Antifungal effect of Arnica montana and Hamamelis virginiana against Candida species

Objetivo ­ Avaliar a atividade antifúngica dos extratos glicólicos de Arnica montana e Hamamelis virginiana contra cepas de Candida spp. A candidíase é uma infecção fúngica comum, portanto, a pesquisa de novos agentes antifúngicos tem sido um alvo interessante. Várias plantas apresentaram atividades biológicas e, portanto, podem ser fontes promissoras de produtos naturais com atividades an-tifúngicas. Métodos ­ As atividades antifúngicas dos extratos glicólicos foram avaliadas por meio da determinação da concentração inibitória mínima (CIM) de acordo com o protocolo M27-S3 do Clinical and Laboratory Standards Institute (2008). Resultados ­ O ex-trato glicólico de A. montana apresentou a atividade antifúngica mais forte contra C. tropicalis, com concentração inibitória mínima (CIM) de 10% v/v e concentração fungicida mínima (MFC) de 80% v/v, seguido por C. krusei e C. glabrata, com valores de MIC e MFC de 20% v/v. Além disso, avaliamos a toxicidade dos dois extratos glicólicos no modelo Galleria mellonella usando as curvas de sobre-vivência de larvas tratadas com os extratos. Nossos resultados demonstraram que os extratos glicólicos de A. montana e H. virginiana não exibiram toxicidade contra larvas de G. mellonella e demonstraram atividade antifúngica contra espécies de Candida spp. Con-clusão ­ Assim, ambos os extratos são candidatos promissores para o desenvolvimento de novos agentes antifúngicos.

Objective ­ To evaluate the antifungal activity of Arnica montana and Hamamelis virginiana glycolic extracts against Candida strains. Methods ­ The antifungal activities of glycolic extracts were investigated by determination of the minimum inhibitory concentration (MIC) according to protocol M27-S3 of Clinical and Laboratory Standards Institute (2008). Results ­ A. montana glycolic extract showed the strongest antifungal activity against C. tropicalis, with a minimum inhibitory concentration (MIC) of 10% v/v and a minimum fungicidal concentration (MFC) of 80% v/v, then C. krusei and C. glabrata, with MIC and MFC values of 20% v/v. H. virginiana glycolic extract ex-hibited stronger activity against C. albicans and C. tropicalis, with MIC and MFC values of 10% v/v, than against C. glabrata, C. krusei, and C. parapsilosis, with MIC and MFC values of 20% v/v. Moreover, we evaluated the toxicity of the two glycolic extracts in the Galleria mellonella model using the survival curves of larvae treated with the two extracts. Our results demonstrated that the glycolic extracts of A. montana and H. virginiana exhibited no toxicity against G. mellonella larvae and demonstrated antifungal activity against Candida spe-cies. Conclusion ­ Thus, both extracts are promising candidates for the development of novel antifungal agents.

Toxicidad pulmonar por dasatinib / Dasatinib-Related Pulmonary Toxicity

Paciente de sexo masculino, 70 años, con leucemia mieloide crónica en tratamiento con dasatinib, desarrolla insuficiencia respiratoria asociada a toxicidad pulmonar por dicho fármaco.

70-year-old male patient with chronic myeloid leukemia receiving treatment with da satinib develops respiratory failure associated with pulmonary toxicity related to such drug.

The in vivo imaging of zebrafish for chemical vascular toxicity assessment / 中华预防医学杂志

Objective: To evaluate the vascular toxicity of chemicals by a real-time observation approach using the transgenic zebrafish. Methods: The spatiotemporal vascular alterations of transgenic zebrafish after chemical exposure were assessed by laser confocal microscopy and high-content screening analysis, respectively. Results: The method using Laser Confocal Microscopy (LCM) is easier to operate and yields high-resolution images, while it is lower throughput and inefficient. In contrast, high-content analysis (HCA) analysis obtains high-quality data of vascular toxicity manifesting whole blood vasculature, whereas it requires delicate operation procedures and advanced experimental conditions. Conclusion: Two kinds of zebrafish imaging methods each have advantages and disadvantages. LCM is suitable for the evaluation of a small number of chemicals. HCA, a cutting-edge technology, has great potential for chemical safety assessment allowing high throughput vascular toxicity tests of a good number of chemicals at a time.

