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| 1 | Discovery of natural berberine-derived nitroimidazoles as potentially multi-targeting agents against drug-resistant Escherichia coli显示文摘A series of natural berberine-derived nitroimidazoles as novel antibacterial agents were designed, synthesized and characterized by nuclear magnetic resonance(NMR), infrared spectra(IR), and high resolution mass spectra(HRMS) spectra. The antimicrobial evaluation showed that some target molecules exhibited moderate to good inhibitory activities against the tested bacteria and fungi including clinical drug-resistant strains isolated from infected patients. Especially, 2-fluorobenzyl derivative8 f not only gave strong activity against drug-resistant E. coli with the minimal inhibitory concentration(MIC) value of0.003 m M, 33-fold more active than norfloxacin, but also exhibited low toxicity toward RAW 264.7 cells and less propensity to trigger resistance. The aqueous solubility and Clog P values of target compounds were investigated to elucidate the structureactivity relationships. Molecular docking and quantum chemical studies for compound 8 f rationally explained its antibacterial effect. The further exploration of antibacterial mechanism revealed that the highly active compound 8 f could effectively permeabilize E. coli cell membrane and intercalate into DNA isolated from resistant E. coli to form 8 f-DNA complex that might block DNA replication to exert the powerful bioactivities. Compound 8 f could also selectively address resistant E. coli from a mixture of various strains. | Guo-Biao Zhang Swetha Kameswari Maddili Vijai Kumar Reddy Tangadanchu Lavanya Gopala Wei-Wei Gao Gui-Xin Cai Cheng-He Zhou | 2018 | Science China Chemistry2018，61，5： | 5 |
| 2 | 喹唑酮咪唑类化合物的设计、合成及其抗菌活性与靶向DNA研究显示文摘多药耐药菌的频繁出现已日益严重威胁人类健康,开发结构新型的抗菌药物已成为全世界战胜耐药菌的重要课题.本文设计合成了一系列具有抗微生物潜力的酰腙桥链的喹唑酮咪唑类新化合物,其结构经核磁共振氢谱(~1H NMR)、核磁共振碳谱(^(13)C NMR)和高分辨质谱(HRMS)进行表征.生物活性研究发现,一些目标化合物具有较好的抗微生物活性,特别是十八烷基衍生物6h和4-氟苄基取代的化合物7i,抗痢疾杆菌和大肠杆菌DH52的活性是氯霉素的2.5~3.3倍,抗黄曲霉菌活性是临床药物氟康唑的28和8.4倍.用紫外-可见光谱法进行了高活性化合物7i靶向DNA的初步研究,发现咪唑衍生物7i可嵌入小牛胸腺DNA形成7i-DNA超分子络合物,从而阻断DNA复制,展现出较好的抗细菌活性.分子模拟研究表明,活性分子7i与DNA碱基通过氢键结合.该类化合物作为新型抗真菌黄曲霉菌专一特效药及新型抗细菌药值得深入研究. | 曹泉诚 王辉 Tangadanchu Vijai Kumar Reddy Gopala Lavanya 蔡桂鑫 周成合 | 2017 | 中国科学:化学2017，47，7： | 5 |
| 3 | Hepatoprotective activity of Hepax-A polyherbal formulation显示文摘Objective:To evaluate the hepatoprotective potential of Hepax,a polyherbal formulation,against three experimentally induced hepatotoxicity models in rats.Methods:Hepatoprotective activity of Hepax was studied against three experimentally induced hepatotoxicity models,namely, carbon tetrachloride(CCl_4),paracetamol and thiocetamide induced hepatotoxicity in rats. Results:Administration of hepatotoxins(CCl_4,paracetamol and thiocetamide) showed significant morphological,biochemical and histological deteriorations in the liver of experimental animals. Pretreatment with Hepax had significant protection against hepatic damage by maintaining the morphological parameters(liver weight and liver weight to organ weight ratio) within normal range and normalizing the elevated levels of biochemical parameters(SGPT,SCOT,ALP and total bilirubin),which were evidently showed in histopathological study.Conclusions:The Hepax has highly significant hepatoprotective effect at 100 and 200 mg/kg,p.o.on the liver of all the three experimental animal models. | VC Devaraj B Gopala Krishna GL Viswanatha Jagadish V Kamath Sanjay Kumar | 2011 | Asian Pacific Journal of Tropical Biomedicine2011，1，2： | 4 |
