Effects of bisphenol A on streptozotocin treated female mice

Bisphenol A (BPA) alters blood glucose homeostasis and is a likely risk factor for diabetes. In this study, we examined the effects of a single BPA dose in adult female mice treated with streptozotocin (STZ) for 13 days under ad libitum conditions. Four groups were used. On day one, groups I and III received sesame oil, and groups II and IV BPA. On the fifth day, and for seven consecutive days, groups I and II received citrate buffer and groups III and IV, STZ. Body weight and biochemical analyses were performed, using histology and hepatic enzymes to evaluate liver injury. Liver mRNA expression for several signaling pathways was studied using real-time PCR. BPA had no adverse effects on weight and biochemical parameters. It did produce a small increase in tail blood glucose levels in STZ mice, as well as liver cytotoxicity and histological changes in other organs. BPA moderately increases the severity of lesions induced by STZ. Both chemicals induced the expression of the peroxisome proliferator-activated receptors (PPAR), although there was no clear effect when the two were combined. The results showed moderate changes in the liver of adult mice treated with STZ and BPA.

Direct effect of p, p'-DDT on mice liver

ABSTRACT Contact with the pesticide dichlorodiphenyltrichloroethane (p,p′-DDT) can be the cause of various harmful effects in humans, wildlife, and the environment. This pesticide is known to be persistent, lipophilic, resistant to degradation, and bioaccumulive in the environment and to be slowly released into bloodstream. Growing evidence shows that exposure to DDT is linked to type 2 diabetes mellitus. Individuals exposed to elevated levels of DDT and its metabolite have an increased prevalence of diabetes and insulin resistance. To evaluate these possible relationships, experiments were performed on eight-week-old female mice, divided into three groups (n = 10 per group): Group 1 received a vehicle-control intraperitoneal (i.p.) injection of sesame oil; Groups 2 and 3 received an i.p. dose of 50 and 100 µg/g p,p′-DDT respectively, dissolved in sesame oil. All groups were treated once daily for four days. Real-time PCR analysis of several genes was undertaken. Additionally, biochemical parameters and histopathological changes were measured. NQO1, HMOX1, NR1I3 and NR3C1 were up-regulated in DDT-exposed animals compared to the vehicle control group, while only SREBP1 was down-regulated in the 100 µg/g group. MTTP and FABP5, not previously reported for DDT exposure, but involved in regulation of fatty acid fluxes, could also function as biomarkers cross-talking between these signaling pathways. These results suggest that beyond epidemiological data, there is increasing molecular evidence that DDT may mimic different processes involved in diabetes and insulin resistance pathways.

RESUMO O contato com o praguicida diclorodifeniltricloroetano (p, p'-DDT) pode ser a causa de vários efeitos nocivos sobre os seres humanos, animais silvestres e o meio ambiente. Sabe-se de sua característica de bioacumulação, ser altamente persistente no meio ambiente, lipofílico, resistente à degradação e lentamente liberado na corrente sanguínea. Existe uma evidência crescente de que a exposição ao DDT pode ser ligada a Diabetes mellitus tipo 2. Os indivíduos expostos a níveis elevados de DDT e seu metabólito apresentam maior prevalência de diabetes e resistência à insulina. A fim de obter informações sobre essas possíveis relações, camundongos fêmeas de oito semanas de idade foram divididos em três grupos (n = 10 por grupo): Grupo 1 recebeu um veículo de óleo de gergelim via i.p.; os Grupos 2 e 3 receberam, via i.p., 50 e 100 µg/g de p, p'-DDT, respectivamente, dissolvidos em óleo de gergelim. Todos os grupos foram tratados uma vez ao dia durante quatro dias. Além da análise de PCR em Tempo Real de vários genes, os parâmetros bioquímicos e alterações histopatológicas também foram medidos. A expressão gênica do mRNA dos genes NQO1, HMOX1, NR1I3 e NR3C1 foi maior nos animais expostos ao DDT, em comparação ao grupo controle, enquanto a expressão gênica do SREBP1 diminuiu na concentração de 100 µg/g. Os genes MTTP e FABP5 envolvidos na regulação do fluxo de ácidos graxos, embora não estudados quanto à exposição ao DDT, também podem funcionar como biomarcadores de resposta cruzada entre essas vias de sinalização. Esses resultados sugerem que, além de dados epidemiológicos, há cada vez mais evidências moleculares de que o DDT poderia, de fato, imitar diferentes processos que envolvem as rotas de diabetes e de resistência à insulina.

