The antimicrobial activity of lapachol and its thiosemicarbazone and semicarbazone derivatives

Lapachol was chemically modified to obtain its thiosemicarbazone and semicarbazone derivatives. These compounds were tested for antimicrobial activity against several bacteria and fungi by the broth microdilution method. The thiosemicarbazone and semicarbazone derivatives of lapachol exhibited antimicrobial activity against the bacteria Enterococcus faecalis and Staphylococcus aureus with minimal inhibitory concentrations (MICs) of 0.05 and 0.10 µmol/mL, respectively. The thiosemicarbazone and semicarbazone derivatives were also active against the pathogenic yeast Cryptococcus gattii (MICs of 0.10 and 0.20 µmol/mL, respectively). In addition, the lapachol thiosemicarbazone derivative was active against 11 clinical isolates of Paracoccidioides brasiliensis, with MICs ranging from 0.01-0.10 µmol/mL. The lapachol-derived thiosemicarbazone was not cytotoxic to normal cells at the concentrations that were active against fungi and bacteria. We synthesised, for the first time, thiosemicarbazone and semicarbazone derivatives of lapachol. The MICs for the lapachol-derived thiosemicarbazone against S. aureus, E. faecalis, C. gattii and several isolates of P. brasiliensis indicated that this compound has the potential to be developed into novel drugs to treat infections caused these microbes.     

Species richness,endemism and conservation of Mexican gymnosperms

An analysis of the distribution patterns of 124 Mexican gymnosperm species was undertaken, in order to detect the Mexican areas with high species richness and endemism, and with this information to propose areas for conservation. Our study includes an analysis of species richness, endemism and distributional patterns of Mexican species of gymnosperms based on three different area units (states, biogeographic provinces and grid-cells of 1° × 1° latitude/longitude). The richest areas in species and endemism do not coincide; in this way, the Sierra Madre Oriental province, the state of Veracruz and a grid-cell located in the state of Oaxaca were the areas with the highest number of species, whereas the Golfo de México province, the state of Chiapas and a grid-cell located in this state were the richest areas in endemic species. A weighted endemism and corrected weighted endemism indices were calculated, and those grid-cells with high values in both indices and with high species richness were considered as hotspots; these grid-cells are mainly located in Southern and Central Mexico.     

Track analysis and conservation priorities in the cloud forests of Hidalgo,Mexico

Abstract . A track analysis based on the distributional patterns of 967 species of vascular plant taxa (gymnosperms, angiosperms and pteridophytes) was performed to assess conservation priorities for cloud forests in the state of Hidalgo, Mexico, ranged in the municipalities of Chapulhuacán, Eloxochitlán, Molocotlán, Pisaflores, Tenango de Doria, Tlahuelompa and Tlanchinol, as well as five floristically equivalent areas in the states of Veracruz (Teocelo and Helechales), Tamaulipas (Gómez Farías), Morelos‐México (Ocuilan) and Oaxaca (Huautla de Jiménez). In order to detect generalized tracks we employed a new parsimony method, where clades (considered equivalent to generalized tracks) are defined forbidding homoplasy and acting like a compatibility algorithm. Several generalized tracks were found connecting these areas. Cloud forests of Chapulhuacán were connected according to three different generalized tracks and thus have a higher value, qualifying as a priority area for the conservation of cloud forests in the state of Hidalgo.     

Environmental assessment of multi-functional building elements constructed with digital fabrication techniques

Purpose

Digital fabrication is revolutionizing architecture, enabling the construction of complex and multi-functional building elements. Multi-functionality is often achieved through material reduction strategies such as functional or material hybridization. However, these design strategies may increase environmental impacts over the life cycle. The integration of functions may hinder the maintenance and shorten the service life. Moreover, once a building element has reached the end of life, hybrid materials may influence negatively its recycling capacity. Consequently, the aim of this paper is to analyze the influence of multi-functionality in the environmental performance of two digitally fabricated architectural elements: The Sequential Roof and Concrete-Sandstone Composite Slab and to compare them with existing standard elements.

