Synthesis and Biological Evaluation of Amoxicillin Loaded Hybrid Material Composite Spheres Against Methicillin-Resistant Staphylococcus aureus

2020 ◽  
Vol 21 ◽  
Author(s):  
Muhammad Arfat Yameen ◽  
Amir Zeb ◽  
Raza E Mustafa ◽  
Sana Mushtaq ◽  
Nargis Aman ◽  
...  
Keyword(s):  
Mtt Assay ◽  
Hybrid Material ◽  
Ag Nanoparticles ◽  
Hybrid Composite ◽  
Synthesis Method ◽  
Biological Evaluation ◽  
Vitro Assay ◽  
Cytotoxicity Studies ◽  
Material Composite

Background: Incoherent use of antibiotics has led toward resistance in MRSA, which is becoming multidrugresistant with high rate of virulence in the community and hospital settings. Objective: Synergistic anti-MRSA activity was investigated in this study for hybrid material composite spheres of amoxicillin, Ag nanoparticles and chitosan which were prepared by one-step synthesis method and various characterizations were performed. Methods: Antimicrobial-susceptibility assay on MRSA was achieved by disc diffusion and agar dilution techniques while agar well diffusion was used for hybrid composite spheres. The in vitro and cytotoxicity studies was done by skin abrasion mouse model and MTT assay on RD cell respectively. Results: All isolates were resistant with the tested antibiotics except vancomycin. MIC against MRSA showed high resistance with amoxicillin from 4 to 128 mg L-1. The mean diameter of chitosan spheres and Ag nanoparticles was 02 mm and 277 nm respectively. Morphology of spheres was uneven, varied, porous and irregular in SEM and Ag nanoparticles presence and formation was also seen in micrograph. No substantial interface among drug, nanoparticles and polymer was found in XRD and IR showed characteristic peaks of all compound in the formulation. The in vitro assay showed augmented anti-MRSA activity with amoxicillin loaded hybrid composite spheres (22-29 mm). A significant reduction in microbial burden (~6.5 log10 CFU ml-1) was seen in vivo with loaded hybrid composite spheres formulation. The MTT assay indicated no potential cytotoxicity with hybrid composite spheres. Conclusion: Synergistic effect, amoxicillin, new hybrid formulation, anti-MRSA activity, composite spheres. nanoparticles.

scholarly journals Green synthesis of silver, iron and gold nanoparticles of lycopene extracted from tomato: their characterization and cytotoxicity against COLO320DM, HT29 and Hella cell

2021 ◽  
Vol 32 (2) ◽  
Author(s):  
Kiran P. Shejawal ◽  
Dheeraj S. Randive ◽  
Somnath D. Bhinge ◽  
Mangesh A. Bhutkar ◽  
Sachin S. Todkar ◽  
...  
Keyword(s):  
Cervical Cancer ◽  
Gold Nanoparticles ◽  
Green Synthesis ◽  
Color Change ◽  
Synthesis Method ◽  
Vitro Assay ◽  
Prepared Nanoparticles ◽  
Cytotoxicity Studies ◽  
Ht 29

AbstractOur study aimed at development of Silver, Iron and Gold nanoparticles of Lycopene isolated from tomato by using green synthesis technique and to evaluate its anticancer potential against colorectal and cervical cancer. Lycopene was extracted by benzene extraction method and the silver, iron and gold nanoparticles were developed by green synthesis method. 1% aqueous extract of isolated Lycopene was mixed with 1% solutions of AgNO3, FeCl3 and HAuCl4 solutions and incubated at ambient temperature for 3–4 h separately and observed for the color change which is an indicative of formation of the nanoparticles. The prepared nanoparticles were characterized by FTIR, SEM, XRD analysis and evaluated for their antimicrobial potential. The cytotoxicity studies were carried out by in vitro assay like MTT, SRB and Tryphan blue method against Colo 320 DM, HT 29, and Hella. SEM showed nanosized particles of 50–100 nm range, whereas no antimicrobial activity was exhibited by the prepared nanoparticles. In MTT assay the LyAgNP showed maximum 41.41 ± 0.4124% inhibition against COLO320DM, whereas LyGNP exhibited 41.47 ± 0.4469% inhibition against HT 29 and LyAgNP showed 40.9 ± 0.6908% inhibition against Hella cells. In SRB assay LyAgNP showed maximum 82.68 ± 1.1798% inhibition against COLO320DM, whereas LyGNP exhibited maximum 91.21 ± 0.2372% inhibition against HT29 and 87.98 ± 0.5878% inhibition against Hella cells. In tryphan blue assay against COLO320DM, HT29 and Hella cells, the maximum inhibition exhibited by the prepared nanoparticles were observed as LyGNP 83.45 ± 0.4694%, LyAgNP 88.05 ± 0.1870% and LyAgNP65.47 ± 0.4766%. We conclude that the developed nanoparticles of Lycopene exhibited potential anticancer activity against Colorectal and cervical cancer cell as compared with pure Lycopene.