Advanced progress of ex vivo biosensor assay in toxicological evaluation / 中华预防医学杂志

The ex vivo biosensor assay is developed to assess the health effects and toxicological mechanism of environmental pollutants with internal environment homeostasis changes by integrating the in vivo exposure evaluation, in vitro outcomes analysis, and systematic environment component screening. This toxicology testing model combines the real-world exposure of people in the field and the study of molecular mechanism exploration in lab experiments to overcome the shortcomings of a single toxicology method. It provides a new technique and perspective for toxicity testing and risk assessment in mesoscale between macroscopic population study and microscopic mechanism exploration.

Progress in the application of three-dimensional cell culture model in toxicity tests of xenobiotic / 中华预防医学杂志

In the process of xenobiotic toxicity prediction and risk assessment, in vitro cell culture models possess high practical application value. With the rapid development of biological technologies such as three-dimensional (3D) bio-printing, organoid culture and organ-on-a-chip systems, in vitro cell culture models have made great progress. Sharing the similarities in structure, function and the physiological environment with tissues or organs in vivo, hazard identification and dose-response analysis based on 3D cell culture models provide access to more accurate toxicity data as a theoretical basis for risk assessment and risk management of chemicals. This review summarizes the establishment of three typical 3D cell culture models, i.e., human cell line-based co-culture model, 3D-printed scaffold-based cell culture model and organoids, and their application in toxicity tests of xenobiotics.

Advances in high-content screening applications in toxicology research / 中华预防医学杂志

The toxicity data of chemicals and drugs increases rapidly, while the animal experimental-based tests method could not meet the current demand of health risk assessment. The high-throughput screening techniques based on in vitro alternative models, integrating with computational methods and information technology to establish toxicity tests strategy promises to address this problem. High-content screening (HCS) technology uses automated microscopy and quantitative image platforms to perform multi-parameter and high-throughput phenotypic analysis via a visualization and quantification manner, and to quickly and effectively assess toxicity and prioritization of chemicals, which promotes the development of in vitro toxicity tests and computational toxicology. HCS technology has been included as an important tool for Toxicity Testing in the 21st Century (Tox21) and chemical risk prioritization. Its applications have been widely utilized in the research field of toxicity tests and chemical toxicity mechanisms. In this review, we describe the development of HCS technology, technical points, toxicological applications, and the future directions and challenges of HCS, so as to provide references for the toxicity testing technology and risk assessment methodology.

Advances in alternative methods upon the vision for toxicity testing in the 21st century / 中华预防医学杂志

With the increase of global chemical production and the aggravation of population exposure and health risks, higher requirements are put forward for chemical toxicity testing and safety evaluation.'Toxicity testing in the 21st century: a vision and a strategy' has greatly promoted the reform of toxicity testing. Toxicity testing in the new era has made great progress by using new models, new methods and new strategies, combined with interdisciplinary and high-tech advantages. While improving the efficiency of chemical toxicity testing, it also realizes more comprehensive, multi-level and high-quality data acquisition and toxicity evaluation, which provides strong support for the exploration of toxicity mode, toxicity mechanism and toxicity pathway. Focusing on the current alternative new methods of toxicity testing, this issue invites many scholars to introduce and summarize high-content analysis, three-dimensional (3D) cell culture technology, Ex vivo test, single cell sequencing and zebrafish experimental methods, in order to promote the leapfrog development of chemical toxicity testing and evaluation in China.

