Pharmacokinetics and Biological Activity of Cucurbitacins.

Cucurbitacins are a class of secondary metabolites initially isolated from the Cucurbitaceae family. They are important for their analgesic, anti-inflammatory, antimicrobial, antiviral, and anticancer biological actions. This review addresses pharmacokinetic parameters recently reported, including absorption, metabolism, distribution, and elimination phases of cucurbitacins. It includes recent studies of the molecular mechanisms of the biological activity of the most studied cucurbitacins and some derivatives, especially their anticancer capacity, to propose the integration of the pharmacokinetic profiles of cucurbitacins and the possibilities of their use. The main botanical genera and species of American origin that have been studied, and others whose chemo taxonomy makes them essential sources for the extraction of these metabolites, are summarized.

Amphipterygium adstringens (Schltdl.) Schiede ex Standl (Anacardiaceae): An Endemic Plant with Relevant Pharmacological Properties.

Diseases, such as cancer, peptic ulcers, and diabetes, as well as those caused by drug-resistant infectious agents are examples of some of the world's major public health problems. Amphipterygium adstringens (Schltdl.) Schiede ex Standl is an endemic tree to Mexico. Its stem bark has been used medicinally since pre-Hispanic times, but in recent decades it has been scientifically proven that it has properties that help counteract some diseases; extracts with organic solvents of the plant are outstanding for their anticancer, gastroprotective, and antimicrobial properties; terpenes and long-chain phenols have been identified as the main active compounds. Currently, overharvesting is causing a sharp reduction in natural populations due to an increase in demand for the stem bark by people seeking to improve their health and by national and transnational companies seeking to market it. Because of the growing interest of the world population and the scientific community, we reviewed recent studies on the bioactive properties of A. adstringens. Through the orderly and critical compendium of the current knowledge of A. adstringens, we provide a reference for future studies aimed at the rational use and protection of this valuable endemic natural resource.

Use of Gamma Radiation for the Genetic Improvement of Underutilized Plant Varieties.

Agricultural biodiversity includes many species that have biological variants (natives, ecotypes, races, morphotypes). Their use is restricted to local areas because they do not fulfill the commercial requirements; however, it is well documented that these species are a source of metabolites, proteins, enzymes, and genes. Rescuing and harnessing them through traditional genetic breeding is time-consuming and expensive. Inducing mutagenesis may be a short-time option for its genetic improvement. A review of outstanding research was carried out, in order to become familiar with gene breeding using gamma radiation and its relevance to obtain outstanding agronomic characteristics for underutilized species. An approach was made to the global panorama of the application of gamma radiation in different conventional crop species and in vitro cultivated species, in order to obtain secondary metabolites, as well as molecular tools used for mutation screening. The varied effects of gamma radiation are essentially the result of the individual responses and phenotypic plasticity of each organism. However, even implicit chance can be reduced with specific genetic breeding, environmental adaptation, or conservation objectives.

Repurposing of Anticancer Drugs for the Treatment of Bacterial Infections.

Despite the fact that bacterial infections are one of the leading causes of death worldwide and that mortality rates are increasing at alarming rates, no new antibiotics have been produced by the pharmaceutical industry in more than a decade. The situation is so dire that the World Health Organization warned that we may enter a "post-antibiotic era" within this century; accordingly, bacteria resistant against all known antibiotics are becoming common and already producing untreatable infections. Although several novel approaches to combat bacterial infections have been proposed, they have yet to be implemented in clinical practice. Hence, we propose that a more plausible and faster approach is the utilization of drugs originally developed for other purposes besides antimicrobial activity. Among these are some anticancer molecules proven effective in vitro for eliminating recalcitrant, multidrug tolerant bacteria; some of which also protect animals from infections and recently are undergoing clinical trials. In this review, we highlight the similarities between cancer cells/tumors and bacterial infections, and present evidence that supports the utilization of some anticancer drugs, including 5-fluorouracil (5-FU), gallium (Ga) compounds, and mitomycin C, as antibacterials. Each of these drugs has some promising properties such as broad activity (all three compounds), dual antibiotic and antivirulence properties (5-FU), efficacy against multidrug resistant strains (Ga), and the ability to kill metabolically dormant persister cells which cause chronic infections (mitomycin C).

Role of quorum sensing in bacterial infections.