Synthesis and studies of thiazolidinedione–isatin hybrids as α-glucosidase inhibitors for management of diabetes

2021 ◽  
Vol 13 (5) ◽  
pp. 457-485
Author(s):  
Ramandeep Kaur ◽  
Rajnish Kumar ◽  
Nilambra Dogra ◽  
Ashok Kumar ◽  
Ashok Kumar Yadav ◽  
...  
Keyword(s):  
In Silico ◽  
Binding Free Energy ◽  
Biological Evaluation ◽  
Free Energy Calculations ◽  
Standard Drug ◽  
Glucosidase Inhibitors ◽  
Cytotoxicity Studies ◽  
Cytotoxicity Assessment

Aim: Keeping in view the side effects associated with clinically used α-glucosidase inhibitors, novel thiazolidinedione–isatin hybrids were synthesized and evaluated by in vitro, in vivo and in silico procedures. Materials & methods: Biological evaluation, cytotoxicity assessment, molecular docking, binding free energy calculations and molecular dynamics studies were performed for hybrids. Results: The most potent inhibitor A-10 (IC50 = 24.73 ± 0.93 μM) was competitive in manner and observed as non-cytotoxic. A-10 possessed higher efficacy than the standard drug (acarbose) during in vivo biological testing. Conclusion: The enzyme inhibitory potential and safety profile of synthetic molecules was recognized after in vitro, in vivo, in silico and cytotoxicity studies. Further structural optimization of A-10 can offer potential hit molecules suitable for future investigations.

scholarly journals Synthesis, Stability, and Antidiabetic Activity Evaluation of (−)-Epigallocatechin Gallate (EGCG) Palmitate Derived from Natural Tea Polyphenols

Molecules ◽  
2021 ◽  
Vol 26 (2) ◽  
pp. 393
Author(s):  
Bingbing Liu ◽  
Zhengzhong Kang ◽  
Weidong Yan
Keyword(s):  
Synthesis Method ◽  
Epigallocatechin Gallate ◽  
Antidiabetic Activity ◽  
Molar Ratio ◽  
Synthetic Approach ◽  
Vitro Assay ◽  
Docking Simulations ◽  
Palmitoyl Chloride ◽  
Novel Approach

This work describes a novel approach for the synthesis of (−)-epigallocatechin gallate (EGCG) palmitate by a chemical-synthesis method, where the elevated stability of the EGCG derivative is achieved. Various parameters affecting the acylation process, such as the base, solvent, as well as the molar ratio of palmitoyl chloride, have been studied to optimize the acylation procedure. The optimized reaction condition was set as follows: EGCG/palmitoyl chloride/sodium acetate was under a molar ratio of 1:2:2, with acetone as the solvent, and the reaction temperature was 40 °C. Under the optimized condition, the yield reached 90.6%. The EGCG palmitate (PEGCG) was isolated and identified as 4′-O-palmitoyl EGCG. Moreover, the stability of PEGCG under different conditions was proved significantly superior to EGCG. Finally, PEGCG showed better inhibition towards α-amylase and α-glucosidase, which was 4.5 and 52 times of EGCG, respectively. Molecular docking simulations confirmed the in vitro assay results. This study set a novel and practical synthetic approach for the derivatization of EGCG, and suggest that PEGCG may act as an antidiabetic agent.

