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Background: Colon carcinoma poses a significant health challenge globally, particularly in developed nations where sedentary lifestyles, poor dietary choices, and genetic factors play a crucial role in its prevalence. Chemotherapy, the primary treatment method, carries severe side effects that can jeopardize patients' lives. Herbal extracts such as Ocimum Basillicum extract have shown effectiveness against cancer cells. Additionally, nanoparticles can significantly enhance drug delivery efficacy in these scenarios. Aim: This article aims to investigate the impact of copper nanoparticles coated with Ocimum Bassilicum at chemoradiotherapy of Colon Carcinoma to hopefully create new treatment options with fewer side effects for patients. Methodology: CuO bio-NPs were produced by the addition of 15 mL of extract dropwise to 80 mL of a 5 mM Cu (OAc)2 aqueous solution, which was then refluxed for 2 h at 100 °C. The mixture gradually became darker brown in color as a result of the heating procedure. The production of CuO NPs and the hydrogen-donating activity of antioxidant phenols within the plant are signaled by surface plasmon resonance excitation, which is the cause of this. In the cell culture, LS174t colon cancer cells were treated with OB extract, CuNPs, and OB-coated CuNPs with and without different radiation levels in order to assess cell viability, through the MTT assay, and the pro-apoptotic BAX and anti-apoptotic BCL2 expressions, through qPCR assay. Results: The results demonstrate a decrease in cell viability and the expression of BCL2 and an increase in the expression of BAX especially when treated with OB-coated CuNPs and even furthermore when paired with radiation therapy. Conclusions: After doing the clinical trial studies, the recent nanoparticles can be used for the treatment of Colorectal carcinoma.
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The present research studied the cytotoxicity, antioxidant, and antidiabetic activities of biogenically synthesized silver nanoparticles (AgNPs) using Ziziphora clinopodioides (Z. clinopodioides) as a green mediator. Scanning electron microscopy (SEM), transmission electron microscopy (TEM), and ultraviolet-visible spectroscopy (UV-Vis) were employed to determine AgNPs. In the in vivo experiment, the model rats were categorized into different groups receiving 50, 100, 200, and 400 µg/kg of AgNPs and diabetic, positive, and normal groups (n = 10) using a random division. A single dose of streptozotocin (STZ) at 60 mg/kg was administered to induce diabetes and hepatotoxicity in rats. The administration of AgNPs was performed via intragastric administration for 25 days. On the final day, the levels of glucose and biochemical enzymes, namely aspartate aminotransferase (AST), alkaline phosphatase (ALP), alanine transaminase (ALT), and gamma-glutamyltransferase (GGT), were assessed in the serum. Following tissue processing, liver sections with a thickness of 5 µm were prepared. Later, the total volume of different liver components, such as hepatocytes, sinusoids, portal vein, central vein, hepatic arteries, and bile ducts, was measured. The portal vein and bile duct volumes did not vary significantly in groups treated by AgNPs. However, the volume of the central vein and hepatic arteries exhibited noticeable variations in groups treated by AgNPs. After administration of streptozotocin, the volume of hepatocytes and sinusoids increased significantly. However, treatment with a high dose of AgNPs significantly decreased the volume of hepatocytes and sinusoids. In diabetic rats, administering AgNPs reduced the fasting blood glucose levels compared to the model group. In addition, AgNPs decreased the elevated levels of AST and ALP enzymes in a manner that depended on the dosage of AgNPs used. This research demonstrates the hepatoprotective and antidiabetic properties of AgNPs, suggesting their potential implications as hepatoprotective and antidiabetic supplements to prevent diabetes.
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Current methods of colon cancer treatment, especially chemotherapy, require new treatment methods due to adverse side effects. One important area of interest in recent years is the use of nanoparticles as drug delivery vehicles since several studies have revealed that they can improve the target specificity of the treatment thus lowering the dosage of the drugs while preserving the effectiveness of the treatment thus reducing the side effects. The use of traditional medicine has also been a favorite topic of interest in recent years in medical research, especially cancer research. In this research work, the green synthesis of Fe nanoparticles was carried out using Mentha spicata extract and the synthesized nanoparticles were identified using FT-IR, XRD, FE-SEM and EDS techniques. Then the effect of Mentha spicata, Fe nanoparticles, and Mentha spicata -loaded Fe nanoparticles on LS174t colon cancer cells, and our result concluded that all three, especially Mentha spicata -loaded Fe nanoparticles, have great cytotoxic effects against LS174t cells, and exposure to radiotherapy just further intensified these results. The in vitro condition revealed alterations in the expression of pro-apoptotic BAX and anti-apoptotic Bcl2, suggesting a pro-apoptotic effect from all three components, particularly the Mentha spicata-loaded Fe nanoparticles. After further clinical trials, these nanoparticles can be used to treat colon cancer.
