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1.
Heliyon ; 10(6): e27386, 2024 Mar 30.
Artículo en Inglés | MEDLINE | ID: mdl-38560691

RESUMEN

The Allium turcicum L. (Zuzubak) plant as a cultivated vegetable have various health benefits and consumed as a food. Due to the shortcoming evidence in literature and the importance of this plant in folk medicine, in the present study, for the first time, we evaluated the bioactive profile of components (using LC-MS/MS), cytotoxicity, anticancer, antioxidant, and antibacterial prospectives of Zuzubak methanol extract. Reported results show that the extract is rich in bioactive compounds and has anticancer activity with breast cancer cells (MCF-7), human prostate cancer cells (DU-145), and Human osteosarcoma cancer Cell lines of (IC50) in dose dependent manner in the concentration range of 31.25 µg/mL and 2000 µg/mL for 24 and 48 h. Western blotting results determined that the extract significantly suppressed the growth of U2OS, MCF-7, and DU-145 cancer cells by down expression of Ang-1 (angiogenic protein) and Beclin-1 (autophagy protein) and overexpression of Bax (a proapoptotic protein). The oxidative stress indices showed a reduction in RPE-1 and MCF-7 cells and an upsurge in U2OS and DU-145 cells. Additionally, the antimicrobial assay showed suppression of the growth of various pathogenic microorganisms in 4.00-8.00 µg/concentrations of Zuzubak extract using the microdilution method. The phytochemicals identified showed promising anticancer, antioxidant effects, and antimicrobial properties, representing a valuable herbal source for drug development studies.

2.
Acta Neurol Belg ; 124(3): 911-918, 2024 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-38361171

RESUMEN

INTRODUCTION: Dyke-Davidoff-Masson Syndrome (DDMS) is a clinical syndrome that causes different clinical symptoms and is defined by volume decrement in one cerebral hemisphere. In this study, we aimed to evaluate the involvement of the normal-appearing contralateral hemisphere in 16 pediatric patients with DDMS using diffusion-weighted imaging (DWI). MATERIALS AND METHODS: Brain MRIs were retrospectively reviewed between January 2014 and January 2023. Sixteen pediatric patients radiologically compatible with DDMS were included in the study. Sixteen children who had undergone brain MRI, most commonly for headaches and whose MRI findings had been completely normal, were included as the control group. Apparent diffusion coefficient (ADC) values of the deep gray and white matter of the normal-appearing hemisphere in the patient group were calculated and compared with that of the control group. RESULTS: The ADC values of the gray and white matters of the patient and control groups were not statistically different. However, in the patient group, the ADC values of the gray and white matters in males were remarkably lower than in females (p = 0.038, p = 0.037, respectively). CONCLUSION: The difference in the ADC values of the contralateral hemisphere between females and males in the patient group suggests that the normal-appearing hemisphere may have been affected by DDMS. Although, the exact mechanism of this effect is not known. Therefore, in patients with DDMS, contralateral hemisphere involvement in cerebral hemiatrophy and hemispherectomy should be evaluated clinically and radiologically.


Asunto(s)
Imagen de Difusión por Resonancia Magnética , Humanos , Masculino , Femenino , Niño , Estudios Retrospectivos , Imagen de Difusión por Resonancia Magnética/métodos , Adolescente , Preescolar , Sustancia Blanca/diagnóstico por imagen , Sustancia Blanca/patología , Lateralidad Funcional/fisiología , Sustancia Gris/diagnóstico por imagen , Sustancia Gris/patología
3.
Brain Res ; 1828: 148762, 2024 Apr 01.
Artículo en Inglés | MEDLINE | ID: mdl-38228258