scholarly journals Synthesis, Antiproliferative Activity and Molecular Docking Studies of 1,3,5-Triaryl Pyrazole Compound as Estrogen α Receptor Inhibitor Targeting MCF-7 Cells Line

Molekul ◽  
2020 ◽  
Vol 15 (1) ◽  
pp. 18
Author(s):  
Noval Herfindo ◽  
Riska Prasetiawati ◽  
Daniel Sialagan ◽  
Neni Frimayanti ◽  
Adel Zamri
Keyword(s):  
Molecular Docking ◽  
Antiproliferative Activity ◽  
Docking Simulation ◽  
Docking Studies ◽  
Biological Evaluation ◽  
One Pot ◽  
Vitro Assay ◽  
Oxidative Aromatization ◽  
Mcf 7

This research has been successfully synthesized three compounds of 1,3,5-triaryl pyrazole derivatives by two steps reaction. Firstly, pyrazoline (4a-c) compound was obtained by one-pot reaction of aromatic ketones, aldehyde and hydrazine in basic condition. Then, pyrazole (5a-c) compound was obtained by oxidative aromatization of compound 4 in the presense of acetic acid. Chemical structure of predicted molecules was confirmed by FTIR, NMR and HRMS spectroscopy data analysis. Antiproliferative activity of compound 5a-c were evaluated by in vitro assay against MCF-7 cells line and molecular docking simulation against ERα (PDB ID: 3ERT) using MOE 2019. Biological evaluation result showed that pyrazole compounds had weak antiproliferative activity against MCF-7 cells with IC50 were > 1000 µM, whereas the docking studies agrees the result.

In vitro validation of camphene as a potential antiviral agent against betanodavirus causing viral nervous necrosis in barramundi

2021 ◽  
Vol 19 ◽  
Author(s):  
Ruby Singh ◽  
Prachi Srivastava ◽  
Deepika Anand ◽  
Pani K. Prasad
Keyword(s):  
Mtt Assay ◽  
Viral Infections ◽  
Rna Virus ◽  
Antiviral Agent ◽  
Sea Bass ◽  
Viral Nervous Necrosis ◽  
Cytotoxicity Studies ◽  
In Silico Studies ◽  
Juvenile Stages

Introduction:: Viral infections are major threat to aquaculture industry throughout the world. Betanodavirus is one of the most infectious virus that causes highest mortality in larval and juvenile stages of Lates calcarifer commonly known as Barramundi. Methods:: Methods: It is a single stranded positive sense RNA virus and causes viral nervous necrosis (VNN). VNN is caused by RNA virus which gets transmitted both horizontally and vertically so the most effective method against this virus is to vaccinate the fish, however vaccination becomes difficult since the disease is associated with the outbreaks in larval and juvenile stages which are not that much immunocompetent. In our previous in silico studies we proved the stability of camphene as a better phytochemical agent. Results:: In continuation to prove the authenticity of Camphene as potential antiviral agent against betanodavirus, its in vitro validation was performed. Sea bass kidney cell line (SISK) was selected for carrying out the in vitro studies and cytotoxicity studies of Camphene in the SISK was was done by MTT assay. Based on the analysis of MTT assay different dosage of camphene were selected viz.,(0.2, 0.5, 1, 1.5, 2, 2.5, 5, 10, 20, 30 μg/ml). The SISK cells were infected with virus inoculum (200μl). Further the antiviral activity of Camphene on infected SISK cells by Betanodavirus was elucidated with the help of quantitative Real time PCR(qPCR) on the 3rd and 5th day of infection. Conclusion:: Analysis of results depictecd that the dose of camphene 2 to 10 μg/ml is the safest dose against Betanodavirus. Hence this is aptly revealed that camphene can be used as potential antiviral agent against Betanodavirus.

Design, Synthesis of novel coumarin conjugated acetamides as promising anticancer agents: An in-silico and in-vitro approach.

