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1.
Int J Biol Macromol ; 266(Pt 2): 131282, 2024 May.
Artigo em Inglês | MEDLINE | ID: mdl-38565369

RESUMO

IRF9 is a crucial component in the JAK-STAT pathway. IRF9 interacts with STAT1 and STAT2 to form IFN-I-stimulated gene factor 3 (ISGF3) in response to type I IFN stimulation, which promotes ISG transcription. However, the mechanism by which IFN signaling regulates Malabar grouper (Epinephelus malabaricus) IRF9 is still elusive. Here, we explored the nd tissue-specific mRNA distribution of the MgIRF9 gene, as well as its antiviral function in E. malabaricus. MgIRF9 encodes a protein of 438 amino acids with an open reading frame of 1317 base pairs. MgIRF9 mRNA was detected in all tissues of a healthy M. grouper, with the highest concentrations in the muscle, gills, and brain. It was significantly up-regulated by nervous necrosis virus infection and poly (I:C) stimulation. The gel mobility shift test demonstrated a high-affinity association between MgIRF9 and the promoter of zfIFN in vitro. In GK cells, grouper recombinant IFN-treated samples showed a significant response in ISGs and exhibited antiviral function. Subsequently, overexpression of MgIRF9 resulted in a considerable increase in IFN and ISGs mRNA expression (ADAR1, ADAR1-Like, and ADAR2). Co-immunoprecipitation studies demonstrated that MgIRF9 and STAT2 can interact in vivo. According to the findings, M. grouper IRF9 may play a role in how IFN signaling induces ISG gene expression in grouper species.


Assuntos
Bass , Fator Gênico 3 Estimulado por Interferon, Subunidade gama , Animais , Fator Gênico 3 Estimulado por Interferon, Subunidade gama/metabolismo , Fator Gênico 3 Estimulado por Interferon, Subunidade gama/genética , Bass/genética , Bass/imunologia , Bass/metabolismo , Nodaviridae , Proteínas de Peixes/genética , Proteínas de Peixes/metabolismo , Doenças dos Peixes/virologia , Doenças dos Peixes/imunologia , Sequência de Aminoácidos , Poli I-C/farmacologia , Regulação da Expressão Gênica/efeitos dos fármacos , Antivirais/farmacologia , Regiões Promotoras Genéticas , Filogenia , RNA Mensageiro/genética , RNA Mensageiro/metabolismo
2.
Drug Des Devel Ther ; 18: 597-612, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38436040

RESUMO

Purpose: New bioactive anthraquinone derivatives are investigated for antibacterial, tyrosinase inhibitory, antioxidant cytotoxic activity, and molecular docking. Methods: The compounds were produced using the grindstone method, yielding 69 to 89%. These compounds were analyzed using IR, 1H, and 13C NMR and elemental and mass spectral methods. Additionally, the antibacterial, antioxidant, and tyrosinase inhibitory activities of all the synthesised compounds were evaluated. Results: Compound 2 showed remarkable tyrosinase inhibition activity, with an (IC50: 13.45 µg/mL), compared to kojic acid (IC50: 19.40 µg/mL). It also exhibited moderate antioxidant and antibacterial activities with respect to the references BHT and ampicillin, respectively. Kinetic analysis revealed that the tyrosinase inhibitory activity of compound 2 was non-competitive and competitive, whereas that of compound 1 was low. All compounds (1-8) were significantly less active than doxorubicin (LC50: 0.74±0.01µg/mL). However, compound 2 affinity for the 2Y9X protein was lower than kojic acid, with a lower docking score (-8.6 kcal/mol compared to (-4.7 kcal/mol), making it more effective. Conclusion: All synthesized compounds displayed remarkable antibacterial, tyrosinase inhibitory, antioxidant, and cytotoxic activities, with compound 2 showing exceptional potency as a multitarget agent. Anthraquinone substituent groups may offer the potential for the development of treatments. The derivatives were synthesized using the grindstone method, and their antibacterial, antioxidant, tyrosinase inhibitory, and cytotoxic activities were inspected. Molecular docking and molecular dynamics simulations were performed using compound 2 and kojic acid to validate the results and confirm the stability of the compounds.


