Chiral Mono- and α-Diimines and Their Pd(II) Complexes with Anticancer Activity

The aim of this review is to provide mainly an outlook of the synthesis and characterization of chiral mono- and α-diimines ligands and their Pd(II) complexes carried out in our group in the last few years. Some other issues with simple chiral imines synthesized in our lab are also outlined. The report includes details about their versatile coordination patterns, biological activity in cancer cell lines, and engaging properties in different fields, such as materials science

Multipurpose reservoir performance analysis: a case study on the Billings sub-basin

As a result of economic development, multiple and extensive uses of water resources have caused an imbalance between the demands and the water supply in reservoirs. Thus, the present study analyzed the performance of the Billings Reservoir, located in the Alto Tietê basin - São Paulo, in terms of meeting the demands of urban water supply and electricity generation simultaneously. For that, three operating scenarios for the Reservoir were considered: the first, different numbers of water transfer and fixed consumptive demand were adopted; in the second, the transfer of water was suppressed and different consumptive demands were considered; the third, used the indirect potable water reuse as an aid to recharge the Reservoir and considered different consumptive demands. The statistical performance indicators reliability, resilience, vulnerability and Water Sustainability Index were calculated. And based on the results obtained for Scenario 1, the curve of performance criteria versus reservoir pumping, reliability, resilience, and water sustainability index increased and vulnerability in the system reduced significantly. The Scenario 2, according to the curve of performance criteria versus demand flow, demonstrated that the increase in water demand implies significant reductions in reliability, resilience and water sustainability, and reflects in the increase of system vulnerability. Finally, the Scenario 3 demonstrated that the recharge of the reservoir when employing reuse water provides improvements in reservoir performance compared to Scenario 2 and promotes the reduction of environmental impacts from the release of the sewage system into Billings. It was possible to observe the relevant role of the water supply to the Billings Reservoir, in terms of meeting its demands and water sustainability when adopting the multiple use of water.O presente estudo analisou o desempenho do Reservatório Billings, inserido na bacia do Alto Tietê - São Paulo, quanto à sua capacidade de atender as demandas de abastecimento urbano e de geração de energia elétrica concomitantemente. Para isso, foram considerados três cenários de operação para o Reservatório: no primeiro, adotou-se diferentes valores de transferência de água para o Reservatório, além de demanda consuntiva fixa; no segundo, a transferência de águas foi suprimida e considerou-se diferentes demandas consuntivas; no terceiro, empregou-se o reúso potável indireto da água como auxílio para recarga do Reservatório, e considerou-se diferentes demandas consuntivas. Os indicadores de desempenho estatísticos confiabilidade, resiliência e vulnerabilidade e o Índice de Sustentabilidade Hídrica foram calculados. Os resultados obtidos para o Cenário 1, pelo cruzamento entre os fatores critérios de desempenho versus bombeamento do reservatório, indicaram que a confiabilidade, a resiliência e o Índice de Sustentabilidade Hídrica aumentaram, ao passo que a vulnerabilidade do sistema diminuiu significativamente. No Cenário 2, observou-se que o aumento da demanda hídrica implica em reduções significativas da confiabilidade, da resiliência e da sustentabilidade hídrica e um aumento da vulnerabilidade do sistema. Por último, o Cenário 3 demonstrou que a recarga do Reservatório por meio da água de reúso proporciona melhorias no seu desempenho se comparado ao Cenário 2, e beneficia a redução dos impactos ambientais provindos do lançamento dos esgotos na Billings. Concluiu-se que o planejamento de um sistema de Reservatório é um fator essencial para que ele possa satisfazer as múltiplas demandas e que, como uma solução parcial a fim de aumentar o aporte de água na Billings, a inserção da prática do reúso da água é uma ideia importante a ser considerada, pois poderá auxiliar na alimentação hídrica do Reservatório até que a transferência de águas dos rios Tietê e Pinheiros volte a ser viável, como foi projetado inicialmente

Metforminium Decavanadate as a Potential Metallopharmaceutical Drug for the Treatment of Diabetes Mellitus

