ChemInform Abstract: A Remarkably Simple One‐Step Procedure for the Preparation of α‐Bromo‐α,β‐Unsaturated Carbonyl Compounds

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Five-And Six-Membered Cyclic a-Acylvinyl Anionic Synthons: Synthesis of a-Trimethylsilyl-α ,ß-Unsaturated Cycloalkenones and their Conversion into 2-(hydroxydimethylsilyl)cycloalk-2-Enones through Carbon-Silicon Bond Scission

Five- and six-membered -trimethylsilyl-,-unsaturated cycloalkenones were prepared by the Wurtz-Fittig coupling reaction of the corresponding 6-bromo1,4 dioxaspiro[4,n]cycloalk-6-enes with sodium and chlorotrimethylsilane. Upon treatment with anhydrous AlCl3, the compounds underwent carbon-silicon bond scission to yield a novel class of compounds: the 2- (hydroxydimethylsilyl)cycloalk-2-enone

FORMULATION AND EVALUATION OF AN HERBAL ANTI-INFLAMMATORY GEL CONTAINING TRIGONELLA FOENUM GREACUM SEED EXTRACT

Objective: The present study was aimed to develop topical gel containing Trigonella foenum greacum (fenugreek) seed extract using carbopol-934, Hydroxypropyl methylcellulose K4M (HPMC K4M) as gelling agents and to investigate the anti-inflammatory activity of suitable gel formulation.Methods: Gels were prepared using carbopol-934, HPMC K4M individually as well as in combination as gelling agents. Prepared formulations were evaluated for various physicochemical properties. Based on in vitro permeation study, the best gel formulation was chosen and it was subjected to in vivo anti-inflammatory activity studies using carrageenan-induced rat paw edema model and kept for stability studies for a period of three months.Results: Gels prepared with a combination of carbopol-934 & HPMC K4M as gelling agent showed highest drug release of 88.02±0.06 % after 8 h of in vitro release study when compare to other formulations. Among the prepared formulations of fenugreek, gels prepared with a combination of carbopol-934 & HPMC K4M showed significant reduction of paw edema (57.78%) when compared to the control topical base group after 3 h from carrageenan injection.Conclusion: Fenugreek has high potential as an anti-inflammatory agent when formulated as an herbal gel for topical use and can be effective in acute inflammatory disorders.Â

Functionalization and Modification of Naphthaquinone Analogs as HER2 Kinase Inhibitors

HER2 overexpression in breast cancer tumors predicts lower overall survival. Because of the aggressive nature of HER2 tumors and the association with metastatic disease, the HER2 receptor holds great promise as a therapeutic target in metastatic breast cancer. We are developing small molecule inhibitors that bind to the ATP binding site of the tyrosine kinase domain in order to inhibit tyrosine auto-phosphorylation. This process controls biological pathways that mediate the cell growth. In normal cells this process is highly controlled. We are targeting the modification of the side chain of the hydroxy methyl group of 2-Hydroxy methyl-5,8-dimethoxy-1,4-naphthaquinone. These compounds should inhibit the tyrosine kinase cascade of reactions thereby suppressing the overexpression of HER2 shutting down the tumor growth. The synthesis and characterization of a series of substituted naphthaquinone analogs with different increasing chain lengths will be reported

Microfluidic Digital ELISA towards Single Cell Analysis

Cell-to-cell heterogeneity predicts a multitude of functions for homeostasis and development of disease states. These minute variations can make a massive impact in understanding the main components involved in a disease such as cancer. Tracking the protein expression in single cells is in great need as they enable the study of heterogeneous behaviors, but the main challenges are the requirement of the methodologies that are sensitive enough to detect low copy number of protein molecules within a wide dynamic range. Low copy proteins cannot be neglected as they can provide information about the phenotypic responses involved. Moreover, traditional analog methods are not suitable for detecting such small numbers as they give an average measurement, differentiating unique cells and quantifying population distributions would be problematic. Digital immunoassays have emerged as a robust technology for ultrasensitive detection of proteins. Here we engineered a multiplexed microfluidic digital ELISA platform with microarray structures for analyzing multiple proteins with low sample volume and high sensitivity. Cross communication between individual reactions, diffusing of reagents into bulk solutions and evaporation of solvents could be critical. To address this concern, we have developed a portable, automated instrument for sealing the microwells in the chambers with high pressure for conducting chemi- fluorescent reactions with increased resolution and sensitivity. With our developed platform, we can detect up to 15 biomarkers. We also applied our digital platforms for the detection of PSA aptamer with biotinylated lectins

