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Target-based anticancer indole derivatives and insight into structure-activity relationship:A mechanistic review update(2018—2021)

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Acta Pharmaceutica Sinica B 2022年第7期12卷 3006-3027页

作者： Ashima Dhiman Rupam Sharma rajesh k.singh Department of Pharmaceutical Chemistry Shivalik College of PharmacyIKG Punjab Technical UniversityJalandhar 140126India

Cancer,which is the uncontrolled growth of cells,is the second leading cause of death after heart *** drugs,especially to specific genes and proteins involved in growth and survival of cancer cells,is the prime need of research *** moiety,which is a combination of aromatic-heterocyclic compounds,is a constructive scaffold for the development of novel *** to its bioavailability,high unique chemical properties and significant pharmacological behaviours,indole is considered as the most inquisitive scaffold for anticancer drug *** is illustrated by the fact that the *** and Drug Administration(FDA)has recently approved several indole-based anticancer agents such as panobinostat,alectinib,sunitinib,osimertinib,anlotinib and nintedanib for clinical ***,hundreds of studies on the synthesis and activity of the indole ring have been published in the last three *** into account the facts stated above,we have presented the most recent advances in medicinal chemistry of indole derivatives,encompassing hot articles published between 2018and 2021 in anticancer drug *** recent advances made towards the synthesis of promising indole-based anticancer compounds that may act via various targets such as topoisomerase,tubulin,apoptosis,aromatase,kinases,etc.,have been *** review also summarizes some of the recent efficient green chemical synthesis for indole rings using various catalysts for the period during 2018—*** review also covers the synthesis,structure-activity relationship,and mechanism by which these leads have demonstrated improved and promising anticancer *** molecules under clinical and preclinical stages are classified into groups based on their cancer targets and presented in tabular form,along with their mechanism of *** goal of this review article is to point the way for medicinal chemists to design and develop effective indole-based anticancer agents.

关键词： Indole Synthesis Anticancer Structure-activity relationship Topoisomerase Apoptosis Aromatase inhibitors Tubulin inhibitors

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Precision phenotyping of contrasting potato(Solanum tuberosum L.) varieties in a novel aeroponics system for improving nitrogen use efficiency: In search of key traits and genes

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Journal of Integrative Agriculture 2020年第1期19卷 51-61页

作者： Jagesh k.TIWARI Sapna DEVI Tanuja BUCkSETH Nilofer ALI rajesh k.singh Rasna ZINTA Vijay k.DUA Swarup k.CHAkRABARTI Indian Council of Agricultural Research-Central Potato Research Institute

With increasing population, degrading soil health, limited arable land area, and high cost of nitrogen(N) fertilizers, improving nitrogen use efficiency(NUE) of potato is an inevitable approach to save the environment and achieve sufficient tuber yields with less N fertilizer supply. Recently, we have developed an aeroponics system to study NUE in potato using genomics, physiology, and breeding approaches. This study aims on precision phenotyping of plants of two distinct potato varieties(kufri Gaurav, N efficient;kufri Jyoti, N inefficient) in the novel aeroponics system. Plants were grown in aeroponics under controlled conditions with low N(0.75 mmol L^-1NO3^-) and high N(7.5 mmol L^-1NO3^-) levels. Plant biomass, root traits, total chlorophyll content, and plant N were increased with increasing N supply, whereas higher NUE parameters namely NUE, agronomic NUE(Ag NUE), N uptake efficiency(NUp E), harvest index(HI), and N harvest index(NHI) were observed at low N. An NUE efficient cv. kufri Gaurav showed higher tuber dry weight, fresh tuber yield, tuber number per plant, early start of tuber harvesting, root traits, stolon traits, NUE parameters, and higher amino acid(aspartic acid and asparagine) content at low N supply. Higher expression of nitrate reductase(NR), nitrite reductase(NIR), and asparagine synthetase(AS) genes was observed in the leaf tissues of kufri Gaurav at high N. Thus, aeroponics-based precision phenotyping enables identification of NUE efficient genotypes based on key traits and genes involved in improving NUE in potato. Further, this study suggests that the potential of aeroponics can be utilized to investigate N biology in potato under different N regimes.