RESUMEN

Toxoplasma gondii is a single-celled parasite that causes a disease called toxoplasmosis. It can reach the central nervous system, but the mechanism of T. gondii disrupting the functioning of these brain regions occurs in bradyzoite stage of parasite, causing brain damage by forming tissue cysts in brain. In our study, the effects of T. gondii on locomotor activity, anxiety, learning and memory, and norepinephrine (NE), levodopa (L-DOPA), dopamine (DA) and 3,4-D-dihydroxyphenylacetic acid (DOPAC) catecholamines in amygdala, striatum, prefrontal cortex and hippocampus regions of the brain were investigated in bradyzoite stage. Twenty male Albino mice Mus musculus, 4-5 weeks old, weighing 20-25 g, were used. T. gondii inoculated to mice intraperitonealy with 48-50-hour passages of T. gondii RH Ankara strain. For intraperitoneal inoculation of mice 5x104 tachyzoites per mouse. No inoculation was made in control group (n: 20). Locomotor activity behavior in open field test (OFT), anxious behavior in elevated plus maze (EPM), and learning behavior in novel object recognition (NOR) tests were evaluated. NE, L-DOPA, DA and DOPAC were measured by HPLC in brain tissues of amygdala, striatum, prefrontal cortex and hippocampus. A decrease was observed in the locomotor activity, anxiety and learning values of the T. gondii group compared to the control group (p < 0.05). The heighten in NE and L-DOPA levels in amygdala tissue of T. gondii group compared to control group, an elevation in NE, L-DOPA, DA and DOPAC levels in striatum tissue, and an increase in levels of NE in prefrontal cortex tissue were detected in monoamine results. In hippocampus tissue, an increase was observed in DA levels, while a decrease was observed in NE, L-DOPA and DOPAC levels. In our study, it has been shown that T. gondii in bradyzoite stage reduces locomotor activity, causes learning and memory impairment, and has anxiogenic effects.


Asunto(s)
Toxoplasma , Toxoplasmosis , Ratones , Masculino , Animales , Levodopa , Ácido 3,4-Dihidroxifenilacético , Encéfalo , Dopamina , Norepinefrina
4.
J Biomol Struct Dyn ; 42(5): 2341-2357, 2024 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-37098809

RESUMEN

Various studies conducted on Centaurea species indicate that the relevant plant is good source of bioactive phytochemicals. In this study, in vitro studies were used to determine bioactivity properties of methanol extract of Centaurea mersinensis - endemic species in Turkey - on extensive basis. Furthermore, the interaction of target molecules, identified for breast cancer and phytochemicals in the extract, was investigated via in silico analyses to support findings received in vitro. Scutellarin, quercimeritrin, chlorogenic acid and baicalin were primary phytochemicals in the extract. Methanol extract and scutellarin had higher cytotoxic effects against MCF-7 (IC50=22.17 µg/mL, and IC50=8.25 µM, respectively), compared to other breast cancer cell lines (MDA-MB-231, SKBR-3). The extract had strong antioxidant properties and inhibited target enzymes, especially α-amylase (371.69 mg AKE/g extract). The results of molecular docking indicate that main compounds of extract show high-strength bonding to the c-Kit tyrosine among target molecules identified in breast cancer, compared to other target molecules (MMP-2, MMP-9, VEGFR2 kinase, Aurora-A kinase, HER2). The tyrosinase kinase (1T46)-Scutellarin complex showed considerable stability in 150 ns simulation as per MD findings, and it was coherent with optimal docking findings. Docking findings and HOMO-LUMO analysis results corresponds with in vitro experiments. Medicinal properties of phytochemicals, which was determined to be suitable for oral use along with ADMET, were found to be within normal limits except for their polarity properties. In conclusion, in vitro and in silico studies indicated that the relevant plant yields promising results regarding its potential to develop novel and effective medicational products.Communicated by Ramaswamy H. Sarma.


Asunto(s)
Apigenina , Neoplasias de la Mama , Centaurea , Glucuronatos , Humanos , Femenino , Simulación del Acoplamiento Molecular , Metanol/química , Extractos Vegetales/farmacología , Extractos Vegetales/química , Centaurea/química , Fitoquímicos/farmacología , Fitoquímicos/química , Antioxidantes/farmacología , Antioxidantes/química
5.
Radiol Bras ; 56(1): 27-35, 2023.
Artículo en Inglés | MEDLINE | ID: mdl-36926356

RESUMEN

The anatomical structure of the temporal bone is quite complex. There are a great number of anatomical variations that are often confused with temporal bone pathologies, especially fractures. It is important that radiologists and surgeons be able to recognize such variations.


O osso temporal é uma estrutura anatômica óssea bastante complexa. Apresenta grande número de variações anatômicas, que muitas vezes são confundidas com lesões ou doenças, principalmente fraturas. O reconhecimento dessas variações é importante para radiologistas e cirurgiões.

