Chemical Biology Letters <p>Chemical Biology Letters is a peer reviewed indexed international journal for publication of research and review articles from Medicinal Chemistry, BioChemistry, Chemical Biology, Drug Development and Drug Delivery related studies.</p> ScienceIn Publishing en-US Chemical Biology Letters 2347-9825 Green synthsized Allium cepa nanoparticles with enhanced antiprotozoal activities for E. gingivalis <p>Allium cepa has phytochemical characteristics well known to be used in our gastronomy. Due to its particle size, low systemic bioavailability is the major disadvantage associated to be used it for medicinal purpose. These limitations can be overcome by the converting the bulk size particles to nanosized particles. The present study was to prepare the nano-particles of Allium cepa with improved aqueous solubility, and to investigate their efficacy invitro against Entamoeba gingivalis, a protozoan associated with poor oral hygiene leading to advanced periodontal disease. Allium cepa nanoparticles of the size ranging 85–95 nm with the aqueous solubility of upto 3 mg/mL were prepared, and the anti-amoebic activities were tested in-vitro against Entamoeba gingivalis (ATCC 30927). The trophozoites of Entamoeba gingivalis were cultured in the presence of Allium cepa’s Bulk/nano- particles or metronidazole, the inhibition caused by each particles type at various concentrations was calculated by counting the viable trophozoites under the inverted microscope. Allium cepa nanoparticles showed inhibitory results of more than 80%, which is comparable with that of standard drug Metronidazole against <em>E. gingivalis</em> demonstrating its use as a potential anti-parasitic herbal drug.</p> Ramesh Kumar Sumi Nandwani Dr Suman Dr Samander Kaushik Copyright (c) 2020 ScienceIn 2020-11-27 2020-11-27 7 4 247 250 Phytochemical screening, GC-MS analysis and In-vitro Antioxidant potential of Parthenium hysterophorus Stem sequentially extracted fractions <p>Oxidative stress (OS) is involved in pathophysiological events of different diseases. Antioxidants mitigate and suppress the adverse effect of OS in the body. Due to lesser side effects and cost effectiveness natural antioxidant is a choice of people nowadays. The present study was designed to characterize/analyze phytochemicals and antioxidant potential in Parthenium hysterophorus (Asteraceae) stem (PHS) sequentially extracted fractions. Chemical characterization of PHS samples was carried out using Gas Chromatography-Mass Spectrometry (GC-MS) and Spectrophotometric techniques. Comparative antioxidant potential in PHS fractions was studied using in vitro antioxidant models. Thin layer chromatography (TLC) was performed to show a differential occurrence of phytochemicals in test fractions and related radical scavenging potential. PHS fractions showed differential presence of compounds. Appreciable radical scavenging, reducing power, and metal ion chelation potential was found in PHS fractions. In conclusion, P. hysterophorus stem may be considered a good source of natural antioxidant compounds.</p> Shashank Kumar Abhay Kumar Pandey Copyright (c) 2020 ScienceIn 2020-10-15 2020-10-15 7 4 235 241 Novel 5-Nitro Isatin derivatives as DNA Gyrase inhibitors: synthesis, anti-microbial evaluation, molecular docking, ADMET predictions and QSAR studies <p>Novel series of 5-nitroindoline-2-ones was synthesized starting from 5-nitroindoline-2,3-dione <strong>2 </strong>and 2-(5-nitro-2-oxoindolin-3-ylidene)hydrazine-1 carbothioamide <strong>3</strong>. Compounds were evaluated for their antimicrobial activities. The data showed that compounds <strong>2</strong> and <strong>6b</strong> have excellent antimicrobial activities against the two tested strains of G+ve bacteria <em>Staphylococcus aureus</em> and<em> Streptococcus</em> and <em>E. coli </em>when compared with the standards. Furthermore, <em>in-vitro</em> enzyme assay and molecular docking studies were performed for the compounds <strong>2</strong> and <strong>6b </strong>against <em>E. coli </em>DNA gyrase B. Prediction of ADMET properties and QSAR study of compounds was carried out respectively.