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Long-range (LoRa) communication has attracted much attention recently due to its utility for many Internet of Things applications. However, one of the key problems of LoRa technology is that it is vulnerable to noise/interference due to the use of only up-chirp signals during modulation. In this paper, to solve this problem, unlike the conventional LoRa modulation scheme, we propose a modulation scheme for LoRa communication based on joint up- and down-chirps. A fast Fourier transform (FFT)-based demodulation scheme is devised to detect modulated symbols. To further improve the demodulation performance, a hybrid demodulation scheme, comprised of FFT- and correlation-based demodulation, is also proposed. The performance of the proposed scheme is evaluated through extensive simulation results. Compared to the conventional LoRa modulation scheme, we show that the proposed scheme exhibits over 3 dB performance gain at a bit error rate of 10−4.

Abstract The Z‐source inverter is one of the most interesting power electronic converters. Over the past decades, research and development have been in high demand to meet the challenges for improving the converter performance with reduced weight and cost while having high efficiency along with high gain or boost factor. Since the inception, tons of resolutions, customizations, and improvements have appeared to achieve these performance goals. To overcome the most common drawback, i.e. the low boost factor of classical Z‐source inverters, the switched inductor/capacitor and switched boost Z‐source inverter topologies have become predominant in the recent epoch. Furthermore, the higher component voltage stress, discontinuous input current, and high inrush start‐up current issues have also been addressed and solved in various literature as part of this topical advancement. In this study, a comprehensive review of various switched impedance network‐based Z‐source inverter topologies has been accomplished for providing a quick report to researchers and engineers so that they can consider this as a one‐stop solution for selecting inverters from this group. The overall study covers the methodology, features, and relevant important results of the latest switched Z‐source inverter models in order to demonstrate the coordination between pitfalls and improvements.

Aniba canelilla (Kunth) Mez is an aromatic tree from Amazon region whose essential oil presents 1-nitro-2-phenylethane (NP) and methyleugenol (ME) as major compounds. Several properties are attributed to Aniba canelilla essential oil (ACEO), such as antifungal. Onychomycoses are fungal nail infections that require novel therapeutic alternatives, especially topical ones. However, to ensure the success of topical therapy, the active compound should be able to penetrate/permeate the nail plate, which is challenging due to the highly keratinized composition of this structure. Thus, the aims of this article were to develop, validate and apply a high-performance liquid chromatography method (HPLC-UV) to quantify NP and ME in porcine hoof extract (PHE) and receptor fluid (RF) during in vitro permeation/retention studies in nail model, for which porcine hoof membranes were used. For method development, two Designs of Experiment (DoE) were adopted: 2 3 Full Factorial and Box-Behnken. Retention times of 5.65 and 7.49 min were achieved for NP and ME, respectively. The method was full validated for NP and ME quantification in receptor fluid, in accordance with the recommended parameters by ICH Q2(R1) Guideline. In addition, the method was full validated for NP and ME quantification in porcine hoof extract, considering the parameters and criteria of ICH M10 Guideline. In vitro permeation/retention studies were carried out in nail model, and promising results were obtained. NP reached the receptor fluid in the order of 441.1 ± 92.1 µg/cm 2 at 72 h. The amount of NP and ME retained into porcine hoof membrane was 1272.6 ± 225.7 µg/cm 2 and 84.7 ± 20.4 µg/cm 2 , respectively, at 72 h. Our findings open perspective to develop topical formulations containing ACEO as active compound aiming the management of onychomycosis., Competing Interests: Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2023 Elsevier B.V. All rights reserved.)

Trichomoniasis is a common sexually transmitted infection that poses significant complications for women. Challenges in treatment include adverse effects and resistance to standard antimicrobial agents. Given this context, a sesame seed oil nanoemulsion (SONE) was developed and showed anti-Trichomonas vaginalis activity. To facilitate the local application of SONE, a polysaccharide film was developed using xanthan gum (XG) and κ-carrageenan gum (CG). A blend of XG and CG (at 2 %, ratio 1:3) plasticized with glycerol produced a more promising film (XCF) than using the gums individually. The film containing SONE (SONE-XCF) was successfully obtained by replacing the aqueous solvent with SONE via solvent evaporation technique. The hydrophilic SONE-XCF exhibited homogeneity and suitable mechanical properties for vaginal application. Furthermore, SONE-XCF demonstrated mucoadhesive properties and high absorption capacity for excessive vaginal fluids produced in vaginitis. It also had a disintegration time of over 8 h, indicating long retention at the intended site of action. Hemolysis and chorioallantoic membrane tests confirmed the safety of the film. Therefore, SONE-XCF is a biocompatible film with a natural composition and inherent activity against T. vaginalis, possessing exceptional characteristics that make it appropriate for vaginal application, offering an interesting alternative for trichomoniasis treatment., Competing Interests: Declaration of competing interest The authors declare the following financial interests/personal relationships which may be considered as potential competing interests: Leticia Cruz reports was provided by Federal University of Santa Maria. Leticia Cruz reports a relationship with Federal University of Santa Maria that includes: employment. The authors declare no conflit of interest., (Copyright © 2023 Elsevier B.V. All rights reserved.)

Essential oils (EOs) are products of secondary metabolism with recognized organoleptic characteristics and biological properties. Recently, there has been a growing demand for EOs in the national and international market, mainly due to the recognition of their use as complementary medicine practices, and the increased use in the industries of pharmaceutics, cosmetics, well-being, veterinary and agroecology, boosting the productive sector. In this context, EOs from grasses of the Cymbopogon (Poaceae) are promising sources of bioactive compounds, due to their recognized biological properties, such as anti-inflammatory, antibacterial, antifungal, antidiabetic, repellent, and larvicide. Thus, the present study aims to carry out a review of the scientific literature of the main works related to the evaluation of the antifungal action of essential oils extracted from plants of the Cymbopogon genus, compiling the species that showed the best results and relating them to their main chemical constituents. This review covers the following species: C. citratus, C. flexuosus, C. winterianus, C. martinii, C. nardus, C. giganteus, C. schoenanthus, C. khasans, and C. proximus. Among them, C. citratus was the most assessed, being associated with the vast majority of studies (61.9 %), and it was also the species that showed the best results in terms of MIC., (© 2023 Wiley-VHCA AG, Zurich, Switzerland.)

The ostrich oil (OO) has been topically used for decades to treat skin diseases. Its oral use has been encouraged through e-commerce advertising several health benefits to OO without scientific evidence on its safety or effectiveness. This study presents the chromatographic profile of a commercially available OO and its acute and 28-day repeated dose in vivo toxicological profiles. OO anti-inflammatory and antinociceptive effects were also investigated. Omega-9 (ω-9; oleic acid; 34.6%) and -6 (linoleic acid; 14.9%) were detected as OO main constituents. A high single dose of the OO (2 g/kg of ω-9) demonstrated no or low acute toxicity. However, when orally treated with OO (30-300 mg/kg of ω-9) for 28 consecutive days, mice exhibited altered locomotor and exploratory activities, hepatic damage, and increased hindpaw sensitivity accompanied by increased levels of cytokine and brain-derived neurotrophic factor in their spinal cords and brains. Lack of anti-inflammatory or antinociceptive activities was also evidenced in 15-day-OO treated mice. These results indicate that chronic consumption of OO induces hepatic injury, in addition to neuroinflammation and subsequent hypersensitivity and behavioural changes. Thus, there is no evidence to support OO use to treating illness in humans., Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2023 Elsevier Ltd. All rights reserved.)