6.
Molecules ; 28(6)2023 Mar 07.
Artículo en Inglés | MEDLINE | ID: mdl-36985400

RESUMEN

The current work's main objective was to determine the chemical composition of Amygdalus communis (AC) leaf extract and examine the antibacterial and cytotoxic properties of biosynthesized gold nanoparticles (AuNPs). The chemical composition of AC leaf extract was determined using LC-ESI/MS/MS to detect compounds that may be responsible for the reducing, stabilizing, and capping steps in the synthesis of nanoparticles and their biological activities. The AC-AuNPs were spherical, with a particle size lower than 100 nm and a face-centered cubic structure. The EDX spectrum confirmed the formation of AuNPs and a negative zeta potential value (-27.7 mV) suggested their physicochemical stability. The in vitro cytotoxic efficacy of the AC-AuNPs against colorectal adenocarcinoma (Caco-2), glioma (U118), and ovarian (Skov-3) cancer cell lines and human dermal fibroblasts (HDFs) was evaluated by MTT assay. CaCo-2 cell proliferation was effectively inhibited by the AC-AuNPs at concentrations between 25 and 100 g mL-1. The AC-AuNPs exerted preeminent antimicrobial activity against Bacillus subtilis with an MIC of 0.02 µg/mL, whilst good activity was shown against Staphylococcus aureus bacteria and Candida albicans yeast with an MIC of 0.12 µg/mL. Ultimately, the results support the high antibacterial and anticancer potential of biosynthesized AuNPs from AC leaf extract.


Asunto(s)
Antiinfecciosos , Antineoplásicos , Nanopartículas del Metal , Prunus dulcis , Humanos , Oro/farmacología , Oro/química , Células CACO-2 , Espectrometría de Masas en Tándem , Nanopartículas del Metal/química , Antiinfecciosos/farmacología , Antiinfecciosos/química , Antibacterianos/química , Antineoplásicos/farmacología , Antineoplásicos/química , Extractos Vegetales/farmacología , Extractos Vegetales/química , Tecnología Química Verde
7.
Radiol. bras ; 56(1): 27-35, Jan.-Feb. 2023. graf
Artículo en Inglés | LILACS-Express | LILACS | ID: biblio-1422529

RESUMEN

Abstract The anatomical structure of the temporal bone is quite complex. There are a great number of anatomical variations that are often confused with temporal bone pathologies, especially fractures. It is important that radiologists and surgeons be able to recognize such variations.


Resumo O osso temporal é uma estrutura anatômica óssea bastante complexa. Apresenta grande número de variações anatômicas, que muitas vezes são confundidas com lesões ou doenças, principalmente fraturas. O reconhecimento dessas variações é importante para radiologistas e cirurgiões.

8.
Chem Biol Drug Des ; 101(3): 740-748, 2023 03.
Artículo en Inglés | MEDLINE | ID: mdl-36366959

RESUMEN

Cyclotrichium origanifolium is a medicinal plant belonging to the Lamiaceae family. In this study, phenolic content analysis, antimicrobial effects, and cytotoxic effects of extracts of C. origanifolium were investigated. In the extracts, phenolic compound analysis by the liquid chromatography-electrospray ionization-tandem mass spectrometry method, antimicrobial effect by the minimum inhibition concentration method, and cytotoxic effect on human dermal fibroblasts (HDF), glioblastoma cell (U87), ovarian adenocarcinoma cell (Skov-3), and human colorectal adenocarcinoma cell (CaCo-2) cancer cell lines were investigated. Cytotoxicity analyses were performed by the MTT method. In addition, the GST and AChE enzyme activities of the extracts were also measured. Around 18 compounds were detected in both the methanol and ethanol extract. It was found that the best antimicrobial effect on Gram-negative Pseudomonas aeruginosa was on methanol extract, while the ethanol extract was on Candida albicans fungus (respectively, 2.50 mg/ml, 5.0 µg/ml). A 500 µg/ml of methanol extract has been shown to have cytotoxic activity high effect on HDF cells. GST and AChE activity were found to decrease in a concentration-dependent manner.


