Synthesis and pharmacological screening of new isatin-3-[N2-(benzimidazol-1- acetyl)]hydrazone

Twenty new isatin-3-[N2-(benzimidazol-1-acetyl)]hydrazones (IV) were synthesized from ten different isatin-3-[N2–(chloroacetyl)] hydrazones (III) by reacting with benzimidazole and 2-methyl benzimidazole. The intermediates were obtained from isatin hydrazones (II) on condensation with chloroacetyl chloride. These compounds were characterized by IR, 1H NMR and mass spectra. All the compounds were screened for antimicrobial, antioxidant and cytotoxic activity. Some of the new compounds showed promising antibacterial and antifungal activity.               KEY WORDS: Antibacterial activity, Antifungal activity, Antioxidant activity, Cytotoxic activity, Benzimidazole, Isatin Bull. Chem. Soc. Ethiop. 2019, 33(2), 321-329. DOI: https://dx.doi.org/10.4314/bcse.v33i2.1

CONSIDERATION OF RESOURCEFUL DATA AGGREGATION IN SENSING OF MOBILE SYSTEMS

Ad-hoc networks maintain routing among any pair of nodes while sensor networks encompass an additional dedicated communication prototype. Security concerns in ad-hoc networks are comparable to those within sensor networks and were enumerated in literature; however the defence method developed in support of ad-hoc networks is not unswervingly appropriate towards sensor networks. Because of restriction in bandwidth as well as buffer space, delay tolerant networks are susceptible to flood attacks. Although numerous schemes were projected to protect against flood attacks on Internet as well as in wireless networks, they believe constant connectivity moreover cannot be unswervingly applied to delay tolerant networks that have irregular connectivity. Networks of disruption tolerant consist of mobile nodes approved by human beings and networks facilitate data transport when mobile nodes are simply occasionally associated, making them suitable for functions where no communication transportation is accessible. We make use of rate limiting to protect against flood attacks within delay tolerant networks. Each node has an edge above packets that it, like a source node, can transmit towards network in every time period. Our fundamental idea of discovery is claim-carry-and-check. Proposed system works in a dispersed manner, does not depend on any online central authority or else infrastructure, which well suits environment of delay tolerant networks and employs well-organized constructions to maintain computation, communication as well as storage cost small

MESUAFERRIN A-BIOACTIVE FLAVONOID ISOLATED FROM THE BARK OF MESUA FERREA L. AGAINST PHOSPHOLIPASE A2, CYCLOOXYGENASE AND LIPOXYGENASE: AN IN VITRO, IN VIVO AND IN SILICO APPROACH

Objective: The main objective of the present study was to evaluate the anti-inflammatory activity of isolated bioactive flavonoid Mesuaferrin-A from the bark of Mesuaferrea L. by in vitro, in vivo and in silico approach.Methods: To evaluate the effect of isolated bioactive flavonoid Mesuaferrin-A on arachidonic acid metabolizing enzymes (PLA2, COX-2 and 5-LOX) using in vitro methods, followed by carrageenan-induced paw edema model by in vivo and to determine the binding orientation and interactions of Mesuaferrin-A onarachidonic acid metabolizing enzymes (PLA2, COX-2 and 5-LOX) crystal proteins using molecular docking (in silico) studies.Results: Mesuaferrin-A exhibited a dose-dependent significant 5-LOX inhibitory and considerable COX-2 inhibitory activity by in vitro, The inhibitory activities of 5-LOX and COX-2 at 100µg/ml were found to be 78.67%, 81.03% with IC50 values of 45.22µg/ml and 35.74µg/ml respectively. Whereas Mesuaferrin-A showed less PLA2 inhibitory activity. Mesuaferrin-A showed 68.34% inhibitory activity at 400 mg/kg body weight at the late phase of carrageenan-induced paw edema, and In silico studies demonstrated that Mesuaferrin-A strongly binds with 5-LOX and COX-2, these strong binding affinity of Mesuaferrin-A on active site amino acids of 5-LOX and COX-2 may be responsible for inhibition of enzyme activity. Mesuaferrin-A showeda comparable 5-LOX and COX-2 inhibition activity with (positive control).Conclusion: It was concluded that Mesuaferrin-A act as 5-LOX and COX dual inhibitor, from the results it was suggests that Mesuaferrin-A, may be an effective preventive and therapeutic approach for patients with inflammatory-related diseases