Indonesian clove cigarettes-called " kretek " due to the crackling sound that can be heard when the product burns-are tobacco products containing clove and the " saus ", a mixture of essential oils and plant extracts whose ingredients are mostly kept in secret. It is important to determine which ingredients those are to properly assess the effects that clove cigarettes can cause. An organoleptic, qualitative and quantitative analysis was made in 9 different brands of clove cigarettes obtained in Brazil. Nicotine, eugenol, menthol, and β-caryophyllene were quantified through gas chromatography coupled to mass spectrometry. The samples presented 20 different compounds, and all samples had a different combination of the compounds. Nicotine concentrations were generally higher than eugenol, and lower than nicotine concentration in a conventional cigarette. One sample had menthol even though the cigarette pack did not inform that it was a menthol product. There were traces of 2 unusual substances. Clindamycin is an antibiotic that can be used to treat bacterial infections in respiratory airways, and octodrine is an amphetaminic stimulant used in nutritional supplements, considered as a substance of doping by the World Anti-Doping Association. The presence of both substances was not tested using certified reference materials, but its possible presence raises concern about the compounds in kretek cigarettes. There should be more studies about the contents of clove cigarettes, to improve antitobacco legislations and regulations. This way it would be possible to properly inform the risks of smoking clove cigarettes and to diminish the number of tobacco users throughout the world., (© The Author(s) 2022. Published by Oxford University Press. All rights reserved. For Permissions, please email: journals.permissions@oup.com.)

Ethnopharmacological Relevance: Inflammation is the body's normal protective response to injury and is stimulated by pathogens, toxic compounds, damaged cells or radiation, promoting healing and restoring homeostasis to the injured tissue. Leaves of Piper gaudichaudianum Kunth, known as "pariparoba" are widely used in folk medicine for the relief of toothache, while the fresh roots are used as anti-inflammatory and to treat liver disorders. For P. mikanianum (Kunth) Steud is known as "aguaxima", is widely used in the treatment of inflammation, rheumatism and ulcer, with its roots being used for stomach disorders and as a diaphoretic in intermittent fevers., Aim of the Study: Therefore, this work aims to chemically characterize the essential oil of Piper gaudichaudianum and Piper mikanianum, as well as the evaluation of neutrophil antichemotactic activity of both essential oils in order to complement the information of its traditional use, taking the leaves as plant material and, with that, corroborating its use in folk medicine for the treatment of inflammatory diseases., Materials and Methods: The essential oil from leaves of both Piper species were obtained from crushed fresh samples, by hydrodistillation using a Clevenger type-apparatus for 4 h. The yield determination was performed as vol/wt (v/w) and in triplicate. The amount of essential oil obtained was quantified in mL. The identification and quantification of the compounds was performed using gas chromatography-mass spectrometry (GC-MS) and gas chromatography-flame ionization detection (GC-FID). The in vitro anti-inflammatory activity was evaluated using the model of modified Boyden chamber. In this test the essential oils were tested for their ability to inhibit leukocyte chemotaxis stimulated by Escherichia coli lipopolysaccharide., Results: The chemical composition of the essential oils revealed the identification of 26 constituents for P. gaudichaudianum being the sesquiterpenes β-selinene (14.0%) and viridiflorene (10.5%) the main compounds, followed by caryophyllene oxide (9.3%) and (E)-nerolidol (9.0%). For P. mikanianum essential oil, β-myrcene (17.2%) and bicyclogermacrene (26.3%) were the major components in the monoterpenes and sesquiterpene fractions, respectively. The essential oils were also tested for their ability to inhibit neutrophil chemotaxis in vitro when stimulated by Escherichia coli lipopolysaccharide. Both essential oils showed antichemotactic effect with reduction in migration of 0-72.2% for P. gaudichaudianum and 8.6-100% for P. mikanianum to same concentrations, suggesting a response to acute inflammatory processes., Conclusions: Since up to date there is no report of this biological activities by this mechanism (antichemotactic assay) for essential oils this species. These results showed that the essential oils of P. gaudichaudianum and P. mikanianum have a great capacity to inhibit neutrophil chemotaxis in an inflammatory process, in a dose-dependent way, suggesting anti-inflammatory potential, by preventing its accumulation at the injury site with the possibility of tissue damage. Findings of these studies support the traditional use of these species in the treatment of inflammatory processes., (Copyright © 2022 Elsevier B.V. All rights reserved.)

The harmonics exacerbated by the integration of distributed energy such as wind power has been extensively studied. However, the interaction and propagation mechanism between harmonic sources in the hydro-wind complementary generation system are still not clear. To tackle this challenge, the presented study establishes the hydro-wind complementary generation system model and explores the harmonics propagation and interaction in all components. Then three operation mode of complementary system (scenario 1: stand-alone Hydroelectric Generating System, scenario 2: stand-alone Wind Farm (WF) and scenario 3: complementary generation system) are selected. The results demonstrate that the integration of HGS diminishes the harmonic at DFIG side but at the grid side. In complementary generation system, the THD u rises but the corresponding THD i declines due to the regulation of power grid. Furthermore, the odd harmonics interactions analysis reveal that the doubly-fed induction generator's (DFIG) side and the stator's side are the two high-risk sources in the complementary generation process. The presented results provide a basis for power quality evaluation of hydro-wind complementary generation system., Competing Interests: Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2022 ISA. Published by Elsevier Ltd. All rights reserved.)

Few studies were performed on the volatile components' properties of propolis from native Brazilian stingless bees. This work sought to extract, chemically characterize, and evaluate of the antimicrobial properties of volatile oils from propolis of the stingless bees Melipona quadrifasciata quadrifasciata (MQ) and Tetragonisca angustula (TA). The volatile oils from the pulverized propolis samples were obtained in a Clevenger apparatus and characterized by gas chromatography coupled to mass spectrometry (GC/MS) and to flame ionization detector (GC-FID). All samples showed promising activity against Mycoplasma pneumoniae, with MICs from 103 to 224 μg mL -1 , nonetheless, they were less active against cell walled bacteria. Activity against Candida species was moderate, but one MQ sample showed a MIC value of 103 μg mL -1 against C. tropicallis. Oils' fractionation showed no improvement in antibacterial activity. The promising antibacterial effect against this microorganism is likely related to the synergism between the components of the volatile oils., (© 2022 Wiley-VHCA AG, Zurich, Switzerland.)

