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1.
Environ Geochem Health ; 44(2): 399-408, 2022 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-33515377

RESUMO

Lindane and DDT (1,1,1-trichloro-2,2-bis(4-chlorophenyl)ethane) are pesticides from the group of persistent organic pollutants. These compounds, due to lipophilic properties, accumulate in tissues of organisms, are transmitted through the food chain and ultimately threaten human health. The long-term use of pesticides led to soil and water pollution. Microbial degradation of organochlorine compounds is the most eco-friendly method of polluted soil recultivation. Effective degradation of lindane and DDT soil pollution under the influence of introduced destructive bacteria was shown in the laboratory conditions. The concentration of lindane in the soil decreased by 75% and of DDT-by 56% in 30 days. The red clover seedlings increased pesticides degradation in the soil by 20%. The destruction of pesticides in soil was more intense than in the mineral medium. The DGGE analysis of microorganism associations introduced in contaminated soil was possible to follow the survival of the introduced associations. The use of microorganisms-destructors of organochlorine compounds, and plants as well as the biodegradation potential of the soil is a promising direction in the recultivation of polluted soils.


Assuntos
Praguicidas , Poluentes do Solo , Trifolium , Bactérias/metabolismo , Biodegradação Ambiental , DDT/análise , Humanos , Praguicidas/análise , Solo , Poluentes do Solo/análise , Trifolium/metabolismo
2.
Steroids ; 140: 131-143, 2018 12.
Artigo em Inglês | MEDLINE | ID: mdl-30315840

RESUMO

Synthetic transformations of steroids for drug discovery and improvement of drug effectiveness have been an important part of modern medicinal chemistry and pharmaceutical sciences. Pentacyclic triterpenoids, being represented in the nature by various structures and biogenetically related to steroids, can largely expand the spectrum of biologically active steroidal agents via synthesis of the so-called "triterpenoid-steroid" hybrids. In the presented work, the nitrile anion cyclizations of 3,4-secolupane and 3,4-seco-oleanane nitriles and follow-up synthetic transformations of the cyclized products with formation of the gemm-dimethyl-free A ring "triterpenoid-steroid" hybrids were studied. Furthermore, the resulting cyclic compounds were modified at C3, C4, and/or C5 positions of ring A, as well as at C20, C28, and C30 positions of the isopropylidene moiety in the case of lupane triterpenoids. The cytotoxic effect of the synthesized compounds against seven cancer cell lines HEp-2, HCT 116, MS, RD TE32, A549, MCF7, and PC3 was evaluated. The in silico identification of potential anticancer protein targets with regard to the compounds, which were active at micromolar concentrations against tested cell lines, was carried out. The molecular docking studies showed that compound 19, which demonstrated most pronounced cytotoxicity (IC50 0.64-3.17 µM) against all tested cell lines, fits well the active sites of CDK6 and HER2/neu.


Assuntos
Simulação de Acoplamento Molecular , Esteroides/química , Triterpenos/química , Triterpenos/farmacologia , Antineoplásicos/síntese química , Antineoplásicos/química , Antineoplásicos/metabolismo , Antineoplásicos/farmacologia , Domínio Catalítico , Linhagem Celular Tumoral , Quinase 6 Dependente de Ciclina/química , Quinase 6 Dependente de Ciclina/metabolismo , Humanos , Receptor ErbB-2/química , Receptor ErbB-2/metabolismo , Relação Estrutura-Atividade , Triterpenos/síntese química , Triterpenos/metabolismo
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