关键词： aeroponics precision phenotyping potato nitrogen use efficiency

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R2R3-MYB transcription factors, StmiR858 and sucrose mediate potato flavonol biosynthesis

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Horticulture Research 2021年第1期8卷 378-390页

作者： Sen Lin rajesh k.singh Moehninsi Duroy A.Navarre Irrigated Agriculture Research and Extension Center Washington State UniversityProsserWAUSA USDA-Agricultural Research Service ProsserWAUSA Present address:Department of Biotechnology CSIR-Institute of Himalayan Bioresource TechnologyPalampurHimachal Pradesh 176061India

Flavonols and other phenylpropanoids protect plants from biotic and abiotic stress and are dietarily desirable because of their health-promoting *** ability to develop new potatoes(Solanum tuberosum)with optimal types and amounts of phenylpropanoids is limited by lack of knowledge about the regulatory *** sucrose increased flavonols,whereas overexpression of the MYB StAN1 induced sucrolytic gene *** StAN1 protein bound promoter fragments from sucrolytic genes(SUSY1 and INV1).Two additional MYBs and one microRNA were identified that regulated potato *** analysis showed MYB12A and C increased amounts of flavonols and other *** flavonol amounts in light-exposed organs were much higher those in the *** levels of StMYB12A and C were high in flowers but low in *** overexpression of miR858 altered potato flavonol *** StmiR858 expression was much lower in flowers than leaves and correlated with flavonol amounts in these ***,these findings support the hypothesis that sucrose,MYBs,and miRNA control potato phenylpropanoid metabolism in a finely tuned manner that includes a feedback loop between sucrose and *** findings will aid in the development of potatoes with phenylpropanoid profiles optimized for crop performance and human health.

关键词： properties. finding media

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Dual PPAR delta/gamma agonist offer therapeutic potential for Alzheimer's disease

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Neural Regeneration Research 2024年第6期19卷 1175-1176页

作者： Ian Steinke Meenakshi singh rajesh Amin Department of Drug Discovery and Development Auburn UniversityAuburn AlabamaALUSA

The increasing incidence of Alzheimer's disease(AD)in the aging population,indicates the critical need for the development of novel targeted molecular therapies for ameliorating AD ***,clinical and preclinical evidence demonstrates that peroxisomal proliferator activating receptors(PPAR)agonists regulate energy and lipid homeostasis in models of diabetes,as well as improve spatial memory in animal models of AD(khan et al.,2019).

关键词： Alzheimer clinical homeostasis

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Multimodality Medical Image Fusion Based on Pixel Significance with Edge-Preserving Processing for Clinical Applications

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Computers, Materials & Continua 2024年第3期78卷 4317-4342页

作者： Bhawna Goyal Ayush Dogra Dawa Chyophel Lepcha rajesh singh Hemant Sharma Ahmed Alkhayyat Manob Jyoti Saikia Department of ECE and UCRD Chandigarh UniversityMohaliPunjab140413India Chitkara University Institute of Engineering and Technology Chitkara UniversityPunjab140401India Department of ECE Uttaranchal Institute of TechnologyUttaranchal UniversityDehradun248007India IES College of Technology IES UniversityBhopal462044India College of Technical Engineering The Islamic UniversityNajaf54001Iraq Department of Electrical Engineering University of North FloridaJacksonvilleFL32224USA

Multimodal medical image fusion has attained immense popularity in recent years due to its robust technology for clinical *** fuses multiple images into a single image to improve the quality of images by retaining significant information and aiding diagnostic practitioners in diagnosing and treating many ***,recent image fusion techniques have encountered several challenges,including fusion artifacts,algorithm complexity,and high computing *** solve these problems,this study presents a novel medical image fusion strategy by combining the benefits of pixel significance with edge-preserving processing to achieve the best fusion ***,the method employs a cross-bilateral filter(CBF)that utilizes one image to determine the kernel and the other for filtering,and vice versa,by considering both geometric closeness and the gray-level similarities of neighboring pixels of the images without smoothing *** outputs of CBF are then subtracted from the original images to obtain detailed *** further proposes to use edge-preserving processing that combines linear lowpass filtering with a non-linear technique that enables the selection of relevant regions in detailed images while maintaining structural *** regions are selected using morphologically processed linear filter residuals to identify the significant regions with high-amplitude edges and adequate *** outputs of low-pass filtering are fused with meaningfully restored regions to reconstruct the original shape of the *** addition,weight computations are performed using these reconstructed images,and these weights are then fused with the original input images to produce a final fusion result by estimating the strength of horizontal and vertical *** standard quality evaluation metrics with complementary properties are used for comparison with existing,well-known algorithms objectively to validate the fusion *** results from th

关键词： Image fusion fractal data analysis biomedical diseases research multiresolution analysis numerical analysis

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Robust Facial Biometric Authentication System Using Pupillary Light Reflex for Liveness Detection of Facial Images

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Computer Modeling in Engineering & Sciences 2024年第4期139卷 725-739页