Psidium cattleyanum has two morphotypes: one with yellow fruits and other with red fruits. The leaves are popularly used as anti-inflammatory. However, no distinction is made between the types. Therefore, this study compared chemical and pharmacological data of both morphotypes to select proper biomarkers to ensure P. cattleyanum leaves quality. After extraction optimization by experimental design, 28 samples were analyzed by HPLC. Using Principal Component Analysis, it was possible to detect two chemotypes, unrelated to the color of the fruits. However, the extracts obtained from both chemotypes seemed to play similar anti-inflammatory effect, demonstrated by anti-chemotactic activity. The compounds common to both chemotypes were isolated and identified as hyperoside, miquelianin and quercitrin; these compounds also demonstrated anti-inflammatory potential. Since both chemotypes played similar activity, along with the isolated flavonoids, these flavonoids were selected as biomarkers for quality control of P. cattleyanum leaves. Following ICH guidelines, a HPLC method was validated. In summary, this study demonstrated that hyperoside, miquelianin and quercitrin can be used as biomarkers for quality control of P. cattleyanum leaves and a method was developed and validated to be used interchangeably for both morpho- and chemotypes., (Copyright © 2022 Elsevier B.V. All rights reserved.)

Introduction: The general lack of knowledge about the composition of clove cigarettes and the large number of terms that can be used to define different types of cigarettes that contain cloves makes it difficult to find scientific articles focused on the subject. We reviewed the publications that cited clove cigarettes to assess their relevance., Methods: We searched publications on Scopus, ScienceDirect, PubMed, and Portal CAPES during the first semester of 2021, without date restrictions. Through a quality assessment, the studies found were assorted in ten different categories., Results: Indonesian clove cigarettes-also known as kretek -are a mixture of tobacco and cloves rolled in a cigarette and sprayed with oils, plant extract, and food flavorings, in an unknown quantity and composition, different from each brand, which is usually kept in secret. Due to the relatively low prevalence of use in the general population, most publications on tobacco products tend to ignore clove cigarettes or place them in an existing category. Clove cigarettes can be hand-rolled, machine-made, filtered, unfiltered, and each form can be named differently. The interchangeable use of each term, sometimes grouping conventional cigarettes in the mix, can lead the researcher to consider a publication that should be excluded., Conclusion: The existing regulations on flavored cigarettes, although well-intentioned, are still somewhat vague and broad, leaving possible loopholes that can be exploited by the tobacco industries. Fully understanding the precise effects caused by clove cigarettes can be an important tool in future discussions about tobacco control.

This paper presents a voltage control mode (VCM)-based super-twisting algorithm-sliding mode controller (STA-SMC) and current control mode (CCM)-based STA-SMC for islanded and grid-connected operations of single-phase inverters interfaced with distributed energy resources (DERs), respectively. The external disturbances are modeled by considering the effects of load currents or load voltages depending on operational modes whiles parametric uncertainties are modeled based on their variations from nominal values. Therefore, the proposed controllers are robust against external disturbances, parametric uncertainties, and variations in loading conditions. Simulation studies are conducted in the MATLAB/Simulink platform for both single and multiple DERs which are interfaced through single-phase inverters to the main grid or loads. The results are also analyzed through comparative studies with different controllers and it is found that the proposed controllers perform better than existing controllers., Competing Interests: Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2021 ISA. Published by Elsevier Ltd. All rights reserved.)

Curcumin presents a promising anti-inflammatory potential, but its low water-solubility and bioavailability hinder its application. In this sense, cocrystallization represents a tool for improving physicochemical properties, solubility, permeability, and bioavailability of new drug candidates. Thus, the aim of this work was to produce curcumin cocrystals (with n-acetylcysteine as coformer, which possesses anti-inflammatory and antioxidant activities), by the anti-solvent gas technique using supercritical carbon dioxide, and to test its antinociceptive and anti-inflammatory potential. The cocrystal was characterized by differential scanning calorimetry, powder X-ray diffraction and scanning electron microscopy. The cocrystal solubility and antichemotaxic activity were also assessed in vitro. Antinociceptive and anti-inflammatory activities were carried out in vivo using the acetic acid-induced abdominal writhing and carrageenan-induced paw oedema assays in mice. The results demonstrated the formation of a new crystalline structure, thereby confirming the successful formation of the cocrystal. The higher solubility of the cocrystal compared to pure curcumin was verified in acidic and neutral pH, and the cocrystal inhibited the chemotaxis of neutrophils in vitro. In vivo assays showed that cocrystal presents increased antinociceptive and anti-inflammatory potency when compared to pure curcumin, which could be related to an improvement in its bioavailability., (© 2022. The Author(s), under exclusive licence to Springer Nature Switzerland AG.)

Cuphea genus (Lythraceae) popularly known in Brazil as " sete-sangrias ", it's described as antimicrobial, anti-inflammatory, diuretic and antihypertensive mainly. Investigating the chemotactic ability plays an important role in the identification of new anti-inflammatory agents. Thus, this research aims to assay the antichemotactic activity of hydroethanolic extracts of C. calophylla , C. carthagenensis , C. glutinosa , and C. racemosa as well as the compounds miquelianin and myricitrin. The antichemotactic activity of the hydroethanolic extracts, miquelianin, and myricitrin were assayed at concentrations 0.001 to 10   µg/mL in the lipopolysaccharide-induced chemotaxis on rat polymorphonuclear neutrophils. All the assayed samples displayed antichemotactic activity with reduction of the neutrophil migration in the range of 4.46-100%, and an IC 50 value in the range of 0.30-1.24   µg/mL. Thus, this study demonstrates that the extracts hydroethanolic of Cuphea species, miquelianin, and myricitrin display a significant antichemotactic activity. Therefore, in future studies, extracts from Cuphea spp. could be used as anti-inflammatory drugs.

The present study investigates the chemical composition, anti-inflammatory, and antihypertensive activities, in vitro, from extracts of Cuphea lindmaniana and Cuphea urbaniana leaves. The extraction was performed ultrasound-assisted, and UHPLC/MS analysis was in positive mode ionization. The anti-inflammatory activity of the extracts and miquelianin were assayed at concentrations 0.001-10 μg/mL by chemotaxis on rat polymorphonuclear neutrophils. The antihypertensive activity was performed by angiotensin-converting enzyme (ACE) inhibition. From the nineteen proposed compounds, six of them are described for the first time in this genus. The extracts displayed antichemotactic effect with a reduction of 100 % of the neutrophil migration, in vitro, in most concentrations. The ACE-inhibition presented results ranging from 19.58 to 22.82 %. In conclusion, C. lindmaniana and C. urbaniana extracts contain a rich diversity of flavonoids and display in vitro anti-inflammatory and antihypertensive potential. Thus, this study could serve as a scientific baseline for further investigation, on developmental novel products with therapeutic actions., (© 2021 Wiley-VHCA AG, Zurich, Switzerland.)

