Bioactivity of the Andean aromatic plants Aloysia citriodora and Bursera graveolens essential oils against the blowfly Calliphora vomitoria

Tropical Andes is a biodiversity hot spot rich in aromatic plant species, whose potential as a source of active compounds for insect pests’ control is still largely underexploited. Here, the Essential Oils (EOs) extracted from two Ecuadorian plants, the shrub Aloysia citriodora (Verbenaceae) and the tree Bursera graveolens (Burseraceae), were chemically analysed and tested for their bioactivity against the blue blowfly Calliphora vomitoria (Linnaeus, 1758) (Diptera: Calliphoridae). This fly is a vector of pathogenic microorganisms, dangerous in factories and stores where fresh meat is processed, stored, and sold. The main components of the A. citriodora EO are geranial and limonene, while in the B. graveolens EO they are limonene and α-terpineol. The effects of the two EOs were evaluated against C. vomitoria by a behavioural assay in a two-choice olfactometer (concentrations range 0.07-2.8 μL L-1 air). Besides, the insecticidal properties of the two EOs were tested by fumigation (EOs concentrations from 6.06 to 36.36 μL L-1 air), by contact with topical applications using a Burkard micro dispenser (EOs dose from 0.10 to 0.60 μl EO/fly), and by ingestion of a mucilage containing EOs (from 15 to 75 μl EO mL-1 mucilage), sucrose, and agarose. Furthermore, the ovicidal activity was assessed (concentrations from 0.006 to 0.075 μL EO cm-2 of filter paper). The results of the behavioural assay showed a stronger repellent effect exerted by the A. citriodora EO, while all the toxicity tests revealed dose-dependent mortality of the blowflies and eggs

Responses from olfactory sensilla of Sitophilus zeamais to Andean essential oils.

Lamiaceae species are well-known in traditional medicine. In the last years, Essential Oils (EOs) of many Lamiaceae have showed to be excellent repellents and/or insecticides. Tropical Andes are extremely rich in endemic flora, possible source of new bioactive substances. Here, we verified the insect repellent activity of the EOs extracted from Clinopodium tomentosum and C. nubigenum, two Lamiaceae typical of the Ecuadorian Andes. The two EOs were tested against the maize weevil Sitophilus zeamais (Motschulsky) (Coleoptera: Curculionidae), one of the most destructive pests of stored and processed cereals. To characterize the olfactory sensilla of S. zeamais, its antennal structure was investigated by scanning and transmission electron microscopy. The electrophysiological and behavioural responses of the insect to the EOs were then investigated by electroantennography and olfactometer trials. The morphological study revealed the presence of three types of sensilla (Basiconic Sensillum 1, 2, and Grooved Peg Sensillum), that could be involved in the perception of the EOs volatile compounds. Accordingly, the electroantennography showed a positive dose-dependent response of the insect antennae to both the EOs. The behavioural tests displayed a significative repellence of the EOs, starting from 8.4 μL L-1 air, and that the efficacy and readiness of the response to the stimulus was higher for C. tomentosum. In conclusion, both the EOs are detected by the insect by its antennae and exert a strong repellent effect. The results confirm that Andean flora represents a valuable source of unexploited bioactive substances that can be utilized as promising tools for foodstuff pests’ control

Quantitative Systems Pharmacology and Biased Agonism at Opioid Receptors: A Potential Avenue for Improved Analgesics

Chronic pain is debilitating and represents a significant burden in terms of personal and socio-economic costs. Although opioid analgesics are widely used in chronic pain treatment, many patients report inadequate pain relief or relevant adverse effects, highlighting the need to develop analgesics with improved efficacy/safety. Multiple evidence suggests that G protein-dependent signaling triggers opioid-induced antinociception, whereas arrestin-mediated pathways are credited with modulating different opioid adverse effects, thus spurring extensive research for G protein-biased opioid agonists as analgesic candidates with improved pharmacology. Despite the increasing expectations of functional selectivity, translating G protein-biased opioid agonists into improved therapeutics is far from being fully achieved, due to the complex, multidimensional pharmacology of opioid receptors. The multifaceted network of signaling events and molecular processes underlying therapeutic and adverse effects induced by opioids is more complex than the mere dichotomy between G protein and arrestin and requires more comprehensive, integrated, network-centric approaches to be fully dissected. Quantitative Systems Pharmacology (QSP) models employing multidimensional assays associated with computational tools able to analyze large datasets may provide an intriguing approach to go beyond the greater complexity of opioid receptor pharmacology and the current limitations entailing the development of biased opioid agonists as improved analgesics

