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Traditional conservation techniques for mapping highly biodiverse areas assume there to be satisfactory knowledge about the geographic distribution of biodiversity. There are, however, large gaps in biological sampling and hence knowledge shortfalls. This problem is even more pronounced in the tropics. Indeed, the use of only a few taxonomic groups or environmental surrogates for modelling biodiversity is not viable in mega-diverse countries, such as Brazil. To overcome these limitations, we developed a comprehensive spatial model that includes phylogenetic information and other several biodiversity dimensions aimed at mapping areas with high relevance for biodiversity conservation. Our model applies a genetic algorithm tool for identifying the smallest possible region within a unique biota that contains the most number of species and phylogenetic diversity, as well as the highest endemicity and phylogenetic endemism. The model successfully pinpoints small highly biodiverse areas alongside regions with knowledge shortfalls where further sampling should be conducted. Our results suggest that conservation strategies should consider several taxonomic groups, the multiple dimensions of biodiversity, and associated sampling uncertainties.

AimThe knowledge of biodiversity facets such as species composition, distribu-tion and ecological niche is fundamental for the construction of biogeographichypotheses and conservation strategies. However, the knowledge on these facetsis affected by major shortfalls, which are even more pronounced in the tropics.This study aims to evaluate the effect of sampling bias and variation in collec-tion effort on Linnean, Wallacean and Hutchinsonian shortfalls and diversitymeasures as species richness, endemism and beta-diversity.LocationBrazil.MethodsWe have built a database with over 1.5 million records of arthro-pods, vertebrates and angiosperms of Brazil, based on specimens deposited inscientific collections and on the taxonomic literature. We used null models totest the collection bias regarding the proximity to access routes. We also testedthe influence of sampling effort on diversity measures by regression models. Toinvestigate the Wallacean shortfall, we modelled the geographic distribution ofover 4000 species and compared their observed distribution with models. Toquantify the Hutchinsonian shortfall, we used environmental Euclidean distanceof the records to identify regions with poorly sampled environmental condi-tions. To estimate the Linnean shortfall, we measured the similarity of speciescomposition between regions close to and far from access routes.ResultsWe demonstrated that despite the differences in sampling effort, thestrong collection bias affects all taxonomic groups equally, generating a patternof spatially biased sampling effort. This collection pattern contributes greatly tothe biodiversity knowledge shortfalls, which directly affects the knowledge onthe distribution patterns of diversity.Main conclusionsThe knowledge on species richness, species composition andendemism in the Brazilian biodiversity is strongly biased spatially. Despite dif-ferences in sampling effort for each taxonomic group, roadside bias affectedthem equally. Species composition similarity decreased with the distance fromaccess routes, suggesting collection surveys at sites far from roads couldincrease the probability of sampling new geographic records or new species. ObjetivoO conhecimento das facetas da biodiversidade como composição, distribuição e nicho ecológico das espécies é fundamental para a construção de hipóteses biogeográficas e estratégias de conservação. No entanto, o conhecimento sobre essas facetas é afetado por grandes déficits, que são ainda mais pronunciados nos trópicos. Este estudo visa avaliar o efeito do viés de amostragem e variação no esforço de coleta sobre os déficits e medidas de diversidade de Linnean, Wallacean e Hutchinsonian como riqueza de espécies , endemismo e beta-diversidade.LocalizaçãoBrasil.MétodosConstruímos um banco de dados com mais de 1,5 milhão de registros de artrópodes, vertebrados e angiospermas do Brasil, com base em espécimes depositados em coleções científicas e na literatura taxonômica. Utilizamos modelos nulos para testar o viés de coleta quanto à proximidade das vias de acesso. Também testamos a influência do esforço amostral nas medidas de diversidade por meio de modelos de regressão. Para investigar o déficit Wallaceano, modelamos a distribuição geográfica de mais de 4.000 espécies e comparamos sua distribuição observada com modelos. Para quantificar o déficit hutchinsoniano, utilizamos a distância euclidiana ambiental dos registros para identificar regiões com condições ambientais pouco amostradas. Para estimar o déficit de Linne, medimos a similaridade da composição de espécies entre regiões próximas e distantes das vias de acesso. Resultados Demonstramos que apesar das diferenças no esforço amostral, o forte viés de coleta afeta igualmente todos os grupos taxonômicos, gerando um padrão de esforço amostral enviesado espacialmente. Esse padrão de coleta contribui muito para as deficiências de conhecimento da biodiversidade, o que afeta diretamente o conhecimento sobre os padrões de distribuição da diversidade.Principais conclusõesO conhecimento sobre riqueza de espécies, composição de espécies e endemismo na biodiversidade brasileira é fortemente enviesado espacialmente. Apesar das diferenças no esforço amostral para cada grupo taxonômico, o viés de beira de estrada os afetou igualmente. A similaridade da composição de espécies diminuiu com a distância das vias de acesso, sugerindo que levantamentos de coleta em locais distantes de estradas podem aumentar a probabilidade de amostragem de novos registros geográficos ou novas espécies.