Volatile oils (VOs) obtained from the aerial parts of species from the Disynaphiinae subtribe (genera Acanthostyles, Campovassouria, Disynaphia, Grazielia, Raulinoreitzia, and Symphyopappus) of Eupatorieae (Asteraceae) collected in Rio Grande do Sul, southern Brazil, were characterized using GC-MS. The yield of VOs relative to fresh material ranged from 0.2 to 1.7% between the Disynaphiinae subtribe samples (Acanthostyles buniifolius, Campovassouria cruciata, Disynaphia ericoides, D. ligulifolia, D. spathulata, Symphyopappus casarettoi, S. reticulatus, S. itatiayensis, Grazielia gaudichaudieana, G. intermedia, G. nummularia, G. serrata, Raulinoreitzia crenulata, and R. tremula). The VOs in this subtribe were mainly composed of terpene compounds. Compositional multivariate analysis demonstrated clustering between the samples of Grazielia and Raulinoreitzia on one side, which contain relatively higher proportions of monoterpenes, and Disynaphia and Campovassouria, which contain more oxygenated sesquiterpenes. The samples of Symphyopappus and Acanthostyles, which contain more sesquiterpene hydrocarbons, were located between these two main groups. Multivariate analysis accounting for the recent proposals of subtribal recircumscription of Eupatorieae was also performed. The odd chemistry of S. itatiayensis was in accordance with the recent attempts to exclude it from the genus Symphyopappus., (Copyright © 2021 Elsevier Ltd. All rights reserved.)

Breast and cervical cancer represent a major problem of women's global public health. Here, we investigated the chemical composition of essential oils from leaves and flowers of T. ostenii and the antineoplastic potential in a cervical cancer and breast cancer cell line, SiHa and MCF-7; and non-tumoral cells, HaCat. The chemical analysis revealed a predominance of oxygenated monoterpenes in both essential oils. The IC50 after 24 h of treatment was 72 ng/mL for EO 1 and 83 ng/mL for EO 2 in SiHa cells. For MCF-7 the IC50 was 174.3 ng/mL for EO 1. For HaCat cells it was 54.45 ng/mL for EO 1 and 20.83 ng/mL for EO 2. A synergistic effect with both essential oils and cisplatin was also verified. SiHa cells had their wound healing capacity reduced after 48 h of treatment with EO 2 and both essential oils were able to significantly inhibit the adhesion process and clonogenic ability after 24 h of treatment. Our results suggest a long-lasting inhibitory activity in SiHa cells because of the low recovery capacity of cells after treatment withdrawal. Flow cytometer with annexin V/propidium iodide demonstrated a majority cell death through late apoptosis after 24, 48 and 72 hours of treatment.

The purpose of this work was to determine the chemical composition and evaluate the antichemotactic, antioxidant, and antifungal activities of the essential oil obtained from the species Cryptocarya aschersoniana Mez, Cinnamomum amoenum (Ness & Mart.) Kosterm., and Schinus terebinthifolia Raddi, as well as the combination of C. aschersoniana essential oil and terbinafine against isolates of dermatophytes. Allo-aromadendrene, bicyclogermacrene, and germacrene B were identified as major compounds in essential oils. The essential oil of C. aschersoniana shown 100 % inhibitory effect on leukocyte migration at the concentration of 10 μg/mL while S. terebinthifolia oil presented 80.1 % inhibitory effect at the same concentration. Only S. terebinthifolia oil possessed free-radical-scavenging activity which indicates its antioxidant capacity. The essential oils were also tested against fungal isolates of dermatophyte species (Trichophyton rubrum, Trichophyton mentagrophytes, Microsporum canis and Microsporum gypseum), resulting in MIC ranging from 125 μg/mL to over 500 μg/mL. C. aschersoniana oil combined with terbinafine resulted in an additive interaction effect. In this case, the essential oil may act as a complement to conventional therapy for the topical treatment of superficial fungal infections, mainly because it is associated with an anti-inflammatory effect., (© 2019 Wiley-VHCA AG, Zurich, Switzerland.)

Background: Several species of Salvia are used as medicinal plants around the world. Biological activities of isolated compounds have been described, being diterpenes frequently responsible for the effects., Purpose: Isolation of diterpenes from Salvia uliginosa Benth. and evaluation of the antichemotactic and leishmanicidal activities of the isolated compounds., Study Design: To isolate diterpenes from S. uliginosa and evaluate their antichemotactic and leishmanicidal activities in vitro., Methods: The exudate of S. uliginosa was obtained by rapidly dipping the aerial parts in dichloromethane. The compounds were isolated by repeated column chromatography over silica gel. The effects on L. amazonensis growth, survival, DNA degradation, ROS generation, as well as the antichemotactic activity and cytotoxicity of the compounds towards human erythrocytes and macrophages were evaluated., Results: A novel icetexane diterpene, isoicetexone (IsoICT) along with the known diterpenes icetexone (ICT), and 7-acetoxy-6,7-dihydroicetexone were isolated from the dichloromethane surface exudate of S. uliginosa. The structures were elucidated using NMR and MS experiments, and by comparison with previously reported data. IsoICT and ICT at low concentrations caused completely inhibition of neutrophils migration in vitro. In addition, IsoICT and ICT showed high leishmanicidal activity against L. amazonensis, induced ROS production in parasites and presented low cytotoxicity against macrophages and human erythrocytes, and moderate to high selectivity index., Conclusion: These data indicated that IsoICT and ICT exhibit potent antichemotactic and leishmanicidal effects. Further studies are needed in order to evaluate the in vivo activities as well as the toxicity of the compounds., (Copyright © 2018. Published by Elsevier GmbH.)

Investigating the influence of seasonal variations on biological activities is important for pharmacological studies and metabolic engineering. Therefore, this study was conducted to determine the variation of the chemical composition of essential oils obtained from Nectandra megapotamica leaves, collected at different stages of plant development, as well as its influence on the biological activities. A total of 38 compounds were identified that accounted for 97⁻99.2% of the chemical composition of the oils. Major differences were observed in the monoterpenic fraction, representing 5.1% of the compounds identified in the productive rest phase to 37.1% in the blooming phase. Bicyclogermacrene and germacrene D were the predominant compounds identified in the oil of all collections. Furthermore, limonene, β-pinene, and spathulenol were identified predominantly in the samples of blooming and fruiting phases. The oils exhibited significant antichemotactic activity and different effects in scavenging the radical 2,2-diphenyl-1-picrylhydrazyl. Variations were also observed in the antifungal activity, with the minimum inhibitory concentrations ranging from 125 to 500 μg/mL. These results demonstrate the influence of monoterpenes, primarily limonene, α-pinene, and β-pinene, on the bioactivities of the oil. Studies investigating the variations in the chemical composition of essential oil may offer a strategy to produce a compound or a group of compounds of interest to industries with a specific pharmacological focus.

Pomegranate is of current interest owing to the existing potential for industrial uses of fruit peels. This includes its availability as a raw vegetable material, a byproduct that constitutes residue in the use of the species and is recognized as a functional product, and beneficial health properties, as will be demonstrated in the studies cited. Therefore, it is necessary to ensure its effectiveness and safety. Toward this end, the aim of this study was to develop and validate an analytical method for the separation and quantification of total punicalagin present in the bark of the fruit of Punica granatum by HPLC. Purity tests such as water determination and total ashes were also performed. The ability of the extract and enriched fraction of punicalagin to inhibit leukocyte migration in vitro was determined by the Boyden's chamber method. The developed HPLC method demonstrated good separation and quantification of the punicalagin α and β anomers. The method is efficient and reliable, and can ultimately be used for the analysis of the extract of pomegranate. The crude extract and the fraction of punicalagins significantly inhibited leukocyte migration at concentrations of 1 and 10 μg/mL in relation to the negative control, indicating potential antichemotactic action., (© 2018 John Wiley & Sons, Ltd.)