Assuntos
Agaricales , Antineoplásicos , Ciclopentanos , Monofenol Mono-Oxigenase , Simulação de Acoplamento Molecular , Antioxidantes/farmacologia , Cinética , Antibacterianos/farmacologia , Antraquinonas/farmacologia
3.
Heliyon ; 10(4): e25285, 2024 Feb 29.
Artigo em Inglês | MEDLINE | ID: mdl-38370249

RESUMO

In this study, rifaximin with copper (Cu) and copper oxide (CuO) nanoparticles (NPs) were synthesised. The resultant CuO nanoparticles were used to degrade Rhodamine B (RhB) and Coomassie Brilliant Blue (G250). Rifaximin copper and copper oxide nanoparticles were characterised using Fourier-transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), scanning electron microscopy (SEM), ultraviolet-visible spectroscopy (UV), X-ray Photoelectron Spectroscopy (XPS), Transmission Electron Microscopy (TEM), and gas chromatography-electrochemical mass spectrometry (GC-EI-MS). An FT-IR study confirmed the formation of Cu in the 562 cm-1 peak range. Rifaximin Cu and CuO Nanoparticles displayed UV absorption peaks at 253 nm and 230 nm, respectively. Coomassie Brilliant Blue G250 was completely decolourised in Cu nanoparticles at 100 %, and Rhodamine B was also decolourised in Rifaximin CuO nanoparticles at 73 %, although Coomassie Brilliant Blue G250 Rifaximin Cu nanoparticles absorbed a high percentage of dye decolorization. The aerobic oxidation of isopropanol conversion was confirmed by GC-MS analysis. Retention time of 27.35 and 30.32 was confirmed using Cu and CuO nanoparticles as the final products of 2-propanone. It is used in the textile and pharmaceutical industries for aerobic alcohol oxidation. Rifaximin CuO nanoparticles highly active in aerobic oxidation. The novelty of this study is that, for the first time, rifaximin was used for the synthesis of copper and copper oxide nanoparticles, and it successfully achieved decolorization and aerobic oxidation.

4.
Heliyon ; 10(3): e25168, 2024 Feb 15.
Artigo em Inglês | MEDLINE | ID: mdl-38356501

RESUMO

Anthraquinones and coumarins have excellent pharmacological activities and are an important class of natural plant metabolites with various biological activities. In this study, anthraquinone-9,10-dione and coumarin derivatives were combined to develop a novel anthraquinone-connected coumarin-derivative sequence. The synthesised novel anthraquinone-connected coumarin derivatives (1a-t) were screened for in vitro antibacterial, antioxidant, and tyrosinase inhibitory activities. The antibacterial activities of the synthesised compounds (1a-t) were tested against both gram-positive and gram-negative bacteria. Specifically, compound 1t was more active against E. aerogenes than ciprofloxacin. With regard to antioxidant activity, compound 1o (50.68 % at 100 µg/mL) was highly active compared to the other compounds, whereas it was less active than the standard BHT (76.74 % at 100 µg/mL). In terms of compound 1r (9.31 ± 0.45 µg/mL) was highly active against tyrosinase inhibitory activity compared with kojic acid (10.42 ± 0.98 µg/mL). In the molecular docking study, compound 1r had a higher docking score (-8.8 kcal mol-1) than kojic acid (-1.7 kcal mol-1). DFT calculations were performed to determine the energy gap of highly active compound 1r (ΔE = 0.11) and weakly active compound 1a (ΔE = 0.12). In this study, we found that every molecule displayed significant antibacterial, antioxidant, and tyrosinase inhibitory properties. Based on these reports, compounds 1r and 1t may act as multi-target agents.