Although Brazil is a megadiverse country and thus a conservation priority, no study has yet quantified conservation gaps in the Brazilian protected areas (PAs) using extensive empirical data. Here, we evaluate the degree of biodiversity protection and knowledge within all the Brazilian PAs through a gap analysis of vertebrate, arthropod and angiosperm occurrences and phylogenetic data. Our results show that the knowledge on biodiversity in most Brazilian PAs remain scant as 71% of PAs have less than 0.01 species records per km2. Almost 55% of Brazilian species and about 40% of evolutionary lineages are not found in PAs, while most species have less than 30% of their geographic distribution within PAs. Moreover, the current PA network fails to protect the majority of endemic species. Most importantly, these results are similar for all taxonomic groups analysed here. The methods and results of our countrywide assessment are suggested to help design further inventories in order to map and secure the key biodiversity of the Brazilian PAs. In addition, our study illustrates the most common biodiversity knowledge shortfalls in the tropics. Fil: Oliveira, Ubirajara. Universidade Federal de Minas Gerais; Brasil Fil: Soares-Filho, Britaldo Silveira. Universidade Federal de Minas Gerais; Brasil Fil: Paglia, Adriano Pereira. Universidade Federal de Minas Gerais; Brasil Fil: Brescovit, Antonio Domingos. Governo do Estado de Sao Paulo. Secretaria da Saude. Instituto Butantan; Brasil Fil: De Carvalho, Claudio J. B.. Universidade Federal do Paraná; Brasil Fil: Silva, Dasniel Paiva. Instituto Federal Goiano; Brasil Fil: Teixeira de Rezende, Daniella. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Parque Centenario. Museo Argentino de Ciencias Naturales “Bernardino Rivadavia”; Argentina Fil: Leite, Felipe Sá Fortes. Universidade Federal de Vicosa; Brasil Fil: Batista, João Aguiar Nogueira. Universidade Federal de Minas Gerais; Brasil Fil: Barbosa, João Paulo Peixoto Pena. Governo do Estado de Sao Paulo. Secretaria da Saude. Instituto Butantan; Brasil Fil: Stehmann, João Renato. Universidade Federal de Minas Gerais; Brasil Fil: Ascher, John S.. National University Of Singapore; Singapur Fil: De Vasconcelos, Marcelo Ferreira. Instituto Prístino; Brasil Fil: De Marco, Paulo. Universidade Federal de Goiás; Brasil Fil: Löwenberg-Neto, Peter. Universidade Federal da Integração Latino-Americana; Brasil Fil: Ferro, Viviane Gianluppi. Universidade Federal de Goiás; Brasil Fil: Santos, Adalberto J.. Universidade Federal de Minas Gerais; Brasil

Previous article in issueNext article in issue Fonseca and Venticinque (2018) (hereafter FV) present a critical assessment of a paper in which we attempt to estimate the biodiversity coverage of the Brazilian conservation units (Oliveira et al., 2017). We appreciate their contribution to this important debate. We have no doubts that conservation planning should be based on a variety of information sources, including not only the coverage of species? ranges but also the contribution of each area to the preservation of ecosystem services, landscape features and socioeconomic and cultural aspects. This systematic and integrative conservation planning is certainly a complex process, which requires the contribution of experts from different fields. However, we have shown, in this reply, that our paper (Oliveira et al., 2017) aims to quantify the knowledge and protection gaps of biodiversity in protected areas, not to propose priority areas or to test whether the current proposal of priority areas is efficient. Objectives and the conclusions of our paper. We hope this short response can clarify this debate. Fil: Oliveira, Ubirajara. Universidade Federal de Minas Gerais; Brasil Fil: Soares Filho, Britaldo Silveira. Universidade Federal de Minas Gerais; Brasil Fil: Paglia, Adriano Pereira. Universidade Federal de Minas Gerais; Brasil Fil: Brescovit, Antonio Domingos. Governo do Estado de Sao Paulo. Secretaria da Saude. Instituto Butantan; Brasil Fil: de Carvalho, Claudio J. B.. Universidade Federal do Paraná; Brasil Fil: Silva, Daniel Paiva. Instituto Federal Goiano; Brasil Fil: Teixeira de Rezende, Daniella. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Parque Centenario. Museo Argentino de Ciencias Naturales “Bernardino Rivadavia”; Argentina Fil: Leite, Felipe Sá Fortes. Universidade Federal de Viçosa; Brasil Fil: Batista, João Aguiar Nogueira. Universidade Federal de Minas Gerais; Brasil Fil: Barbosa, João Paulo Peixoto Pena. Governo do Estado de Sao Paulo. Secretaria da Saude. Instituto Butantan; Brasil Fil: Stehmann, João Renato. Universidade Federal de Minas Gerais; Brasil Fil: Ascher, John S.. National University Of Singapore; Singapur Fil: Vasconcelos, Marcelo Ferreira de. Instituto Prístino; Brasil Fil: De Marco, Paulo. Universidade Federal de Goiás; Brasil Fil: Löwenberg-Neto, Peter. Universidade Federal Da Integração Latino-americana; Brasil Fil: Ferro, Viviane Gianluppi. Universidade Federal de Goiás; Brasil Fil: Santos, Adalberto J.. Universidade Federal de Minas Gerais; Brasil

A promising antitumor xanthone derivative was optimized following a multidimensional approach that involved the synthesis of 17 analogues, the study of their lipophilicity and solubility, and the evaluation of their growth inhibitory activity on four human tumor cell lines. A new synthetic route for the hit xanthone derivative was also developed and applied for the synthesis of its analogues. Among the used cell lines, the HL-60 showed to be in general more sensitive to the compounds tested, with the most potent compound having a GI50 of 5.1 μM, lower than the hit compound. Lipophilicity was evaluated by the partition coefficient (K(p)) of a solute between buffer and two membrane models, namely liposomes and micelles. The compounds showed a logK(p) between 3 and 5 and the two membrane models showed a good correlation (r(2)=0.916) between each other. Studies concerning relationship between solubility and structure were developed for the hit compound and 5 of its analogues.

