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1.
Curr Med Chem ; 19(17): 2773-93, 2012.
Article in English | MEDLINE | ID: mdl-22455584

ABSTRACT

This review is focused on recent developments on hydroxypyri(mi)dines, as aluminum and actinide chelating agents to combat the toxicity due to accumulations of these metal ions in human body resulting from excessive metal exposure. After a brief update revision of the most common processes of aluminum (Al) exposure, as well as the associated toxicities and pathologies, we will focus on the current available Al chelators and future perspective as potential antidotes of Al toxicity. Due to the similarity between Al and Fe, a major emphasis is given to the hydroxypyridinone and hydroxypyrimidinone chelators, since they are analogues of the current iron chelators in clinical use (DFP and DFO). This review includes issues such as molecular design strategies and corresponding effects on the associated physico-chemical properties, lipo-hydrophilic balance, toxicity, in vivo bioassays and current clinical applications. The hydroxypyri(mi)dine chelators are also suitable for other hard metal ions, such as the radiotoxic actinides, and so a brief review is included on the applications of these chelators in actinides scavenging.


Subject(s)
Actinoid Series Elements/toxicity , Aluminum/toxicity , Pyridines/chemistry , Pyridines/pharmacology , Pyrimidines/chemistry , Pyrimidines/pharmacology , Actinoid Series Elements/chemistry , Aluminum/chemistry , Animals , Antidotes/chemistry , Antidotes/pharmacology , Chelating Agents/chemistry , Chelating Agents/pharmacology , Humans
2.
Prostate Cancer Prostatic Dis ; 15(1): 36-44, 2012 Mar.
Article in English | MEDLINE | ID: mdl-21894175

ABSTRACT

The objective of this study was to clarify the role of bisphosphonates in the treatment of osteoporosis in patients with prostate adenocarcinoma under androgen deprivation therapy (ADT). The Medline, EMBASE, Cancerlit and the American Society of Clinical Oncology abstract databases were searched for published randomized, placebo-controlled trials evaluating the usage of bisphosphonates in patients with prostate cancer (PC) under ADT. The outcomes assessed were fracture, osteoporosis, incidence of adverse events and changes in bone mineral density (BMD) during treatment. A total of 15 articles (2634 participants) were included in the meta-analysis. Treatment with bisphosphonates showed a substantial effect in preventing fractures (risk ratio (RR), 0.80; P = 0.005) and osteoporosis (RR, 0.39; P <0.00001). Zoledronic acid showed the best number needed to treat (NTT), compared with placebo, in relation to fractures and osteoporosis (NNT = 14.9 and NNT = 2.68, respectively). The between-group difference (bisphosphonates vs placebo) in the lumbar spine and femoral neck BMD were 5.18 ± 3.38% and 2.35 ± 1.16%, respectively. This benefit of bone loss prevention could be reached without major side effects (cardiovascular or gastrointestinal events). Bisphosphonates are effective in preventing bone loss in patients with PC who are under ADT.


Subject(s)
Androgens/metabolism , Bone Density Conservation Agents/therapeutic use , Diphosphonates/therapeutic use , Osteoporosis/prevention & control , Prostatic Neoplasms/therapy , Aged , Bone Density/drug effects , Bone Density Conservation Agents/adverse effects , Diphosphonates/adverse effects , Humans , Male , Osteoporosis/etiology , Prostatic Neoplasms/complications , Prostatic Neoplasms/metabolism , Randomized Controlled Trials as Topic
3.
Bioorg Med Chem ; 18(1): 274-81, 2010 Jan 01.
Article in English | MEDLINE | ID: mdl-19926293

ABSTRACT

A series of new analogues of trifluralin (TFL) were synthesized and characterized in view of changing the unfavorable properties that limits its use as antileishmanial agent. Some of the TFL analogues display more activity than a standard drug (miltefosine) against the promastigote forms of Leishmania infantum and Leishmania donovani and the intracellular form (THP-1 infected with L. infantum). All analogues showed a clear advantage over miltefosine, as they are not hemolytic. Some analogues can conjugate these characteristics with reduced cell toxicity and improved intracellular activity.


Subject(s)
Antiprotozoal Agents/chemistry , Antiprotozoal Agents/pharmacology , Leishmania/drug effects , Leishmaniasis/drug therapy , Trifluralin/chemistry , Trifluralin/pharmacology , Antiprotozoal Agents/chemical synthesis , Cell Death/drug effects , Cell Line , Erythrocytes/drug effects , Hemolysis/drug effects , Humans , Leishmania donovani/drug effects , Leishmania infantum/drug effects , Trifluralin/chemical synthesis
4.
J Fluoresc ; 17(6): 701-6, 2007 Nov.
Article in English | MEDLINE | ID: mdl-17665290

ABSTRACT

Absorption spectra and fluorescence data in nonpolar solvents are reported for seven novel dehydroabietic acid-based diarylamines, which have potential as components of hole transport layers for molecular electronic devices. This bulky group has been found to improve the possibilities for film formation of these compounds, and in this study we show that this does not significantly affect their fluorescence characteristics, which are similar to diphenylamine.