5.
RSC Adv ; 14(1): 677-688, 2024 Jan 02.
Artigo em Inglês | MEDLINE | ID: mdl-38173593

RESUMO

In this study, we developed a novel pyrazolo[3,4-c]pyrazole derivative with antibacterial and antifungal activities that shows great potential for treating infectious diseases. To evaluate the binding affinity of 1AJ0 and 1AI9 proteins for developing potent antibacterial and antifungal compounds, we used the Vitex negundo (VN) leaf extract as the capping and reducing agent and reacted it with Fe2O3 and Cu(OAc)2 solutions to synthesize the VN-Fe3O4-CuO nanocatalyst. The newly synthesized compounds were confirmed using Fourier transform infrared spectroscopy, transmission electron microscopy, UV-visible spectroscopy, and X-ray diffraction analyses. Antibacterial screening revealed that compound 1g was highly active against Escherichia coli (MIC: 1 µg mL-1) and was much more effective than the standard ciprofloxacin. Compound 1b showed a higher antifungal activity than clotrimazole against Candida albicans (MIC: 0.25 µg mL-1) and cytotoxic activity against MCF-7 cancer cell lines. Compounds 1a-1l were exhibited low cytotoxicity activity compared to the standard doxorubicin (LC50: 21.05 ± 0.82 µg mL-1). To further support the discovery of new active antibacterial agents, compounds 1g and 1b and proteins 1AJ0 and 1AI9 were examined using the AutoDock Vina program and were compared with the standards ciprofloxacin and clotrimazole. With the 1AJ0 protein, compound 1g had a higher docking score (-3.7 kcal mol-1) than ciprofloxacin (-5.6 kcal mol-1), and with the 1AI9 protein, compound 1b had a higher docking score (-4.8 kcal mol-1) than clotrimazole (-4.4 kcal mol-1). Additionally, molecular dynamics simulation was used to investigate the most probable binding mode of compounds 1b and 1g with 1AI9 and 1AJ0, respectively. The VN-Fe3O4-CuO catalyst was used to prepare pyrazolo[3,4-c]pyrazole derivatives, which were successfully characterized and screened for antimicrobial and cytotoxic activities, molecular docking, and molecular dynamics simulation studies.

6.
BMC Chem ; 17(1): 155, 2023 Nov 18.
Artigo em Inglês | MEDLINE | ID: mdl-37980500

RESUMO

This paper deals with the evaluation of novel imidazole molecules for their antimicrobial and larvicidal activities. A series of imidazole derivatives 1(a-f) and 2(a-e) were prepared by the Mannich base technique using a Cu(II) catalyst. The Cu(phen)Cl2 catalyst was found to be more effective than other methods. FTIR, elemental analyses, mass spectrometry, 1H NMR, and 13C NMR spectroscopy were performed to elucidate the structures of the synthesised compounds. Antimicrobial and larvicidal activities were investigated for all compounds. The antibacterial activity of compounds (2d) and (2a) were highly active in S.aureus (MIC: 0.25 µg/mL) and K.pneumoniae (MIC: 0.25 µg/mL) compared to ciprofloxacin. Compound (1c) was significantly more effective than clotrimazole in C.albicans (MIC: 0.25 µg/mL). Molecular docking studies of compound 2d showed a higher binding affinity for the 1BDD protein (- 3.4 kcal/mol) than ciprofloxacin (- 4.4 kcal/mol). Compound 1c had a higher binding affinity (- 6.0 kcal/mol) than clotrimazole (- 3.1 kcal/mol) with greater frontier molecular orbital energy and reactivity properties of compound 1c (∆E gap = 0.13 eV). The activity of compound 1a (LD50: 34.9 µg/mL) was more effective in the Culex quinquefasciatus than permethrin (LD50: 35.4 µg/mL) and its molecular docking binding affinity for 3OGN protein (- 6.1 kcal/mol). These newly synthesised compounds can act as lead molecules for the development of larvicides and antibiotic agents.

7.
Prev Med ; 174: 107620, 2023 09.
Artigo em Inglês | MEDLINE | ID: mdl-37451554

RESUMO

Currently, the risks posed by bacteria are becoming increasingly important. It now appears that the cell wall of Anammox image bacteria is very different from what has been generally considered for many years. Not every textbook contains the peptidoglycan on the cell wall of Anammox image bacteria - the sugar-protein chain that strengthens the cells of most bacteria. Most researchers in this Anammox image bacteria diseased identification wanted to find out what gave the Anammox image cell its stability. It used powerful cryo-electron microscopes to examine the bacterial cell wall and find the exact structure of the peptidoglycan. A new algorithm is proposed to discover that Anammox image bacteria contain peptidoglycan, which completes a theory in microbiology. The identification of different diseases is listed, and the proposed model compares the exact results while comparing the parameters like accuracy, precision, recall, and F1-Score. Keywords: Anammox image bacteria, cell wall, cell stability, cryo-electron, microscope images, accuracy, precision, recall, F1-score.


