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1.
Sensors (Basel) ; 23(9)2023 Apr 30.
Artigo em Inglês | MEDLINE | ID: mdl-37177633

RESUMO

In many countries, water quality monitoring is limited due to the high cost of logistics and professional equipment such as multiparametric probes. However, low-cost sensors integrated with the Internet of Things can enable real-time environmental monitoring networks, providing valuable water quality information to the public. To facilitate the widespread adoption of these sensors, it is crucial to identify which sensors can accurately measure key water quality parameters, their manufacturers, and their reliability in different environments. Although there is an increasing body of work utilizing low-cost water quality sensors, many questions remain unanswered. To address this issue, a systematic literature review was conducted to determine which low-cost sensors are being used for remote water quality monitoring. The results show that there are three primary vendors for the sensors used in the selected papers. Most sensors range in price from US$6.9 to US$169.00 but can cost up to US$500.00. While many papers suggest that low-cost sensors are suitable for water quality monitoring, few compare low-cost sensors to reference devices. Therefore, further research is necessary to determine the reliability and accuracy of low-cost sensors compared to professional devices.

2.
Eur J Med Chem ; 148: 165-177, 2018 Mar 25.
Artigo em Inglês | MEDLINE | ID: mdl-29459276

RESUMO

A new series of amphiphilic η6-areneruthenium(II) compounds containing phenylazo ligands (group I: compounds 1a, 1b, 2a and 2b) and phenyloxadiazole ligands (group II: compounds 3a, 3b, 4a and 4b) were synthesized and characterized for their anti-glioblastoma activity. The effects of the amphiphilic η6-areneruthenium(II) complexes on the viability of three human glioblastoma cell lines, U251, U87MG and T98G, were evaluated. The azo-derivative ruthenium complexes (group I) showed high cytotoxicity to all cell lines, whilst most oxadiazole-derivative complexes (group II) were less cytotoxic, except for compound 4a. The cationic complexes 2a, 2b and 4b were more cytotoxic than the neutral complexes. Compounds 2a and 2b caused a significant reduction in the percentage of cells in the G0/G1 phase, with concomitant increases in the G2/M phase and fragmented DNA in the T98G cell line. The η6-areneruthenium(II) compounds were also tested in cell lines that overexpress the multidrug ABC transporters P-gp, MRP1 and ABCG2. Compounds 2b and 4a were substrates for the P-gp protein, with resistance indexes of 8.6 and 1.9, respectively. Compound 2b was also a substrate for ABCG2 and MRP1 proteins, with lower resistance indexes (1.8 and 1.6, respectively). The contribution of multidrug ABC transporters to the cytotoxicity of compound 2b in T98G cells was evidenced, since verapamil (a characteristic inhibitor of MRP1) increased the cytotoxicity of compound 2b at concentrations up to 20 µmol L-1, whilst GF120918 and Ko143 (specific inhibitors of P-gp and ABCG2, respectively) had no significant effect. In addition, we showed that compound 2b interacts with glutathione (GSH), which could explain its cellular efflux by MRP1. Our results showed that the amphiphilic η6-areneruthenium(II) complexes are promising anti-glioblastoma compounds, especially compound 2b, which was cytotoxic for all three cell lines, although it is transported by the three main multidrug ABC transporters.


Assuntos
Transportadores de Cassetes de Ligação de ATP/metabolismo , Resistência a Múltiplos Medicamentos , Glioblastoma/tratamento farmacológico , Rutênio/farmacologia , Compostos Azo , Transporte Biológico , Linhagem Celular Tumoral , Glioblastoma/patologia , Humanos , Ligantes , Compostos Organometálicos/farmacologia , Oxidiazóis
3.
Eur J Med Chem ; 122: 291-301, 2016 Oct 21.
Artigo em Inglês | MEDLINE | ID: mdl-27376492

RESUMO

Breast cancer resistance protein (BCRP/ABCG2) is one of the major transporters involved in the efflux of anticancer compounds, contributing to multidrug resistance (MDR). Inhibition of ABCG2-mediated transport is then considered a promising strategy for overcoming MDR in tumors. We recently identified a chromone derivative, namely MBL-II-141 as a selective ABCG2 inhibitor, with relevant in vivo activity. Here, we report the pharmacomodulation of MBL-II-141, with the aim of identifying key pharmacophoric elements to design more potent selective and non-toxic inhibitors. Through rational structural modifications of MBL-II-141, using simple and affordable chemistry, we obtained highly active and easily-made inhibitors of ABCG2. Among the investigated compounds, derivative 4a, was found to be 3-fold more potent than MBL-II-141. It was similarly efficient as the reference inhibitor Ko143 but with the advantage of a lower intrinsic cytotoxicity, and therefore constitutes the best ABCG2 inhibitor ever reported displaying a very high therapeutic ratio.


Assuntos
Membro 2 da Subfamília G de Transportadores de Cassetes de Ligação de ATP/antagonistas & inibidores , Neoplasias da Mama , Cromonas/química , Cromonas/farmacologia , Desenho de Fármacos , Cromonas/síntese química , Células HEK293 , Humanos , Relação Estrutura-Atividade
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