Our previous work has described a library of thioxanthones designed to have dual activity as P-glycoprotein modulators and antitumor agents. Some of these compounds had shown a significant cell growth inhibitory activity towards leukemia cell lines, without affecting the growth of non-tumor human fibroblasts. However, their effect in cell lines derived from solid tumors has not been previously studied. The present work aimed at: (i) screening this small series of compounds from an in-house library, for their in vitro cell growth inhibitory activity in human tumor cell lines derived from solid tumors; and (ii) initiate a study of the effect of the most potent compound on apoptosis. The tumor cell growth inhibitory effect of 27 compounds was first analysed in different human tumor cell lines, allowing the identification of a hit compound, TXA1. Its hydrochloride salt TXA1 HCl was then synthesized, to improve solubility and bioavailability. Both TXA1 and TXA1 HCl inhibited the growth of MCF-7, NCI-H460, A375-C5, HeLa, 786-O, Caki-2 and AGS cell lines. The effect of TXA1 HCl in MCF-7 cells was found to be irreversible and was associated, at least in part, with an increase in cellular apoptosis. IPATIMUP integrates the i3S Research Unit, which is partially supported by FCT, the Portuguese Foundation for Science and Technology. This work is funded by FEDER funds through the Operational Programme for Competitiveness Factors-COMPETE and National Funds through the FCT-Foundation for Science and Technology, under the projects FEDER COMPETE FCOMP-01-0124-FEDER-015752, FCOMP-01-0124-FEDER-011057, NORTE-07-0162-FEDER-00018—“Contributos para o reforço da capacidade do IPATIMUP enquanto actor do sistema regional de inovação” and NORTE-07-0162-FEDER-000067—“Reforço e consolidação da capacidade infraestrutural do IPATIMUP para o sistema regional de inovação”, both supported by Programa Operacional Regional do Norte (ON.2—O Novo Norte), through FEDER funds under the Quadro de Referência Estratégico Nacional (QREN). This research was partially supported by the Strategic Funding UID/Multi/04423/2013 through national funds provided by FCT—Foundation for Science and Technology and European Regional Development Fund (ERDF), in the framework of the programme PT2020. The authors also thank FCT for the grant of R.T. Lima (SFRH/BPD/68787/2010) and QREN for the grant of D. Sousa (NORTE-07-0124-FEDER-000023).

Com aproximadamente 800 espécies descritas, Chelodesmidae constitui a segunda maior família em Polydesmida; seus membros ocorrem na América do Sul (subfamília Chelodesminae) e oeste Africano (subfamília Prepodesminae). Hoffman, ao examinar e ilustrar inúmeros caracteres em seu extensivo trabalho com a família, propôs numerosas tribos, a maioria em Chelodesminae. Empregando o uso de caracteres morfológicos, a monofilia e a relação de 18, das 19 tribos de Chelodesminae, são testadas. Duas matrizes de dados contendo 68 terminais e 70 caracteres e 68 terminais e 65 caracteres foram construídas. Para as análises, foi utilizada pesagem implícita de caracteres am ambas as matrizes de caracteres com valores de concavidade igual a 10,23926 e 15,136, resultando em uma árvore cada. A primeira de 411 passos (IC=21; IR=66) e a segunda de 401 passos (IC=22; IR=65). No atual conjunto de dados, a maioria das tribos propostas é monofilética; exceções são Batodesmini, Leptodesmini, Macrocoxodesmini, Strongylomorphini