Assuntos
Oxidação Anaeróbia da Amônia , Peptidoglicano , Humanos , Peptidoglicano/metabolismo , Oxirredução , Anaerobiose , Bactérias/metabolismo
8.
Chemosphere ; 318: 137928, 2023 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-36706811

RESUMO

In this research, we looked at how heterostructure fabrication, phase ratio, and crystalline nature affect the photocatalytic activity of ZnO/ZnFe2O4 nanocomposite for the degradation of Rhodamine B (RhB) dye when exposed to sunlight irradiation. Magnetic ZnO/ZnFe2O4 hybrid nanocomposites were made using a co-precipitation technique. The synthesized hybrid nanocomposite were analyzed using a variety of characterization techniques to understand more about their chemical, crystallinity, and photoactive characteristics. Using UV-Visible spectra, the absorption and photocatalytic efficiency of photocatalysts were investigated. By using XPS and FTIR measurements, the surface composition and functionalization of the produced nanocomposite were observed. The synthesized ZnO/ZnFe2O4 nanocomposites exhibit irregular morphologies, and the average crystallite size is about 30 nm, by the findings of the transmission electron microscope. When exposed to solar light for 90 min, the prepared photocatalysts exceed ZnO nanoparticles in terms of photocatalytic performance by more than 45%. Pseudo-first-order kinetics governs the adsorption of RhB onto nanocomposite surfaces. Finally, the ZnO/ZnFe2O4 nanocomposites were employed for antibacterial treatments against the waterborne pathogens Escherichia coli (E.coli) and Staphylococcus aureus (S.aureus). The outcomes demonstrated that the optimal disinfection efficiency against E. coli and S. aureus germs were 98.6 and 97.4%, respectively, associated with superior cycling durability. Therefore, this work offers a simple and rapid approach to the development of hybrid nanocomposites that could be used to create various photocatalytic and optical materials.


Assuntos
Poluentes Ambientais , Nanocompostos , Óxido de Zinco , Óxido de Zinco/química , Escherichia coli , Poluentes Ambientais/química , Staphylococcus aureus , Nanocompostos/química , Catálise
9.
Front Chem ; 11: 1303479, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-38268759

RESUMO

The grindstone process, which uses tyrosinase as a catalyst, was used to create analogues of geranylacetone. Tyrosinase was used to prepare the Mannich base under favourable reaction conditions, resulting in a high yield. All synthesized compounds were characterized using FTIR, Nuclear magnetic resonance, and mass spectral analyses. The active geranylacetone derivatives (1a-l) were investigated for larvicidal activity against Culex quinquefasciatus; compound 1b (LD50:20.7 µg/mL) was noticeably more effective than geranylacetone (LD50: >100 µg/mL) and permethrin (LD50: 24.4 µg/mL) lead compounds because of their ability to kill larvae and use them as pesticides. All compounds (1a-1l) were found to be low toxic, whereas compounds 1b, 1d, and 1k were screened for antifeedant screening of non -aquatic target for the toxicity measurement against marine fish Oreochromis mossambicus at 100 µg/mL caused 0% mortality in within 24 h. Molecular docking studies of synthesised compound 1b and permethrin docked with 3OGN, compound 1b demonstrated a greater binding affinity (-9.6 kcal/mol) compared to permethrin (-10.5 kcal/mol). According to these results, the newly synthesised geranylacetone derivatives can serve as lead molecules of larvicides agents.

10.
Drug Des Devel Ther ; 16: 4021-4039, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-36439378

RESUMO

Purpose: This study aims to determine the analgesic activity of 1,4-dihydropyridine hybrid benzamide derivatives. These hybrid derivatives were synthesized, and their analgesic activity was studied. The synthesis method applied was a one-step reaction involving a green chemistry approach. Methods: The compounds were prepared via the amination method with a yield ranging between 82% and 93%. The title compounds were confirmed by means of IR, 1H and 13C NMR, and mass spectral analyses. The pharmacological activity of all the synthesized compounds was evaluated, and the analgesic activities were monitored in vivo (by tail immersion methods), with a digital analgesiometer. The drug response and damage of tail ata concentration of 10 mg/kg were measured by tail-flicking latency. Results: The activity of compound 2c (81.35% activity at 5mg/kg) can be correlated with its salicylamidemoiety (13.99% activity at 5mg/kg), and diclofenac showed comparable activity (79.21% activity at 5mg/kg reference drugs). Compound 2c has a higher potential to inhibit COX proteins compared to diclofenac. The drug-like nature of the molecule 2c corresponds to its ADME properties. Conclusion: In this study, all the synthesized compounds were found to possess significant analgesic activities; particularly, the performance of compound 2c is excellent. Thus, the preparative method described is an apt route for developing novel therapeutic formulations.