Scaling Qubit Readout with Hardware Efficient Machine Learning Architectures

Reading a qubit is a fundamental operation in quantum computing. It translates quantum information into classical information enabling subsequent classification to assign the qubit states `0' or `1'. Unfortunately, qubit readout is one of the most error-prone and slowest operations on a superconducting quantum processor. On state-of-the-art superconducting quantum processors, readout errors can range from 1-10%. High readout accuracy is essential for enabling high fidelity for near-term noisy quantum computers and error-corrected quantum computers of the future. Prior works have used machine-learning-assisted single-shot qubit-state classification, where a deep neural network was used for more robust discrimination by compensating for crosstalk errors. However, the neural network size can limit the scalability of systems, especially if fast hardware discrimination is required. This state-of-the-art baseline design cannot be implemented on off-the-shelf FPGAs used for the control and readout of superconducting qubits in most systems, which increases the overall readout latency as discrimination has to be performed in software. In this work, we propose HERQULES, a scalable approach to improve qubit-state discrimination by using a hierarchy of matched filters in conjunction with a significantly smaller and scalable neural network for qubit-state discrimination. We achieve substantially higher readout accuracies (16.4% relative improvement) than the baseline with a scalable design that can be readily implemented on off-the-shelf FPGAs. We also show that HERQULES is more versatile and can support shorter readout durations than the baseline design without additional training overheads

PROGRAMMABLE GENERATOR PRODUCING VIRTUAL ARBITRARY TEST PATTERNS

The suggested hybrid plan efficiently combines test compression with LBIST, where both techniques could work synergistically to provide top quality tests. It is composed of a straight line finite condition machine driving a suitable phase shifter, and it arrives with numerous features permitting this product to create binary sequences with preselected toggling (PRESTO) activity. We introduce a means to instantly select several controls from the generator offering simple and easy, precise tuning. This paper describes a minimal-power (LP) generator able to creating pseudorandom test designs with preferred toggling levels that has been enhanced fault coverage gradient in comparison using the best-to-date built-in self-test (BIST)-based pseudorandom test pattern machines. Exactly the same strategy is subsequently used to deterministically advice the generator toward test sequences with enhanced fault-coverage-to pattern-count ratios. In addition, this paper proposes an LP test compression way in which enables shaping the exam power envelope inside a fully foreseeable, accurate, and versatile fashion by adapting the PRESTO-based logic BIST (LBIST) infrastructure. Experimental results acquired for industrial designs illustrate the practicality from the suggested test schemes and therefore are reported herein

Novel Frame Work for Blockchain Based Votingapplication Using Ethereum Virtual Machine

Blockchain fills in as a scattered record development which licenses propelled assets for be executed in decentralized framework which works in a common manner. In bound together systems everything depends upon the central structure and the outcomes of throwing a voting form system were not exact considering the way that anyone can change. These kinds of results are wrong and not trustworthy by the people who are voting. The Voting machines that are accessible as of now rely upon the servers which are centralized. Here the people who are voting have to keep belief on the concentrated individuals for the accurate results. So, the contemplating decentralized law-based systems that can settle on the political choice procedure very snappy and easy. These scattered systems are the most praised advancement improvement in this present genuine world. Here Blockchain advancement has various wide extent of usages starting and beginning from distributing statistics, economics etc. Here the blockchain advancement is used as a help of achieve this just assembled application that depends concerning a decentralized appropriated application. Here, the structure works in the way as follows, the transactions or understandings whichever executed are changed over into machine reasonable method of reasoning that engages and ensures understanding among various people who are in the organization, and in like manner who has the solidarity to support their individual money exchanges, different activities and opposite party challenges that are associated with their checking and observing. Smart understandings will be enabled and they are to be passed on into a blockchain space or stage, the amount of possible use cases for this development will be checked and improves amazingly. The most critical use of this blockchain is that to empty the prerequisite for pariahs in the two individuals when all is said in done and the private parts, to end up being progressively capable and effective

Assessment of Genetic Diversity in Guava (Psidium guajava) Germplasm Using Microsatellites

