Molecular pathways with role to play in oral cancer: A mini-review
Oral cancer is the sixth most prevalent type of cancer worldwide and third in India out of the different cancer types identified. Mouth and oral cancers collectively refer to cancers of the buccal cavity, lips, oropharynx, hypopharynx, and larynx. Genetic anomalies, the upregulation of several proteins, the deregulation of tumor-suppressive and oncogenes, and risk factors like alcohol and tobacco consumption are a few examples of the known irregularities that contribute to the development of oral cancer through the accumulation of various carcinogenic substances. Oral cancer is caused and developed by multiple molecular and cellular pathways such as PI3K/AKT/mTOR, Ras-Raf-MEK-ERK pathway, Wnt signaling, NF-κB pathway, Hippo pathway, etc. In addition, various genes including TP53, PTEN, CDKN2A, HRAS, PIK3CA, NOTCH1, IRF6, TP63, etc. are also involved in this malignancy. Therefore, it is crucial to have a deep understanding of these pathways to properly understand the development of oral cancer. This short review focuses on compiling together various signaling and molecular pathways accountable for oral carcinoma development.
Synthesis of Indole-Oxadiazole coupled isoxazole hybrids as potent EGFR targeting anticancer agents
The synthesis of new indole-oxadiazole coupled isoxazole hybrids (6a–o) synthesized by the Cu(I)-catalyzed reaction of in situ generated nitrile oxides with 3-(3,5-dichloro-4-methoxyphenyl)-5-(1-(prop-2-yn-1-yl)-1H-indol-3-yl)-1,2,4-oxadiazole in good yields have been reported here. The chemical structures of all newly synthesized hybrids were confirmed by 1H-NMR, 13C-NMR, and Mass spectra. All synthesized compounds were screened for their in vitro cytotoxicity against two breast cancer cell lines MCF-7 and MDA-MB-231 respectively. All the derivatives were more active against MCF7 than MDA-MB-231 cancer cells and few compounds showed better activity than the standard erlotinib. The ability of more potent compounds to inhibit EGFR tyrosine kinase, one of the key enzymes involved in breast carcinomas was evaluated by in vitro enzymatic assay and it was found that the compound (6g) and (6m) had more inhibitory activity IC50 values 0.311±0.05 and 0.203±0.03 mM than erlotinib (IC50=0.421±0.03 mM).
Synthesis of 1,4-disubstituted-1,2,3-Triazole derivatives for investigation of inhibition and molecular docking studies against Xanthine Oxidase
This study evaluates the inhibition effect of new 1,4-disubstituted-1,2,3-triazoles against Xanthine Oxidase supplemented by molecular modelling. Nine compounds of 1,4-disubstituted-1,2,3-triazoles by Sharpless’s approach have been synthesized in this report. The structures of the synthesized compounds were characterized using FT-IR, 1H and 13C-NMR and Mass spectroscopies Among these synthesized molecules (5-bromothiophen-2-yl)(1-(3-fluorobenzyl)-1H-1,2,3-triazole-4-yl)methanone (9f) and (5-Bromothiophen-2-yl(1-(4-methoxybenzyl)-1H-1,2,3-triazole-4-yl)methanone (9h) showed better activity against Xanthine oxidase (XO) compared to allopurinol. In the light of the XO inhibition results, triazoles having of ketone moiety (9f-i) were found to be more active than triazoles of ketone-free (9a-e). These results were supported by docking models. The docking calculations of the target XO with nine available compounds showed good binding energies with favourable binding interactions. These findings were particularly evident that 9f (BE -7.29 kcal/mol) and 9h (BE -7.59 kcal/mol) are represented encouraging higher inhibition properties towards xanthine oxidase (XO), compared to allopurinol as a reference compound. Significant binding energies and interactions obtained by performing the docking studies are demonstrated, in particular, that the compounds 9f and 9h may be more potential bio compounds than the positive compounds, allopurinol, and febuxostat.
