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Selenium Nanoparticles (Se-NPs) are known for their antioxidant and anti-inflammatory activities, which are effective in preventing oxidative damage and improving physiological processes.
This study aimed at investigating the effects of biosynthesized Se-NPs on bone marrow-derived Endothelial Progenitor Cells (bone marrow-derived EPCs) and blood-derived endothelial progenitor cells (blood-derived EPCs) isolated from rabbits in vitro.
The cultured EPCs incubated with biosynthesized Se-NPs at the concentrations of 0.19, 0.38, 0.76, 1.71, 3.42, 7.03, 14.25, 28.50, 57, 114, and 228μg/ml for 48h. After screening the proliferative potential of the Se-NPs by the MTT assay, the best concentrations were selected for Real-Time quantitative Polymerase Chain Reaction (RT-qPCR). Real-time quantification of Vascular Cell Adhesion Molecule 1 (VCAM-1), lectin-like oxidized Low-Density Lipoprotein (LDL) receptor-1 (LOX-1), endothelial Nitric Oxide Synthase (eNOS), and Monocyte Chemoattractant Protein-1 (MCP-1) gene exprvities for bone marrow-derived EPCs and blood-derived EPCs. Our findings suggested that Se-NPs could be considered as an effective agent that may ameliorate vascular problems.
This was the first report to demonstrate the effects of Se-NPs on proliferative, anti-oxidative, and anti-inflammatory activities for bone marrow-derived EPCs and blood-derived EPCs. Our findings suggested that Se-NPs could be considered as an effective agent that may ameliorate vascular problems.
Indole based heterocyclic compounds plays important roles in pharmaceutical chemistry due to their unexpected biological and pharmacological properties.
Herein, we describe novel biological properties (antioxidant, antimicrobial and anticancer) of 3-bromo-1-ethyl-1H-indole (BEI) structure.
BEI was synthesized from 1-Methyl-2-phenylindole and N-bromosuccinimide and were characterized by using 1H and 13C NMR. 1H and 13C NMR. Cytotoxity was determined by MTT assay. Apoptosis analysis of BEI was determined by Arthur™ imagebased Cytometer. Different methods was applied to assessed the antioxidant activity of BEI. Molecular docking studies were conducted to determine the interactions of bonding between GST isozymes and BEI.
According to the antioxidant and antimicrobial activity assays, BEI compound showed less total antioxidant activity compared to trolox standard whereas it showed moderate antimicrobial activity against Aspergillus niger and Phytophora eryhtrospora. Notably, BEI compound demonstrated substantial selective cytotoxicity for the first time towards cancer cell lines and there existed significant decrease in the percentage of live cells treated with BEI, in comparison to the control ones. Interestingly, BEI exhibited a promising glutathione S-transferase isozymes inhibition.
The results of this study suggest that BEI seems to be a promising molecule to be used in design of new anticancer agents that provide superiority to present commercial anticancer drugs.
The results of this study suggest that BEI seems to be a promising molecule to be used in design of new anticancer agents that provide superiority to present commercial anticancer drugs.
Silver nanoparticles (AgNPs) are one of the most investigated nanostructures in recent years, which gives more challenging and promising qualities in different biomedical applications. The AgNPs synthesized by the green approach provide potential healthcare benefits over chemical approaches, including improvement of tissue restoration, drug delivery, diagnosis, environmentally friendly and a boon to cancer treatment.
In the current scenario, the development of safe and effective drug delivery systems is the utmost concern of formulation development scientists as well as clinicians.
Google, Web of Science, PubMed, portals have been searched for potentially relevant literature to get latest developments and updated information related to different aspects of green synthesized AgNPs along with their biomedical applications especially in the treatment of different types of cancers.
The present review highlights the latest published research regarding the different green approaches for the synthesis of AgN
The search for novel metallic chemical compounds with toxicogenic effects have been of great importance for more efficient cancer treatment.
The study evaluated the cytotoxic, genotoxic and mutagenic activity of organoteluran RF07 in S-180 cell line.
The bioassays used were cell viability with 3-(4,5-dimethyl-2-thiazole)-2,5-diphenyl-2-H-tetrazolium bromide (MTT) test, evaluation of apoptosis and necrosis using fluorescence and flow cytometry, cytokinesis-block micronucleus test and comet assay. The compound was tested at 1; 2.5 and 5 µM.
The results showed the cytotoxicity of RF07 at concentrations of 2.5, 5, 10 and 20 µM when compared to the negative control. For genotoxicity tests, RF07 showed effects in all concentrations assessed by increased index and frequencies of damage and mutagenic alterations. The compound was also cytotoxic due to the significant decrease in nuclear division index, with significant values of apoptosis and necrosis. The results of fluorescence and flow cytometry showed apoptosis as the main type of cell death caused by RF07 at 5 µM, which is thought to avoid an aggressive immune response of the organism.
In addition to cytotoxic and genotoxic effects, RF07 creates good perspectives for future antitumor formulations.
In addition to cytotoxic and genotoxic effects, RF07 creates good perspectives for future antitumor formulations.
