55 research outputs found

    Autonomous Agriculture Robot for Smart Farming

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    This project aims to develop and demonstrate a ground robot with intelligence capable of conducting semi-autonomous farm operations for different low-heights vegetable crops referred as Agriculture Application Robot(AAR). AAR is a lightweight, solar-electric powered robot that uses intelligent perception for conducting detection and classification of plants and their characteristics. The system also has a robotic arm for the autonomous weed cutting process. The robot can deliver fertilizer spraying, insecticide, herbicide, and other fluids to the targets such as crops, weeds, and other pests. Besides, it provides information for future research into higher-level tasks such as yield estimation, crop, and soil health monitoring. We present the design of robot and the associated experiments which show the promising results in real world environments.Comment: 12 pages, 8 figures and code available.To be publishe

    Aegle marmelos fruit extract attenuates isoproterenol-induced oxidative stress in rats

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    Myocardial infarction is a major public health concern and the leading cause of death throughout the world. The present study investigates the ability of Aegle marmelos fruit extract to prevent pathological changes and oxidative stress after isoproterenol induced myocardial infarction in rats. In vitro studies showed that Aegle marmelos fruit extract possesses antioxidant activity. Administration of isoproterenol (85 mg/kg body weight) to rats resulted in significantly elevated plasma transaminases, lactate dehydrogenase and creatine kinase, however, cardiac tissue analyses showed decreased activity of the above enzymes compared to experimental control rats. Further, isoproterenol administration significantly increased plasma and cardiac tissue thiobarbituric acid reactive substances and lowered the activities of cardiac tissue superoxide dismutase, catalase, reduced glutathione, glutathione peroxidase and glutathione-S-transferase when compared to control groups. Pretreatment with Aegle marmelos fruit extract at a dose of 150 mg/kg body weight for a period of 45 days significantly prevented the observed alterations. Our data suggest that Aegle marmelos fruit extract exerts its protective effect by decreasing thiobarbituric acid reactive substances and elevating antioxidants status in isoproterenol treated rats. Both biochemical and histopathological results in the isoproterenol-induced myocardial infarction model emphasize the beneficial action of Aegle marmelos fruit extract as a cardioprotective agent

    Renal protective effect of ellipticine against streptozotocin induced diabetic nephropathy in rats via suppression of oxidative stress and inflammatory mediator

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    ABSTRACT Purpose: Diabetes mellitus is a serious health problem worldwide, and diabetic nephropathy is the complication. The diabetic nephropathy considerably enhances the oxidative stress, glycation, lipid parameters and inflammatory reaction. Ellipticine has potent free radical scavenging and anti-inflammatory effect. Methods: In the current study, our objectives were to thoroughly examine the renal protective effects of ellipticine in a rat model of streptozotocin (STZ)-induced diabetic nephropathy (DN) and to elucidate the underlying mechanisms involved. For the induction of diabetic nephropathy, streptozotocin (50 mg/kg) was used, and rats were separated into groups and given varying doses of ellipticine (2.5, 5 and 7.5 mg/kg). The body weight, and renal weight were estimated. The inflammatory cytokines, renal biomarkers, inflammatory antioxidant, and urine parameters were estimated. Results: Result showed that ellipticine considerably enhanced the body weight and reduced the renal tissue weight. Ellipticine treatment significantly (P < 0.001) repressed the level of blood urea nitrogen, serum creatinine, uric acid, blood glucose and altered the lipid parameters. Ellipticine significantly (P < 0.001) repressed the level of malonaldehyde and boosted the glutathione, catalase, superoxide dismutase, and glutathione peroxidase. Ellipticine treatment significantly (P < 0.001) reduced the inflammatory cytokines and inflammatory mediators. Conclusions: Ellipticine could be a renal protective drug via attenuating the inflammatory reaction, fibrosis and oxidative stress in streptozotocin induced rats

    A green bio-organic catalyst (taurine) promoted one-pot synthesis of (R/S)-2-thioxo-3,4-dihydropyrimidine(TDHPM)-5-carboxanilides: chiral investigations using circular dichroism and validation by computational approaches

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    Owing to the massive importance of dihydropyrimidine (DHPMs) scaffolds in the pharmaceutical industry and other areas, we developed an effective and sustainable one-pot reaction protocol for the synthesis of (R/S)-2-thioxo-DHPM-5-carboxanilides via the Biginelli-type cyclo-condensation reaction of aryl aldehydes, thiourea and various acetoacetanilide derivatives in ethanol at 100 °C. In this protocol, taurine was used as a green and reusable bio-organic catalyst. Twenty-three novel derivatives of (R/S)-TDHPM-5-carboxanilides and their structures were confirmed by various spectroscopy techniques. The aforementioned compounds were synthesized via the formation of one asymmetric centre, one new C–C bond, and two new C–N bonds in the final product. All the newly synthesized compounds were obtained in their racemic form with up to 99% yield. In addition, the separation of the racemic mixture of all the newly synthesized compounds was carried out by chiral HPLC (Prep LC), which provided up to 99.99% purity. The absolute configuration of all the enantiomerically pure isomers was determined using a circular dichroism study and validated by a computational approach. With up to 99% yield of 4d, this one-pot synthetic approach can also be useful for large-scale industrial production. One of the separated isomers (4R)-(+)-4S developed as a single crystal, and it was found that this crystal structure was orthorhombic

    A green bio-organic catalyst (taurine) promoted one-pot synthesis of (R/S)-2-thioxo-3,4-dihydropyrimidine(TDHPM)-5-carboxanilides: chiral investigations using circular dichroism and validation by computational approaches

