Antioxidant, anti-acetylcholinesterase and cytotoxic activities of ethanol extracts of peel, pulp and seeds of exotic Brazilian fruits Antioxidant, anti-acetylcholinesterase and cytotoxic activities in fruits

Ethanol extracts of powdered genipap (Genipa americana L), umbu (Spondia tuberosa A.) and siriguela (Spondia purpurea L) prepared from separate pulp, seeds and peel were investigated for their (i) antioxidant capacity, which was evaluated by various known methods; (ii) acetylcholinesterase (AChE) inhibitory activity; and (iii) cytotoxic effect on corneal epithelial cells of sheep. The highest values of total phenolic content were obtained with peel and seed extracts. Siriguela and umbu (seeds and peel) extracts displayed the highest antioxidant activities. Lipid peroxidation assays using mimetic biomembranes and mouse liver homogenates indicated that genipap pulp is a promising antioxidant. The investigation of phenols and organic acid contents revealed the presence of quercetin, citric and quinic acids, chlorogenic acid derivatives, among others, in several extracts, with the highest amount found in siriguela seeds. Genipap pulp and siriguela seed ethanol extracts presented an AChE inhibition zone similar to that of the positive control, carbachol. AChE inhibition assay with chlorogenic acid, one of the main constituents of siriguela seeds, revealed that this acid showed activity similar to that of the control physostigmine. These data suggest that these extracts are potentially important antioxidant supplements for the everyday human diet, pharmaceutical and cosmetic industries. (C) 2012 Elsevier Ltd. All rights reserved.

A new HPLC-DAD-MS/MS method for the simultaneous determination of major compounds in the crude extract of Lychnophora salicifolia Mart. (Brazilian arnicao) leaves: Application to chemical variability evaluation

Lychnophora salicifolia Mart., which occurs in the Brazilian Cerrado in the states of Bahia and Minas Gerais as well as in the southeast of the state of Goias, is the most widely distributed and also the most polymorphic species of the genus. This plant is popularly known to have anti-inflammatory and analgesic activities. In this work, we have studied the variation in terms of polar metabolites of ninety-three Lychnophora salicifolia Mart, specimens collected from different regions of the Brazilian Cerrado. Identification of the constituents of this mixture was carried out by analysis of the UV spectra and MS data after chromatographic separation. Twenty substances were identified, including chlorogenic acid derivatives, a flavonoid C-glucoside, and other sesquiterpenes. The analytical method was validated, and the reliability and credibility of the results was ensured for the purposes of this study. The concentration range required for analysis of content variability within the analyzed group of specimens was covered with appropriate values of limits of detection and quantitation, as well as satisfactory precision and recovery. A quantitative variability was observed among specimens collected from the same location, but on average they were similar from a chemical viewpoint. In relation to the study involving specimens from different locations, there were both qualitative and quantitative differences among plants collected from different regions of Brazil. Statistical analysis revealed that there is a correlation between geographical localization and polar metabolites profile for specimens collected from different locations. This is evidence that the pattern of metabolites concentration depends on the geographical distribution of the specimens. (C) 2012 Elsevier B.V. All rights reserved.

The revision of the Brazilian Forest Act: increased deforestation or a historic step towards balancing agricultural development and nature conservation?

Almost two-thirds of the Brazilian territory still has prevalence of natural vegetation. Although not all pristine, much of these areas have high conservation value. 170 million hectare (Mha) of the natural vegetation is located within Federal and State protected areas. Most of the remaining 367 Mha is on private agriculture lands, where the Forest Act is the most important legal framework for conservation. In July 2010, the Brazilian parliament began the analysis of a substitutive legislation for the Forest Act. The main motivations for the revision is that, on the one hand, it has been found ineffective in protecting natural vegetation, and on the other hand, it is perceived as a barrier against development in the agriculture sector. The substitutive Forest Act, as it presently stands, does not represent a balance between existing standpoints and objectives; it may drive development towards either more private protection through market-driven compensation actions, or increased deforestation and less nature protection/restoration. This article uses outcomes from modeling analyses to discuss weaknesses of the substitutive Forest Act and to suggest possible improvements. (C) 2011 Elsevier Ltd. All rights reserved.

