as their unique properties such as surface and quantum effects. Moreover, we discuss the strategies for the controlled synthesis of metal nanomaterials based on the top-down and bottom-up approaches, focusing our discussion on their formation mechanisms in liquid-phase in terms of both thermodynamic and kinetic control. Finally, we point out the promising applications of controlled nanomaterials in the field of nanocatalysis and plasmon-enhanced catalysis, describing some of the current challenges in these fields.

Journal ArticleDOI
TL;DR: An overview is provided of the status of research at the frontiers of investigation of the chemistry and photochemistry of two classes of natural plant pigments, the anthocyanins and the betalains, as well as of the pyranoanthocyanin pigments formed during the maturation of red wine.
Abstract: An overview is provided of the status of research at the frontiers of investigation of the chemistry and photochemistry of two classes of natural plant pigments, the anthocyanins and the betalains, as well as of the pyranoanthocyanin pigments formed from anthocyanins during the maturation of red wine. Together, anthocyanins and betalains are responsible for almost all of the red, purple and blue colors of fruits and flowers and anthocyanins and pyranoanthocyanins are major contributors to the color of red wines. All three types of pigments are cationic below about pH 3, highly colored, non-toxic, reasonably soluble in water or alcohol and fairly stable to light. They exhibit good antioxidant or antiradical activity and, as part of our diet, confer a number of important health benefits. Systematic studies of model compounds containing the basic chromophoric groups of these three types of pigments are providing a deeper understanding of the often complex chemistry and photochemistry of these pigments and their relationship to the roles in vivo of these pigments in plants. These natural pigments are currently being exploited as starting materials for the preparation of novel semi-synthetic dyes, pigments and fluorescence probes.

Journal ArticleDOI
Ruy José Válka Alves1, Marcelo Weksler1, João Alves de Oliveira1, Paulo A. Buckup1, José P. Pombal1, Hélcio R.G. Santana2, Adriano Lúcio Peracchi3, Alexander W.A. Kellner1, Alexandre Aleixo4, Alfredo Langguth5, Alzira Maria Paiva de Almeida2, Ana Luisa Albernaz4, Camila C. Ribas6, Carla Zilberberg1, Carlos E. V. Grelle1, Carlos Frederico Duarte Rocha7, Carlos José Einicker Lamas8, Célio F. B. Haddad9, Cibele R. Bonvicino, Cynthia P. A. Prado9, Daniela Oliveira de Lima10, Denise de Cerqueira Rossa-Feres9, Fabrício R. Santos11, Fátima Regina Gonçalves Salimena12, Fernando A. Perini11, Flávio Alicino Bockmann8, Francisco Luís Franco13, Gisele Mendes Lessa del Giudice14, Guarino R. Colli15, Ima Célia Guimarães Vieira4, Jader Marinho-Filho15, Jane Margaret Costa de Frontin Werneck2, Jorge Abdala Dergam dos Santos14, Jorge Luiz do Nascimento, Jorge Luiz Nessimian1, José Luis Passos Cordeiro2, Kleber Del Claro16, Leandro O. Salles1, Lilian Casatti9, Lucia Helena R. Py-Daniel12, Luís Fábio Silveira8, Luís Felipe Toledo17, Luiz Fernando Seixas De Oliveira1, Luiz Roberto Malabarba18, Marcelo de Assumpção Pereira da Silva8, Márcia Souto Couri1, Marcio Martins8, Marcos D.S. Tavares8, Marcos Sobral19, Marcus Vinícius Vieira1, Maria Auxiliadora Oliveira2, Mário C. C. de Pinna8, Michael John Gilbert Hopkins6, Mirco Solé20, Naércio A. Menezes8, Paulo Passos1, Paulo Sérgio D'Andrea2, Pedro Cordeiro Estrela de Andrade Pinto5, Pedro Lage Viana4, Peter Mann de Toledo21, Roberto E. Reis22, Roberto do Val Vilela2, Rogério Pereira Bastos23, Rosane G. Collevatti23, Rui Cerqueira1, Santiago Castroviejo-Fisher22, Ulisses Caramaschi1 
TL;DR: This legal framework was meant to improve governmental control over systems of biotechnology research using genetic material and associated chemical compounds, which are central points of the Nagoya Protocol and the Convention on Biological Diversity.
Abstract: Beginning in November 2018, Brazilian legislation regulating access to genetic heritage and associated traditional knowledge will cause a bureaucratic collapse of Biodiversity research in Brazil. Law number 13.123/2015 and Decree 8772/2016 impose severe barriers to basic and applied research, and to international cooperation by introducing mandatory registry of research access to native organisms in Brazil. This legal framework was meant to improve governmental control over systems of biotechnology research using genetic material and associated chemical compounds, which are central points of the Nagoya Protocol (CBD 2011) and the Convention on Biological Diversity (CBD 1992, 2012). However, the requirements imposed by the mandatory registry of research in the new National System for Governance of Genetic Heritage and Associated Traditional Knowledge (SisGen), the system of Material Transfer Agreements (MTAs), and the need to record access to organismal data prior to publication of scientific results or exportation of specimens for scientific research are technically impracticable and not part of the Nagoya Protocol or CBD ..