Asunto(s)
Adenocarcinoma , Antiinfecciosos , Lamiaceae , Humanos , Espectrometría de Masas en Tándem/métodos , Antioxidantes/química , Extractos Vegetales/farmacología , Extractos Vegetales/química , Metanol , Células CACO-2 , Cromatografía Liquida , Fenoles/química , Etanol , Antiinfecciosos/farmacología
9.
Nat Prod Res ; 37(1): 123-129, 2023 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-34219549

RESUMEN

Senecio angulatus L.f. is a flowering plant from the Asteraceae family that is native to South Africa and which was observed recently in the north and the east of Algeria. This study was aimed for the first time, to evaluate concomitantly phytochemical profiles, using LC-ESI/MS analysis, following by testing and assessing in vitro antioxidant and antiacetylcholinesterase activities of these specific species. The results indicated that the hydromethanolic and the acetate extracts have shown remarkable potent inhibitory effects on AChE with IC50 of (6.04 ± 0.05; 6.72 ± 0.10 µg/mL) respectively along with antioxidant potential of acetate for FRAP and phenanthroline methods with A0.5 of (11.15 ± 0.72; 5.72 ± 0.13 µg/mL) successively. Moreover, a high amount of cynarin and trans-ferulic acid was found in this extract whilst butanolic extract has recorded the highest amount of chlorogenic acid. Indeed phenolic compounds usually have a hydroxyl in their structure which may contribute significantly to the antioxidant activity.


Asunto(s)
Antioxidantes , Senecio , Antioxidantes/química , Senecio/química , Extractos Vegetales/farmacología , Extractos Vegetales/química , Cromatografía Liquida , Fitoquímicos/farmacología
10.
Cell Mol Biol (Noisy-le-grand) ; 69(14): 211-216, 2023 Dec 20.
Artículo en Inglés | MEDLINE | ID: mdl-38279434

RESUMEN

Verbascum thapsus (VT) is a medicinal plant that is used in folk medicine to treat a variety of ailments. For this study, the biological functions of VT methanol extract were determined in vitro. The plant's methanol extract was created through the maceration process. The phytochemical composition of plant extracts was investigated using liquid chromatography-electrospray ionization tandem mass spectrometry (LC-ESI-MS/MS). The antioxidant capacity of the extract was determined using the DPPH (2,2-diphenyl-1-picrylhydrazil) and ABTS (2,2-azinobis (3-ethylbenzothiazoline-6-sulfonic acid) tests and its cytotoxicity was assessed using the MTT ((3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide, a tetrazole)) assay on the Caco-2 (human colorectal adenocarcinoma cells), LNCaP (Lymph Node Carcinoma of the Prostate), and HEK293 cell lines (Human embryonic kidney 293 cells) used to model colon, prostate, and non-cancerous cells. VT extract showed low DPPH and ABTS radical scavenging activities compared to standard antioxidants at 30 mg/ml concentration. In addition, it was determined that VT extract inhibited acetylcholinesterase enzyme.


Asunto(s)
Antioxidantes , Benzotiazoles , Ácidos Sulfónicos , Verbascum , Masculino , Humanos , Antioxidantes/farmacología , Antioxidantes/química , Espectrometría de Masas en Tándem , Células CACO-2 , Acetilcolinesterasa , Metanol/química , Células HEK293 , Extractos Vegetales/farmacología , Extractos Vegetales/química , Fitoquímicos/análisis
11.
J Obstet Gynaecol ; 42(6): 2018-2024, 2022 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-35666949

RESUMEN

The plasma levels of homoarginine (h-Arg) and methylated arginine have proven to be an independent cardiovascular risk factor. We aimed to determine the h-Arg and methyl arginine levels in serums of high-risk pregnancy causing potential complications. These participants were divided into four groups as the control group with quadruple test, the high-risk group quadruple test the control group with binary test, the high-risk group with quadruple test that have a positive result from second-trimester screening with a cut-off value of 1 in 300. The serum methyl arginine and homoarginine levels were analysed with liquid chromatography-tandem mass spectrometry. Serum h-Arg levels were found to be higher in high-risk groups compared to control groups and it was also detected higher in the groups with quadruple test than the groups with binary test (p < .05). H-Arg levels in the groups showed strong negative correlation with age and serum inhibin-A levels (r = -0.288, p < .001). Also, there was a strong negative correlation between serum asymmetric dimethylarginine (ADMA) and serum inhibin-A levels (r = -0.352, p < .001). H-Arg may be a new risk marker to detect high-risk pregnancies in early pregnancy. In addition to, methylated arginine such as ADMA has a key regulator in a physiological concentration of h-Arg.IMPACT STATEMENTWhat is already known on this subject? H-Arg levels decrease may be associated with preeclampsia, GDM, macrosomia, low birth weight, and preterm delivery in pregnancy.What do the results of this study add? Serum h-Arg levels were found to be higher in high-risk groups. Additionally, h-Arg levels and ADAM, one of the methylated arginines in the groups showed a strong negative correlation with serum inhibin-A levelsWhat are the implications of these findings for clinical practice and/or further research? H-Arg may be a new risk marker to detect high-risk pregnancies.


