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Antimalarial activity of a novel series of artemisinin-derived 1, 2, 3-triazole dimers

Asian Pacific Journal of Tropical Medicine 2019年第5期12卷 195-203页

作者： Kabita Gogoi gokul baishya Biswajit Saikia Nabin Chandra Barua Chandrajit Dohutia Akalesh Kumar Verma Anil Prakash ICMR-Regional Medical Research Centre,N.E. CSIR-North-East Institute of Science and Technology Digboi College,Chemistry Department Pratiksha Institute of Pharmaceutical Scinces Cotton University,Zoology Department ICMR-National Institute for Research in Environmental Health ICMR-Regional Medical Research Centre N.E. CSIR-North-East Institute of Science and Technology Digboi College Chemistry Department Pratiksha Institute of Pharmaceutical Scinces Cotton University Zoology Department ICMR-National Institute for Research in Environmental Health

Objective: To obtain suitable artimisinin-based drug candidates with high antimalarial ***: Three different reaction schemes were used to synthesize a total of 15 artemisininbased *** first synthetic scheme involved the synthesis of diazido aliphatic and aromatic compounds from commercially available dihalides and azido derivatives of *** second scheme consisted of the reaction of dibromoaliphatic compounds with sodium azide in dimethylformamide which yielded the desired ***-based compounds on treatment with sodium azide and bromotrimethylsilane in dichloromethane produced the most potent compound *** potent compound GB-1 was synthesized from artemisinin by treatment with alcohols in the presence of Aberlyst-15 in anhydrous *** third scheme involved the Huisgen 1,3-dipolar cycloaddition between the synthesized aliphatic and aromatic diazides and two alkyne derivatives of artemisinin to obtain the desired artemisinin dimers with average ***: The best in vitro antiplasmodial activity was shown by the compound GB-2 registering IC_(50) value 0.066 μg/mL against chloroquine-sensitive and 0.865 μg/mL against chloroquineresistant strains of Plasmodium *** suppressed 59.0% parasitaemia in vivo of rodent malaria parasite Plasmodium berghei in Swiss albino model at 50 μg/kg body weight *** docking interactions of Plasmodium falciparum ATP6(PfATP6) protein revealed strong bonding of GB-2 with Thr255 residue which is likely to be the reason for excellent antimalarial activity of this ***: Two compounds GB-1 and GB-2 exhibited excellent in vitro antiplasmodial activity and fair in vivo antimalarial *** the two, GB-2 showed better activity which could be attributed to its strong bonding interactions with Thr255 as evidenced from the molecular docking *** helped in identifying artemisinin analogues possessing good antimalarial properties a

关键词： Antimalarial activity Artemisinin derivatives Huisgen reaction Triazole dimers Plasmodium berghei Plasmodium falciparum Molecular docking

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Analytical approach for the design of convoluted air suspension and experimental validation

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Acta Mechanica Sinica 2019年第5期35卷 1093-1103页

作者： gokul Prassad Sreenivasan Malar Mohan Keppanan Department of Mechanical Engineering College of EngineeringGuindyAnna UniversityChennai 600025India

An improved analytical design to investigate the static stiffness of a convoluted air spring is developed and presented in this *** air spring provides improved ride comfort by achieving variable volume at various strokes of the *** analytical relation is derived to calculate the volume and the rate of change in the volume of the convoluted bellow with respect to various suspension *** expression is used in the equation to calculate the variable stiffness of the *** obtained analytical characteristics are validated with a detailed experiment to test the static vertical stiffness of the air *** convoluted air bellow is tested in an Avery spring-testing apparatus for various *** bellow is modeled in the ABAQUS environment to perform finite element analysis(FEA)to understand and visualize the deflection of the bellow at various elevated internal pressures and external *** proposed air spring model is a fiber-reinforced rubber bellow enclosed between two metal *** Mooney-Rivlin material model was used to model the hyperelastic rubber material for *** the results,it is observed that the experimental and analytical results match with a minor error of 7.54%.The derived relations and validations would provide design guidance at the developmental stage of air *** expressions would also play a major role in designing an effective active air suspension system by accurately calculating the required stiffness at various loads.