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The growing concern about microorganism infections, especially hospital-acquired infections, has driven the demand for effective and safe agents in recent years. Herein, novel nanocomposites were prepared based on layered double hydroxides (LDH NPs), Fe2O3nanoparticles (Fe2O3NPs), and chitosan hydrogel beads in different concentrations. The characteristics and composition of the prepared materials were investigated by various techniques such as XRD, FESEM, and FTIR. The results indicate that the nanocomposites are synthesized successfully, and each component is present in hydrogel matrixes. Then, their biomedical properties, including antibacterial, antifungal, and antioxidant activity, were examined. Our findings demonstrate that the antimicrobial activity of nanocomposites significantly depends on the concentration of each component and their chemical groups. It shows itself in the result of the inhibitory zone of all bacteria or fungi samples. The obtained results indicate that the nanocomposite of Chitosan-hydrogel beads with 20% LDH and Fe2O3(CHB-LDH-Fe2O3%20) and Chitosan-hydrogel beads based on 20% LDH (CHB-LDH%20) showed excellent antibacterial and antifungal properties against all tested bacteria and fungi (P ≤ 0.01). In addition, the antioxidant effects of the synthesized materials (especially CHB-LDH Fe2O3%20 and CHB-LDH%20) were investigated, showing high antioxidant efficacy against DPPH free radicals (P ≤ 0.01). According to our findings, we can say that these materials are promising biomaterials for inhibiting some infectious bacteria and fungi.
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Quitosana , Antibacterianos/química , Antibacterianos/farmacologia , Antifúngicos/farmacologia , Antioxidantes/farmacologia , Bactérias , Materiais Biocompatíveis/farmacologia , Quitosana/química , Quitosana/farmacologia , Hidrogéis/química , Hidrogéis/farmacologia , Hidróxidos/química , Fenômenos MagnéticosRESUMO
In the present study, biocompatible nanofibers containing aqueous extracts from Muscari neglectum (M. neglectum) plants (produced nanofiber) were prepared and their antifungal and cytotoxicity effects were investigated. For this purpose, the extracts obtained from flowers, stem leaves, and fresh onion from M. neglectum were lyophilized at various concentrations. Produced nanofibers were prepared using electrospinning techniques. During the electrospinning process, two auxiliary natural polymers including gelatin and chitosan were used. After synthesis, the physicochemical properties of the nanofibers were confirmed by Scanning Electron Microscopy (SEM), Fourier-transform infrared spectroscopy (FTIR), and X-ray energy diffraction spectroscopy (EDS or EDX), and Differential Scanning Calorimetry (DSC). The electrospun produced nanofibers have continuous and uniform structures. The cytotoxicity assay of these electrospun nanofibers were done on Human dermal fibroblast cell (HDF) and HUVEC cell (Human Umbilical Endothelial Cells) lines and results showed that nanofiber doesn't have any toxicity to normal cell lines. For anti-fungal activity tests, the appropriate amounts of nanofibers containing M. neglectum were placed in media with five different fungal species utilizing two methods: disc diffusion and well diffusion. In vitro results showed that all electrospun nanofibers containing M. neglectum had strong antifungal activity against Candida albicans, Glabrata, Parapacillus, Guillermoides, Crocus fungi species. Our findings also showed that nanofibers containing 86.88% polyvinyl alcohol/ gelatin/ chitosan/ M. neglectum root extract (produced nanofibers) were had better swelling and physicochemical properties and stronger antifungal activity than others (fiber formed with plant root). In a nutshell, natural nanofibers can be used as a beneficial drug delivery system.
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Quitosana , Nanofibras , Antifúngicos/farmacologia , Quitosana/química , Quitosana/farmacologia , Células Endoteliais , Gelatina/química , Gelatina/farmacologia , Humanos , Nanofibras/química , Polímeros/química , Álcool de Polivinil , Espectroscopia de Infravermelho com Transformada de FourierRESUMO
At the moment, metallic nanoparticles especially copper nanoparticles are administrated for the cure of different disorders, such as tumor and cancer. In recent years, many chemotherapeutic supplements have been formulated by copper nanoparticles. In the present study, copper nanoparticles were prepared and synthesized in aqueous medium using Camellia sinensis leaf extract. The as-prepared Cu2O nanoparticles was thoroughly characterized using XRD, FT-IR, FESEM, EDX, TEM and X-ray elemental mapping techniques. The as-synthesized Cu2O/C. sinensis NPs applied as novel nanocatalyst for the synthesis of annulated fused pyrano[2,3-d]pyrimidinones via a one-pot, three-component condensation of a barbituric acid, aromatic aldehydes, and malonitrile or ethylcyanoacetate under mild condition at 25 °C. Main properties of this facile method are the involves an easy work-up procedure, avoidance of hazardous or polluting chemicals, significant yields under mild conditions, and one-pot reaction. We assessed the anti-human ovarian cancer potentials of these nanoparticles against Caov-3, SW-626, and SK-OV-3 cell lines. For investigating the antioxidant activities of CuCl2â 2H2O, C. sinensis, and copper nanoparticles, the DPPH free radical test was used. For the determining of anti-human ovarian cancer properties of CuCl2â 2H2O, Camellia sinensis leaf aqueous extract, copper nanoparticles, and Carboplatin (Standard positive control), MTT assay was used on normal (HUVECs) and human ovarian cancer (Caov-3, SW-626, and SK-OV-3) cell lines. Copper nanoparticles had high cell death and anti-human ovarian cancer properties against Caov-3, SW-626, and SK-OV-3 cell lines. Among the above cell lines, the best result was gained in the cell line of SW-626. According to the above findings, it looks copper nanoparticles green-synthesized by Camellia sinensis leaf aqueous extract have the potential to be used as a chemotherapeutic material for human ovarian cancers.