5.
J Fluoresc ; 16(2): 227-31, 2006 Mar.
Article in English | MEDLINE | ID: mdl-16470348

ABSTRACT

The absorption and fluorescence spectra, lifetimes and quantum yields of a series of triarylaminequinoxaline bipolar compounds, with and without the bulky dehydroabietic acid group, have been studied in toluene solution. This bulky group is introduced to improve solubility and thermal properties of these systems. It is shown that this does not affect their spectral or photophysical behavior. The compounds show relatively strong fluorescence, with the emission maximum strongly dependent upon the substituents present. Oxidation potentials have also been determined in acetonitrile solution, and again indicate that introduction of the resin acid moiety has no effect on these properties.

6.
Cad Saude Publica ; 17(5): 1123-40, 2001.
Article in Portuguese | MEDLINE | ID: mdl-11679888

ABSTRACT

This study uses a spatial-temporal model to analyze the spatial spread of the AIDS epidemic (adult cases) in the municipality of Rio de Janeiro, Brazil, during three periods: 1988-1990, 1991-1993, and 1994-1996. City districts were used as the geographic units of analysis. A spatial analysis was also performed for pediatric AIDS cases due to vertical HIV transmission, according to period of birth, 1985-90 and 1991-96. For total adult AIDS cases, the initial period was characterized by a polygonal cluster located around the harbor area, which expanded from west to east. Among homosexual cases, in situ growth predominated, and a decrease in the intensity of the diffusion process was observed from the second to the final period. Among heterosexual cases, the epidemic displayed a relevant geographic spread, mainly from 1988-1990 to 1991-1993. Among female cases in the final time period, a cluster of high incidence rates was found towards the northwest, including very poor areas. Among pediatric cases in 1991-1996, a significant correlation was found between AIDS incidence rates and poverty levels in the respective municipal districts. The results suggest that a more complete understanding of AIDS spatial-temporal dynamics can make a major contribution to preventive measures.


Subject(s)
Acquired Immunodeficiency Syndrome/epidemiology , Models, Statistical , Space-Time Clustering , Acquired Immunodeficiency Syndrome/transmission , Adult , Brazil/epidemiology , Disease Outbreaks , Female , Humans , Incidence , Infant, Newborn , Infectious Disease Transmission, Vertical , Male , Pregnancy
7.
J Nat Prod ; 64(6): 761-6, 2001 Jun.
Article in English | MEDLINE | ID: mdl-11421739

ABSTRACT

In this work, studies on the arylation of anilines derived from dehydroabietic acid, the main component of disproportionated rosin, are presented. The redox properties of the new diarylamines were investigated by cyclic voltammetry, and their free radical scavenging activity was tested by reduction of the 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical. Three of the diarylamines with lower oxidation potential proved to be as active as isopropyldiphenylamine (IPPD) and superior to tert-butylhydroxytoluene (BHT), both commercially available synthetic antioxidants.


Subject(s)
Abietanes , Diterpenes/chemistry , Free Radical Scavengers/chemistry , Phenanthrenes/chemistry , Bismuth , Catalysis , Copper , Diterpenes/chemical synthesis , Diterpenes/pharmacology , Electrochemistry , Free Radical Scavengers/chemical synthesis , Free Radical Scavengers/isolation & purification , Indicators and Reagents , Phenanthrenes/chemical synthesis , Phenanthrenes/pharmacology , Spectrophotometry, Ultraviolet , Spectroscopy, Fourier Transform Infrared
8.
Int J Biometeorol ; 45(1): 13-21, 2001 Feb.
Article in English | MEDLINE | ID: mdl-11411410

ABSTRACT

In this paper, the quality of the wine from the Dão (Viseu) region of Portugal is examined and relationships between wine quality and climatic variability are obtained using spectral and correlation analysis to determine the structure of the temporal variations. The spectra of the series of quality of wine values show statistically significant oscillations coherent with those found in the series of teleconnection indices. The series cover a period of 33 years. A significant correlation was obtained between wine quality and minimum air temperature in May, December and total precipitation in April. The teleconnection circulation indices are used to provide some physical insight into the most significant oscillating components of the climatic and the wine quality series. We found significant and positive correlations between the quality of the wine and the Southern Oscillation Index (SOI) of August and negative with the SOI of January and with the North Atlantic Oscillation of April. Wine quality and climatic series can be predicted using statistical models depending on significant oscillations.