Asunto(s)
Homoarginina , Embarazo de Alto Riesgo , Arginina , Femenino , Humanos , Recién Nacido , Inhibinas , Óxido Nítrico , Embarazo
12.
Turk Thorac J ; 23(1): 32-37, 2022 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-35110198

RESUMEN

OBJECTIVE: To compare the value of chest computed tomography at 1-mm and 5-mm slice thickness in terms of computed tomography severity score and computed tomography evaluation time in the diagnosis of COVID-19. MATERIAL AND METHODS: Sixty-five patients were included in the study group who are reverse-transcription polymerase chain reaction-positive for COVID-19 and had chest computed tomography. The 1 mm and 5 mm reconstructed images were evaluated in 2 different sessions with 4-week intervals by 2 certificated general radiologists. The presence of COVID-19-related findings, COVID-19 final category, and evaluation time were recorded. Thin and thick slices were compared for these variables and inter-reader reliability calculated with the Statistical Package for the Social Sciences (SPSS) for Windows. RESULTS: There was no significant difference between the COVID-19-related findings on thorax computed tomography between 1-mm and 5-mm slices except crazy paving appearance, microvascular enlargement, and septal thickening. The frequency of the final categories of computed tomography results was consistent between the thick and thin slices. The computed tomography assessment time was significantly lower in 5 mm slices. The inter-reader reproducibility analysis results demonstrated good and excellent reproducibility of measurements between readers for both slice thicknesses. CONCLUSION: It was found that 5-mm reconstruction thickness of chest computed tomography can be employed for the initial detection of COVID-19-related findings and the final diagnostic category-related COVID-19 rather than 1-mm slices with a faster availability of results which can be beneficial on pandemic hospitals.

13.
Nat Prod Res ; 36(18): 4672-4680, 2022 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-34866505

RESUMEN

Astragalus ponticus Pall. species was investigated for its antiproliferative effects on HeLa cells. Two new chalcones (B5 and B8) along with eight known compounds (B1, B2, B3, B6, B7, B10, B14 and B15) were isolated by following bioactivity guided isolation methods. In addition, from non-active fraction, three cycloartane glycosides (B11, B12 and B13) were isolated. Molecular structures of these isolated compounds were revealed by using spectroscopic methods like MS, 1D and 2D NMR and a single crystal X-ray diffraction analysis. New compounds B5 and B8 showed the highest antiproliferative activities against HeLa cells (IC50 values of 36.6 and 20.6 µM, respectively) while the rest showed high and low activities. Non-endemic species attract relatively low attention from the scientific community but this study demonstrates that valuable new compounds, which might be used as ingredients in medicinal preparations, can be obtained from these materials.


Asunto(s)
Planta del Astrágalo , Chalcona , Chalconas , Planta del Astrágalo/química , Chalconas/farmacología , Glicósidos/química , Células HeLa , Humanos , Estructura Molecular
14.
Environ Sci Pollut Res Int ; 29(13): 19642-19656, 2022 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-34718956

RESUMEN

The toxic effects of mercury in earthworms and the potential alleviation effect of hydrogen-rich water (HRW) using ATR-FTIR and LC-MS analysis methods were investigated. Different concentrations of mercury chloride (H1: 5 µg/mL, H2: 10 µg/mL, H3: 20 µg/mL, H4: 40 µg/mL, and C1: control) and mercury chloride prepared in hydrogen-rich water (H5: 5 µg/mL, H6: 10 µg/mL, H7: 20 µg/mL, H8: 40 µg/mL, and C2: control) were injected into earthworms. The changes and reductions in some bands representing proteins, lipids, and polysaccharides (3280 cm-1, 2922 cm-1, 2855 cm-1, 1170 cm-1, and 1047 cm-1) showed that protective effects could occur in groups prepared with hydrogen-rich water. In the FTIR results, it was found that these bands in the H3 group were more affected and decreased by the influence of mercury on earthworms than the H7 group prepared with hydrogen. LC-MS analysis showed that the changes in some ions of the highest dose groups (H4 and H8) were different, and mercury caused oxidative DNA damage in earthworms. When the high-level application groups of mercury, i.e., H4 and H8 were compared with the controls, the ion exchange ([M + H] + ; m/z 283.1) representing the 8-Oxo-dG level in earthworms was higher in the H4 group than the H8 group. This reveals that HRW exhibited the potential ability to alleviate the toxic effects of mercury; however, a longer period of HRW treatment may be necessary to distinguish an obvious effect. The ATR-FTIR spectroscopy provided a rapid and precise method for monitoring the changes in biological tissues caused by a toxic compound at the molecular level.