Potential interaction of components from essential oils with dengue virus proteins / Potencial interacción de componentes de aceites esenciales con proteínas del virus del dengue

An antiviral drug for treatment of dengue is an urgent necessity. In this study in silico activities of essential oils components on dengue virus (DENV) were evaluated, and beta-Caryophyllene was subjected to biological examination to assess inhibition of DENV-2 replication. Components previously optimized were coupled with viral proteins prepared, using AutoDock Vina. Theoretical affinity values varied between -4.0 and -7.3 kcal/mol. alpha-copaene, beta-bourbonene, germacrene D, spathulenol, beta-caryophyllene, caryophyllene oxide and (+)- epi-bicyclosesquiphellandrene showed the greatest interaction with viral proteins. beta-caryophyllene inhibits DENV-2 in vitro (50 percent inhibitory concentration [IC50] = 22.5 +/- 5.6 uM [4.6 +/- 1.1 ug/mL] and resulted non-cytostatic with a selectivity index value of 71.1. The in silico results permit infer that DENV proteins are potential targets for the concomitant docking of various essential oils components. Biological examination suggest that beta-caryophyllene acts on very early steps of the viral replication cycle and it might prove virucidal.

Una droga antiviral para tratamiento del dengue es una necesidad urgente. En este estudio se evaluó la actividad in silico de componentes de aceites esenciales sobre el virus del dengue (VDEN) y el beta-cariofileno se seleccionó para evaluar la inhibición sobre la replicación in vitro del VDEN-2. Los componentes previamente optimizados fueron acoplados con proteínas virales preparadas, utilizando AutoDock Vina. Los valores de afinidad variaron entre -4.0 and -7.3 kcal/mol. alfa-Copaeno, beta-bourboneno, germacreno D, spatulenol, beta- cariofileno, óxido de cariofileno y (+)-epi-biciclosesquifellandreno presentaron la mayor interacción con las proteínas virales. beta-Cariofileno inhibió VDEN-2 in vitro (Concentración inhibitoria 50 [IC50] = 22.5 +/- 5.6 uM [4.6 +/- 1.1 ug/mL] y resultó no-citostático con índice de selectividad de 71.1. Los resultados in silico indican que proteínas del VDEN son blancos potenciales para varios componentes. El análisis biológico sugiere que el beta-cariofileno actúa en etapas tempranas de la replicación viral y podría ser virucida.

Composition, anti-quorum sensing and antimicrobial activity of essential oils from Lippia alba

Many Gram-negative pathogens have the ability to produce N-acylhomoserine lactones (AHLs) as signal molecules for quorum sensing (QS). This cell-cell communication system allows them to coordinate gene expression and regulate virulence. Strategies to inhibit QS are promising for the control of infectious diseases or antibiotic resistant bacterial pathogens. The aim of the present study was to evaluate the anti-quorum sensing (anti-QS) and antibacterial potential of five essential oils isolated from Lippia alba on the Tn-5 mutant of Chromobacterium violaceum CV026, and on the growth of the gram-positive bacteria S. aureus ATCC 25923. The anti-QS activity was detected through the inhibition of the QS-controlled violacein pigment production by the sensor bacteria. Results showed that two essential oils from L. alba, one containing the greatest geranial:neral and the other the highest limonene:carvone concentrations, were the most effective QS inhibitors. Both oils also had small effects on cell growth. Moreover, the geranial/neral chemotype oil also produced the maximum zone of growth inhibition against S. aureus ATCC 25923. These data suggest essential oils from L. alba have promising properties as QS modulators, and present antibacterial activity on S. aureus.

Aspectos epidemiológicos de la diabetes mellitus y su relación con los contaminantes ambientales / Epidemiological aspects of diabetes mellitus and its relationship with enviromental pollutants

Biochemical processes involving insulin and its receptor are responsible for regulating carbohydrate and fat metabolism. Disruption of these signaling pathways could lead to obesity, insulin resistance and diabetes, among other health problems. Diabetes has a global impact and its high prevalence has been associated with genetic and environmental factors. Recently, there has been a strong interest in establishing the relationship between type II diabetes and exposure to environmental contaminants, particularly persistent organic pollutants (POPs). This association has is based on epidemiological evidence and results from in vitro and in vivo experiments. In this review, the authors present some of the epidemiological aspects of diabetes, the biochemical pathways involved in insulin action, and how these environmental toxicants have impacted on population, through diverse mechanisms, to produce this disease. While several authors consider that the etiology of diabetes has a very important component derived from exposure to environmental pollutants, it is clear that there is still a substantial amount of work to develop in order to identify cause-effect relationships and the mechanisms involved.