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Antineoplásicos/farmacologia , Cobre/farmacologia , Sequestradores de Radicais Livres/farmacologia , Nanopartículas Metálicas/química , Neoplasias Ovarianas/tratamento farmacológico , Extratos Vegetais/farmacologia , Antineoplásicos/química , Camellia sinensis/química , Catálise , Linhagem Celular Tumoral , Cobre/química , Ensaios de Seleção de Medicamentos Antitumorais , Feminino , Sequestradores de Radicais Livres/química , Química Verde , Células Endoteliais da Veia Umbilical Humana , Humanos , Extratos Vegetais/química , Folhas de Planta/química , Piranos/síntese química , Pirimidinas/síntese químicaRESUMO
Editor's Note: this Article has been retracted; the Retraction Note is available at https://doi.org/10.1038/s41598-020-77741-4 .
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In recent days, the green synthesized nanomagnetic biocomposites have been evolved with tremendous potential as the future catalysts. This has encouraged us to design and synthesis of a novel Au NPs immobilized pectin modified magnetic nanoparticles (Fe3O4/Pectin/Au). It was meticulously characterized using advanced analytical techniques like FT-IR, FESEM, TEM, EDX, XPS, VSM, XRD and ICP-OES. We investigated the chemical applications of the material in the catalytic reduction of nitroarenes using N2H4.H2O as the reducing agent in the EtOH/H2O solvent without any promoters or ligands. Due to strong paramagnetism, the catalyst was easily recovered and reused in 11 cycles without considerable leaching or loss in reactivity. The green protocol involves several advantages like mild conditions, easy workup, high yields, and reusability of the catalyst. Furthermore, the desired nanocomposite was employed in biological studies like anti-oxidant assay by DPPH radical scavenging test. Subsequently, on exhibiting a good IC50 value in the DPPH assay, we extended the bio-application of the Fe3O4/Pectin/Au in the anticancer study of adenocarcinoma cells of human lungs using three cancer cell lines, PC-14, LC-2/ad and HLC-1 and a normal cell line HUVEC. The best result was accomplished in PC-14 cell lines with the lowest IC50 values.
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Neoplasias Pulmonares/tratamento farmacológico , Nanopartículas de Magnetita/química , Nanocompostos/química , Pectinas/química , Catálise , Linhagem Celular Tumoral , Compostos Férricos/química , Compostos Férricos/farmacologia , Ouro/química , Ouro/farmacologia , Células Endoteliais da Veia Umbilical Humana , Humanos , Nanopartículas de Magnetita/uso terapêutico , Nanocompostos/uso terapêutico , Pectinas/farmacologia , Espectroscopia de Infravermelho com Transformada de FourierRESUMO
This work describes an eco-friendly approach for in situ immobilization of Au nanoparticles on the surface of Fe3O4 nanoparticles, with help of Agar and ultrasound irradiations, without using any toxic reducing and capping agents. The structure, morphology, and physicochemical properties were characterized by various analytical techniques such as Fourier transformed infrared spectroscopy (FT-IR), field emission scanning electron microscopy (FESEM), transmission electron microscopy (TEM), energy dispersive X-ray spectroscopy (EDS), X-ray diffraction (XRD), inductively coupled plasma (ICP) and vibrating sample magnetometer (VSM). The desired catalyst showed great efficiency in the reductive degradation of methylene orange (MO) dye over NaBH4 at room temperature. The MO was fully reduced in only 70 s and achieved rate constant of 9.6 × 10-2 s-1. The catalyst was reused for 10 runs without significant loss in catalytic activity. Cell viability of Fe3O4/agar/Au NPs was very low against breast adenocarcinoma (MCF7), breast carcinoma (Hs 578Bst), infiltrating ductal cell carcinoma (Hs 319.T), and metastatic carcinoma (MDA-MB-453) cell lines without any cytotoxicity on the normal cell line. According to the above findings, the Fe3O4/agar/Au NPs may be administrated for the treatment of several types of human breast carcinoma in humans.