Journal ArticleDOI
TL;DR: This is the first report of the chemical composition of PI-EO and results suggest that the essential oils under evaluation have high potential to control the phytopathogenic fungus S. sclerotiorum.
Abstract: Even though essential oils from Piper aduncum (Piperaceae) have different biological activities, little is known about their application to agricultural areas. White mold is a plant disease caused by the phytopathogen Sclerotinia sclerotiorum, which needs to be controlled by alternative measures. This study aimed at evaluating the effect of essential oils from P. aduncum leaves (PL-EO) and inflorescences (PI-EO) on the mycelial growth of S. sclerotiorum. Essential oils from P. aduncum were obtained by hydrodistillation by a Clevenger-type apparatus while their chemical composition was analyzed by GC-MS and GC-FID. Piperitone (23.4 %), myristicin (12.4 %), terpinen-4-ol (12.3 %), β-caryophyllene (7.2 %), α-humulene (6.9 %), germacrene-D (6.9 %) and dillapiol (6.3 %) were the main constituents found in oils from P. aduncum. The in vitro antifungal activity showed that PI-EO dose above 30 µL inhibited mycelial growth in 100 %, whereas PL-EO at 50 µL inhibited it in 98.74 %. This is the first report of the chemical composition of PI-EO and results suggest that the essential oils under evaluation have high potential to control the phytopathogenic fungus S. sclerotiorum.

Journal ArticleDOI
TL;DR: The antibacterial and antibiofilm activities of the antimicrobial peptide P34, characterized as a bacteriocin-like substance (BLS P34) were tested against planktonic and sessile cells of Staphylococcus aureus and Enterococcus faecalis isolated from foods.
Abstract: The adhesion ability of bacteria to abiotic surfaces has important implications in food industries, because these organisms can survive for long periods through the biofilm formation. They can be transferred from one place to another in the industry causing contamination of the food processing environment. In this study, the antibacterial and antibiofilm activities of the antimicrobial peptide P34, characterized as a bacteriocin-like substance (BLS P34) were tested against planktonic and sessile cells of Staphylococcus aureus and Enterococcus faecalis isolated from foods. The BLS P34 showed inhibitory effect against all planktonic cells of E. faecalis. The inhibition of biofilm formation and the eradication of pre-formed biofilm were evaluated with the crystal violet assay and with the reduction of 3-bromide [4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium. The BLS P34 promoted a reduction of percentage of adhered microbial cells on the surface, not being able to perform the complete elimination of biofilm formation. The metabolic activity of S. aureus biofilms decreased considerably between 41-95%. However, E. faecalis cells showed up metabolically stimulated. The BLS P34 has the potential antibiofilm for the species S. aureus. Studies suggest more detailed approaches to a better understanding of the interactions between the antimicrobial and bacterial cells within the biofilm structure.

Journal ArticleDOI
TL;DR: This paper aims to gather and discuss important information about nonylphenol, such as physical chemistry properties, toxicity and analytical methods in various matrices, seen as a critical environmental pollutant.
Abstract: This paper aims to gather and discuss important information about nonylphenol, such as physical chemistry properties, toxicity and analytical methods in various matrices. As a degradation product of ethoxylated alkylphenols, nonylphenol presents a higher degree of reactivity than its precursor. Due to its harmful effects on the environment, use and production of nonylphenol has been banned in European Union countries, alongside their precursors. The guide on quality of drinking water (USEPA) recommends a maximum concentration of 28 µg L-1 for fresh water. In Brazil, there is no clear legislation containing values ​​of maximum concentration of nonylphenol. Due to this lack of regulation, a continuous monitoring is necessary of this pollutant in environmental samples. This paper aims to encourage further studies on nonylphenol, seen as a critical environmental pollutant. For proper monitoring is necessary to have reliable analytical methods and easy to perform in routine analysis.