Objectives: The aim of this study was to evaluate the antifungal, antichemotactic and antioxidant activities of Schinus lentiscifolius essential oil, as well as its combined effect with terbinafine and ciclopirox, against dermatophytes., Methods: Essential oil was analysed by GC-MS. The antifungal activity and the mechanism of action were determined by broth microdilution, sorbitol and ergosterol assays, as well as scanning electron microscopy. The checkerboard method was used for evaluating the interactions with commercial antifungal agents. The antioxidant and antichemotactic activities were measured using the DPPH and the modified Boyden chamber methods, respectively., Key Findings: Chemical analysis revealed the presence of 33 compounds, the primary ones being γ-eudesmol (12.8%) and elemol (10.5%). The oil exhibited 97.4% of antichemotactic activity and 37.9% of antioxidant activity. Antifungal screening showed effect against dermatophytes with minimum inhibitory concentration values of 125 and 250 μg/ml. Regarding the mechanisms of action, the assays showed that the oil can act on the fungal cell wall and membrane. Synergistic interactions were observed using the combination with antifungals, primarily terbinafine., Conclusions: Schinus lentiscifolius essential oil acted as a chemosensitizer of the fungal cell to the drug, resulting in an improvement in the antifungal effect. Therefore, this combination can be considered as an alternative for the topical treatment of dermatophytosis., (© 2018 Royal Pharmaceutical Society.)

Eupatorium tremulum is a South American shrub reported to cause cattle digestive intoxication, of which the volatile oil, mainly composed by bisabolane- and amorphane-type sesquiterpenoids, exhibits high quantitative variability. This report describes the application of chemometric tools for the identification of volatile compounds that characterize phenophasical changes in the plant. Preblooming, blooming, and postblooming specimens were paired-sampled and submitted to hydrodistillation and GC-MS analysis. Differential results were analyzed by orthogonal projection to latent structures-discriminant analysis (OPLS-DA), and the substances with different distribution in each phase were highlighted. Mean results between phases were submitted to factor analysis (FA), and correlations between the variables were demonstrated. Preblooming to blooming phase change was characterized by decreased levels of amorpha-4-en-7-ol (13) and epi-α-bisabolol (19) and increased amounts of amorpha-4,7(11)-diene (1). Blooming to postblooming change was characterized by decreases in 1, germacrene D (2), and β-bisabolene (4) and increases in 13 and 19. Finally, enhanced levels of 1, 4, and 2 reflected the change from the postblooming to the preblooming phase. FA revealed a strong correlation in the variability between the bisabolane hydrocarbons, possibly related to its common enzymatic origin. Another strong source of negative correlation showed bisabolane- and amorphane-type alcohols, on one side, and amorphane-type furans, on the other side, to occur in two alternative oxidation routes. Finally, 1 was strongly negatively correlated to its oxidized furan and ketofuran derivatives [verboccidentafuran (16) and 3-oxo-verboccidentafuran (23)] and additionally to a third compound, putatively identified as a biosynthetic intermediate between this hydrocarbon and the furans, amorpha-4,7(11)-dien-8-one (20).

Background: The copaiba oil is a common natural product used in cosmetic industry and as a nutraceutical product. However, lack of quality control and scarce knowledge about its antimicrobial activity is a point of concern. The proposal of this study was to investigate the physicochemical properties and the antimicrobial activity of five commercial brands of copaiba oil., Methods: Acidity and ester index, refractory index, solubility in alcohol, and thin layer chromatography were performed to verify the physicochemical properties of five commercial copaiba oils sold in local pharmacies. Ultra performance liquid chromatography coupled with diode-array detection and electrospray ionization quadrupole time-of-flight mass spectrometry (UPLC-DAD/ESI-Q-TOF-MS) was used to investigate diterpene acids while the volatile compounds were analysed by gas chromatography-mass spectrometry (GC-MS). Antibacterial and antifungal activities were also evaluated by agar diffusion technique; and minimal inhibitory concentration and maximal bactericidal concentration were defined for each sample and bacteria., Results: The physical-chemical analysis revealed heterogeneity between all samples analysed. The A1 sample showed characteristics of copaiba oil and was mainly composed by hydrocarbon sesquiterpenes (29.95% β-bisabolene, 25.65% Z-α-bergamotene and 10.27% β-cariophyllene). Among diterpene acids, the UPLCDAD/ESI-Q-TOF-MS data are compatible with presence of copalic and/or kolavenic acid (m/z 305 [M + H]+). Candida albicans was sensitive to almost all samples at high concentration and Saccaromyces. Cerevisiae showed sensitivity to A1 sample at 100 mg/mL. Although variable, all samples showed antibacterial activity. Significant activity was seen for A3 (19.0 ±0 and 15.6 ±0.5 mm), A4 (16.6 ±0.5 and 15.6 ±0 mm), and A5 (17.1 ±0 and 17.1 ±0 mm) on Staphylococcus saprophyticus and S. aureus, respectively. All samples were active against Klebsiella pneumoniae showing ≥15 mm diameter halo inhibition; and only A2 was active against Eschirichia coli. Phytopatogens tested revealed resistance of Ralstonia solanacearum CGH12 to all samples and susceptibility of Xcv 112 strain of Xanthomonas campestris pv campestris to almost all samples. MIC and MMC showed bacteriostatic effect against clinical interest bacteria and bactericidal effect against phytopatogens., Conclusions: The results from physicochemical analysis reinforce the fact that it is imperative to include simple conventional methods in the analysis of oil products. The analysis of copaiba oil gives safe products and purity which ensure products with quality. Also, since copaiba oil is an over-the-counter product the results indicate that pharmacosurveillance must be improved by the governmental regulation agency to avoid microorganism resistance selection and to achieve better international quality products.

Context: Glechon spathulata Benth. and Glechon marifolia Benth. (Lamiaceae, Mentheae) are aromatic plants used in traditional medicine for the treatment of viral infections., Objective: The chemical composition and antiviral and antifungal activities of Glechon spathulata and Glechon marifolia essential oils were investigated., Materials and Methods: The oils were obtained by hydrodistillation and analyzed by GC-FID and GC-MS. Anti-herpes virus (HSV-1) activity was examined in Vero cells by yield reduction assay, in doses of 0.0095% v/v and 0.039% v/v, for G. spathulata and G. marifolia oil, respectively. Antifungal activity was carried by the broth microdilution method, in oil concentrations that ranged from 5.2 to 500 µg/mL., Results: β-Caryophyllene (14.2% and 32.2% for G. spathulata and G. marifolia, respectively) and bicyclogermacrene (17.1% and 16.5%, respectively) were the major components of both oils. At noncytotoxic concentrations of the essential oils, the viral titer was reduced by up to 2 log10 for KOS and VR-733 strains. The antifungal activity was observed against Trichophyton rubrum (MIC 10-83 µg/mL) and Epidermophyton floccosum (MIC 83-500 µg/mL). The oil of G. spathulata exhibited activity against the three strains tested (KOS, VR733, and 29-R), whereas G. marifolia oil was active against two strains, KOS and VR733., Discussion and Conclusion: The chemical composition for G. spathulata and G. marifolia essential oils is very similar. The oil of G. spathulata can be promising as a new antifungal agent against dermatophytes. The findings add important information to the biological activity of Glechon species essential oils, specifically its antiviral and antidermatophytic properties.