TITANS OF CAPITALISM IN THE MODERNIZATION OF BRAZILIAN TERRITORY: URBAN AND AWARDS PUBLIC ASSISTANCE DURING THE FIRST REPUBLIC (1889-1930)

In Brazil, the newly created Republic expressed interests of the elite increasingly committed to foreign capital. The Rio de Janeiro saw accumulate vast resources in trade and finance, deriving for industrial applications. The city appears as articulator of Brazilian territory and mediation between it and the international market. In the capital of the Republic, the conservative plan would sweep the old city and inaugurate images copied from Europe and installed in the tropics with civilizing purpose. This materialized with infrastructure financing and loans to entrepreneurs in Europe and North America, awarded public service concessions. The project relied on strong support of mayors (members or representatives of the companies involved in the reforms). This work aims to address the relationship between the mayors of Rio de Janeiro during the First Republic and international capital, focusing on strategies for the production of new spaces in motion the modernization of Brazil and its international image.

Brazilian exchange rate complexity: Financial crisis effects

With the financial market globalization, foreign investments became vital for the economies, mainly in emerging countries. In the last decades, Brazilian exchange rates appeared as a good indicator to measure either investors' confidence or risk aversion. Here, some events of global or national financial crisis are analyzed, trying to understand how they influenced the "dollar-real" rate evolution. The theoretical tool to be used is the Lopez-Mancini-Calbet (LMC) complexity measure that, applied to real exchange rate data, has shown good fitness between critical events and measured patterns. (C) 2011 Elsevier B.V. All rights reserved.

Impacts of Trade in Non-timber Forest Products on Cooperation among Caboclo Households of the Brazilian Amazon

Trade in non-timber forest products (NTFPs) has been touted as promoting forest conservation and enhancing the well-being of local residents through increased cash income, which is considered a positive outcome. However, research on cooperation has demonstrated that increased market access and income may strengthen or weaken cooperation. Because cooperation is essential for community resilience in small-scale societies, negative effects on people's well-being can be expected if increased NTFP trade reduces cooperation. To evaluate whether NTFP trade affected cooperation, we used household data (survey and systematic observations) to compare the frequency of cooperation in two communities of Brazilian Amazon Caboclos, one of which engaged in NTFP trade, while the other did not. Cooperation was less frequent in the community trading NTFPs, but neither household cash income nor household participation in NTFP exploitation was associated with cooperative behavior. Decreased frequency most likely derived from indirect effects of NTFP trade, such as less time to fish or socialize, or other outcomes observable only at the community level, such as income inequality, the influx of new residents and consequent population growth. Our results indicate that conservation and development projects based on NTFP trade may negatively impact social and economic well-being of local communities.

Dihydrocinnamic acid derivatives from Hortia species and their chemotaxonomic value in the Rutaceae

Phytochemical studies of Hortia brasiliana and Hortia oreadica (Rutaceae) have led to the identification of three novel dihydrocinnamic acids: 5-methoxy-2,2-dimethyl-2H-1-benzopyran-8-propanoic acid, 5,6-dimethoxy-2,2-dimethyl-2H-1-benzopyran-8-propanoic acid and erythro-2-hydroxy-4-methoxy-3-(1,2,3-trihydroxy-3-methylbutyl) benzenepropanoic acid from H. brasiliana and the second compound and six known dihydrocinnamic acids from H. oreadica. Engler included Hortia as the single Neotropical genus in the Toddalioideae subtribe Toddaliinae. However, the range of dihydrocinnamic acid derivatives found in H. brasiliana and H. oreadica show that they contain similar compounds to other species of Hortia and clearly point to their phytochemical affinities with other Rutoideae species. (C) 2012 Elsevier Ltd. All rights reserved.

Synthesis and characterization of a diruthenium(II,III)-ketoprofen compound and study of the in vitro effects on CRC cells in comparison to the naproxen and ibuprofen derivatives

A new diruthenium(II,III) complex, of formula [Ru2Cl(ket)(4)], Ruket, containing the non-steroidal anti-inflammatory drug ketoprofen was synthesized and mainly characterized by electrospray ionization mass spectrometry (ESI-MS), UV-Vis-IR electronic spectroscopy and FTIR and Raman vibrational spectroscopies. The four drug-carboxylato bridging ligands stabilize a Ru-2(II,III) mixed valent core in a paddlewheel type structure as confirmed by ESI mass spectra, electronic and vibrational spectroscopies and magnetic measurements. Ruket and the analogous compounds containing ibuprofen, Ruibp, and naproxen, Runpx, were tested for the biological effects in the human colon carcinoma cells HT-29 and Caco-2 expressing high and low levels of COX-2 respectively. All compounds only weakly affected the proliferation of the colorectal cancer cells HT-29 and Caco-2, and similarly only partially inhibited the production/activity of MMP-2 and MMP-9 by HT-29 cells, suggesting that COX-2 inhibition by these drugs can only partially be involved in the pharmacological effects of these derivatives. (c) 2012 Elsevier Ltd. All rights reserved.