New potential drugs based on vanadium are being developed as possible treatments for diabetes mellitus (DM) and its complications. In this regard, our working group developed metforminium decavanadate (MetfDeca), a compound with hypoglycemic and hypolipidemic properties. MetfDeca was evaluated in models of type 1 and type 2 diabetes mellitus, on male Wistar rats. Alloxan-induction was employed to produce DM1 model, while a hypercaloric-diet was employed to generate DM2 model. Two-month treatments with 3.7 μg (2.5 μM)/300 g/twice a week for DM2 and 7.18 μg (4.8 μM)/300 g/twice a week for DM1 of MetfDeca, respectively, were administered. The resulting pharmacological data showed nontoxicological effects on liver and kidney. At the same time, MetfDeca showed an improvement of carbohydrates and lipids in tissues and serum. MetfDeca treatment was better than the monotherapies with metformin for DM2 and insulin for DM1. Additionally, MetfDeca showed a protective effect on pancreatic beta cells of DM1 rats, suggesting a possible regeneration of these cells, since they recovered their insulin levels. Therefore, MetfDeca could be considered not only as an insulin-mimetic agent, but also as an insulin-enhancing agent. Efforts to elucidate the mechanism of action of this compound are now in progress

Assessment of major depressive disorder model in rat

El trastorno depresivo mayor (MDD) es una enfermedad caracterizada por la presencia de dos o más episodios depresivos consecutivos, es un factor de riesgo para cometer suicidio. La mayoría de las terapias antidepresivas se basan en el mantenimiento de la serotonina (5-HT) en la hendidura sináptica. El modelo debulbectomía olfatoria bilateral (OBX) tiene características similares al trastorno depresivo humano. El objetivo de este trabajo es caracterizar a la bulbectomía olfatoria como un modelo de depresión en ratas. Los resultados obtenidos muestran cambios fisiológicos y conductuales que son comparables a la depresión humana, las ratas bulbectomizadas disminuyeron de peso comparadas con los grupos control y cirugía sin extracción, la presencia de la hiperactividad es reducida después de 21 días de tratamiento con antidepresivos, la respuesta alterada a los estímulos adversos y la disminución del acicalamiento puede ser comparado con síntomas de depresión en humanos.Major depressive disorder (MDD) is a disease characterized by the presence of two or more depressive episodes. It is a risk factor to commit suicide. The most common antidepressant therapies are based on maintaining serotonin (5-HT) in the synaptic cleft. The bilateral olfactory bulbectomy (OBX) in rat model have characteristics similar to human depressive disorder. The aim of this work is to characterize olfactory bulbectomy as a depressive major model in rats. These results show physiological and behavioral changes that are comparable to human depression; bulbectomized rats have decreased weight compared to control and surgery without extraction groups, the presence of hyperactivity is reduced after 21 days of treatment with antidepressants (SSRI), altered response to adverse stimuli and a decrease of grooming can be equated a symptom of depression in humans

Energy Drink Administration in Combination with Alcohol Causes an Inflammatory Response and Oxidative Stress in the Hippocampus and Temporal Cortex of Rats

Energy drinks (EDs) are often consumed in combination with alcohol because they reduce the depressant effects of alcohol. However, different researches suggest that chronic use of these psychoactive substances in combination with alcohol can trigger an oxidative and inflammatory response. These processes are regulated by both a reactive astrogliosis and an increase of proinflammatory cytokines such as IL-1β, TNF-α, and iNOS, causing cell death (apoptosis) at the central and peripheral nervous systems. Currently, mechanisms of toxicity caused by mixing alcohol and ED in the brain are not well known. In this study, we evaluated the effect of chronic alcohol consumption in combination with ED on inflammatory response and oxidative stress in the temporal cortex (TCx) and hippocampus (Hp) of adult rats (90 days old). Our results demonstrated that consuming a mixture of alcohol and ED for 60 days induced an increase in reactive gliosis, IL-1β, TNF-α, iNOS, reactive oxygen species, lipid peroxidation, and nitric oxide, in the TCx and Hp. We also found immunoreactivity to caspase-3 and a decrease of synaptophysin in the same brain regions. The results suggested that chronic consumption of alcohol in combination with ED causes an inflammatory response and oxidative stress, which induced cell death via apoptosis in the TCx and Hp of the adult rats