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Ágar , Neoplasias da Mama/tratamento farmacológico , Corantes Fluorescentes/química , Ouro , Nanopartículas de Magnetita , Nanopartículas Metálicas , Ágar/química , Ágar/farmacologia , Neoplasias da Mama/metabolismo , Neoplasias da Mama/patologia , Catálise , Feminino , Ouro/química , Ouro/farmacologia , Humanos , Células MCF-7 , Nanopartículas de Magnetita/química , Nanopartículas de Magnetita/uso terapêutico , Nanopartículas Metálicas/química , Nanopartículas Metálicas/uso terapêuticoRESUMO
Biocomposite nanomaterials have been evolved as the new generation catalysts and therapeutic supplement in these days. Magnetically isolation has added new features to this category. This has encouraged us to synthesize a novel Ag NP adorned chitosan-alginate dual bio-polysaccharide (two of the more versatile polysaccharides) modified core-shell magnetic nanocomposite (Fe3O4/CS-Alg/Ag NPs). The material was meticulously characterized following different physicochemical techniques, such as, FT-IR, ICP-OES, FESEM, EDX, atomic mapping, TEM, VSM, XRD and XPS studies. The as synthesized material was catalytically explored in the one-pot multicomponent synthesis of biologically potent 2H-indazolo[2,1-b]phthalazine-trione derivatives involving a wide range of substrates. The reactions were ended up with excellent yields under solvent-free heating conditions. The catalyst recyclability, heterogeneity and leaching tests were performed to ensure its high stability and robustness. It could be reused as much as 10 times in succession with almost unchanged catalytic performances. In the lung protective part of the present research, the human lung toxicity was induced by α-Guttiferin. The cell viability of lung MRC-5, CCD19Lu, WI-38, and BEAS-2B cell lines was measured by trypan blue assay. Caspase-3 activity was assessed by the caspase activity colorimetric assay kit and mitochondrial membrane potential of lung cells was studied by Rhodamine123 fluorescence dye. Terminal deoxynucleotidyl transferase dUTP nick end labeling (TUNEL) test was used to show DNA fragmentation and apoptosis of lung cells. Also, the Rat inflammatory cytokine assay kit was used to measure the concentrations of inflammatory cytokines. The catalyst-treated cell cutlers significantly (p ≤ 0.01) reduced the DNA fragmentation, caspase-3 activity, and inflammatory cytokines concentrations, and raised the mitochondrial membrane potential and cell viability in the high concentration of α-Guttiferin-treated lung MRC-5, CCD19Lu, WI-38, and BEAS-2B cells. The best result of lung protective properties of catalyst against α-Guttiferin was seen in the high dose of catalyst i.e., 4 µg. DPPH test revealed similar antioxidant potentials for catalyst and butylated hydroxytoluene. The catalyst inhibited half of the DPPH molecules in the concentration of 171 µg/mL. According to the above results, catalyst can be administrated as a lung protective drug for the treatment of lung diseases after approving in the clinical trial studies in humans.
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Alginatos/química , Quitosana/química , Indazóis/química , Pulmão/citologia , Ftalazinas/química , Prata/farmacologia , Umbeliferonas/efeitos adversos , Animais , Catálise , Linhagem Celular , Sobrevivência Celular/efeitos dos fármacos , Citocinas/metabolismo , Humanos , Pulmão/efeitos dos fármacos , Pulmão/imunologia , Nanopartículas de Magnetita , Potencial da Membrana Mitocondrial/efeitos dos fármacos , Ratos , Prata/química , Espectroscopia de Infravermelho com Transformada de FourierRESUMO
In this research, we prepared and formulated a neuroprotective supplement (copper nanoparticles in aqueous medium utilizing Crocus sativus L. Leaf aqueous extract) for determining its potential against methadone-induced cell death in PC12. The results of chemical characterization tests i.e., FE-SEM, FT-IR, XRD, EDX, TEM, and UV-Vis spectroscopy revealed that the study showed that copper nanoparticles were synthesized in the perfect way possible. In the TEM and FE-SEM images, the copper nanoparticles were in the mean size of 27.5 nm with the spherical shape. In the biological part of the present research, the Rat inflammatory cytokine assay kit was used to measure the concentrations of inflammatory cytokines. Terminal deoxynucleotidyl transferase dUTP nick end labeling (TUNEL) test was used to show DNA fragmentation and apoptosis. Caspase-3 activity was assessed by the caspase activity colorimetric assay kit and mitochondrial membrane potential was studied by Rhodamine123 fluorescence dye. Also, the cell viability of PC12 was measured by trypan blue assay. Copper nanoparticles-treated cell cutlers significantly (p ≤ 0.01) decreased the inflammatory cytokines concentrations, caspase-3 activity, and DNA fragmentation and they raised the cell viability and mitochondrial membrane potential in the high concentration of methadone-treated PC12 cells. The best result of neuroprotective properties was seen in the high dose of copper nanoparticles i.e., 4 µg. According to the above results, copper nanoparticles containing C. sativus leaf aqueous extract can be used in peripheral nervous system treatment as a neuroprotective promoter and central nervous system after approving in the clinical trial studies in humans.