Asunto(s)
Mercurio , Oligoquetos , Animales , Hidrógeno/química , Mercurio/toxicidad , Espectroscopía Infrarroja por Transformada de Fourier , Espectrometría de Masas en Tándem , Agua/química
15.
J Food Biochem ; 45(12): e13975, 2021 12.
Artículo en Inglés | MEDLINE | ID: mdl-34676566

RESUMEN

Daucus carota L. ssp. major (DCM) plant is widely used in traditional medicine to treat some types of cancer and various diseases. Therefore, we evaluated the biological activities of this plant to define its effects against prostate cancer (PCa), Alzheimer's disease (AD), oxidation, and diabetes mellitus (DM) as well as identified its phenolic composition. To determine the anti-cancer properties of the plant extract, we treated PCa cells with the extract at a concentration range of 0.25, 0.5, 1, 2, and 4 mg/ml. Significant results were obtained against the PC3 cells compared to normal PNT1a prostate epithelial cells. As a result of precise measurements at the millimolar level, it was observed that the plant extract showed an effective inhibition (IC50 ) against glutathione S-transferase (GST; 12.84 mM), acetyl cholinesterase (AChE; 15.07 mM), and α-Gly (11.75 mM) enzymes when compared with standard inhibitors. Antioxidant activities of DCM methanol extract were determined via two well-known in vitro techniques. The extracts showed antioxidant activities against the DPPH and ABTS+ . The LC-ESI-MS/MS was used to determine the phenolic compounds of methanol extract from DCM. Chlorogenic acid (2,089.096 µg/g), shikimic acid (193.14 µg/g), and coumarin (113.604 µg/g) were characterized as major phenolic compounds. In addition, the interactions of chlorogenic acid, chrysin, coumarin, and shikimic acid with the used three enzymes have been calculated using molecular docking simulation. PRACTICAL APPLICATIONS: Plant natural phenolic compounds have protective effects such as anti-inflammatory, antioxidant, anticarcinogen, and enzyme inhibitory. Therefore, it has an important place in the food and pharmaceutical industry. The present study aims to reveal the enzyme inhibitory, antioxidant, and anticarcinogenic properties of the Daucus carota ssp. Major (DCM) plant extract. Significant results were obtained against the PC3 cells compared to normal PNT1a prostate epithelial cells. DCM extract demonstrated considerable antioxidant activity and inhibitory potential on used metabolic enzymes. These biological effects are thought to have a relationship with rich chemical composition.


Asunto(s)
Acetilcolinesterasa , Daucus carota , Glutatión Transferasa , Glicósido Hidrolasas , Humanos , Masculino , Simulación del Acoplamiento Molecular , Células PC-3 , Fitoquímicos , Extractos Vegetales/farmacología , Próstata , Espectrometría de Masas en Tándem
16.
Biophys Chem ; 277: 106629, 2021 10.
Artículo en Inglés | MEDLINE | ID: mdl-34126547

RESUMEN

Many plant species have a large diversity of secondary metabolites with different biological activities. This study aims to assess the phenolic constituent, enzyme inhibitory and antioxidant activities of the aqueous (water) and methanol extracts of Inula discoidea. The enzyme assays showed effective enzyme inhibition of the methanol extract against acetylcholinesterase (AChE), butyrylcholinesterase (BChE), glutathione S-transferase (GST), and α-glycosidase (α-Gly) enzymes. The IC50 values for AChE, BChE, GST, and α-Gly were found as 38.5 mg/mL, 34.65 mg/mL, 77.0 mg/mL, and 40.76 mg/mL, respectively. Antioxidant properties of the aqueous and methanol extracts of I. discoidea were determined by four well-known in vitro techniques (ABTS, CUPRAC, DPPH, and FRAP methods). The antioxidant values of both water and methanol extracts were found to be better than the standard antioxidants (BHA, BHT, ascorbic acid, and α-tocopherol) in ABTS and CUPRAC methods. According to an updated LC-MS/MS technique analysis, quinic acid (21.08 mg/g), protocatechuic acid (4.49 mg/g), and gallic acid (0.48 mg/g) were found as major phenolic compounds of the plant extract. The binding interactions of major phenolic compounds of I. discoidea with the AChE, BChE, GST, and α-Gly enzymes were investigated by the molecular docking studies.


