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1.
Molecules ; 27(14)2022 Jul 20.
Artigo em Inglês | MEDLINE | ID: mdl-35889493

RESUMO

A group of novel trimethoxyphenyl (TMP)-based analogues were synthesized by varying the azalactone ring of 2-(3,4-dimethoxyphenyl)-4-(3,4,5-trimethoxybenzylidene)oxazolone 1 and characterized using NMR spectral data as well as elemental microanalyses. All synthesized compounds were screened for their cytotoxic activity utilizing the hepatocellular carcinoma (HepG2) cell line. Compounds 9, 10 and 11 exhibited good cytotoxic potency with IC50 values ranging from 1.38 to 3.21 µM compared to podophyllotoxin (podo) as a reference compound. In addition, compounds 9, 10 and 11 exhibited potent inhibition of ß-tubulin polymerization. DNA flow cytometry analysis of compound 9 shows cell cycle disturbance at the G2/M phase and a significant increase in Annexin-V-positive cells compared with the untreated control. Compound 9 was further studied regarding its apoptotic potential in HepG2 cells; it decreased the level of MMP and Bcl-2 as well as boosted the level of p53 and Bax compared with the control HepG2 cells.


Assuntos
Antineoplásicos , Apoptose , Antineoplásicos/química , Linhagem Celular Tumoral , Proliferação de Células , Ensaios de Seleção de Medicamentos Antitumorais , Estrutura Molecular , Relação Estrutura-Atividade , Tubulina (Proteína)/metabolismo , Moduladores de Tubulina/farmacologia
2.
Sci Rep ; 12(1): 12842, 2022 07 27.
Artigo em Inglês | MEDLINE | ID: mdl-35896783

RESUMO

Drought stress is among the major threats that affect negatively crop productivity in arid and semi-arid regions. Probably, application of some additives such as biochar and/or brassinosteroids could mitigate this stress; however, the mechanism beyond the interaction of these two applications is not well inspected. Accordingly, a greenhouse experiment was conducted on wheat (a strategic crop) grown under deficit irrigation levels (factor A) i.e., 35% of the water holding capacity (WHC) versus 75% of WHC for 35 days while considering the following additives, i.e., (1) biochar [BC, factor B, 0, 2%] and (2) the foliar application of 24-epibrassinolide [BR, factor C, 0 (control treatment, C), 1 (BR1) or 3 (BR2) µmol)]. All treatments were replicated trice and the obtained results were statistically analyzed via the analyses of variance. Also, heat-map conceits between measured variables were calculated using the Python software. Key results indicate that drought stress led to significant reductions in all studied vegetative growth parameters (root and shoot biomasses) and photosynthetic pigments (chlorophyll a, b and total contents) while raised the levels of oxidative stress indicators. However, with the application of BC and/or BR, significance increases occurred in the growth attributes of wheat plants, its photosynthetic pigments, especially the combined additions. They also upraised the levels of enzymatic and non-enzymatic antioxidants while decreased stress indicators. Furthermore, they increased calcium (Ca), phosphorus (P) and potassium (K) content within plants. It can therefore be deduced that the integral application of BR and BC is essential to mitigate drought stress in plants.


Assuntos
Secas , Triticum , Brassinosteroides/farmacologia , Carvão Vegetal , Clorofila A , Plantas , Água/farmacologia
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