Influence de la toxicité hématologique chimio-induite sur l'observance de la chimiothérapie anticancéreuse à Ouagadougou / Influence of haematological toxicity on the observance of cancer chemotherapy in Ouagadougou

Contexte et Objectif. Déterminer l'infl uence des toxicités hématologiques induites par la chimiothérapie sur l'adhésion à une chimiothérapie anticancéreuse chez des patients traités pour un cancer à l'hôpital universitaire Yalgado Ouédraogo (Ouagadougou, Burkina Faso). Méthodes. Il s'est agi d'une étude rétrospective ayant analysé les dossiers médicaux des patients cancéreux suivis par le service de cancérologie du CHU-YO. Tous les adultes ayant reçu six séances d'une première ligne de chimiothérapie ont été inclus. Pour chaque patient, nous avons analysé toutes les numérations formule sanguines effectuées environ 16 à 18 jours après la cure de chimiothérapie précédente et 3 à 5 jours avant la suivante. Ont été considérés comme observants, les patients ayant respecté tous les intervalles inter-cures. Résultats. Vingt-six patients (27,6%) ont présenté au moins un épisode d'anémie, 46 patients (48,9%) ont au moins un épisode de neutropénie et 9 patients (9,6%) ont au moins un épisode de thrombopénie. Les neutropénies de grade 3 et 4 représentaient de 67,9% à 87% des cas de neutropénie. Aucun cas de thrombopénie de grade 3 ou 4 n'a été observé. Vingt-deux patients ont respecté tous les intervalles intercures. Après ajustement sur les autres toxicités hématologiques en analyse multivariée, la neutropénie était associée de manière signifi cative au non-respect de la chimiothérapie (OR: 0,43). Conclusion. L'amélioration de la disponibilité et de l'accessibilité des moyens de prévention et de traitement des toxicités hématologiques pourraient permettre une amélioration de l'observance de la chimiothérapie anticancéreuse.

Aim and Objective. This study aims to identify the infl uence of chemotherapy induced haematological toxicities on adherence to anti-cancer chemotherapy in patients treated for cancer at Yalgado Ouédraogo University Hospital (Ouagadougou, Burkina Faso). Methods. This study was grounded on the analysis of the medical fi les of the patients, and the consultation and hospitalisation registers for the cancer patients who were monitored by the oncology department of CHU-YO. All adults having received six treatment sessions as fi rst-line chemotherapy were taken into account. For each patient, we analysed all the blood counts carried out approximately 16 to 18 days after the previous treatment session, and 3 to 5 days before the following one. Were considered adherent patients, the patients who complied with every intertreatment interval. Results. 26 patients (27.6%) presented with at least one episode of anaemia, 46 patients (48.9%) with at least one episode of neutropenia, and 9 patients (9.6%) with at least one episode of thrombocytopenia. Grade 3 and grade 4 neutropenia represented from 67.9% to 87% of neutropenia cases. No case of grade 3 and grade 4 thrombocytopenia was noticed. Twenty-two patients respected all the inter-treatment intervals. Adjusted on the other haematological toxicities as a multivariate analysis, neutropenia was significantly associated to non-adherence to chemotherapy (OR: 0.43). Conclusion. Improving availability and access to prevention and treatment for haematological toxicities could lead to improving adherence to anti-cancer chemotherapy

Tartrazina induce genotoxicidad en linfocitos de BALB/c Mus musculus / Tartrazine induces genotoxicity in BALB/c Mus musculus lymphocytes