Overactive bladder-18 years - Part II

Traditionally, the treatment of overactive bladder syndrome has been based on the use of oral medications with the purpose of reestablishing the detrusor stability. The recent better understanding of the urothelial physiology fostered conceptual changes, and the oral anticholinergics - pillars of the overactive bladder pharmacotherapy - started to be not only recognized for their properties of inhibiting the detrusor contractile activity, but also their action on the bladder afference, and therefore, on the reduction of the symptoms that constitute the syndrome. Beta-adrenergic agonists, which were recently added to the list of drugs for the treatment of overactive bladder, still wait for a definitive positioning - as either a second-line therapy or an adjuvant to oral anticholinergics. Conservative treatment failure, whether due to unsatisfactory results or the presence of adverse side effects, define it as refractory overactive bladder. In this context, the intravesical injection of botulinum toxin type A emerged as an effective option for the existing gap between the primary measures and more complex procedures such as bladder augmentation. Sacral neuromodulation, described three decades ago, had its indication reinforced in this overactive bladder era. Likewise, the electric stimulation of the tibial nerve is now a minimally invasive alternative to treat those with refractory overactive bladder. The results of the systematic literature review on the oral pharmacological treatment and the treatment of refractory overactive bladder gave rise to this second part of the review article Overactive Bladder - 18 years, prepared during the 1st Latin-American Consultation on Overactive Bladder.Univ Fed Sao Paulo, EPM, Sao Paulo, SP, BrazilUniv Sao Paulo, Dept Urol, BR-05508 Sao Paulo, SP, BrazilFac Med ABC, Dept Urol, Sao Paulo, SP, BrazilUniv Los Andes, Dept Urol, Bogota, ColombiaEscuela Med Mil, Dept Urol, Mexico City, DF, MexicoHosp Clin Jose San Martin, Catedra Urol, Buenos Aires, DF, ArgentinaMae de Deus Ctr Hosp, Dept Urol, Porto Alegre, RS, BrazilUniv Fed Ciencias Saude Porto Alegre, Porto Alegre, RS, BrazilAC Camargo Hosp, Dept Urol, Sao Paulo, SP, BrazilHosp Clinico Fuerza Area Chile, Santiago, ChileInst Mexicano Seguro Social, Mexico City, DF, MexicoHosp Souza Aguiar, Dept Urol, Rio De Janeiro, RJ, BrazilComplejo Med Policial Churruca Visca, Serv Urol, Buenos Aires, DF, ArgentinaCtr Policlin Valencia Vina, Valencia, VenezuelaHosp Pablo Tobon Uribe, Medellin, ColombiaClin Indisa, Serv Urol, Providencia, ChileCtr Reabilitacao & Readaptacao Dr Henriqe Santill, Goiania, Go, BrazilHosp Univ Caracas, Serv Urol, Caracas, VenezuelaUniv Fed Ceara, Div Urol, Fortaleza, Ceara, BrazilUniv Fed Sao Paulo, EPM, Sao Paulo, SP, BrazilWeb of Scienc