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Cobre/química , Crocus/química , Nanopartículas Metálicas/química , Metadona/toxicidade , Extratos Vegetais/farmacologia , Animais , Antioxidantes/farmacologia , Sobrevivência Celular/efeitos dos fármacos , Citocinas/metabolismo , Ensaios de Seleção de Medicamentos Antitumorais , Inflamação , Concentração Inibidora 50 , Potencial da Membrana Mitocondrial , Microscopia Eletrônica de Varredura , Microscopia Eletrônica de Transmissão , Células PC12/efeitos dos fármacos , Folhas de Planta/química , Ratos , Espectrofotometria Ultravioleta , Espectroscopia de Infravermelho com Transformada de Fourier , Difração de Raios XRESUMO
The aim of the experiment was a green synthesis of cobalt nanoparticles from the aqueous extract of Ziziphora clinopodioides Lam (CoNPs) and assessment of their cytotoxicity, antioxidant, antifungal, antibacterial, and cutaneous wound healing properties. The synthesized CoNPs were characterized using different techniques including UV-Vis., FT-IR spectroscopy, X-ray diffraction (XRD), energy dispersive X-ray spectrometry (EDS), scanning electron microscopy (SEM), and transmission electron microscopy (TEM). According to the XRD analysis, 28.19 nm was measured for the crystal size of NPs. TEM and SEM images exhibited a uniform spherical morphology and average diameters of 29.08 nm for the biosynthesized nanoparticles. Agar diffusion tests were done to determine the antibacterial and antifungal characteristics. Minimum inhibitory concentration (MIC), minimum bactericidal concentration (MBC), and minimum fungicidal concentration (MFC) were specified by macro-broth dilution assay. CoNPs indicated higher antibacterial and antifungal effects than many standard antibiotics (p ≤ 0.01). Also, CoNPs prevented the growth of all bacteria at 2-4 mg/mL concentrations and removed them at 2-8 mg/mL concentrations (p ≤ 0.01). In the case of antifungal effects of CoNPs, they inhibited the growth of all fungi at 1-4 mg/mL concentrations and destroyed them at 2-16 mg/mL concentrations (p ≤ 0.01). The synthesized CoNPs had great cell viability dose-dependently and indicated this method was nontoxic. DPPH free radical scavenging test was done to assess the antioxidant potentials, which revealed similar antioxidant potentials for CoNPs and butylated hydroxytoluene. In vivo experiment, after creating the cutaneous wound, the rats were randomly divided into six groups: untreated control, treatment with Eucerin basal ointment, treatment with 3% tetracycline ointment, treatment with 0.2% Co(NO3)2 ointment, treatment with 0.2% Z. clinopodioides ointment, and treatment with 0.2% CoNPs ointment. These groups were treated for 10 days. For histopathological and biochemical analysis of the healing trend, a 3 × 3 cm section was prepared from all dermal thicknesses at day 10. Use of CoNPs ointment in the treatment groups substantially raised (p ≤ 0.01) the wound contracture, hydroxyl proline, hexosamine, hexuronic acid, fibrocyte, and fibrocytes/fibroblast rate and remarkably decreased (p ≤ 0.01) the wound area, total cells, neutrophil, and lymphocyte compared to other groups. In conclusion, CoNPs can be used as a medical supplement owing to their non-cytotoxic, antioxidant, antibacterial, antifungal, and cutaneous wound healing effects. Additionally, the novel nanoparticles (Co(NO3)2 and CoNPs) were good inhibitors of the α-glycosidase, and cholinesterase enzymes.
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The present report represents the synthesis of a novel Pd NPs immobilized over a natural polysaccharide (pectin) coated Fe3O4 magnetic nanocomposite material (Fe3O4@pectin/Pd) for investigating the cardiovascular protective effects. The biomolecular functionalization not only stabilizes the ferrite nanoparticles from agglomeration but also provides an environment for the biogenic reduction of Pd2+ ions. This protocol is a promising breakthrough for the synthesis of a quasi-heterogeneous catalyst, a bridge between heterogeneous and homogeneous medium. The structure, morphology and physicochemical properties of the material were characterized utilizing various analytical techniques like FT-IR, FE-SEM, TEM, VSM, EDX-elemental mapping, ICP, EDX and XPS. The catalyst showed excellent reactivity in C-C and C-N cross coupling reactions via Suzuki and Buchwald-Hartwig reactions respectively. An array of different biphenyls and aryl amines were then procured by reactions of various aryl halides with phenylboronic acid or secondary amines over the catalyst affording good to excellent yields. The catalyst was easily recoverable using an external magnet and thereafter recycled for several trials with insignificant palladium leaching or loss in catalytic performance. To investigate the cardiovascular protective activities of catalyst, the MTT assay was done on Human Aortic Endothelial Cells (HAEC), Human Coronary Artery Endothelial Cells (HCAEC), and Human Pulmonary Artery Endothelial Cells (HPAEC) cell lines. Nanocatalyst-treated cell cutlers significantly (p ≤ 0.01) decreased the caspase-3 activity, and DNA fragmentation. It raised the cell viability and mitochondrial membrane potential in the high concentration of Mitoxantrone-treated HAEC, HCAEC, and HPAEC cells. According to the above findings, nanocatalyst can be administrated as a cardiovascular protective drug for the treatment of cardiovascular diseases after approving in the clinical trial studies in humans.