作者： Puja S.Prasad Adepu Sree Lakshmi Sandeep kautish Simar Preet singh rajesh kumar Shrivastava Abdulaziz S.Almazyad Hossam M.Zawbaa Ali Wagdy Mohamed CSE Department Geethanjali College of EngineeringHyderabadTelangana501301India Department of Computer Science LBEF CampusKathmandu44600Nepal School of Computer Science Engineering and Technology(SCSET) Bennett UniversityGreater Noida201310India Department of Computer Engineering College of Computer and Information SciencesKing Saud UniversityP.O.Box 51178Riyadh11543Saudi Arabia CeADAR Ireland’s Centre for AI Technological University DublinDublinD07 EWV4Ireland Operations Research Department Faculty of Graduate Studies for Statistical ResearchCairo UniversityGiza12613Egypt Applied Science Research Center Applied Science Private UniversityAmman11937Jordan

Pupil dynamics are the important characteristics of face spoofing *** face recognition system is one of the most used biometrics for authenticating individual *** main threats to the facial recognition system are different types of presentation attacks like print attacks,3D mask attacks,replay attacks,*** proposed model uses pupil characteristics for liveness detection during the authentication *** pupillary light reflex is an involuntary reaction controlling the pupil’s diameter at different light *** proposed framework consists of two-phase *** the first phase,the pupil’s diameter is calculated by applying stimulus(light)in one eye of the subject and calculating the constriction of the pupil size on both eyes in different video *** above measurement is converted into feature space using kohn and Clynes model-defined *** Support Vector Machine is used to classify legitimate subjects when the diameter change is normal(or when the eye is alive)or illegitimate subjects when there is no change or abnormal oscillations of pupil behavior due to the presence of printed photograph,video,or 3D mask of the subject in front of the *** the second phase,we perform the facial recognition ***-invariant feature transform(SIFT)is used to find the features from the facial images,with each feature having a size of a 128-dimensional *** features are scale,rotation,and orientation invariant and are used for recognizing facial *** brute force matching algorithm is used for matching features of two different *** threshold value we considered is 0.08 for good *** analyze the performance of the framework,we tested our model in two Face antispoofing datasets named Replay attack datasets and CASIA-SURF datasets,which were used because they contain the videos of the subjects in each sample having three modalities(RGB,IR,Depth).The CASIA-SURF datasets showed an 89.9%Equal Err

关键词： SIFT pupil CASIA-SURF pupillary light reflex replay attack dataset brute force

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Designing of tragacanth gum-poly [2-(methacryloyloxy) ethyl] dimethyl-(3-sulfopropyl) ammonium hydroxide and poly(acrylamide) based hydrogels for drug delivery and wound dressing applications

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Medicine in Novel Technology and Devices 2024年第2期22卷 90-101页

作者： kavita Devi Ashima Sharma rajesh kumar Baljit singh Department of Chemistry Himachal Pradesh UniversityShimla171005India Department of Physiology Indira Gandhi Medical CollegeShimlaIndia

Bioactive tragacanth gum(TG)was functionalized by covalent crosslinking of poly[2-(methacryloyloxy)ethyl]dimethyl-(3-sulfopropyl)ammonium hydroxide(PMEDSAH)to design network structure in form of hydrogel wound dressings(HWD).These copolymers were encapsulated with antibiotic drug vancomycin to enhance wound healing potential of the *** copolymers were characterized by SEM,AFM,FTIR,13C NMR,XRD,and TGA-DSC *** demonstrated uneven heterogeneous morphology and AFM revealed rough surface of *** of synthetic component into HD was confirmed by FTIR and 13C *** dressings absorbed 8.491.03 g/g simulated wound fluid and exhibited non-hemolytic(3.70.02%hemolytic potential)and antioxidant(37.421.54%free radical scavenging in DPPH assay)*** required 35.05.0 mN detachment force to get it detach from the mucosal surface during mucoadhesive *** strength was found to be 1.880.13 N/mm2 during mechanical stability *** dressings were permeable to O2/H2O and impermeable to *** of drug vancomycin occurred through non-Fickian diffusion mechanism and release profile was best described by korsmeyer-Peppas kinetic ***,these results revealed that these hydrogels could be explored as materials for hydrogel wound dressings.