RESUMEN Objetivos. Determinar el efecto genotóxico de la tartrazina en linfocitos de sangre periférica de Mus musculus BALB/c. Materiales y métodos. Se realizó un estudio experimental, a través de cinco grupos, con cinco ratones en cada uno. Se les registró el peso durante 17 semanas y, en la semana 15 se les administró suero fisiológico (control negativo), dicromato de potasio 25 mg/kg de peso corporal (pc) (control positivo) y tartrazina a dosis de 0,75 mg/kg pc, 7,5 mg/kg pc y 75 mg/kg pc, durante siete días, a excepción del control positivo que fue en dosis única. Luego, cada 24 h se obtuvo una muestra de sangre periférica de la cola y se realizó el frotis, secado y coloración. Posteriormente, se realizó el conteo de 1000 linfocitos por muestra de cada ratón, en todos los tratamientos. Resultados. Los tres tratamientos con tartrazina no causaron diferencias significativas en el peso de ratones a la semana 15, pero sí produjeron diferencias significativas en la frecuencia de linfocitos micronucleados, siendo el tratamiento con tartrazina de 75 mg/kg pc el de mayor efecto genotóxico, induciendo un promedio de 1,63 ± 0,08 linfocitos micronucleados, comparado con el control positivo que generó un promedio de 1,42 ± 0,08 linfocitos micronucleados. Conclusiones. La tartrazina produjo un efecto genotóxico, incrementando el número de linfocitos micronucleados, a dosis de 0,75; 7,5 y 75 mg/kg pc y no afecta el peso corporal durante siete días de administración en M. musculus BALB/c.

ABSTRACT Objectives. To determine the genotoxic effect of tartrazine on peripheral blood lymphocytes of BALB/c Mus musculus. Materials and methods. An experimental study was carried out using five groups, with five mice in each group. Their weight was registered for 17 weeks, and at week 15 they were administered physiological saline solution (negative control), potassium dichromate at 25 mg/kg body weight (bw) (positive control) and tartrazine at doses of 0.75 mg/kg bw, 7.5 mg/kg bw and 75 mg/kg bw, for seven days, with the exception of the positive control which was a single dose. Then, every 24 hours, a peripheral blood sample was obtained from the tail, which was then smeared, dried and stained. Subsequently, 1000 lymphocytes were counted for each sample from each mouse, for all treatment groups. Results. The three tartrazine treatments did not cause significant differences in the weight of mice at week 15, but did produce significant differences in the frequency of micronucleated lymphocytes, with the 75 mg/kg bw tartrazine treatment having the greatest genotoxic effect, inducing an average of 1.63 ± 0.08 micronucleated lymphocytes, compared to the positive control which obtained an average of 1.42 ± 0.08 micronucleated lymphocytes. Conclusions. Tartrazine produced a genotoxic effect, increasing the number of micronucleated lymphocytes, at doses of 0.75; 7.5 and 75 mg/kg bw and did not affect body weight during seven days of administration to BALB/c M. musculus.

Phytochemical composition, antifungal activity, in vitro and in vivo toxicity of Syzygium cumini (L) Skeels leaves extract / Composición fitoquímica, actividad antifúngica, toxicidad in vitro e in vivo del extracto de hojas de Syzygium cumini (L) Skeels

This study determined phytochemical composition, antifungal activity and toxicity in vitro and in vivo of Syzygium cumini leaves extract (Sc). Thus, was characterized by gas chromatography coupled to mass spectrometry and submitted to determination of Minimum Inhibitory (MIC) and Fungicidal concentrations (MFC) on reference and clinical strains of Candida spp. and by growth kinetics assays. Toxicity was verified using in vitro assays of hemolysis, osmotic fragility, oxidant and antioxidant activity in human erythrocytes and by in vivo acute systemic toxicity in Galleria mellonella larvae. Fourteen different compounds were identified in Sc, which showed antifungal activity (MIC between 31.25-125µg/mL) with fungistatic effect on Candida. At antifungal concentrations, it demonstrated low cytotoxicity, antioxidant activity and neglible in vivotoxicity. Thus, Sc demonstrated a promising antifungal potential, with low toxicity, indicating that this extract can be a safe and effective alternative antifungal agent.