关键词： Air spring Numerical modeling Convoluted bellows Fiber-reinforced bellow

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Structural, Thermal, Linear and Nonlinear Optical Studies on New NLO Crystal∶DL-Threonium Trichloroacetate

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Journal of Rare Earths 2006年第Z1期24卷 249-252页

作者： Gubendiran Ramesh Kumar Srinivasan gokul Raj Rajagopal Mohan Ramasamy Jayave Department of Physics Presidency college Chennai-600 005 India Department of Physics Presidency college Chennai-600 005 India Department of Physics Presidency college Chennai-600 005 India Department of Physics Presidency college Chennai-600 005 India Crystal Growth Centre Anna University Chennai-600 025 India

Crystals of DL-threonium trichloroacetate (DLTTCA) was synthesized from an aqueous solution by slow evaporation technique. The grown crystals were characterized by X-ray diffraction, Fourier transform infrared spectroscopy, UV-Vis-NIR and SHG measurements. Vibrational structure of the crystal was elucidated from FTIR analysis and the hydrogen bond interactions were discussed in detail. The ultraviolet transparent cutoff falls at 212 nm. Thermal stability of the compound was also studied. The powder SHG efficiency of the compound was measured as 0.62 times to that of KDP.

关键词： growth from solution nonlinear optical materials

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Influence of Annealing on Physical Properties of CdO Thin Films Prepared by SILAR Method

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Journal of Materials Science & Technology 2013年第1期29卷 17-21页

作者： B.gokul P.Matheswaran R.Sathyamoorthy PG and Research Department of Physics Kongunadu Arts and Science College (Autonomous)

Cadmium oxide （CdO） thin films were prepared by successive ionic layer adsorption and reaction （SILAR） method and annealed at 250-450 ℃ for 2 h. The prepared films were characterized by X-ray diffraction （XRD）, optical spectroscopy, scanning electron microscopy （SEM） and Hall effect measurement. The XRD analysis reveals that the films were polycrystalline with cubic structure. Both crystallinity and the grain size were found to increase with increasing annealing temperature. SEM analysis shows the porous nature of the surface with spherical nanoclusters. Energy dispersive spectroscopic analysis （EDS） confirmed the presence of Cd and O elements without any additional impurities. The films exhibited maximum transmittance （82%-86%） in infra-red （IR） region. Transmittance was found to decrease with increasing annealing temperature （Eg） was in the range of 2.24-2.44 eV. Hall effect measurement shows an and the estimated band gap energy ncrease in carrier concentration and a decrease in resistivity with increasing annealing temperature. The carrier concentration （N） and resistivity （p） of about 1.26 × 1022 cm-3 and 8.71 × 10 3 Ω cm are achieved for the film annealed at 450 ℃ for 2 h.

关键词： Annealing Porous structure Hall effect Electrical resistivity

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Female sex in experimental traumatic brain injury research:forging a path forward

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Neural Regeneration Research 2022年第3期17卷 550-552页

作者： Theresa Currier Thomas Caitlin E.Bromberg gokul Krishna Department of Child Health University of Arizona College of Medicine-Phoenix BARROW Neurological Institute at Phoenix Children’s Hospital PhoenixAZUSA Phoenix VA Health Care System PhoenixAZUSA Arizona State University TempeAZUSA

Traumatic brain injury(TBI) is a leading cause of death and disability worldwide,with estimates indicating that -50% of the world's population will acquire a head injury at some point in their lifetime(Maas et al.,2017).Mild TBIs account for -80% of all reported cases,with up to 43% of all TBI patients reporting symptoms beyond 2 weeks *** of 2016,only 7% of preclinical TBI experiments included both male and female sexes,and fewer studies analyzed the data using sex as a biological variable(Spani et al.,2018).