Differential effects on membrane permeability and viability of human keratinocyte cells undergoing very low intensity megasonic fields

Among different therapeutic applications of Ultrasound (US), transient membrane sonoporation (SP) - a temporary, non-lethal porosity, mechanically induced in cell membranes through US exposure - represents a compelling opportunity towards an efficient and safe drug delivery. Nevertheless, progresses in this field have been limited by an insufficient understanding of the potential cytotoxic effects of US related to the failure of the cellular repair and to the possible activation of inflammatory pathway. In this framework we studied the in vitro effects of very low-intensity US on a human keratinocyte cell line, which represents an ideal model system of skin protective barrier cells which are the first to be involved during medical US treatments. Bioeffects linked to US application at 1 MHz varying the exposure parameters were investigated by fluorescence microscopy and fluorescence activated cell sorting. Our results indicate that keratinocytes undergoing low US doses can uptake drug model molecules with size and efficiency which depend on exposure parameters. According to sub-cavitation SP models, we have identified the range of doses triggering transient membrane SP, actually with negligible biological damage. By increasing US doses we observed a reduced cells viability and an inflammatory gene overexpression enlightening novel healthy relevant strategies

Correlated Component Analysis for diffuse component separation with error estimation on simulated Planck polarization data

We present a data analysis pipeline for CMB polarization experiments, running from multi-frequency maps to the power spectra. We focus mainly on component separation and, for the first time, we work out the covariance matrix accounting for errors associated to the separation itself. This allows us to propagate such errors and evaluate their contributions to the uncertainties on the final products.The pipeline is optimized for intermediate and small scales, but could be easily extended to lower multipoles. We exploit realistic simulations of the sky, tailored for the Planck mission. The component separation is achieved by exploiting the Correlated Component Analysis in the harmonic domain, that we demonstrate to be superior to the real-space application (Bonaldi et al. 2006). We present two techniques to estimate the uncertainties on the spectral parameters of the separated components. The component separation errors are then propagated by means of Monte Carlo simulations to obtain the corresponding contributions to uncertainties on the component maps and on the CMB power spectra. For the Planck polarization case they are found to be subdominant compared to noise.Comment: 17 pages, accepted in MNRA

Ultrasound delivery of Surface Enhanced InfraRed Absorption active gold-nanoprobes into fibroblast cells: a biological study via Synchrotron-based InfraRed microanalysis at single cell level

Ultrasound (US) induced transient membrane permeabilisation has emerged as a hugely promising tool for the delivery of exogenous vectors through the cytoplasmic membrane, paving the way to the design of novel anticancer strategies by targeting functional nanomaterials to specific biological sites. An essential step towards this end is the detailed recognition of suitably marked nanoparticles in sonoporated cells and the investigation of the potential related biological effects. By taking advantage of Synchrotron Radiation fourier transform infrared micro-spectroscopy (SR-microftiR) in providing highly sensitive analysis at the single cell level, we studied the internalisation of a nanoprobe within fibroblasts (NIH-3T3) promoted by low-intensity US. To this aim we employed 20 nm gold nanoparticles conjugated with the IR marker 4-aminothiophenol. The significant Surface Enhanced Infrared Absorption provided by the nanoprobes, with an absorbance increase up to two orders of magnitude, allowed us to efficiently recognise their inclusion within cells. Notably, the selective and stable SR- microftiR detection from single cells that have internalised the nanoprobe exhibited clear changes in both shape and intensity of the spectral profile, highlighting the occurrence of biological effects. Flow cytometry, immunofluorescence and murine cytokinesis-block micronucleus assays confirmed the presence of slight but significant cytotoxic and genotoxic events associated with the US-nanoprobe combined treatments. our results can provide novel hints towards US and nanomedicine combined strategies for cell spectral imaging as well as drug delivery-based therapies

Opioid activity profiles of oversimplified peptides lacking in the protonable N-terminus