Journal ArticleDOI
TL;DR: The current panorama of drug research and development (R&D) with emphasis on some of the major advances brought to clinical trials and to the market in the past five years is examined.
Abstract: Cancer is one of the leading causes of death worldwide. With the increase in life expectancy, the number of cancer cases has reached unprecedented levels. In this scenario, the pharmaceutical industry has made significant investments in this therapeutic area. Despite these efforts, cancer drug research remains a remarkably challenging field, and therapeutic innovations have not yet achieved expected clinical results. However, the physiopathology of the disease is now better understood, and the discovery of novel molecular targets has refreshed the expectations of developing improved treatments. Several noteworthy advances have been made, among which the development of targeted therapies is the most significant. Monoclonal antibodies and antibody-small molecule conjugates have emerged as a worthwhile approach to improve drug selectivity and reduce adverse effects, which are the main challenges in cancer drug discovery. This review will examine the current panorama of drug research and development (R&D) with emphasis on some of the major advances brought to clinical trials and to the market in the past five years. Breakthrough discoveries will be highlighted along with the medicinal chemistry strategies used throughout the discovery process. In addition, this review will provide perspectives and updates on the discovery of novel molecular targets as well as drugs with innovative mechanisms of action.

Journal ArticleDOI
TL;DR: A new three-parameter lifetime model called the Lindley Weibull distribution is introduced, which accommodates unimodal and bathtub, and a broad variety of monotone failure rates, and some of its mathematical properties including ordinary and incomplete moments, quantile and generating functions and order statistics are provided.
Abstract: We introduce a new three-parameter lifetime model called the Lindley Weibull distribution, which accommodates unimodal and bathtub, and a broad variety of monotone failure rates. We provide a comprehensive account of some of its mathematical properties including ordinary and incomplete moments, quantile and generating functions and order statistics. The new density function can be expressed as a linear combination of exponentiated Weibull densities. The maximum likelihood method is used to estimate the model parameters. We present simulation results to assess the performance of the maximum likelihood estimation. We prove empirically the importance and flexibility of the new distribution in modeling two data sets.

Journal ArticleDOI
TL;DR: A novel use of yellow sweet potato in breads is showed, which brings benefits to consumers' health and for the agricultural business, and an increase in water activity, moisture, orange coloring, and carotenoids is observed.
Abstract: Yellow sweet potato is mostly produced by small farmers, and may be a source of energy and carotenoids in the human diet, but it is a highly perishable crop. To increase its industrial application, yellow sweet potato flour has been produced for use in bakery products. This study aimed to evaluate the technological quality and the carotenoids content in sweet breads produced with the replacement of wheat flour by 0, 3, 6, and 9% yellow sweet potato flour. Breads were characterized by technological parameters and β-carotene levels during nine days of storage. Tukey's test (p<0.05) was used for comparison between means. The increase in yellow sweet potato flour concentrations in bread led to a decrease of specific volume and firmness, and an increase in water activity, moisture, orange coloring, and carotenoids. During storage, the most significant changes were observed after the fifth day, with a decrease in intensity of the orange color. The β-carotene content was 0.1656 to 0.4715 µg/g in breads with yellow sweet potato flour. This work showed a novel use of yellow sweet potato in breads, which brings benefits to consumers' health and for the agricultural business.

Journal ArticleDOI
TL;DR: The essential oil of C. aschersoniana showed high activity against L. amazonensis promastigote forms, however, it also demonstrated a relatively high cytotoxicity on mouse peritoneal macrophages, the first report of the chemical composition and the leishmanicidal and cytotoxic activities of the leaf essential oil.
Abstract: Leishmaniasis is an endemic disease caused by protozoa of the genus Leishmania, which affects around two million people worldwide. One major drawback in the treatment of leishmaniasis is the emergence of resistance to current chemotherapeutics. Medicinal and aromatic plants constitute a major source of natural organic compounds. In this study, the leaf essential oil of Cryptocarya aschersoniana was obtained by hydrodistillation in a Clevenger-type apparatus, and the chemical composition was analyzed by GC-MS and GC-FID. The essential oil of these species was predominantly constituted by monoterpene hydrocarbons (48.8%). Limonene (42.3%), linalool (9.7%) and nerolidol (8.6%) were the main constituents in the oil of C. aschersoniana. The in vitro activity of the oil was evaluated against the promastigote forms of Leishmania amazonensis, the causative agent of cutaneous leishmaniasis in humans. The essential oil of C. aschersoniana showed high activity against L. amazonensis promastigote forms (IC50 = 4.46 µg/mL), however, it also demonstrated a relatively high cytotoxicity on mouse peritoneal macrophages (CC50 = 7.71 µg/mL). This is the first report of the chemical composition and the leishmanicidal and cytotoxic activities of the leaf essential oil of C. aschersoniana.

