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1.
Chem Biodivers ; 20(11): e202301210, 2023 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-37743258

RESUMEN

The novel benzothiazole sulfonate hybrid derivatives containing azomethine group were synthesized and characterized using 1 H-NMR, 13 C-NMR, and HR-MS analysis. The potential enzyme inhibition activities against pancreatic lipase of the novel benzothiazole sulfonate hybrid derivatives containing azomethine group were screened with in vitro and in silico methods. IC50 values of compounds 5 b (23.89 µM), 5 i (28.87 µM), and 5 f (30.13±4.32) were found to be more effective pancreatic lipase inhibitors than orlistat (57.75 µM) in vitro studies. Also, the binding affinities of compounds 5 b (-8.7 kcal/mol), 5 i (-8.6 kcal/mol), and 5 f (-8.9 kcal/mol) were found potential inhibitors for pancreatic lipase in silico studies. In addition, the absorption distribution, metabolism, and excretion properties (ADME), molecular properties, toxicity estimation, and bioactivity scores of the synthesized compounds were scanned. It was found to have the ability to cross the brain-blood barrier for compounds 5 a, 5 b, 5 c, and 5 d. All compounds were calculated to be taken orally as drugs, suitable for absorption in the intestinal tract and not carcinogenic, as well as very strongly bound to plasma proteins. Finally, compound 5 f was observed to be the best inhibitor for pancreatic lipase according to in vitro and in silico studies.


Asunto(s)
Benzotiazoles , Lipasa , Estructura Molecular , Relación Estructura-Actividad , Lipasa/metabolismo , Simulación del Acoplamiento Molecular
2.
Int J Phytoremediation ; 25(14): 2001-2013, 2023.
Artículo en Inglés | MEDLINE | ID: mdl-37434299

RESUMEN

The current study is to elucidate the responses of maize seedlings to excess copper and acetone O-(2-naphthylsulfonyl)oxime (NS) pretreatment. The study was divided into the following experimental groups: 18 h distilled water (DW) control (C), 6 h 0.3 mM NS + then 12 h DW (NS), 6 h DW + then 12 h 1 mM CuSO4.5H2O (CuS), 0.3 mM NS for 6 h + then 1 mM CuSO4.5H2O (NS + CuS) for 12 h. When the NS + CuS group is compared with the CuS group; It accumulated 10% more copper, while the ABA, H2O2, MDA, and carotenoid contents decreased significantly, the total chlorophyll, proline, gallic acid, ascorbic acid, catechol, trans-P-qumaric acid, and cinnamic acid contents increased. While SOD activity, which is one of the antioxidant system enzymes, decreased with NS application, GPX, CAT, and APX activities increased despite copper stress. When all the findings are evaluated as a whole, exogenous NS, despite excessive copper, ameliorated the adverse effects of copper stress by increasing the effectiveness of the enzymatic and non-enzymatic components of the antioxidant system and the contents of phenolic substances. In addition, increasing the copper content by 10% reveals its importance in terms of NS phytoremediation.Abbreviation: Style-sheet: When full form and abbreviated form both are used as keywords, retain both as provided by the author.


Considering the potential of NS in terms of phytoremediation and phytomining, it was determined that approximately 10% more copper was accumulated.Exogenous acetone O-(2-naphthylsulfonyl)oxime (NS), a synthetic sulfonate derivative oxime, to maize seedlings under copper stress increased the activity of enzymatic and non-enzymatic components of the antioxidant defense system.By increasing the content of phenolic compounds known for their electron-donating properties, NS supported the antioxidant defense system and contributed to the scavenging of radicals.