    Get PDF
    Owing to the massive importance of dihydropyrimidine (DHPMs) scaffolds in the pharmaceutical industry and other areas, we developed an effective and sustainable one-pot reaction protocol for the synthesis of (R/S)-2-thioxo-DHPM-5-carboxanilides via the Biginelli-type cyclo-condensation reaction of aryl aldehydes, thiourea and various acetoacetanilide derivatives in ethanol at 100 °C. In this protocol, taurine was used as a green and reusable bio-organic catalyst. Twenty-three novel derivatives of (R/S)-TDHPM-5-carboxanilides and their structures were confirmed by various spectroscopy techniques. The aforementioned compounds were synthesized via the formation of one asymmetric centre, one new C–C bond, and two new C–N bonds in the final product. All the newly synthesized compounds were obtained in their racemic form with up to 99% yield. In addition, the separation of the racemic mixture of all the newly synthesized compounds was carried out by chiral HPLC (Prep LC), which provided up to 99.99% purity. The absolute configuration of all the enantiomerically pure isomers was determined using a circular dichroism study and validated by a computational approach. With up to 99% yield of 4d, this one-pot synthetic approach can also be useful for large-scale industrial production. One of the separated isomers (4R)-(+)-4S developed as a single crystal, and it was found that this crystal structure was orthorhombic

    Development of potent and selective inhibitors for ATR: an adjuvant for DNA damage based chemotherapeutics

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    Inhibition of DNA damage checkpoint and repair function has been a challenging as well a promising approach in cancer therapy. ATR kinase is one of the key mediator of DNA damage response which induces cell cycle arrest and DNA repair via its downstream proteins. Blocking ATR has proved to prevent the Chk1 pathway from stalled replication fork and enhances the replication stress and premature mitotic entry. In addition inhibition of ATR can selectively sensitize the cancer cell to radio and chemotherapy, due to defective DNA damage signaling through the loss of ATM or p53 mutation in cancer cell. Due to its inherent role in DDR, ATR has been explored as a potential target in enhancing the effect of radiation and chemo-therapy in addition enables highly selective targeting the cancer cell through synthetic lethality. Despite the attractiveness of ATR inhibition in the cancer therapy, specific ATR inhibitors have remained indefinable. Further, there is a limited proof of concept data for ATR inhibition. Considering these facts and challenges we will be presenting some preliminary results with respect to In-silico design, synthesis and evolution of potential and selective inhibitors for ATR.by Sivapriya Kirubakaran, Vijay Thiruvenkatam and Althaf Shai

    In-silico modeling and docking studies of Atagia Telangiectasia and Rad3-related protein (ATR) kinase

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    by Althaf Shaik, Sivapriya Kirubakaran and Vijay Thiruvenkata

    Insights into supramolecular assembly formation of diethyl aryl amino methylene malonate (DAM) derivatives assisted via non-covalent interactions

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    The crystal structures of four derivatives of diethyl 2-(((aryl)amino)methylene)malonate (DAM) have been studied by single crystal X-ray diffraction. The molecular structures of all the four derivatives were found to be in co-planar conformation. The detailed analysis of molecular conformation in four derivatives reveals the presence of a common strong intramolecular N–H⋯O hydrogen bonding, forming a ring of graph-set motif S11 (6). The effect of chloro and nitro substitution on their relative strengths of hydrogen bonding are analyzed here. Particularly, in compound 1, additional intramolecular hydrogen bonding between –NO2 and N–H was observed that results in the formation of another six-membered chelate ring. On the other hand in case of compound 3, we have observed type-I Cl⋯Cl interaction for the first time in this class of compounds. Further, Hirshfeld surface has been generated that is mapped with dnorm shape index and curvedness to summarize the weak interactions and examine the molecular shapes in all four derivatives. Effect of nitro (1 and 2) and chloro (3 and 4) substitution on the C⋯H, N⋯O and C⋯O interaction is highlighted in molecular contour and 2D fingerprint plots.by Althaf Shaik, Deekshi Angira and Vijay Thiruvenkata

    Evaluation of MBP tagged-hATR kinase domain catalytic activity with p53 Ser-15 phosphorylation

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    DNA damage response (DDR) pathways form an integral part of the body’s repair machinery, and ATR (ataxia-telangiectasia and Rad3-related kinase) protein is one of the key mediators in the DDR pathway that helps in maintaining genomic integrity. A growing body of evidence suggests that inhibition of ATR can help sensitize tumor cells to combinatorial treatment. However, specific ATR kinase inhibitors have largely remained elusive until now. Despite much interest in the protein for more than a decade, there has been little characterization of only the kinase domain, an essential target site for a variety of ATR inhibitors. Here, we report our findings for the bacterial expression, purification, and biological characterization of this potentially important recombinant kinase domain, which could further be considered for structure elucidation studies. Introduction of a solubility partner, i.e., maltose binding protein (MBP), at the N-terminus of the ATR kinase domain generated a soluble form of the protein, i.e., MBP-tagged hATR kinase domain (MBP-ATR-6X His), which was found to be catalytically active, as assessed by substrate p53 Ser-15 phosphorylation (EPPLSQEAFADLWKK). Our results also highlight the prospect of utilization of the overexpressed recombinant ATR kinase domain in characterization of kinase domain specific inhibitors.by Rashmi Bhakuni, Althaf Shaik and Sivapriya Kirubakara
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