Asunto(s)
Acetilcolinesterasa , Butirilcolinesterasa , Inula , Simulación del Acoplamiento Molecular , Fitoquímicos
17.
Bioorg Chem ; 107: 104606, 2021 02.
Artículo en Inglés | MEDLINE | ID: mdl-33476865

RESUMEN

In this study, new 1,2,3-triazole derivatives containing chalcone core (1-7) were synthesized. Obtained compounds were characterized by IR, 1H NMR, 13C NMR, and mass studies. Characterized compounds (1-7) inhibitory effects were tested against the glutathione S-transferase (GST), acetylcholinesterase (AChE), and Butyrylcholinesterase (BChE). Their Ki values were in the range of 5.88-11.13 µM on AChE, 5.08-15.12 µM on BChE, and 9.82-13.22 µM on GST. Remarkable inhibitory effects were obtained against three tested metabolic enzymes. Also, binding scores of the best-inhibitors against AChE, BChE, and GST enzymes were detected as -9.969 kcal/mol, -10.672 kcal/mol, and -8.832 kcal/mol, respectively. Isoindoline-1,3-dione and benzothiophene moieties played a critical role in the inhibition of AChE and BChE enzymes, respectively. Phenylene and triazole moieties had the most important interactions for inhibition of the GST enzyme. Therefore, in vivo and in silico results indicated that these compounds can be considered in drug design processes for the treatment of some diseases including Alzheimer's disease (AD), leukemia, and some type of cancer.


Asunto(s)
Acetilcolinesterasa/metabolismo , Butirilcolinesterasa/metabolismo , Inhibidores de la Colinesterasa/síntesis química , Inhibidores Enzimáticos/síntesis química , Glutatión Transferasa/metabolismo , Triazoles/química , Acetilcolinesterasa/química , Enfermedad de Alzheimer/tratamiento farmacológico , Enfermedad de Alzheimer/patología , Sitios de Unión , Butirilcolinesterasa/química , Inhibidores de la Colinesterasa/metabolismo , Inhibidores de la Colinesterasa/uso terapéutico , Inhibidores Enzimáticos/metabolismo , Inhibidores Enzimáticos/uso terapéutico , Glutatión Transferasa/antagonistas & inhibidores , Humanos , Simulación del Acoplamiento Molecular , Unión Proteica , Estructura Terciaria de Proteína , Relación Estructura-Actividad , Triazoles/metabolismo , Triazoles/uso terapéutico
18.
Sci Rep ; 10(1): 2946, 2020 02 19.
Artículo en Inglés | MEDLINE | ID: mdl-32076064

RESUMEN

In this study, we report a facile and effective production process of palladium nanoparticles supported on polypyrrole/reduced graphene oxide (rGO/Pd@PPy NPs). A novel electrochemical sensor was fabricated by incorporation of the prepared NPs onto glassy carbon electrode (GCE) for the simultaneous detection of ascorbic acid (AA), dopamine (DA) and uric acid (UA). The electrodes modified with rGO/Pd@PPy NPs were well decorated on the GCE and exhibited superior catalytic activity and conductivity for the detection of these molecules with higher current and oxidation peak intensities. Simultaneous detection of these molecules was achieved due to the high selectivity and sensitivity of rGO/Pd@PPy NPs. For each biomolecule, well-separated voltammetric peaks were obtained at the modified electrode in cyclic voltammetry (CV) and differential pulse voltammetry (DPV) measurements. Additionally, the detection of these molecules was performed in blood serum samples with satisfying results. The detection limits and calibration curves for AA, DA, and UA were found to be 4.9 × 10-8, 5.6 × 10-8, 4.7 × 10-8 M (S/N = 3) and ranging from 1 × 10-3 to 1.5 × 10-2 M (in 0.1 M PBS, pH 3.0), respectively. Hereby, the fabricated rGO/Pd@PPy NPs can be used with high reproducibility, selectivity, and catalytic activity for the development of electrochemical applications for the simultaneous detection of these biomolecules.