ANTIMICROBIAL POTENTIAL OF HYDROGEL INCORPORATED WITH PLGA NANOPARTICLES OF CROSSANDRA INFUNDIBULIFORMIS

Objective: Present study is aimed at formulation of Hydrogel containing Poly Lactic Glycolic Acid (PLGA) nanoparticles incorporated with ethanolic extract of Crossandra infundibuliformis (EECI) and investigate the efficacy of hydrogel nanoparticles as a carrier of antimicrobial constituents. Methods: Poly Lactic Glycolic Acid (PLGA) nanoparticles containing ethanolic extract of Crossandra infundibuliformis (EECI) were synthesized by an emulsion-evaporation method and their physicochemical properties were studied. Polymeric PLGA nanoparticles were then incorporated into gel matrix, using Hydroxy Propyl Methyl Cellulose (HPMC K4M) as a base. The antibacterial activity of nanoparticulated hydrogel formulations were evaluated by agar well diffusion method against Staphylococcus aureus, Bacillus subtilis, Escherichia coli and Pseudomonas aeruginosa. Results: Nanoparticulate hydrogel formulations exhibited high viscosity, neutral pH with good spreadability which is appropriate for transdermal application as well as showed prolonged drug release from optimized formulation up to 24 h. Nanoparticulate hydrogel formulations were effective inhibitors of all the micro-organisms with more promising activity against Staphylococcus aureus. Conclusion: Nanoparticulate hydrogel formulation can be used as a feasible alternative to conventional formulations of Crossandra infundibuliformis extract with advanced permeation characteristics of antimicrobial constituents for transdermal application

Excerpts of Daivavyapashraya Chikitsa in unpublished manuscript Kashyapa Samhita - A New Outlook

The concept of Daivavyapashraya Chikitsa (a modality of treatment based on past deeds and pleasing of god) has been given least importance in the available Ayurvedic classics. Here is the study of a manuscript named Kashyapa Samhita which is quite different from deemed Kashyapa Samhita that is known off. The study was carried out by deciphering and critically editing six manuscripts collected from IPGT & RA (with accession no. 6512 and 10779), Tanjore Sarasvati Mahal Library (with accession no. 11045), Sampurnananda Library, Varanasi (with accession no. 1088604) and Oriental Research Institute, Mysore (with accession no. A129), MS University Baroda Library (with accession no. 13474B). This manuscript brings out ample references regarding Daivavyapashraya Chikitsa for different diseases caused due to sinful acts

Internet of Things Based Smart Agriculture and Applications

Introduction of internet of things brought many changes in different fields like medical, transportation etc. Advancement of this technology has become one of the major advantages to live a happy and smart life. And due to the recent climatic conditions which are rapidly changing, it has become difficult for the farmer to use the regular practice. Mainly agriculture includes farming and cattle management, this paper discuss about few applications that result in effective farming and efficient cattle management. This paper gives a brief idea to the reader about hardware components that can be implemented in agricultural practices. The main intention of this paper is to convert traditional agriculture to smart agriculture by implementing various applications like smart irrigation system, livestock monitoring system, smart greenhouses and agricultural drones. In all, the applications discussed in this paper include the information collected by these systems are sent as alerts or Short Messaging Services (SMS) to the farmers. It also narrates , why we need smart agriculture and what are different applications to be implemented in one’s farm

STRUCTURE-BASED MULTITARGETED MOLECULAR DOCKING ANALYSIS OF PYRAZOLE-CONDENSED HETEROCYCLICS AGAINST LUNG CANCER

Objective: The significant drawbacks of chemotherapy are that it destroys healthy cells, resulting in adverse effects. Hence, there is a need to adopt new techniques to develop cancer-specific chemicals that target the molecular pathways in a non-toxic fashion. This study aims to screen pyrazole-condensed heterocyclics for their anticancer activities and analyse their enzyme inhibitory potentials EGFR, ALK, VEGFR and TNKS receptors. Methods: The structures of the compounds were confirmed by IR, NMR and Mass spectral studies. The in silico techniques applied in this study were molecular docking and pharmacophore modeling to analyse the protein-ligand interactions, as they have a significant role in drug discovery. Drug-likeness properties were assessed by the Lipinski rule of five and ADMET properties. Anticancer activity was performed by in vitro MTT assay on lung cancer cell lines. Results: The results confirm that all the synthesised pyrazole derivatives interacted well with the selected targets showing docking scores above-5 kcal/mol. Pyrazole 2e interacted well with all the four lung cancer targets with its stable binding mode and was found to be potent as per the in vitro reports, followed by compounds 3d and 2d. Pharmacophore modeling exposed the responsible features responsible for the anticancer action. ADMET properties reported that all the compounds were found to have properties within the standard limit. The activity spectra of the pyrazoles predicted that pyrazolopyridines (2a-2e) are more effective against specific receptors such as EGFR, ALK and Tankyrase. Conclusion: Thus, this study suggests that the synthesised pyrazole derivatives can be further investigated to validate their enzyme inhibitory potentials by in vivo studies