Although the varietal diversity is fairly rich in guava, most varieties lack one or more desirable characters. Hence, attempts were made for improving specific traits, viz., attractive pink pulp colour, soft seeds, medium fruit size, high TSS and high ascorbic acid. Genetic diversity analysis is a prerequisite for identifying potential parents in breeding programs and germplasm conservation. Molecular characterization helps discriminate closely-related genotypes, as, this technique is unaffected by environment, rendering it more reliable. In this study, 48 polymorphic SSRs screened from a total of 115 SSR markers were used for analyzing marker segregation in 72 guava accessions. Statistical analysis was done using IDENTITY1.0 and CERVUS 3.0 software. Cluster analysis was done with DARwin 5.0 software, using Wards Minimum Variance method, and weighted group neighbour joining method, to check reliability of grouping among clusters. The trend in grouping was found to be similar in both methods. Dendrograms generated showed that the hybrids clustered with their parents; exotic collections fell into two different sub-groups based on productivity; the wild species formed one group; and Navalar cultivars from Dharwad clustered together, reflecting similar origin

Quercetin activates vitamin D receptor and ameliorates breast cancer induced hepatic inflammation and fibrosis

AimsTo explore the hepatoprotective role of quercetin and its novel molecular mechanism of action on breast cancer associated hepatic inflammation and fibrosis via Vitamin D receptor (VDR).Main methodsWe used Ehrlich Ascites Carcinoma (mouse mammary carcinoma) model for our in-vivo experiments and human breast cancer cell lines for in-vitro assays. We inoculated 1.5 × 106 Ehrlich ascites carcinoma cells into female Swiss albino mice. Quercetin (50 mg/kg) was administered intraperitoneally for 15 days. Liver enzymes activity was determined using a spectrophotometric assay. The hallmarks of inflammation and fibrosis were determined using Immunohistochemistry. The effect of quercetin on tumor formation was elucidated using human breast cancer cell lines and chick chorioallantoic membrane assay. Docking study was performed to explore the binding mode of quercetin with VDR.Key findingsIn EAC tumor-bearing mice, cell numbers, tumor volume, body weight and liver weight were dramatically increased, while they significantly decreased in mice treated with quercetin. Additionally, the peritoneal neo-angiogenesis was also significantly suppressed in the quercetin-treated mice, compared to the control. In addition, quercetin treated EAC tumor bearing mice had lower levels of liver enzymes, decreased hepatic inflammation and fibrosis compared with EAC tumor bearing mice. Docking study confirmed VDR-quercetin interaction. Furthermore, in-vitro assays and chick chorioallantoic membrane assay revealed the Vitamin D mimicking effect of quercetin.SignificanceDietary flavonoid, quercetin could act as a promising therapeutic drug to suppress the breast cancer induced tumor angiogenesis, hepatic inflammation, and fibrosis possibly via activation of VDR

Inflammation-Associated Nitrotyrosination Affects TCR Recognition through Reduced Stability and Alteration of the Molecular Surface of the MHC Complex

Nitrotyrosination of proteins, a hallmark of inflammation, may result in the production of MHC-restricted neoantigens that can be recognized by T cells and bypass the constraints of immunological self-tolerance. Here we biochemically and structurally assessed how nitrotyrosination of the lymphocytic choriomeningitis virus (LCMV)-associated immunodominant MHC class I-restricted epitopes gp33 and gp34 alters T cell recognition in the context of both H-2Db and H-2Kb. Comparative analysis of the crystal structures of H-2Kb/gp34 and H-2Kb/NY-gp34 demonstrated that nitrotyrosination of p3Y in gp34 abrogates a hydrogen bond interaction formed with the H-2Kb residue E152. As a consequence the conformation of the TCR-interacting E152 was profoundly altered in H-2Kb/NY-gp34 when compared to H-2Kb/gp34, thereby modifying the surface of the nitrotyrosinated MHC complex. Furthermore, nitrotyrosination of gp34 resulted in structural over-packing, straining the overall conformation and considerably reducing the stability of the H-2Kb/NY-gp34 MHC complex when compared to H-2Kb/gp34. Our structural analysis also indicates that nitrotyrosination of the main TCR-interacting residue p4Y in gp33 abrogates recognition of H-2Db/gp33-NY complexes by H-2Db/gp33-specific T cells through sterical hindrance. In conclusion, this study provides the first structural and biochemical evidence for how MHC class I-restricted nitrotyrosinated neoantigens may enable viral escape and break immune tolerance