Quorum sensing (QS) is cell communication that is widely used by bacterial pathogens to coordinate the expression of several collective traits, including the production of multiple virulence factors, biofilm formation, and swarming motility once a population threshold is reached. Several lines of evidence indicate that QS enhances virulence of bacterial pathogens in animal models as well as in human infections; however, its relative importance for bacterial pathogenesis is still incomplete. In this review, we discuss the present evidence from in vitro and in vivo experiments in animal models, as well as from clinical studies, that link QS systems with human infections. We focus on two major QS bacterial models, the opportunistic Gram negative bacteria Pseudomonas aeruginosa and the Gram positive Staphylococcus aureus, which are also two of the main agents responsible of nosocomial and wound infections. In addition, QS communication systems in other bacterial, eukaryotic pathogens, and even immune and cancer cells are also reviewed, and finally, the new approaches proposed to combat bacterial infections by the attenuation of their QS communication systems and virulence are also discussed.

Periodontal status of teeth restored with crowns and their contralateral homologues, Valdivia. Chile / Estado periodontal de dientes rehabilitados con prótesis fija unitaria y sus homólogos contralaterales, Valdivia - Chile

To determine periodontal status of fixed single prostheses (FSP) installed in 2013 at Austral University of Chile, and its contralateral homologue (CH). Methods: A group of patients with FSP installed during 2013, who met the selection criteria and agreed to participate in the study were evaluated. Probing depth, attachment level; bleeding on probing and dental plaque index for each FSP and CH were measured in 2014; biological width invasion was also evaluated. One FSP and one CH were measured per patient, and in 6 sites for each tooth. Results: Seventy-four patients were evaluated. The majority were women (73 percent); posterior teeth accounted for 63.5 percent. The majority of participants had history of previous periodontal disease (85.1 percent), of which 58.7 percent was Periodontitis. Six of the patients with a history of gingivitis progressed to periodontitis (23.07 percent); while 100 percent of patients with no history of periodontal disease maintained their condition. Only 4 of the FSP evaluated showed biological invasion width. Discussion: Similar results were found for FSP and CH teeth with respect to probing depth, clinical attachment level and bleeding on probing. However, a difference in relation to dental plaque index was observed: positive in 58.1percent CH and positive in 29.7 percent FSP. Under the conditions of this study, it is concluded that the periodontal status of teeth with FSP does not differ from CH...

Objetivo: Determinar el estado periodontal de los dientes rehabilitados con prótesis fija unitaria (PFU) realizadas el año 2013 en Universidad Austral de Chile, y la de su homólogo contralateral (HCL). Material y método: Se evaluaron los pacientes con PFU realizadas durante el 2013 que cumplieron con los criterios de selección y aceptaron participar. Se midió durante el año 2014: profundidad al sondaje, nivel de inserción, sangramiento al sondaje e índice de placa para cada PFUy HCL; y se consignó invasión del ancho biológico. Se midió una PFU y un HCL por cada paciente, y 6 sitios por cada diente. Se utilizó estadística descriptiva. Resultados: Se evaluaron 74 pacientes de los cuales 73 por ciento fueronmujeres. El 63,5 por ciento de los dientes evaluados fueron posteriores. El 85,1 por ciento tenía antecedentes de enfermedad periodontal previa, de los cuales el 58,7 por ciento correspondió aPeriodontitis. De los pacientes con antecedentes de gingivitis, 6 progresaron a periodontitis (23,07 por ciento); mientras que el 100 por ciento de los pacientes sin antecedentes de enfermedad periodontal mantuvieron su condición. Sólo 4 de las PFU evaluadas tenían Invasión del ancho biológico.Discusión: Se encontraron resultados similares entre PFU y HCL para las variables profundidad al sondaje,nivel de inserción clínica y sangramiento al sondaje. Sinembargo, hubo diferencias en índice de placa, positivo en un 58,1 por ciento de los HCL y en un 29,7 por ciento, de las PFU. Bajo las condiciones del presente estudio se concluye que el estado periodontal de los dientes rehabilitados con PFU no difiere del estado de los HCL...