e Telonychopodini. A tribo monoespecífica Gonorygmatini surge interna a Telonychopodini. A polifilia de Macrocoxodesmini é confirmada. Ambas as árvores de pesagem implícita mostram Chelodesminae monofilética. Assim, a subfamília é composta por, além dos grupos parafiléticos e polifiléticos, pelas tribos monofiléticas: Arthrosolaenomeridini, Caraibodesmini, Chelodesmini, Chondrodesmini, Cornalatini, Dibolostethini, Gonorygmatini, Lepturodesmini, Platinodesmini, Priodesmini, Trichomorphini e Trachelodesmini. Todas são restritas à América do Sul e América Central, bem como as ilhas do Caribe With close to 800 described species, the Chelodesmidae constitute the second largest family in Polydesmida; its members occurring in South America (subfamily Chelodesminae) and western Africa (subfamily Prepodesminae). Hoffman, examining and illustrating numerous characters in his extensive work on the family, proposed numerous tribes, mainly in the Chelodesminae. Employing morphological characters, the monophyly and the interelationship of the 18 chelodesmine tribes are tested. Two data matrixes were built, one with 68 terminals and 70, and another with 68 terminals and 65 characters. For the analysis, implied weighting was used in both data matrixes with k values as 10,23926 and 15,136, resulting in one tree each. The first with 411 steps (CI=21; RI=66) and the second with 401 steps (CI=22; RI=65). In this dataset, the majority of tribes are monophyletic; exceptions are Batodesmini, Leptodesmini, Macrocoxodesmini, Strongylomorphini e Telonychopodini. The mono-specific tribe Gonorygmatini appears internally to Telonychopodini. The polyphyly of Macrocoxodesmini is confirmed. Both implied weighting trees shows Chelodesminae as monophyletic. This way, the subfamily is composed by, despite the paraphyletic and polyphyletic groups, for the monophyletic tribes: Arthrosolaenomeridini, Caraibodesmini, Chelodesmini, Chondrodesmini, Cornalatini, Dibolostethini, Gonorygmatini, Lepturodesmini, Platinodesmini, Priodesmini, Trichomorphini e Trachelodesmini. All tribes are restrict to South and Central Americas, as well to Caribbean Islands

The benzopyran and dihydrobenzopyran moieties can be considered as "privileged motifs" in drug discovery being good platforms for the search of new bioactive compounds. These moieties are commonly found fused to the xanthonic scaffold belonging to the biologically important family of the generally designated prenylated xanthones. Several pyranoxanthones have shown promising antitumor activity and since most of them are from natural origin, the biosynthetic pathway only allows a particular pattern of substitution which limits their structural diversity and renders any broad structure-activity study hard to be established. Accordingly, with the aim of rationalizing the importance of the fused ring orientation and oxygenation pattern in pyranoxanthones, this study describes the synthesis of 14 new pyranoxanthones and evaluation of their cell growth inhibitory activity in four human tumor cell lines as well as their lipophilicity in two membrane models. This systematic approach allowed establishing structure-activity and structure-lipophilicity relationships for the obtained compounds in combination with 6 previously described compounds. From this work an angular pyranoxanthone scaffold emerged as particularly promising, presenting a potent cell growth inhibitory activity and suitable drug-like lipophilicity.