HSP70 is a survival factor for tumor cells in transformation and in tumor progression as well as in anti-apoptotic response.
Several inhibitors targeting HSP70 ATPase function displayed off-target affect but PES which targets HSP70 substrate binding domain prevents tumor cell survival prominently. However, PES may not bind HSP70 in the absence of nucleotide. This research aimed to design a unique inhibitor molecule that work both in the presence and absence of nucleotides to amplify inhibition.
A set of chimeric coumarine-pyrazole derivatives determined by in silico techniques and synthesized to elucidate their inhibitory effects. Cell viability experiments displayed KBR1307 as the most efficient inhibitor. A set of characterization experiments performed, and results compared to that of PES agent. Binding constant, ATP hydrolysis rate, and percent aggregation determined in the presence and absence of inhibitors.
In silico docking experiments showed that only KBR1307 bind HSP70 substrate binding domain and interact with cochaperone interface. Binding experiments indicated that KBR1307 bind HSP70 both in the presence and absence of nucleotides but PES not. Both inhibitors significantly lower HSP70 ATPase activity and substrate protein disaggregation activity. However, KBR1307 display lower IC50 value at MCF-7 cell line compared to PES. Lomeguatrib Both inhibitors do not alter HSP70 secondary structure composition and overall stability.
KBR1307 effectively inhibits HSP70 compared to PES and provides promising template for novel anticancer drug development.
KBR1307 effectively inhibits HSP70 compared to PES and provides promising template for novel anticancer drug development.With the emergence of the novel severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2), the whole world is suffering from atypical pneumonia, which resulted in more than 559,047 deaths worldwide. In this time of crisis and urgency, the only hope comes from new candidate vaccines and potential antivirals. However, formulating new vaccines and synthesizing new antivirals are a laborious task. Therefore, considering the high infection rate and mortality due to COVID-19, utilization of previous information, and repurposing of existing drugs against valid viral targets have emerged as a novel drug discovery approach in this challenging time. The transmembrane spike (S) glycoprotein of coronaviruses (CoVs), which facilitates the virus's entry into the host cells, exists in a homotrimeric form and is covered with N-linked glycans. S glycoprotein is known as the main target of antibodies having neutralizing potency and is also considered as an attractive target for therapeutic or vaccine development. Similarly, targeting of N-linked glycans of S glycoprotein envelope of CoV via carbohydrate-binding agents (CBAs) could serve as an attractive therapeutic approach for developing novel antivirals. CBAs from natural sources like lectins from plants, marine algae and prokaryotes and lectin mimics like Pradimicin-A (PRM-A) have shown antiviral activities against CoV and other enveloped viruses. However, the potential use of CBAs specifically lectins was limited due to unfavorable responses like immunogenicity, mitogenicity, hemagglutination, inflammatory activity, cellular toxicity, etc. Here, we reviewed the current scenario of CBAs as antivirals against CoVs, presented strategies to improve the efficacy of CBAs against CoVs; and studied the molecular interactions between CBAs (lectins and PRM-A) with Man9 by molecular docking for potential repurposing against CoVs in general, and SARSCoV- 2, in particular.Topoisomerases are reported to resolve the topological problems of DNA during several cellular processes, such as DNA replication, transcription, recombination, and chromatin remodeling. Two types of topoisomerases (Topo I and II) accomplish their designated tasks by introducing single- or double-strand breaks within the duplex DNA molecules, and thus maintain the proper structural conditions of DNA to release the topological torsions, which is generated by unwinding of DNA to access coded information, in the course of replication, transcription, and other processes. Both the topoisomerases have been looked at as crucial targets against various types of cancers such as lung, melanoma, breast, and prostate cancers. Conceptually, targeting topoisomerases will disrupt both DNA replication and transcription, thereby leading to inhibition of cell division and consequently stopping the growth of actively dividing cancerous cells. Since the discovery of camptothecin (an alkaloid) as an inhibitor of Topo I in 1958, a molecular docking, molecular dynamics simulation and QSAR to assess and predict the safety, efficacy, potency and identification of these potent anti-cancerous therapeutic molecules.Immunotherapy emerges as a treatment strategy for breast cancer marker, diagnosis and treatment. In this review, monoclonal antibodies (mAbs)-based passive and peptide vaccines as active immunotherapy approaches like activation of B-cells and T-cells are studied. Passive immunotherapy is mAbs-based therapy effective against tumor cells, which acts by targeting HER2, IGF 1R, VEGF, BCSC and immune checkpoints. Neuropeptide Y (NPY) and GPCR are the areas of interest to target BC metastases for on-targeting therapeutic action. Neuropeptide S (NPS) or NPS receptor 1, acts as a biomarker for Neuroendocrine tumors (NET), mostly characterized by synaptophysin and chromogranin-A expression or Ki-67 proliferation index. The protein fusion technologies arise as a promising avenue in plant expression systems for increased recombinant Ab accumulation and cost-efficient purification. Recently, mAbs-based immunotherapy effectiveness is appreciated as a novel therapeutic combination of chemotherapy and immunotherapy to reduce the side effects and improve therapeutic responsiveness.