Journal ArticleDOI
TL;DR: Yerba mate response to P was affected by edaphic and plant factors, and this was not accompanied by increased P in leaf tissue in all conditions tested.
Abstract: Native to subtropical region of South America, yerba mate is responsive to P under some conditions, but the degree of influence of genetic and soil on the growth and composition of the leaf is unknown. The aim of study was to evaluate plant growth, nutrients and potentially toxic elements in leaves of yerba mate clones in response to P application in acid soils. In greenhouse condition, two yerba mate clone seedlings were grown (210 days) in pots, each clone in a completely randomized design in factorial scheme (with and without P; four acid soils). The elemental composition of leaves and the growth of plants were determined. Phosphorus promoted plant growth, but this was not accompanied by increased P in leaf tissue in all conditions tested. The P effect on the elemental composition varied: decrease/null (N, K, Mg, Mn, Cu, Ni, B, Mo, Al, Cd); increase/null (C/N, C, Ca, Fe, V); increase/decrease/null (Zn, Ba, Pb) and; null (Cr). The soils affect the elemental composition of the leaves, especially Mn, with accumulation greater than 1000 mg kg-1. The Ba, Pb, Al and Zn in the leaves varied among clones. Yerba mate response to P was affected by edaphic and plant factors.

Journal ArticleDOI
TL;DR: This review try to introduce and contemplate some relevant topics for enzymeBioelectrochemistry, such as the immobilization of the enzymes at electrode surfaces, the electron transfer, the bioelectrocatalysis, and new techniques conjugated with electrochemistry vising understand the kinetics and thermodynamics of redox proteins.
Abstract: Bioelectrochemistry can be defined as a branch of Chemical Science concerned with electron-proton transfer and transport involving biomolecules, as well as electrode reactions of redox enzymes. The bioelectrochemical reactions and system have direct impact in biotechnological development, in medical devices designing, in the behavior of DNA-protein complexes, in green-energy and bioenergy concepts, and make it possible an understanding of metabolism of all living organisms (e.g. humans) where biomolecules are integral to health and proper functioning. In the last years, many researchers have dedicated itself to study different redox enzymes by using electrochemistry, aiming to understand their mechanisms and to develop promising bioanodes and biocathodes for biofuel cells as well as to develop biosensors and implantable bioelectronics devices. Inside this scope, this review try to introduce and contemplate some relevant topics for enzyme bioelectrochemistry, such as the immobilization of the enzymes at electrode surfaces, the electron transfer, the bioelectrocatalysis, and new techniques conjugated with electrochemistry vising understand the kinetics and thermodynamics of redox proteins. Furthermore, examples of recent approaches in designing biosensors and biofuel developed are presented.

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TL;DR: The highest antibacterial activity of ethanolic extract (Banarasi paan) may be attributed to the presence of phytosterols in the leaf varieties, and Antioxidant and antimicrobial potential study will help to build a database and promote the utilization of betel leaf as a medicinal herb.
Abstract: Piper betle L., is an evergreen perennial creeper belonging to family Piperaceae and is known to possess numerous medicinal properties. Current study focuses on evaluating antioxidant and antimicrobial potential of betel leaf. For the present study, distilled water, hexane, acetone and ethanolic extracts of two varieties of betel leaves: Meetha paan and Banarasi paan were used. Biochemical tests such as proximate analysis (moisture, ash, protein, lipids, minerals viz., sodium and potassium), antioxidant activity tests (DPPH radical scavenging activity, total phenolics, ascorbic acid, reducing power) and antimicrobial test (antibacterial and antifungal susceptibility test) against four pathogens viz., B. subtilis, E. coli, A. niger and S. cerevisiae were determined. Ethanolic extract had the highest antioxidant activity (89.46% inhibition), while the aqueous extract exhibited lowest antioxidant activity (62.03% inhibition). With increasing concentration (5, 10, 25 and 50 µg/mL), the reducing power of leaf extracts also increased. The ascorbic acid was not significant in Banarasi paan (5.21mg/100 g) and Meetha paan (5.20mg/100 g). The highest antibacterial activity of ethanolic extract (Banarasi paan) may be attributed to the presence of phytosterols in the leaf varieties. Antioxidant and antimicrobial potential study will help to build a database and promote the utilization of betel leaf as a medicinal herb.