Assuntos
Diclofenaco , Compostos Heterocíclicos , Simulação de Acoplamento Molecular , Anti-Inflamatórios não Esteroides/química , Analgésicos/química , Benzamidas/farmacologia
11.
Molecules ; 26(21)2021 Nov 03.
Artigo em Inglês | MEDLINE | ID: mdl-34771072

RESUMO

The synthesis of nanoparticles is most important in the context of cancer therapy, particularly copper nanoparticles, which are widely used. In this work, copper(II)-tyrosinase was isolated from potato peel powder. Copper nanoparticles (Tyr-Cu(II)-AEEA NPs) were synthesized via the reaction of tyrosinase with N-aminoethylethanolamine to produce Cu(II)-NPs and these were characterized by means of FT-IR, UV-Spectroscopy, XRD, SEM, TEM and a particle size analyzer. These Tyr-Cu(II)-AEEA NPs were tested as anticancer agents against MCF-7 breast cancer cells. Fluorescence microscopy and DNA fragmentation were also performed, which revealed the inhibiting potentials of Cu(II)-AEEA NPs and consequent cell death; Tyr-Cu(II)-AEEA NPs show potential cytotoxicity activity and this nano material could be contemplated as an anticancer medicament in future investigations.


Assuntos
Antineoplásicos/farmacologia , Complexos de Coordenação/farmacologia , Cobre/farmacologia , Etanolaminas/farmacologia , Nanopartículas Metálicas/química , Monofenol Mono-Oxigenase/metabolismo , Solanum tuberosum/metabolismo , Antineoplásicos/química , Antineoplásicos/metabolismo , Proliferação de Células/efeitos dos fármacos , Complexos de Coordenação/química , Complexos de Coordenação/metabolismo , Cobre/química , Cobre/metabolismo , Ensaios de Seleção de Medicamentos Antitumorais , Etanolaminas/química , Etanolaminas/metabolismo , Feminino , Humanos , Células MCF-7 , Microscopia de Fluorescência , Solanum tuberosum/química
12.
Drug Des Devel Ther ; 15: 787-802, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-33654383

RESUMO

PURPOSE: This study aimed to determine the extent of contribution of dopamine to antioxidant and anti-tyrosinase activities, by dopamine addition to vanillin. This study achieved the synthesis of dopamine-associated vanillin Mannich base derivatives prepared via a one-step reaction involving a green chemistry approach, and investigation of antioxidant and anti-tyrosinase activities. METHODS: Novel one-pot synthesis of Mannich base dopamine-connected vanillin (1a-l) derivatives can be achieved via green chemistry without using a catalyst. Newly-prepared compounds were characterised with FTIR and NMR (1H and 13C) spectra, mass spectra, and elemental analyses. In total, 12 compounds (1a-l) were synthesised and their antioxidant and anti-tyrosinase activities evaluated. Antioxidant activities of 2,2-diphenyl-1-picrylhydrazyl (DPPH), nitric oxide (NO), hydrogen peroxide (H2O2), and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), and diammonium assays, ABTS•+ radical scavenging, and linoleic acid peroxidation were used to screen all synthesised compounds (1a-l) for anti-tyrosinase activities and cytotoxicity against MCF-7 and Vero cell lines;. RESULTS: The compound 1k inhibited (IC50:11.02µg/mL) the DPPH-scavenging activity to a greater extent than the standard BHT (IC50:25.17µg/mL), and showed high activity in H2O2 and NO scavenging assays. Compound 1e was more potent (96.21%) against ABTS and compound 1k was more potent (95.28%) against 2,2'-azobis(2-amidinopropane)dihydrochloride antioxidant than the standard trolox. All synthesised compounds were screened for anti-tyrosinase inhibitory activity. Compound 1e had higher activity against tyrosinase (IC50=10.63 µg/mL), than kojic acid (IC50=21.52µg/mL), and was more cytotoxic (GI50 0.01µM) against MCF-7 cell line than the doxorubicin standard and other tested compounds. CONCLUSION: In this study, all compounds were found to possess significant antioxidant and anti-tyrosinase activities. Compounds 1e and 1k performed well, compared with other compounds, in all assays. In addition, this study successfully identified several promising molecules that exhibited antioxidant and anti-tyrosinase activities.