Association between abdominal obesity and periodontal disease: cross-sectional study / Asociación de la obesidad abdominal y enfermedad periodontal: estudio de corte transversal

The aim of the study is to determine the association. between abdominal obesity and periodontal disease by means of multivariate analysis. Materials and method: A cross -sectional observational study was carried out. From March to April 2014, patients admitted to the Dental SciencesBuilding at Universidad Austral de Chile were subjected to a clinical periodontalexamination. Periodontitis was defined by a probing pocket depth equal to orgreater than 4mm in at least one site of the teeth in two different quadrants,along with active bleeding within 30 seconds after probing. Abdominal obesity was defined by waist-hip ratio with values equal to or greater than 0.90 for men and 0.88 for women. Oral hygiene was assessed by Simplified Oral Hygiene Index. Smoker status was determined after undergoing an interview. Results: The sample comprised 136 participants (51 males and 85 females), with a mean age of 40.6+/-15.1 years. Prevalence of periodontal disease was 49.2 percent and obesity was 50.7 percent. A 62.3 percent of the patients showed both, periodontal disease and obesity. A statistically significant association between abdominal obesity (Odds ratio (OR)=2.4, 95 percent confidence interval (CI): 1.1, 5.1), cigarette comsumption(OR=4.0, 95 percent CI: 1.0, 16.5), poor oral hygiene (OR=2.8, 95 percent CI: 1.3, 5.9) and periodontal disease was established. Conclusion: There is a statically significant association between abdominal obesity and periodontal disease...

El objetivo es determinar la asociación de la obesidad abdominal y la enfermedad periodontal por medio de un análisis multivariado. Material y métodos: Se realizó un estudio observacional de corte transversal en donde se evaluaron pacientes ingresados al Edificio de las Ciencias Odontológicas de la Universidad Austral de Chile en los meses de marzo y abril del año 2014. Fueron sometidos a un examen clínico – periodontal. La periodontitis se determinó con una profundidad al sondaje igual o superior a 4 mm. en al menos un sitio del diente en dos cuadrantes diferentes con sangrado activo hasta 30 segundos luego del sondaje; y la obesidad abdominal mediante el Índice cintura/cadera con valores igual o mayores a 0.9 en hombres y 0.88 en mujeres. Se evaluó la higiene oral mediante el Índice de Higiene Oral Simplificado; y la condición de fumador mediante un interrogatorio. Resultados: Se incluyeron 136 participantes (51 hombres y 85 mujeres) con una edad media de 40.6 años +/- 15.1 DE. La prevalencia de periodontitis fue 49.2 por ciento y de obesidad 50.7 por ciento. Un 62.3 por ciento presentó periodontitis y obesidad abdominal. Se estableció una asociación estadísticamente significativa entre obesidad abdominal (Odds ratio = 2.4, 95 por ciento Intervalo de confianza: 1.1, 5.1], consumo de tabaco (Odds ratio = 4.0, 95 por ciento Intervalo de confianza: 1.0, 16.5), higiene oral pobre (Odds ratio = 2.8, 95 por ciento Intervalo de confianza: 1.3, 5.9) y enfermedad periodontal. Conclusión: Existe una asociación estadísticamente significativa entre la obesidad abdominal y la enfermedad periodontal...

Oral hygiene, periodontal status and treatment needs among 12-year-old students, Castro, Chile, 2014 / Higiene bucal, estado y necesidad de tratamiento periodontal en escolares de 12 años, Castro-Chile, 2014

The present study aims to determine the level of oral hygiene, periodontal status and treatment needs, indicating if there are differences between men and women, in 12-year-old students from Castro, Los Lagos region, during March and April of 2014. A cross-sectional study was carried out. A total of 242 12-year-old students from municipal and subsidized private schools in Castro were selected through a stratified random sample representative of each school. Students were evaluated by a calibrated examiner to determine the Simplified Oral Hygiene Index (OHI-S) and the Community Periodontal Index of Treatment Needs (CPITN). Data were transferred to a Microsoft Excel spreadsheet and statistically analyzed to calculate the amount and percentage of the variables. Mann-Whitney U-test was used for comparison between genders. From the total, 59.5 percent of the students have regular hygiene. Also, 86.4 percent of the assessed adolescents have gingivitis and 13.6 percent of them have periodontitis. The periodontal treatment need indicates that 58 percent of the students require oral hygiene instructions and scaling. No statistically significant differences were found for gender. There is a higher prevalence of periodontal diseases associated with regular oral hygiene than the regional and national reference in 12-year-old adolescents in Castro. Then, it is necessary to teach and promote specific public health strategies based on epidemiological data...