Los procesos bioquímicos que involucran la insulina y su receptor son los responsables de regular el metabolismo de carbohidratos y grasas. La alteración de estas vías de señalización puede conllevar a obesidad, resistencia a la insulina y diabetes, entre otros problemas de salud. La diabetes impacta a nivel global y su alta prevalencia ha sido asociada con factores genéticos y ambientales. Recientemente ha surgido un amplio interés por establecer la relación existente entre la diabetes tipo 2 y la exposición a contaminantes ambientales, en especial los compuestos orgánicos persistentes (COPs). Esta asociación está basada en evidencia epidemiológica y resultados de experimentos in vitro e in vivo. En esta revisión los autores presentan algunos de los aspectos epidemiológicos de la diabetes, las rutas bioquímicas que participan en la acción de la insulina, y como estos tóxicos ambientales han impactado sobre la población, a través de diversos mecanismos, para producir esta enfermedad. Si bien algunos autores consideran que la etiología de la diabetes tiene un componente importante derivado de la exposición a contaminantes ambientales, es claro que aún falta mucho por desarrollar para identificar verdaderas relaciones causa-efecto y los mecanismos involucrados.

Chemical composition and bioactivity of Piper auritum and P. multiplinervium essential oils against the red flour beetle, Tribolium castaneum (Herbst) / Composición química y bioactividad de los aceites esenciales de Piper auritum y P. multiplinervium contra el escarabajo rojo de la harina, Tribolium castaneum (Herbst)

Stored grain insects have shown resistance to synthetic insecticides, fact that has promoted the use of vegetable species for integrated pest management. Piper auritum and P. multiplinervium are two plants from the Piperaceae family present in the department of Chocó, Colombia, one of the most important hot spots of biodiversity in the world. This study was conducted to determine the repellent activity and toxicity of essential oils (EOs) isolated from these plants against Tribolium castaneum, using the area preference and contact toxicity methods, respectively. P. auritum EO presented greater repellency than P. multiplinervium, the first showed 100 percent lethality at minimum tested exposure period (24 h) whereas the second reached 16 percent at 72 h. EOs were analyzed by gas chromatography-mass spectrometry. P. auritum major components were safrole (93.2 percent) and miristicine (4.3 percent), whereas for P. multiplinervium were beta-elemene (9.0 percent), trans-beta-caryophyllene (5.3 percent) and caryophyllene oxide (4.1 percent). It is speculated that the repellent effect of P. auritum may be related to its safrole content, a known repellent. These results evidenced Piper species could be used for development of repellents against T. castaneum.

Los insectos de los granos almacenados han mostrado resistencia a los insecticidas sintéticos, hecho que ha promovido el uso de especies vegetales para el manejo integrado de plagas. Piper auritum y P. multiplinervium son dos plantas de la familia Piperaceae presentes en el departamento del Chocó, Colombia, uno de los puntos de biodiversidad más importantes del mundo. En este estudio fue determinada la actividad repelente y toxicidad de los aceites esenciales (AE) aislados de estas plantas contra Tribolium castaneum, utilizando el método de área de preferencia y toxicidad por contacto, respectivamente. El AE de P. auritum presentó mayor repelencia que el de P. multiplinervium, el primero mostró 100 percent de letalidad al menor tiempo de exposición (24 h), mientras que el segundo alcanzó el 16 percent a las 72 h. Los AEs fueron analizados por cromatografía de gases-espectrometría de masas. Los componentes principales de P. auritum fueron safrol (93.2 percent) y miristicina (4.3 percent), mientras que para P. multiplinervium fueron beta-elemene (9.0 percent), trans-beta-cariofileno (5.3 percent) y óxido de cariofileno (4.1 percent). Se cree que el efecto repelente de P. auritum puede estar relacionado con su contenido de safrol, un repelente conocido. Estos resultados evidencian que las especies de Piper podrían ser utilizadas para el desarrollo de repelentes contra T. castaneum.

Búsqueda en bases de datos de actividad biológica de moléculas quinoides / Database search on biological activity of quinoid molecules

Introducción: las quinonas son moléculas biológicas ampliamente distribuidas en la naturaleza. Recientemente el grupo de investigación de productos naturales, de la Universidad de Cartagena; obtuvo por extracción de plantas del género tabebuia y por síntesis química un número importante de estos compuestos. Sin embargo, con el fin de seguir profundizando en los estudios de sus actividades y su relación con el tipo de estructura lineal o angular se realizó una revisión en varias bases de datos. Objetivo: buscar información que permitiera conocer si los compuestos obtenidos se encontraban reportados; así como también la actividad biológica y los bioensayos realizados a estas moléculas in vivo, in vitro e in silico. Métodos: esta investigación fue desarrollada con el uso de un diseño que aplicó la edición de moléculas, mediante la interfaz gráfica de servidores (PUBCHEM CHEMIDPLUS ADVANCE, CHEBI) y una búsqueda de datos complementarios en la base de datos PUBMED. Los datos de la actividad biológica más relevantes fueron relacionados con la estructura química de los compuestos sintetizados y de los análogos suministrados por PUBMED. Resultados: de los compuestos hallados en las bases de datos, 24 presentaron código en la base de datos PUBCHEM, 12 mostraron reportes de actividad biológica en las bases de datos, y se encontró que el mayor número de bioensayos fue reportado con furanonaftoquinonas, seguido por naftoquinonas. Conclusiones: la actividad citotóxica y anticancerígena en diferentes líneas celulares, representa el mayor número de bioensayos realizados a estos compuestos.