Assuntos
Antineoplásicos/farmacologia , Antioxidantes/farmacologia , Benzaldeídos/farmacologia , Dopamina/farmacologia , Inibidores Enzimáticos/farmacologia , Monofenol Mono-Oxigenase/antagonistas & inibidores , Animais , Antineoplásicos/síntese química , Antineoplásicos/química , Antioxidantes/síntese química , Antioxidantes/química , Benzaldeídos/química , Benzotiazóis/antagonistas & inibidores , Compostos de Bifenilo/antagonistas & inibidores , Sobrevivência Celular/efeitos dos fármacos , Chlorocebus aethiops , Dopamina/química , Inibidores Enzimáticos/síntese química , Inibidores Enzimáticos/química , Química Verde , Humanos , Peróxido de Hidrogênio/antagonistas & inibidores , Células MCF-7 , Estrutura Molecular , Monofenol Mono-Oxigenase/metabolismo , Óxido Nítrico/antagonistas & inibidores , Picratos/antagonistas & inibidores , Ácidos Sulfônicos/antagonistas & inibidores , Células Vero
13.
Saudi J Biol Sci ; 28(1): 1123-1127, 2021 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-33424406

RESUMO

An endangered and rare species Aloe pseudorubroviolacea from the plant family Asphodelaceae which is presently recorded as endangered in Saudi Arabia collected from Al-Baha region of Saudi Arabia its GPS Latitude and Longitude coordinates 19.8345, 41.5481. The chloroplast matK and rbcL gene was considered in this study based on molecular identification the size is about 571 and 664 bp respectively. From the sequence analysis the gene matK and rbcL confirm that this species is very much closely related with A. rubroviolacea and also inter related with the species Astroloba rubriflora, Chrysopogon gryllus, Chortolirion angolense shows about 98.7% sequence homology. The partial matK and rbcL gene sequence discriminate Aloe pseudorubroviolacea from the closely related plant species, A. rubroviolacea. The gene sequence of rbcL discriminates the species from Chrysopogon gryllus and Chortolirion angolense, demonstrates the nucleotide variations in 3 different sites (623C/T; 653C/T; 700C/A). This study showed that matK and rbcL sequence region of chloroplast gene used to authenticate the samples of A. pseudorubroviolacea and which provide to help in correct identification and conservation process of this medicinally valuable endangered plant species.

14.
Saudi J Biol Sci ; 27(4): 1130-1138, 2020 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-32256175

RESUMO

The ZnO particle with varieties of morphology was prepared from ice-cube of zinc ammonium complex at boiling water surface in 1 min induction of thermal shock. The zinc ammonium complex in ice cube was developed using zinc acetate and biologically activated ammonia in 1 hr and kept in the freezer. Temperature gradient behaviour of the water medium during thermal shock was captured by the thermal camera and thermometer. Morphology study revealed a variety of flower-like ZnO particles with variable size from 1.0 to 2.5 µm. Further, ZnO particle morphologies were tuned by adding trisodium citrate and hexamine to obtain uniform spherical (2-3 µm) and flower (3-4 µm) shapes, respectively. XRD patterns revealed that all ZnO samples are of a hexagonal structure. Photocatalytic inactivation of E. coli has been investigated using various particle morphologies of ZnO in an aqueous solution/overcoated glass slide under sunlight. The photo-inactivation of E. coli by ZnO particles in suspension condition was better when compared to a coated glass slide method. AFM study confirmed the destruction of bacterial cell wall membrane by the photocatalytic effect. The particles morphology of photocatalyst is well dependent on antibacterial activity under sunlight.

15.
Saudi J Biol Sci ; 27(2): 666-675, 2020 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-32210686

RESUMO

To evaluate phytochemical constituents from the methanolic extracts of medicinal plants Aloe castellorum and Aloe pseudorubroviolacea. The cytotoxic activity of Aloe castellorum and Aloe pseudorubroviolacea leaf extracts against Human colon cancer cell line (HCT-116) was also assessed. The two medicinal plant extracts having significant cytotoxic activity, meanwhile the methanolic extract of Aloe castellorum shows higher cytotoxic activity than Aloe pseudorubroviolacea extract. The Aloe castellorum shows remarkable activity against respective cell line than control. The characteristic chemical constituents of Aloe castellorum and Aloe pseudorubroviolacea leaf extracts were recognized from Gas chromatography and Mass spectrometry (GC-MS) technique. The molecular docking studies also support the cytotoxic activity.

