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1.
Mariyappan Vaithiyalingam Dr. Ramasamy Mohan Kumar Dr. Chinnaperumal Kamaraj Vimal Sugumar Nandhagopal Manivannan Shine Kadaikunnan Gajanan Ghodake 《化学与生物多样性》2023,20(6):e202300315
Citral ( 1a ), a bioactive component of Cymbopogon citratus (lemongrass) could be isolated and semi-synthetic analogs synthesized with improved therapeutic properties. Herein we first report describes citral ( 1a ) as a primary material for the synthesis of benzimidazole derivatives between various o-phenylenediamines ( 2a – l ) in the presence of Diisopropylethylamine (DIPEA) as a commercially available environmentally benign base, ethanol as a green solvent and the yield of all benzimidazole derivatives ( 3a – l ) was between 68–76 %; The semi-synthetically prepared benzimidazole derivatives ( 3a – l ) were assessed for their anti-bacterial and anti-fungal properties. The benzimidazole compounds ( 3a – b , and 3g – j ) exhibit good anti-microbial activity. In addition, in silico study was carried out to determine the specific binding affinity of the diamine halogen substituted benzimidazole derivatives to the specific target proteins. In silico analysis revealed a high correlation between docking results and experimental results. Finally, benzimidazole demonstrated significant antibacterial and antifungal activity. Zebrafish embryos were subjected to In vivo toxicological test found that all of the benzimidazole compounds ( 3a – l ) were non-toxic and had low embryotoxicity after 96 h, with an LC50 of 36.425 μg, which could facilitate the design of novel antimicrobial agents using a cost-effective method. 相似文献
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Quantal transmission at purinergic junctions: stochastic interaction between ATP and its receptors. 总被引:1,自引:0,他引:1
The time course of most quantal currents recorded with a small diameter electrode placed over visualized varicosities of sympathetic nerve terminals that secrete ATP was determined: these had a time to reach 90% of peak of 1.3-1.8 ms and a time constant of decay of 12-18 ms; they were unaffected by blocking ectoenzymes or the uptake of adenosine. Monte Carlo methods were used to analyze the stochastic interaction between ATP, released in a packet from a varicosity, and the underlying patch of purinoceptors, to reconstitute the time course of the quantal current. This leads to certain restrictions on the possible number of ATP molecules in a quantum (about 1000) and the density of purinoceptors at the junctions (about 1000 microns-1), given the known geometry of the junction and the kinetics of ATP action. The observed quantal current has a relatively small variability (coefficient of variation < 0.1), and this stochastic property is reproduced for a given quantum of ATP. Potentiation effects (of about 12%) occur if two quanta are released from the same varicosity because the receptor patch is not saturated even by the release of two quanta. The simulations show that quantal currents have a characteristically distinct shape for varicosities with different junctional cleft widths (50-200 nm). Finally, incorporation of an ectoenzyme with the known kinetics of ATPase into the junctional cleft allows for a quantal current of the observed time course, provided the number of ATP molecules in a quantum is increased over the number in the absence of the ATPase. 相似文献
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Selvaraj Jayaraman Vishnupriya Veeraraghavan Radhika Nalinakumari Sreekandan Surapaneni Krishna Mohan Sumetha Suga Deiva Suga Devakumar Kamaraj Sonaimuthu Mohandoss Ponnulakshmi Rajagopal 《Bioinformation》2020,16(11):893
Type 2 diabetes mellitus (T2DM) is linked with Glycogen synthase kinase-3 β.Therefore, it is ofinterest to document molecular docking analysis data of compounds from Justica adhatoda L with glycogen synthase kinase-3 β. We report the binding features of ethambutol, pyrazinamide, stigmasterol and vasicoline with GSK-3 β. 相似文献
4.
Venkatasamy Vignesh Durairaj Rajesh Karuppaiah Parthiban Sridhar Arun Kamaraj Sathish Kumar Ramasamy Thirumurugan 《International journal of peptide research and therapeutics》2021,27(3):1709-1718
International Journal of Peptide Research and Therapeutics - Subtilosin A, a cyclic peptide from Bacillus subtilis is known for its antimicrobial activity against a diverse range of bacteria.... 相似文献
5.