</p> walaa S El-serwy Neama A Mohamed Emad M. M Kassem Eman S. Nossier Al Shimaa G. Shalaby Copyright (c) 2020 ScienceIn Publishing 2020-07-31 2020-07-31 7 4 197 206 Design, synthesis, ADME prediction and anti-hyperglycemic evaluation of new alkoxyimino-substituted phenyl carboxylic acids as potent alpha-glucosidase inhibitors <p>In an attempt to further explore the role of substituted carboxylic acid derivatives as antidiabetic agent, a series of alkoxyimino-substituted carboxylic acid derivatives (<strong>101-206</strong>) were designed, synthesized and evaluated for their inhibitory potential against <span class="aCOpRe">a</span>-amylase and <span class="aCOpRe">a</span>-glucosidase enzyme. Among all the tested compounds, <strong>102</strong> &amp;<strong> 105</strong> has displayed the most potent activity against <span class="aCOpRe">a</span>-glucosidase with the IC<sub>50</sub> of 142.21±1.8 mM and 182.83±2.43 mM respectively, as compared to the standard drug acarbose (136.89±1.67 mM). Based on the inhibition percentage, the inhibition activity of <strong>102 </strong>and <strong>105</strong> on <span class="aCOpRe">a</span>-glucosidase had higher potential than <span class="aCOpRe">a</span>-amylase. The mode of binding interactions between the <span class="aCOpRe">a</span>-glucosidase enzyme and the compound <strong>102</strong> was established to be uncompetitive using kinetic analysis. The predicted drug-likeness properties (Lipinski parameters and in silico ADME properties) of the compounds revealed their suitability as potential drug candidate.</p> Manisha Khatri Ritika Singh Samreen Fatima Neetu Sain Copyright (c) 2020 ScienceIn Publishing 2020-08-07 2020-08-07 7 4 207 214 Medicinal applications of Saffron plant in Neurological disorders <div><span lang="EN-US">Saffron (<em>Crocus sativus</em> L.) has been widely used in traditional or phytomedicine as a treatment of neurological disorders.</span><span lang="EN-US"> The saffron is showing great potential to treat various neurological diseases without any apparent side effects. As there are very limited drugs available for the treatment of neurological diseases, saffron provides hope to treat the brain disorders and conditions </span><span lang="EN-US">such as anxiety, depression, Alzheimer's disease, and Parkinson's disease. </span><span lang="EN-US">This brief review deals with medicinal applications of saffron plant towards neurological diseases</span></div> Pushpendra Singh Prem Prakash Sharma Copyright (c) 2020 ScienceIn 2020-11-27 2020-11-27 7 4 242 246 1,3,4 Oxadiazole: An emerging scaffold to target different growth factors and kinases <p>Five member heterocyclic 1,3,4-oxadiazole derivatives were synthesized and evaluated for their anticancer activity. Compounds containing 1,3,4-oxadiazole ring in their structure are characterised by multidirectional biological activity. The important mechanism behind tumor suppression by 1,3,4-Oxadiazole is related with the inhibition of different growth factors, enzymes and kinases etc. The 1,3,4-Oxadiazole scaffold is a five member heterocyclic ring having versatile activities and created interest for synthetic organic and medicinal chemists for the designing of novel compounds having anti- cancer activity. There are great potential in the development of the simple and small 1,3,4-oxadiazole nucleus which is present in various compounds that possess considerable pharmcological properties such as anticancer and aimed to evaluate new products. The main aim of this review article is to highlight the targeted activity of 1,3,4-Oxadiazole derivatives and their structure activity relationship to generate potential anticancer agents.</p> Ankita Bharwal Monika Gupta Copyright (c) 2020 ScienceIn 2020-10-14 2020-10-14 7 4 225 235 Treatment of Type 2 diabetes mellitus (T2DM): Can GLP-1 Receptor Agonists fill in the gaps? <p>Type 2 diabetes mellitus (T2DM) is a chronic metabolic syndrome, which occurs due to increased glucose levels in the human body. There has been lot of work in developing novel approaches to tackle this disease. GLP-1 receptor (GLP-1R), one of the class-B G-protein-coupled receptors (GPCR), is a budding molecular target to design drugs for treating type 2 diabetes. In this review, authors have summarized the physiological actions of Glucagon-like peptide-1 receptor (GLP-1R) and current available drugs based on GLP-1 RAs. Some of the exemplary studies in this area have been examined in detail. Authors conclude that development of degradation-resistant, long-acting GLP-1 receptor agonists is a promising area of research and lot of work needs to be done to understand its mechanism of action.</p> Smriti Sharma Vinayak Bhatia Copyright (c) 2020 ScienceIn 2020-08-14 2020-08-14 7 4 215 224