Subject(s)
Wine/standards , Analysis of Variance , Climate , Meteorological Concepts , Portugal , Quality Control , Temperature
9.
Cad Saude Publica ; 16(## Suppl 1): 7-19, 2000.
Article in Portuguese | MEDLINE | ID: mdl-10904386

ABSTRACT

Mean AIDS incidence rates were calculated for three time periods, 1987-89, 1990-92, and 1993-96, using reported adult AIDS cases by county. The analysis included the following variables: "population of counties for resident AIDS cases"; "proportion of population residing in urban areas", and "concentration of poverty", stratifying by gender and exposure categories. The Southeast region has experienced the lowest increase, contrasting with the steep rise observed in the North and South between the second and third study periods. Comparing variations in incidence rates from 1990-92 and 1993-96 by region or population, the greatest increase was among women. In the larger cities, AIDS cases among "homo/bisexual men" predominate, although the proportion of cases among men who have sex with men has decreased as heterosexual cases have undergone a continuous increase. IDUs have been the core stratum in medium-sized counties. For the smallest counties, heterosexual transmission has been the basic element in local dynamics. Even though AIDS is still an urban phenomenon in Brazil, the epidemic is spreading to rural counties. Until recently it has mainly affecting relatively more affluent areas, but there is now an evident spread of the epidemic to poorer areas.


Subject(s)
Acquired Immunodeficiency Syndrome/epidemiology , Disease Outbreaks , Residence Characteristics , Acquired Immunodeficiency Syndrome/transmission , Adolescent , Adult , Brazil/epidemiology , Disease Notification , Female , Humans , Incidence , Male , Retrospective Studies , Socioeconomic Factors
10.
J Epidemiol Community Health ; 54(7): 530-6, 2000 Jul.
Article in English | MEDLINE | ID: mdl-10846196

ABSTRACT

STUDY OBJECTIVES: To establish the geographical relation of health conditions to socioeconomic status in the city of Rio de Janeiro, Brazil. DESIGN: All reported deaths in the municipality of Rio de Janeiro, from 1987 to 1995, obtained from the Mortality Information System, were considered in the study. The 24 "administrative regions" that compose the city were used as the geographical units. A geographical information system (GIS) was used to link mortality data and population census data, and allowed the authors to establish the geographical pattern of the health indicators considered in this study: "infant mortality rate"; "standardised mortality rate"; "life expectancy" and "homicide rate". Information on location of low income communities (slums) was also provided by the GIS. A varimax rotation principal component analysis combined information on socioeconomic conditions and provided a two dimension basis to assess contextual variation. MAIN RESULTS: The 24 administrative regions were aggregated into three different clusters, identified as relevant to reflect the socioeconomic variation. Almost all health indicator thematic maps showed the same socioeconomic stratification pattern. The worst health situation was found in the cluster composed of the harbour area and northern vicinity, precisely in the sector where the highest concentration of slum residents are present. This sector of the city exhibited an extremely high homicide rate and a seven year lower life expectancy than the remainder of the city. The sector that concentrates affluence, composed of the geographical units located along the coast, showed the best health situation. Intermediate health conditions were found in the west area, which also has poor living standards but low concentration of slums. CONCLUSIONS: The findings suggest that social and organisation characteristics of low income communities may have a relevant role in understanding health variations. Local health and other social programmes specifically targeting these communities are recommended.


Subject(s)
Health Status Indicators , Mortality , Poverty Areas , Social Class , Adolescent , Adult , Aged , Brazil/epidemiology , Censuses , Child , Child, Preschool , Data Interpretation, Statistical , Homicide/statistics & numerical data , Humans , Infant , Infant Mortality , Infant, Newborn , Life Expectancy , Middle Aged , Software
11.
Cad Saude Publica ; 15(1): 15-28, 1999.
Article in Portuguese | MEDLINE | ID: mdl-10203443

ABSTRACT

This ecological analysis addresses the association between income inequality and health status in the municipality of Rio de Janeiro. Data were analyzed using geo-processing and multiple regression techniques. The following health indicators were used: infant mortality rate; standardized mortality rate; life expectancy at birth; and homicide rate among 15-29-year-old males. Patterns of income inequality were assessed through income distribution indicators: Gini index, Robin Hood index, and top 10 %/bottom 40% average income ratio. The results indicate significant correlations between income distribution indicators and health indicators, providing additional empirical evidence of the association between health status and income inequality. For the homicide rate, the effect of the indicator "density of slum residents" was also relevant, suggesting that further deterioration in health standards may be due to social disruption of deprived communities and the resultant increase in criminal activity. The geo-epidemiological analysis presented here highlights the association between adverse health outcomes and residential concentration of poverty. Social policies focused on slum residents are needed to reduce the harmful effects of relative deprivation.


Subject(s)
Health Status Indicators , Income , Poverty , Adolescent , Adult , Age Factors , Brazil , Female , Homicide/statistics & numerical data , Humans , Infant , Infant Mortality , Infant, Newborn , Life Expectancy , Male , Poverty Areas , Regression Analysis
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