Uma análise cladística baseada em parcimônia é utilizada para testar o monofiletismo do gênero Odontopeltis e suas relações com outras espécies de gêneros anteriormente relacionados. A matriz de dados compreende 15 terminais e 47 caracteres. A análise cladística com pesagem implícita de caracteres de concavidade igual a 2,012 resultou em uma árvore mais parcimoniosa com 99 passos (IC = 58; IR = 73). As seguintes sinapomorfias sustentam o clado Odontopeltis e são propostas como diagnoses para o gênero: (1) Formato do órgão de Tömösvary sub-oval; (2) borda do ozóporo simples; (3) dobras retrolaterais no acropódito; e (4) presença de um par de macro-cerdas delimitando o fim da região pré-femoral e o início da região femoral, no gonopódio. Para padronização das descrições de genitália, foi analisada toda a terminologia do gonopódio dos machos da família Chelodesmidae. O gonopódio dos machos é, então, formado por peças cujas homologias às peças das pernas é incerta: coxa, cânula, região pré-femoral, processo pré-femoral, região femoral e solenômero. Para o gênero Odontopeltis é proposta uma terminologia da genitália à parte, devido às modificações no gonopódio. O gênero é composto por 13 espécies, sendo oito espécies válidas e cinco insertis sedis, sendo elas: Odontopeltis conspersus, O. anchisteus, O. clarazianus, O. giganteus, O. sp. nov. 1, O. sp. nov. 2, O. sp. nov. 3 e O. sp. nov. 4, e as espécies insertis sedis são: O. próxima, O. gracilipes, O. decoloratus, O. borellii e O. balzanii. A tribo Macrocoxodesmini se mostrou parafilética e, portanto, foi desmembrada. A tribo Telonychopodini se manteve monofilética e o gênero Odontopeltis de fato não pertence a esta tribo. A cladistic analysis based on parsimony is used to test the monophyly of the genus Odontopeltis and its relationship with related genera. The data matrix comprises 15 terminal taxa and 47 characters. The implied weighted analysis, with concavity 2,012, resulted in a 99 steps most parsimonious tree (CI = 58; RI = 73). The following sinapomorphies supports the clade Odontopeltis and are proposed as diagnosis characters for the genus: (1) Tömösvary organ sub-oval shaped; (2) ozopores edge simple; (3) retrolateral rims on acropodite; and (4) presence of macrobristles delimiting the end of the prefemoral region and the beginning of the femoral region, on the gonopods. To standardize the genitalia description, the terminology for the gonopods of the family Chelodesmidae was reviewed. Then, the male gonopods are composed by: coxae, cannula, prefemoral region, prefemoral process, femoral region and solenomere. There is no attempt to relate the homology of legs pieces with gonopod pieces. It\'s proposed a terminology for the gonopods of the genus Odontopeltis due to the modifications on the gonopods. The genus comprises 13 species, where eight are valid species and five are insertis sedis: Odontopeltis conspersus, O. anchisteus, O. clarazianus, O. giganteus, O. sp. nov. 1, O. sp. nov. 2, O. sp. nov. 3 and O. sp. nov. 4, and the insertis sedis species are: O. proxima, O. gracilipes, O. decoloratus, O. borellii and O. balzanii. The Macrocoxodesmini tribe showed as a paraphyletic group and, therefore, was dissolved. The Telonychopodini tribe is monophyletic and the genus Odontopeltis, indeed, do not belong to this tribe.

