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This study investigated the biological activity of the silver coordination compound K-22. The IC50 values of K-22 on cancer cell lines range from 0.797 µg/mL to 3.426â µg/mL, indicating that K-22 might preferably inhibit A549, Saos-2, MCF-7, and HT-29 cell proliferation and thus have better therapeutic activity. Furthermore, K-22 stimulated apoptosis via up-regulation of the mRNA and protein expression level of Bax/Bcl-2 ratio in A549, Saos-2, MCF-7, and HT-29. K-22 exhibited antimicrobial activity against S.â aureus, E.â faecalis, K.â pneumonia, P.â aeruginosa, C.â utilis, and C.â albicans. Experimental results show that the compound has inhibitory potential with an IC50 value of 178.10â µM for the BChE (butyrylcholinesterase) enzyme, which has a vital role in the progression of Alzheimer's disease. As a result, compound K-22 exhibits a strong potential for medical use due to its anticancer, antibacterial, antifungal, and anti-Alzheimer properties.
Assuntos
Antifúngicos , Butirilcolinesterase , Antifúngicos/farmacologia , Butirilcolinesterase/metabolismo , Prata/farmacologia , Staphylococcus aureus/metabolismo , Antibacterianos/farmacologiaRESUMO
In this study, biological activities of silver nanoparticles (AgNP) synthesized by green synthesis method using the fruit extract of Gilaburu (Viburnum opulus L.) plant were investigated. The characterization of the synthesized AgNPs was performed by ultraviolet visible region spectroscopy (UV-Vis), Fourier transform - infrared spectroscopy (FTIR), scanning electron microscopy (SEM), and X-ray diffraction (XRD) techniques. The crystal size was found to be 52.32 nm when the XRD data were calculated with the Debye-Scherrer's equation. The antimicrobial activities of extract and AgNPs were investigated by microdilution and disk diffusion methods. Antibiofilm activities were examined by the crystal violet technique. The cytotoxic effects of the extract and AgNPs against MCF-7(human breast cancer) and HUVEC (human umbilical vein endothelial cells) cell lines were evaluated by MTT assay. The IC50 valuesfor the HUVEC line were found to be 0.97 mg/mL (AgNP) and 85.24 mg/mL (extract), while the IC50 values for the MCF-7 line were determined as 0.022 µg/mL (AgNP) and 0.021 µg/mL (extract). To our knowledge, this is the first report to comprehensively examine the biological activities of V. opulus L. extract and biosynthetic AgNPs.
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Four new dicyanoargentate(I)-based complexes 1-4 were synthesized from certain metal ions with a tetradentate ligand [N, N-bis (2-hydroxyethyl) -ethylenediamine; N-bishydeten] and determined by diverse procedures (elemental, thermal, FT-IR, ESI-MS for 1-3 and, magnetic susceptibility and EPR for 1, and 2) including crystal analysis of 4. The crystal method revealed that complex 4 has a sandwich-type like polymeric chemical structure with layers formed by [Cd(N-bishydeten)2]2+ cations and [Ag(CN)2]- anions. The complexes were further characterized by fluorescence and UV spectroscopy to determine their physicochemical features. The complexes displayed a DNA binding activity within the same range as found for cisplatin, in addition to their strong stability in the presence of the physiological buffer system. The complexes were also investigated for pharmacological properties like interaction with DNA/Bovine serum albumin, anticancer and antibacterial activities. Physicochemical studies of DNA with the complexes suggested that the interaction mode between them are possibly both intercalative and groove binding types. These spectroscopic measurements also show that there may be a binding tendency between BSA and the complexes via hydrogen or Van der Waals bonds. The viability tests demonstrated that all the complexes exhibited antibacterial (1-4) and anticancer effects (2-4) toward ten diverse bacterial strains and three tumor cells (HT-29 colon adenocarcinoma, HeLa cervical cancer, and C6 glioma), respectively.
Assuntos
Antibacterianos/química , Antibacterianos/farmacologia , Antineoplásicos/química , Antineoplásicos/farmacologia , Antibacterianos/síntese química , Antineoplásicos/síntese química , Linhagem Celular Tumoral , Células HT29 , Células HeLa , Humanos , Espectroscopia de Infravermelho com Transformada de FourierRESUMO
The interaction of the coordination compounds with biological molecules resulted in the investigation of the drug potential of these molecules. In this study, enzyme inhibition of DSA (1-3) coordination compounds that were previously investigated for their anticancer and antibacterial properties was investigated. Also, DSA (1-3) had Ki values of 635.30 + 152.62, 184.01 + 90.05, and 163.03 ± 60.01 µM against human carbonic anhydrase I, 352.23 ± 143.09, 46.2 ± 15.47, and 54.117 ± 18.80 µM against AChE, 310.64 ± 97.35, 35.54 ± 7.01, and 101.51 ± 15.314 µM against BChE, respectively. The biological activity values of these compounds against enzymes whose name are AChE, BChE, and hCAI were compared. Ellman and Verporte methods were used for the study of these enzymes. Cholinesterase inhibitors, also known as anti-cholinesterase and cholinesterase blocking drugs, are chemicals that prevent the breakdown of the neurotransmitter acetylcholine or butyrylcholine. They may be used as drugs for Alzheimer's and myasthenia gravis. It is a common method for comparing biological activity values of nickel complexes with molecular docking calculations. Nickel complexes were studied against enzymes that are human carbonic anhydrase isozyme I for ID 2CAB (hCA I), butyrylcholinesterase for ID 1P0I (BChE), and acetylcholinesterase for ID 1EEA (AChE), respectively.