Methods

A method based on the life-cycle assessment (LCA) framework is applied for the evaluation of the environmental implications of multi-functionality in digital fabrication. The evaluation consists of the comparison of embodied impacts between a multi-functional building element constructed with digital fabrication techniques and a conventional one, both with the same building functions. Specifically, the method considers the lifetime uncertainty caused by multi-functionality by considering two alternative service life scenarios during the evaluation of the digitally fabricated building element. The study is extended with a sensitivity analysis to evaluate the additional environmental implications during end-of-life processing derived from the use of hybrid materials to achieve multi-functionality in architecture.

Results and discussion

The evaluation of two case studies of digitally fabricated architecture indicates that their environmental impacts are very sensitive to the duration of their service life. Considering production and life span phases, multi-functional building elements should have a minimum service life of 30 years to bring environmental benefits over conventional construction. Furthermore, the case study of Concrete-Sandstone Composite Slab shows that using hybrid materials to achieve multi-functionality carries important environmental consequences at the end of life, such as the emission of air pollutants during recycling.

Conclusions

The results from the case studies allow the identification of key environmental criteria to consider during the design of digitally fabricated building elements. Multi-functionality provides material efficiency during production, but design adaptability must be a priority to avoid a decrease in their environmental performance. Moreover, the high environmental impacts caused by end-of-life processing should be compensated during design.

     

2-Benzoylpyridine-N(4)-tolyl thiosemicarbazones and their palladium(II) complexes: Cytotoxicity against leukemia cells

The palladium(II) complexes [Pd(2Bz4oT)Cl], [Pd(2Bz4mT)Cl], and [Pd(2Bz4pT)Cl] were prepared with N(4)-ortho- (H2Bz4oT) N(4)-meta- (H2Bz4mT) and N(4)-para- (H2Bz4pT) tolyl-thiosemicarbazones derived from 2-benzoylpyridine. The free thiosemicarbazones proved to be highly cytotoxic against Jurkat, HL60 and the resistant HL60.Bcl-X_L leukemia cell lines at nanomolar concentrations, but were much less cytotoxic to HepG2 human hepatoma cells. Upon coordination to palladium(II) the cytotoxic activity against all studied cell lines decreases. However, the high cytotoxicity of the free thiosemicarbazones against leukemia, together with their hepatotoxic profile similar to that of cisplatin suggest that N(4)-tolyl thiosemicarbazones have potential as chemotherapeutic drug candidates.     

Caterpillars of Eumaeus childrenae (Lepidoptera: Lycaenidae) feeding on two species of cycads (Zamiaceae) in the Huasteca region, Mexico

There are few genera of butterflies that feed on cycads. Among them the genus Eumaeus (Lycaenidae) presents aposematic coloration in all its life stages. In this work we report for the first time the herbivory of young leaflets of Ceratozamia mexicana and Zamia fischeri (Zamiaceae) by caterpillars of E. childrenae in their natural habitat in the Huasteca region, Mexico.     

An angiotensin I-converting enzyme mutation (Y465D) causes a dramatic increase in blood ACE via accelerated ACE shedding

Background

Angiotensin I-converting enzyme (ACE) metabolizes a range of peptidic substrates and plays a key role in blood pressure regulation and vascular remodeling. Thus, elevated ACE levels may be associated with an increased risk for different cardiovascular or respiratory diseases. Previously, a striking familial elevation in blood ACE was explained by mutations in the ACE juxtamembrane region that enhanced the cleavage-secretion process. Recently, we found a family whose affected members had a 6-fold increase in blood ACE and a Tyr465Asp (Y465D) substitution, distal to the stalk region, in the N domain of ACE.

Methodology/Principal Findings

HEK and CHO cells expressing mutant (Tyr465Asp) ACE demonstrate a 3- and 8-fold increase, respectively, in the rate of ACE shedding compared to wild-type ACE. Conformational fingerprinting of mutant ACE demonstrated dramatic changes in ACE conformation in several different epitopes of ACE. Cell ELISA carried out on CHO-ACE cells also demonstrated significant changes in local ACE conformation, particularly proximal to the stalk region. However, the cleavage site of the mutant ACE - between Arg1203 and Ser1204 - was the same as that of WT ACE. The Y465D substitution is localized in the interface of the N-domain dimer (from the crystal structure) and abolishes a hydrogen bond between Tyr465 in one monomer and Asp462 in another.

Conclusions/Significance

The Y465D substitution results in dramatic increase in the rate of ACE shedding and is associated with significant local conformational changes in ACE. These changes could result in increased ACE dimerization and accessibility of the stalk region or the entire sACE, thus increasing the rate of cleavage by the putative ACE secretase (sheddase).     