El presente estudio, pretende determinar el grado de higiene bucal, estado y necesidad de tratamiento periodontal en escolares de 12 anos de la ciudad de Castro, región de Los Lagos, durante el año 2014, indicando si existen diferencias entre hombres y mujeres. Corresponde a un estudio observacional descriptivo transversal. Se seleccionaron 242 escolares de 12 anos de la ciudad de Castro de establecimientos municipales y particulares subvencionados a través de una muestra aleatoria estratificada representativa de cada colegio. Los alumnos fueron evaluados durante marzo y abril de 2015, por un examinador calibrado (K= 0,86) para determinar el Indice de Higiene Oral Simplificado (IHO-S) y el estado y necesidad de tratamiento periodontal a través del Indice Comunitario de Necesidad de Tratamiento Periodontal(CPITN). Los datos fueron traspasados a una planilla de Microsoft Excel y analizados estadísticamente calculando cantidad y porcentaje de las variables. Para la comparación entre genero se utilizo el test estadístico U de Mann-Whitney. Se observo que un 59,5 por ciento de los alumnos presentan una higiene regular. Asimismo, un 86,4 por ciento de los escolares evaluados presentan gingivitis y un 13,6 por ciento periodontitis. La necesidad de tratamiento periodontal indica que un 58 por ciento requiere destartraje supragingival e instrucción en higiene bucal. No se encontraron diferencias estadísticamente significativas entre genero. Existe una mayor prevalencia que la referencia a nivel regional y nacional de enfermedades periodontales en escolares de 12 anos asociadas a una higiene bucal regular. Es necesario inculcar y fomentar estrategias de salud publica especificas basadas en datos epidemiológicos...

Anti-Helicobacter pylori activity of plants used in Mexican traditional medicine for gastrointestinal disorders.

AIM OF THE STUDY: Helicobacter pylori is the major etiological agent of chronic active gastritis and peptic ulcer disease and is linked to gastric carcinoma. Treatment to eradicate the bacteria failed in many cases, mainly due to antibiotic resistance, hence the necessity of developing better therapeutic regimens. Mexico has an enormous unexplored potential of medicinal plants. This work evaluates the in vitro anti-H. pylori activity of 53 plants used in Mexican traditional medicine for gastrointestinal disorders. MATERIALS AND METHODS: To test the in vitro antibacterial activity, agar dilution and broth dilution methods were used for aqueous and methanolic extracts, respectively. RESULTS: Aqueous extracts of Artemisia ludoviciana subsp. mexicana, Cuphea aequipetala, Ludwigia repens,and Mentha x piperita (MIC 125 to <250 microg/ml) as well as methanolic extracts of Persea americana, Annona cherimola, Guaiacum coulteri, and Moussonia deppeana (MIC <7.5 to 15.6 microg/ml) showed the highest inhibitory effect. CONCLUSIONS: The results contribute to understanding the mode of action of the studied medicinal plants and for detecting plants with high anti-Helicobacter pylori activity.

Anti-Helicobacter pylori activity of anacardic acids from Amphipterygium adstringens.

Amphipterygium adstringens (Schltdl.) Standl. (Anacardiaceae) is widely used in traditional Mexican medicine for the treatment of gastritis and ulcers. In this work, we studied the anti-Helicobacter pylori activity of its bark, this Gram-negative bacterium is considered the major etiological agent of chronic active gastritis and peptic ulcer disease, and it is linked to gastric carcinoma. From a bio-guided assay of the fractions obtained form a continuous Soxhlet extraction of the bark, we identified that petroleum ether fraction had significant antimicrobial activity against Helicobacter pylori. From this fraction, we isolated an anacardic acids mixture and three known triterpenes: masticadienonic acid; 3alpha-hydroxymasticadienonic acid; 3-epi-oleanolic; as well as the sterol beta-sitosterol. Only the anacardic acids mixture exhibits a potent dose-dependent antibacterial activity (MIC=10 microg/ml in broth cultures). It is enriched in saturated alkyl phenolic acids (C15:0, C16:0, C17:0 C19:0) which represents a novel source of these compounds with potent anti-Helicobacter pylori activity. The promising use of anacardic acids and Amphipterygium adstringens bark in the development of an integral treatment of Helicobacter pylori diseases is discussed.