The alkaloid extracts of four Huperzia and one Lycopodiella species, from Brazilian habitats, were tested for their in vitro anticholinesterase activities. IC(50) values showed a potent acetylcholinesterase inhibition for H. reflexa (0.11 ± 0.05 μg/mL), followed by H. quadrifariata (2.0 ± 0.3 μg/mL), H. acerosa (5.5 ± 0.9 μg/mL), H. heterocarpon (25.6 ± 2.7 μg/mL) and L. cernua (42.6 ± 1.5 μg/mL). A lower inhibition of butyrylcholinesterase was observed for all species with the exception of H. heterocarpon (8.3 ± 0.9 μg/mL), whose alkaloid extract presented a selectivity for pseudocholinesterase. Moreover, the chemical study of the bioactive extracts performed by GC-MS, revealed the presence of a number of Lycopodium alkaloids belonging to the lycopodane, flabellidane and cernuane groups. Surprisingly, the potent acetylcholinesterase inhibitors huperzines A and B were not detected in the extracts, suggesting that other alkaloids may be responsible for such an effect.

Acanthamoeba is a free-living amoebae genus that causes amoebic keratitis which is a painful sight-threatening disease of the eyes. Its treatment is difficult, and the search for new drugs is very important. Here, essential oils obtained from the aerial parts of Croton pallidulus, Croton isabelli, and Croton ericoides (Euphorbiaceae), native plants of Southern Brazil, were tested against Acanthamoeba polyphaga and analyzed by gas chromatography and gas chromatography-mass spectrometry. The essential oils of C. pallidulus and C. isabelli were characterized by the presence of sesquiterpenes: germacrene D (15.5 %), terpinen-4-ol (13.2 %), and β-caryophyllene (13.1 %) in C. pallidulus and bicyclogermacrene (48.9 %) in C. isabelli. The essential oil of C. ericoides presented mainly monoterpenes, β-pinene (39.0 %) being the main component. Laboratory tests were carried out to determine the effect of the essential oils against A. polyphaga trophozoites. The essential oil of C. ericoides was the most active, killing 87 % of trophozoites at the concentration of 0.5 mg/mL. The essential oil of C. pallidulus killed only 29 % of the trophozoites at the same concentration. The essential oil of C. isabelli presented the lowest activity, killing only 4 % of the trophozoites at the concentration of 10 mg/mL. The essential oils of the three species showed cytotoxic effect by the methyl thiazolyl tetrazolium (MTT) method in Vero cells. The oil of C. ericoides, which showed the highest amoebicidal activity, was the most cytotoxic on these mammalian cells.

Biological indicators are widely used to monitor genotic compounds and air quality in urban environments. Parmotrema tinctorum and Teloschistes exilis have been used to verify the presence of pollutants and analyze morphophysiological alterations in the thallus of species caused by their action. Species were exposed for seven months, in an urban area, in southern Brazil. Mutagenicity and cytotoxicity of PM10 organic extracts were assessed in the Salmonella/microsome assay at two stations. High concentrations of S, Pb, Cr, Zn and Hg were registered in the last period of exposure and more significant morphophysiological damages were verified in the lichens. Generally a higher mutagenic activity is observed in organic extracts of airborne particulate matter during the first months and in the third period of exposure of lichens. In addition, nitro compounds was detected through nitro-sensitive strains. Lichens and mutagenic biomarkers enabled the evaluation of air quality and the presence of environmentally-aggressive compounds., (Copyright © 2011. Published by Elsevier Ltd.)

Baccharis trimera commonly named 'carqueja', is wide-spread in South America and are used as raw material for herbal medicines. A reversed-phase liquid chromatography (RP-LC) method coupled to diode array detector was developed for the analysis of caffeoylquinic acids (CQAs), the main compounds responsible for its digestive activity. The identity of the quinic acids was established by mass spectrometry and were them: 5-O-[E]-caffeoylquinic acid, 3,4-O-[E]-dicaffeoylquinic acid, 3,5-O-[E]-dicaffeoylquinic acid, 4,5-O-[E]-dicaffeoylquinic acid and a tricaffeoylquinic acid. The RP-LC method for the quantitation of the caffeoylquinic acids was validated according to ICH guidelines, based on the following parameters: linearity, selectivity, robustness, limits of detection and quantification, precision and recovery. Hydroalcoholic extracts were prepared by the maceration of the plant material with ethanol:water 1:1 (v/v) in a 0.1:25 g mL(-1) plant:solvent ratio in a water bath at 40°C. Validation data indicated that the HPLC method proposed is suitable for the analysis of caffeoylquinic acids in B. trimera raw material. The results of the LOD and LOQ analyses for the 5-CQA were 4.1 μg mL(-1) and 12.5 μg mL(-1), respectively, 1.3 μg mL(-1), 3.9 μg mL(-1) for 4,5-diCQA and 1.7 μg mL(-1), 5.1 μg mL(-1) for triCQA. The levels of total CQAs ranged from 2.1 to 4.0 g% (w/w). The influence of season harvest and site collection was also evaluated and variations were observed in the results and can be related to phonologic phase, different locations, seasons and soil. Long term and photostability of plant material were carried out and was observed a stable behavior during the time of the experiments., (Copyright © 2011 Elsevier B.V. All rights reserved.)

Acanthamoeba species are free-living amoebae that constitute an etiological agent of Acanthamoeba keratitis, an illness that may cause severe ocular inflammation and blindness and has a very difficult treatment. These molecules that are found in plants may be an alternative for the development of new drugs. Plants of the genus Pterocaulon (Asteraceae) are used in folk medicine as an antiseptic and antifungal agent. In this work, we analyzed Pterocaulon polystachyum essential oil and assessed its amoebicidal activity against Acanthamoeba polyphaga. The leaves of the fresh plant submitted to hydrodistillation yielded 0.15% (w/v) of essential oil that was analyzed by gas chromatography-mass spectrometry being E-sesquilavandulyl acetate as the major component, representing 43.8% of the oil. For the assessment of the amoebicidal activity, concentrations of 20, 10, 5, 2.5, and 1.25 mg/mL of essential oil were tested, being lethal to 100% of the A. polyphaga trophozoites at the concentrations of 10 and 20 mg/mL in 24 and 48 h. The cytotoxic effect of essential oil was also tested in mammalian cells using MTT assay. Amoebicidal activity results are in accordance with previous work in which the lipophilic compounds from this plant were active against Acanthamoeba castellanii. However, further studies with the major component of the essential oil will be carried out.