Este estudio determinó la composición fitoquímica, la actividad antifúngica y la toxicidad in vitro e in vivo del extracto de hojas de Syzygium cumini (Sc). Así, se caracterizó mediante cromatografía de gases acoplada a espectrometría de masas y se sometió a determinación de Concentraciones Mínimas Inhibitorias (CMI) y Fungicidas (MFC) sobre cepas de referencia y clínicas de Candida spp. y mediante ensayos de cinética de crecimiento. La toxicidad se verificó mediante ensayos in vitro de hemólisis, fragilidad osmótica, actividad oxidante y antioxidante en eritrocitos humanos y por toxicidad sistémica aguda in vivo en larvas de Galleria mellonella. Se identificaron catorce compuestos diferentes en Sc, que mostraron actividad antifúngica (CMI entre 31.25-125 µg/mL) con efecto fungistático sobre Candida. En concentraciones antifúngicas, demostró baja citotoxicidad, actividad antioxidante y toxicidad in vivo insignificante. Por lo tanto, Sc demostró un potencial antifúngico prometedor, con baja toxicidad, lo que indica que este extracto puede ser un agente antifúngico alternativo seguro y eficaz.

Spermic Toxicity Test of Medical Devices for Human Assisted Reproductive Technology / 中国医疗器械杂志

In order to provide a thorough summary and analysis over sperm toxicity evaluation of medical devices for human

Embryonic Toxicity Test of Medical Devices for Human Assisted Reproductive Technology / 中国医疗器械杂志

OBJECTIVE@#To introduce the test methods of embryo toxicity applied to medical devices for human assisted reproductive technology (ARTMD), and provide the evaluation reference.@*METHODS@#The embryo toxicity test methods of ARTMD were summarized, and the key procedures and challenges in their safety evaluation were also discussed.@*RESULTS@#Establishing sensitive and stable test system is important to guarantee the safety and efficacy of ARTMD.@*CONCLUSIONS@#It remains development opportunities in improving sample preparation, extending test technology and expending evaluation method.

Characterization and cytotoxic activity on glial cells of alkaloid-enriched extracts from pods of the plants Prosopis flexuosa and Prosopis nigra (Fabaceae) / Caracterización, y actividad citotóxica en células gliales, de extractos enriquecidos con alcaloides de vainas de las plantas Prosopis flexuosa y Prosopis nigra (Fabaceae)

Introduction: Prosopis spp. pods have shown to be a potential source of protein and energy in livestock. However, prolonged ingestion of some of these species produces neurological symptoms in ruminants. Objective: In the present study, the alkaloid content and the in vitro neurotoxic activity of alkaloid enriched-extracts from P. flexuosa and P. nigra pods were determined in order to elucidate the mechanism of animal poisoning caused by these species. Methods: The main alkaloids present in both extracts were analysed by high performance liquid chromatography-high resolution mass spectrometry (HPLC-HRMS). The cytotoxic activity of Prosopis alkaloid enriched-extracts in primary mixed glial cell culture was assessed by phase contrast microscopy and using neutral red, and lactate dehydrogenase (LDH) activity assays. Results: Juliprosine and juliprosopine were identified in P. flexuosa pods, while the absence of these alkaloids in P. nigra was confirmed. Both extracts (5-30 μg/mL) induced in a dose dependent manner, morphological alterations, such as swelling, enlargement and detachment from the culture surface. Consistent with this, decrease in cell viability and release of LDH 48 hours after exposure, revealed that P. flexuosa pods was significantly more cytotoxic than P. nigra. Conclusions: In P. flexuosa pods, juliprosine and juliprosopine alkaloids were identified for the first time. Moreover, the present study suggests that the cytotoxic effect displayed by both extracts is due to its alkaloid content. However, the presence of piperidine alkaloids in P. flexuosa could explain the greater cytotoxicity on glial cells with respect to P. nigra that was not shown to contain these alkaloids.