16.
Saudi J Biol Sci ; 26(4): 673-680, 2019 May.
Artigo em Inglês | MEDLINE | ID: mdl-31048991

RESUMO

The objective of this study was to investigate brine shrimp cytotoxicity, larvicidal, nematicidal, and antifeedant activities of novel piperidin-connected 2-thioxo-imidazolidin-4-one derivatives. The activities of target compounds were compared with some naturally occurring (-)-pinidinol, hydantocidin, and positive controls. Target compounds were synthesized via cyclocondensation method. The compounds were synthesized and then characterized by infrared spectroscopy, 1H NMR, 13C NMR, mass spectral, and elemental analyses. Brine shrimp cytotoxicity assay was investigated using freshly hatched, free-swimming nauplii of Artemiasalina. Larvicidal screening was performed against urban mosquito larvae (Culex quinquefasciatus). Nematicidal activity was evaluated using juvenile nematodes of Meloidogyne javanica. Regarding antifeedant activity, marine-acclimated Oreochromis mossambicus fingerlings were used. Compounds 3a-c (piperidin-connected 2-thioxoimidazolidin-4-one) were found to be lethal to the second instar larvae of mosquito, which produced LD50 values of 1.37, 6.66, 6.51 µg/mL, compared to compounds (-) pinidinol and hyantocidin LD50 values of 18.28 and 22.11 µg/mL respectively. Compound 3a-c was found to kill 100% of fish fingerlings within 6 h at 20 µg/mL, with LD50 values of 1.54, 1.79, 1.52 µg/mL, compared to compounds (-) pinidinol and hyantocidin with LD50 values of 10.21 and 21.05 µg/mL respectively. Compound 3c with LD50 value of 1.57 µg/mL demonstrated high nematicidal activity compared to compound 3a, 3b, (-) Pinidinol and Hyantocidin LD50 values of 6.45, 2.42, 14.25, 26.30 µg/mL respectively. Therefore, the 2-thioxoimidazolidin-4-one with piperidin ring showed high potential cytotoxic, larvicidal, nematicidal, and antifeedent activities.

17.
Saudi J Biol Sci ; 25(7): 1387-1392, 2018 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-30505186

RESUMO

Evaluation of antioxidant and anticancer activities were screened by various Saururus chinensis root extracts. Four solvents (ethyl acetate, methanol, ethanol, and water) extracts were investigated for their total flavonoids, phenol contents and their antioxidant activity of DPPH (2,2-diphenyl-1-picrylhydrazyl), NO (nitric oxide), H2O2 (hydrogen peroxide), ABTS 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonicacid)diammonium assays, FRAP (ferric reducing ability of plasma) assays and anticancer activity. The total phenolic and flavonoid content of extracts were determined by using FC (Folin-Ciocalteu) and AlCl3 colorimetric assay method. Total flavonoid content in these plants ranged from 24.7 to 72.1 mg g-1 and amount of free phenolic compounds was between 11.2 and 67.1 mg g-1 extract. The all extracts have significant levels of phenolics and flavonoids content. Anticancer activity was screened for MCF-7 breast cancer cell line. Ethanol extract shows significant of antioxidant activity and water extract shows significant of anticancer activity compared with standard (BHT) butylated hydroxy toluene. These ethanol and water extracts could be considered as a natural source for using antioxidant, and anticancer agents compared to commercial available synthetic drugs.

18.
Nanoscale Res Lett ; 13(1): 315, 2018 Oct 04.
Artigo em Inglês | MEDLINE | ID: mdl-30288618

RESUMO

To address the growing challenges from drug-resistant microbes and tumor incidence, approaches are being undertaken to phytosynthesize metal nanoparticles, particularly silver nanoparticles, to get remedial measure. In this study, an attempt has been made to utilize a major biowaste product, pomegranate fruit peel (Punica granatum), to synthesize silver nanoparticles. The silver nanoparticles (AgNPs) were synthesized using the aqueous extract of pomegranate peel. The formation of synthesized AgNPs was confirmed through UV-Vis spectroscopy, X-ray diffraction (XRD), transmission electron microscopy (TEM), scanning electron microscopy (SEM), and energy-dispersive X-ray spectroscopy (EDX) as well as through the change of the colorless aqueous solution to a dark brown solution. Using UV-Vis spectroscopy, the dark brown solution showed a Plasmon resonance band peak at 378 nm in UV-Vis spectroscopy after reacting for 24, 48, and 72 h. The XRD report revealed that the AgNPs had a cubic structure. The TEM and SEM report showed the nanoparticles were equally distributed in the solution, with a spherical shape and size ranging from 20 to 40 nm and with an average particle size of 26.95 nm. EDX imaging also confirmed the presence of AgNPs. The synthesized AgNPs were found to exhibit good antimicrobial effects on Gram-negative and Gram-positive bacteria, particularly the pathogens Escherichia coli (ATCC 25922), Pseudomonas aeruginosa (ATCC 27584), Proteus vulgaris (ATCC 8427), Salmonella typhi (ATCC 14028), Staphylococcus aureus (ATCC 29213), Staphylococcus epidermidis (MTCC 3615), and Klebsiella pneumonia. The cytotoxic effects of AgNPs were also tested against a colon cancer cell line (RKO: ATCC® CRL-2577™), and it was observed that the viabilities were 56% and 61% on days 3 and 5, respectively, with exposure to 12.5 µg of AgNPs. This simple, economic, and eco-friendly method suggests that the AgNPs biosynthesized using pomegranate peel extract may be a novel, potent solution for the development of a drug for colon cancer that also has antibacterial activity.