Impact of resistin gene polymorphism on insulin resistance and Type 2 diabetes in Iraqi Babylon province patients
Resistin is cysteine-rich polypeptide produced by adipocytes and macrophages. This study aims to assess the role of resistin and its gene polymorphisms (rs-34861192 G>A, NG-023447 C>G) as potential link between obesity and insulin resistance in the development of T2DM. Blood samples were collected from 120 participants (60 control are divided into 30 normal weight and 30 obese without T2DM) and (60 patients of Type 2 dm DM) are divided into 30 normal weight and 30 obese). Resistin and insulin levels were increased significantly in the patients’ group (p<0.05). Gene analysis indicated that rs-34861192 was associated significantly (P<0.01) with T2DM in dominant, recessive, and co-dominant models. The rs-34861192 AA genotype showed a significant difference in normal-weight and obese T2DM compared to control (P<0.001) only. The significant difference of GG genotype in normal-weight patients than control exclusively. In the diabetic patients, mutant genotype (AA) of rs34861192 was associated with circulating resistin level. The expression of retn gene was high. Genotype AA of rs- 34861192 was correlated positively with folding change. Mutant AA of rs-34861192 G>A plays an important role in development of T2DM through its effect on resistin levels in the circulation that considered as a major factor for developing T2DM.
Synthesis of novel phthalimide-based piperazine conjugated analogs as anti-malarial agents
In the present report, we synthesized twelve novel phthalimide analogs and evaluated for antiplasmodial efficacy on Plasmodium falciparum culture. Two molecules exhibited significant inhibition percentages at 1 µM concentration without any apparent cytotoxicity on HepG2 cells. Inhibitory concentration (IC50) for both the hit compounds 6d and 8a was observed in micromolar range, 1.20 µM and 1.66 µM, respectively. Extensive in silico studies conducted indicate plasmepsin IX as a possible target for inhibitory activity of the reported molecules.
A special issue covering the recent advances in field of Energy – Renewable and Non-renewable energy resources advances including development of smart and functional materials for development of new energy resources as well as advancement of existing energy resources
Energy is the utmost resource of essential need in development of human beings and science. Research in New energy materials defines the materials of future. Different Functional materials, nanomaterials and green materials are the leading arena in development of new energy resources. This special is envisaged to compile the research advances and knowledge for development of energy resources.
The special issue solicit the articles from all fields of energy research, few subfield to mention include:
Solar Energy Materials Perovskite Solar Cells Battery and Energy storage materials Bio Materials Green Energy sources developments (Biofuels – Biodiesel, BioCNG, Bioethanol) Chemistry of Energy materials Fuel Cells All advances in Energy materials development Photovoltaic nanomaterials Perovskite cells, Nanophotonics, Nanosolar cells, New nanomaterials for solar energy harvesting, Nanothermal energy systems, Nanosystems for harvesting mechanical and other forms of energy Nanogenerator, higher efficiency nanomaterials for existing energy systems (production, transportation and storage), Nanostorage systems for energy – Nanobattery (design and development) Carbon Nano & material development for Energy resources New Chips development for Energy management Nanomaterials for Energy Environmental issues concerned with energy systems MEMS, Semiconductor design for energy systems Carbon nanomaterials based energy generation and storage systems new nanoenergy nanomaterials properties evaluation and all other research advances related to Energy
Dr. B.S. Chhikara University of Delhi, Delhi, India.
Authors need to submit their manuscript in the Energy materials section of the journal. The manuscript should be formatted as per journal format provided in author guidelines section.
Article types: Research Article, Review Article, Short Communications, Experts Opinion article (contact editors before submission of Experts opinions articles).
Last date: The submissions are open now, author can submit their manuscript now, the last date for submissions to be considered in this issue is October 31.