Introducción: Las vainas de diversas especies de Prosopis muestran ser una potencial fuente de proteínas y energía para el ganado. Sin embargo, la ingestión prolongada de algunas de estas especies produce síntomas neurológicos en los rumiantes. Objetivo: En el presente estudio se determinó el contenido de alcaloides y la actividad neurotóxica in vitro de los extractos enriquecidos con alcaloides obtenidos en las vainas de P. flexuosa y P. nigra, con el fin de dilucidar el mecanismo de la intoxicación animal causada por estas especies. Métodos: Los principales alcaloides presentes en ambos extractos se analizaron mediante cromatografía líquida de alto rendimiento-espectrometría de masas de alta resolución (HPLC-HRMS). La actividad citotóxica de los extractos enriquecidos con alcaloides de Prosopis se determinó en cultivos primarios de células gliales mixtas y se evaluó mediante microscopía de contraste de fase y utilizando ensayos de actividad de rojo neutro y de deshidrogenasa láctica (LDH). Resultados: Se identificaron la juliprosina y la juliprosopina en las vainas de P. flexuosa, mientras que se confirmó la ausencia de estos alcaloides piperidínicos en P. nigra. Ambos extractos (5-30 μg/mL) indujeron, de manera dependiente a la dosis, alteraciones morfológicas, como hinchazón, agrandamiento y desprendimiento de la superficie de cultivo. En consecuencia, la disminución de la viabilidad celular y la liberación de la LDH después de 48 horas de exposición, reveló que las vainas de P. flexuosa eran significativamente más citotóxicas que las de P. nigra. Conclusiones: El presente estudio muestra la presencia de los alcaloides juliprosina y juliprosopina en vainas de P. flexuosa y sugiere que el efecto citotóxico mostrado por ambos extractos se debe al contenido de alcaloides. Sin embargo, la presencia de estos alcaloides piperidínicos en P. flexuosa podría explicar la mayor citotoxicidad en las células gliales con respecto a P. nigra que no mostró que tuviera estos alcaloides.

A review: Antimicrobial activity and toxicity analysis of the peel of banana, pomegranate, papaya, and citrus fruits (lemon and orange)

ABSTRACT@#Fruits have nutrients and health-promoting compounds and usually fruits are eaten fresh with minimally processed. To meet rising demand, the production and processing of horticultural crops of fruits have grown massively in response to the population and changing dietary habits. It is rarely known that some fruit wastes, including peel, actually have their own advantages to humans as well as industry. In fact, these fruit wastes, including fruit peel, should be handled and used to minimise the environmental impacts. The functional properties of the peel of banana, pomegranate, papaya, and citrus fruits such as lemon and orange can beneficially help in the production of new health products and in food industries. Antimicrobial compounds in fruit peel play an important role in inhibiting the microbial growth, specifically pathogenic microorganisms such as Escherichia coli, Bacillus aureus, Campylobacter, Salmonella, and Staphylococcus aureus. The antimicrobial compounds present in the fruit peel are typically secondary metabolites consisting, in particular, of phenolic compounds, steroids and alkaloids, which give certain functional effects on human health. It has been reported that every fruit peel has its own antimicrobial compounds which are responsible for inhibiting microbial growth. These fruit peel, despite their beneficial effects, have also been shown to have toxicity effects on their consumption depending on the amount of doses used in the implementation. This review covers physiological properties, chemical properties, antimicrobial activity, and the toxicity analysis of the fruit peels from banana, pomegranate, papaya, and citrus fruits.

Efeitos tóxicos dos sedimentos do estuário do rio Capibaribe em embriões de zebrafish (Danio rerio) / Toxic effects of sediments of the Capibaribe estuary on zebrafish embryos (Danio rerio)