19.
Saudi J Biol Sci ; 25(6): 1227-1235, 2018 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-30174527

RESUMO

A new series of 1,4-dihydropyridine derivatives (2a-h, 3a-e, and 4a-e) were systematically designed and synthesized via ultrasound irradiation methods with easy work-up and good yields. Compounds structures were confirmed by IR, 1H NMR, 13C NMR, and mass spectra. The synthesized compounds were screened for both antimicrobial and anticoagulant activities. Compound 2e (MIC: 0.25 µg/mL) was highly active against Escherichia coli and compound 2c (MIC: 0.5 µg/mL) was also highly active against Pseudomonas aeruginosa compared with ciprofloxacin. (MIC: 1 µg/mL) The antifungal activity of 2c (MIC: 0.5 µg/mL) against Candida albicans was high relative to that of clotrimazole (MIC: 1 µg/mL). Anticoagulant activity was determined by activated partial thromboplastin time (APTT) and prothrombin time (PT) coagulation assays. Compound 4-(4-hydroxyphenyl)-2,6-dimethyl-N3,N5-bis(5-phenyl-1,3,4-thiadiazol-2-yl)-1,4-dihydropyridine-3,5-dicarboxamide 3d (>1000 s in APTT assays) was highly active in anticoagulant screening compared with the reference of heparin. Cytotoxicity was evaluated using HepG2 (liver), HeLa (cervical), and MCF-7 (breast) cancer cell lines, with high toxicities observed for 2c (GI50 = 0.02 µm) against HeLa cell line and 2e (GI50 = 0.03 µm) equipotant against MCF-7 cell line. Therefore, the compounds 2e, 2c and 3d can serve as lead molecules for the development of new classes of antimicrobial and anticoagulant agent.

20.
Fish Shellfish Immunol ; 73: 245-251, 2018 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-29277365

RESUMO

The purpose of the present study was to find out the effect of dietary enriched button mushroom, Agaricus bisporus at 1%, 5%, and 10% levels on growth performance, hematology, nonspecific immune responses, and disease resistance in catfish, Clarias gariepinus against Flavobacterium columnare for a period of four weeks. The percentage weight gain and specific growth rate (SGR) were higher in the infected fish fed with 5% A. bisporus enriched diet than with 1% and 10% diets. The red blood cell (RBC), white blood cell (WBC), hematocrit (PCV), and haemoglobin (Hb) values are similar (p > .05) among the experimental groups at the end of fourth week. The phagocytic activity, complement activity, and lysozyme activity were significantly enhanced in the infected fish fed with 5% A. bisporus diet during the experimental period; however, it was significantly enhanced with 10% A. bisporus enriched diet only on weeks 2 and 4. On the other hand, the respiratory burst (RB) activity increased significantly in the infected fish fed with 5% and 10% A. bisporus enriched diets. When fed with 5% A. bisporus diet the cumulative mortality was very low (10%), followed by a high survival rate (89%) in the infected fish; nevertheless, the cumulative mortality was 25% and 20% while it was 74% and 79% when fed with 1% and 10% enriched diets. The present study recommends a dietary supplement of A. bisporus at 5% or 10% level to achieve better growth without side effect, and enhance the nonspecific immune system that prevent mortalities from F. columnare infection in C. gariepinus.


Assuntos
Agaricus/química , Peixes-Gato/imunologia , Resistência à Doença/efeitos dos fármacos , Doenças dos Peixes/imunologia , Imunidade Inata/efeitos dos fármacos , Ração Animal/análise , Animais , Peixes-Gato/sangue , Peixes-Gato/crescimento & desenvolvimento , Dieta/veterinária , Suplementos Nutricionais/análise , Infecções por Flavobacteriaceae/imunologia , Flavobacterium/fisiologia
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