Small-molecules against Oxidative stress mediated Neurodegenerative diseases
Neurodegenerative diseases, marked by the gradual deterioration of neuronal structure and function, impose a significant burden on global healthcare systems. Oxidative stress, resulting from an imbalance between reactive oxidant production and cellular antioxidant defense, is believed to play a significant role in the development of various neurodegenerative disorders, including Alzheimer’s disease, Parkinson’s disease, and Huntington’s disease. Recently, there has been a growing interest in exploring small compounds as potential therapeutic agents to counteract oxidative stress. In addition to highlighting the potential of small molecules to prevent oxidative stress-mediated neuronal damage, this article provides an overview of the function of oxidative stress in neurodegenerative illnesses. Targeting numerous oxidative stress-related pathways, a number of small molecules, including both natural and synthetic antioxidants, have shown promise for neuroprotective benefits. These substances neutralise reactive oxidants, boost endogenous antioxidant defences, reduce inflammation, alter mitochondrial function, and encourage neurotrophic growth.
Molecular links between metabolome and epigenome: AMPK-TET2 signalling pathway and their natural activators
Emerging evidence suggests that sustained diabetes-associated factors such as inflammation, hyperinsulinemia, and hyperglycemia are major contributors to aberrant cell proliferation and subsequent neoplastic transformation. Epidemiological studies have also highlighted that diabetes promoting a sedentary lifestyle, with or without the direct involvement of insulin, is frequently linked to cancer. However, our knowledge regarding the molecular mechanisms that correlate hyperglycemia to oncogenic transformations remains limited. In this regard, a recent study has proved that hyperglycemia inactivates AMPK, destabilizing the TET2 and its tumour-suppressive role and ultimately predisposing diabetes mellitus patients to cancer. We must explore a reverse pharmacology-based ethnopharmacological approach to managing hyperglycemia associated with oncogenesis. Botanical-derived natural products have greater structural and functional diversity with fewer or no side effects on humans. The present review discusses the molecular relationship between hyperglycemia and cancer progression and the impact of natural products as therapeutic agents on the hyperglycemia-cancer-associated signaling pathway.
One of the most notable adverse effects of acidifying air quality is damage to materials exposed to the atmosphere. Systematic fields and laboratory experiments have been done to understand the mechanisms underlying the impacts of pollutants on the measurement of damage and estimate the cost of damage. In this study, authors have synthesized nano polymer film, which is transparent, resistant to acids and flexible. The as-synthesized nano polymer film was characterized using UV-Visible Spectroscopy, FTIR Spectroscopy and Scanning Electron Microscope (SEM). Coating of the nano polymer film was done onto various monuments stone samples and studied their corrosion in the presence of acids.
Association of C-peptide with novel hormones in children with type 1 diabetes: A rising potentials for more reliable biomarkers.
Type 1 diabetes is a heterogeneous disorder caused by reduced β-cell mass as a result of T-cell mediated autoimmune destruction. C-peptide is a linker chain cleaved from proinsulin to produce the mature, functional insulin hormone. Irisin is a novel adipo-myokine plays a crucial role in glucose homeostasis regulation. Preptin is a peptide hormone synthesized in β-cells and plays a role in augmenting insulin secretion. The current study aims to investigate preptin and irisin levels in diabetic children and determine their correlation with C-peptide and the development of this disease. This study recruited 90 children, divided into two groups: 45 patients and 45 controls. Commercial ELISA kits were used to measure C-peptide, irisin, and preptin. C-peptide levels were significantly decreased among the patients’ group (P<0.05). Preptin and irisin levels were significantly increased in the patients’ group (P<0.05). C-peptide was noticeably correlated with preptin, irisin and RBS (P <0.05). Preptin and irisin levels also had a positive correlation with RBS (P<0.05). In regression analysis, irisin had a strong association with C-peptide. In conclusion, irisin was a considerable predictive marker for the residual β-cells through its association with preptin and C-peptide in regression analysis. Preptin might be an indicator of insulin resistance.