Introduction: quinones are biological molecules widely distributed on the nature. Recently the group of natural products of the University of Cartagena (Colombia) obtained by extraction of plants of genus tabebuia and by chemistry synthesis an important number of these compounds. However with the purpose of made more detailed studies about the biological activity and structural type reported for these compounds, (naphtoquinone and furanonaphtoquinone linear o angular) reviewed in several database. Objective: search information that allows us to know 1) The compounds were already registered 2) Biological activity and bioassay performed to these molecules, in vivo, in vitro and in silico. Methods: this research was developed using a design of review than involved the edition of molecules by a graphic interface of server (PUBCHEM CHEMIDPLUS ADVANCE, CHEBI) and supplementary data search in PUBMED database. The most relevant data about biological activity was related with chemical structure of the synthesized compounds and their analogues obtained from databases. Results: the compounds tested on the database, 24 were already on PUBCHEM database, 12 molecules show reports of biological activity on the databases. Founding that bigger number of bioassays was reported with furanonaphtoquinones, followed by naphtoquinones. Conclusion: the cytotoxic and anticancer activity in cell lines of different type, represent the most of performed bioassay.

Chemical control of Aedes aegypti: a historical perspective / Control químico de Aedes aegypti: una perspectiva histórica

Objective: To describe the use of chemical insecticides throughout history as the main tool to fight against Aedes aegypti, a vector of dengue virus. Methods: A text mining approach was conducted on databases, such as PUBMED and SCIENCE DIRECT, using the keywords “Aedes aegypti”, combined with the words “insecticides”, “resistance”, “organochlorines”, “organophosphates”, “carbamates” and “pyrethroids”. Results related to historical information dealing with the chemical control of Aedes aegypti, in particular those containing data on insecticide resistance for this species, were scrutinized and analyzed. Results: Different chemical groups have been utilized to control A. aegypti, including organochlorine, organophosphate, carbamate and pyrethroid insecticides. In general, the tendency has been to replace a particular pesticide, for which resistance had been detected, for a new one, mosquito-sensitive, and with little evidence of deleterious effects derived from its use. The spread of resistance has been registered in several countries of America, Asia and Africa. Two mechanisms have been highly cited to be responsible for the resistance; the increase activity of detoxifying enzymes, and structural changes in the insecticide target site, mostly within the central nervous system. Conclusion: Excessive use of chemical insecticides and the lack of dosing control have led to widespread resistance in A. aegypti, as no “safer” alternative chemical options are available for vector control in different countries, impacting human health.

Objetivo: Describir el uso de insecticidas químicos a través de la historia como la principal herramienta contra Aedes aegypti, un mosquito vector del virus del dengue. Métodos: Una búsqueda en minería de textos fue realizada en bases de datos como PubMedy Science Direct, utilizando las palabras clave “Aedes aegypti”, en combinación con “insecticidas”, “resistencia”, “organoclorados”, “organofosforados”,“carbamatos” y “piretroides”.Resultados afines con la información histórica relacionada con el control químico del mosquito Aedes aegypti, en particular las que contienen datos sobre la resistencia a insecticidas de esta especie, fueron examinados y analizados. Resultados: Diferentes grupos químicos han sido desarrollados para el control de A. aegypti, siendo los más utilizados organoclorados, organofosforados, carbamatos y piretroides. En general, la tendencia ha sido la de sustituir un pesticida particular, para el que ha sido detectado resistencia, por uno nuevo, mosquito-sensible, y con evidencia de efectos perjudiciales derivados de su uso. La propagación de la resistencia se ha registrado en varios países de América, Asia y África. Dos mecanismos han sido altamente referenciados de ser responsable de la resistencia, el aumento de actividad de las enzimas de desintoxicación, y los cambios estructurales en el sitio de destino de los insecticidas, en su mayoría dentro del sistema nervioso central. Conclusión: El uso excesivo de insecticidas químicos y la falta de control de dosificación han dado lugar a una resistencia generalizada en Aedes aegypti, y alternativas químicas “más seguras” no están disponibles para el control de vectores en diferentes países, afectando la salud humana.