O presente estudo utilizou embriões de Danio rerio expostos aos elutriatos dos sedimentos estuarinos do rio Capibaribe, dos períodos chuvoso e seco, e analisou os efeitos letais, teratogênicos, bem como a frequência cardíaca. Os testes de toxicidade com os embriões seguiram as diretrizes da OECD 236. Mediante os resultados obtidos, a frequência cardíaca e a teratogenicidade foram os efeitos mais observados nos animais quando submetidos às amostras. Entre os efeitos teratogênicos, o retardo geral no desenvolvimento dos embriões foi o mais frequente durante as análises. Tais efeitos tóxicos se modificaram entre os pontos e entre os períodos de coleta. Essa variação de toxicidade pode estar relacionada à diversidade de atividades realizadas no entorno desse estuário, a influência do regime de chuvas, marés e correntes, indicando que a análise dos efeitos subletais e da teratogenicidade em embriões de D. rerio constitui bom parâmetro para avaliações de toxicidade de amostras ambientais.(AU)

The present study used Danio rerio embryos exposed to the elutriates of the estuarine sediments of the Rio Capibaribe, from the rainy and dry periods, where the lethal effects, teratogenic and heart rate were analyzed. Embryotoxicity tests followed the guidelines of OECD 236. Based on the results obtained, heart rate and teratogenicity demonstrated higher sensitivity to the samples. Among the teratogenic effects, the general delay in embryo development was the most frequent effect during the analyzes. These toxic effects changed between the points and between the collection periods. This variation of toxicity may be related to the diversity of activities carried out around this estuary, the influence of rainfall, tides, and currents, indicating the analysis of sublethal effects and teratogenicity in the D. rerio embryos are useful parameters for toxic evaluation of environmental samples.(AU)

PEG-PCL Nanocapsules Containing Curcumin: Validation of HPLC Method for Analyzing Drug-loading Efficiency, Stability Testing and Cytotoxicity on NIH-3T3 Cell Line

Abstract Curcumin (CUR) shows potential use for treating cancer. However, CUR has low solubility and reduced bioavailability, which limit its clinical effect. Therefore, the development of nanocarriers can overcome these problems and can ensure the desired pharmacological effect. In addition, it is mandatory to prove the quality, the efficacy, and the safety for a novel nanomedicine to be approved. In that sense, this paper aimed (a) to prepare CUR-loaded polyethylene glycol-poly(ε-caprolactone) nanocapsules; (b) to validate an analytical method by high performance liquid chromatography (HPLC) for quantifying CUR in these nanoformulations; (c) to evaluate the physicochemical stability of these formulations; and to investigate their cytotoxicity on NIH-3T3 mouse fibroblast cells. The HPLC method was specific to CUR in the loaded nanocapsules, linear (r = 0.9994) in a range of 10.0 to 90.0 µg.mL-1 with limits of detection and quantification of 0.160 and 0.480 µg.mL-1, respectively. Precision was demonstrated by a relative standard deviation lower than 5%. Suitable accuracy (102.37 ± 0.92%) was obtained. Values of pH, particle size, polydispersity index, and zeta potential presented no statistical difference (p > 0.05) for CUR-loaded nanoparticles. No cytotoxicity was observed against NIH-3T3 mouse embryo fibroblast cell line using both the tetrazolium salt and sulforhodamine B assays. In conclusion, a simple and inexpensive HPLC method was validated for the CUR quantification in the suspensions of nanocapsules. The obtained polymeric nanocapsules containing CUR showed suitable results for all the performed assays and can be further investigated as a feasible novel approach for cancer treatment.

Investigation of New Benzimidazole Derivative Compounds Effects on A549 Cell Line