(1) Background: Our previous studies unveiled the hit thioxanthone TXA1 as an inhibitor of,P-glycoprotein (drug efflux pump) and of human tumor cells growth, namely of melanoma cells. SinceTXA1 is structurally similar to lucanthone (an autophagy inhibitor and apoptosis inducer) and to N10-substituted phenoxazines (isosteres of thioxanthones, and autophagy inducers), this study aimed at further assessing its cytotoxic mechanism and evaluating its potential as an autophagy modulator in A375-C5 melanoma cells; (2) Methods: Flow cytometry with propidium iodide (PI) for cell cycle profile analysis; Terminal deoxynucleotidyl transferase dUTP nick end labeling (TUNEL) assay, flow cytometry with Annexin V/PI labeling and Western blot for apoptosis analysis were conducted. A pharmacophore approach was used for mapping TXA1 onto pharmacophores for autophagy induction. Autophagy analyses included transmission electron microscopy for visualization of autophagic structures, fluorescence microscopy for observation of monodansylcadaverine (MDC) staining, pattern of LC3 expression in the cells and acridine orange staining, and Western blot for autophagic proteins expression; (3) Results: TXA1 induced autophagy of melanoma cells at the GI50 concentration (3.6 μM) and apoptosis at twice that concentration. Following treatment with TXA1, autophagic structures were observed, together with the accumulation of autophagosomes and the formation of autophagolysosomes. An increase in LC3-II levels was also observed, which was reverted by 3-methyladenine (3-MA) (an early stage autophagy-inhibitor) but further increased by E-64d/pepstatin (late-stage autophagy inhibitors). Finally, 3-MA also reverted the effect of TXA1 in cellular viability; (4) Conclusion: TXA1 decreases the viability of melanoma cells by modulation of autophagy and may, therefore, serve as a lead compound for the development of autophagy modulators with antitumor activity. This work was financed by FEDER—Fundo Europeu de Desenvolvimento Regional funds through the COMPETE 2020—Operacional Programme for Competitiveness and Internationalisation (POCI), Portugal 2020, and by Portuguese funds through FCT—Fundação para a Ciência e a Tecnologia/ Ministério da Ciência, Tecnologia e Inovação in the framework of the project “Institute for Research and Innovation in Health Sciences (POCI-01-0145-FEDER-007274)”. The work was also funded by ERDF, COMPETE, and FCT under the projects PTDC/SAU-OSM/101437/2008, PTDC/MAR-BIO/4694/2014, and INNOVMAR—reference NORTE-01-0145-FEDER-000035, Research Line NOVELMAR. The authors also thank: FCT for D. Sousa and R.T. Lima grants (PTDC/SAU-FCT/100930/2008 and SFRH/BPD/68787/2010, respectively), QREN for D. Sousa grant (NORTE-07-0124-FEDER-000023).