New agents with potential leishmanicidal activity identified by virtual screening of chemical databases: New agents with potential leishmanicidal activity / Nuevos agentes con potencial actividad leishmanicida identificados mediante tamizaje virtual

Introduction and Objectives: Leishmaniosis, a disease caused by a protozoan parasite, remains a serious public health problem threatening about 350 million people around the world, of which 12 million are believed to be currently infected (WHO 2010). To date, there are no vaccines against the species of parasites and the treatment is based only on chemotherapy with toxic-, expensive- and inefficient- drugs. There is an urgent need for better drugs against Leishmania, the etiological agent of the disease. The main anti-leishmanial drug used in Colombia is meglumineantimoniate [chemical name according to the International Union of Pure and Applied Chemistry (IUPAC): Hydroxy-dioxostiborane; (2R,3R,4R,5S)- 6-methylaminohexane-1,2,3,4,5-pentol, (C7H17NO5)], which is not efficient in the treatment of infections caused by Leishmania braziliensis, the most prevalent specie in the Caribbean coast of Colombia. Methods: We performed an in silico virtual screening of several datasets including ChemBridge and Pubchem. We virtually screened a total of 28.755 compounds against a 3D model of 6-phosphoglucono -lactonase (6-PGL) from Leishmania braziliensis to identify novel inhibitors.Molecular docking of databases was performed using the software Sybyl 8.0 and AutoDockVina. Results: The initial virtual screening using a structure-based method identified 10 compounds, which were later tested with AutodockVina and classified according to their docking scores. Conclusions: These novel and potential inhibitors constitute new drug candidates that must be biologically tested to define their value as an alternative chemotherapeutic agent in the treatment of these protozoan infections. Salud UIS 2013; 45 (1): 33-40.

Introducción y Objetivos: Leishmaniosis, una enfermedad causada por un parásito protozoario, representa un serio problema de salud pública que amenaza a cerca de 350 millones de personas alrededor del mundo, de los cuales se cree que unos 12 millones se encuentran actualmente infectados (WHO 2010). A la fecha no existen vacunas contra las especies del parásito y el tratamiento está basado solo en la quimioterapia con medicamentos tóxicos, costosos, e ineficientes. Existe una necesidad urgente por mejores medicamentos contra Leishmania, el agente etiológico de la enfermedad. El principal medicamento en Colombia usado contra la leishmaniosis es el antimoniato de meglumine [nombre químico según los parámetrosde la International Union of Pure and Applied Chemistry (IUPAC): Hydroxy-dioxostiborane; (2R,3R,4R,5S)-6- methylaminohexane-1,2,3,4,5-pentol, (C7H17NO5)], el cual no es eficiente en el tratamiento de infecciones causadas por Leishmania braziliensis, la especie más prevalente en la costa Caribe de Colombia. Métodos: En este trabajo efectuamos un tamizaje virtual in silico de varias bases de datos incluyendo ChemBridge y Pubchem. Con el objetivo de identificar nuevos inhibidores, un total de 28.755 compuestos fueron tamizados virtualmente contra un modelo 3D de la enzima 6-phosphoglucono -lactonase (6-PGL) de Leishmania braziliensis. El acoplamiento molecular de las bases de datos se efectuó con el programa Sybyl 8.0 y AutoDock Vina. Resultados: mediante tamizaje virtual basado en la estructura se identificaron10 compuestos, los cuales fueron posteriormente evaluados con AutodockVina y clasificados de acuerdo a los puntajes de acoplamiento. Conclusiones: Estos nuevos potenciales inhibidores constituyen candidatos a medicamentos que deben ser evaluados biológicamente para definir su valor como alternativas quimioterapéuticas en el tratamiento de estas infecciones parasíticas. Salud UIS 2013; 45 (1): 33-40.

Relación entre la composición química y la actividad antioxidante del aceite esencial de Ocimum basilicum L. cultivado bajo diferentes tratamientos de fertilizante / Relationship between the chemical composition and the antioxidant activity of essential oil of Ocimum basilicum L. grown under different fertilizer treatments