Recently, we described cyclopeptide opioid agonists containing the D-Trp-Phe sequence. To expand the scope of this atypical pharmacophore, we tested the activity profiles of the linear peptides Ac-Xaa-Phe-Yaa (Xaa = L/D-Trp, D-His/Lys/Arg; Yaa = H, GlyNH2). Ac-D-Trp-PheNH2 appeared to be the minimal binding sequence, while Ac-D-Trp-Phe-GlyNH 2 emerged as the first noncationizable short peptide (partial) agonist with high \u3bc-opioid receptor affinity and selectivity. Conformational analysis suggested that 5 adopts in solution a \u3b2-turn conformation. \ua9 2012 American Chemical Society

Assessment of the Life Cycle Environmental Impact of the Olive Oil Extraction Solid Wastes in the European Union

There is an increasing interest in developing sustainable systems in the European Union (EU) to recover and upgrade the solid wastes of the olive oil extraction process, i.e. wet husk. A Life Cycle Environmental Impact Assessment (LCIA) of wet husk has been carried out aiming at facilitating an appropriate Life Cycle Management of this biomass. Three scenarios have been considered, i.e. combustion for domestic heat, generation of electric power, and composting. The Environmental Product Declaration and the ReCiPe method were used for Life Cycle Impact Assessment. Domestic heating and power generation were the most important impact factors in damaging human health, ecosystems, and natural resources depletion. Composting was 2-4 orders of magnitude less impacting than domestic heat and power generation. Considering human health, the impact of climate change, human toxicity and particulate matter formation represented the main impact categories. Considering ecosystems, climate change and natural land transformation were the main impact categories. Within natural resources, fossil fuel depletion was impacted three orders more than metal depletion. Within domestic heating and power generation scenarios, storage of wet husk along with the extraction by organic solvent, and the waste treatment were the most impacting phases for global warming potential, ozone layer depletion, acidification and non renewable fossil resources depletion. The results obtained for the waste disposal have been comparatively assessed with respect to the environmental impact of the olive oil production chain

Essential oils against Varroa destructor: a soft way to fight the parasitic mite of Apis mellifera

Essential oils (EOs) extracted from the aromatic plants Artemisia annua, Artemisia verlotiorum, Cinnamomum verum, and Citrus reticulata were investigated as repellents against the honey bees parasitic mite Varroa destructor. In laboratory tests, all EOs except C. reticulata exerted significant repellent activity against the mite after 24 h exposure. C. verumwas the most effective EO against V. destructor (median effective concentration EC50 =1.30 μL L−1), and the least toxic against honey bees (EC50 = 13.29 μL L−1). Because of its high selectivity ratio (A. mellifera LD50/V. destructor EC50 = 10.22), C. verum EO was then tested to control varroosis in colonies in field trials. The results of open field tests confirmed the efficacy observed in the laboratory. After one week of treatment, colonies treated with the EO showed a significant reduction of V. destructor infestation (about 65% at the dose of 25.0 μL L−1) and no negative effects on A. mellifera. Overall, our experiment indicated that C. verum EO could be used to effectively control varroosis in the hive with no side effects on the bee colonies

Liquid hydridosilane precursor prepared from cyclopentasilane via sonication at low temperatures without the action of light

AbstractWe report on a liquid hydridosilane precursor ink prepared via the ultrasonically induced ring-opening polymerisation of cyclopentasilane (Si5H10) without irradiation by ultraviolet light. The sonication is carried out in N2 atmosphere at temperatures between 20 and 75°C. We use size exclusion chromatography (SEC) to show polymer growth and estimate molecular mass with increasing sonication time. In combination with UV–vis transmission measurements, further SEC analysis is used to compare solutions subjected to either purely thermal or ultrasonic treatment at the same process temperature and for the same duration. Our findings provide strong evidence showing that the initiation of the polymerisation is sonocatalytic in nature and not thermic due to the macroscopic temperature of the solution. The liquid precursor is used to produce homogeneous hydrogenated amorphous silicon (a-Si:H) thin films via spin coating and pyrolytic conversion. The optoelectronic properties of the films are subsequently improved by hydrogen radical treatment. Fourier transform infrared spectroscopy (FTIR) is used to determine a compact film morphology and electrical conductivity measurements show that the layers attain a light-to-dark photosensitivity ratio of 2×103 making them suitable for application in optoelectronic devices