K. Nithya Khalid A.I.M. Bukhari V. Valluvaparidasan M. Rajakumar K. Karunanithi A. Ramesh Sundar 《Archives Of Phytopathology And Plant Protection》2013,46(16):1997-2007
Red rot, caused by Colletotrichum falcatum Went, is one of the most important diseases of sugarcane (Saccharum officinarum L.). The pathogen shows a great diversity in virulence as a number of pathotypes are known to occur in nature. In the present study, the toxin producing ability and genetic variability among isolates of C. falcatum collected from major sugarcane growing areas of Tamil Nadu, India were analysed. The C. falcatum isolates differed significantly in their ability to produce toxin in vitro. The toxin from C. falcatum isolate Cf 671a induced the maximum electrolyte leakage (300 μS) from sugarcane leaf tissues. The genetic relatedness of the isolates of C. falcatum differing in toxin production potential was investigated by using RAPD analysis. Analysis of the genetic coefficient matrix derived from the scores of RAPD profiles showed that minimum and maximum percent similarities among the tested C. falcatum isolates were in the range of 19 to 95% respectively. The phylogenetic analysis by the UPGMA identified two main clusters. Cluster A contains only one isolate (Cf 98061) and all the other isolates were placed in Cluster B confirming high genetic diversity among the isolates. No correlation was observed between clustering of the C. falcatum isolates in the dendrogram and their toxin producing abilities. 相似文献
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Oressia Zalucki Rebecca Day Benjamin Kottler Shanker Karunanithi Bruno van Swinderen 《Fly》2015,9(1):7-15
General anesthetics achieve behavioral unresponsiveness via a mechanism that is incompletely understood. The study of genetic model systems such as the fruit fly Drosophila melanogaster is crucial to advancing our understanding of how anesthetic drugs render animals unresponsive. Previous studies have shown that wild-type control strains differ significantly in their sensitivity to general anesthetics, which potentially introduces confounding factors for comparing genetic mutations placed on these wild-type backgrounds. Here, we examined a variety of behavioral and electrophysiological endpoints in Drosophila, in both adult and larval animals. We characterized these endpoints in 3 commonly used fly strains: wild-type Canton Special (CS), and 2 commonly used white-eyed strains, isoCJ1 and w1118. We found that CS and isoCJ1 show remarkably similar sensitivity to isoflurane across a variety of behavioral and electrophysiological endpoints. In contrast, w1118 is resistant to isoflurane compared to the other 2 strains at both the adult and larval stages. This resistance is however not reflected at the level of neurotransmitter release at the larval neuromuscular junction (NMJ). This suggests that the w1118 strain harbors another mutation that produces isoflurane resistance, by acting on an arousal pathway that is most likely preserved between larval and adult brains. This mutation probably also affects sleep, as marked differences between isoCJ1 and w1118 have also recently been found for behavioral responsiveness and sleep intensity measures. 相似文献
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Wang X Zhao Q Vargas M Dong Y Sriraghavan K Keiser J Vennerstrom JL 《Bioorganic & medicinal chemistry letters》2011,21(18):5320-5323
Dispiro 1,2,4-trioxanes and 1,2,4,5-tetraoxanes had superior efficacy against Fasciola hepatica than the corresponding ozonides (1,2,4-trioxolanes). For highest efficacy, spiroadamantane and carboxymethyl substructures were required. Three compounds completely cured F. hepatica-infected mice at single oral doses of 50mg/kg and two were partially curative at single doses of 25mg/kg. 相似文献
10.
Jayavel Sridhar Radhakrishnan Sabarinathan Shanmugam Siva Balan Ziauddin Ahamed Rafi Paramasamy Gunasekaran Kanagaraj Sekar 《基因组蛋白质组与生物信息学报(英文版)》2011,(Z2)
In the past few decades, scientists from all over the world have taken a keen interest in novel functional units such as small regulatory RNAs, small open reading frames, pseudogenes, transposons, integrase binding attB/attP sites, repeat elements within the bacterial intergenic regions (IGRs) and in the analysis of those junk regions for ge- nomic complexity. Here we have developed a web server, named Junker, to facilitate the in-depth analysis of IGRs for examining their length distribution, four-quadrant... 相似文献