2020 ◽  
Vol 20 ◽  
Author(s):  
Mamatha S. V ◽  
S. L. Belagali ◽  
Mahesh Bhat ◽  
Vijay M. Kumbar
Keyword(s):  
Anticancer Activity ◽  
Cell Lines ◽  
Mtt Assay ◽  
Anticancer Agents ◽  
In Silico ◽  
Active Sites ◽  
Biological Activities ◽  
Biological Evaluation ◽  
Mcf 7

Background: Coumarin and benzophenone possess a vast sphere of biological activities whereas thiazoles display various pharmacological properties. Hence we focused on incorporation of coumarin and thiazole core to the benzophenone skeleton to enhance the bioactivity anticipating their interesting biological properties. Objective: The objective of the current work is synthesis and biological evaluation of a novel series of coumarin fused thiazole derivatives. Methods: A novel series of Coumarin conjugated thiazolyl acetamide hybrid derivatives were synthesized by multistep reaction sequence and were characterized by the FT-IR, LCMS and NMR spectral techniques. The newly synthesized compounds were screened for anticancer activity by in-silico and in-vitro methods. The cytotoxicity of the synthesized unique compounds had been executed for two different cancer cell lines MCF-7 (Breast cancer) and KB (Oral cancer) in comparison with standard paclitaxel by MTT assay. Results: The compound 7f is the potent motif with an acceptable range of IC 50 values for anticancer activity were 63.54 µg/ml and 55.67 µg/ml, against the MCF-7 and KB cell lines, respectively. Molecule docking model revealed that this compound formed three conventional hydrogen bonds with the active sites of the amino acids MET 769, ARG 817 and LYS 721. Conclusion: Compound 7f with two methyl groups on the phenoxy ring and one 4-position methoxy group on the benzoyl ring, showed a significant cytotoxic effect. An advantageous level of low toxicity against normal cell line (L292) by MTT assay was determined.

scholarly journals Monocytes-based in vitro assay for a preliminary biocompatibility assessment of blood-contacting devices

2019 ◽  
Vol 17 ◽  
pp. 205873921882047
Author(s):  
Claudia Gemelli ◽  
Alexis Grande ◽  
Sergio Ferrari ◽  
Aldo Tomasi ◽  
Aurora Cuoghi
Keyword(s):  
Experimental Approach ◽  
Biological Evaluation ◽  
In Vitro Assay ◽  
Enzyme Linked Immunosorbent Assay ◽  
Cellular Model ◽  
Cell Toxicity ◽  
Vitro Assay ◽  
Device Interaction ◽  
Extractable Compounds

The biological evaluation of biomaterials is currently defined by the ISO-10993 norm in which parts four and five are dedicated to emo-compatibility and cell toxicity, respectively. Our study will provide a novel in vitro experimental approach for the biocompatibility assessment of biomaterials or medical devices using human primary monocytes as cellular model. In these new settings, human monocytes are exposed to a medium containing the extractable compounds derived from materials or devices; subsequently, cell toxicity and pro-inflammatory effects are analysed through MTT assay, flow cytometry and enzyme-linked immunosorbent assay (ELISA) methodologies. These experimental procedures offer the advantage to use a human and primary cell context belonging to the immune system, in order to accurately predict the nature of blood/device interaction occurring during a clinical application. To validate the reliability of this method, we also reported a comparative study between two different membranes showing a different level of biocompatibility. On the bases of these data, it is possible to state that this new experimental model represents a good approach to investigate the effects induced by a biomaterial on cell death and inflammation using human, primary monocytes.

scholarly journals Synthesis, Cytotoxicity Assessment and Optical Properties Characterization of Colloidal GdPO4:Mn2+, Eu3+ for High Sensitivity Luminescent Nanothermometers Operating in the Physiological Temperature Range

Nanomaterials ◽  
2020 ◽  
Vol 10 (3) ◽  
pp. 421 ◽  
Author(s):  
Kamila Maciejewska ◽  
Blazej Poźniak ◽  
Marta Tikhomirov ◽  
Adrianna Kobylińska ◽  
Łukasz Marciniak
Keyword(s):  
Synthesis Method ◽  
High Sensitivity ◽  
Relative Sensitivity ◽  
Spectroscopic Properties ◽  
Physiological Temperature ◽  
Temperature Range ◽  
Cytotoxicity Studies ◽  
Cytotoxicity Assessment