Introducción: la albahaca, Ocimum basilicum L. (Lamiaceae), es originaria del Asia meridional, principalmente de la India. Esta planta es conocida por sus propiedades medicinales. El aceite esencial es utilizado para el tratamiento de la depresión y otros problemas neurológicos, es considerada como una especie promisoria en cuanto al aprovechamiento industrial de su aceite esencial. Objetivos: determinar las variaciones en el rendimiento, la composición química y actividad antioxidante del aceite esencial de Ocimum basilicum L., cultivada bajo distintos tratamientos de fertilizante. Métodos: plantas de Ocimum basilicum L. se cultivaron bajo 3 tratamientos de fertilización diferentes. Un grupo control sin fuente orgánica o inorgánica, y 2 con diferentes concentraciones de fuente orgánica pero con la misma de inorgánica. El aceite esencial de las plantas adultas se obtuvo mediante destilación por arrastre con vapor y su composición química se determinó por cromatografía de gases acoplada a espectrometría de masas. La actividad antioxidante del aceite se midió usando el ensayo de 1,1-difenil-2-picrilhidrazilo. Las comparaciones entre medias de diferentes grupos se hicieron utilizando ANOVA. Resultados: el rendimiento del aceite esencial no fue influenciado por el tratamiento con fertilizantes, este presentó alta proporción de compuestos aromáticos (estragol y eugenol) y monoterpenos oxigenados (linalool y eucaliptol). Hubo variación significativa en el contenido de eugenol y en la actividad antioxidante del aceite esencial de acuerdo con el tratamiento de fertilización. Conclusiones: de acuerdo con la composición química, el aceite esencial de Ocimum basilicum es clasificado como de quimiotipo egipcio. Su actividad antioxidante in vitro hace de esta planta una fuente interesante para su aplicación como antioxidante natural, en particular, cuando es cultivada sin aplicación de fertilizante.

Introduction: Ocimum basilicum L. (Lamiaceae) known as albahace, is native from southern Asia, mainly from India.This plant is known for its medicinal properties. The essential oil is used to treat depression and other neurological problems, being considered as a promising species in terms of the industrial utilization of that oil. Objectives: to determine variations in yield, chemical composition and antioxidant activity of the essential oil of Ocimum basilicum L., grown under distinct fertilizer treatments. Methods: Ocimum basilicumL. plants were grown under three different fertilizer treatments. A control group without organic or inorganic source, and two groups with different concentrations of organic sources but with the same concentration of inorganic source. The essential oil of adult plants was obtained The steam distillation served to obtain the adult plant's essential oil and the gas chromatography coupled to mass spectrometry method determined its chemical composition. The antioxidant activity was measured using the 1,1-diphenyl-2-pycrilhydrazil assay. The comparisons of the means of the three groups were made with ANOVA. Results: the yield of the essential oil was not influenced by the fertilizer treatment. It showed high proportion of aromatic compounds (estragole and eugenol) and oxygenated monoterpenes (linalool and eucalyptol). There was significant variation in the content of eugenol and in the antioxidant activity according to the fertilizer treatment. Conclusions: according to the chemical composition, the essential oil of Ocimum basilicum is classified as the Egyptian chemotype. The in vitro antioxidant activity of the essential oil makes this plant an interesting natural antioxidant, in particular, when it is grown without fertilizer.

Perfil de la expresión génica en células sanguíneas aisladas de carpinteros expuestos a solventes orgánicos en Sucre (Colombia) / Gene expression profile in blood cells isolated from carpenters exposed to organic solvents in Sucre (Colombia)

Resumen Objetivo: El objetivo de este estudio fue evaluar la expresión de genes asociados con estrés oxidativo, inflamación y daño al ácido desoxirribonucleico (ADN) en trabajadores de carpinterías en Sucre (Colombia). Materiales y métodos: Aleatoriamente fueron seleccionados 41 individuos de sexo masculino: 28 expuestos y 13 controles, con edades entre 32.3±7.9 y 33.2±8.4 años, respectivamente. Se colectaron muestras de sangre periférica y se realizaron análisis hematológicos y de marcadores de daño hepático. En 24 individuos expuestos y 10 controles se realizó análisis de expresión génica para marcadores de estrés oxidativo, inflamación y daño al ADN usando reacción en cadena de la polimerasa en tiempo real. Resultados: Los parámetros hematológicos y de daño hepático estuvieron dentro de los valores de referencia. La expresión génica de la P53 y BCL-2, genes asociados con el daño al ADN, fue significativamente mayor para el grupo expuesto en comparación con el grupo control. Conclusión: En ausencia de cambios en marcadores hematológicos o de daño hepático, personas expuestas a solventes en Sucre tienen niveles de expresión elevados para los genes P53 y BCL-2. Estos genes podrían ser candidatos útiles como biomarcadores moleculares relacionados con la exposición a solventes.