关键词： Hydrogel dressings Drug delivery Wound dressings Vancomycin

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Bioremediation of Textile Azo Dyes Amido Black 10B, Reactive Black 5, Reactive Blue 160 by Lentinus squarrosulus AF5 and Assessment of Toxicity of the Degraded Metabolites

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Advances in Microbiology 2024年第2期14卷 137-161页

作者： Anshu Mathur Chandrachur Ghosh Partha Roy Ramasare Prasad rajesh Pratap singh Department of Biosciences and Bioengineering Indian Institute of Technology Roorkee Roorkee India

Bioremediation is an eco-compatible and economical approach to counter textile dye menace. The isolated Lentinus squarrosulus AF5 was assessed for decolourization of textile azo dyes, and had shown ~93%, 88% and 70% decolorization of Reactive blue 160 (RB160), Reactive black 5 (RB5) and Amido black 10B (AB10B) respectively. Further analysis using UV-vis, HPLC, and FTIR, 1H NMR had shown the degradation of the dyes. Toxicity analysis of the metabolites was performed using seed germination and plant growth on two agriculturally important plants Guar (Cyamopsis tetragonoloba) and wheat (Triticum aestivum) as well as cytotoxicity analysis using the human keratinocyte cell line (HaCaT). The dye mix appeared inhibitory for seed germination (20% - 40%), whereas metabolites were non-inhibitory for germination. Treatment of HaCaT cells with of dye mix and metabolites led into 45% and ~100% of cell viability of HaCaT cells respectively. Therefore, metabolites following degradation of the dye mix were observed to be non-toxic.

关键词： Lentinus squarrosulus AF5 Azo Dyes FTIR 1H NMR Catabolism Cytotoxicity

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Effects of supplemental xylanase and xylooligosaccharides on production performance and gut health variables of broiler chickens

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Journal of Animal Science and Biotechnology 2022年第1期13卷 166-180页

作者： Amit k.singh Birendra Mishra Michael R.Bedford rajesh Jha Department of Human Nutrition Food and Animal SciencesUniversity of Hawaii at ManoaHonoluluHI 96822USA AB Vista Feed Ingredients MarlboroughWiltshireUK

Background:This study evaluated the effects of supplemental xylanase and xylooligosaccharides(XOS)in a cornsoybean meal(SBM)-based diet on growth performance and intestinal health of broilers.A total of 288 day-old chicks(Cobb 500)were allocated to 36 floor pens(8 birds/pen)equally in 9 dietary treatments in a 3×3 factorial *** treatments were combinations of 3 levels of xylanase(0,0.005% and 0.01% Econase XT)and 3 levels of prebiotics(0,0.005% and 0.01% XOS)added to basal mash diets formulated in three phases(starter,d 0-14;grower,d 15-28;finisher,d 29-42).The feed intake and body weights were recorded *** d 42,ileal sections were collected for histomorphometric and gene expression analysis,and cecal content was collected for determining short-chain fatty acids(SCFA)and ***:Xylanase linearly(P0.05).Supplemental xylanase and XOS did not affect average daily feed intake and feed conversion ratio(P>0.05).Xylanase and XOS did not change villus height(VH)or crypt depth(CD)ratio(P>0.05).However,xylanase exhibited a trend(P=0.097)on VH:CD *** inclusion of 0.01%XOS without xylanase increased the level of IL-10(a marker of anti-inflammatory cytokine)and IL-4(a T-cell differentiation cytokine)genes compared with control(P0.05).However,the mean proportion of family Ruminococcaceae was increased by the supplemental 0.01% xylanase(P<0.01).Conclusion:It can be concluded that XOS can enhance cecal fermentation,while xylanase can increase the body weight gain along with the ferment

关键词： Gene expression Histomorphology Microbiota Poultry Prebiotics Short-chain fatty acid Xylooligosaccharide

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A New Stable Algorithm to Compute Hankel Transform Using Chebyshev Wavelets

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Communications in Computational Physics 2010年第7期8卷 351-373页

作者： rajesh k.Pandey Vineet k.singh Om P.singh PDPM Indian Institute of Information Technology Design and Manufacturing JabalpurIndia Birla Institute of Technology and Science-Pilani Goa CampusGoaIndia Department of Applied Mathematics Institute of TechnologyBanaras Hindu UniversityVaranasiIndia

A new stable numerical method,based on Chebyshev wavelets for numerical evaluation of Hankel transform,is proposed in this *** Chebyshev wavelets are used as a basis to expand a part of the integrand,r f(r),appearing in the Hankel transform *** transforms the Hankel transform integral into a Fourier-Bessel *** truncating the series,an efficient and stable algorithm is obtained for the numerical evaluations of the Hankel transforms of order ν>−*** method is quite accurate and stable,as illustrated by given numerical examples with varying degree of random noise terms εθ_(i) added to the data function f(r),where θ_(i) is a uniform random variable with values in[−1,1].Finally,an application of the proposed method is given for solving the heat equation in an infinite cylinder with a radiation condition.

关键词： Hankel transforms Bessel functions Chebyshev wavelets random noise term

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