Herein, a novel synthesis method of colloidal GdPO4:Mn2+,Eu3+ nanoparticles for luminescent nanothermometry is proposed. XRD, TEM, DLS, and zeta potential measurements confirmed the crystallographic purity and reproducible morphology of the obtained nanoparticles. The spectroscopic properties of GdPO4:Mn2+,Eu3+ with different amounts of Mn2+ and Eu3+ were analyzed in a physiological temperature range. It was found that GdPO4:1%Eu3+,10%Mn2+ nanoparticles revealed extraordinary performance for noncontact temperature sensing with relative sensitivity SR = 8.88%/°C at 32 °C. Furthermore, the biocompatibility and safety of GdPO4:15%Mn2+,1%Eu3+ was confirmed by cytotoxicity studies. These results indicated that colloidal GdPO4 doped with Mn2+ and Eu3+ is a very promising candidate as a luminescent nanothermometer for in vitro applications.

scholarly journals Synthesis and Biological Evaluation of Haloalkyl Phosphate Triester Derivatives of araA and araC

1992 ◽  
Vol 3 (2) ◽  
pp. 79-84 ◽  
Author(s):  
C. McGuigan ◽  
B. C. N. M. Jones ◽  
S. M. Tollerfield ◽  
P. A. Riley
Keyword(s):  
Epithelial Cells ◽  
Antiviral Drug ◽  
Biological Evaluation ◽  
In Vitro Assay ◽  
Vitro Assay ◽  
Free Nucleotides ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

Novel phosphate triester derivatives of the antiviral drug araA and the anti-leukaemic agent araC have been prepared as membrane-soluble pro-drugs of the bio-active free nucleotides. In particular, novel trichloro- and trifluoroethyl phosphates have been prepared using phosphorochloridate chemistry, and are fully characterized. An in vitro assay indicates inhibition, by each of the compounds, of thymidine incor-portion by mammalian epithelial cells. It is notable that the trichloroethyl derivative is most active in each case, and in the case of araC its activity appears to exceed that of the parent nucleoside.

An in vitro testing of chemoresistance in leukaemic patients

Biologia ◽  
2009 ◽  
Vol 64 (1) ◽  
Author(s):  
Jozef Hatok ◽  
Tatiana Matáková ◽  
Juraj Chudej ◽  
Ján Staško ◽  
Miroslava Dobrotová ◽  
...  
Keyword(s):  
Mtt Assay ◽  
Study Drug ◽  
Cellular Level ◽  
In Vitro Testing ◽  
In Vitro Test ◽  
Vitro Assay ◽  
Drug Concentrations ◽  
Leukaemic Cells ◽  
Relapsed Disease

AbstractThe fact that leukaemic cells are primarily or secondarily resistant to cytostatics is a serious phenomenon, which leads to the failure of chemotherapy of malignant diseases in clinical practise. Some detoxification and transporting systems are responsible for the generation of chemoresistance on the cellular level and the decrease of effectiveness in treatment. In vitro testing of chemoresistance of leukaemic cells is presently an inseparable component of “tailoring” therapy in the developing field of predictive oncology. The aim of this work was to estimate profiles of drug resistance, based on the predictive in vitro test, and to help in choosing the most effective cytostatic. The 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazoline (MTT) assay was used, based on the direct effect of cytostatics on the viability of leukaemic cells in vitro. The number of living leukaemic cells was evaluated by a computer program, where LC50 (concentration of cytostatics lethal to 50% of leukaemic cells) was established from the achieved dose-relation curves. Seventy-one samples of leukaemic cells isolated from the patients’ peripheral blood or bone marrow were examined. All samples were tested to 3 cytostatics minimally. It was found by the in vitro assay, that resistance to dexamethasone, prednisolone, etoposide and vincristine is increased in patients with acute myeloid leukaemia disease, compared to the acute lymphoblastic leukaemia patients. In patients with a relapsed disease population, leukaemic cells are highly heterogeneous in the MTT assay. It was concluded that the MTT assay can be used to study drug interactions in vitro in leukaemia samples. The type of interaction was highly different between patients, and depended on drug concentrations.

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