关键词： injury death

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Enhanced Security with Improved Defensive Routing Mechanism in Wireless Sensor Networks

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Computer Systems Science & Engineering 2023年第6期45卷 2795-2810页

作者： R.Sabitha C.gokul Prasad S.Karthik Department of Computer Science&Engineering SNS College of TechnologyCoimbatoreTamilnaduIndia Department of Electronics and Communication Engineering SNS College of EngineeringCoimbatoreTamilnaduIndia

In recent scenario of Wireless Sensor Networks(WSNs),there are many application developed for handling sensitive and private data such as military information,surveillance data,tracking,***,the sensor nodes of WSNs are distributed in an intimidating region,which is non-rigid to *** recent research domains of WSN deal with models to handle the WSN communications against malicious attacks and *** traditional models,the solution has been made for defending the networks,only to specific ***,in real-time applications,the kind of attack that is launched by the adversary is not ***,on developing a security mechanism for WSN,the resource constraints of sensor nodes are also to be *** that note,this paper presents an Enhanced Security Model with Improved Defensive Routing Mechanism(IDRM)for defending the sensor network from various ***,for efficient model design,the work includes the part of feature evaluation of some general attacks of *** IDRM also includes determination of optimal secure paths and Node security for secure routing *** performance of the proposed model is evaluated with respect to several factors;it is found that the model has achieved better security levels and is efficient than other existing models in WSN *** is proven that the proposed IDRM produces 74%of PDR in average and a minimized packet drop of 38%when comparing with the existing works.

关键词： Enhanced security model wireless sensor networks improved defensive routing mechanism secure paths node security

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Hepatoprotective activity of Macrothelypteris torresiana (Gaudich.) aerial parts against CCl4-induced hepatotoxicity in rodents and analysis of polyphenolic compounds by HPTLC

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Journal of Pharmaceutical Analysis 2017年第3期7卷 181-189页

作者： Sumanta Mondal Debjit Ghosh Seru Ganapaty Surya Vamsi gokul Chekuboyina Manisha Samal GITAM Institute of Pharmacy GITAM University Visakhapatnam-530045 Andhra Pradesh India Department of Chemistry GITAM Institute of ScienceGITAM UniversityVisakhapatnam-530045Andhra PradeshIndia

Macrothelypteris torresiana is a fern species belonging to the family Thelypteridaceae. The present study was conducted to evaluate hepatoprotective potential of ethanol extract from M. torresiana aerial parts(EEMTAP)and detect the polyphenolic compounds present in the extract using high performance thin layer chromatography(HPTLC). Hepatoprotective potential of EEMTAP were tested at doses of 300 and 600 mg/kg, per os(p.o.), on Wistar albino rats. The extract and silymarin treated animal groups showed significant decrease in activities of different biochemical parameters like serum glutamic oxaloacetic transaminase(SGOT), serum glutamate-pyruvate transaminase(SGPT), and alkaline phosphatase(ALP), which were elevated by carbon tetrachloride(CCl_4) intoxication. The levels of total bilirubin and total protein along with the liver weight were also restored to normalcy by EEMTAP and silymarin treatment. After CCl_4 administration, the levels of hepatic antioxidant enzymes such as glutathione(GSH) and catalase(CAT) were decreased whereas the level of hepatic lipid peroxidation(LPO) was elevated. The levels of these hepatic antioxidant enzymes were also brought to normalcy by EEMTAP and silymarin treatment. Histological studies supported the biochemical findings, and treatment with EEMTAP at doses of 300 and 600 mg/kg, p.o. was found to be effective in restoring CCl_4-induced hepatotoxicity in rats. A simple HPTLC analysis was conducted for the detection of polyphenolic compounds in EEMTAP, and the result revealed the presence of caffeic acid as phenolic acid and quercetin as flavonoid. The proposed HPTLC method is simple and concise and provides a good resolution of caffeic acid and quercetin from other constituents present in EEMTAP.