Density Functional Theory (DFT) Study of Edaravone Derivatives as Antioxidants

Quantum chemical calculations at the B3LYP/6-31G* level of theory were employed for the structure-activity relationship and prediction of the antioxidant activity of edaravone and structurally related derivatives using energy (E), ionization potential (IP), bond dissociation energy (BDE), and stabilization energies(Delta E-iso). Spin density calculations were also performed for the proposed antioxidant activity mechanism. The electron abstraction is related to electron-donating groups (EDG) at position 3, decreasing the IP when compared to substitution at position 4. The hydrogen abstraction is related to electron-withdrawing groups (EDG) at position 4, decreasing the BDECH when compared to other substitutions, resulting in a better antioxidant activity. The unpaired electron formed by the hydrogen abstraction from the C-H group of the pyrazole ring is localized at 2, 4, and 6 positions. The highest scavenging activity prediction is related to the lowest contribution at the carbon atom. The likely mechanism is related to hydrogen transfer. It was found that antioxidant activity depends on the presence of EDG at the C-2 and C-4 positions and there is a correlation between IP and BDE. Our results identified three different classes of new derivatives more potent than edaravone.

An investigation about Brazilian mango and grape exports

Purpose - The objective of this paper is to characterise the transactions between European buyers and Brazilian mango and grape producers. Design/methodology/approach - The method selected for this paper was multiple case studies. The Brazilian mango and grape supply chains' export activities to Europe were investigated. The field research was undertaken in Brazil, Germany, The Netherlands and the UK. In total, 41 face-to-face interviews were carried out. Findings - The supermarkets' literature tends to generalise the strategies of retailers focusing on differentiation and preferred suppliers. However, in empirical research conducted in the UK, Germany and The Netherlands it is possible to conclude that the procurement strategies of supermarkets can vary sharply. The results reveal the presence of different agents who demand different quality standards. The level of intensity depends on consumer behaviour, the features of product commercialised and the characteristics of the production segment in each country. Research limitations/implications - First, in relation to the empirical method there is a limitation because the case study does not allow statistical generalisation. Consequently, it will be interesting to undertake quantitative research in order to quantify the variables presented and their impact on the structure of value chains. Second, the research focuses only on two stages of the supply chain, producers and buyers. Practical implications - The differences between UK and German supermarkets challenge the supermarket literature, which tends to generalise the strategies of retailers focusing on differentiation and preferred suppliers. Originality/value - The study shows that the issue of influence and activities of retail agents along the value chain can be analysed taking several variables into consideration: the products commercialised; the distribution segment; and the consumer market. This result opens the way for analysing different structures of the value chain and the impact of these differences on the entry of producers for developing countries into the global market.

Systematic UPLC-ESI-MS/MS Study on the Occurrence of Staurosporine and Derivatives in Associated Marine Microorganisms from Eudistoma vannamei

Former bioactivity-guided analysis of the marine invertebrate Eudistoma vannamei led to the isolation of staurosporine derivatives, which revealed strong cytotoxic activity against several human cancer cell lines. The occurrence of such alkaloids in E. vannamei may be correlated to the presence of associated biota, such as Streptomyces bacteria. In agreement to this hypothesis, marine microorganisms associated with E. vannamei were recovered and cultured, leading to a total of 84 isolated bacterial strains. Gas phase fragmentation reactions of staurosporine and derivatives were systematically studied and the analyzed results further supported by computational chemistry studies. The resulting fragment patterns were used to search for the presence of different derivatives in extracts of isolated microorganisms, thereby using LC-MS/MS analysis in MRM mode. These results evidenced that one isolated Streptomyces sp. was able to generate staurosporine, while none of the hydroxy-7-oxo derivatives were detected. Finally, significant cytotoxic activity against human cancer lines was observed for one of the extracts.