Fruits of Myrcianthes pungens Berg. Legr. (Myrtaceae), known as guabiju, are widely consumed fresh as well as dried, processed into jam, marmalade, and juices. In this study, chemical composition and antichemotactic and antioxidant activities of fruits from a wild type (GB) and 2 genotypes, PL2 and PL1, of guabiju were investigated. Total anthocyanins for the genotypes ranged from 334 to 531 mg/100 g dry weight (dwt). Total flavonoids and polyphenols ranged from 79.8 to 154 mg/100 g and 2438 to 4613 mg/100 g (dwt), respectively. A reversed phase liquid chromatography method with photodiode array detection was used to determine chemical profiles of the main anthocyanins found in the extracts. An HPLC method for the quantification of flavonoids is proposed, providing a simple procedure with rapid sample preparation. All samples contained 5 identical anthocyanidins, distributed differently, with cyanidin as the main compound. Identified flavonoids were quercitrin, hyperoside, and isoquercitrin; their relative amounts varied among the extracts. The antioxidant activity of guabiju methanolic extract was comparable to that of Trolox, and at a test concentration of 0.25 mg/mL, GB and PL2 activities were higher than those exhibited by Trolox. Total dry extracts of guabiju exhibited greater inhibition of chemotaxis at a concentration of 4 μg/mL, except for GBH (wild-type hydrolyzed extract) which already presented high values at a concentration of 2 μg/mL. These results suggest that the consumption of this fruit, rich in polyphenols, may be beneficial to human health. Practical Application: The paper is the first attempt on the improvement of this native fruit, since it is widely consumed regularly as part of the South American diet. The content of phenolic compounds demonstrates that consumption of guabiju would be beneficial to human health. Differences among samples, originating from open pollination of plants growing on the same site, lead to the conclusion that improvements can be made in the chemical composition and beneficial activity of guabiju fruits by simply selecting genotypes for these characteristics among open-pollinated seedlings., (© 2011 Institute of Food Technologists®)

Unlabelled: Strawberry guava (Psidium cattleianum Sabine) is a native fruit of Brazil widely consumed fresh and used in the food industry. In this context, the present study deals with the chemical characterization and the antioxidant activity of the red (Psidium cattleianum) and yellow (P. cattleianum var. lucidum Hort.) strawberry guava fruits, cultivars Irapuã and Ya-Cy, respectively. Knowledge of chemical composition is fundamental to human nutrition, contributing to the quality of foods. Phenolic compounds in both fruits were analyzed by HPLC-DAD and the total flavonoid content was determined by the Folin-Ciocalteu assay. The antioxidant activity was evaluated by the total reactive antioxidant (TRAP) method. Psidium cattleianum presented a higher content of polyphenolic compounds than P. cattleianum var. lucidum (501.33 and 292.03 mg/100 g, respectively), with hyperoside being one of the major flavonoids identified for both cultivars. In addition to flavonoids, P. cattleianum presented an anthocyanin, identified as cyanidin. The antioxidant activity varied in a concentration-dependent manner for both strawberry guava species. The volatile oils in fruits and fatty acids in seeds were quantified by GC-EM. The analysis of the essential oil of yellow strawberry guava was compared with a previous study on the red cultivar, revealing β-caryophyllene as the main component in both oils. The fatty acid composition was also quite similar and was especially characterized by the presence of unsaturated fatty acids (86.25% and 76%, respectively), among which linoleic acid as the most abundant., Practical Application: In this study, the chemical characterization and the antioxidant activity of the red (Psidium cattleianum) and yellow (P. cattleianum var. lucidum Hort.) strawberry guava fruits were investigated. This is important for potential application of strawberry guava as functional food. Moreover, it may be the experimental basis for further development and use in food industry., (© 2011 Institute of Food Technologists®)

Calea serrata Less. (Asteraceae), an endemic species of south Brazil known as "quebra-tudo", is used in Afro-Brazilian religious rituals and in folk medicine for treating liver disorders. Phytochemical studies of the n-hexane extract of this plant demonstrated the presence of precocene II, a benzopyran derivative known for its insecticidal activity. The aim of this work was to isolate this benzopyran and determine the chemical composition of the essential oil of C. serrata and further to evaluate the acaricidal activity of the essential oil and precocene II against the larvae of Rhipicephalus (Boophilus) microplus. The LC(99.9) and LC(50) values obtained with the oil, which presents precocene II and sesquiterpenes, were 3.94 μL/mL and 0.28 μL/mL, respectively. For precocene II this values were 4.25mg/mL and 1.78 mg/mL, respectively. The results indicate a synergistic interaction between the components of the oil and precocene II., (Copyright © 2011 Elsevier B.V. All rights reserved.)

Flavonoids are polyphenols that are ubiquitous in plants and frequently consumed in the diet. They are suggested to have many beneficial actions on human health, including anti-inflammatory activity. Their properties have been studied in a number of cell types, but little is known about their effects on neutrophil biology. Consequently, we selected 25 flavonoids with different structural features to evaluate their in vitro inhibition of rat polymorphonuclear neutrophil (PMN) chemotaxis, employing a modified Boyden chamber. Migratory activity was measured towards a chemotactic stimulant, formyl-Met-Leu-Phe or lipopolysaccharide. Furthermore, the cytotoxic effect of flavonoids on PMNs was determined by the release of cytosolic lactate dehydrogenase (LDH). Ten flavonoids significantly retarded the migration of PMNs with at least one of the concentrations tested in a range between 0.625 and 100 µM; the best antichemotactic agents were flavone, flavonol, quercetin and rutin. None of the flavanones evaluated presented any significant inhibition of migration in this assay. Our findings indicated that non-hydroxylated flavones possess a better antichemotactic activity when compared to flavones with hydroxy groups. The presence of a sugar moiety in rutin did not produce any increase in this effect, when compared to the respective aglycone analogue. Finally, none of the flavonoids exhibited cell toxicity and for many of these flavonoids this is the first report of the inhibition of PMN chemotaxis., (© Georg Thieme Verlag KG Stuttgart · New York.)