Current knowledge of fungi from Neotropical montane cloud forests: distributional patterns and composition

Montane cloud forests in the Neotropics harbor a great wealth of biological diversity and a large number of endemic species. Here, we present (i) a comprehensive data mining exercise of fungi from Neotropical montane cloud forests (NMCF), (ii) an extensive review of the current knowledge of fungal richness, distribution and composition, and (iii) a preliminary analysis of fungal endemicity in Mexican montane cloud forests. Based on a survey of literature and other sources, we assembled a database of 6349 records representing 2962 fungal species in NMCF. The computed individual-based species rarefaction curve remained non-asymptotic, and the extrapolation curve estimated an expected increment of 42% in the number of species by doubling the sampling effort. Fungal species richness was highest in NMCF from Mesoamerica, particularly from Mexico and Costa Rica. Fungi from Mesoamerica, Caribbean and South America are significantly different at diverse taxonomic levels, and there is a little overlap in the fungal species recorded from these regions. The analyses of endemicity of the Mexican dataset performed with parsimony and Bayesian methods were highly complementary. They showed the following areas of endemicity supported by the congruent distribution of fungal species: (i) two main regions in the Trans-Mexican Volcanic Belt (TMVB); (ii) a region in the southern part of Veracruz; and (iii) a region located in the eastern part of TMVB with affinities with Sierra Madre Oriental and the Chiapan-Guatemala Highlands. This last area was supported by five species of Glomeromycota and is consistent with an area of endemicity previously found in vascular plants. In this study, we provide a perspective on gaps in knowledge regarding the diversity and distribution of fungi in NMCF, and provide a full dataset of fungal records with geographical, bibliographic and taxonomic information.     

Phylogenetic Composition of Angiosperm Diversity in the Cloud Forests of Mexico

Several members of the most ancient living lineages of flowering plants (angiosperms) inhabit humid, woody, mostly tropical habitats. Here we assess whether one of these forest types, the cloud forests of Mexico (CFM), contain a relatively higher proportion of phylogenetically early-diverging angiosperm lineages. The CFM houses an extraordinary plant species diversity, including members of earliest-diverging angiosperm lineages. The phylogenetic composition of CFM angiosperm diversity was evaluated through the relative representation of orders and families with respect to the global flora, and the predominance of phylogenetically early- or late-diverging lineages. Goodness-of-fit tests indicated significant differences in the proportional local and global representation of angiosperm clades. The net difference between the percentage represented by each order and family in the CFM and the global flora allowed identification of clades that are overrepresented and underrepresented in the CFM. Early-diverging angiosperm orders and families were found to be neither over- nor underrepresented in the CFM. A slight predominance of late-diverging phylogenetic levels among overrepresented clades, however, was encountered in the CFM. The resulting pattern suggests that cloud forests provide habitats where the most ancient angiosperm lineages have survived in the face of accumulating species diversity belonging to phylogenetically late-diverging lineages.     

Biogeography, current knowledge and conservation of threatened vascular plants characteristic of Mexican temperate forests

The main goal of this study is to document the biogeographical patterns, current status and conservation of 24 species of vascular plants in Mexico, all of them recorded in some risk category in the Mexican official publication named ‘Norma Oficial Mexicana 059’ (NOM-059) and some of them in the IUCN red lists (the World Conservation Union) and CITES (Convention on International Trade in Endangered Species); many of these species are linked to Mexican cloud forests and other temperate vegetation types. Distribution maps of these 24 species were generated with information obtained from specialized literature, herbarium specimens, institutional databases, and field work; with this information, the patterns of richness and endemism of these species were obtained. For this, the Mexican territory was divided using a grid system based on a chart index (scale 1:50,000 system composed by grids of 15' × 20'). Also, we up to date the knowledge of these species and their populations and current habitats, and evaluate their geographic distribution in relation to the current Mexican National Parks and Reserves System and Mexican Priority Regions for Conservation. We also discuss some changes of categories in the NOM-059 and suggest the urgent incorporation of some of the species in the recent IUCN Red Data List of Threatened Species (2003). Most of the species studied require special policies for their conservation due to problems that affect their natural populations; also we consider that these taxa are underrepresented in the current Mexican System of Natural Protected Areas, especially those with restricted distributions.