Assuntos
Doença de Alzheimer/tratamento farmacológico , Epilepsia/tratamento farmacológico , Glaucoma/tratamento farmacológico , Simulação de Acoplamento Molecular/métodos , Níquel/uso terapêutico , Humanos , Estrutura Molecular , Níquel/farmacologia , Relação Estrutura-AtividadeRESUMO
Today, nanoparticles are effectively used in different areas. Initially, physical and chemical methods were used in the synthesis of nanoparticles. Biosynthesis (green synthesis) has emerged as an alternative to overcome the toxic effects of chemically synthesized nanoparticles. In this study, green synthesis of silver nanoparticles (AgNPs) with the leaf extract of Anthurium andraeanum was performed. UV-Vis spectrophotometry, scanning transmission electron microscopy, and XRD were applied to characterize the biosynthesized nanoparticles. As a result of the characterization, the spectra showed that a spectrum at a wavelength of about 419 nm and a spherical size of 38 nm nanoparticles was formed. Antibacterial and biofilm inhibition activities of AgNPs against gram-positive and gram-negative bacteria were determined. AgNPs at a concentration of 1 mg/mL showed antibacterial activity against all of the bacterial strains. In the antibiofilm activity study, the highest inhibition percentage was obtained against the P. fluorescens strain at 87.1%, at a concentration of 0.5 mg/mL.
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Coordination compounds containing dicyanoargentate(I) have remarkable biological potential due to their therapeutic antibacterial, antifungal, antibiofilm, and anticancer properties. In this study, a new dicyanoargentate(I)-based complex was synthesized and characterized by various procedures (elemental, thermal, FT-IR for complex) involving crystal analysis of the complex. In addition, the biological activity of this new compound on the acetylcholinesterase (AChE) enzyme, an important enzyme for the nervous system, was investigated. When the infrared (IR) spectrum of the complex is examined, the OH vibration peak resulting from H2O molecules in the structure at 3948-3337 cm-1 and at 2138 cm-1, along with a CN peak coordinated to Ag, can be seen, indicating that the mass remaining in the thermal degradation of the complex at 1000 ⦠C is the weight corresponding to the metal mixture consisting of K+Ag (calc.: 68.06). The crystal method revealed that the complex has a sandwich-like, polymeric chemical structure with layers formed by K+ cations and [Ag(CN)2H2O]- anions. Therefore, the AChE enzyme has potential therapeutic uses in improving ACh levels in brain cells, in reducing various side effects, and in improving cognitive impairment, especially in advanced Alzheimer's disease patients. In this study, the activity of this newly synthesized complex on AChE was also investigated. As a result of this research, [Ag(CN)2(H2O)K] had 0.0282 ± 0.010 µM Ki values against AChE. The compound was therefore a good inhibitor for the AChE enzyme. This type of compound can be used for the development of novel anticholinesterase drugs.
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Four compounds -two (2 and 3) completely new- of composition [Ni(edbea)Ag3(CN)5] (1), [Cu(edbea)Ag2(CN)4]·H2O (2), [Cd(edbea)Ag3(CN)5]·H2O (3) and [Cd(edbea)2] [Ag(CN)2]2·H2O (4) {edbea; 2,2'-(ethylenedioxy)bis (ethylamine)}, were synthesized and characterized using elemental, FT-IR, X-Ray (4), thermal, variable temperature magnetic measurement (1 and 2) and biological techniques. The DNA/BSA binding affinities of 2 and 3 were evaluated by UV-Vis spectrophotometric titrations, ethidium bromide exchange experiments and electrophoretic mobility measurements. Compounds 1 and 4 have previously been characterized and shown to reduce the proliferation and migration of tumor cells. For the sake of clarity, 1 precise mechanism of action on microbial organisms and temperature magnetic measurement were determined. The crystallographic analyses showed that 4 was built up of [Cd(edbea)2]II cations and [Ag2(CN)4]II anions. Complexes demonstrated a remarkable antibacterial (1-4), antifungal (1-4) and antiproliferative activities (2 and 3) to ten human bacterial pathogens, four plant pathogenic fungi or three tumor cells (HeLa, HT29, and C6), respectively. Therefore, our results strongly confirm that cell proliferation, cell morphology, Bcl-2, P53 changes and apoptosis can be related to the pharmacological effects of the complexes as suitable candidate for clinical trials.
Assuntos
Antineoplásicos , Apoptose/efeitos dos fármacos , Cádmio , Proliferação de Células/efeitos dos fármacos , Complexos de Coordenação , DNA/química , Soroalbumina Bovina/química , Prata , Animais , Antibacterianos/química , Antibacterianos/farmacologia , Antifúngicos/química , Antifúngicos/farmacologia , Antineoplásicos/química , Antineoplásicos/farmacologia , Cádmio/química , Cádmio/farmacologia , Bovinos , Complexos de Coordenação/química , Complexos de Coordenação/farmacologia , Células HeLa , Humanos , Prata/química , Prata/farmacologiaRESUMO
A novel potentiometric sensor based on ionophore (Cd(NH2CH2CH2OCH2CH2OCH2CH2NH2)Ag3(CN)5) for the determination of ß-N-oxalyl-L-α, ß-diaminopropionic acid (ODAP) is developed. The ODAP-selective membrane sensor demonstrates high sensitivity and short response time. The detection limit of the ODAP-selective membrane sensor is about 2 × 10(-6) mol L (-1) and the response time is shorter than 6 s. The linear dynamic range of the ODAP-selective membrane sensor is between ODAP concentrations of 1.0 × 10(-2) and 1 × 10(-6) mol L (-1). The ODAP-selective membrane sensor exhibits good operational stability for at least one week in dry conditions at 4-6°C. It has a reproducible and stable response during continuous work for at least 10 h with a relative standard deviation of 0.28% (n = 18).