Two series of new semisynthetic triterpene derivatives: differences in anti-malarial activity, cytotoxicity and mechanism of action

Background The discovery and development of anti-malarial compounds of plant origin and semisynthetic derivatives thereof, such as quinine (QN) and chloroquine (CQ), has highlighted the importance of these compounds in the treatment of malaria. Ursolic acid analogues bearing an acetyl group at C-3 have demonstrated significant anti-malarial activity. With this in mind, two new series of betulinic acid (BA) and ursolic acid (UA) derivatives with ester groups at C-3 were synthesized in an attempt to improve anti-malarial activity, reduce cytotoxicity, and search for new targets. In vitro activity against CQ-sensitive Plasmodium falciparum 3D7 and an evaluation of cytotoxicity in a mammalian cell line (HEK293T) are reported. Furthermore, two possible mechanisms of action of anti-malarial compounds have been evaluated: effects on mitochondrial membrane potential (ΔΨm) and inhibition of β-haematin formation. Results Among the 18 derivatives synthesized, those having shorter side chains were most effective against CQ-sensitive P. falciparum 3D7, and were non-cytotoxic. These derivatives were three to five times more active than BA and UA. A DiOC6(3) ΔΨm assay showed that mitochondria are not involved in their mechanism of action. Inhibition of β-haematin formation by the active derivatives was weaker than with CQ. Compounds of the BA series were generally more active against P. falciparum 3D7 than those of the UA series. Conclusions Three new anti-malarial prototypes were obtained from natural sources through an easy and relatively inexpensive synthesis. They represent an alternative for new lead compounds for anti-malarial chemotherapy.

A three-pronged approach to social business: a Brazilian multi-case analysis

Social businesses present a new paradigm to capitalism, in which private companies, non-profit organizations and civil society create a new type of business with the main objective of solving social problems with financial sustainability and efficiency through market mechanisms. As any new phenomenon, different authors conceptualize social businesses with distinct views. This article aims to present and characterize three different perspectives of social business definitions: the European, the American and that of the emerging countries. Each one of these views was illustrated by a different Brazilian case. We conclude with the idea that all the cases have similar characteristics, but also relevant differences that are more than merely geographical. The perspectives analyzed in this paper provide an analytical framework for understanding the field of social businesses. Moreover, the cases demonstrate that in the Brazilian context the field of social business is under construction and that as such it draws on different conceptual influences to deal with a complex and challenging reality.

Inclusive business and poverty: prospects in the Brazilian context

Inclusive business is a term currently used to explain the organizations that aim to solve social problems with efficiency and financial sustainability by means of market mechanisms. It can be said that inclusive businesses are those targeted at generating employment and income for groups with little or no market mobility, in keeping with the standards of so-called "decent jobs" and in a self-sustaining manner, i.e., generating profit for the enterprises, and establishing relationships with typical business organizations as suppliers of products and services or in the distribution of this type of production. This article discusses the different concepts found in the scientific literature on inclusive businesses. It also analyses data from a survey conducted with the audiences of Social Corporate Responsibility seminars held by FIEMG. This analysis reveals that prospects, risks and idealizations similar to those found in inclusive business theories can also be found among individuals that run social corporate responsibility projects, even if this designation is new for them. The connection between companies and poverty, especially in relation to inclusive businesses, seems full of stumbling blocks and traps in the Brazilian context.

Systematic UPLC-ESI-MS/MS study on the occurrence of staurosporine and derivatives in associated marine microorganisms from Eudistoma vannamei

Former bioactivity-guided analysis of the marine invertebrate Eudistoma vannamei led to the isolation of staurosporine derivatives, which revealed strong cytotoxic activity against several human cancer cell lines. The occurrence of such alkaloids in E. vannamei may be correlated to the presence of associated biota, such as Streptomyces bacteria. In agreement to this hypothesis, marine microorganisms associated with E. vannamei were recovered and cultured, leading to a total of 84 isolated bacterial strains. Gas phase fragmentation reactions of staurosporine and derivatives were systematically studied and the analyzed results further supported by computational chemistry studies. The resulting fragment patterns were used to search for the presence of different derivatives in extracts of isolated microorganisms, thereby using LC-MS/MS analysis in MRM mode. These results evidenced that one isolated Streptomyces sp. was able to generate staurosporine, while none of the hydroxy-7-oxo derivatives were detected. Finally, significant cytotoxic activity against human cancer lines was observed for one of the extracts.