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TL;DR: This review shows an outline of manuscripts that report the immobilization of enzymes as LB films since the 1980's, and also some examples of how the surface properties of the floating monolayer prepared previously to the transfer to the solid support are important to determine the efficiency of the resulting device.
Abstract: In this review we discuss about the immobilization of enzymes in Langmuir-Blodgett films in order to determine the catalytic properties of these biomacromolecules when adsorbed on solid supports. Usually, the conformation of enzymes depends on the environmental conditions imposed to them, including the chemical composition of the matrix, and the morphology and thickness of the film. In this review, we show an outline of manuscripts that report the immobilization of enzymes as LB films since the 1980's, and also some examples of how the surface properties of the floating monolayer prepared previously to the transfer to the solid support are important to determine the efficiency of the resulting device.

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TL;DR: The results suggest that activation of phenylpropanoid pathway represent a source of nonenzymatic antioxidants that protect at P. glandulosa against oxidative stress when exposed to cadmium and copper.
Abstract: The aim of the present work is to evaluate the changes on the phenylalanine ammonia lyase (PAL) activity, phenolic compounds accumulation and photochemical efficiency in leaves of P. glandulosa treated with Cd2+ (0.001 M) and Cu2+ (0.52 M) concentrations for 96 h under hydroponic conditions. The results showed that only leaves treated with copper had a decrease in photochemical efficiency and leaf epidermal polyphenols in P. glandulosa leaves after 96 h of exposure. On the other hand the reverse-phase HPLC analysis revealed higher levels of phenolic compound (gallic, vanillic and caffeic acids) and flavonoids (rutin and kaempferol-3-O-glucosides) in plant leaves from Cu and Cd-treatments with respect to control plants. Finally, highest increments in PAL activity was observed in extracts of leaves treated with Cu and Cd (about 205 and 284%), respectively, with respect to control plants after 96 h treatment. These suggest that activation of phenylpropanoid pathway represent a source of nonenzymatic antioxidants that protect at P. glandulosa against oxidative stress when exposed to cadmium and copper. Hence future studies are necessary to elucidate the participation of phenylpropanoid pathway in the reduction of metal toxicity in Prosopis species.

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TL;DR: It was determined anatomical features useful for diagnosis of the species which, together with identification of the chemical compounds and its histolocalization, provides support to their quality control.
Abstract: Solidago chilensis Meyen, belonging to the family Asteraceae, is a plant native to South America and the only representative of the genus in Brazil. This species is popularly known as "arnica" and is used to treat bruises, muscle pain and inflammation. The objective of this work was to contribute to the pharmacognostic standardization of S. chilensis. Cross-sections were obtained, by freehand, for microscopic analysis of root, stem and leaf; for these parts of the plant maceration was also performed according to the method of Jeffrey. For the leaf were still made paradermal sections, scanning electron microscopy analysis, phytochemical and histochemical tests. Thus, it was determined anatomical features useful for diagnosis of the species which, together with identification of the chemical compounds and its histolocalization, provides support to their quality control.

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TL;DR: Heterogeneity of genetic constitution in the studied population, which is favorable to breeding, is indicated, as it indicates the possibility to identify superior and divergent individuals.
Abstract: Knowledge of the genetic variability of a population is essential to guide its preservation and maintenance in addition to increasing the efficiency of genetic breeding programs. On this basis, this study was conducted to evaluate the genetic diversity of Coffea canephora genotypes using multivariate statistical procedures applied to a set of morpho-agronomic variables. The materials employed in this study constitute a crop located in Vila Valerio - ES, Brazil, where the genotypes are arranged in a randomized-blocks experimental design with four replicates. Significant differences were detected by the F test at the 1% or 5% probability levels among the genotypes for all evaluated traits, demonstrating heterogeneity of genetic constitution in the studied population, which is favorable to breeding, as it indicates the possibility to identify superior and divergent individuals. Based on the generalized Mahalanobis distance, the most divergent combinations were obtained between genotypes 23 and 10 (256.43) and 23 and 17 (250.09). The clusters formed by Tocher's optimization and the UPGMA hierarchical method agreed, both similarly grouping the genotypes into three clusters. Of the analyzed traits, mature fruit weight (19.08%), yield (15.50%), plant diameter (12.42%), and orthotropic-shoot internode length (10.94%) were the most efficient to explain the dissimilarity among the genotypes.