In Vitro and In Vivo Activities of Ruthenium(II) Phosphine/Diimine/Picolinate Complexes (SCAR) against Mycobacterium tuberculosis

Rifampicin, discovered more than 50 years ago, represents the last novel class of antibiotics introduced for the first-line treatment of tuberculosis. Drugs in this class form part of a 6-month regimen that is ineffective against MDR and XDR TB, and incompatible with many antiretroviral drugs. Investments in R&D strategies have increased substantially in the last decades. However, the number of new drugs approved by drug regulatory agencies worldwide does not increase correspondingly. Ruthenium complexes (SCAR) have been tested in our laboratory and showed promising activity against Mycobacterium tuberculosis. These complexes showed up to 150 times higher activity against MTB than its organic molecule without the metal (free ligand), with low cytotoxicity and high selectivity. In this study, promising results inspired us to seek a better understanding of the biological activity of these complexes. The in vitro biological results obtained with the SCAR compounds were extremely promising, comparable to or better than those for first-line drugs and drugs in development. Moreover, SCAR 1 and 4, which presented low acute toxicity, were assessed by Ames test, and results demonstrated absence of mutagenicity. © 2013 Pavan et al.

In vitro targeting of Polo-like kinase 1 in bladder carcinoma: Comparative effects of four potent inhibitors

Despite the improvements in neoadjuvant chemotherapy, the outcome of patients with advanced bladder cancer has changed very little over the past 30 years. In the present study we tested and compared the in vitro antitumor activities of four different inhibitors of Polo-like kinase 1 (PLK1) (BI 2536, BI 6727, GW843682X, and GSK461364), against 3 bladder carcinoma cell lines RT4, 5637 and T24. The impact on radiosensitivity and drug interactions in simultaneous treatments with cisplatin, methotrexate, and doxorubicin were also investigated. Our results showed that PLK1 inhibition prevented cell proliferation and clonogenicity, causing significant inhibition of invasion of tumor cells, though modest differences were observed between drugs. Moreover, all PLK1 inhibitors induced G2/M arrest, with the subsequent induction of death in all 3 cell lines. Drug interactions studies showed auspicious results for all PLK1 inhibitors when combined with the commonly used cisplatin and methotrexate, though combinations with doxorubicin showed mostly antagonistic effects. Comparably, the four PLK1 inhibitors efficiently sensitized cells to ionizing radiation. Our findings demonstrate that irrespective of the inhibitor used, the pharmacological inhibition of PLK1 constrains bladder cancer growth and dissemination, providing new opportunities for future therapeutic intervention. However, further laboratorial and preclinical tests are still needed to corroborate the usefulness of using them in combination with other commonly used chemotherapeutic drugs. © 2013 Landes Bioscience.

Efeitos da ingestão de Yacon (Smallanthus sonchifolius) sobre o processo de carcinogênese de cólon induzido pela 1, 2-dimetilhidrazina em ratos wistar

Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)

Síntese em fase sólida e estudos comformacionais de análogos contendo TOAC de um peptídeo de rã Hypsiboas albopunctatus

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

Ácido giberélico(GA3) na indução do florescimento de orquídeas

Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)

Uso do extrato pirolenhoso: Efeito no solo e nas plantas de tomate

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

Utilização so ácido graxo ômega-3 na hipertrigliceridemia de indivíduos com HIV/Aids: relação com níveis de citocinas

Pós-graduação em Doenças Tropicais - FMB

Avaliação de amidos nativos em condições de estresse adaptados ao processamento de alimentos

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Avaliação de extratores químicos na determinação de silício disponível em solos cultivados com cana-de-açúcar

Pós-graduação em Agronomia (Energia na Agricultura) - FCA

Produção de ácido lático por lactobacilos em diferentes meio de cultivo

Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)

Estudo da adesão dentinária em restaurações realizadas com ionômero modificado por resina: influência de técnicas restauradoras e do preparo cavitário

Pós-graduação em Ciência Odontólogica - FOA

Eficácia anti-helmíntica comparativa da associação albendazole, levamisole e ivermectina à moxidectina 1% em ovinos naturalmente infectados por nematódeos gastrintestinais

Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)

Condicionamento fisiológico, fitorreguladores e qualidade de sementes de milho-doce

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

Fisiologia pós-colheita de rosas cortadas cv. Vega

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

Processo infeccioso de Pseudocercospora musae e severidade da Sigatoka Amarela da bananeira em função do silício, potássio e cálcio em solução nutritiva

Yellow Sigatoka leaf spot, caused by Pseudocercospora musae (Mycosphaerella musicola), is one of main threats to banana production around the world. However, information regarding the infection process of P. musae and the influence of mineral nutrition on the disease severity could help with cultural control strategies and increase the fruit yield. Therefore, this work aimed to characterize the infectious process of P. musae in banana leaves, to study the effect of silicon (Si) and the interaction between potassium (K) and calcium (Ca) on the Yellow Sigatoka leaf spot severity. In the first study, samples were inoculated on the abaxial leaf surface with P. musae and analyzed at 12, 24, 36, 48, 72, 96, 120, 144, and 168 hours after inoculation (HAI) as well as 36 and 50 days after inoculation (DAI). The conidia germinated between 24 and 36 HAI and penetrated through the stomata between 96 and 120 HAI, or usually from 144 HAI. P. musae colonized intercellularly the spongy parenchyma at 36 DAI and inter- and intracellularly the palisade parenchyma at 50 DAI. The sporulation occurred at 50 DAI on the adaxial leaf surfaces. In the second study, banana plants grown in nutrient solution with 0; 0.5; 1.0; 1.8 and 3.6 mmol L -1 of silicic acid (H 4SiO 4) were inoculated with conidial suspension. The disease severity was assessed and data were integrated in the area under the disease severity progress curve (AUDSPC). The lower AUDSPC was 49.27% for the concentration of 3.05 mmol L -1 of H 4SiO 4 compared to plants grown without Si addition. Regarding silicon accumulation, at 3.6 mmol L -1 H4SiO 4, leaf Si content was 23.53% higher compared to the control. In the third study, plants grown in nutrient solution with 5 K concentrations (1, 2, 4, 6, and, 8 mmol L -1 ) combined with 5 Ca concentrations (1, 3, 5, 7, and, 9 mmol L -1 ), forming 25 treatments, were inoculated with conidial suspension. The disease severity was assessed and the data were integrated in the AUDSPC. There was no interaction between concentrations of K and Ca for AUDSPC, although the AUDSPC increased with the increase of K concentrations from 1 to 6 mmol L -1 . The K increase led to a reduction in chlorophyll a and b contents and in the N, P, Mg, B, Cu, Zn, and, Mn nutrients as well as increased the total plant dry weight.