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Cardiotônicos/síntese química , Compostos Férricos/química , Nanopartículas Metálicas/química , Paládio/química , Pectinas/química , Apoptose , Cardiotônicos/farmacologia , Catálise , Células Cultivadas , Células Endoteliais/efeitos dos fármacos , Células Endoteliais/metabolismo , Endotélio Vascular/citologia , HumanosRESUMO
In recent decade, the entrance of α-N-heterocyclic thiosemicarbazones derivates (Triapne, COTI-2 and DpC) in clinical trials for cancer and HIV-1 has vastly increased the interests of medicinal chemists towards this class of organic compounds. In the given study, a series of eighteen new (3a-r) 3-ethoxy salicylaldehyde-based thiosemicarbazones (TSC), bearing aryl and cycloalkyl substituents, were synthesized and assayed for their pharmacological potential against carbonic anhydrases (hCA I and hCA II), cholinesterases (AChE and BChE) and α-glycosidase. The hCA I isoform was inhibited by these novel 3-ethoxysalicylaldehyde thiosemicarbazone derivatives (3a-r) in low nanomolar levels, the Ki of which differed between 144.18 ± 26.74 and 454.92 ± 48.32 nM. Against the physiologically dominant isoform hCA II, the novel compounds demonstrated Kis varying from 110.54 ± 14.05 to 444.12 ± 36.08 nM. Also, these novel derivatives (3a-r) effectively inhibited AChE, with Ki values in the range of 385.38 ± 45.03 to 983.04 ± 104.64 nM. For BChE was obtained with Ki values in the range of 400.21 ± 35.68 to 1003.02 ± 154.27 nM. For α-glycosidase the most effective Ki values of 3l, 3n, and 3q were with Ki values of 12.85 ± 1.05, 16.03 ± 2.84, and 19.16 ± 2.66 nM, respectively. Moreover, the synthesized TCSs were simulated using force field methods whereas the binding energies of the selected compounds were estimated using MM-GBSA method. The findings indicate the present novel 3-ethoxy salicylaldehyde-based thiosemicarbazones to be excellent hits for pharmaceutical applications.
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Aldeídos/química , Inibidores da Anidrase Carbônica/química , Inibidores da Colinesterase/química , Inibidores de Glicosídeo Hidrolases/química , Tiossemicarbazonas/química , Acetilcolinesterase/metabolismo , Aldeídos/síntese química , Aldeídos/farmacologia , Butirilcolinesterase/metabolismo , Anidrase Carbônica I/antagonistas & inibidores , Anidrase Carbônica I/metabolismo , Anidrase Carbônica II/antagonistas & inibidores , Anidrase Carbônica II/metabolismo , Inibidores da Anidrase Carbônica/síntese química , Inibidores da Anidrase Carbônica/farmacologia , Inibidores da Colinesterase/síntese química , Inibidores da Colinesterase/farmacologia , Inibidores de Glicosídeo Hidrolases/síntese química , Inibidores de Glicosídeo Hidrolases/farmacologia , Humanos , Simulação de Acoplamento Molecular , Termodinâmica , Tiossemicarbazonas/síntese química , Tiossemicarbazonas/farmacologia , alfa-Glucosidases/metabolismoRESUMO
A nanomicelle based drug delivery systems is a formulation that can improve the bioavailability and dissolution rate of water-insoluble drugs. In this study, the Dextran-Poly Lactic-co-Glycolic Acid copolymer was synthesized with esterification reaction, confirmed using the fourier-transform infrared spectroscopy and nuclear magnetic resonance. The used method for nanomicelle preparation was nanoprecipitation and the critical micelle concentration value was obtained 10 µg/mL. The particle size of the nanomicelle was less than 100 nm ± 4 nm with narrow size distribution (Polydispersity index = 0.06). Hydrocortisone was loaded to this system. The obtained results for the encapsulation efficiency were 79%, and the drug release was adjusted to a first-order kinetic model with 90% release of drug within the 12 h. The MTT assay showed that even in the high concentration of micelle, the cell viability was remained higher than 90%. Considering the toxicity investigation findings, the Dextran-Poly Lactic-co-Glycolic Acid micellar systems can be suggested as a considerable drug delivery system in hydrocortisone pharmaceutical dosage forms.