Abstract Objective: The aim of this study was to evaluate the expression of genes related to oxidative stress, inflammation and deoxyribonucleic acid (DNA) damage in carpentry workers from Sucre, Colombia. Materials and methods: 41 male individuals were randomly selected, 28 exposed and 13 controls, with ages 32.3 ± 7.9 and 33.2 ± 8.4 years old, respectively. Peripheral blood samples were collected and used for hematological and liver damage markers analysis. Gene expression analysis for oxidative stress, inflammation and DNA markers was performed using Real-Time Polymerase Reaction on 24 exposed and 10 controls. Results: Hematological parameters and liver damage markers were found within the reference values. Gene expression of P53 and BCL-2, genes related to DNA damage, was significantly greater for the exposed group when compared with the control group. Conclusion: In the absence of hematological or hepatic damage markers, individuals exposed to solvents in Sucre have increased gene expression for P53 and BCL2. These genes may be useful candidates as molecular biomarkers related to solvent exposure.

Chemical composition and antioxidant activity of essential oils isolated from Colombian plants / Composição química e atividade antioxidante de óleos essenciais isolados de plantas da Colombia

Treze óleos essenciais de plantas da Colômbia, obtido por hidrodestilação ou hidrodestilação assistida por microondas, da planta inteira, caule, folhas e flores, foram analisados por técnicas de espectrometria de massa acoplada a cromatografia gasosa. Foi avaliada a citotoxicidade de óleos essenciais utilizando o ensaio com Artemia salina e suas atividades antioxidantes medindo seus efeitos sobre os níveis de substâncias reativas ao ácido tiobarbitúrico em microssomas de fígado de rato induzida por Fe2+/H2O2. Cinco óleos apresentaram alta citotoxicidade (LC50<10 µg/mL) sobre o ensaio de Artemia salina. A atividade antioxidante do óleo essencial de Ocotea sp., Tagetes lucida e Lippia alba (quimiotipo geranial) apresentaram os menores valores de Concentração Eficaz (CE50), na ordem de 31,1, 37,9 e 94,9 µg/mL, respectivamente. Os principais componentes desses óleos foram α-pineno (42 por cento), estragol (95,7 por cento) e geranial (30,4 por cento), respectivamente. Elettaria cardamomum e Lippia alba (quimiotipo carvona, Tolima) apresentaram moderada atividade antioxidante com valores de CE50 de 130,5 e 174,4 µg/mL, respectivamente. Os óleos essenciais de mollis Minthostachys mollis, Lippia alba (quimiotipo carvona, Cundinamarca), e Piper sanctifelisis não mostraram atividade antioxidante (CE50>1000 µg/mL).

Thirteen essential oils from Colombian plants, obtained by hydrodistillation or microwave-assisted hydrodistillation of total plant, stem, leaves, and flowers were analyzed by gas-chromatography-mass spectrometry techniques. Cytotoxicity of essential oils was assessed using the brine shrimp assay, and their antioxidant activities measuring their effects on the levels of thiobarbituric acid reactive substances on rat liver microsomes induced by Fe2+/H2O2. Five oils showed high cytotoxicity (LC50<10 µg/mL) on the brine shrimp assay. The antioxidant activity of the essential oil from Ocotea sp., Tagetes lucida and Lippia alba (geranial chemotype) showed the lowest mean effective concentrations (EC50), with values of 31.1, 37.9 and 94.9 µg/mL, respectively. The main components for these oils were α-pinene (42 percent), estragole (95.7 percent) and geranial (30.4 percent), respectively. Elettaria cardamomum and Lippia alba (carvone chemotype, Tolima) presented moderate antioxidant activities with EC50 values of 130.5 and 174.4 µg/mL, respectively. Essential oils from Minthostachys mollis, Lippia alba (carvone chemotype, Cundinamarca), and Piper sanctifelisis did not show antioxidant activity (CE50>1000 µg/mL).

Toxicity of the essential oil of the cytral chemotype of Lippia alba (Mill.) N. E. Brown

The essential oil (EO) of Lippiaalba (Mill.) N. E. Brown (Verbenaceae) has been traditionally used to treat several diseases. In this study, the acute toxic effects of the citral chemotype of L. alba EO were evaluated in mice. Animals were treated via intraperitoneal receiving the L. alba essential oil at doses between 50 and 2500 mg/kg, and the control group received sesame oil (vehicle). The EO induced dose-dependent neurotoxic effects at doses greater than 1000 mg/kg, including decreased locomotion, motor skills and muscle strength, hypotonia, dyspnea, kyphosis and convulsions. The EO was lethal at a dose of 2500 mg/kg. Animals receiving 1000 mg/kg were euthanized at the end of the treatment period and their blood and livers were collected for analysis. Mice exposed to L. alba EOpresented significantly greater plasma alanine aminotransferase (ALT) activities than the control group. Liver histological changes included mild inflammation, in particular, an increase in nuclear size. Compared to vehicle control group, changes in expressionfor selected genes were significant for FABP5, a fatty acid transport related gene. In summary, the intraperitoneal administration of L. alba EO (citral chemotype) causes neurological damage in mice at doses equal or greater than 1500 mg/kg, whereas at 1000 mg/kg, it generates mild liver damage. Therefore, the systemic use of this EO raises concerns about its safety.