Abstract Chronic inflammation is a common indication of several diseases, e.g. asthma, chronic obstructive pulmonary disease (COPD), atherosclerosis, etc. Benzimidazole derivatives are preferable compounds to design new analgesic and anti-inflammatory substances due to their unique biological features. We aimed to investigate the effect of a newly synthesized benzimidazole derivative, ORT-83, on A549 human lung adenocarcinoma cell line. ORT-83 was synthesized, and a non-cytotoxic concentration of ORT-83 on A549 cells was detected with MTT assay. To analyze the anti-inflammatory effect of ORT-83, an inflammatory cell culture model was established by stimulating A549 cell line with IL1-β (10 ng/ml). After 2 hours of treatment with IL1-β to induce inflammation, A549 cells were exposed to ORT-83 (0.78 µg/ml) for 24 hours. Thereafter gene expression analyses were performed with qRT-PCR. We found that ORT-83 significantly suppressed the gene expression levels of the proinflammatory cytokines; IL-6, NFkB, and TNF-α. However, the increased levels of IL-10 (2.8 folds) by IL-1β induction did not change after ORT-83 and/or dexamethasone (Dex: positive control) treatments. While Dex; a COX-2 inhibitor, reduced the COX-2 expression level in inflammatory cells from 10.03 folds to 0.71 folds, ORT-83 reduced its level to 4.37 folds. iNOS expression levels did not change in any experimental groups. In conclusion, we showed that ORT-83 exerted its anti-inflammatory effects by repressing the gene expression of proinflammatory cytokines in the inflammation-induced A549 cell line. Although ORT-83 had a weaker COX-2 inhibitory effect compared to Dex, it was shown to be still a strong anti-inflammatory compound.

Anatomical, Histochemical and Biological Studies of Clusia grandiflora Splitg. (Clusiaceae)

Abstract Clusia grandiflora belongs to an important botanical family which is known for its medicinal value, however there are few reports in literature about the species, highlighting the relevance of this study. Anatomical studies with leaves and stems were performed using traditional techniques. In this investigation it was identified particularities of the species such as the presence of vascular system arranged in an opened arc-shaped with the flexed ends towards the inside of the arch with accessory bundles in the petiole. In histochemical studies, performed with different reagents, alkaloids, phenols substances, carbohydrates and lipids were located. The cytotoxic activity of the extracts was performed by tetrazole salt and showed promising results for ethanolic extracts of stems (IC50 human colon cells of 24.30 μg/ mL) and leaves (IC50 ascites gastric cells of 44.15 μg/ mL), without cell membrane disruption of erythrocytes. The antibacterial activity was evaluated by tryptic soy agar and minimal inhibitory concentration assays and showed positive results for Pseudomonas aeruginosa and Escherichia coli, with better result for adventitious roots (32 μg/ mL and 16 μg/ mL, respectively), stems (64 μg/ mL and 32 μg/ mL, respectively) and leaves (64 μg/ mL and 32 μg/ mL, respectively) ethanolic extracts. Thus, these studies were able to characterize the species and show its potential as promising source of active substances.

Development of a Phytocosmetic Enriched with Pequi (Caryocar brasiliense Cambess) Oil

Abstract The pulp oil of Caryocar brasiliense Camb., better known as pequi, is used in the typical cuisine of the Brazilian Cerrado region. It is also used in folk medicine to combat several types of disease of the respiratory system and skin. However, since its exploration is purely extractive, the exhaustion of this plant is already foreseen. Thus, in order to establish the sustainable use of pequi and contribute to its maintenance, this study aimed to develop a phytocosmetic with antioxidant and photoprotective properties using the oil of this fruit. Initially, the cytotoxicity of the oil was evaluated in order to establish the safety of its use and its fatty acid composition. Then, from the cream enriched with the oil, it was evaluated the antioxidant and photoprotector potentials, quantified the total phenolic content and examined the quality of the formulation. Pequi oil showed high percentages of palmitic (52.11%) and oleic (44.57%) fatty acids and absence of cytotoxicity. The analysis of the cream revealed 168.8 mg of total phenols in gallic acid equivalent per 100 g of oil. The evaluation of antioxidant activity showed an EC50 of 2.921 mg/mL and a capacity of inhibiting the lipoperoxidation process higher than 100%. The obtained sun protection factor was 11.40 at the concentration of 6.25 mg/mL. The quality tests revealed small disturbances in the cream stability that can be solved by further research and improvement of the formulation. The pequi oil can be converted into a phytocosmetic of great commercial value.