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In this work, a novel molecularly imprinted electrochemical sensor (MIES) has been fabricated based on electropolymerization of a molecularly imprinted polymer (MIP) onto a glassy carbon electrode (GCE) modified with gold-palladium alloy nanoparticles (AuPd NPs)/polydopamine film (PDA)/multiwalled carbon nanotubes-chitosan-ionic liquid (MWCNTs-CS-IL) for voltammetric and impedimetric determination of cholestanol (CHO). Modifications applied to the bare GCE formed an excellent biocompatible composite film which was able to selectively detect CHO molecules. Modifications applied to the bare GCE were characterized by scanning electron microscopy (SEM), cyclic voltammetry (CV) and electrochemical impedance spectroscopy (SEM). Under optimal experimental conditions, the sensor was able to detect CHO in the range of 0.1-60 pM and 1-50 pM by EIS and DPV, respectively. Moreover, the sensor showed high sensitivity, selectivity, repeatability, reproducibility, low interference and good stability towards CHO determination. Our records confirmed that the sensor was successfully able to the analysis real samples for determination of CHO.
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Colestanol/análise , Técnicas Eletroquímicas/instrumentação , Técnicas Eletroquímicas/métodos , Impressão Molecular , Técnicas Biossensoriais , Limite de DetecçãoRESUMO
Candidiasis is the origin of several chronic diseases and causes a wide range of symptoms from mucosal to systemic and deadly infections. Vaginal patches are one of the best drug delivery systems for the treatment of fungal infections in the vaginal environment, so a mucoadhesive film containing drugs such as clotrimazole and metronidazole is commercially available for patients. In the present study, a physicochemical comparison is made between clotrimazole loaded film and nanofiber fabricated with the new hybrid mucoadhesive formulation of dextran and alginate. Toxicity testing was performed using the MTT assay. Bioadhesion and antifungal effects were investigated for fibers and films. The release behavior of clotrimazole from two systems was evaluated by Franz cell in each case. The most important difference between nanofibrous and film mats were obtained in antifungal, mucoadhesive, Young's modulus and morphology. The nanofiber has a higher antifungal effect and two-fold adhesive to the mouse tissue, than film. The inherent flexibility of nanofiber obviated the need for a plasticizer, which may have cytotoxic side effects. The Clotrimazole loaded nanofibrous of Alginate/Dextran mats were successfully electrospun. They exhibited more bioadhesive with higher and faster antifungal properties versus similar formulation film. Further in vivo investigation is required for their application in vaginal candidiasis.
Assuntos
Antibacterianos , Antifúngicos , Candidíase Vulvovaginal/tratamento farmacológico , Clotrimazol , Nanofibras , Administração Intravaginal , Antibacterianos/química , Antibacterianos/farmacologia , Antifúngicos/química , Antifúngicos/farmacologia , Linhagem Celular , Clotrimazol/química , Clotrimazol/farmacologia , Feminino , Humanos , Nanofibras/química , Nanofibras/uso terapêuticoRESUMO
In this work, a novel and very interesting analytical methodology based on coupling of digital image processing and three-way calibration has been developed for determination of nitrite in food samples. Nitrite in contact with Griess reagent is able to produce a red-colored azo dye whose color intensity is correlated with nitrite concentration and here, a piece of Whatman filter paper impregnated with Griess reagent was used as the platform of the sensor and a SONY Xperia Z5 cell phone was used for image capturing from the sensor surface. To generate second-order data, the F-number of the camera's sensor was changed as an instrumental parameter. Two calibration models were constructed by unfolded partial least squares-residual bilinearization (U-PLS/RBL) and multiway-PLS/RBL (N-PLS/RBL) and then, their performance for prediction of nitrite concentration in test samples was evaluated and the results confirmed a good performance for U-PLS/RBL (REP = 3.25 ppm, RMSEP = 8.82 ppm, RMSEC = 4.62 ppm, Q 2 = 0.99, γ -1 = 0.05 and LOD = 0.1 ppm) which was better than that for N-PLS/RBL (REP = 13.98 ppm, RMSEP = 37.86 ppm, RMSEC = 6.46 ppm, Q 2 = 0.98, γ -1 = 0.07 and LOD = 0.15 ppm) in predicting concentration of nitrite in test samples which motivated us to choose it for the analysis of cabbage, carrot, lettuce, watermelon, onion, potato, kielbasa and sausage as real samples.