El aceite esencial (AE) de Lippia alba(Mill.) NE Brown (Verbenaceae) ha sido utilizado tradicionalmente para tratar varias enfermedades. En este estudio, los efectos tóxicos agudos del AE de Lippia alba quimiotipo citral fueron evaluados en ratones. Los animales fueron tratados por vía intraperitonealrecibiendo el AE en dosis entre 50 y 2500 mg/kg de peso, y el grupo control aceite de sésamo (vehículo). Dosis superiores a 1000 mg/kg del AE mostraron efectos neurotóxicos incluyendo disminución de la locomoción e hipotonía, disnea, cifosis y convulsiones. El AE fue letal a la dosis de 2500 mg/kg. Veinticuatro horas después de que los animales fueron tratados con 1000 mg/kg del AE se les realizó eutanasia y su sangre e hígado fueron recolectados para análisis. Los ratones expuestos al AE de L. alba, presentaron actividad alanina aminotransferasa (ALT) en plasma significativamente mayor que el grupo control. Dentro de los cambios histológicos hepáticos se incluyen inflamación leve, en particular, un aumento del tamaño nuclear. En comparación con el grupo control, la expresión de genes seleccionados tuvo diferencias significativas para FABP5, un gen relacionado con el transporte de ácidos grasos. En conclusión, la administración intraperitoneal del AE de L. alba (quimiotipo citral) causa dañosneurológicos en ratones a una dosis igual o superior a 1500 mg/kg, mientras que a 1000 mg/kg, genera daño hepático leve. Por lo tanto, el uso sistémico de este AE plantea preocupaciones en cuanto a su seguridad.

Actividad repelente de los aceites esenciales de Lippia origanoides, Citrus sinensis, y Cymbopogon nardus cultivadas en Colombia frente a Tribolium castaneum, Herbst / Repellent activity of the essential oils from Lippia origanoides, Citrus sinensis, and Cymbopogon nardus cultivated in Colombia against Tribolium castaneum, Herbst

Objetivo: El objetivo de este estudio fue evaluar la actividad repelente de tres aceites esenciales (AE) y un repelente comercial frente a la especie Tribolium castaneum, Herbst, una de las principales plagas de cereales y productos almacenados. Materiales y métodos: La actividad repelente fue medida utilizando el método de área de preferencia, además fue determinada la concentración de aceite esencial capaz de repeler el 50% de los insectos (CR50). La prueba T pareada fue utilizada para encontrar diferencias significativas entre el número de insectos presentes en las áreas tratadas y no tratadas. Resultados: Todos los AEs mostraron actividad repelente contra T. castaneum, y la magnitud del efecto fue dependiente de la concentración utilizada. Los AE con mayor repelencia fueron los extraídos de Lippia origanoides y Citrus sinensis, mientras que el aceite con menor actividad fue el de Cymbopogon nardus. Discusión: Aunque en términos de CR50 el AE de C. nardus mostró actividad repelente inferior a la de L. origanoides y C. sinensis, el primero presentó una eficacia superior a la del producto comercial IR3535. Estos AEs han mostrado propiedades repelentes frente a organismos diferentes a T. castaneum, lo cual sugiere que su espectro de acción es amplio. Conclusiones: Los resultados han demostrado que los AEs de la flora colombiana son una fuente importante de repelentes, por lo que podrían ser usados para el control biológico de insectos.

Objective: The aim of this study was to evaluate the repellent activity of three essential oils (EO), and a commercial repellent against species Tribolium castaneum Herbst, a major pest of grain and stored products. Materials and methods: The repellent activity was measured using the area of preference method, as well as the concentration of essential oil that is capable of repelling 50% of the insects (RC50). A paired T test was used to find significant differences between the number of insects present in the treated and untreated areas. Results: All EOs showed repellent activity against T. castaneum, and the magnitude of the effect was dose-dependent. The AE with the highest repellence were those extracted from Lippia origanoides and Citrus sinensis, whereas the one with the lowest activity was that from Cymbopogon nardus. Discussion: Although in terms of RC50 the EO from C. nardus showed repellent activity lower than those registered for L. origanoides and C. sinensis, the first had a greater efficacy than that showed by the commercial product IR3535. These Eos have shown repellent properties against organism different from T. Castaneum, suggesting that they have a wide spectrum of action. Conclusions: The results have shown that EOs from Colombian flora are an important source of repellents, which could be used for biological control of insects.