| 4 | The deubiquitinase OTUB1 augments NF-κB-dependent immune responses in dendritic cells in infection and inflammation by stabilizing UBC13显示文摘Dendritic cells(DCs)are indispensable for defense against pathogens but may also contribute to immunopathology.Activation of DCs upon the sensing of pathogens by Toll-like receptors(TLRs)is largely mediated by pattern recognition receptor/nuclear factor-κB(NF-κB)signaling and depends on the appropriate ubiquitination of the respective signaling molecules.However,the ubiquitinating and deubiquitinating enzymes involved and their interactions are only incompletely understood.Here,we reveal that the deubiquitinase OTU domain,ubiquitin aldehyde binding 1(OTUB1)is upregulated in DCs upon murine Toxoplasma gondii infection and lipopolysaccharide challenge.Stimulation of DCs with the TLR11/12 ligand T.gondii profilin and the TLR4 ligand lipopolysaccharide induced an increase in NF-κB activation in OTUB1-competent cells,resulting in elevated interleukin-6(IL-6),IL-12,and tumor necrosis factor(TNF)production,which was also observed upon the specific stimulation of TLR2,TLR3,TLR7,and TLR9.Mechanistically,OTUB1 promoted NF-κB activity in DCs by K48-linked deubiquitination and stabilization of the E2-conjugating enzyme UBC13,resulting in increased K63-linked ubiquitination of IRAK1(IL-1 receptor-associated kinase 1)and TRAF6(TNF receptor-associated factor 6).Consequently,DC-specific deletion of OTUB1 impaired the production of cytokines,in particular IL-12,by DCs over the first 2 days of T.gondii infection,resulting in the diminished production of protective interferon-γ(IFN-γ)by natural killer cells,impaired control of parasite replication,and,finally,death from chronic T.encephalitis,all of which could be prevented by low-dose IL-12 treatment in the first 3 days of infection.In contrast,impaired OTUB1-deficient DC activation and cytokine production by OTUB1-deficient DCs protected mice from lipopolysaccharide-induced immunopathology.Collectively,these findings identify OTUB1 as a potent novel regulator of DCs during infectious and inflammatory diseases. | Floriana Mulas Xu Wang Shanshan Song Gopala Nishanth Wenjing Yi Anna Brunn Pia-Katharina Larsen Berend Isermann Ulrich Kalinke Antonio Barragan Michael Naumann Martina Deckert Dirk Schlüter | 2021 | Cellular & Molecular Immunology2021，18，6： | 4 |
| 5 | Constitutive renal Rel/nuclear factor-κB expression in Lewis polycystic kidney disease rats显示文摘AIM:To determine the temporal expression and pattern of Rel/nuclear factor(NF)-κB proteins in renal tissue in polycystic kidney disease(PKD). METHODS: The renal expression of Rel/NF-κB proteins was determined by immunohistochemistry, immunofluorescence and immunoblot analysis in Lewis polycystic kidney rats(LPK, a genetic ortholog of human nephronopthsis-9) from postnatal weeks 3 to 20. At each timepoint, renal disease progression and the mR NA expression of NF-κB-dependent genes(TNFa and CCL2) were determined. NF-κB was also histologicaly assessed in human PKD tissue.RESULTS: Progressive kidney enlargement in LPK rats was accompanied by increased renal cell proliferation and interstitial monocyte accumulation(peaking at weeks 3 and 10 respectively), and progressive interstitial fibrosis(with a smooth muscle actin and Sirius Red deposition significantly increased compared to Lewis kidneys from weeks 3 to 6 onwards). Rel/NF-κB proteins(phosphorylated-p105, p65, p50, c-Rel and RelB) were expressed in cystic epithelial cells(CECs) of LPK kidneys as early as postnatal week 3 and sustained until latestage disease at week 20. From weeks 10 to 20, nuclear p65, p50, Rel B and cytoplasmic IκBa protein levels, and TNFa and CCL2 expression, were upregulated in LPK compared to Lewis kidneys. NF-κB proteins were consistently expressed in CECs of human PKD. The DNA damage marker γ-H2AX was also identified in the CECs of LPK and human polycystic kidneys. CONCLUSION: Several NF-κB proteins are consistently expressed in CECs in human and experimental PKD. These data suggest that the upregulation of both the canonical and non-canonical pathways of NF-κB signaling may be a constitutive and early pathological feature of cystic renal diseases. | Michelle HT Ta Kristina G Schwensen David Liuwantara David L Huso Terry Watnick Gopala K Rangan | 2016 | World Journal of Nephrology2016，5，4： | 2 |
| 6 | Treatment of low- strength soluble wastewater using an anaerobic baffled reactor (ABR) 显示文摘 | Gopala Krishna G V T Kumarb P Kumarb P | 2009 | Journal of Environmental Management2009，90，1： | 1 |