Asunto(s)
Antioxidantes , Cobre , Antioxidantes/metabolismo , Antioxidantes/farmacología , Cobre/toxicidad , Zea mays , Acetona/farmacología , Estrés Oxidativo , Peróxido de Hidrógeno/farmacología , Oximas/farmacología , Biodegradación Ambiental , Plantones
3.
Int J Phytoremediation ; 24(7): 721-729, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-34464220

RESUMEN

The main purpose of study is to determine if Acetone O- (4-chlorophenylsulfonyl) oxime (AO) has a positive effect on maize seedlings under copper (Cu) stress or not. Seedlings were allocated to following experimental groups: 18-hour distilled water (DW) Control (C), ago 6-hour 0.66 mM AO + later 12-hour DW (AO), ago 6-hour DW + later 12-hour 1 mM Cu (Cu), ago 6-hour 0.66 mM AO + later 12-hour 1 mM Cu (AO + Cu). The results showed that AO + Cu caused approximately three times more copper accumulation compared to Cu treatment. AO and AO + Cu treatments significantly decreased membrane damage and H2O2 formation compared to its control. The proline content was significantly increased in AO and AO + Cu compared to its control. While the highest catalase, Guaiacol Peroxidase and superoxide dismutase activity was observed in Cu application, the highest ascorbate peroxidase activity was determined in AO application. It was observed that AO had a protective effect on chlorophyll content and RWC, but a positive effect on carotenoid content could not be determined. In addition, the effects of AO on the content of 17 phenolic substances in maize leaves were determined. In the light of the current findings, AO may prevent the formation of radical compounds.


The fact that Acetone O-(4 chlorophenylsulfonyl) oxime (AO) caused approximately three times more copper accumulation indicates that it has a significant potential for phytoremediation studies. Despite the fact that AO resulted in approximately three times more copper accumulation, it is surprising that the Maize plant was able to continue its almost normal metabolic activities. AO alleviated the adverse effects of stress by affecting the hormones and antioxidant system of the plant. If AO is used with hyper accumulator plants, it may have the potential to obtain effective solutions in heavily copper-contaminated soils.


Asunto(s)
Antioxidantes , Plantones , Acetona/farmacología , Antioxidantes/metabolismo , Ascorbato Peroxidasas/metabolismo , Biodegradación Ambiental , Catalasa/metabolismo , Cobre , Peróxido de Hidrógeno/farmacología , Estrés Oxidativo , Oximas/farmacología , Especies Reactivas de Oxígeno/farmacología , Superóxido Dismutasa/metabolismo , Zea mays/metabolismo
4.
Int J Phytoremediation ; 22(4): 420-426, 2020.
Artículo en Inglés | MEDLINE | ID: mdl-32156154

RESUMEN

The aim of this study is to determine the effect of GA on maize seedlings as well as its antioxidative effect under copper (Cu) stress. To that end, maize seedlings were exposed to 1.5 mM GA and 1 mM Cu solutions, and the seedlings were allocated to following experimental groups: 18-hr distilled water (DI) (Control), 6-hr GA + 12-hr DI (GA), 6-hr DI + 12-hr Cu (Cu), 6-hr GA + 12-hr Cu (GA + Cu), 12-hr Cu +6-hr GA (Cu + GA), and 18-hr GA and Cu mixture (GA = Cu). The experiment was designed by randomized block design with three repetitions. The results showed that GA alone and GA + Cu treatments significantly decreased membrane damage and H2O2 formation compared to the other treatments. GA formation was determined to be highest in turn in treatments GA + Cu and GA alone. The proline content significantly decreased in treatments GA alone and GA + Cu. The highest catalase (CAT) activity was observed in GA alone application, whereas GA + Cu treatment led to increase in guaiacol peroxidase (GPX), superoxide dismutase (SOD), and ascorbate peroxidase (APX) activities. GA has a protective effect on chlorophyll contents and relative water content (RWC), but not on carotenoid levels under Cu stress. Overall, GA alone application or GA + Cu stress may prevent the formation of reactive oxygen species (ROS) due to chelation effect of GA.


Asunto(s)
Plantones , Zea mays , Antioxidantes , Ascorbato Peroxidasas , Biodegradación Ambiental , Catalasa , Cobre , Ácido Gálico , Peróxido de Hidrógeno , Estrés Oxidativo , Superóxido Dismutasa
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