关键词： Macrothelypteris torresiana Hepatoprotective activity HPTLC fingerprint Caffeic acid Quercetin

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Next generation sequencing in oral disease diagnostics

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World Journal of Stomatology 2018年第2期6卷 6-10页

作者： gokul Sapna Sridharan gokul Department of periodontics Nair Hospital Dental College Oral Pathology and Microbiology YMT Dental College and Hospital

DNA sequencing is the method of identifying the precise order of DNA nucleotides within a molecule. The information of DNA sequencing is of prime requisite for basic biological research as well as in various clinical *** can be used to determine the individual genetic sequence, larger genetic regions, chromosomes as well as to sequence RNA and proteins. Since the first DNA sequencing in 1970s, there has been tremendous advancements in the technologies aimed to determine the entire human genome. The need for rapid and accurate sequencing of human genome has resulted in the introduction of next generation sequencing(NGS) technology. NGS refers to the secondgeneration DNA sequencing technologies where millions of DNA can be sequenced simultaneously. Some of the next gen sequencing methods employed are Roche/454 life science, Illumina/Solexa, SOLiD system and *** of NGS in decoding the genomic database of various oral diseases may possess therapeutic and prognostic value. This presentation provides an overview of the basics of NGS and their potential applications in oral disease diagnostics.

关键词： Molecular diagnostics Next generation sequencing Illumina Oral diseases Oral cancer

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Mathematical model of thermal effects of blinking in human eye

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International Journal of Biomathematics 2016年第1期9卷 111-134页

作者： D. B. Gurung K. C. gokul P. R. Adhikary Department of Natural Sciences (Mathematics) School of Science Kathmandu University Post Box 6250 Kathmandu Nepal

Blinking is regarded as the continuous interrupted eyelid closure or opening and its thermal effect will compromise between these two. During a blink, the heat loss via convection, radiation and tear evaporation from cornea is prevented, warm tear is lay- ered across corneal surface and the vessels of the palpebral conjunctiva provide heat to anterior eye. In most of the thermal models in human eye that are found in literatures, effect of blinking is not included, simulation is carried out only in open eye. Thus, in this paper, thermal effects of blinking are investigated using one-dimensional finite element method in transient state case. The bio-heat transfer process is simulated during different blinking rates, lid closure and opening. The simulation is carried out using normal and extreme values of ambient temperatures, blood temperatures, evaporation rates, blood perfusion rates, and lens thermal conduetivities. Blinking is found to increase corneal and lens temperature by 1.29℃ and 0.78℃ respectively when compared to open eye. The results obtained from this model are useful in predicting temperature distribution in different laser eye surgeries, hyperthermia and cryosurgery treatment of eyelid carci- noma, choroidal melanoma and can be used for diagnosing temperature-related diseases.

关键词： Bio-heat transfer eyelid blinking finite element method.

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Crustal Deformation Revealed by GPS in Kumaun Himalaya,India

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Journal of Mountain Science 2014年第1期11卷 41-50页

作者： Rakesh K.DUMKA Bahadur S.KOTLIA Kireet KUMAR gokul S.SATYAL Lalit M.JOSHI Institute of Seismological Research Centre of Advanced Study in Geology Kumaun University G.B.Pant Institute of Himalayan Environment and Development

The foremost Global Positioning System(GPS) derived measurements in the Kumaun Himalaya indicate that most of the crustal motion of the Indian plate is accommodating towards the base as well as on the hanging wall of Main Central Thrust(MCT).Deformation pattern within the Kumaun Himalaya varies from south to north and indicates maximum deformation rate near *** study,based on the campaign mode GPS survey during 2003- 2006,reveals that the area between north of North Almora Thrust(NAT) and at the base of Great Himalaya registers maximum strain rate,which is lowered towards the Trans Himadri Fault(THF).The GAMIT-GLOBK processed campaign data of the area show that currently,the Himalayan Frontal Fault(HFF) and Main Boundary Thrust(MBT) are locked with the Indian plate,and a 6.7 ± 2.5 mm/yr of horizontal shortening is taking place between the Lesser Himalaya and Peninsular India.

关键词： Kumaun Himalaya Faults thrust systems Deformation Convergence Crustal strain

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