19.
Bioorg Chem ; 94: 103333, 2020 01.
Artículo en Inglés | MEDLINE | ID: mdl-31677859

RESUMEN

Achillea schischkinii Sosn. is an endemic plant species and it belongs to Asteraceae family. It is distributed widely in the Central and East Anatolia. This study was carried out for evaluation of the antioxidant activity, enzyme inhibition effect, elemental and phenolic content of A. schischkinii. Briefly, acetylcholinesterase (AChE), butyrylcholinesterase (BChE), α-glycosidase (α-Gly), and glutathione S-transferase (GST) enzymes were strongly inhibited by A. schischkinii. IC50 values for AChE, BChE, α-Gly, and GST enzymes were found as 19.3 mg/mL, 15.4 mg/mL, 69.3 mg/mL, and 34.7 mg/mL respectively. The antioxidant activity of the sample was evaluated by four different in vitro bioanalytical methods. Besides, the concentrations of twelve elements in A. schischkinii were analyzed by ICP-MS technique. Zn (50.6 ppm), Mn (23.0 ppm), and Cu (12.7 ppm) were found as major elements. Furthermore, catechin (20.8 µg/mg extract), trans-ferulic acid (18.3 µg/mg extract), and gallic acid (11.2 µg/mg extract) were characterized as major phenolic compounds by using HPLC. PRACTICAL APPLICATIONS: Acetylcholinesterase, butyrylcholinesterase, α-glycosidase, and glutathione s-transferase enzymes have crucial functions on metabolism. Enzyme inhibition or activation mostly attributed to some health disorders such as Alzheimer's disease, Diabetes mellitus, cancer and hyperglycemia. Phenolic contents are responsible for effective biological activity. This study evaluated the phenolic content and antioxidant activity of Achillea schischkinii as well as the inhibition effect against four metabolic enzymes. The results would be beneficial for using the plant in the food industry and pharmacological process.


Asunto(s)
Achillea/química , Antioxidantes/farmacología , Cromatografía Líquida de Alta Presión/métodos , Inhibidores Enzimáticos/farmacología , Espectrometría de Masas/métodos , Antineoplásicos/efectos adversos , Antioxidantes/aislamiento & purificación , Cisplatino/efectos adversos , Resistencia a Antineoplásicos/efectos de los fármacos , Activación Enzimática/efectos de los fármacos , Fenoles/análisis
20.
J Pharm Biomed Anal ; 179: 112961, 2020 Feb 05.
Artículo en Inglés | MEDLINE | ID: mdl-31732404

RESUMEN

Herein, the biogenic platinum nanoparticles (Pt NPs) were synthesized by using black cumin seed (Nigella sativa L.) extract as a reducing agent. The biogenic platinum nanoparticles synthesized by black cumin seed extract was characterized in detail by Transmission Electron Microscopy (TEM), UV-vis spectrophotometer, X-ray diffraction (XRD), X-ray photoelectron spectroscopy (XPS). According to TEM analysis, Pt nanoparticles have spherical shapes and sizes between 1-6 nm. Moreover, the biogenic Pt NPs was assessed for its cytotoxicity effect on MDA-MB-231 breast and HeLa cervical cancer lines and their antibacterial effect against selected strains of gram-positive and negative bacteria. The cytotoxicity and bacterial tests showed the effectiveness of biogenic Pt nanoparticles. Dose-dependent toxicity effects were shown in the MDA-MB-231 breast and HeLa cervical cancer lines (IC50: 36.86 µg/mL and 19.83 µg/mL, respectively). In addition, Pt NPs showed high zone diameters against gram-positive and gram-negative bacteria at concentrations of 100 and 500 µg/ml. These results contribute to the development of the pharmaceutical industry as a potential antibacterial and anticancer agent.


Asunto(s)
Antibacterianos/farmacología , Antineoplásicos Fitogénicos/farmacología , Nigella sativa/química , Extractos Vegetales/farmacología , Antibacterianos/administración & dosificación , Antibacterianos/aislamiento & purificación , Antineoplásicos Fitogénicos/administración & dosificación , Antineoplásicos Fitogénicos/aislamiento & purificación , Neoplasias de la Mama/tratamiento farmacológico , Línea Celular Tumoral , Relación Dosis-Respuesta a Droga , Femenino , Bacterias Gramnegativas/efectos de los fármacos , Bacterias Grampositivas/efectos de los fármacos , Células HeLa , Humanos , Concentración 50 Inhibidora , Nanopartículas del Metal , Extractos Vegetales/administración & dosificación , Platino (Metal)/química , Semillas , Neoplasias del Cuello Uterino/tratamiento farmacológico
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