Overactive bladder-18 years - Part I

Overactive bladder syndrome is one of the lower urinary tract dysfunctions with the highest number of scientific publications over the past two decades. This shows the growing interest in better understanding this syndrome, which gathers symptoms of urinary urgency and increased daytime and nighttime voiding frequency, with or without urinary incontinence and results in a negative impact on the quality of life of approximately one out of six individuals - including both genders and almost all age groups. The possibility of establishing the diagnosis just from clinical data made patients' access to specialized care easier. Physiotherapy resources have been incorporated into the urological daily practice. A number of more selective antimuscarinic drugs with consequent lower adverse event rates were released. Recently, a new class of oral drugs, beta-adrenergic agonists has become part of the armamentarium for Overactive Bladder. Botulinum toxin injections in the bladder and sacral neuromodulation are routine modalities of treatment for refractory cases. During the 1st Latin-American Consultation on Overactive Bladder, a comprehensive review of the literature related to the evolution of the concept, epidemiology, diagnosis, and management was conducted. This text corresponds to the first part of the review Overactive Bladder 18-years.Univ Fed Sao Paulo, EPM, Rua Dr Oscar Monteiro Barros 617-141, BR-05641010 Sao Paulo, SP, BrazilUniv Sao Paulo, Dept Urol, BR-05508 Sao Paulo, SP, BrazilFac Med ABC, Dept Urol, Sao Paulo, SP, BrazilUniv Los Andes, Dept Urol, Bogota, ColombiaEscuela Med, Dept Urol, Mexico City, DF, MexicoHosp Clin Jose San Martin, Catedra Urol, Buenos Aires, DF, ArgentinaMae de Deus Ctr Hosp, Dept Urol, Porto Alegre, RS, BrazilUniv Fed Ciencias Saude Porto Alegre, Porto Alegre, RS, BrazilAC Camargo Hosp, Dept Urol, Sao Paulo, BrazilHosp Clin Fuerza Area Chile, Santiago, ChileInst Mexicano Seguro Social, Mexico City, DF, MexicoHosp Souza Aguiar, Dept Urol, Rio De Janeiro, RJ, BrazilComplejo Med Policial Churruca Visca, Serv Urol, Buenos Aires, DF, ArgentinaCtr Policlin Valencia Vina, Valencia, VenezuelaHosp Pablo Tobon Uribe, Medellin, ColombiaClin Indisa, Serv Urol, Providencia, ChileCtr Reabilitacao & Readaptacao Dr Henriqe Santill, Goiania, Go, BrazilHosp Univ Caracas, Serv Urol, Caracas, VenezuelaUniv Fed Ceara, Div Urol, Fortaleza, Ceara, BrazilUniv Fed Sao Paulo, EPM, Rua Dr Oscar Monteiro Barros 617-141, BR-05641010 Sao Paulo, SP, BrazilWeb of Scienc

Carcinogenicity of cobalt, antimony compounds, and weapons-grade tungsten alloy

The complete evaluation of the carcinogenicity of cobalt, antimony compounds, and weapons-grade tungsten alloy will be published in Volume 131 of the IARC Monographs.[Excerpt] In March, 2022, a Working Group of 31 scientists from 13 countries met remotely at the invitation of the International Agency for Research on Cancer (IARC) to finalise their evaluation of the carcinogenicity of nine agents: cobalt metal (without tungsten carbide or other metal alloys), soluble cobalt(II) salts, cobalt(II) oxide, cobalt(II,III) oxide, cobalt(II) sulfide, other cobalt(II) compounds, trivalent antimony, pentavalent antimony, and weapons-grade tungsten (with nickel and cobalt) alloy. For cobalt metal and the cobalt compounds, particles of all sizes were included in the evaluation. These assessments will be published in Volume 131 of the IARC Monographs.1 Cobalt metal and soluble cobalt(II) salts were classified as “probably carcinogenic to humans” (Group 2A) based on “sufficient” evidence for cancer in experimental animals and “strong” mechanistic evidence in human primary cells. Cobalt(II) oxide and weapons-grade tungsten alloy were classified as “possibly carcinogenic to humans” (Group 2B) based on “sufficient” evidence in experimental animals. Trivalent antimony was classified as “probably carcinogenic to humans” (Group 2A), based on “limited” evidence for cancer in humans, “sufficient” evidence for cancer in experimental animals, and “strong” mechanistic evidence in human primary cells and in experimental systems. Cobalt(II,III) oxide, cobalt(II) sulfide, other cobalt(II) compounds, and pentavalent antimony were each evaluated as “not classifiable as to its carcinogenicity to humans” (Group 3).[...