RESUMO
OBJECTIVE: To assess the wound healing potential of Pimpinella anisum on cutaneous wounds in diabetic rats. METHOD: Full-thickness excisional wounds were made on the back of male, Sprague-Dawley rats with diabetes. The rats were randomly allocated into four treatment groups: 1ml basal cream; tetracycline (3%); Pimpinella anisum 10% for 14 days; and a control group. At days seven, 14 and 21 post-injury, five animals of each group were euthanised, and wounds were assessed through gross, histopathological and oxidant/antioxidant evaluations. Additionally, the dry matter and hydroxyproline contents of the skin samples were measured. RESULTS: A total of 60 rats were used in the study. A significant decrease in the wound size was observed in treated animals with Pimpinella anisum compared with other groups during the experiment. Additionally, treatment with Pimpinella anisum decreased the number of lymphocytes and improved the number of fibroblasts at the earlier stages and increased a number of fibrocytes at the later stages of wound healing. Other parameters such as re-epithelialisation, tissue alignment, greater maturity of collagen fibres and large capillary-sized blood vessels revealed significant changes when compared with the control. Pimpinella anisum significantly reverted oxidative changes of total antioxidant capacity, malondialdehyde and glutathione peroxidase induced by diabetic wounds (p<0.05). Furthermore, it significantly increased the dry matter and hydroxyproline contents at various stages of wound healing (p<0.05). CONCLUSION: The present study showed that application of Pimpinella anisum extract promotes wound healing activity in diabetic rats. The wound-healing property of Pimpinella anisum can be attributed to the phytoconstituents present in the plant.
Assuntos
Diabetes Mellitus Experimental/induzido quimicamente , Diabetes Mellitus Experimental/tratamento farmacológico , Fitoterapia/métodos , Pimpinella/química , Extratos Vegetais/uso terapêutico , Estreptozocina/efeitos adversos , Cicatrização/efeitos dos fármacos , Animais , Humanos , Masculino , Modelos Animais , Ratos , Ratos Sprague-DawleyRESUMO
Facile green synthesis of copper nanoparticles from different biological procedures has been indicated, but among all, biosynthesis of copper nanoparticles from medicinal plants is considered as the most suitable method. The use of medicinal plant material increases the therapeutical effects of copper nanoparticles. The aim of this study was green synthesis of copper nanoparticles from aqueous extract of Falcaria vulgaris leaf (CuNPs) and assessment of their cytotoxicity, antioxidant, antifungal, antibacterial, and cutaneous wound healing properties. These nanoparticles were characterized by X-ray diffraction (XRD), fourier-transform infrared spectroscopy (FT-IR), ultraviolet-visible spectroscopy (UV), transmission electron microscopy (TEM), and field emission scanning electron microscopy (FE-SEM) analysis. The synthesized CuNPs had great cell viability dose-dependently (Investigating the effect of the CuNPs on human umbilical vein endothelial cell (HUVEC) line) and indicated this method was nontoxic. Also, 2,2-diphenyl-1-picrylhydrazyl (DPPH) test was done to assess the antioxidant activities, which indicated similar antioxidant potentials for CuNPs and butylated hydroxytoluene. In part of cutaneous wound healing property of CuNPs, after creating the cutaneous wound, the rats were randomly divided into six groups: treatment with 0.2% CuNPs ointment, treatment with 0.2% CuSO4 ointment, treatment with 0.2% F.â¯vulgaris ointment, treatment with 3% tetracycline ointment, treatment with Eucerin basal ointment, and untreated control. These groups were treated for 10â¯days. Treatment with CuNPs ointment remarkably increased (pâ¯≤â¯.01) the wound contracture, vessel, hexosamine, hydroxyl proline, hexuronic acid, fibrocyte, and fibrocytes/fibroblast rate and substantially reduced (pâ¯≤â¯.01) the wound area, total cells, neutrophil, and lymphocyte compared to other groups. In antibacterial and antifungal parts of this research, the concentration of CuNPs with minimum dilution and no turbidity was considered minimum inhibitory concentration (MIC). To determine minimum fungicidal concentration (MFC) and minimum bactericidal concentration (MBC), 60⯵L MIC and three preceding chambers were cultured on Sabouraud Dextrose Agar and Muller Hinton Agar, respectively. The minimum concentration with no fungal and bacterial growth were considered MFC and MBC, respectively. CuNPs inhibited the growth of all fungi at 2-4â¯mg/mL concentrations and removed them at 4-8â¯mg/mL concentrations (pâ¯≤â¯.01). In case of antibacterial effects of CuNPs, they inhibited the growth of all bacteria at 2-8â¯mg/mL concentrations and removed them at 4-16â¯mg/mL concentrations (pâ¯≤â¯.01). The results of XRD, FT-IR, UV, TEM, and FE-SEM confirm that the aqueous extract of F.â¯vulgaris leaf can be used to yield copper nanoparticles with notable amount of antioxidant, antifungal, antibacterial, and cutaneous wound healing potentials without any cytotoxicity. Further clinical trials are necessary for confirmation these therapeutical effects of CuNPs in human.