Context: Copaiba oil is an oleoresin made up of resin acids and volatile compounds, and it is obtained by tapping the trunks of trees that are members of the Copaifera L. (Leguminoseae) genus and are found in tropical parts of Latin America., Objective: This study analyzed the chemical composition of Copaifera multijuga Hayne oil and conducted preclinical trials to investigate anti-inflammatory effects and any action it may have on the central nervous system (CNS) of rats., Materials and Methods: The chemical analysis was carried out using gas chromatography with mass spectroscopy. Anti-inflammatory activity was measured by leucocytes mobilization, by chemotaxis assay in Boyden's chamber, and by pleurisy model in rats. CNS effect was determined by plus maze and open-field assays. The statistical test applied was analysis of variance (ANOVA) followed by Tukey's test or ANOVA followed by Duncan's test., Results: The oil was composed of sesquiterpenes with the predominance of β-caryophyllene (36.0%), followed by α-copaene (18.8%), β-bisabolene (8.5%), and α-trans-bergamotene (7.0%). Data demonstrated that at 100 and 200 mg/kg doses and at a concentration of 200 μl/ml copaiba essential oil presented anti-inflammatory effects both in vivo and in vitro based on reduced leukocyte migration to the rats' pleural cavity and to the chemotactic agent lipopolysaccharide solution, respectively. During the experiments investigating CNS effects, locomotive and exploratory activities were reduced and the animals' anxiety increased at 100 and 200 mg/kg., Conclusion: The results obtained suggest that copaiba oil has an interesting anti-inflammatory effect and important effect on the CNS.

Hesperozygis ringens (Benth.) Epling (Lamiaceae) is a strongly aromatic plant employed popularly for its antiparasitic properties. The leaves afforded 4% of essential oil constituted mainly by pulegone (86%). Laboratory tests were carried out to determine the toxicity of the essential oil species on engorged females and larvae of the cattle tick Riphicephalus (Boophilus) microplus using the adult immersion test (AIT) and the larval immersion test (LIT). It was observed that the essential oil at the concentration of 50 microL/mL and 25 microL/mL inhibited the egg laying significatively in relation to the controls and the eggs from these treated females were affected by the oil; the hatching was inhibited in 95% and 30%, respectively. In the LIT it was verified that the LC(99.9), LC(50) and LC(1) was 0.541 microL/mL, 0.260 microL/mL and 0.015 microL/mL, respectively. Pulegone, isolated from the oil, showed similar effect on the females and on the larvae, indicating that it is responsible for the oil activity., (Copyright 2009 Elsevier Ltd. All rights reserved.)

The GC-MS analysis revealed that the leaf essential oils of Myrciaria tenella (DC.) Berg and Calycorectes sellowianus O. Berg (Myrtaceae) were composed of 34 and 37 compounds, respectively. The main constituents of M. tenella oil were beta-caryophyllene (25.1%), and spathulenol (9.7%), while for C. sellowianus were guaiol (13.1%) and beta-caryophyllene (8.6%). The anti-inflammatory effect of both essential oils was investigated in vitro and in vivo. Both oils reduced significantly (p < 0.005) the treated neutrophils chemotaxis with 93% and 91% inhibition for M. tenella and C. sellowianus, respectively. However, in the systemic treatment with the essential oils (50 mg/kg p.o.) only the M. tenella oil was able to significantly reduce the carrageenan-induced paw edema with a similar effect to that observed for indomethacin (10 mg/kg), the positive control.

We have studied the apoptotic pathway activated in response to marine sponge extracts of Polymastia janeirensis. The effect on intracellular ROS production was also examined. Exposure of U138MG glioma cell line to doses higher than 5 microg/mL has decreased glioma cell viability, with an IC(50) <15 microg/mL for both aqueous and organic extracts. However, extracts at higher doses (50 and 100 microg/mL) have stronger cytotoxic effects, decreasing more than 90% of glioma cell viability. The antioxidant Trolox (100 microM) reversed the cell death percentage induced by extracts at 10 and 25 microg/mL. The type of cell death induced by such high doses was predominantly necrosis, while a high percentage of apoptotic glioma cells was found at 10 microg/mL. Moreover, inhibition of caspase-8 with Z-IETD (a caspase-8 inhibitor) had no effect on the amount of apoptosis induced by 10 microg/mL, but inhibition of caspase-9 with Z-LEHD (a caspase-9 inhibitor) decreased apoptosis. We also observed a dose-dependent increase in ROS production, and similarly to effects observed on viability of glioma cells, and on cell death, higher doses also had more severe effects. Co-treatment with Trolox significantly reduced ROS production by extracts at doses lower than 50 microg/mL. This is a first report demonstrating that marine sponge extracts of P. janeirensis induce oxidative cell death through a caspase-9 apoptotic pathway.

The essential oils obtained from the aerial parts of five species of Cunila (Lamiaceae) native to Southern Brazil were analyzed by GC and GC/MS. The oil of Cunila angustifolia was characterized by sabinene; Cunila incana is rich in alpha-pinene and beta-pinene, Cunila spicata and Cunila microcephala presented menthofuran as the main component, and in the essential oil of Cunila incisa, the major component was 1,8-cineole. Laboratory tests were carried out to determine the effect of the essential oils of the above cited plants on larvae of the cattle tick Riphicephalus (Boophilus) microplus. C. angustifolia, C. incana, and C. spicata were the most active samples killing almost the totality of the larvae. C. incisa and C. microcephala showed low acaricidal effect.

Marine sponges have been prominently featured in the area of cancer research. Here, we examined the anti-proliferative effects of crude extracts (aqueous and organic) of the Brazilian marine sponge Polymastia janeirensis in the U138MG human glioma cell line. Moreover, we examined the effects of extracts on selective cytotoxicity in the glioma cells in comparison with a normal cell culture. Exposure of glioma cells to treatments (24 h) resulted in cell number decrease at all doses tested, with both aqueous and organic extracts (IC(50) <20 and <30 microg/ml, respectively). Parallel to this result, sponge extracts reduced glioma cell viability (IC(50) <15 microg/ml for both extracts). However, higher doses (50 and 100 microg/ml) induced a stronger cytotoxic effect when compared to the lower dose tested (10 microg/ml), inhibiting more than 80% of cellular growth and viability. Propidium iodide uptake and flow cytometry analysis further showed that sponge extracts caused necrosis in the glioma cell line at higher doses, while a high percentage of apoptotic glioma cells were observed at 10 microg/ml. Moreover, apoptosis was prevented by the pan-caspase inhibitor Z-VAD, suggesting that marine sponge extracts, at lower doses, induce caspase-dependent apoptosis in U138MG glioma cells. Surprisingly the extracts herein tested were more effective than temozolomide, a potent inductor of apoptosis used for the treatment of malignant gliomas. Furthermore, our results suggested a selectivity cytotoxic effect on glioma cell line in comparison with a normal cell culture, since the effect on viability found in glioma cells was not observed in astrocyte cultures with the lower dose (10 microg/ml). Thus, this marine sponge may be considered a good candidate for development of new cancer medicines with antitumor activity against gliomas.

The dichloromethane and n-butanol extracts obtained from fresh bulbs of Hippeastrum vittatum (Amaryllidaceae), collected in Southern Brazil, were evaluated for their cytotoxic activity in vitro against five human cell lines (HT29 colon adenocarcinoma, H460 non-small cell lung carcinoma, RXF393 renal cell carcinoma, MCF7 breast cancer, and OVCAR3 epithelial ovarian cancer), using the sulphorhodamine B assay. Both extracts showed potential antiproliferative activity. From CH(2)Cl(2) fraction, three alkaloids were isolated: lycorine, vittatine and montanine. The two last compounds were submitted to the antiproliferative assay and the highest level of cytotoxicity was found for the alkaloid montanine.