| 7 | The Relative Importance Of Teaching, Research and Service In Performance Evaluation Of Marketing Faculty 显示文摘 | Gopala K Ganesh & Niranjan Tripathy | 1996 | Marketing Education Review1996，6，1： | 1 |
| 8 | Micro-mechanical modeling of machining of FRP composites – Cutting force analysis显示文摘 | G. Venu Gopala Rao P. Mahajan N. Bhatnagar | 2006 | Composites Science and Technology2006，，3： | 1 |
| 9 | Sky-hook Control of on Linear Quarter Car Model Traversing Rough Road Matching Performance of LQG Control显示文摘 | Rao L V V Gopala Narayanan S | 2009 | Journal of Sound and Vibration2009，323，： | 1 |
| 10 | Inhibition of nuclear factor-kappa B activation reduces cortical tubulointerstitial injury in proteinuric rats显示文摘 | Gopala K Rangan YW Yuet-Ching T | | 0，，： | 1 |
| 11 | Synergizing rice s-tern borer pheromone with addition of plant extracts and vitamin E in Indian 显示文摘 | Rama Gopala Varma N Krishnaiah K Pasalu L C | 2002 | Plant Prot2002，30，2： | 1 |
| 12 | Rice bran oil:nature's healthful oil显示文摘 | Gopala Krishna A G | 2013 | Inform2013，24，4： | 1 |
| 13 | Corrosion behavior of ultrafine-grained AA2024 aluminum alloy produced by cryorolling显示文摘The objectives of this study were to produce ultrafine-grained(UFG) AA2024 aluminum alloy by cryorolling followed by aging and to evaluate its corrosion behavior. Solutionized samples were cryorolled to ~85% reduction in thickness. Subsequent aging resulted in a UFG structure with finer precipitates of Al_2CuMg in the cryorolled alloy. The(1) solutionized and(2) solutionized and cryorolled samples were uniformly aged at 160°C/24 h and were designated as CGPA and CRPA, respectively; these samples were subsequently subjected to corrosion studies. Potentiodynamic polarization studies in 3.5 wt% NaCl solution indicated an increase in corrosion potential and a decrease in corrosion current density for CRPA compared to CGPA. In the case of CRPA, electrochemical impedance spectroscopic studies indicated the presence of two complex passive oxide layers with a higher charge transfer resistance and lower mass loss during intergranular corrosion tests. The improved corrosion resistance of CRPA was mainly attributed to its UFG structure, uniform distribution of fine precipitates, and absence of coarse grain-boundary precipitation and associated precipitate-free zones as compared with the CGPA alloy. | P. Laxman Mani Kanta V.C. Srivastava K. Venkateswarlu Sharma Paswan B. Mahato Goutam Das K. Sivaprasad K. Gopala Krishna | 2017 | International Journal of Minerals,Metallurgy and Materials2017，24，11： | 1 |
| 14 | Treatment of low-strength soluble wastewater using an anaerobic baffled reactor (ABR) 显示文摘 | Gopala Krishna G V T Kumar P Kumar P | 2009 | Journal of Environmental Management2009，90，1： | 1 |
| 15 | Treatment of low-strength complex wastewater suing an anaerobic baf-fled reactor(ABR)显示文摘 | Gopala Krishna G V T Kumar P Kumar P | 2008 | Bioresour Technol2008，99，17： | 1 |
| 16 | Treatment of low-strength soluble wastewater using an anaerobic baf- fled reactor (ABR)显示文摘 | Gopala Krishna G V T Kumar P Kumar P | 2009 | J Environ Manage2009，90，1： | 1 |
| 17 | Correlated Sources over Wireless Channels:Cooperative Source-Channel Coding 显示文摘 | ARUL D MURUGAN PRAVEEN K GOPALA HESHAM EL GAMAL | 2004 | IEEE Journal on Selected Areas in Communications2004，22，6： | 1 |
| 18 | Volume of fluid methods for immiscible-fluid and free-surface flows显示文摘 | Gopala V R Wachem B G | 2008 | Chemical Engineering Journal2008，141，123： | 1 |
| 19 | Treatment of low strength complex wastewater using an anaerobic baffled reactor (ABR)显示文摘 | G.V.T. Gopala Krishna Pramod Kumar Pradeep Kumar | 2008 | Bioresource Technology2008，，17： | 1 |
| 20 | Com-plex wastewater treatment using an anaerobic baffled reactor显示文摘 | G V T Gopala Krishna Pramod Kumar Pradeep Kumar | 2007 | Environmental Progress2007，26，4： | 1 |
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